Bactericidal

J Clin Periodontol, 1991 Jul, 18(6), 468 - 73
Antibacterial dentifrices . Clinical data and relevance with emphasis on zinc/triclosan; Gjermo P et al.; The present review concerns the effect on plaque and gingivitis of some antibacterial dentifrices . The difficulties of including cationic agents in conventional dentifrice formulations are briefly discussed . The focus is on 2 recently introduced dentifrices with triclosan as the active ingredient . One aims at providing a slow release reservoir of triclosan in the oral cavity by delivering the substance dissolved in a lipophilic copolymer . 3-month results indicate a modestly improved effect on plaque and gingivitis compared to that of triclosan alone . Long-term studies are needed before conclusions on the clinical relevance can be drawn . The other dentifrice on the market utilises the principle of additive effects by combining triclosan and zinc citrate in the formulation . The combination appears to be more effective against plaque and gingivitis than either compound alone . Studies of up to 1 year duration indicate that the level of oral hygiene and gingival health obtained through an initial period of motivation and oral hygiene instruction can be maintained by regular use of the test dentifrice, while most subjects in the control group returned to pre-experimental levels . Microbiological monitoring indicates no major shifts in plaque ecology nor any development of resistant bacteria, and adverse side-effects have not been observed . It is concluded that the new approaches to chemical plaque control may be beneficial to the population at large, and thus of great clinical relevance.

Jpn J Antibiot, 1991 Jul, 44(7), 732 - 5
{Enhancement of susceptibility of sulbactam/cefoperazone-treated bacteria to phagocytes}; Tanaka T et al.; Effects of sulbactam/cefoperazone (SBT/CPZ) on the host-parasite relationship were studied using an established mouse macrophage cell line . Since SBT inactivates some types of beta-lactamase strongly, a combination of SBT with CPZ shows marked antibacterial activities against the bacteria producing beta-lactamases . In addition, sub-MIC levels of SBT/CPZ made Escherichia coli more susceptible to bactericidal activity of macrophage . This study provides evidence that SBT/CPZ works in partnership with host defense mechanism against bacterial infections in clinical situations.

Bioconjug Chem, 1991 Jul-Aug, 2(4), 281 - 91
Iron transport mediated drug delivery systems: synthesis and antibacterial activity of spermidine- and lysine-based siderophore-beta-lactam conjugates; McKee JA et al.; Conceptually, the penetration of beta-lactam antibiotics through the bacterial cell wall can be enhanced by utilizing various active transport systems such as the active iron-transport system that exists in bacteria . Several beta-lactam-siderophore analogue (microbial iron chelators) conjugates were prepared to investigate this approach . Thus, monocyclic (oxamazin) and bicyclic (carbacephalosporin) beta-lactams were separately linked to dihydroxybenzoyl derivatives of spermidine and lysine . The antibacterial activity of these conjugates has been investigated and the potential use of the iron-transport system as a drug-delivery system is discussed.

Khirurgiia (Mosk), 1991 Jul, (7), 11 - 4
{Treatment of moist gangrene of the foot in patients with diabetes mellitus}; Prokhorov AV et al.; The authors generalized their experience in the treatment of 159 patients aged 21 to 84 with diabetes mellitus and pyonecrotic lesions of the lower limbs . On the basis of the results of rheovasography, aortoarteriography, and roentgenography of the foot bones they concluded that to prognosticate the possibility of preserving the supporting function of the limb, not only the level and extent of the gangrene but also the state of the main and the collateral blood flow in the limb and the spread of bone destruction in the foot must be taken into account . Pathogenetic nonoperative treatment including antibacterial therapy, transfusion of hemo- and rheomodulators, and the use of hemosorption made it possible to convert moist to dry gangrene in 86.8% of patients, expand the indications for "minor" amputations, and reduce the number of high amputations from 56.2 to 35.8% and the total mortality from 10.2 to 4.4%.

Boll Soc Ital Biol Sper, 1991 Jul, 67(7), 673 - 80
{Differentiation activity of pyridoxal thiosemicarbazone and its copper and cobalt complexes on Friend erythroleukemia cells}; Albertini R et al.; Thiosemicarbazones are a wide group of organic derivatives whose biological activities are a function of the parent aldehyde or ketone and of the coordination metal type . Some thiosemicarbazones possess a broad spectrum of potentially useful chemotherapeutic properties (antitumor, antibacterial, antiviral, antimalarial) . The present study reports the biological effects of pyridoxal thiosemicarbazone, H2L, and relative complexes with copper, {(Cu(HL)(OH2))2}++ and with cobalt, {Co(III)(L)(HL)} on the differentiation of Friend erythroleukemia cells (FLC) . They are murine proerythroblasts chronically infected by a producing Friend leukemia virus complex; their exposure to dimethylsulfoxide (Me2SO) or other chemical agents induces these cells to terminal erythroid differentiation, therefore these cells represent a good model of differentiation in vitro . Here we describe induction differentiation experiment of pyridoxal thiosemicarbazone and relative complexes of copper and cobalt on FLC performed with concentrations of 50 ug/ml (ligand), 2 ug/ml (complexes) . These have little effects on cell proliferation at doses used in these experiments . Higher doses have evident cytotoxic effects . The treatment with the copper complex induces a moderate differentiation of FLC and enhances effects on erythroid differentiation of Me2SO-induced FLC . On the contrary H2L and {Co(III)(L)(HL)} haven't inducing effects or enhancing effects on Me2SO-induced FLC hemopoietic differentiation . In conclusion, the present study shows that copper complexes of pyridoxal thiosemicarbazone exert action of inducing agent and are able to enhance Me2SO-induced FLC hemopoietic differentiation.

Rev Invest Clin, 1991 Jul-Sep, 43(3), 205 - 10
{Cicatricial, antibacterial and antimycotic effects of tepescohuite in experimental animals}; Palacios C et al.; The cicatricial and antibacterial effects of the sterile powder of the barks of tepescohuite (Mimosa tenuiflora), 2% mupirocin ointment, and 0.9% saline were compared . The experiment was performed in rabbits with chemically induced burns clinically, histopathologically, bacteriologically, and mycologically controlled . No statistically significant difference was found among the three treatment modalities . Due to the potentially hepatotoxic effects and low therapeutic efficacy of tepescohuite it should not be used in human beings.

Drugs Aging, 1991 Jul-Aug, 1(4), 303 - 16
The effect of aging on host defences . Implications for therapy; Scordamaglia A et al.; Immunosenescence is a well known physiological phenomenon resulting from reduced efficiency of the immune system in the elderly . It has been studied both in animal models and in humans . In this review attention is focused on T cell responsiveness, since this cell type is both a marker of the immune response and one of the main targets of several drugs . For this latter reason, most studies of the effect of drugs on the immune system have been performed with reference to the effects on T lymphocytes . In the second part of the article experimental data concerning several drugs and drug classes {steroids, calcium antagonists, theophylline, histamine H1- and H2-receptor antagonists, sodium cromoglycate (cromolyn sodium), pirenzepine, rosaprostol, beta 2-mimetics, antibiotics and antibacterials} and immune responsiveness are reviewed . Lastly, the clinical perspectives of pharmacological treatment in aged subjects in relation to immunosenescence are evaluated.

Biull Eksp Biol Med, 1991 Jul, 112(7), 65 - 7
{Effects of sodium hypochlorite on oxygen balance and functional state of the small intestine in experimental peritonitis}; Kulaev GK et al.; Sodium hypochlorite, administrated intravenously and intraperitoneally, leads to normal oxygen balance, metabolism and motility of small intestine in peritonitis . Anti-hypoxia effect of this substance is realized by an increase of oxygen content in the blood . It is useful to use sodium hypochlorite in general peritonitis for antibacterial therapy and against tissue hypoxia without side effects.

Farmaco, 1991 Jul-Aug, 46(7-8), 887 - 97
Synthesis and in vitro antibacterial properties of 2-(3-bromo-5-isoxazolylideneamino-oxy)acetamido-beta-lactam derivatives; Sala A et al.; The synthesis of new 2-(3-bromo-5-isoxazolylideneamino-oxy)acetic acids and their condensation derivatives with suitable beta-lactam nuclei is reported . Their antibacterial properties have been tested in vitro . An interesting activity against Gram-positive bacteria including beta-lactamase-producing microorganisms was found among the cephalosporanic acid derivatives.

Farmaco, 1991 Jul-Aug, 46(7-8), 843 - 60
Synthesis and immunomodulating activity of condensed N-aryl-2-cyano-3-oxo-3-pyrazolyl-propanamides; Doria G et al.; A series of condensed N-aryl-2-cyano-3-oxo-3-pyrazolyl-propanamides were synthesized and evaluated for immunomodulating activity following intraperitoneal administration . These new molecules were found to enhance macrophage cytotoxicity and stimulate host mediated antibacterial defences in mice . The compound 3-cyano-3-(1,4-dihydro-1-phenyl-{1}-benzothiopyrano{4,3-c}pyrazol- 3-yl}-3-oxo-N-phenyl-propanamide, chosen for wider pharmacological investigation, proved effective in preventing adjuvant-induced arthritis development in rats.

J Protozool, 1991 Jul-Aug, 38(4), 421 - 5
In vitro production of lysine from 2,2'-diaminopimelic acid by rumen protozoa; Onodera R et al.; Rumen protozoa can produce lysine from free 2,2'-diaminopimelic acid (DAP) . However, the quantitative importance of this transformation has been disputed; lysine contents of protozoal incubation supernatants reported by Onodera & Kandatsu and Masson & Ling show a 26-fold difference . The in vitro experimental methods of both groups were compared to determine the causes of this difference . Lysine production was proportional to DAP concentration . Results with rumen protozoa from sheep or goats were similar . The incubation medium and deproteinizing procedure of the Welsh group gave a two-fold increase in lysine production compared with Japanese protocols . Omissions of rice starch from protozoal incubations slightly increased lysine production, whereas omissions of antibacterial agents resulted in varying, yet relatively small changes . The greatest cause of the difference was the number of rumen protozoa incubated . When this factor was taken into account, the difference in the maximum rates of lysine production between the Welsh and Japanese groups was only three-fold, namely 4.5 versus 15.0 nmol lysine/10(5) protozoa/h . Adding other amino acids to the incubations suggested that DAP uptake by rumen protozoa may occur via transport system ASC . The importance of DAP metabolism by protozoa as a source of lysine for ruminant host animals is discussed.

Chem Pharm Bull (Tokyo), 1991 Jul, 39(7), 1726 - 30
Studies on the chemical modification of monensin . III . Synthesis and sodium ion transport activity of macrocyclic monensylamino acid-1,29-lactones; Nakamura A et al.; Monensylglycine (2a) was lactonized to macrocyclic monensylglycine-1,29-lactone (3a) by Corey's method . Lactonization of monensylamino acids (2b--d) to monensylamino acid-1,29-lactones (3b--d) was carried out by utilizing the template effect of K+ ion . Monobenzyl esters of dicarboxylic monensylamino acids (5e--f) also were lactonized followed by debenzylation to yield carboxylic monensylamino acid-1,29-lactones (3e--f) . Sodium ion transport activity of monensin (1) and the lactones (3) was measured in a liquid membrane and in guinea pig erythrocyte membrane . Monensylaspartic acid-1,29-lactone (3e) exhibited 2.5 times higher activity than 1 in the liquid membrane . Monensylalanine-1,29-lactone (3b), monensylphenylalanine-1,29-lactone (3c), and monensyltyrosine-1,29-lactone (3d), having smaller Na+ ion transport activity than 3e, showed weak antibacterial activity, while 3e was inactive in biological tests, probably due to the lower lipophilicity.

Clin Pharmacokinet, 1991 Jul, 21(1), 11 - 26
Pharmacokinetics of rectal drug administration, Part I . General considerations and clinical applications of centrally acting drugs; van Hoogdalem E et al.; Generally, oral administration is the route of choice in the daily practice of pharmacotherapy . However, in some circumstances this is impractical or even impossible (during nausea and vomiting or convulsions, in uncooperative patients and before surgery) . In these cases, the rectal route may represent a practical alternative and rectal administration is now well accepted for delivering, for example, anticonvulsants, non-narcotic and narcotic analgesics, theophylline, antiemetics and antibacterial agents, and for inducing anaesthesia in children . It may also represent an interesting alternative to intravenous or other injection routes of drug administration . The rate and extent of rectal drug absorption are often lower than with oral absorption, possibly an inherent factor owing to the relatively small surface area available for drug uptake . In addition, the composition of the rectal formulation (solid vs liquid, nature of the suppository base) appears to be an important factor in the absorption process by determining the pattern of drug release . This relation between formulation and drug uptake has been clearly demonstrated for drugs like diazepam, paracetamol (acetaminophen), indomethacin, methadone and diflunisal . Coadministration of absorption-promoting agents (surfactants, sodium salicylate, enamines) represents another approach towards manipulating rectal drug absorption, although this concept requires further research concerning both efficacy and safety . For a number of drugs the extent of rectal absorption has been reported to exceed oral values, which may reflect partial avoidance of hepatic first-pass metabolism after rectal delivery . This phenomenon has been reported for morphine, metoclopramide, ergotamine, lidocaine (lignocaine) and propranolol . Rectal drug delivery in a site- and rate-controlled manner using osmotic pumps or hydrogel formulations may provide opportunities for manipulating systemic drug concentrations and drug effects . The extent of first-pass metabolism may be influenced (lidocaine), depending on the site of drug administration in the rectum . The rate of delivery may determine systemic drug action and side effects (nifedipine), and it may affect the local action of concurrently administered absorption promoters on drug uptake (cefoxitin) . Local irritation is increasingly being acknowledged as a possible complication of rectal drug therapy . Long term medication with rectal ergotamine and acetylsalicylic acid, for example, may result in rectal ulceration, and irritation after a single administration of several drugs and formulations has been described . The assessment of tolerability and safety is imperative in the design of rectal formulations . Recent studies corroborate the clinical relevance of rectal drug therapy, and the value of the rectal route as an alternative to parenteral administration has been assessed for several drugs, e.g . diazepam, midazolam, morphine and diclofenac.(ABSTRACT TRUNCATED AT 400 WORDS)

Yakugaku Zasshi, 1991 Jul, 111(7), 386 - 92
{Studies on quinolone antibiotics . III . Synthesis and antibacterial activity of 5-amino-7-(2-aminoalkoxy)-1-cyclopropyl-6-fluoro-1,4- dihydro-4-oxoquinoline-3-carboxylic acid and their derivatives}; Yoshida T et al.; 5-Amino-7-(2-aminoalkoxy)-1-cyclopropyl-6-fluoro-1,4-dihydro-4- oxoquinoline-3-carboxylic acid and their derivatives (10, 11) were prepared and their antibacterial activities were evaluated . As a result of in vitro antibacterial screening, the compounds having mono- or di-methyl (11d, e) group at alpha-position of amino group were most effective among the 7-aminoalkoxy derivatives . Structure-activity relationship of these compounds is also discussed.

J Biol Chem, 1991 Jun 25, 266(18), 11510 - 7
The cecropin locus . Cloning and expression of a gene cluster encoding three antibacterial peptides in Hyalophora cecropia; Gudmundsson GH et al.; Cecropins A, B, and D are antibacterial peptides of 35-37 amino acids that are synthesized in pupae of the Cecropia moth (Hyalophora cecropia) as a response to a bacterial infection . cDNA cloning has shown that the cecropins are made as preproproteins that are processed in four steps to the mature peptides . We have now cloned the genes for preprocecropins A and D, data that together with earlier work on the B gene has made it possible to deduce the arrangement of the cecropin locus . The genes for the three cecropins are organized in a large cluster spanning 20 kilobases of DNA and for each gene there is one copy/haploid genome . The size of the cluster is in part due to long distances between the genes and to the presence of insertion elements in the introns of the A and D genes . The cecropin genes are not expressed in parallel . Transcripts for cecropins A and B appear within 2 h after injection of live bacteria, they reach a maximum after 48 h, and they are continuously expressed at this level for several days . The D gene has a delayed pattern of expression where transcripts appear within 48-96 h and reach a maximum after 144 h . In consonance is also the production of the mature cecropins A, B, and D where the active cecropins A and B are detected in the hemolymph within 10-24 h while the D form is not detected until 48 h post infection . Control injections with sterile saline produced only a weak induction of the cecropin genes.

J Biol Chem, 1991 Jun 25, 266(18), 11518 - 21
A highly repetitive, mariner-like element in the genome of Hyalophora cecropia; Lidholm DA et al.; A highly repetitive DNA element, homologous to the mariner transposon of Drosophila mauritiana was found in the intron of the gene for cecropin A, an antibacterial peptide from the Cecropia moth . The mariner-like elements (MLE) represent a homogeneous population with a copy number of about 1000/genome . Sequencing analysis showed it to be 1255 base pairs long, including 38-base pair terminal inverted repeats . The MLE contains a defective reading frame . Nevertheless, the putative product is clearly homologous to the predicted translation product encoded by mariner . In consonance is also the fact that the inverted repeats are highly conserved between the two elements and that the overall DNA homology is 48% . Since the mariner element is present in several Drosophila species closely related to Drosophila melanogaster and since MLE is present in the lepidopteran Cecropia, a route of horizontal transfer is indicated rather than vertical transmission from a common ancestor . This suggests the possible use of mariner for the construction of an interspecies vector.

J Antibiot (Tokyo), 1991 Jun, 44(6), 646 - 58
Synthesis and biological activity of 1-N-{4-(substituted)amidino and guanidino-2-hydroxybutyryl}kanamycins A and B; Yamasaki T et al.; The synthesis and biological properties of 1-N-{4-(substituted)amidino and guanidino-2-hydroxybutyryl}kanamycins A and B are described . Reaction of 3,3",6'-tri-N-tert-butoxycarbonyl-amikacin with an appropriate amidinating or guanidinating reagent and subsequent deblocking gave a series of amikacin derivatives having an amidino or guanidino group on the 4"'-position . The corresponding kanamycin B analogs were also prepared by a similar procedure . Among these derivatives, 1-N-(4-formamidino- and guanidino-2-hydroxybutyryl)kanamycins A (7a and 7k) and B (11 and 14) exhibited antibacterial activity similar to the corresponding 4-amino analogs . The nephrotoxic potential of selected compounds is also briefly discussed.

Minerva Med, 1991 Jun, 82(6), 387 - 94
{An open comparative study of sulbactam/ampicillin vs mezlocillin in adult and pediatric patients . Efficacy and tolerability}; Chiodo F et al.; Sulbactam is a beta-lactamase inhibitor that, when combined with ampicillin, extends its antibacterial activity against beta-lactamases producing organisms . The clinical efficacy and safety of the sulbactam/ampicillin (S/A) combination versus mezlocillin (M), was assessed in a prospective comparative randomised study . Sixty-five patients (12 children), with lower respiratory tract infections (40), UTIs (20), and skin/soft tissue infections (5), were treated with S/A (32) or M (33 patients), given IV or IM . The two treatment groups did not significantly differ in types of infection, infecting organisms, and severity of underlying disease . Explicit criteria were used to define infections, clinical response, local and systemic tolerability, and adverse effects . A total of 33 organisms were isolated; 3/33 were resistant to S/A, 7/33 to M, and 15/33 to A alone . A successful clinical outcome (cure + improvement), was obtained in 29 out of 30 assessable patients in the S/A group, and in 30/31 in the M group . Both treatments resulted 100% effective in eradicating infecting pathogens: this confirms their high bactericidal activity, also against bacterial species showing remarkable antibiotic resistance patterns, and in variously immunocompromised hosts . Both S/A and M; therapeutic courses were well tolerated; only four out of the 61 assessable patients (2 in S/A, and 2 in M group), experimented mild, transient side-effects, that did not require modification of the treatment regimens . We conclude that both S/A and M appeared very safe and effective drugs; in regard to clinical and microbiological effectiveness and local and systemic tolerability, no statistically significant differences (p greater than 0.05) between the two groups were observed, in treating various bacterial infections, in both adult and paediatric age.

APMIS, 1991 Jun, 99(6), 487 - 91
How do animal phagocytes process bacterial lipopolysaccharides?
Munford RS.
Phagocytic cells, the front-line defense against bacterial invasion, have enzymes that deacylate and dephosphorylate the toxic lipid A moiety of gram-negative bacterial lipopolysaccharide (LPS, also called endotoxin) . These enzymes may detoxify LPS without destroying its immunogenicity or antigenicity--in fact, the polysaccharide region of LPS often resists degradation in vivo and retains its antigenic epitopes for long periods of time . The net result, detoxification of LPS with preservation of its immunogenic and antigenic properties, may prevent excessive inflammatory responses while promoting the development of antibacterial immunity.

Jpn J Antibiot, 1991 Jun, 44(6), 625 - 34
{Clinical evaluation of fleroxacin in gynecological infections}; Matsuda S et al.; Fleroxacin (FLRX), a new quinolone oral antibacterial agent, was studied in the field of obstetrics and gynecology, and the following results were obtained . 1 . Clinical efficacy was evaluated in 105 patients (intrauterine infection 38, adnexitis 28, extragenital organ infection 29, others 10), with an exclusion of 9 patients out of a total of 114 patients . FLRX was orally administered at 200 mg or 300 mg once daily . 2 . Clinical efficacy rates were 37/38 (97.4%) in intrauterine infection, 26/28 (92.9%) in adnexitis, 29/29 (100%) in extragenital organ infection and 10/10 (100%) in others . 3 . Efficacy rates classified by isolated organisms were 23/23 (100%) in single infections by Gram-positive organisms, 11/13 (84.6%) in those by Gram-negative organisms, 8/9 (88.9%) in those by anaerobic organisms and 15/19 (78.9%) in mixed infections . 4 . Side effects were observed in 4 cases (3.5%); gastrointestinal disorder with diarrhea and diarrhea in 1 patient each and insomnia in 2 patients . In laboratory examination, eosinophilia and elevation of GOT and GPT were noted in 1 patient each (1.9%) . Based on the above results, we consider that FLRX is a useful drug for the obstetrical and gynecological infections.

J Am Vet Med Assoc, 1991 Jun 1, 198(11), 1941 - 5
Evaluation of surgical scrub and antiseptic solutions for surgical preparation of canine paws; Swaim SF et al.; The purpose of the prospective study reported here was to evaluate surgical preparation of canine paws . Three combinations of surgical scrub solutions and antiseptic solutions were used: (1) 7.5% povidone-iodine scrub/10% povidone-iodine solution; (2) 2% chlorhexidine acetate scrub/2% chlorhexidine diacetate solution; and (3) tincture of green soap/70% isopropyl alcohol . The control was warm (38 to 42 C) tap water . Four microbial colony counts were used to evaluate surgical preparation of 4 paws of 8 dogs . Specimens were obtained from the paws for a baseline microbial flora count . After surgical scrub was performed, additional specimens were obtained for bacteriologic culturing . Antiseptic was applied followed by collection of another specimen for bacteriologic culturing . A final specimen was obtained following a 24-hour period under a sterile occlusive bandage . The 3 scrub solutions and the tap water control resulted in lower colony counts following scrubbing of the paws; however, only the 3 antiseptic solutions resulted in further colony count reduction after their application . Evaluation of residual colony counts isolated from specimens taken after a 24-hour period under a sterile occlusive bandage revealed chlorhexidine and povidone-iodine scrub/antiseptic combinations to be similar in antibacterial activity, with significantly (P less than or equal to 0.05) lower colony counts than those from specimens of paws treated with either the tincture of green soap/isopropyl alcohol combination or the tap water control . The lack of a significant difference between the bacterial counts immediately after surgical preparation with povidone-iodine and chlorhexidine and their respective 24-hour residual counts, indicated no particular advantage to surgical preparation and occlusive bandaging 24 hours prior to surgery.(ABSTRACT TRUNCATED AT 250 WORDS)

Ortop Travmatol Protez, 1991 Jun, (6), 1 - 5
{Experimental substantiation of using gentacycol for prevention of wound infection in gunshot bone fractures of the extremities}; Shaposhnikov IuG et al.; There have been experimentally studied the antibacterial properties of the preparation "gentacycol" developed in the research institute of antibiotics . Its effective agent is gentamycin and as the matrix of a carrier modified collagen is used . It is indicated that in vitro and at implantation in preliminary infected ordinary and gunshot osseous wounds in rabbits and dogs gentacycol inhibits the growth of aerobic and, that is especially important, anaerobic microflora, limits the development of inflammatory Process and stimulates, to a certain extent, reparative osteogenesis . The obtained data allows to recommend gentacycol application for prophylaxis of wound infection in treatment of gunshot limb bone injuries.

Bioorg Khim, 1991 Jun, 17(6), 849 - 54
{Synthesis and antibacterial activity of eremomycin esters through the carboxyl group}; Pavlov AIu et al.; Methyl, benzyl and diphenylmethyl esters of the glycopeptide antibiotic eremomycin were obtained by its treatment with corresponding diazoalkanes . The esters have high antibacterial activity but are less active than the parent antibiotic.

Khirurgiia (Mosk), 1991 Jun, (6), 109 - 11
{Biologically active helevin-based compositions in the treatment of pleural empyema}; Vishnevskii AA et al.; The article analyses the method of topical open treatment of postoperative pyothorax in 17 patients with the use of biologically active helevin-based compositions . The control group was made up of 11 patients with a similar suppurative process who received topical treatment by the same method but with the use of ointments with antibiotics and antiseptics on a fat base . With the use of biologically active compositions (BAC) on a helevin-base, the empyema cavity was completely freed from the pyonecrotic masses and its walls filled with granulation tissue on day 7 of treatment . In the control group the cavity was completely cleansed only on day 19 of treatment . It is shown that BAC possesses a high antibacterial effect not only due to the antibacterial components but because it is based on the laws of physical antiseptics.

Biochim Biophys Acta, 1991 May 7, 1064(2), 256 - 66
Formation of ion channels in planar lipid bilayer membranes by synthetic basic peptides; Anzai K et al.; We made use of a planar lipid bilayer system to examine the action of synthetic basic peptides which model the prepiece moiety of mitochondrial protein precursors and have antibacterial activity against Gram-positive bacteria . The sequences of the peptides used were as follows: Ac-(Ala-Arg-Leu)3-NHCH3 (3(3}, Ac-(Leu-Ala-Arg-Leu)2-NHCH3 (4(2}, Ac-(Leu-Ala-Arg-Leu)3-NHCH3 (4(3}, Ac-(Leu-Leu-Ala-Arg-Leu)2-NHCH3 (5(2} . These peptides interacted differently with planar lipid bilayer membranes and membrane conductance increased by the formation of ion channels . The effects of the peptides on the macroscopic current-increase and on the probability of channel formation, at the single channel level were in the order of 4(3) greater than 4(2) approximately 5(2) much greater than 3(3), a finding which correlates with the antibacterial activity of these peptides . The micromolar (microM) order concentration at which the channel was formed resembles that causing antibacterial activity . Thus, the peptide antibacterial activity may occur through an increase in ion permeability of the bacterial membrane . The single-channel properties were investigated in detail using 4(3), the peptide with the highest ion channel-forming activity . Many types of channels were observed with respect to conductance (2-750 pS) and voltage dependency of gating . However, the channels were all cation-selective . These results suggest that the ion channels formed by peptide 4(3) may be able to take on a variety of conformations and/or assembly.

Khirurgiia (Mosk), 1991 May, (5), 13 - 8
{Peritoneo-enteric lavage in generalized purulent peritonitis during multiple organ insufficiency}; Davydov IuA et al.; The article analyses two matched groups of patients with generalized purulent peritonitis of 72-hour duration in the stage of polyorganic insufficiency . There were 100 patients . Application of organ-resuscitation measures in the abdominosplanchnic zone is the key moment of the surgical treatment of patients with generalized purulent peritonitis . In view of this, peritoneoenteric lavage with oxygenated energy mass of 5-10% glucose solution is indicated together with intensive infusion-transfusion, antibacterial therapy, and extracorporeal detoxification for such patients . Combination of peritoneal lavage with enteric through a distal retrograde immobilizing dehydrostatic iliostomy produces the best results.

J Periodontol, 1991 May, 62(5), 312 - 6
Topical application of doxycycline on periodontally involved root surfaces in vitro: comparative analysis of substantivity on cementum and dentin; Demirel K et al.; In this study, substantivity of topically applied doxycycline hydrochloride on root surfaces obtained from patients with periodontal disease was studied in vitro . Cementum and dentin specimens were impregnated with aqueous solutions of doxycycline for 3 minutes, and incubated in serum for 10 minutes, 7 days, and 14 days . Substantivity was determined by agar diffusion inhibition assay . Comparative analyses of cementum versus dentin groups were conducted with 2-way analysis of variance . Results indicated that there was no statistically significant differences between the binding potential of doxycycline to cementum and dentin specimens . Antibacterial effect of specimens treated with the concentration of 100 mg/ml persisted for 14 days, indicating the presence of doxycycline in biologically active form . Our findings demonstrate the long lasting substantivity of doxycycline hydrochloride on periodontally diseased root surfaces and supports the concept of using root surfaces as a substrate for the deposition and slow release for local tetracycline delivery.

J Med Chem, 1991 May, 34(5), 1732 - 9
Synthesis, hydrolysis rates, supercomputer modeling, and antibacterial activity of bicyclic tetrahydropyridazinones; Jungheim LN et al.; Bicyclic tetrahydropyridazinones, such as 13, where X are strongly electron-withdrawing groups, were synthesized to investigate their antibacterial activity . These delta-lactams are homologues of bicyclic pyrazolidinones 15, which were the first non-beta-lactam containing compounds reported to bind to penicillin-binding proteins (PBPs) . The delta-lactam compounds exhibit poor antibacterial activity despite having reactivity comparable to the gamma-lactams . Molecular modeling based on semiempirical molecular orbital calculations on a Cray X-MP supercomputer, predicted that the reason for the inactivity is steric bulk hindering high affinity of the compounds to PBPs, as well as high conformational flexibility of the tetrahydropyridazinone ring hampering effective alignment of the molecule in the active site . Subsequent PBP binding experiments confirmed that this class of compound does not bind to PBPs.

Mutat Res, 1991 May, 260(1), 65 - 72
Genotoxicity testing of chloramphenicol in rodent and human cells; Martelli A et al.; The results of this work, carried out to extend the limited information at present available on the genotoxic potential of chloramphenicol (CAP), indicate that in millimolar concentrations this antibacterial agent produced a minimal amount of DNA fragmentation in both V79 cells and metabolically competent rat hepatocytes . Moreover, a level of DNA-repair synthesis indicative of a weak but positive response was detected in primary cultures of liver cells obtained from 2 of 3 human donors, and a borderline degree of repair was present in those prepared from rats . The promutagenic character of CAP-induced DNA lesions was confirmed by a low but significant increase in the frequency of 6-thioguanine-resistant clones of V79 cells, which, however, was absent when the exposure was done in the presence of co-cultured rat hepatocytes . Finally, oral administration to rats of 1/2 LD50 CAP did not increase the incidence of either micronucleated polychromatic erythrocytes or micronucleated hepatocytes . Taken as a whole these findings suggest that CAP should be considered a compound intrinsically capable of producing a very weak genotoxic effect, but only at concentrations about 25 times higher than those occurring in patients treated with maximal therapeutic dosages.

Plast Reconstr Surg, 1991 May, 87(5), 917 - 24
In vitro toxicity testing for antibacterials against human keratinocytes; Smoot EC 3rd et al.; The use of cultured human keratinocytes in an in vitro comparison of topical antibacterial toxicity for epithelial cells was examined . The complement of three assessments allows testing of epithelial migration, growth, and survival . The three assessments included (1) flow cytometry for determination of cell survival, (2) a comparison of confluent cell culture growth after antibacterial exposures, and (3) an evaluation of cell migration using a technique of dermal explants to study radial migration . A comparative ranking of the toxicities of the various topical antibacterials was determined with the three assessments . This has confirmed anecdotal reports that many of the topical antibacterials are cell-toxic and may inhibit wound healing . This information can be directly extrapolated to the clinical setting, unlike many of the animal data for wound healing that currently exist.

J Nat Prod, 1991 May-Jun, 54(3), 785 - 95
Biologically active metabolites from Xenorhabdus spp., Part 2 . Benzopyran-1-one derivatives with gastroprotective activity; McInerney BV et al.; Two novel antibiotic compounds, named xenocoumacins 1 {2} and 2 {3}, with potent antiulcer activity were isolated from cultures of Xenorhabdus spp . Both compounds exhibit antibacterial activity and potent antiulcer activity against stress-induced ulcers when dosed orally . In addition, 2 has antifungal activity . Their chemical structures were determined by extensive 1H-nmr, 13C-nmr, and mass spectral studies to be 3,4-dihydro-8-hydroxy-1H-2-benzopyran-1-one derivatives.

Antibiot Khimioter, 1991 May, 36(5), 30 - 3
{Ways of increasing the effectiveness of antibacterial therapy in newborns}; Strachunskii LS; Ways for increasing antibiotic therapy efficacy in newborns are discussed . They are the following: consideration of the structure of the antibiotic use, improvement of infection diagnosis, the use of computers in epidemiological supervision of antibiotic resistance, the use of "old" antibiotics in new dosage forms, pharmacokinetic monitoring . The data on the frequency of the antibiotic use in newborns in maternity hospitals, at home and in neonatal departments as well as on diagnosis and treatment of chlamydiosis in newborns are presented . Requirements to the computer programs on control of antibiotic resistance are described . With the account of the requirements an original epidemiological program for personal computers was developed . The results of the pharmacokinetic monitoring of the use of sisomicin and amikacin are presented as well.

Antibiot Khimioter, 1991 May, 36(5), 14 - 6
{Prevention of postoperative infectious complications with suture materials containing gentamicin}; Iushkov SF et al.; Sutural materials containing antibiotics such as gentamicin and tetracycline were studied on dogs with respect to the action on development of inflammation reactions after operations on the large intestine . It was shown that the antibacterial surgical threads had a prophylactic action and inhibited infection development . There was noted a significant advantage of the threads over the control ones not containing the antibiotics . The inflammatory reactions were less intensive and of shorter duration . The terms of onset and completion of the reparation also markedly shortened.

Res Vet Sci, 1991 May, 50(3), 301 - 7
Distribution of penicillin-G and spiramycin to tissue cages and subcutaneous tissue fluid in calves; Bengtsson B et al.; Antibacterial drug concentrations in serum, tissue cage fluid (TCF) and subcutaneous tissue fluid (SF), sampled either by filter paper discs or by microcapillaries, were measured after single intramuscular injections of potassium penicillin-G (KPG), procaine penicillin-G (PPG) and spiramycin adipate in calves . Concentration-time curves had essentially similar profiles in serum and SF, but peak levels were lower and occurred later in SF . From approximately four hours after drug administration, penicillin-G levels in SF were similar to levels in serum after KPG as well as after PPG administration . Elimination half-life (t1/2) of penicillin-G in serum was similar to t1/2 in SF after PPG administration but was longer in SF than in serum after KPG administration . Spiramycin concentrations were higher in SF than in serum and the t1/2 of spiramycin in SF was longer than in serum . For all three drugs, the t1/2 was longer in TCF than in serum and concentration-time curves in TCF were characterised by a slow rise and decline . The two methods of sampling SF, by filter paper discs and by microcapillaries, gave similar but not identical results . Penetration into SF and TCF, measured as the total area under curve ratio, was better for spiramycin than for penicillin-G, but the latter drug had a higher penetration ratio to TCF in the first 12 hours.

Pathol Biol (Paris), 1991 May, 39(5), 503 - 6
{Diffusion of imipenem in synovial fluid}; Pechinot A et al.; The diffusion of imipenem (IMP) in the knee joint was studied after a 1 g i.v . administration of Tienam over one hour . The synovial fluid was collected under anesthesia during arthroscopy carried out for mechanical lesions of the knee (meniscal lesions after ligamental injuries or sequelae after meniscectomy), in 3 groups of six patients at one, two, or three hours after the end of injection of IMP . The concentrations of IMP determined by high performance liquid chromatography (HPLC) were: 42.5, 20.1, 9.3 and 5.7 mg/l in the blood at T0, T1, T2 and T3 hr, respectively; 20.4, 13.0 and 7.9 mg/l in the synovial fluid at T1, T2 and T3, respectively . The decrease of IMP concentrations in the synovial fluid was 1,5 times as low as in serum . On account of its broad-spectrum antibacterial activity and our data, IMP could be used in perioperative prophylaxis of the knee joint surgery.

Pathol Biol (Paris), 1991 May, 39(5), 471 - 9
{Evaluation of an automated system in bacteriology . Application to bacteriological susceptibility tests}; Philippin JL et al.; Susceptibility tests have been compared between a new automated system and the reference method by agar diffusion . The COBAS-Micro apparatus for bacterial susceptibility tests is intended for rapid determinations with, normally, an incubation time of 5 h at 37 degrees C . Its is compatible with strains requiring greater than 18 h incubation . With this technique a large range of antibacterial substances (greater than 60) can be studied, in groups of fifteen . With the help of a computerized soft-ware, one growth-index:EPR (End Point Ratio) is calculated, in comparison with a standard, for each antibacterial agent tested and expressed in three categories: SIR . The findings are optimized according to the limits prescribed by the NCCLS . The reference method, by agar-diffusion, is as described by the Comite de l'Antibiogramme de la Societe Francaise de Microbiologie (CA-SFM) . A total of 1,048 strains were tested by the two techniques: 518 Gram negative rods, 530 Gram positive cocci, with four common antibiotics . The percentages of agreement between the two groups were: 96% full agreement and minor discrepancy, 4% major and very major discrepancy . This automated system seems to be perfectly suitable for susceptibility testing in a routine laboratory, especially with strains isolated from ambulatory patients.

Vrach Delo, 1991 May, (5), 96 - 8
{Variants in the manifestations of the generalized form of yersiniosis}; Bondarev LS et al.; The clinical manifestations of generalized yersiniosis were studied in 61 patients . Primary generalized form was observed in 18 patients . Predecessors were gastroenteritis, appendicular syndrome . Clinical manifestations were polymorphous . All patients revealed fever and exanthema, 5%--catarrhal phenomena, 63.3%--lymphadenitis, 86%--arthralgia, 39.2%--gastrointestinal disorders, 114%--icteric syndrome . In 7.6% the course was protracted with recurrences of fever, exanthema, jaundice, diarrhea, formation of arthritis, Reiter's syndrome . Antibacterial treatment was carried out by aminoglycosides, cephalosporins.

Rev Infect Dis, 1991 May-Jun, 13(3), 496 - 503
Empiric therapy with amphotericin B in febrile granulocytopenic patients; Walsh TJ et al.; The early diagnosis of invasive fungal infection in granulocytopenic patients remains unreliable . Granulocytopenic patients who are persistently or recurrently febrile despite therapy with appropriate antibacterial agents are at high risk for the development of such infection . Two randomized clinical trials demonstrated that the empiric administration of amphotericin B to persistently or recurrently febrile granulocytopenic patients decreased the frequency, morbidity, and mortality of invasive fungal infection; these effects were especially marked in profoundly granulocytopenic patients who were not receiving antifungal prophylaxis . Current studies continue to indicate that prompt empiric administration of amphotericin B to persistently or recurrently febrile granulocytopenic patients ensures earlier treatment of deep mycoses . The roles of newer antifungal triazole compounds and of liposomal and lipid complexes of amphotericin B in empiric antifungal therapy must be investigated further in thoughtfully designed, randomized clinical trials.

Grud Serdechnososudistaia Khir, 1991 May, (5), 30 - 3
{Experimental premises and 1st experiences in the clinical use of antibacterial vascular prostheses under circumstances of increased risk of suppuration}; Dronov AF et al.; It was shown on the basis of laboratory and experimental data that created antibacterial vascular prostheses are marked, on the main, by local bacteriostatic and anticoagulative effect . It was found that heparin concentration of 3 to 500 U per 1 kg collagen causes a hyperadhesive effect on blood platelets and facilitates the formation of the primary thrombocytic thrombus . The free surface energy grows in this case from 34 +/- 0.8 to 66.3 +/- erg/cm2 . The optimal thromboresistant effect occurs in heparin content of 1 U per 1 mg collagen . That this choice is correct is confirmed on examination of the inner surface of the prostheses with an electron microscope after being in the blood flow for 45 minutes . Bifurcation and linear antibacterial prostheses were used in 9 patients with a high risk of suppuration verified by cultures of discharge from ulcers and lymph nodes, and the presence of lymphangitis and lymphadenitis . The effect was positive in 8 patients, 2 of them had superficial suppuration of the operative wounds.

Klin Med (Mosk), 1991 May, 69(5), 66 - 8
{Effect of antibacterial therapy on absorption of food in chronic bronchitis}; Akimova LA et al.; An absorptive function of the small intestine was examined in 79 chronic bronchitis patients on antibacterial therapy which is believed to induce dysbacteriosis . These factors seem essential in development of malabsorption syndrome observed in relevant patients.

Parodontol, 1991 May, 2(2), 151 - 7
{Subgingival irrigation in periodontal therapy}; Schlagenhauf U et al.; Subgingival plaque control is a decisive factor in periodontal therapy . Up to the present, removal of plaque and calculus by repeated scaling procedures has been regarded as the only viable method to achieve this goal . Recent investigations, however, suggest that the topical application of antibacterial substances or subgingival irrigation procedures are capable of yielding comparable improvements of periodontal health . This review paper is dedicated to subgingival irrigation . Besides an overview of techniques and results, we discuss our own experiences, including two case presentations . The results so far are encouraging . Nevertheless, due to the general lack of scientific data with extended time intervals, this method is not suitable yet as an alternative to conventional procedures in periodontal routine care . Until further long-term evidence has been gathered, subgingival irrigation should be regarded only as a valuable adjunct to scaling and root planing.

Proc Natl Acad Sci U S A, 1991 May 1, 88(9), 3792 - 6
Antibiotic magainins exert cytolytic activity against transformed cell lines through channel formation; Cruciani RA et al.; Magainins are an ionophoric class of vertebrate peptides with antibiotic activity against various microorganisms . Here we show that magainin 2 and synthetic analogues can rapidly and irreversibly lyse hematopoietic tumor and solid tumor target cells with a relative cytotoxic potency that parallels their antibacterial efficacy and at concentrations that are relatively nontoxic to well-differentiated cells . The cytotoxicity is prevented by cell depolarization . Magainins represent a natural cytolytic agent in vertebrates and may provide another therapeutic strategy for certain tumors.

Antimicrob Agents Chemother, 1991 May, 35(5), 910 - 5
Escherichia coli resistant to cephalosporins and quinolones is still susceptible to the cephalosporin-quinolone ester Ro 23-9424; Pace J et al.; Ro 23-9424 is a broad-spectrum antibacterial agent consisting of a cephalosporin (desacetylcefotaxime) linked through an ester bond to a fluoroquinolone (fleroxacin) . Its activity against mutants of Escherichia coli TE18 resistant to both antibacterial components was examined . E . coli TE18 overproduces the AmpC beta-lactamase and is resistant to several cephalosporins, including desacetylcefotaxime (MIC, 50 micrograms/ml), although it is still susceptible to Ro 23-9424 (MIC, 0.2 microgram/ml) . Thirty-five spontaneous, two-step mutants of E . coli TE18 which were resistant to fleroxacin (MIC, 50 micrograms/ml) were isolated . In the mutants, replicative DNA biosynthesis (permeabilized cells) was resistant to fleroxacin, and some mutants had porin abnormalities . However, all remained susceptible to Ro 23-9424 (MIC, 0.5 microgram/ml) . Examination of beta-lactamase activity in the parent strain revealed that it hydrolyzes desacetylcefotaxime more rapidly than it does Ro 23-9424 . Thus, Ro 23-9424 may be less susceptible to the gram-negative, chromosomal beta-lactamases that hydrolyze several broad-spectrum cephalosporins and may be effective in cases in which neither of its two components is active.

J Periodontol, 1991 May, 62(5), 341 - 50
Enhanced repair and regeneration of periodontal lesions in tetracycline-treated patients . Case reports; Moskow BS et al.; A group of cases is presented in which dramatic repair and regeneration of periodontal tissues lost as a result of periodontitis have occurred following systemic administration of tetracycline either alone or in combination with other forms of periodontal therapy . The nature and extent of regeneration demonstrated in these patients appears to be more dramatic than what has been shown previously when more conventional forms of periodontal therapy were utilized, even including bone grafting and guided tissue regeneration . The type of repair described has been shown in many instances to be long standing and is probably not totally related to the antibacterial characteristics of tetracycline . It is suggested that the ability of this drug to inhibit collagenolytic enzymes (collagenases) may have influenced the favorable clinical results achieved . The anti-collagenolytic properties of tetracycline are being considered with increasing frequency in the treatment of other systemic diseases characterized by collagen breakdown such as corneal ulcers, rheumatoid arthritis, diabetes, and dystrophic epidermolysis bullosa . Given the highly collagenous nature of the tissues of the periodontium, this report suggests that tetracycline could be of considerable value in the treatment of some types of periodontitis.

Antimicrob Agents Chemother, 1991 Apr, 35(4), 648 - 52
Global and regional cerebral metabolic rate of 2-{18F}fluoro-2-deoxy-D-glucose in the presence of ofloxacin, a gamma-aminobutyric acid a receptor antagonist; Camargo EE et al.; We investigated the effects of ofloxacin, a new antibacterial quinolone gamma-aminobutyric acid A receptor antagonist, on the global and regional cerebral metabolic rates of glucose (cMRgl) . Twelve healthy normal male volunteers (mean age, 26.7 years) were studied in a double-blind, placebo-controlled protocol of 11 days' duration . Results of a total of 42 positron emission tomography studies were obtained for these subjects: 12 base line, 18 during placebo, and 12 during ofloxacin administration . The conditions under which repeat positron emission tomography studies of the same subject were performed were reproduced as closely as possible . cMRgl was measured in 24 brain regions . The global cMRgl for base line, placebo, and ofloxacin were 8.82 +/- 1.17, 8.24 +/- 1.17, and 8.79 +/- 1.18 mg/min/100 g, respectively (mean +/- 1 standard deviation) . The mean global differences between base line and placebo and between ofloxacin and placebo were 5.1 and 6.6%, respectively . Analysis of variance of both the global and the regional cMRgl showed no statistical difference between base-line, placebo, and ofloxacin studies . Variations in cMRgl found in this study were not related to the presence of ofloxacin . Results of our study demonstrate that ofloxacin does not increase or decrease cMRgl beyond the limits of variability of the study.

Biochemistry, 1991 Apr 9, 30(14), 3518 - 26
Influence of environment on the antifolate drug trimethoprim: energy minimization studies; Fisher CL et al.; Environmental effects on trimethoprim (TMP), an inhibitor of bacterial dihydrofolate reductase (DHFR), were investigated with energy minimizations in vacuo, in the crystal, and in aqueous solution . The conformations, harmonic dynamics, and energetics of the antibacterial drug calculated in these environments were compared with each other and with those of two enzyme-bound drugs . Valence and torsion angles and their energies and overall intra- and intermolecular energies compensated one another in the minimized TMP structures . The conformations of the isolated and aqueous molecules were similar to that of TMP bound to chicken liver DHFR, while the structures from the TMP crystal and from the Escherichia coli DHFR complex were unique . Since neither the small-molecule crystal nor a local minimum of the isolated molecule gave the conformation of TMP bound to the bacterial enzyme, a combination of several experimental and theoretical techniques may be necessary to probe accessible conformations of a molecule.

J Biol Chem, 1991 Apr 5, 266(10), 6644 - 9
Organization and expression of the immunoresponsive lysozyme gene in the giant silk moth, Hyalophora cecropia; Sun SC et al.; Lysozyme is one of the antibacterial proteins that are produced by the giant silk moth Hyalophora cecropia in response to bacterial infection or injury . As an essential step toward the understanding of the mechanisms involved in the immune response, we have isolated and characterized the lysozyme gene from Cecropia . The complete nucleotide sequence of the gene as well as the immediate flanking sequences have been determined . The gene includes three exons . Its first intron contains a repetitive sequence . In the evolutionary aspect, the Cecropia lysozyme gene and two vertebrate lysozyme genes have been found to maintain a similar organization pattern of exons . The lysozyme gene has been found to be strongly induced by lipopolysaccharides and a phorbol ester as well as bacteria . In the induction by bacteria, the lysozyme transcript appears at about 2 h, reaches to the maximum level at about 24 h, and then declines . Comparison of the 5'-flanking sequences with several other genes involved in the immune response of H . cecropia and Drosophila melanogaster revealed a kappa B-like consensus sequence . This sequence is specifically recognized by a nuclear protein from the induced pupa.

Clin Microbiol Rev, 1991 Apr, 4(2), 150 - 5
Functions and activities of the Area Committee on Microbiology of the National Committee for Clinical Laboratory Standards; Washington JA; The Area Committee on Microbiology of the National Committee for Clinical Laboratory Standards has responsibility for the development of guidelines and standards in the field of clinical microbiology . Through the consensus process, representatives from government, industry, and professional societies have developed standards on antibacterial susceptibility testing (M2, M7, and M11), antimycobacterial susceptibility testing (M24), quality assurance on commercially prepared microbiological culture media (M22), evaluation of production lots of dehydrated Mueller-Hinton agar (M6), and preparation and testing of fetal bovine serum for use as cell culture growth supplement (M25) and guidelines on bactericidal tests (M26), protection of laboratory workers from infections transmitted by blood, body fluids, and tissue (M29), blood film examination for parasites (M15), and development of in vitro susceptibility testing criteria and quality control parameters (M23).

J Am Acad Dermatol, 1991 Apr, 24(4), 580 - 3
Embolic abscesses in hereditary hemorrhagic telangiectasia; Swanson DL et al.; Hereditary hemorrhagic telangiectasia is an inherited disorder in which patients may have multiple telangiectases and arteriovenous fistulas in the skin and internal organs . Patients can suffer from a variety of serious clinical complications, including abscess formation . We report two patients in whom neurologic symptoms developed from embolic abscesses, one for whom this complication was fatal . The reported incidence and microbiologic features of this complication are similar to that of endocarditis in patients with valvular heart disease . We believe that patients with hereditary hemorrhagic telangiectasia should receive similar antibacterial prophylaxis for procedures placing them at risk for bacteremia.

J Antibiot (Tokyo), 1991 Apr, 44(4), 415 - 21
Studies on beta-lactam antibiotics . II . Synthesis and antibacterial activity of cephalosporins with substituted 1,3-dithietane directly attached to the C-3 position; Nagano N et al.; Preparation of cephalosporins bearing a 1,3-dithietane ring attached to the C-3 position using intramolecular rearrangement are described . The diastereoisomers (6a-I and 6a-II) were separated by silica gel column chromatography . These 3-{4-(carbamoyl carboxymethylene)-1,3-dithietane-2-yl}cephems showed comparable activity against Gram-negative bacteria to that of ceftazidime.

J Med Chem, 1991 Apr, 34(4), 1468 - 75
New derivatives of kanamycin B obtained by modifications and substitutions in position 6" . 1 . Synthesis and microbiological evaluation; Van Schepdael A et al.; The clinical use of the potent, wide-spectrum aminoglycoside antibiotics is limited by oto- and nephrotoxicities . The latter is related to the binding of these polycationic drugs to negatively charged phospholipids and to the subsequent inhibition of lysosomal phospholipases . In order to explore the influence of a modification of the hydrophobic/hydrophilic balance at a specific site of an aminoglycoside, kanamycin B has been chemically modified in position 6" by substitution of the hydroxyl group with a halogen atom (or a pseudohalogen group), or an amino, an amido, a thioalkyl, or an alkoxy group, each series containing increasingly bulkier chains . Examination of the antibacterial activity of the synthesized compounds revealed a negative correlation between the size of the 6"-substituent and the antibacterial activity against kanamycin B sensitive Gram-positive and -negative organisms . Only derivatives with small substituents in position 6", namely chloro, bromo, azido, amino, methylcarbamido, acetamido, methylthio, methylsulfinyl, O-methyl, O-ethyl, and O-isopropyl, showed acceptable activity (geometric mean of minimum inhibitory concentrations for Gram-negative strains less than or equal to 2.5 mg/L; value for kanamycin B, 0.5 mg/L) . In vitro toxicological evaluation of all derivatives and computer-aided conformational analysis of selected compounds inserted in a phosphatidylinositol monolayer are presented in the following paper in this issue.

Minerva Urol Nefrol, 1991 Apr-Jun, 43(2), 53 - 63
{Cystic kidney disease in the adult . Update}; Alberti C et al.; Genetic changes on the extracellular matrix of nephron basal lamina seem to underlie the pathogenesis of renal cystic disease, as also confirmed by experimental results . The cysts behave as dynamic structures and repeat some physiological features of the nephron segment which gave origin to them . These properties reflect, for instance, on the pharmacokinetics of antibacterial drugs . New imaging techniques detect more and more asymptomatic cystic formations of very little volume . Moreover, a better definition of some complications, such as haemorrhage and infections, is afforded by the RX- and RM-CT and the use of specific radiopharmaceuticals (67Ga-citrate, 99mTc-sulfur-colloids, 111In-labeled leucocytes).

Antibiot Khimioter, 1991 Apr, 36(4), 24 - 6
{Antibacterial and therapeutic effectiveness of a pectin from sea grass Zostera}; Zaporozhets TS et al.; The kinetics of the antibacterial activity of zosterin, a polysaccharide preparation of a sea grass belonging to Zoster, was studied . By its chemical structure zosterin is a low ++methoxylated pectin . In vitro the preparation markedly inhibited the growth of ++Gram-negative and ++Gram-positive organisms: S . aureus, E . coli, Y . pseudotuberculosis, S . typhimurium and Ps . aeruginosa . On a model of experimental pseudotuberculosis++ infection caused by oral contamination of mice F1 (CBA X C57B1) with a suspension of Y . pseudotuberculosis zosterin was shown to have a therapeutic effect . It protected 30 to 40 per cent of the animals when administered per os simultaneously with or 24 hours after the contamination . The results are in favour of the zosterin further investigation as a preparation useful in prevention of intestinal infections in persons being in contact with the patients.

Bioorg Khim, 1991 Apr, 17(4), 561 - 6
{Use of mass spectrometry with chemical ionization in screening antibacterial antibiotics with a broad spectrum of action (aminoglycosides and macrolides)}; Rozynov BV et al.; It is shown that mass-spectrometry with ammonia desorption chemical ionization (ADCI) can be used for identification of aminoglycosides and macrolides at the initial stages of screening . ADCI can also be used for selection of strains which form the lowest amounts of by-products, as well as for optimization of biosynthetic conditions.

J Chemother, 1991 Apr, 3(2), 75 - 8
Beta-lactamase: lessons in the art of survival; Citri N; 1 . A beta-lactamase molecule is a marvelous device enabling its marker to thrive in a hostile and potentially lethal environment . What is more, the protective effect is extended to otherwise vulnerable organisms, securing their survival in the sheltered neighborhood . Curiously, such environmental implications had no discernible impact on the strategy of antibacterial chemotherapy . Moreover, traditional diagnostic routines are largely responsible for the sheltered survival of susceptible pathogens . 2 . For half a century, since their existence was discovered by Abraham and Chain, beta-lactamases have never ceased to amaze us with an ever-widening spectrum of structural and functional variants, appearing in increasingly rapid succession in an ever broader range of bacteria . Whereas the phenomenon itself was the predicted outcome of unguarded expansion of beta-lactam therapy, its scope is a testimony to the unique advantage of an otherwise irrelevant, and thus freely modifiable and transmissible, enzyme as a key to survival . 3 . Perhaps the least expected lesson is to be had from the adaptive behaviour of the beta-lactamase molecule itself . Faced with virtually countless structural variations on the beta-lactam theme, nearly all created so as to frustrate its function, the beta-lactamase molecule proves to be so versatile in overcoming so many of its potential inhibitors that it makes us reflect on the evolutionary significance of coping and survival at the molecular level.

Vestn Khir Im I I Grek, 1991 Apr, 146(4), 26 - 8
{Antiviral cellular resistance in acute sepsis}; Tulupov AN et al.; The antiviral cellular resistance was studied in 22 patients with acute sepsis of different etiology . The acute sepsis was found to develop as a rule against the background of substantially decreased antiviral cellular resistance . So, treatment of this category of patients should include not only antibacterial and antimycotic, but also antiviral methods of therapy.

J Chromatogr, 1991 Mar 22, 541(1-2), 393 - 400
Improvement of chemical analysis of antibiotics . XVII . Application of an amino cartridge to the determination of residual sulphonamide antibacterials in meat, fish and egg; Ikai Y et al.; A simple, rapid and reliable method for the determination of residual sulphonamide antibacterials (SAs) (sulphathiazole, sulphisozole, sulphamethoxazole, sulphadiazine, sulphamerazine, sulphadimidine, sulphamonomethoxine, sulphadimethoxine, sulphamethoxypyridazine and sulphaquinoxaline) in meat, fish and egg was developed using a combination of high-performance liquid chromatography (HPLC) and clean-up with an amino-type prepacked cartridge . SAs were extracted with ethyl acetate and applied to a Baker 10 amino cartridge . After elution from the cartridge, SAs were determined by HPLC . The recoveries at the level of 0.5 ppm were 73.7-99.1% and the detection limits were 0.05 ppm . The analysis time per sample was about 45 min.

Chem Pharm Bull (Tokyo), 1991 Mar, 39(3), 672 - 8
Carbapenem and penem antibiotics . VII . Synthesis and antibacterial activity of 1 beta-methyl-2-(quaternary heteroaromatic-thiomethyl) carbapenems; Imuta M et al.; The synthesis and antibacterial activity of a series of 1 beta-methylcarbapenems having quaternary heteroaromatic-thiomethyl groups at the C-2 position are described . Both 2-hydroxymethyl and 2-chloromethyl carbapenems (1 and 7) respectively served as the common key intermediates for the preparation of these compounds . Of these, the 4-pyridiniothiomethyl derivatives exhibited the best antibacterial properties and turned out to possess high in vivo efficacy as well.

Chem Pharm Bull (Tokyo), 1991 Mar, 39(3), 663 - 71
Carbapenem and penem antibiotics . VI . Synthesis and antibacterial activity of 2-heteroaromatic-thiomethyl and 2-carbamoyloxymethyl 1-methylcarbapenems; Imuta M et al.; The synthesis and antibacterial activity of the 1-methylcarbapenems, 2-heteroaromatic-thiomethyl and 2-carbamoyloxymethyl derivatives having a 6-{(R)-1-hydroxyethyl} side chain, are described . The introduction of a methyl substituent at the C-1 position was accomplished by a newly developed procedure using crotyl halides and zinc dust . The 2-hydroxymethyl carbapenems as key intermediates allowed an easy entry into the preparation of title carbapenems.

Chem Pharm Bull (Tokyo), 1991 Mar, 39(3), 658 - 62
Carbapenem and penem antibiotics . V . Synthesis and antibacterial activity of 2-functionalized-methyl 1-methylcarbapenems related to asparenomycins; Imuta M et al.; The synthesis of 1 alpha- and/or 1 beta-methylcarbapenems, 2-unsubstituted and 2-(5-methyl-1,3,4-thiadiazol-2-yl)thiomethyl derivatives having a 1-(hydroxy)methylethylidene or cyclic carbonate side chain at the C-6 position, is described . The in vitro antibacterial activities of these compounds and their corresponding 1-unsubstituted carbapenems are compared.

Chem Pharm Bull (Tokyo), 1991 Mar, 39(3), 555 - 7
Incarnal . A new antibacterial sesquiterpene from Basidiomycetes; Takazawa H et al.; A new sesquiterpene, incarnal, was isolated from culture fluid of Gloeostereum incarnatum (Japanese name: Nikawaurokotake) . Incarnal inhibited the growth of gram-positive bacteria at 6.25-12.5 micrograms/ml . The structure of incarnal has been determined to be (1-hydroxy-2,10,10-trimethyl)-3-methylene- tricyclo{6.3.0.0(2.6)}undec-5,7-diene-4,9-dione by X-ray diffraction and spectroscopic methods.

Urol Nefrol (Mosk), 1991 Mar-Apr, (2), 17 - 21
{The correction of immunodeficiency states in patients with acute suppurative pyelonephritis}; Buglova SE et al.; The analysis of the examination findings of 54 patients with purulent pyelonephritis showed a great variety of immunological changes, which appeared both as differences in the types of abnormal immunity parameters and in the degree of the recorded pathological conditions . T-cell immunity deficiency was revealed in 55.6% of the patients, in a half of whom it was associated with humoral factor deficiency . In 25.9% of the patients the immunograms were similar to those in the controls and in 18.5% they were indicative of humoral immunity activation . Supplement of T-activin to the conventional antibacterial therapy contributed to an early immunological and clinical remission . The immunomodulatory effect was associated with the initial immune deficiency and manifested itself by higher relative and absolute T-lymphocyte contents along with elimination of their subpopulation imbalance . The effect proved to be less profound on the humoral immunity system . The arrest of an inflammatory reaction was evidenced by a decrease in beta-lysine levels in the serum up to normal ones . In contrast, antibacterial therapy without immunomodulation deteriorated the abnormal ratios of immunocompetent cells . The findings suggest that it is essential to take an individual approach to the use of immunomodulating therapy in patients with acute purulent pyelonephritis, taking into account not only clinical but immunological indications . It is most advisable to apply T-activin in cases of T-cell immune deficiencies with a significant imbalance of T-lymphocyte populations.

J Clin Periodontol, 1991 Mar, 18(3), 210 - 2
Effect of glycyrrhizin-containing toothpaste on dental plaque reduction and gingival health in humans . A pilot study; Goultschin J et al.; Glycyrrhizin, the main saponin of licorice, a surfactant producing aqueous gel, was tested for its effect on gingival health, as a supplemental agent in a toothpaste . 40 male and female volunteers brushed their teeth twice daily, with a toothpaste containing 0.25% and 0.50% glycyrrhizin, or a control toothpaste, respectively . All 3 toothpastes contained sodium lauryl sulfate as detergent . The subjects of the 3 groups were examined at days 0, 7, 14, 28, 35 and 42 for plaque, gingival and bleeding indices . The examiner was unaware of subject assignment . None of the brushing regimens with the experimental toothpastes induced significant changes in the examined indices, that were distinct from those observed with the control toothpaste . The decrease (insignificant) in the indices of the study period from 0 to 14 days may be considered as an increased oral hygiene awareness by the subjects examined . Possible explanations for the lack of efficiency in improvement of plaque, gingival and bleeding indices, may have been an insufficient glycyrrhizin concentration and/or chemical incompatibility in a toothpaste containing a mixture of an anionic detergent and an organic antibacterial surface agent.

Pharmacol Toxicol, 1991 Mar, 68(3), 220 - 5
Effects of enoxacin and its combination with 4-biphenylacetate, an active metabolite of fenbufen, on population spikes in rat hippocampal slices; Ito T et al.; The effects of enoxacin, a new quinolone antibacterial agent, and its combination with 4-biphenylacetate (BPA), an active metabolite of the non-steroidal antiinflammatory agent fenbufen, were examined on population spikes induced by electrical stimulation of the stratum radiatum in the CA1 pyramidal cell layer in rat hippocampal slices . Enoxacin (10(-4) M) and bicuculline (10(-6) M) increased the amplitude of the population spikes and anew elicited the second spikes (latency: 10 msec.), while BPA (10(-5) M) decreased the amplitude of the population spikes . However, the combination of enoxacin (10(-6), 10(-5) M) with BPA (10(-5) M) elicited the second spikes or epileptiform bursts with an increase of the population spike amplitude . The dose-response relationships showed that the effect of enoxacin was 100 times potentiated in the presence of BPA (10(-5) M) . The second spikes induced by enoxacin (10(-4) M) were suppressed by muscimol (10(-6) M) and baclofen (10(-6) M), but not by clorazepate (5 x 10(-5) M) and pentobarbital (5 x 10(-5) M) . The second spikes induced by bicuculline (10(-6) M) were suppressed by these four drugs . The second spikes by the combination of enoxacin (10(-6) M) with BPA (10(-5) M) were suppressed by muscimol (5 x 10(-6) M), but not by clorazepate (5 x 10(-5) M) . These results suggest that the combination of enoxacin with BPA exerts a drug interaction to elicit the second spikes or epileptiform bursts with its mode of action different from that of bicuculline.

Pathol Biol (Paris), 1991 Mar, 39(3), 177 - 81
{Effect of intravenous human immunoglobulins on bacterial clearance and mortality in experimental Escherichia coli K 1 septicemia in chicken}; Labarthe JC et al.; The antibacterial effect of intravenous immune globulins (IVIG) was tested in 4 to 6-week-old chickens experimentally infected with a K1 E . coli strain from a neonate with meningitis . Following inoculation of 10(7) E . coli K1 per animal, the chickens were randomized to receive a placebo, 0.25 g/kg, 0,50 g/kg or 1 g/kg of intravenous immune globulins . Injections were performed 4 hours after the bacterial inoculation . Numbers of animals in each group were 30, 19, 30 and 10 for 6-week-old chickens and 9, 10, 9 and 0 for 4-week-old chickens . Bacterial diffusion was evaluated using quantitative cultures of blood from breast capillaries . In the 6-week-old chickens given 0.25 g/kg or 0.50 g/kg of intravenous immune globulins, bacteremia 48 hours after inoculation and mortality were significantly lower than in the placebo group . Administration of intravenous immune globuline in a dose of 1.0 g/kg, however, was followed by increased blood bacteria counts 48 and 72 hours after inoculation . In the 4-week-old chickens, no reduction in bacterial counts or improvement in survival was seen after administration of intravenous immune globulins . These data should provide a basis for a more rational use of intravenous immune globulins in neonates and children.

Infection, 1991 Mar-Apr, 19(2), 64 - 72
Nosocomial pneumonia in children; Jacobs RF; Nosocomial pneumonia continues to be a leading cause of fatal nosocomial infection in the United States . Although there are differences in pathogens by age, the importance of nosocomial pneumonia is apparent in the adult population as well as in the pediatric patient groups . The ability to diagnose these infections utilizing clinical suspicion and microbiologic/rapid diagnostic tests will allow the clinician to effectively treat nosocomial pneumonia in the critically ill patient . Unfortunately, these treatment modalities and preventive measures have not kept pace with our understanding of the pathogenesis of this infection . The pediatric patient population presents several unique and specific infection control, diagnostic and treatment problems for the practicing clinician . The appropriate infection control and isolation policies for specific viral and multiple antibiotic resistant bacterial isolates remains a cornerstone in the prevention of nosocomial pneumonia . The judicious use of empiric antibacterial chemotherapy remains important in the treatment of patients with nosocomial pneumonia . However, in the pediatric patient population the recognition that viral and fungal etiologies are important causes of nosocomial pneumonia challenge the clinician to apply the appropriate diagnostic and effective treatment regimens in pediatric nosocomial pneumonias . The epidemiologic data for the clinician's own institution in regards to etiologic causes of nosocomial pneumonia, drug susceptibility patterns as well as the seasonal and patient distribution of these infections are critical . Nosocomial pneumonia will continue to remain a significant cause of morbidity, mortality, and hospital cost in the United States in the upcoming decades . The advent of new rapid diagnostic testing and improved treatment modalities for effective therapy and prevention will be aided by the advent of immunologic therapy for these disease states.(ABSTRACT TRUNCATED AT 250 WORDS)

Antimicrob Agents Chemother, 1991 Mar, 35(3), 399 - 405
Once-daily aminoglycoside therapy; Gilbert DN; The once-daily administration of aminoglycosides is an attractive concept . In animal experiments and clinical trials, there is either a reduction in or no influence on the risk of toxicity . Less frequent dosing reduces the contact time between host tissue binding sites and drug . Thanks to the PAE and perhaps other as-yet-unrecognized factors, the fall in the level in serum below the MIC does not appear to impair antibacterial efficacy; in fact, the higher peak level in serum may enhance drug efficacy early in a dosage interval . In neutropenic patients, the in vivo PAE may be lost or small-colony variants with a shorter PAE may be selected unless a concomitant beta-lactam is administered . Because it will be some time before data from clinical trials in the United States are available, because the results from the international trials are encouraging, and because there is potential benefit to patients, it seems reasonable for infectious diseases consultants to cautiously initiate the educational process necessary to implement once-daily aminoglycoside therapy in their institutions.

Medicine (Baltimore), 1991 Mar, 70(2), 83 - 90
Lyme disease: clinical features, classification, and epidemiology in the upper midwest; Agger W et al.; Lyme disease can be classified using the terminology of syphilis . In this series of 95 cases from the upper midwest, early cases, defined as an illness of less than 2 months, were more likely to have lived in or recently visited a highly endemic area . Unlike late cases, early cases presented entirely in the nonwinter months (p less than .001) . Early disease was further subdivided into primary and secondary disease . Ninety percent of primary and 43% of secondary cases had erythema migrans, while no late cases had active erythema migrans (p less than .001) . Clinical manifestations of nonspecific inflammation, except for arthralgia, were more common in early than late disease (p less than .01) . In secondary cases, monoarticular arthritis was slightly more common than polyarticular arthritis, with the reverse occurring in late disease (p less than .05) . Indirect fluorescent antibody testing revealed a ratio of IgM to IgG antibodies to be helpful in distinguishing early from late disease . Antibacterial therapy in early, primary cases caused Jarisch-Herxheimer reaction 7% of the time . Despite longer and more frequent parenteral therapy, late Lyme disease frequently required retreatment, owing to poor clinical response (p less than .05).

J Med Chem, 1991 Mar, 34(3), 1155 - 61
Synthesis and biological activity of 5-alkyl-1,7,8-trisubstituted-6-fluoroquinoline-3-carboxylic acids; Hagen SE et al.; A series of 5-alkyl-1,7,8-trisubstituted-6-fluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acids was prepared and evaluated for in vitro and in vivo antibacterial activity . When compared to the 5-hydrogen analogues, the presence of the 5-methyl group enhanced in vitro potency for those compounds containing a cyclopropyl moiety at N1 but decreased potency for those containing an ethyl group at N1 . Replacing the 5-methyl with a 5-ethyl significantly reduced the efficacy . In general, the 5-methyl and 5-hydrogen analogues were equipotent in vivo . Several of the 5-methyl-1-cyclopropylquinolones displayed excellent in vitro and in vivo activity, warranting further development.

J Med Chem, 1991 Mar, 34(3), 1110 - 6
Synthesis and structure-activity relationship of new cephalosporins with amino heterocycles at C-7 . Dependence of the antibacterial spectrum and beta-lactamase stability on the pKa of the C-7 heterocycle; Jung F et al.; Cephalosporins with new aminobenzimidazole and aminoimidazoline heterocycles at C-7 have been synthesized starting with versatile C-7 isocyanide dihalide synthons . The aminobenzimidazoles have a broad spectrum of antibacterial activity, including Gram-positive and Gram-negative organisms, but possess limited beta-lactamase stability . In contrast, the aminoimidazolines have a narrow spectrum of antibacterial activity, limited to Gram-negative strains only, but possess outstanding beta-lactamase stability . Structure-activity relationships are discussed in terms of their dependence on the pKa of the C-7 amino heterocycle, basic C-7 residues giving cephalosporins with exceptional beta-lactamase stability.

J Endod, 1991 Mar, 17(3), 122 - 4
A pilot study of Japanese green tea as a medicament: antibacterial and bactericidal effects; Horiba N et al.; Antibacterial and bactericidal actions of extracts of four kinds of Japanese green tea were tested against 24 bacterial strains isolated from infected root canals . The extracts of all four teas had antibacterial and bactericidal actions against many of the bacteria.

J Nat Prod, 1991 Mar-Apr, 54(2), 416 - 20
Sesquiterpenoids from Brachylaena hutchinsii; Viera PC et al.; The MeOH extract from the bark of Brachylaena hutchinsii yielded two ketoaldehyde sesquiterpenes, 8-ketocopaenal {1} and 8-ketoylangenal {2}, which are also known as brachylaenalones A and B, respectively . In addition to the above-mentioned aldehydes, the corresponding ketoalcohols 8-ketocopaenol {3} and 8-ketoylangenol {4} were also isolated from the same plant, along with a fifth non-ketonic compound, ylangenol {5} . Although the ketoaldehydes 1 and 2 have already been described in the literature, their structures have not been completely established . We describe the isolation, identification, and antibacterial activity of five sesquiterpenes from Bra . hutchinsii and propose new structures for brachylaenalones A and B based on their spectral data.

Zh Mikrobiol Epidemiol Immunobiol, 1991 Mar, (3), 10 - 2
{Tomicide adsorption on bacterial cells}; Butova LG et al.; The capacity of the bacteriocin-like factor of tomicid being adsorbed on microbial cells, depending on the sensitivity of test microorganisms to the preparation, its form and concentration, the duration of the contact of microbial cells with tomicid, the temperature and pH of the incubation medium, was studied . The bacteriocin-like factor of tomicid was found to be capable of nonspecific sorption on microbial cells (in an amount of 64-128 units per mg of dried cell mass) . The decrease of the temperature of the incubation medium to 0 degrees C and its pH to 4.8 and 5.4 inhibited the process of binding this bacteriocin-like factor by microbial cells . The presence of the substance with lysozyme properties in the preparation influenced the process of the adsorption of the main antibacterial component on microbial cells sensitive to lysozyme.

Arzneimittelforschung, 1991 Mar, 41(3), 264 - 6
Synthesis and biological screening of aminothiadiazine dioxides related to trimethoprim; Alkorta I et al.; New derivatives of 3-amino-1,2,6-thiadiazine 1,1-dioxide have been synthesized and their antibacterial, antifungal and DHFR inhibitory activities evaluated . Their chemical structures have been established by means of analytical and NMR spectroscopic data . Among the compounds studied, the 4,4-dibromo derivative 11 showed fungistatic activity against C . albicans.

Xenobiotica, 1991 Mar, 21(3), 309 - 16
The influence of charge transfer complex formation on the antibacterial activity of some tricyclic drugs; Molnar J et al.; 1 . Phenothiazines and structurally related drugs are effective in eliminating bacterial plasmids . 2 . Charge transfer complex formation between chlorpromazine and xanthine dyes with different electron acceptor activities (e.g . fluorescein, eosin, erythrosin and rose bengal) was detected by differential spectrophotometry . Charge transfer complexes were formed between the strong electron acceptor rose bengal and various tricyclic drugs . 3 . On the basis of the wavelength shift, the binding energies of drugs and dyes were estimated . 4 . The temperatures dependence of the reaction indicates charge transfer complex formation rather than a chemical reaction between drugs and dyes . 5 . The anti-plasmid action of the phenothiazines was decreased in the presence of xanthine dyes . As a consequence of competitive inhibition between bacterial binding sites and xanthine dyes, the binding energy of drugs in the plasmid replication system could be determined in the presence of dyes . 6 . Drugs with binding energies in the range of 0.23-2.31 kcal/mol can inactivate the plasmid replication system.

Clin Prev Dent, 1991 Mar-Apr, 13(2), 18 - 22
Taurolin as an oral rinse . II . Effects on in vitro and in vivo plaque regrowth; Reynolds S et al.; A Taurolin solution has been shown previously to possess antibacterial activity, not only by a bactericidal effect but also by reducing bacterial surface adherence . Such mechanisms may contribute to reduction in dental plaque in the mouth, however this remains to be determined . The present study assessed whether a Taurolin rinse could firstly effect bacterial surface growth and, secondly, whether the same rinse could reduce plaque regrowth over a 4-day period . The findings showed that the Taurolin reduced in vitro bacterial surface growth and in vivo plaque regrowth compared to saline, but was not as effective as a chlorhexidine rinse . The findings suggest Taurolin would probably have a moderate effect on plaque and gingivitis in longer-term use.

Stomatologiia (Mosk), 1991 Mar-Apr, (2), 53 - 4
{The prevention of inflammatory complications from uranoplasty by using the baliz-2 preparation}; Avakimian MA et al.; Baliz-2, a new antibacterial drug, was used to prevent nasopharyngeal infection before and after uranoplasty in 25 children with palatal clefts . Sanitation effect of the drug was revealed; the incidence of postoperative inflammatory complications was reduced.

J Med Chem, 1991 Mar, 34(3), 1142 - 54
Synthesis and biological activity of 5-amino- and 5-hydroxyquinolones, and the overwhelming influence of the remote N1-substituent in determining the structure-activity relationship; Domagala JM et al.; A series of 5-amino- and 5-hydroxyquinolone antibacterials substituted at C7 with a select group of common piperazinyl and 3-aminopyrrolidinyl side chains was prepared . These 5-substituted derivatives were compared to the analogous 5-hydrogen compounds for antiinfective activity by using DNA gyrase inhibition, minimum inhibitory concentrations against a variety of bacteria, and in vivo efficacy in the mouse infection model . The influence on the structure-activity relationships of varied substituents at C8 (H, F, Cl) and N1 (ethyl, cyclopropyl, difluorophenyl) was also studied . The results showed that several of the structure-activity conclusions regarding side-chain bulk at C7, the effect of halogen at C8, and the effect of the C5-amino group were greatly influenced by the choice of the N1-substituent . Several outstanding broad spectrum quinolones were identified in this work . In particular, the spectrum and potency of the 7-piperazinyl quinolones could be greatly enhanced by the judicious choice of C5-, C8-, and N1-substituents.

Drug Metab Dispos, 1991 Mar-Apr, 19(2), 376 - 80
Stereoselective glucuronidation of ofloxacin in rat liver microsomes; Okazaki O et al.; The stereoselective glucuronidation of ofloxacin {(+/-)-OFLX}, a new quinolone antibacterial agent, was studied in vitro using rat liver microsomes . OFLX glucuronidation exhibited Michaelis-Menten kinetics in rat liver microsomes . Stereoselective glucuronidation of the optical enantiomers occurred . S-(-)-OFLX glucuronide was produced 7-fold more than R-(+)-OFLX glucuronide with little or no difference in the values of KM of the enantiomers . The value of Vmax/KM for the glucuronide conjugate of S-(-)-OFLX was 8-fold greater than for the conjugate of R-(+)-OFLX . These results demonstrate that OFLX undergoes stereoselective glucuronidation in vitro . Moreover, we studied the in vivo interaction between enantiomers of OFLX in rats to clarify the effects of R-(+)-OFLX on the metabolism and disposition of S-(-)-OFLX . When the racemate {(+/-)-OFLX (20 mg/kg)} or single enantiomer {S-(-)-OFLX (10 mg/kg)} is administered iv to the rat, the serum concentrations of S-(-)-OFLX were higher after racemate administration than those after enantiomer administration, although the dose of S-(-)-OFLX was identical in both cases . These results indicate that R-(+)-OFLX may compete with S-(-)-OFLX in the in vivo glucuronidation . Furthermore, the results of the enantiomeric inhibition study showed that R-(+)-OFLX competitively inhibited S-(-)-OFLX glucuronidation in vitro with a Ki value of 2.92 mM.

J Hosp Infect, 1991 Mar, 17(3), 197 - 206
Non-toxic antiseptic irrigation with chlorhexidine in experimental revascularization in the rat; Severyns AM et al.; The effect of different wound irrigation fluids upon femoral arteries and veins was investigated in the rat, using microsurgical techniques . Toxicity was evaluated by microscopical observation after selective staining of histological slides . Povidone-iodine, 10%, proved to be a very irritant solution, provoking an attack on the vascular endothelium and secondary thrombosis . Chlorhexidine at 0.05%, 0.02% and 0.001% was found by contrast to have a very low toxicity which was comparable to physiological saline . Experimental investigation of antiseptic solutions should not only include the determination of the antibacterial effect, but also the potential for cell toxicity, using an irrigation technique.

J Clin Lab Immunol, 1991 Mar, 34(3), 141 - 4
Immunoglobulin profiles and antibacterial antibody levels in hairy cell leukaemia; Demeter J et al.; Serum immunoglobulin and natural antibody concentrations to environmental antigens have been determined in 26 hairy cell leukaemia (HCL) patients . The serum IgG, IgA and IgM levels as well as the concentration of antibodies to the majority of intestinal bacteria were found to be normal in both groups of HCL patients . In contrast to the data on the impaired humoral immunity of chronic lymphocytic leukaemia (CLL) patients, our results show that in HCL the studied aspects of humoral immunity are normal . Serum IgE levels were found to be significantly decreased in HCL when all patients were taken as a group . The difference was due to the decreased serum IgE concentration of splenectomized HCL patients, while IgE levels of untreated HCL patients did not differ statistically from that of the healthy controls.

Vestn Khir Im I I Grek, 1991 Mar, 146(3), 113 - 5
{Selection of surgical tactics in infected vascular transplants}; Zatevakhin II et al.; The article analyzes a 10-years experience of the clinic work with choice of surgical tactics in infecting vascular transplants after reconstructive operations on the aorta and arteries of lower extremities in 57 of 1079 patients operated upon . The active-waiting tactics using conservative antibacterial methods of treatment was unsuccessful since in 89.7% of cases it resulted in the development of erosive bleedings and in 62.8%--in lethal issues . Preventive reoperations (atypical shunting included) before the development of erosive bleeding in infected vascular transplants reduced the frequency of amputations from 46.2% to 26.6% (in the discharged patients), and reduced lethality almost 4 times (from 62.8% to 16.7%).

Antibiot Khimioter, 1991 Mar, 36(3), 15 - 7
{Early identification of streptothricin group antibiotics}; Terekhova LP et al.; Methodical approaches to detecting cultures producing streptothricins at the early stages of screening new antibiotics were developed . The approaches are based on chromatographic and electrophoretic mobility of streptothricins and the products of their hydrolysis in the extracts from agar cultures of actinomycetes . Application of the method for screening new antibiotics is illustrated with an example . Nine strains of actinomyces with broad antibacterial spectra isolated from soil samples were studied and 6 of them belonging to 4 species were shown to produce streptothricins in agar cultures . The new streptothricin-producing culture S . roseolilacinus was isolated.

Chem Pharm Bull (Tokyo), 1991 Mar, 39(3), 545 - 8
Mechanism of decomposition of cyclic peroxides, 4-alkoxy-1,4-dihydro-2,3-benzodioxin-1-ols, to afford hydroxyl radical; Matsugo S et al.; The decomposition of 4-alkoxy-1,4-dihydro-2,3-benzodioxin-1-ols (1, Bd) in aqueous media was examined . Increasing the water content of the medium accelerated the decomposition of 1 and increased the formation of the corresponding 2-formyl benzoic acid ester (2) as the decomposition product . Electron spin resonance (ESR) studies using dimethylpyrroline N-oxide (DMPO) as a spin trapping reagent had revealed that hydroxyl radicals are formed during the decomposition of 1 (Matsugo et al., FEBS Lett., 184, 25 (1985)) . Thus, water-mediated decomposition of 1 was suggested to occur, affording the ester 2 and hydroxyl radical . Direct involvement of water was confirmed by an 18O isotopic tracer experiment which revealed that 18O was incorporated exclusively into the formyl position of the ester 2 . It is plausible that a hydrated hydroperoxide (5) is formed by the addition of water at the formyl position of the ring-opened structure of 1 at the initial stage of the decomposition of 1 . Preliminary studies on the antibacterial activities of 1 showed moderate cell-killing activity, especially to Pseudomonas strains, and the activity was found to be related to the decomposition of 1.

Pathol Biol (Paris), 1991 Mar, 39(3), 230 - 9
{TNF: antitumoral agent at the border lines of immunity and inflammation}; Branellec D et al.; Tumor Necrosis Factor-alpha (TNF) is mainly produced by activated monocytes and exerts pleiotropic biological effects on a wide variety of both normal and transformed cells . Originally described for its capacity to induce hemorrhagic necrosis of transplantable tumors in vivo and cytolysis of some tumor cells in vitro, TNF has also been shown to play an essential role during the inflammatory response, exerting dual, both beneficial and deleterious, effects . TNF, via a local production appears to be a key cytokine involved in antiviral, antibacterial and antiparasitic host defense mechanisms . Contreversely, deregulation of the inflammatory and immune reactions can be associated with a systemic TNF production, leading to toxic secondary effects . Recent cloning of the TNF receptors has provided additional insights in the complex physiology of TNF . It is now clearly established that both type I and type II TNF receptors can be cleaved and released as TNF binding proteins . The soluble fragments of TNF receptors can inhibit TNF-mediated tumor cell lysis in vitro and might therefore serve as regulators of TNF action . The antitumor potency of TNF also reflects the pleiotropic aspect of TNF . TNF-induced tumor regression, observed in various preclinical studies, appears to result from at least three distinct biological effects: mainly hemorrhagic necrosis via TNF action on tumor endothelium, TNF immunomodulatory activity on immune effector cells, and presumably a direct TNF-mediated cytotoxic effect against tumor cells . From the clinical trials performed with distinct recombinant materials a consensus has emerged about the disappopinting anticancer efficacy of TNF used in systemic administration . Further studies, aimed at better understanding the complex action of TNF, are required to possibly enhance its therapeutic index and subsequently to assess whether TNF still remains a promising therapeutic agent.

Antimicrob Agents Chemother, 1991 Mar, 35(3), 448 - 50
Ciprofloxacin-induced inhibition of topoisomerase II in human lymphoblastoid cells; Bredberg A et al.; The antibacterial activities of the fluorinated 4-quinolones (e.g., ciprofloxacin) have been ascribed to a marked inhibition of bacterial DNA gyrase . In contrast, the influence on purified mammalian DNA enzymes, including topoisomerases, has been reported to be several orders of magnitude weaker, occurring at concentrations higher than 100 micrograms of ciprofloxacin per ml . In this study, using a nondenaturing filter elution method, a marked induction of double-strand DNA breaks in human lymphoblastoid cells exposed to 80 micrograms of ciprofloxacin per ml was seen . The proportion of single-strand versus double-strand DNA breaks was similar to that seen with the topoisomerase II inhibitory antitumor agent VP-16 . The cellular recovery was more rapid after treatment with ciprofloxacin than after treatment with VP-16, displaying a normal elution profile within 15 min at 37 degrees C (60 min for VP-16) . These data indicate that ciprofloxacin has an effect on intracellularly located topoisomerase II in humans.

J Biol Chem, 1991 Feb 15, 266(5), 2753 - 8
Membrane interactions of amphiphilic polypeptides mastoparan, melittin, polymyxin B, and cardiotoxin . Differential inhibition of protein kinase C, Ca2+/calmodulin-dependent protein kinase II and synaptosomal membrane Na,K-ATPase, and Na+ pump and differentiation of HL60 cells; Raynor RL et al.; Interactions of certain naturally occurring, amphiphilic polypeptides with membranes were investigated . Mastoparan (wasp venom toxin), melittin (bee venom toxin), cardiotoxin (cobra venom toxin), and polymyxin B (antibacterial antibiotic) inhibited protein kinase C stimulated by phosphatidylserine bilayer or arachidonate monomer and blocked binding of {3H} phorbol 12,13-dibutyrate to protein kinase C in the presence of phosphatidylserine bilayer, with IC50 values (concentrations causing 50% inhibition) of 1-8 microM . Mastoparan and polymyxin B were much less inhibitory (IC50, 10-20 microM), whereas melittin and cardiotoxin were similarly inhibitory (IC50, 1-4 microM), when protein kinase C was activated instead by synaptosomal membrane . Kinetic analysis indicate that mastoparan inhibited protein kinase C, assayed using phosphatidylserine or synaptosomal membrane as the phospholipid cofactor, competitively with the phospholipid cofactor, in a mixed manner with CaCl2 or diacylglycerol, noncompetitively with histone, and uncompetitively with ATP, with apparent Ki values of 1.6-18.7 microM . Inhibition of Na,K-ATPase in the membrane by these polypeptides had relative potencies different from those for their inhibition of protein kinase C activated by the same membrane preparation; mastoparan and melittin inhibited the two activities with comparable potencies, but polymyxin B and cardiotoxin were far less effective in inhibiting Na,K-ATPase . The same relative inhibitory potencies of the polypeptides (melittin greater than mastoparan greater than polymyxin B) for inhibition of Na,K-ATPase were also noted for their inhibition of Ca2+/calmodulin-dependent protein kinase II, 86Rb uptake (Na+ pump) by HL60 cells and the phorbol ester-induced differentiation of the leukemia cells . These findings were consistent with discrete interactions of the polypeptides with functionally distinct sites on the membrane, leading to differential inhibition of biological activities associated with the membrane . Actions of certain polypeptides appeared to be more specific compared to those of lipid second messengers such as lyso-phosphatidylcholine and sphingosine, and the antineoplastic ether lipid analogs such as 1-O-octadecyl-2-methyl-rac-glycero-3-ophosphocholine.

J Antibiot (Tokyo), 1991 Feb, 44(2), 200 - 9
Synthesis and antibacterial activity of new C-10 quinolonyl-cephem esters; Demuth TP Jr et al.; A series of cephalosporins derived from cephalothin containing an ester-linked quinolonyl substituent at the C-10 position (C-10 quinolonyl-cephem esters) has been prepared and evaluated for in vitro antibacterial activity . The C-10 quinolonyl-cephem esters exhibited a broadened spectrum of activity when compared with cephalothin and the corresponding quinolones, including activity against beta-lactamase-producing bacteria.

Vrach Delo, 1991 Feb, (2), 48 - 51
{The treatment with the polypeptide preparation "Prostatilen" of patients with prostatitis complicated by a sexual functional disorder}; Gorpinchenko II et al.; Results are reported of clinical trials of a drug obtained from the prostate of cattle . Prostatilen possesses an anti-inflammatory, antibacterial, immunomodulating effect, improves urination, stimulates the copulative and generative functions . Prostatilen is recommended for serial production and use in medical practice.

Chem Pharm Bull (Tokyo), 1991 Feb, 39(2), 255 - 9
Studies on glycosylation of the mitomycins . Syntheses of 7-N-(4-O-glycosylphenyl)-9a-methoxymitosanes; Furuhata K et al.; Two new derivatives of glycosyl mitomycin C, 7-N-{4-O-(beta-D-glucopyranosyl and alpha-sialosyl)phenyl}-9a- methoxymitosanes, were synthesized, and their structures were elucidated by analysis of the nuclear magnetic resonance spectra . Field desorption mass spectrometry was successfully used for the confirmation of these structures . The cytotoxic, antibacterial, and antitumor activities of 7-N-(4-glycosylphenyl)-9a- methoxymitosanes were also examined.

Khirurgiia (Mosk), 1991 Feb, (2), 27 - 30
{Intralymphatic antibacterial therapy of acute cholecystitis}; Buianov VM et al.; Clinical examination of 34 patients showed that lymphotropic administration of antibiotics creates concentrations in organs and tissues involved in the inflammatory process in acute cholecystitis which are 1.63-14.95 times higher than those produced by intramuscular injection . Study of the course of the clinical picture of the disease in 122 patients with acute destructive cholecystitis revealed the high efficacy of this method of antibiotic therapy: the laboratory indices of the inflammation became normal within a shorter period of time, the inflammatory process in the gallbladder was arrested more rapidly, the number of postoperative complications fell 2.6 times, and the terms of hospital-stay of the patients reduced by 1.3 times . Lymphotropic antibiotic therapy is more pathogenetic in the management of acute destructive cholecystitis.

Antibiot Khimioter, 1991 Feb, 36(2), 34 - 6
{Evaluation of the effectiveness of antibacterial therapy}; Dmitrieva NV et al.; It is recommended to estimate the clinical effect of antibacterial therapy in patients with different purulent inflammatory complications with an account of the data on both the clinical and bacteriological examinations . The full affect consisted in disappearance of the clinical signs and complete bacteriological sanation of the purulent inflammatory foci . The partial effect was shown by a marked decrease in the clinical manifestations without complete bacteriological sanation of the foci . The ill effect was evidenced by clinical picture having no time course and no favourable time course in bacteriological tests . No effect was indicated by deterioration of the clinical picture and no favourable time course in the bacteriological tests.

J Dent, 1991 Feb, 19(1), 3 - 13
Calcium hydroxide in restorative dentistry; Milosevic A; This paper reviews the various calcium hydroxide preparations available for use in restorative dentistry and their constituents . The significance of individual constituents in relation to the properties of such materials and their mode of therapeutic action with respect to the dentine pulpal response and antibacterial activity is discussed . Applications of calcium hydroxide in restorative dentistry are also reviewed.

J Chromatogr, 1991 Feb 1, 538(2), 484 - 91
Simultaneous determination of residual synthetic antibacterials in fish by high-performance liquid chromatography; Horie M et al.; A simple and rapid high-performance liquid chromatographic (HPLC) method for the simultaneous determination of sulphamonomethoxine (SMMX), sulphadimethoxine (SDMX), sulphisozole (SIZ), nalidixic acid (NA), oxolinic acid (OXA), piromidic acid (PMA), furazolidone (FZ) and sodium nifurstyrenate (NFSA) in cultured fish was developed . The drugs were extracted with 0.2% metaphosphoric acid-methanol (6:4), followed by a Bond Elut C18 clean-up procedure . The HPLC separation was carried out on an Inertsil ODS column (150 x 4.6 mm I.D.) using 5 mM aqueous oxalic acid-acetonitrile (55:45) as the mobile phase with detection at 265 nm (0.04 a.u.f.s.) . The calibration graphs were rectilinear from 1 to 20 ng for OXA, from 2 to 50 ng for SMMX, SDMX, SIZ, NA, PMA and FZ and from 5 to 100 ng for NFSA . The recoveries of each drug added to fish were 65.0-89.5% . The detection limits were 0.02 micrograms/g for OXA, 0.05 micrograms/g for SMMX, SDMX, SIZ, NA, PMA and FZ and 0.1 micrograms/g for NFSA.

J Med Chem, 1991 Feb, 34(2), 656 - 63
Quinolone antibacterials: preparation and activity of bridged bicyclic analogues of the C7-piperazine; Kiely JS et al.; A series of quinolone and naphthyridine antibacterial agents possessing as the C7-heterocycle bicyclic 2,5-diazabicyclo{n.2.m}alkanes, where n = 2, 3 and m = 1, 2, and a series including 4-aminopiperidine and 3-amino-8-azabicyclo{3.2.1}octanes have been prepared and evaluated in vitro and in vivo for antibacterial activity against a variety of Gram-negative and Gram-positive organisms . These compounds were also tested against the target enzyme bacterial DNA gyrase . All the examples investigated are nearly equipotent with the parent 7-piperazinyl analogues . Only endo-7-(3-amino-8-azabicyclo{3.2.1}oct-8-yl)-1-cyclopropyl-6,8-difluoro- 1,4- dihydro-4-oxo-3-quinolinecarboxylic acid displays activity that surpasses that of the piperazine parent.

J Med Chem, 1991 Feb, 34(2), 550 - 5
2,4-Diamino-5-benzylpyrimidines as antibacterial agents . 14 . 2,3-Dihydro-1-(2,4-diamino-5-pyrimidyl)-1H-indenes as conformationally restricted analogues of trimethoprim; Chan JH et al.; A conformationally restricted analogue of trimethoprim (1a) has been prepared by connecting the ortho position of the benzene ring to the methylene linkage with two methylene groups, thus forming a dihydroindene derivative (2b) . The chemistry involved the condensation of barbituric acid with an indanone derivative, followed by a three-step conversion to a 2,4-diaminopyrimidine . The S isomer of 2b was found to have a minimum-energy conformation very similar to that of 1a when bound to Escherichia coli dihydrofolate reductase, in contrast to that of 1a in vertebrate DHFR . Theoretically such a derivative might have increased specificity and activity against the bacterial enzyme . Molecular modeling experiments suggested that the actual decreased activity was due to crowding in the enzyme, caused by the extra atoms needed to restrict the conformation.

J Dent Res, 1991 Feb, 70(2), 107 - 10
Activation of complement by Treponema denticola; Schenkein HA et al.; Oral spirochetes have been shown to be associated with periodontal diseases and are present in increased numbers in lesions of greater severity . In this study, the interaction of Treponema denticola with human complement, a major antibacterial defense system, was examined . For each of two strains of T . denticola, it was found that both the classical and alternative pathways of human complement were activated in human serum upon incubation at 37 degrees C . C3 fragments were deposited on the surface of this organism following complement activation; the fragments bound included both of the major C3-derived opsonic fragments C3b and iC3b . Under incubation conditions identical to those carried out for complement activation in serum, T . denticola failed to degrade purified, hemolytically-active C3, although it readily degraded inactivated C3 . Thus, despite the documented proteolytic activity of this organism, complement activation and deposition of complement-derived opsonins may be important defense mechanisms in the control of infections with T . denticola.

Arch Pharm (Weinheim), 1991 Feb, 324(2), 121 - 7
Imidazo{4,5-b}pyridine derivatives of potential tuberculostatic activity . Part 1: Synthesis and quantitative structure-activity relationships; Bukowski L et al.; New derivatives of imidazo{4,5-b}pyridine and 9H-dipyrido-{1,2-a:3',2'-d}imidazole were synthesized . Antibacterial activity against Mycobacterium tuberculosis of selected compounds was determined . These data were combined with the corresponding bioactivity data previously generated for two other series of imidazo{4,5-b}pyridines . Analysis of Quantitative Structure-Activity Relationships {QSAR} was carried out using nonempirical structural descriptors . Hydrophobicity of the agents studied was found decisive for their activity . A QSAR equation was derived allowing rational design of active derivatives.

J Pediatr, 1991 Feb, 118(2), 178 - 83
Host factors and early therapeutic response in acute otitis media; Carlin SA et al.; To evaluate the relationship between eradication of bacterial infection and clinical improvement in children with otitis media, we reviewed the clinical outcome of bacterial otitis media in patients enrolled in double-blind trials of antibacterial therapy from 1979 to 1988 . Cultures of middle ear exudates showed the distribution of bacterial pathogens to be similar to that observed in other geographic areas . Two hundred ninety-three patients had otitis media caused by bacterial pathogens and underwent repeat tympanocentesis after 3 to 6 days of therapy . Bacteriologic success was demonstrated in 253 patients (86%); 40 patients (14%) had bacteriologic failure . Children who had bacteriologic failure were younger than those with bacteriologic success (median age 10.6 vs 18.5 months; p = 0.001); 38% of patients who had bacteriologic failure were black, compared with 18% of patients with bacteriologic success (p = 0.007) . Gender, history of frequent otitis media, and presence of bilateral otitis media were not risk factors for bacteriologic failure . Clinical success was demonstrated in 261 patients (89%); 32 patients (11%) had clinical failure . Agreement between clinical and bacteriologic response was 86% (95% confidence interval: 81.6% to 89.6%) . Ninety-three percent (236/253) of subjects whose infection was eliminated had clinical resolution, whereas 37% (15/40) of those with bacteriologic failure had persisting symptoms or signs of clinical failure . We conclude that failure to eliminate bacteria from the middle ear is often associated with persistent signs and symptoms . Bacteriologic failure affects children less than 18 months of age almost exclusively . Bacteriologic and clinical failure are frequently discordant; mechanisms unrelated to the bacterial infection may explain some of the persisting clinical signs.

Ann Trop Med Parasitol, 1991 Feb, 85(1), 149 - 63
Mosquito host influences on development of filariae; Townson H et al.; A brief review is presented of the literature relating to factors which limit the capacity of filariae to develop in mosquitoes, with particular emphasis on immune mechanisms . Most insects respond to bacterial infection by the production of potent antibacterial proteins, but little is known of this aspect of the immune response in mosquitoes or of the possible influence of immune proteins on the fate of filarial infections in mosquitoes . A summary account is given of recent experiments with the mosquito Aedes aegypti which involve passive transfer of immune haemolymph together with its in vitro assay and SDS-PAGE examination for induced proteins . These experiments demonstrate the production, in response to inoculation with Brugia pahangi, Escherichia coli, and various components of microbial cell walls, of haemolymph factors which are protective against filarial infection . It remains to be seen whether mosquitoes can produce a specific protective response to infection with eukaryotic organisms such as filaria that is distinctive from that mobilized against bacteria.

J Clin Pathol, 1991 Feb, 44(2), 157 - 9
Harnessing of urease activity of Helicobacter pylori to induce self-destruction of the bacterium; Greig MA et al.; Eradication of Helicobacter pylori with currently available antibacterial agents is unsatisfactory due to the risk of side-effects and the emergence of resistance . The organism rapidly dies in vitro in the presence of urea at pH 6 . When incubated in citrate buffer (pH 6) plus urea (10 mM) the five minute survival was 26% compared with 96% without urea and the survival progressively decreased with increasing urea concentrations, being only 9% in 50 mM urea . The bactericidal effect depended on pH as the organism survived in citrate buffer (pH 7) plus urea (50 mM) . The death of the organism at pH 6 in the presence of urea was prevented by the addition of the competitive urease inhibitor hydroxyurea . These findings indicate that destruction of the organism is mediated by its exceptionally high urease activity . Harnessing this enzyme to induce self-destruction could provide a new approach to eradicating this common infection.

J Med Chem, 1991 Feb, 34(2), 669 - 75
Dual-action cephalosporins: cephalosporin 3'-quaternary ammonium quinolones; Albrecht HA et al.; When cephalosporins exert their biological activity by reacting with bacterial enzymes, opening of the beta-lactam ring can lead to expulsion of the 3'-substituent . A series of cephalosporins was prepared in which antibacterial quinolones were linked to the 3'-position through a quaternary nitrogen . Like the 3'-ester-linked dual-action cephalosporins reported earlier, these compounds demonstrated a broad spectrum of antibacterial activity derived from cephalosporin-like and quinolone-like components, suggesting a dual mode of action.

Eur J Surg, 1991 Feb, 157(2), 97 - 101
Effect of topical zinc oxide on bacterial growth and inflammation in full-thickness skin wounds in normal and diabetic rats; Agren MS et al.; The effects of topical zinc oxide on bacterial growth and inflammation were studied in full-thickness excised cutaneous wounds in normal rats and in hyperglycemic alloxan-diabetic rats . Two concentrations of zinc oxide in a gauze compress (15 or 60 mg/g) were applied to the wounds of the normal rats, but only the higher concentration was used for the diabetic rats . The polymorphonuclear leukocyte count, the alkaline phosphatase activity and bacterial counts in the granulation tissue were recorded on postoperative day 4 . In the normal rats there was no significant intergroup difference in polymorphonuclear leukocyte density, though alkaline phosphatase activity was significantly depressed in those treated with the higher zinc oxide concentration . Bacterial growth in granulation tissue decreased at both zinc oxide concentrations . None of these effects was found in the diabetic rats . The results indicate that hyperglycemic diabetic rats respond differently to local zinc oxide treatment than do normal rats, and that the antibacterial activity of zinc oxide in vivo is not solely due to a direct toxic effect on the bacteria.

Acta Crystallogr C, 1991 Jan 15, 47 ( Pt 1), 112 - 5
Structure of 4-(3-chlorophenyl)thiosemicarbazide; Chattopadhyay D et al.; C7H8ClN3S, Mr = 201.67, monoclinic, P21/c, a = 6.914 (5), b = 4.304 (4), c = 30.306 (3) A, beta = 94.66 (3) degrees, V = 899.0 (1) A3, Z = 4, Dm = 1.54, Dx = 1.490 Mg m-3, lambda (Cu K alpha) = 1.5418 A, mu = 5.54 mm-1, F(000) = 416, T = 298 K, final R = 0.048 for 1219 observed reflections . The S and terminal hydrazinic N atoms are in a trans conformation . As a result of the sigma-electron-withdrawing effect of the Cl atom at the meta position in the phenyl ring with respect to the thiosemicarbazide chain, the net negative charge on the terminal N atom decreases compared to the p-chloro and p-methoxy derivatives . The antibacterial activity of the compound is also lowered.

Cancer Res, 1991 Jan 15, 51(2), 510 - 3
A phase I clinical trial of novobiocin, a modulator of alkylating agent cytotoxicity; Eder JP et al.; Antineoplastic drug resistance is a major obstacle to improved treatment of most adult cancers in humans . Novobiocin, an antibacterial agent which inhibits the eukaryotic topoisomerase II enzyme, increases the cytotoxicity of several alkylating agents in vitro by the formation of lethal DNA-DNA interstrand cross-links, perhaps by decreasing the repair of drug monoadducts . In murine tumors treated in vivo novobiocin markedly potentiates alkylating agent cytotoxicity without concomitant increases in host toxicity . With this background, a Phase I trial of novobiocin and cyclophosphamide was performed in refractory cancer patients . Novobiocin was given p.o . for 96 h; 750 mg/m2 of i.v . cyclophosphamide was administered at 48 h . Thirty-four patients received 65 courses . The dose-limiting toxicity of novobiocin in this trial was vomiting . The maximum tolerated dose was 6 g/day . Six of 34 patients had Grade III or IV mylosuppression but no dose escalation effect was noted . Three patients developed allergic reactions which resolved completely . No other significant toxicity occurred . While no dose-dependent effect on serum novobiocin levels occurred, 18 of 19 patients treated at greater than or equal to 4 g daily had serum levels greater than or equal to 100 micrograms/ml at steady state, a level which corresponds to levels used in vitro and seen in vivo where the murine novobiocin half-life of 82 min is far less than that seen in humans (6.0 h) . Two of 30 evaluable patients had partial responses . Four other patients had stable disease . Four of six had prior disease progression on cyclophosphamide combination therapy . Novobiocin is well tolerated in patients receiving cyclophosphamide and blood levels are in the drug-potentiating range . Phase II trials in cyclophosphamide refractory patients are anticipated.

Clin Ter, 1991 Jan 15, 136(1), 53 - 61
{Bacterial infections . Progress and new prospects in chemo-antibiotic therapy}; Olivieri A et al.; During the last 10 years, a very large number of molecules with antibacterial activity has been developed by pharmaceutic industry . The principal objectives of pharmacological research are to obtain ever wider spectra of activity and increased antibacterial action in order to combat "emerging" agents and those resistant to traditional treatment, as well as longer acting drugs so as to improve patient compliance . These objectives might be attained by the molecules now in the phase of clinical trial, especially by the new injectable or oral cephalosporins and new fluoroquinolones.

J Biol Chem, 1991 Jan 5, 266(1), 112 - 6
Human lysosomal cathepsin G and granzyme B share a functionally conserved broad spectrum antibacterial peptide; Shafer WM et al.; Human neutrophil lysosomal cathepsin G (cat G) exerts broad-spectrum antibacterial action in vitro against Gram-negative and -positive bacteria independent of its serine protease activity . We recently determined that an internal peptide of cat G (HPQYNQR), obtained after digestion of cat G with clostripain, possessed broad-spectrum antibacterial action in vitro, displaying an ED50 of 5 x 10(-5) M . In order to evaluate the structure-antibacterial properties of this peptide, synthetic variants with single alanine substitutions at each position were prepared and tested for antibacterial action . We found that alanine substitution for His-1 or Tyr-4, or certain modifications of the His-1 side chain, produced nonbactericidal peptides . A hexapeptide lacking the COOH-terminal Arg-7 but not a pentapeptide lacking both Gln-6 and Arg-7 possessed in vitro bactericidal activity . Interestingly, the cat G bactericidal peptide displays similarity to sequences within other serine proteases, notably the proposed cytotoxic granzymes present in the cytolytic granules of human and mouse cytotoxic T lymphocytes . We now report that an internal peptide of one human granzyme (granzyme B) with the sequence of HPAYNPK also displays bactericidal action in vitro . Our results suggest that an internal antibacterial domain among human serine proteases cat G and granzyme B has been functionally conserved through evolution perhaps for the purpose of host defense against microbial pathogens and targets of cytotoxic T lymphocyte killing.

Pediatriia, 1991, (4), 35 - 8
{Criteria of chronic state and treatment effectiveness of acute glomerulonephritis without nephrotic syndrome in children}; Sitnikova VP et al.; A study was made of criteria for acute glomerulonephritis chronicity, efficacy of etiotrophic therapy, and of the survival rates in a group of 200 ill children . It has been established that proteinuria ranging within 0.1-0.99 g/l, no arterial hypertension at the disease debut, concomitant urodynamic disorders are of unfavourable prognostic significance for the clinical recovery . A relationship has been discovered between glomerulonephritis chronicity and the patients' sex and age, and preceding diseases . A conclusion is made about the highest efficacy of antibacterial therapy commenced at the first week of the disease, continued for one month . The patients' survival rate for 20 years amounted to 100%.

Klin Khir, 1991, (1), 40 - 3
{Tactics for treating multiple liver abscesses formed after creation of a biliodigestive anastomosis}; Shalimov SA et al.; The authors treated 18 patients with multiple cholangiogenic hepatic abscesses, which developed after creation of the biliodigestive anastomoses due to digestive-biliary reflux with prolonged retention of food masses in the bile ducts, duodenostasis and stenosing of the anastomosis . Puncture of the abscesses under guidance of sonography in combination with complex antibacterial therapy, timely correction of digestive-biliary reflux contributed to achieving the satisfactory result of treatment.

Yakugaku Zasshi, 1991 Jan, 111(1), 19 - 31
{Studies on ouinolone antibiotics . II . Synthesis and antibacterial activity of 7-aminoalkoxy-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxoquinoline-3 -carbo xylic acids and their derivatives}; Yoshida T et al.; 7-Aminoalkoxy-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxoquinoline-3- carboxylic acid and their derivatives were synthesized and their antibacterial activities were evaluated . Among them, compounds having an alkyl group at alpha-position of the amino group were found to have in vitro and in vivo antibacterial activity comparable to that of ciprofloxacin . Structure-activity relationship of these compounds was also stated.

Antibiot Khimioter, 1991 Jan, 36(1), 20 - 2
{Optimal combined use of rifampicin and immunomodulator of microbial origin in experimental Q-Rickettsia infection}; Nikitin AV et al.; Multifactorial analysis of the combined use of rifampicin and an immunomodulator of the microbial origin, such as peptidoglycan, was performed on a model of experimental Q fever in albino mice . On the basis of the experimental results, statistic polynomial models describing the weight of the murine spleens and the titers of the complement-binding antibodies were designed . It was shown that the action of the immunomodulator and antibiotic was highly synergistic with respect to the chemotherapeutic activity and antibody titers . The preventive use of the immunomodulator yielded a 30-fold decrease in a rifampicin therapeutic dose . The use of the immunomodulator also provided a pronounced immunomodulating effect with respect to humoral immunity . Nomographs for optimizing the dose-time parameters of the antibacterial and immunomodulating therapy were plotted.

Antibiot Khimioter, 1991 Jan, 36(1), 14 - 6
{Sensitivity of Pseudomonas to currently used antibacterial drugs}; Antonov IuV et al.; Sensitivity of 184 strains of four Preudomonas species that are of importance from the medical viewpoint was studied . It was shown that all the studied strains were resistant to cefazolin and ampicillin . Sulfomonomethoxine was active only against P . mallei . Gentamicin inhibited the growth of all the strains of P . mallei and 60 per cent of the strains of P . aeruginosa . Among the four studied strains, the causative agent of glanders was the least resistant to the chemotherapeutic drugs . Eleven out of the 16 studied drugs were active against P . mallei . The strains of P . pseudomallei, the organism causing melioidosis were sensitive to 6 drugs: ceftazidime, imipenem, doxycycline, minocycline, chloramphenicol and biseptol . The dime, ceftriaxone, cefsulodin, cefoperazone, cefotaxime, piperacillin and imipenem . The strains of P . cepacia were the most resistant to all the chemotherapeutic drugs studied and only biseptol was active in the concentrations attained in blood of patients (MIC50 12.5 mg/l) . 10 to 70 per cent of the strains were sensitive to ceftazidime, imipenem, doxycycline, minocycline and rifampicin . Therefore, imipenem and ceftazidime were the most active drugs with respect to the causative agents of pseudomonoses . Biseptol, doxycycline and minocycline are also worthy note.

Scand J Plast Reconstr Surg Hand Surg, 1991, 25(1), 19 - 24
Antibacterial effects of zinc oxide, rosin, and resin acids with special reference to their interactions; Soderberg TA et al.; The growth inhibiting capacity of zinc oxide combined with ordinary rosin (Portuguese rosin), abietic acid or dehydroabietic acid was studied using two different methods . To mimic the actual treatment of wounds, circular tapes or sensitivity discs were placed on Muller-Hinton-agar plates that had been seeded with various facultative aerobic bacteria, and the zones of inhibition were measured . The agar dilution method was used to measure the minimum inhibitory concentration (MIC) . Inhibition of growth was restricted to Gram-positive facultative aerobic bacteria for the individual substances zinc oxide, Portuguese rosin, or resin acids, as well as for combinations of these . In general the combination of zinc oxide and dehydroabietic acid was a more potent antibacterial substance than the corresponding combination of zinc with rosin or abietic acid . These combinations commonly had synergistic antibacterial effects.

Ter Arkh, 1991, 63(2), 27 - 30
{Etiologic and pathologic approaches to pharmacotherapy of peptic ulcer}; Grigor'ev PIa et al.; Today the majority of gastroduodenal ulcers, refractory to the treatment and recurrent ones, occur because of the persistence in the gastric mucosa of Helicobacter pylori . The prevalence of the infection in patients with gastroduodenal ulcer together with the efficacy of a number of antibacterial drugs in addition to antisecretory and cytoprotective agents were studied on a large factual material.

Drug Saf, 1991 Jan-Feb, 6(1), 8 - 27
Clinical features and management of adverse effects of quinolone antibacterials; Paton JH et al.; The quinolone antibacterials are proving very useful in the management of infection, notably for the treatment of Gram-negative bacteria . With the increasing use of these drugs, adverse effects are being recognised more often and careful documentation is still required . In general, the quinolones are of low toxicity . Gastrointestinal adverse effects are the most common, and are usually mild; indeed, all adverse events are generally mild and resolve on withdrawal of the offending drug . Certain precautions and contraindications are apparent . Because drug-induced arthropathies occur in juvenile animals, quinolones should not be administered to pregnant or lactating women or to growing children, unless the clinical benefit outweighs the risk . Caution should also be observed in patients with previous epilepsy or severe cerebral arteriosclerosis . Neurological effects may require the use of appropriate neuro- and psychoactive drugs, as well as the withdrawal of the precipitating agent . Hypersensitivity reactions to a fluoroquinolone may require the use of antihistamines, and in some cases topical or systemic steroids, and may well preclude future use of a fluoroquinolone . Dose adjustments may be necessary in patients with reduced renal function, when the measurement of serum concentrations may be desirable . Interstitial nephritis, haematuria and acute renal failure are rare effects of quinolone therapy which will require appropriate management including withdrawal of the precipitating drug . Interactions with theophylline and warfarin are of clinical significance, and may require plasma concentration monitoring and adjustment of dosage.

Surg Gynecol Obstet, 1991, 172 Suppl, 11 - 6
Evolution of beta-lactamase inhibitors; Rolinson GN; In most clinical isolates that are resistant to penicillins, cephalosporins and related compounds, the mechanism of resistance is the production of beta-lactamase enzymes . These enzymes hydrolyze the amide bond in the beta-lactam ring of the compound, producing acidic derivatives that have no antibacterial properties . The rationale for beta-lactamase inhibitors is to overcome this resistance . Early study of beta-lactamase inhibition was begun in the 1940s without success . Interest in beta-lactamase inhibition was renewed with the development of the semisynthetic penicillins in the early 1960s, when it was found that certain of these compounds could function as inhibitors . However, none found clinical application . The screening of microorganisms for possible production of naturally occurring beta-lactamase inhibitors resulted in the discovery of the olivanic acids and, later, clavulanic acid . A formulation of clavulanic acid with amoxicillin was introduced in 1981, and a formulation of clavulanic acid with ticarcillin appeared shortly thereafter . More recently, other beta-lactamase inhibitors have been developed, including sulbactam and tazobactam . A formulation of sulbactam with ampicillin has appeared recently . As a result of beta-lactamase inhibition, amoxicillin and clavulanate and ticarcillin and clavulanate are active against a high proportion of amoxicillin resistant and ticarcillin resistant pathogens . These formulations have been shown to be safe and effective in the treatment of many infections that would not be expected to respond to amoxicillin or ticarcillin alone.

J Biomed Mater Res, 1991 Jan, 25(1), 39 - 51
Fibrin-antibiotic mixtures: an in vitro study assessing the possibility of using a biologic carrier for local drug delivery; Greco F et al.; An in vitro study assessing the kinetics of drug release from antibiotic-fibrin seal compounds and the antibacterial efficacy of the delivered drug has been performed . Antibiotic sensitivity and the amount of drug released was measured by means of agar diffusion test . Standard and experimental curves were established for each antibiotic and each bacterial test in order to evaluate the quantities of the drug released during each 24 h period . The reconstitution of lyophilized human fibrin with an aqueous solution containing an antibiotic resulted in only minor modification of the clotting process, with the exception of those solutions containing cefotaxim and mezlocillin which failed to clot altogether and were excluded from further study . The evaluation of the kinetics of elution of the antibiotics from the fibrin clots showed that all of the antibiotics had been almost completely released by 96 h . The delivered amount of each drug was enough to maintain the Minimal Inhibitory Concentration (MIC) until the 4th day of culture for the most of antibiotics, resulting in a prolonged release of the drug.

Antimicrob Agents Chemother, 1991 Jan, 35(1), 104 - 10
In vitro antibacterial activity of KP-736, a new cephem antibiotic; Maejima T et al.; KP-736, a new cephen antibiotic with a broad antibacterial spectrum and potent antipseudomonal activity, was evaluated for in vitro antibacterial activity in comparison with ceftazidime, cefotaxime, and cefpirome . KP-736 was significantly more active than the test compounds against gram-negative bacteria, including the Pseudomonas group and ceftazidime-, cefotaxime-, or imipenem-resistant strains, but less active against gram-positive bacteria . KP-736 had very high affinities for penicillin-binding protein 3 (PBP 3) of Escherichia coli K-12 and PBP 1A and PBP 3 of Pseudomonas aerugiosa NCTC 10490 and showed potent bactericidal activities against these two strains . It was stable to hydrolysis by penicillinases and cephalosporinases but was slightly hydrolyzed by oxyiminocephalosporinases and type II penicillinase.

Endoscopy, 1991 Jan, 23(1), 19 - 24
Disinfection of fiberscopes by thermochemical disinfection; Boks AL et al.; A new fully automated washing and disinfection machine for fiberscopes was evaluated . This apparatus, the Endoscopic Thermo Disinfector (ETD) uses a combination of heat and a brand name disinfectant containing glutaraldehyde to fulfill its purposes . The disinfectant showed effective antibacterial activity at the concentrations used in the ETD . After artificial contamination of fiberscopes with high concentrations of various bacteria the washing and disinfection process was completely effective . Contaminated debris was also effectively removed from fiberscopes and from the inside of the washing machine during this process . A number of improvements in the design of the washing machine were implemented during the test period and suggestions for further improvements will be considered . Taking into consideration the reported effects of the disinfectant used against viral pathogens, the ETD washing machine effectively cleans and disinfects flexible watertight endoscopes.

Infection, 1991, 19 Suppl 1, S72 - 3
{Use and risk of antibacterial chemotherapy from the medical point of view}; Lode H; The evaluation of the efficacy and possible intolerance of an antibacterial chemotherapy is based on the exact analysis of patient specific signs and symptoms, pathogenetic factors of the specific bacteria and parameters of the specific substance . One has to differentiate between usefulness of the antibiotics (effect) and the possible risks for the patient as well as for the physician involved . Today the legal regulations have become so strict for treatment with new substances in phase II to III studies that in most of the new chemotherapeutic substances the relationship between efficacy and possible intolerance reactions may be judged as optimal for both the patient and the physician . Our own experiences have shown that patients involved in studies with well designed protocols are better controlled and in most instances also better treated than patients treated outside such protocols.

Infection, 1991, 19 Suppl 1, S29 - 32
{Central nervous system side effects of different antibacterial substances}; Stoppe G et al.; This review concerns central nervous system side effects of different antibacterial agents . Special attention is focussed on the new quinolone derivatives, penicillins and cephalosporins . As far as possible, mechanisms of action are discussed as well as therapeutic regimens.

J Med Chem, 1991 Jan, 34(1), 29 - 37
Fluoronaphthyridines and -quinolones as antibacterial agents . 3 . Synthesis and structure-activity relationships of new 1-(1,1-dimethyl-2-fluoroethyl), 1-{1-methyl-1-(fluoromethyl)-2-fluoroethyl}, and 1-{1,1-(difluoromethyl)-2-fluoroethyl} substituted derivatives; Remuzon P et al.; A series of novel N-1-(mono-,-(di- and -(trifluoro-tert-butyl)quinolones and -naphthyridines has been prepared . Structure-activity relationship (SAR) studies indicated that the in vitro antibacterial potency was the following order: 1-(1,1-dimethyl-2-fluoroethyl) greater than 1-{1-methyl-1-(fluoromethyl)-2-fluoroethyl} greater than 1-{1,1-(difluoromethyl)-2-fluoroethyl} substituents . In the quinolone series the monofluoro-tert-butyl derivatives were found to possess better in vitro antibacterial activity than the nonfluorinated-tert-butyl equivalents . In vivo PD50 values of the 1-fluoro-tert-butyl-substituted derivatives reflect pharmacokinetic behavior and incomplete oral absorption.

J Med Chem, 1991 Jan, 34(1), 131 - 9
Three-dimensional structure-activity relationships and receptor mapping of N1-substituents of quinolone antibacterials; Ohta M et al.; Quantitative structure-activity relationships for quinolone antibacterials have been previously examined and a steric parameter L for the N1-substituents found to be important in QSAR equations . But some compounds for which previous QSAR equations could not predict the activity have appeared recently . In this study, conformations of a variety of N1-substituents of quinolone antibacterials were analyzed by a molecular modeling method . An active conformation of each of the compounds was estimated with information of the energy profile calculated by molecular orbital methods and of its biological activity . A model of a receptor corresponding to the N1-substituents was constructed by superposing van der Waals volumes of active conformer of highly active compounds . As a result of these conformational analyses and receptor mapping, it is proposed that there are two different optimum volumes for increasing the activity of quinolone antibacterials and two unfavorable regions for reducing the activity . It is suggested that the steric parameter L which appeared in previous QSAR equations corresponds to one of the optimum volumes of the proposed receptor model . With this receptor model, a relation between structure and activity of the compounds, including those mispredicted compounds in previous QSAR equations is able to be rationalized qualitatively and elegantly . We believe that this receptor model is useful for a prediction of the activity of compounds not yet synthesized as well as for designing new quinolone antibacterials.

Am J Perinatol, 1991 Jan, 8(1), 50 - 2
The effect of filtration of amniotic fluid on the growth of Chlamydia trachomatis and Escherichia coli; Ismail MA et al.; There is increasing concern about Chlamydia trachomatis infection during pregnancy, because of reports of increased maternal, fetal, and neonatal risks . Amniotic fluid is known to possess antibacterial activity and has recently been shown to inhibit formation of chlamydial inclusions in McCoy cell culture . To further characterize the anti-chlamydial factor, we investigated the effect of filtering the fluid (0.45 microns pores) prior to incubation . Amniotic fluid was obtained from 12 women at term gestation, either by amniocentesis, or at cesarean section, Chlamydial inclusion formation was studied in McCoy cell cultures, and Escherichia coli growth was studied by a plate-count method . Filtered amniotic fluid had significantly less inhibitory activity against chlamydial inclusion formation than nonfiltered fluid did . Both filtered and nonfiltered amniotic fluid were equally effective in inhibiting E . coli colony growth . These data suggest that the chlamydial inhibitor in amniotic fluid does not pass through 0.45 microns pores and is larger than the bacterial inhibitor that was reported to be a peptide of low molecular weight.

Am J Physiol, 1991 Jan, 260(1 Pt 1), G7 - 12
Glucose utilization by Kupffer cells, endothelial cells, and granulocytes in endotoxemic rat liver; Meszaros K et al.; There are several types of glucose-consuming, immunologically active nonparenchymal cells interspersed among the glucose-producing parenchymal liver cells . Combining the in vivo 2-deoxyglucose tracer technique with cell separation methods enabled us to investigate the effect of Escherichia coli endotoxin on the rate of glucose utilization by the nonparenchymal cells . Rats were injected with {14C}deoxyglucose, and intracellular 2-deoxyglucose 6-phosphate was determined in different liver cell fractions . Parenchymal, Kupffer, and endothelial cells as well as polymorphonuclear leukocytes (PMN) were separated from the liver by centrifugal elutriation followed by Ficoll-Hypaque density gradient . The number of PMN obtained from the liver was increased severalfold 3 h after endotoxin and was comparable to the number of Kupffer cells . Glucose utilization by the liver of fasted rats was due predominantly to nonparenchymal cells . Endotoxin enhanced the rate of glucose utilization by Kupffer (6.7-fold) and endothelial (2.7-fold) cells and by the infiltrated hepatic PMN (5.4-fold) . Enhanced glucose metabolism of immunologically active cells is part of the hepatic immune response and subserves the antibacterial defense of the body . The activated cells, however, may also have the potential of causing tissue damage by releasing harmful toxic metabolites.

Ann Thorac Surg, 1991 Jan, 51(1), 76 - 80
Altered cellular immune function in the atelectatic lung; Nguyen DM et al.; Pulmonary atelectasis is common and may predispose the lung to infection . We have previously shown that atelectasis impairs alveolar macrophage antibacterial function . This study examines the effect of atelectasis on the cytotoxic function of lymphocytes harvested from the bronchoalveolar space of atelectatic lung segments by bronchoalveolar lavage . Specifically, we studied natural killer and lectin-dependent cell-mediated cytotoxicity in peripheral blood and bronchoalveolar lavage lymphocytes from the atelectatic lower lobes and contralateral normal lobes in a group of 8 dogs . We observed a decline of natural killer and lectin-dependent cell-mediated cytotoxicity to 62.7% and 61.5%, respectively, of preatelectasis control values in the affected lung lobes (p less than 0.01) . Simultaneous measurements of cytotoxic activity of bronchoalveolar lavage lymphocytes harvested from the unaffected contralateral normal lungs were comparable with control values . On the other hand, natural killer and lectin-dependent cell-mediated cytotoxicity activities in peripheral blood lymphocytes were significantly increased in animals having right lower lobe atelectasis (166.7% and 154.7% of pretreated normal control, respectively, p less than 0.01) . Atelectasis was also associated with an influx of polymorphonuclear leukocytes into the bronchoalveolar compartment . These findings confirm the presence of natural killer cells and cytotoxic lymphocytes in the bronchoalveolar compartment and demonstrate an atelectasis-induced impairment of local bronchoalveolar lymphocyte function . Such a dysfunction of local lung cellular host defenses may render the atelectatic lung susceptible to infection.

Yao Xue Xue Bao, 1991, 26(5), 383 - 6
{Synthesis and antibacterial as well as antineoplastic activities of 2,4-diamino-5-methyl-6-(N-methyl-substituted benzyl) aminoquinazolines}; Meng XY et al.; This paper reports four methods for the synthesis of 2,4-diamino-5-methyl-6-(N-methyl-substituted benzyl) aminoquinazolines . Six compounds were synthesized and all these compounds showed good anticancer and antibacterial activities . Among them, I5 showed the strongest inhibition against L1210 Leukemia cell and further research has to be done.

Aesthetic Plast Surg, 1991 Fall, 15(4), 303 - 5
Wound infection in breast augmentation: the role of prophylactic perioperative antibiotics; LeRoy J et al.; Infection after augmentation mammoplasty is not common, with the reported incidence between 1% and 7% . The use of prophylactic antibiotics, however, is widespread in plastic surgery: It was documented in a 1975 survey in which 43% of responding plastic surgeons used prophylactic antibiotics . Fifteen years since this survey, surgeons have witnessed an explosion in antibiotic variety and have participated in their increased use . For many procedures, the use of antibacterials has evolved by convention and personal preference, based often on only anecdotal information . This report is our study of the routine use of antibiotics to prevent wound infection after augmentation mammoplasty.

Yao Xue Xue Bao, 1991, 26(2), 111 - 6
{Studies on pyridonecarboxylic acids as anti-bacterial agents . IX . Study on prodrugs of some pyridonecarboxylic acids}; Li ZR et al.; Synthesis and antibacterial activity of pivaloyloxymethyl esters of norfloxacin, ciprofloxacin and their N-substituted derivatives are reported . In vivo antibacterial activities (ED50) of IIIAa, b, e; IIIBa, e; IVA and IVB were 2.30, 8.48, 4.28, 2.77, 4.46, 5.68 and 0.75 (mg/kg) respectively.

Dtsch Zahn Mund Kieferheilkd Zentralbl, 1991, 79(5), 343 - 7
{The quantitative determination of resistance factors in the saliva of patients with very high caries involvement}; Jentsch H et al.; The unstimulated and stimulated whole saliva of patients with a very high caries experience were used for the determination of the flow rate, total protein, and the antibacterial proteins lysozyme, S-IgA and lactoferrin as well as the peroxidase and thiocyanate being components of the salivary peroxidase system . The concentration, the specific concentration and the secretion rate were calculated.

Fundam Clin Pharmacol, 1991, 5(4), 275 - 83
Determination of free concentration of piroxicam and naproxen in plasma . The influence of experimental conditions in equilibrium dialysis; Hundal O et al.; An equilibrium dialysis method was established in order to investigate possible relationships between free drug concentrations of piroxicam and naproxen and clinical events . Therefore the influence of variations in pH, phosphate concentration and sodium azide concentration of the dialysis buffer on the free concentrations of piroxicam and naproxen was investigated . Piroxicam was found to have a pH-dependent protein binding . Therefore a good control of pH during the dialysis process is necessary . This has been achieved by increasing the buffer capacity of the dialysis buffer, by adding an antibacterial agent to the dialysis buffer and by cleansing the dialysis cells with 70% ethanol before use to prevent bacterial growth . Addition of 0.03% sodium azide as an antibacterial agent and the use of a 0.09 mol/l phosphate buffer gave good pH control . A method to correct for deviations of pH in measurements of free concentrations of piroxicam by a simple mathematical correction has been found . As naproxen was found to have a protein binding independent of pH, a pH-correction is not necessary for this drug . Standardized conditions in determination of protein binding of drugs by equilibrium dialysis are important, as composition of the dialysis buffer and pH of plasma compartment at equilibrium may influence the free concentration measurements . Comparisons of data from experiments using different methods are therefore difficult; the importance of pH-control is stressed . With the methods used in the present investigation, equilibrium dialysis in connection with HPLC, the coefficients of variation for piroxicam and naproxen free concentrations are 5.5% and 7.4%, respectively.

Drugs Exp Clin Res, 1991, 17(3), 175 - 80
In vitro activity of flurithromycin against some genital pathogens; Furneri PM et al.; The in vitro antibacterial activity of a new macrolide drug, flurithromycin, was evaluated in comparison with the activity of erythromycin A against some genital pathogens . The strains tested, C . trachomatis, U . urealyticum . M . hominis, N . gonorrhoeae, S . agalactiae and M . genitalium, were both clinically isolates and ATCC standards . The evidenced activity of flurithromycin is similar to that of erythromycin A . Resistances with both macrolides were found in all M . hominis strains and in one strain of U . urealyticum . No particular differences are exhibited between clinical and standard microorganisms.

Chem Biol Interact, 1991, 80(1), 1 - 41
Molecular mechanisms of quinone cytotoxicity; O'Brien PJ; Quinones are probably found in all respiring animal and plant cells . They are widely used as anticancer, antibacterial or antimalarial drugs and as fungicides . Toxicity can arise as a result of their use as well as by the metabolism of other drugs and various environmental toxins or dietary constituents . In rapidly dividing cells such as tumor cells, cytotoxicity has been attributed to DNA modification . However the molecular basis for the initiation of quinone cytotoxicity in resting or non-dividing cells has been attributed to the alkylation of essential protein thiol or amine groups and/or the oxidation of essential protein thiols by activated oxygen species and/or GSSG . Oxidative stress arises when the quinone is reduced by reductases to a semiquinone radical which reduces oxygen to superoxide radicals and reforms the quinone . This futile redox cycling and oxygen activation forms cytotoxic levels of hydrogen peroxide and GSSG is retained by the cell and causes cytotoxic mixed protein disulfide formation . Most quinones form GSH conjugates which also undergo futile redox cycling and oxygen activation . Prior depletion of cell GSH markedly increases the cell's susceptibility to alkylating quinones but can protect the cell against certain redox cycling quinones . Cytotoxicity induced by hydroquinones in isolated hepatocytes can be attributed to quinones formed by autoxidation . The higher redox potential benzoquinones and naphthoquinones are the most cytotoxic presumably because of their higher electrophilicty and thiol reactivity and/or because the quinones or GSH conjugates are more readily reduced to semiquinones which activate oxygen.

Antibiot Khimioter, 1991 Jan, 36(1), 45 - 6
{Imidazoles in the treatment of ocular mycoses}; Maichuk IuF et al.; The use of a new class of broad spectrum antifungal drugs i.e . imidazoles and in particular ketoconazole in treatment of severe affections of the eye such as mycoses is described . The clinical trials included 40 patients with various forms of mycosis: mycotic canaliculitis (6 patients), mycotic blepharitis (4 patients), mycotic conjunctivitis (7 patients), keratomycosis (17 patients) and mycotic endophthalmitis (6 patients) . Ketoconazole was used in the form of tablets and instillations . The combined treatment included nonsteroid antiinflammatory drugs and antibacterial agents . The clinical trials showed that ketoconazole had pronounced antifungal activity and was rather efficient in treatment of ocular mycoses . Its broad spectrum and low toxicity were recorded.

Probl Tuberk, 1991, (1), 9 - 11
{The use of antioxidants in the complex therapy of patients with infiltrating pulmonary tuberculosis}; Starostenko EV et al.; Clinical and laboratory investigations examined the possibility of a lower load of antibacterial drugs (ABD) in combination with the two antioxidants, alpha-tocopherol and sodium thiosulfate, in combined therapy of patients with infiltrative pulmonary tuberculosis . Higher efficacy of two ABDs supplemented by two antioxidants than three or more ABDs was evidenced by a shorter period of sputum negativity (1.6 +/- 0.26 and 2.7 +/- 0.27 months; p less than 0.01) and higher rates of cavity closure (95.6 +/- 4.3 and 63.2 +/- 6.7%; p less than 0.05).

Pharmacotherapy, 1991, 11(1), 20 - 5
The use of aztreonam in pediatric patients: a review; Bosso JA et al.; Aztreonam is the first monobactam available for use in this country . A parenteral antibiotic, its antibacterial spectrum is limited to gram-negative aerobic pathogens . The drug's pharmacologic, pharmacokinetic, and toxicologic properties are reviewed . Based on early experience in pediatric patients, certain recommendations can be made for the use of aztreonam.

EMBO J, 1991 Jan, 10(1), 163 - 9
The andropin gene and its product, a male-specific antibacterial peptide in Drosophila melanogaster; Samakovlis C et al.; In our study of the cecropin locus in Drosophila we have found a gene for a new peptide, andropin, with antibacterial properties . Transcripts from this gene, Anp, could be detected in newly eclosed males and reached steady-state levels after 1 day . Transcription was strongly induced in response to mating and is strictly confined to the ejaculatory duct of adult males . The deduced peptide sequence reveals a hydrophobic amino terminus with striking similarity to the signal peptide of the cecropins . The sequence of the predicted mature andropin shows no direct homology with the cecropins, but the two peptides may have similar secondary structures . We have synthesized the predicted gene product and shown it to be antibacterial . Crude extracts from male genital tracts show a potent bactericidal activity, and electrophoretic separation revealed at least three antibacterial components, one with the same mobility as the synthetic peptide . It appears that insects have evolved a mechanism for the protection of the seminal fluid and the male reproductive tract against microbial infections.

Aesthetic Plast Surg, 1991 Summer, 15(3), 229 - 32
Mycobacterial infection following blepharoplasty; Kevitch R et al.; A case of exceedingly rare mycobacterial infection following blepharoplasty is recorded . This nursing home employee underwent a combined blepharoplasty, eyelid ptosis correction, and replacement of breast implants . One month later, she developed localized abscesses of both eyelids . Cultures revealed nontuberculous mycobacterial infection . The infection was controlled after ten months of antibacterial therapy using doxycycline . We believe that the patient's exposure to debilitated individuals due to her nursing profession and the presence of a Jones tube in the right lacrimal system were major contributing factors.

Khirurgiia (Sofiia), 1991, 44(3), 45 - 50
{The treatment of calculi in the iliac segment of the ureter by extracorporeal high-energy shockwave lithotripsy}; Nikolov S et al.; Experience is recorded with the treatment of calculi in the iliac segment of the ureter by extracorporal lithotripsy with high-energy stroke waves with lithotriptor of the firm "Dornier", model HM-3 . For a period of 2 1/2 years 18 patients at mean age 38 years have been treated . Retrograde catheterization was always performed before lithotripsy . Successful reposition was achieved in 6 patients . In all others lithotripsy was performed in prone position . Special supporting cushions were manufactured and used; they helped for a more stable position of the patient on the stand, facilitate calculus positioning, the load to the knee joints is reduced, the fluoroscopic time is shortened, thus reducing the radiation load to patient and attending personnel . All patients received antibacterial and spasmolytic therapy . The mean length of stay in the clinic was 3.2 days . The results were good in 94.1 per cent of the cases . No early or late complications of urologic or other nature were observed.

Chemotherapy, 1991, 37(3), 196 - 201
Turbidimetric study of the effect of inoculum density on the response of Escherichia coli to gentamicin under aerobic and anaerobic conditions; Edwards R et al.; The turbidimetric response to gentamicin of two strains of Escherichia coli was examined under aerobic and anaerobic conditions with 3 inocula . Turbidimetry showed that the minimum inhibitory concentration (MIC) was influenced by growth of partially inhibited cultures during the overnight incubation period . Continuous turbidimetric monitoring also allowed the minimum antibacterial concentration (MAC: the lowest concentration to cause an effect on normal growth) to be measured . As judged by the MAC, the effect of inoculum was small over the range 5 x 10(5) to 9 x 10(7) colony-forming units (CFU), but increased substantially as the inoculum was raised further . Exposure to gentamicin under anaerobic conditions caused an average 4-fold rise in the MAC with different inocula.

Sov Med, 1991, (3), 15 - 7
{Surgical treatment of hematogenic spinal osteomyelitis using extra-focal instrumental fixation}; Lavrov VN et al.; A total of 78 cases with acute hematogenic vertebral osteomyelitis are analyzed . Diagnostic errors at the prehospital and hospital stages are specified in 42 cases (53.8 percent), that resulted in late start of adequate treatment . Preoperative antibacterial therapy was carried out 1 to 1.5 months before surgery consisting in radical resection of the focus with replacement of the defect with autotransplant and extra-focal++ fixation with Byzov's apparatus . After surgery the patients started exercises on days 5-10 . This treatment resulted in formation of osseous block at the site of vertebral body resection in 3-4 months in 30.8 percent of cases, in 5-6 months in 57.7 percent, and in 10-12 months in 11.5 percent of patients.

Klin Khir, 1991, (4), 47 - 9
{Principles of complex treatment of infection in emergency surgery}; Kavkalo DN; The analysis of 140 cases of acute surgical sepsis is presented . The general principles for the treatment of sepsis in emergency surgery were established . The most effective are the guided laparotomy in peritoneal sepsis, use of intravascular laser blood irradiation, chemotherapeutical means and dressing materials (polysorb, carboserix, collocyl etc.), different gaseous media (aeroionotherapy, oxygenation, ozonized guided antibacterial medium) which have favourable effect on the reparative processes in the primary foci of infection . Resulting from the use of complex treatment, the decrease in lethality from 75 to 35.7% was noted.

Chemotherapy, 1991, 37 Suppl 2, 31 - 6
Intramuscular imipenem/cilastatin treatment of upper reproductive tract infection in women: efficacy and use characteristics; McGregor JA et al.; We evaluated the efficacy, patient and medical staff acceptance, and costs of intramuscular therapy with imipenem/cilastatin for mild to moderate upper reproductive tract infection in hospitalized women in an open study . Thirty-five patients were enrolled, and 29 successfully completed the protocol . Of these, 90% were satisfactorily treated with imipenem/cilastatin given intramuscularly . Twenty-eight of 29 subjects tolerated the intramuscular injections well, although 7 women noted mild to moderate discomfort during injection . All patients who had previously received intravenous therapy (24/29) stated that they preferred the intramuscular injections to continuation or reinitiation of intravenous treatment . Therapy with intramuscular imipenem/cilastatin (assuming a marketed price per gram of approximately $30) was associated with cost savings in comparison with other regimens offering similar antibacterial coverage . Initial care provider resistance to treatment with intramuscular imipenem/cilastatin was overcome due to patient satisfaction . Intramuscularly administered imipenem/cilastatin was effective, generally well tolerated, and resulted in cost saving . Intramuscular administration of imipenem/cilastatin may be a preferred antibiotic treatment in patients with mild to moderate infection due to susceptible microorganisms.

Pediatriia, 1991, (5), 71 - 7
{Clinico-morphological comparison in children with infectious endocarditis}; Tiurin NA et al.; As many as 21 children suffering from infectious endocarditis (IE) were examined for the clinical and morphological picture of the disease . The patients' age ranged from 2 to 15 years . In 15 children, IE developed in association with different congenital diseases; in one patient, in the presence of rheumatic heart disease, and in 5 patients, in unaffected heart valves . The sectional material was examined in 19 cases whereas the operational material in 2 cases . Analysis of the data obtained has shown that early diagnosis of IE (primary and secondary) may not infrequently be fairly difficult, which is likely to result in the late administration of antibacterial therapy . In addition to the involvement of the valvular apparatus of the heart, the majority of the patients demonstrated the signs of focal myocarditis and postmyocarditic cardiosclerosis, which is one of the causes of the development of refractory heart insufficiency . IE children mostly die from heart insufficiency and thromboembolism.

Probl Tuberk, 1991, (4), 57 - 60
{Change in the content of serum immunoglobulins A, G, M in patients with pulmonary tuberculosis and alcoholism during antibacterial and anti-alcoholism therapy}; Maskeev KM et al.; Serum immunoglobulins A, G, M in 93 patients with pulmonary tuberculosis and suffering from alcoholism at the same time (a core group) were investigated in the course of a combined therapy . A control group consisted of 44 pulmonary tuberculosis patients who were nonalcoholics . Examinations were carried out on their admission to a hospital and 3, 6 and 9-12 months after treatment . The findings proved that the patients of the core group had hyperproduction of main serum immunoglobulins . In the course of a complex antibacterial and antialcoholic therapy the IgA values remained high . A disturbed functional activity of B-lymphocytes is likely to be one of the causes leading to a low efficacy of the tuberculosis treatment among alcoholics.

Probl Tuberk, 1991, (4), 3 - 7
{X-ray semeiotics of functional changes of the respiratory organs in patients with tuberculosis of the lungs and the obstructive syndrome}; Gapon'ko GA et al.; Examination included 178 patients with active pulmonary tuberculosis and moderate obstruction (74 subjects) or severe obstructive syndrome (104 subjects) . The dynamic morphofunctional X-ray examination along with a study of external respiratory function made it possible to study the pattern of functional disturbances in patients with tuberculosis of respiratory organs and concurrent bronchial obstruction . Roentgeno-pneumopolygraphy supplemented with physical exercise tests and berotec specified the localization, extent and the character of disorders of bronchial patency and enabled one to study the compensatory mechanisms of external respiratory function during antibacterial therapy . According to the data of roentgeno-pneumopolygraphy, the more serious air-filling disorders are, the more pronounced the bronchial obstructive changes are, while the degree of respiratory disorders depends on the type and extent of the process and on the duration of the disease and its genesis.

Mater Med Pol, 1991 Jan-Mar, 23(1), 13 - 6
Chemotactic activity of neutrophil granulocytes in old people in health or with symptoms of infection; Pawinska M et al.; Clinical observations point out that the inflammatory process follows a different course in old people as compared to young persons . In the studies on the mechanisms responsible for this difference the chemostatic activity of polymorphonuclear granulocytes was assessed in peripheral blood in healthy elderly persons and in people in the same age group with evidence of infections, mainly of bacterial origin . A decrease was demonstrated of the chemotactic activity of polymorphonuclears in healthy persons aged over 65 years, as compared to young people, and even a more pronounced reduction of this activity in old people with infections . The observed disturbances of the functions of phagocytic cells may be one of the causes of less effective antibacterial defense in the organism during the process of ageing.

Nucleic Acids Symp Ser, 1991, (25), 109 - 10
DNA strand scisson and cell-killing activity of hydroperoxynaphthalimide derivatives upon photoirradiation; Matsugo S et al.; A series of hydroperoxynaphthalimides (1a-1c) and naphthaldiimide (2) that generate hydroxyl radical upon longer wavelength photoirradiation (366 nm) have been devised . They induce DNA strand break at low concentration upon photoirradiation which are inhibited in the presence of hydroxyl radical scavengers such as mannitol or sodium benzoate . The compound 2 showed a sequence specific DNA strand scission at -5'GG-sequence . The formation of 8-hydroxydeoxyguanosine (8-OHdG) is also observed on photoirradiation of 1a or 2 in the presence of dG . The antibacterial activities of these compounds will also be described.

Biomed Sci, 1991, 2(6), 551 - 6
Signal transduction in eukaryotic cells and intracellular parasitism of Legionella; Belyi YuF et al.; A fundamental property of the eukaryotic cell is its ability to respond to external signals . This property becomes extremely important during microbial invasion, when the volume of information to be analyzed by the cellular receptor machinery increases considerably . Cell-surface receptors are influenced by a pool of additional ligands, some of the most important of these being the infecting microorganism, products of bacterial metabolism, virulence factors, as well as regulators produced by the endocrine and immune systems of the infected animal (e.g . antibodies, hormones, lymphokines, and mediators of inflammatory responses) . The consequence of the binding of ligands is the activation of different antibacterial mechanisms, some of which are used by the phagocytes after ingestion of the infectious agent . Inhibition of such antibacterial mechanisms by intruding microorganisms could be achieved by bacterially-induced alterations in signal transduction.

Acta Haematol Pol, 1991, 22(2), 265 - 70
{Granulocyte acid phosphatase activity in patients with Hodgkin's disease}; Dabrowska M et al.; In 24 patients with Hodgkin's disease the activity of acid phosphatase was determined in granulocytes . Its level was only half that in the control group . The causes of this low activity of this enzyme may be increased number of cells without it, exocytosis, and possible influence of substances secreted by the neoplasm . It is suggested that the determination of this activity may be indirectly useful for verification of the efficacy of the antibacterial mechanisms, and also of antitumour resistance of the host.

Nauchnye Doki Vyss Shkoly Biol Nauki, 1991, (10), 109 - 13
{The antibacterial activity of a humic preparation made from the therapeutic peat mud of the Dzalal Abad deposit in Kirghizia}; Gadzhieva NZ et al.; The humic acid from the Dzhalal Abad therapeutic peat muds has been extracted to reveal the mechanisms of interaction between humic acid and microelements in therapeutic muds and to study the mud physiologically active factor . A complex compound of copper with humic and aminoacetic acids has been obtained, their physicochemical and antibacterial properties have been studied.

Probl Tuberk, 1991, (7), 5 - 6
{Early detection of tuberculosis and its pharmacological prevention in children from the epizootologically unfavorable territories}; Niiazbekova KZh et al.; The examination of 2150 children living in the epidemiologically unfavourable territories was carried out for 3 years (1988-1990) by a double Mantoux test with 2 TU PPD-L at a 6-month interval . By the end of the 3rd year primary contamination decreased by 2.8 times and local tuberculosis detection by 6.4 times . In the control group (1457 children) having the Mantoux test with 2 TU PPD-L once a year, primary contamination during the same time decreased by 1.2 times and tuberculosis detection by 1.4 times . Chemoprophylaxis was conducted in 3 groups of children: Group 1 was given only isoniazid for 3 months twice a year; group 2, isoniazid and ethambutol for 2 months once a year; and Group 3, isoniazid alone during 3 months . Chemoprophylaxis effectiveness in the epizootically unfavourable area was significantly higher when the two antibacterial drugs were used for 2 months once a year.

Klin Khir, 1991, (3), 48 - 9
{Use of the "Capromed DQ" thread for closure of the anterior abdominal wall defect during operations for postoperative recurrent ventral hernia}; Polous IuM et al.; A new native synthetic absorbable antibacterial polyamide thread "Capromed DC" was used for liquidation of the abdominal wall defect in operation for postoperative recurrent hernia . The low incidence of complications caused by infection around the non-absorbable ligature was noted.

Grud Serdechnososudistaia Khir, 1991 Jan, (1), 34 - 7
{Surgical interventions in tuberculosis of the lungs without prior antibacterial therapy}; Vagner EA et al.; Operations were performed on 102 patients (93 with tuberculomas, 2 with fibrocavernous tuberculosis, and 7 with infiltrative tuberculosis of the type of caseous pneumonia) without preoperative chemotherapy . Certain difficulties in identification of the nature of the disease in tuberculomas are pointed out . It is shown that only emergency histological study helps to avoid errors . Postoperative complications occurred in 5.9% of patients . Exacerbation of tuberculosis after economical resections in tuberculomas occurred in 2.1% of patients due to a nonradical intervention . The expediency of early interventions which allow the term of treatment to be shortened is shown.

Chin J Biotechnol, 1991, 7(4), 241 - 51
Subcloning and expression of midecamycin polyketide synthase genes from Streptomyces mycarofaciens 1748; Zhu X et al.; A 2.4 kb fragment containing the midecamycin polyketide synthase genes (mps) was subcloned from the preliminary clone pCN8B12 out of the genomic library of midecamycin-producing strain S . mycarofaciens 1748, by using the homologous DNA of the actinorhodin polyketide synthase gene (act I) as hybridization probe . This DNA fragment was subcloned onto Streptomyces/E . coli shuttle vector pMHM3 . A recombinant plasmid pCG2 was obtained . The transformation of the polyketide synthase deficient mutant of actinorhodin-producing strain, S . colicolor TK17, with pCG2 DNA resulted in the production of an antibacterial compound which was similar neither to actinorhodin nor to midecamycin . The transformation of spiramycin-producing strain S . ambofaciens with pCG2 DNA increased spiramycin production in the fermentation broth . The transformation of the regulatory mutant of daunorubicin-producing strain with pCG2 DNA resulted in the production of epsilon-rhodomycinone verified by TLC and HPLC analyses . The pCG2 DNA also could be functionally expressed in tetracenomycin C-producing strain S . glaucescens . However, it could not be expressed in the blocked mutants of erythromycin-producing strain Saccharopolyspora erythrarea WMH 15,261 . These suggest that the pCG2 DNA may complement polyketide synthase gene deficiency or have some regulatory function in certain polyketide antibiotic-producing strains.

Yao Xue Xue Bao, 1991, 26(11), 821 - 8
{Synthesis and biological activities of 2,4-diamino-5-chloro-6-substituted quinazolines}; Liu JQ et al.; Title compounds were synthesized by condensation of 5-chloro-2,4,6-triaminoquinazoline (8) with various substituted benzaldehydes to produce the corresponding Schiff bases, followed by reduction with NaBH4, II and III were obtained by formylation or nitrosation of I respectively . Primary screening for suppressive therapeutic effects against P . berghei in mice showed that eight of the twelve compounds produced 100% suppression when administered orally at dose of 20 mg/kg . The results against L1210 Leukemia cell and B16 melanoma cell in vitro exhibited potent inhibition . Among them four compounds were more active than MTX and SIPI 759 . Further work is in process . Antibacterial tests in vitro showed that a number of compounds possessed moderate activities against Diplococcus pneumoniae.

Yao Xue Xue Bao, 1991, 26(11), 809 - 14
{Studies on reaction and antibacterial activity of 1-aryl-4-ethoxycarbonyl-5-amino-1,2,3-triazole with several electrophilic reagents}; Zhang ZY et al.; Upon treatment of 1-aryl-4-ethoxycarbonyl-5-amino-1,2,3-triazoles (1) with excess acetic acid, acetic anhydride, acetyl chloride, benzoyl chloride, formamide, etc., fourteen new derivatives of 1 were obtained in good yields, such as, 1-H-4-ethoxycarbonyl-5-arylamino-1,2,3-triazoles (2b-d), 1-RCO-4-ethoxycarbonyl-5-arylamino-1,2,3-triazoles (3a-d), 1-aryl-4-ethoxycarbonyl-5-acetylamino-1,2,3-triazoles (4a-d) and 1-formoyl-4-ethoxycarbonyl-5-p-nitrophenylamino-1,2,3-triazole (5a), 1-benzoyl-4-ethoxycarbonyl-5-p-nitrophenylamino-1,2,3-triazoles (5b), 1-p-chlorobenzoyl-4-ethoxycarbonyl-5-p-nitrophenylamino-1,2,3-triazoles (5c) . Some of them were rearrangement products . Structures of all heterocyclic compounds were identified by elemental analyses, IR, 1HNMR and MS . Inhibiting effects of some compounds on B . substilis, E . coli, E . aerogenes and S . aureus were also screened.

Yao Xue Xue Bao, 1991, 26(10), 733 - 40
{Studies on pyridonecarboxylic acids as antibacterial agents . X . Synthesis and structure-activity relationships of 1, 7-disubstituted-6-fluoro-1,4-dihydro-4-oxo-quinoline-3-carboxylic acids}; Chen JX et al.; A series of pyridonecarboxylic acids were prepared . These compounds have different groups including substituted benzenes, furans and isoxazles at the 1-position, or different substituted amino groups at the 7-position . The in vitro antibacterial potencies of these compounds against E . coli . and S . aureus were tested, and structure-activity relationships were discussed.

Eur J Drug Metab Pharmacokinet, 1991, Spec No 3, 473 - 7
Biopharmaceutic evaluation of some 4-quinolone derivatives; Mrhar A et al.; The relationships between physicochemical properties (ionization, solubility, partition, protein binding) of 4-quinolone derivatives and their pharmacokinetics was studied by means of in vitro methods . This information is needed to clarify the erratic absorption behaviour of quinolone antibacterials following oral administration . The ionization constants of ofloxacin (OF), pefloxacin (PF), norfloxacin (NF) and ciprofloxacin (CF) were determined by solubility, potentiometric, spectrophotometric, and octanol-water partition methods . The quinolones are ampholytes showing small values of partition coefficients (order of magnitude 1) resulting from their hydrophilic nature . Within the series, both partition coefficients and the ionization constants differ only slightly (5.5 less than pK1 less than 6.5, and 7.5 less than pK2 less than 8.5) . The intrinsic solubility of nonionized forms of drugs was obtained to be of 1g/l order of magnitude . Linear relationship was observed between the log solubility versus reciprocal temperature . The dissolution of NF is an endothermic reaction with dissolution enthalpy H = 20.4 kJ/mol . In vitro diffusion of OF, PF, NF, and CF was studied by the means of Sartorius in vitro absorption model . The rate of diffusion and the projected in vitro rate of absorption are not functions of structural differences within the series (diffusion rate constant range was 0.5 less than kd less than 5.0 .10-3 cm/min) . Binding of NF, CF, PF and OF to bovine serum albumin (BSA) was studied using equilibrium dialysis in the absence and presence of urea . It was found that the quinolones were moderately bound (40-60%) to BSA and that urea in pathologic concentrations diminished their binding for 10-25%.

Auris Nasus Larynx, 1991, 18(4), 323 - 9
Otitis media induced by inoculation of a chemotactic factor; Nonomura N; Phagocytic cells in middle ear effusion obtained from patients with acute or chronic otitis media, have antibacterial activity which is an element of the host defense system . In addition, they modify inflammatory responses as they release degranulated substances, phospholipid-derived substances, and active oxygens . To demonstrate both the direct and indirect biological activities of chemotactic factor through migrating inflammatory phagocytic cells in acute otitis media, a synthetic chemotactic peptide, formyl-methionyl-leucyl-phenylalanine (fmlp), was inoculated into the middle ear of guinea pigs . Fmlp induced severe vascular damage, mucosal edema, and infiltration of phagocytic cells 1 and 3 days after inoculation and interstitial fibrosis and calcification 2 weeks after inoculation . Chemotactic factor in the middle ear cavity caused middle ear tissue damage and may play a role in the development of acute and chronic otitis media.

Klin Wochenschr, 1991, 69 Suppl 26, 47 - 52
{Antibacterial chemotherapy in the surgical intensive care unit}; Peters G; Nosocomial infections are among the most serious complications encountered in surgical intensive care . The most sufficient antibacterial chemotherapy of these infections is generally based on basic and empiric principles . This includes a correct decision as to the necessity for chemotherapy and the appropriate establishment of dosage, treatment duration, drug monitoring and efficacy control . Several antibiotic regimes for the treatment of the most common nosocomial infections, i.e . pneumonia, peritonitis and sepsis, are discussed.

Ter Arkh, 1991, 63(11), 78 - 80
{Pyoderma vegetans as an early sign of HIV infection}; Potekaev NS et al.; Skin and mucosal lesions are described in a 40-year-old man who suffered from HIV infection in the stage of secondary diseases . The diagnosis was supported by demonstration of antibodies to HIV in the immune blotting test . The clinical manifestations were reduced to steady fever, generalized lymphadenopathy, pyoderma vegetans and chancriform pyoderma, candidiasis of the oral cavity, and seborrheic dermatitis, HIV infection was diagnosed 4 years after the appearance of pyoderma which initially was amenable by external antibacterial agents and then became resistant to them . Eruptions of pyoderma vegetans simulating wide condylomas were located in inguinal folds, on the internal surface of the thighs and scrotum; the chancriform focus was located in the internal preputial layer . The treatment with azothymidine combined with antibacterial and antimycotic agents led to the improvement of the patient's general status and to the reduction of local lesions . However, on recommendations of an unknown witch doctor who started treating him with the aid of reflexotherapy, phytotherapy and bioenergetic actions the patient stopped receiving the treatment prescribed and did not report for control examinations . After 5 months he died of brain edema.

Klin Wochenschr, 1991, 69 Suppl 27, 12 - 5
{Prevention of stress ulcer and pneumonia: sucralfate}; Kappstein I; Pneumonia in ventilated intensive care patients is one of the most serious nosocomial infections with a frequently fatal outcome . Retrograde colonization of the oropharynx originating from the stomach is a recently described phenomenon associated with increased pH values of gastric fluid . Microaspiration of gastric fluid colonized with great numbers of pathogens can lead to ventilator-associated pneumonia . Since the degree of microbial growth is dependent upon the pH of gastric fluid, pH values of gastric aspirates should not exceed pH 4 if stress ulcer prophylaxis is required . It is now known from several clinical studies that the mean pH values of gastric fluid under sucralfate prophylaxis are considerably lower than under conventional stress ulcer prophylaxis . This is at least partly due to the inherent antibacterial activity of the substance . Finally, the most important result is the markedly reduced frequency of pneumonia in ventilated patients compared with conventional prophylaxis regimens.

Microbiol Immunol, 1991, 35(12), 1059 - 71
Antibacterial activity of cefpodoxime against Branhamella catarrhalis; Takenouchi T et al.; The antibacterial activity of cefpodoxime against Branhamella catarrhalis was studied . All of the 65 clinical isolates tested were inhibited at and below 1.56 micrograms/ml, both at 10(7) and at 10(5) CFUs . The following was further studied on B . catarrhalis N-5 which showed average susceptibility to each drug examined . Bactericidal activity was observed at and above the MIC . Scanning and transmission electron microscopy revealed morphological changes, such as cellular swelling, bleb formation, inhibition of septum formation, and lysis, of the cells exposed to cefpodoxime at concentrations around the MIC . Cefpodoxime was poorly hydrolyzed by the beta-lactamase and it showed affinity for two penicillin-binding proteins that had approximate molecular weights of 83 and 74 kilodaltons, with I50 values of 3.7 and 2.1 micrograms/ml, respectively.

Chemotherapy, 1991, 37(5), 303 - 9
Penetration of roxithromycin into bronchial secretions; Boccazzi A et al.; The penetration of an antibacterial agent into the bronchial secretions is a crucial factor in determining its clinical efficacy in the treatment of bacterial respiratory infections . Roxithromycin is a novel macrolide compound active against the most frequent respiratory pathogens . Following administration of 150 mg p.o., we observed a prompt penetration of the compound into bronchial secretions of critically ill patients . Elevated concentrations above the MICs of the commonest susceptible pathogens are reached and maintained until the next administration.

Arch Immunol Ther Exp (Warsz), 1991, 39(1-2), 175 - 9
Formation of beauvericin by selected strains of Beauveria bassiana; Peczynska-Czoch W et al.; Various strains of Beauveria bassiana were cultivated in submerged cultures and examined for their abilities to produce beauvericin, cyclodepsipeptide antibiotic displaying antibacterial and insecticidal properties . It has been found that among twenty four strains of Beauveria bassiana only three produced beauvericin . Apparently, the striking differences among tested strains concerning several secondary product formations have been observed.

Trans R Soc Trop Med Hyg, 1991, 85 Suppl 1, 1 - 3
A review of the treatment of bacterial meningitis; Girgis NI et al.; This is review of our experience in the treatment of meningitis carried out at the Naval Medical Research Unit No . 3 (NAMRU-3), Cairo, Egypt since 1967 . We have demonstrated that the serum and cerebrospinal fluid concentrations of ampicillin and its efficacy when used in the treatment of meningitis are comparable whether they are administered intravenously or intramuscularly . The third generation cephalosporin ceftriaxone was found to be very safe and effective when administered intramuscularly once a day in the treatment of the different types of acute bacterial meningitis . Aztreonam given intramuscularly was successful in the treatment of Gram-negative meningitis caused by multi-resistant organisms . The fatality rates and morbidity were significantly reduced in patients with meningitis when dexamethasone was given in conjunction with antibacterial chemotherapy.

Vestn Akad Med Nauk SSSR, 1991, (12), 50 - 4
{Immunologic correction in the treatment of chronic hematogenic osteomyelitis of long tubular bones in children}; Samsygin SA et al.; Children suffering from chronic osteomyelitis of long tubular bones were compared for the action of the immunomodulating drug tactivin injected subcutaneously and endolymphatically . The study was carried out in 57 patients staying in hospital . The patients were distributed into the following groups: 18 patients entered a group where tactivin was injected subcutaneously, 9 patients made up a group where the drug was administered endolymphatically, and a reference group included 30 patients treated by conventional methods . On admission the patients demonstrated secondary immunodeficiency characterized by the lowering of the absolute and relative T lymphocyte count, a decrease of functional activity in blast transformation of lymphocytes, and dysimmunoglobulinemia . The use of immunomodulation with tactivin whatever the route of administration promoted a more uneventful course of the postoperative period, a decrease of suppurations of the postoperative wounds, reduction of the patient's hospital stay, a decrease in the dose of antibacterial drugs required for continuous treatment, and enhancement of the efficacy of antibacterial therapy . The use of tactivin endolymphatically brings about rapid normalization of the count of T, T active and B lymphocytes, an increase of the indicated parameters to the lower limit of normal on subcutaneous injection . As for the reference group, these parameters continue a progressive lowering.

Chemotherapy, 1991, 37(4), 229 - 38
Penetration of ciprofloxacin and metabolites into human lung, bronchial and pleural tissue after 250 and 500 mg oral ciprofloxacin; Rohwedder R et al.; Ciprofloxacin (CIP) and metabolite concentrations in lung tissue, parietal pleura and bronchial tissue were assessed in 43 adult patients who underwent lung surgery . A single oral dose of CIP was given for prophylaxis of bacterial infections . Two to 6 h prior to tissues sampling, 23 patients received 250 mg and 20 subjects 500 mg of the substance . Blood plasma samples were obtained at the same time as the lung tissue samples . CIP and its metabolites were assayed chemically by high-pressure liquid chromatography (HPLC) . After 250 mg CIP, the individual lung tissue CIP concentrations during the 2- to 6-hour post-dose period ranged from 0.5 to 4.8 mg/kg . In 20 of the 23 lung samples, the CIP concentrations were above 1 mg/kg . After 500 mg CIP, the corresponding lung CIP concentrations ranged from 1.6 to 6.0 mg/kg . The CIP lung concentrations were, irrespective of the dose size, between 2 and 7 times higher than the simultaneous blood plasma concentrations . This indicates an excellent penetration of CIP and its metabolites into lung tissue . Bronchial tissue was obtained in 9 cases . Penetration into bronchial mucosa tissue was good as well, as indicated by tissue/plasma ratio values between 1.5 and 4.4 . Individual CIP concentrations in the patients given 250 mg CIP, ranged from 1.0 to 1.6 mg/kg . In the patients who received 500 mg, the range was from 1.7 to 3.4 mg/kg . Tissue/plasma ratio values between 0.8 and 2.1 indicated that penetration to pleural tissues was good as well . Metabolite concentrations in all of the tissues assayed (lung, bronchial mucosa, pleural tissue) were low when compared to the concentrations of CIP . The concentrations in lung, pleural and bronchial tissue will probably permit low doses in the treatment of most respiratory tract infections . The broad spectrum of antibacterial activity, the good tissue penetration, chemical stability and the good safety record of the substance means that the drug is potentially a useful agent for perioperative antibiotic prophylaxis.

Scand J Urol Nephrol Suppl, 1991, 138, 77 - 82
Prostatitis, prostatosis and prostalgia . Psychogenic or organic disease?
Pavone-Macaluso M, di Trapani D, Pavone C.
The term 'chronic prostatitis syndrome' (C.P.S) encompasses chronic bacterial prostatitis, chlamydia or ureaplasma-associated disease, chronic 'abacterial' prostatitis, and patients with prostatosis or prostatosis or prostalgia . Interesting observations emerged from the evaluation of the clinical material indicating that the patients with abacterial prostatitis and those with prostatosis or prostaglia group have frequent sperm abnormalities and ultrasonographic changes suggesting a more complex pathogenesis than mere congestion and neurosis . Treatment in 144 evaluable patients treated with a long-acting sulphur-trimethoprim combination was almost uniformly well tolerated; Chlamydia was eradicated in all 10 treated patients and 77.4% of patients with bacterial C.P.S . were rendered free of bacteria . Sperm abnormalities were almost invariably resistant to the treatment . Only 44.4% of patients showed a partial improvement, limited to one or more parameters . Results did not differ significantly in the various subgroup . An overall evaluation of results showed that disappearance of every presenting symptom and sign was obtained in 24.3% and a significant improvement in another 25% of patients, including those in the prostatosis-prostalgia group . These results suggest that antibacterial treatment may be followed by favourable clinical results even in patients in whom no bacteria or other aetiological agents could be isolated.

Infection, 1991, 19 Suppl 5, S296 - 302
Pharmacokinetics and hemostasis following administration of a new, injectable oxacephem (6315-S, flomoxef) in volunteers and in patients with renal insufficiency; Andrassy K et al.; Flomoxef is a new oxacephem of broad antibacterial activity . The compound is mainly excreted through the kidneys . Two dose finding studies in patients with various degrees of renal insufficiency revealed that the dosage of flomoxef has to be reduced exactly according to the renal function . Although the N-methylthiotetrazole group has been replaced by a hydroxyethyl group, an inhibitory effect of flomoxef on vitamin K metabolism persisted . This effect was, however, less pronounced than with latamoxef . Only patients with low vitamin K stores are endangered . For those in whom low vitamin K stores are suspected repeated controls of prothrombin time are advised during the treatment . In contrast to latamoxef the platelet system was not affected by flomoxef . With the exception of loose stools in some patients no other clinical side effects during treatment were observed.

Infection, 1991, 19 Suppl 5, S244 - 52
Pharmacological properties of cephalosporins; Christ W; The cephalosporins differ in the substituents attached at the 3 and/or 7 positions of the molecule . Very schematically, substitution at C3 mainly modifies the overall pharmacokinetic properties whereas substitution at position 7 influences the antibacterial characteristics . When using the more common "generation" system for classification, three generations can be distinguished on the basis of their antibacterial spectrum, potency, and their stability to beta-lactamases . The first generation cephalosporins have similar antibacterial and pharmacokinetic characteristics . C3-esterified cephalosporins (e.g . cephalothin and cephapirin) are significantly metabolized . The so-called second generation cephalosporins exhibit only minor differences with respect to the pharmacokinetic properties in contrast to the third generation cephalosporins . The apparent volumes of distribution of most cephalosporins range between seven and 20 1, indicating that they mainly stay in the extracellular space . Plasma protein binding is variable from compound to compound . Generally, the major route of elimination of most cephalosporins is via the kidney except for cefoperazone and ceftriaxone which are both excreted to a large extent by the biliary route . With the exception of cefonicid, cefotetan and cefriaxone, which have longer elimination half-lives (i.e . 4.5, 3.5 and around eight hours), all other cephalosporins have a half-life ranging from 0.5 to 2.5 hours . The pattern of adverse reactions is comparable for all the cephalosporins although there are slight differences in both the incidence and the type of reactions . The major categories of adverse reactions are gastrointestinal, dermatologic, hypersensitivity, haematologic, hepatic, renal as well as CNS effects . Alcohol intolerance (antabus-like effect) can occur when cephalosporins containing the NMTT moiety are administered concomitantly.(ABSTRACT TRUNCATED AT 250 WORDS)

Acta Pharm Nord, 1991, 3(4), 211 - 4
Structure elucidation of the photolysis and hydrolysis products of tinidazole; Salomies H; A labile intermediate in the photolytic rearrangement of the antibacterial drug tinidazole was isolated after photolysis of the drug in acetone . The intermediate was identified through structural studies as 1-{2-(ethylsulphonyl)ethyl}-2-methyl-4-hydroxyimino-5-oxo-im idazole . A second product was identified as N-{2-(ethylsulphonyl)ethyl}-5-methyl-1,2,4-oxadiazole-3-carboxa mid e . A different compound, N-{2-(ethylsulphonyl)ethyl}-oxamide, crystallized in an ethanolic solution of tinidazole exposed for four months on a sunny window sill . Tinidazole was hydrolyzed completely to 2-methyl-5(4)-nitroimidazole when refluxed in 0.1 M NaOH solution, and was converted to 4-nitro isomer when refluxed in water with a catalytic amount of base.

Acta Oncol, 1991, 30(8), 975 - 80
Acute radiation effects on saliva composition in rats with different vitamin A levels in serum; Funegard U et al.; Irradiation of the head and neck often causes loss of salivary gland function which may lead to severe oral discomfort . The effects of a single dose of 25 Gy given to rats with different serum levels of vitamin A were studied . The salivary secretion rate as well as concentrations of protein, hexosamine, amylase and electrolytes, and the activities of two antibacterial glycoproteins were measured . At an adequate level of vitamin A in the diet, irradiation significantly reduced whole saliva secretion rate, and decreased the concentration of salivary sodium, calcium and hexosamine as well as the activity of a glycoprotein agglutinating a serotype c strain of S . mutans . Peroxidase, amylase and potassium were not significantly affected . The reductions seen at an adequate level of vitamin A were not reduced by supplementation of excess dietary retinol . The damage caused by irradiation was enhanced by vitamin A deficiency as seen in the reduced protein and hexosamine concentrations.

Scand J Gastroenterol Suppl, 1991, 187, 9 - 22
Spiral organisms: what are they? A microbiologic introduction to Helicobacter pylori; Lee A; The stomach provides a hostile environment to most microorganisms owing to the antibacterial effect of gastric acidity . However, over the period of mammalian evolution a highly specialized group of bacteria has evolved to inhabit the gastric mucosa . The common features of these bacteria that allow survival in the stomach and colonization of their natural ecologic niche, mucus, are a specialized form of motility, microaerophilism, and very high activity of the enzyme urease . Other important adaptations have been the acquisition of sophisticated mechanisms to evade host defences, and in certain cases tissue damage may result . The most important of these usually spiral-shaped bacteria is Helicobacter pylori . It is proposed that this bacterium is the human gastric spirillum that in most persons lives in harmony with its natural host, resulting in asymptomatic infection . However, if as yet undefined conditions are present, serious disease may result-that is, peptic ulceration . A consequence of long-term infection may be atrophic gastritis, which sets the scene for gastric carcinoma . The more the microbiology of the stomach is studied, the more species of Helicobacter are discovered, such as H . mustelae in the ferret, H . felis in cats and dogs, and 'Gastrospirillum hominis' in primates, cats, dogs, and pigs . These other helicobacters provide us with a wide spectrum of animal models of gastroduodenal disease . To understand mechanisms of pathogenesis, it is suggested that systematic study of all members of the genus will identify important colonizing factors and provide a realistic perspective on the putative virulence factors that have been proposed for H . pylori to date.

Dev Comp Immunol, 1991 Fall, 15(4), 241 - 50
Induction of immunity by latex beads and by hemolymph transfer in Galleria mellonella; Wiesner A; Injection of sterile latex beads into the hemocoel of last instar larvae of Galleria mellonella provoked a strong defense reaction . Cellular defense by hemocytes was followed by enhanced antibacterial activity in hemolymph . Latex-injected insects showed increased survival rates after a challenge injection with high doses of bacteria . Factors which stimulate the production of antibacterial activity could be demonstrated soon after injection by transfer of hemolymph from preinjected to untreated larvae . A large induction capacity in donor hemolymph was accompanied by a strong decrease in the total hemocyte count of free floating hemocytes, resulting from a decrease in number of plasmatocytes and granular cells, the cell types involved in the cellular defense against the injected latex beads . The results presented support the hypothesis that during cellular defense reactions, factors are released from the hemocytes which stimulate the production of antibacterial substances.

Chin J Biotechnol, 1991, 7(1), 33 - 42
Coloning and expression of spiramycin polyketide synthase genes and resistance genes from S . spiramyceticus U-1941; Tang L et al.; The plasmid containing the spiramycin polyketide synthase genes, pCN3H8, was obtained from the genomic library of spiramycin producing strain, S . spiramyceticus U-1941, using homologous DNA to actI and actIII genes as hybridization probes . Restriction analysis of the plasmid pCN3H8 showed that the molecular weight was 44kb . The regions homologous to the actI & actIII genes were localized by Southern hybridization, and corresponding DNA fragments were subcloned onto E . coli-Streptomyces shuttle vector pWHM3 . A recombinant plasmid pCG4 was obtained . Transformation of the pCN3H8 DNA into the polyketide synthase deficient mutant of midecamycin producing strain, S . mycarofaciens subsp . No . 68, resulted in the production of midecamycin A by UV analysis . Transformation of the pCN3H8 DNA into the polyketide synthase deficient mutant of actinorhodin producing strain, S . coelicolor TK17, resulted in the production of an antibacterial compound which was neither similar to actinorhodin in color nor to spiramycin by paper chromatographic analysis . Transformant of S . lividans with pCN3H8 DNA produced an antibacterial compound as well . Resistance to spiramycin was expressed in transformants of spiramycin sensitive strain, S . griseofuscus, with pCN3H8 DNA . A plasmid pSG3 DNA with molecular weight of 7.0kb, isolated from the transformant, might be a result of in vivo deletion of pCN3H8 in S . griseofuscus . Retransformation of pSG3 DNA into S . griseofuscus confirmed that the gene of resistance to spiramycin was on the plasmid pSG3 DNA . Transformation of spiramycin producing strain, S . ambofaciens, with pCG4 or pSG3 DNA increased spiramycin production in fermentation broth.

Arkh Patol, 1991, 53(9), 70 - 3
{Neutrophilic granulocytes and host defense systems}; Mazing IuA; The review shows that neutrophil granulocytes play a key role in the host defence against infection diseases . An important role belongs to the antibacterial cation proteins . Their study allows to create new methods of rapid diagnosis of the host resistance . The use of one of such tests (lysosome-cationic one) showed its high efficiency in the assessment of the disease gravity and the prognosis of complications.

Immunopharmacol Immunotoxicol, 1991, 13(1-2), 135 - 46
Effects of acetyl-L-carnitine oral administration on lymphocyte antibacterial activity and TNF-alpha levels in patients with active pulmonary tuberculosis . A randomized double blind versus placebo study; Jirillo E et al.; Acetyl-L-carnitine (ALC), a drug for the treatment of ageing-related neuroendocrine dysfunctions, was orally administered--2 gm/day for 30 days--to 10 patients with active pulmonary tuberculosis (TBC) . Lymphocyte-mediated antibacterial activity and serum levels of tumor necrosis factor (TNF)-alpha were evaluated before and after treatment, comparing the values with those of 10 TBC patients receiving placebo . Results show that by day 30, antibacterial activity remained unmodified or increased in ALC-treated subjects, while decreased in the placebo group . No influence of ALC on TNF-alpha levels was detectable . These data suggest that the host's immune responses to M . tuberculosis infection can be selectively modulated by drugs acting on the neuroendocrine axis.

Am J Chin Med, 1991, 19(3-4), 223 - 31
Pharmacological studies on aerial parts of Calotropis procera; Mossa JS et al.; The decoction of the aerial part of Calotropis procera is commonly used in Saudi Arabian traditional medicine for the treatment of variety of diseases including fever, joint pain, muscular spasm and constipation . The present investigation was undertaken to confirm its claimed activity in traditional medicine . The ethanol extract of the plant was tested on laboratory animals for its antipyretic, analgesic, anti-inflammatory, antibacterial, purgative and muscle relaxant activities . The results of this study showed a significant antipyretic, analgesic and neuromuscular blocking activity . On smooth muscle of guinea pig ileum, the extract produced contractions which was blocked by atropine supporting its use in constipation . The extract failed to produce significant anti-inflammatory and antibacterial activities . Our phytochemical studies on the aerial parts of C . procera showed the presence of alkaloids, cardiac glycosides, tannins, flavonoids, sterols and/or triterpenes . However, the chemical constituents responsible for the pharmacological activities remains to be investigated . The safety evaluation studies revealed that the use of extract in single high doses (up to 3 g/kg) does not produce any visible toxic symptoms or mortality . However, prolong treatment (90 days) causes significantly higher mortality as compared to control group.

Klin Khir, 1991, (9), 15 - 8
{Preoperative antibacterial therapy in the comprehensive treatment of patients with external biliary fistulas}; Shalimov SA et al.; The experience with antibacterial therapy in 120 patients with choledocholithiasis and cicatricial stricture of the bile ducts complicated by the development of an external biliary fistula is summarized . It was established that intravenous administration of antibiotics at the maximum dosages with purposeful sanation of the bile ducts via the external biliary fistula at the preoperative period improved the immediate and long-term results of treatment of the patients . Only in full-value, adequate correction of disorders in the major bile outflow, the reliable elimination of the external biliary fistula is possible.

Klin Khir, 1991, (9), 1 - 4
{Diagnosis and principles of treatment of obstructive purulent cholangitis}; Shalimov SA et al.; Having substantiated the results of treatment of 425 patients with purulent cholangitis caused by benign obstruction of the bile ducts, the authors suggest their definition of "purulent cholangitis" . The two-stage operative interventions were used . At the first stage, the sparing decompression of the bile ducts, and as well rational regional antibacterial therapy were performed . The lethality reduced from 3 to 1.3%, purulent cholangitis was cupped off in 98.7% of the patients . The indications, methods for performance of endoscopic papillotomy, and as well of closed interventions in obstruction of the bile ducts with the use of a transcutaneous transhepatic approach are presented.

Crit Rev Biotechnol, 1991, 11(3), 193 - 276
Detection of novel secondary metabolites; Franco CM et al.; The study of antibiotics and other fermentation products has shown that a seemingly unlimited number of compounds with diverse structures are produced by microorganisms . The continued high rate of discovery of new chemical entities, in the light of the abundance of microbial products already described, is due to creative screening procedures that incorporate such features as the emphasis on unusual microorgnaisms, their special propagation and fermentation requirements, supersensitive and highly selective assays, genetic engineering both for the biosynthesis of new compounds and in the development of screening systems, early in vivo evaluation, improved isolation techniques, modern procedures for structure determination, computer-assisted identification, and an efficient multidisciplinary approach . This review focuses on the genesis and development of the gamut of methodologies that have led to the successful detection of the wide variety of novel secondary metabolites that include antibacterial, antigungal, antiviral and antitumour antibiotics, enzyme inhibitors, pharmacologically and immunologically active agents, products useful in agriculture and animal husbandry, microbial regulators, and other compounds for which no bioactive role has yet been found.

Ter Arkh, 1991, 63(9), 121 - 5
{Kidney involvement in infectious endocarditis (hematuria)}; Demin AA et al.; As many as 113 patients suffering from infectious endocarditis (IE) were placed under observation . Renal damage was discovered in 28 patients (24.7%) . Hematuria was the common laboratory sign of renal damage . 15% of patients showed microhematuria, 9.7 had macrohematuria . In 15% of patients with IE, hematuria was due to diffuse glomerulonephritis, in 5.3% to renal infarction, and in 4.4% to focal glomerulonephritis . In 3.5% of patients, the nephrotic syndrome developed at the disease onset, it was attended by hematuria and was thus a cause of erroneous diagnoses . The appearance of hematuria at the IE onset, attesting to involvement of the kidneys into the pathological process, complicates the diagnosis and early treatment institution . Detection of the hematuric syndrome in patients with a verified diagnosis of IE requires specification of the character of renal damage . The latter one contributes to a graver and prognostically unfavourable course of IE . In 2 out of 8 patients with associated IE and renal damage, the death was caused by progressive chronic renal failure . Postmortem examination confirmed mesangioproliferative glomerulonephritis in all the subjects; in 4, it was coupled with renal infarction . 14.1% of the patients manifested complete and 3.5% partial disappearance of hematuria under the influence of adequate antibacterial therapy of IE.

Probl Tuberk, 1991, (8), 52 - 5
{Extra-focal instrumental fixation of the spine in the surgical treatment of tuberculous spondylitis}; Lavrov VN; The complex procedure for treating tuberculous spondylitis involving a short-term (1-2 months) antibacterial therapy and early functional resection of the diseased vertebral bodies with defect replacement by an autograft and extra-focal fixation of the resected spinal portion by Byzov's apparatus applied in 492 patients proved to be highly efficacious . The reliable apparatus fixation of the spinal zone operated on allows early (on day 7) activation of patients which promotes functional normalization of organs and systems, activation of reparative processes, shortening of treatment duration and reduction of disabled cases . Clinical and X-ray findings show that a bone block formed 4-6 months after surgery and 67% of the patients finished their therapy during a year . Introduction of the procedure into the treatment of spinal injuries and diseases will be of the socioeconomical value.

Probl Tuberk, 1991, (8), 49 - 51
{Problem of cutaneous tuberculosis}; Kratule RV et al.; Case histories of 97 patients were analysed to study the diagnosis, differential diagnosis and incidence of recurrences of tuberculosis of the skin . A combined examination revealed Basin erythema in 57.7% of the patients, lupus vulgaris in 29.9% and papulonecrotic tuberculosis of the skin in 12.4% . Recurrences were recorded in 15.4% of the cases . Our study gives evidence that tuberculosis of the skin is diagnosed from the combined examination of the patient in which histologic study of a skin biopsy specimen is most essential . The differential diagnosis of tuberculosis of the skin makes difficult the distinction between the disseminated forms and allergic vasculitis and sarcoidosis of the skin . The relapse depends on how adequate the major and antirecurrence courses of antibacterial therapy were.

Probl Tuberk, 1991, (7), 37 - 40
{Diagnosis of mycotic infections in patients with tuberculosis of the respiratory organs}; Solov'eva TN et al.; The basic clinico-diagnostic criteria are given which detect an intercurrent infection caused by opportunistic fungi of the Candida and Aspergillus genus . The antibacterial drugs of nonspecific action used in patients with destructive forms of respiratory tuberculosis promote the growth and reproduction of fungus flora and aggravate the course of the underlying process in the lung tissue . When there is intercurrent mycotic infection, the antifungal therapy produces a clinical effect in patients with combined pathology.

Nauchnye Doki Vyss Shkoly Biol Nauki, 1991, (9), 131 - 5
{The effect of the acidity of the medium on the magnitude of the light-dependent antibacterial activity of chlorophyllides}; Maksimova IV et al.; The influence of medium acidity on the intensity of light-dependent antibacterial activity of chlorophyllides isolated from biomass of microscopic green alga Westella botryoides has been studied . This light-dependent antibacterial activity has been shown to be maximum at low pH values . The ability to suppress the bacterial growth under the action of light decreases in neutral and alkaline media . It has been concluded that the reason of increase of light-dependent antibacterial activity of chlorophyllides at low pH values is formation of pheophorbides out of them

Vestn Akad Med Nauk SSSR, 1991, (9), 24 - 7
{A goal-oriented local approach to the prevention of postoperative suppurative complications}; Kanshin NN et al.; A goal-oriented local approach to the prevention of postoperative purulent complications includes the use of compression suture devices to establish intestinal anastomoses and a complex of measures aimed at preventing surgical wound suppurations . To form compression anastomoses, use was made of the original AKA-2, AKA-4, IZhKA and SPTU devices fitted with compression clamps and of magnet facilities . The complex of measures to prevent postoperative wound suppurations includes optimal methods of laparotomy wound suture and the use of antibacterial suture materials, bathing of the wound by pulsed douche under pressure, local antibacterial prophylaxis by new dosage forms, preventive aspiration lavage and drainage of the wounds . Comparative clinical investigations carried out in more than 3,000 patients have demonstrated the effectiveness of the preventive methods under consideration and a decrease of the rate of postoperative wound suppurations from 11.7 to 2.3% . The rate of anastomosis failure amounted to 2.7%.

Respiration, 1991, 58(3-4), 145 - 9
Long-term low-dose administration of erythromycin to patients with diffuse panbronchiolitis; Nagai H et al.; Although diffuse panbronchiolitis (DPB) has carried a poor prognosis, long-term low-dose administration of erythromycin (EM) is very effective . We administered EM at a daily dose of 400-600 mg to 19 DPB subjects for more than 2 months . Sixteen subjects were relieved from productive cough and dyspnea, and their chest X-ray pictures were improved . We performed a pharmacokinetic study of EM in 11 DPB subjects (8 responders; 3 nonresponders) after the long-term low-dose administration . The maximal serum and sputum levels of EM were below the MICs of clinically pathogenic H . influenzae and P . aeruginosa which were often isolated from the sputum of DPB patients . No difference was observed in the absorption of EM between responders and nonresponders . The results suggested that DPB patients might respond favorably to EM due to mechanisms other than antibacterial activity . Individual variation in the absorption of EM was observed . As EM was effective at very low serum and sputum levels, it was suggested that even 200 mg/day of EM would be effective in DPB patients who had high serum and sputum EM levels and it was necessary to monitor the concentrations of EM in serum and sputum for the treatment of DPB to determine the appropriate dose of EM individually.

Drugs, 1991, 42 Suppl 3, 57 - 60
Clinical trials of cefpodoxime proxetil suspension in paediatrics; Fujii R; The pharmacokinetics, bacteriological and clinical efficacy, and safety of the suspension formulation of cefpodoxime proxetil, an oral cephalosporin antibacterial, were evaluated in paediatric patients with various infections . With single doses of 3 and 6 mg/kg (cefpodoxime equivalent) a dose response was evident in the serum concentration values . Absorption, as evidenced by serum concentrations and areas under the concentration-time curve, was enhanced when the suspension was administered before a meal . The overall clinical efficacy (defined as an excellent or good response) in evaluable patients (those from whom a pathogen was isolated) was 94.7% (451 of 476) . Bacteriological eradication rates were as follows: Gram-positive bacteria 91.3%; Gram-negative bacteria 88.6%, and 90.0% overall . Side effects occurred in 17 (2.29%) patients, and transient and reversible abnormal laboratory values were found in a few patients.

Drugs, 1991, 42 Suppl 3, 13 - 21
A review of the pharmacokinetics of cefpodoxime proxetil; Borin MT; Cefpodoxime proxetil is an orally absorbed broad spectrum third generation cephalosporin antibacterial . It is a prodrug that is de-esterified in vivo to its active metabolite, cefpodoxime . After single- and multiple-dose (12-hourly) administration of cefpodoxime proxetil in the therapeutic dose range of 100 to 400mg of cefpodoxime equivalents, average peak plasma concentrations of cefpodoxime range from 1.0 to 4.5 mg/L and occur between 1.9 and 3.1 hours after administration . The half-life of cefpodoxime ranges from 1.9 to 2.8 hours . The absolute bio-availability of cefpodoxime proxetil tablets is 50%, and absorption is enhanced by concomitant administration of food . Raising gastric pH by pretreatment with antacids or H2-receptor antagonists results in reduced absorption . Binding of cefpodoxime to human plasma or serum protein is low (18 to 23%), suggesting that cefpodoxime should readily transfer across the capillary lining into tissues . Cefpodoxime undergoes minimal metabolism in humans . Drug not absorbed is degraded in the gastrointestinal tract and excreted in the faeces . As expected for a drug eliminated primarily by renal excretion, the disposition of cefpodoxime is altered in patients with impaired renal function; the half-life increases, while apparent plasma clearance and renal clearance decrease . The pharmacokinetics of cefpodoxime after oral administration of cefpodoxime proxetil are not affected by age.

Drugs, 1991, 42 Suppl 4, 25 - 9
Cefixime vs amoxicillin in the treatment of acute otitis media in infants and children; Principi N et al.; Cefixime is a new oral cephamycin antibiotic with a broad spectrum of antibacterial activity in vitro . It is resistant to hydrolysis by most beta-lactamases and has pharmacokinetic characteristics which allow administration in a single daily dose for the treatment of some bacterial infections . The aim of this study was to compare the clinical efficacy of cefixime with that of amoxicillin in the treatment of acute otitis media in 40 children . Cefixime 8 mg/kg was given once daily at bedtime, whereas amoxicillin 50 mg/kg/day was administered in 3 divided doses; both drugs were given for 10 days . 15 days after starting the trial, a favourable clinical response was demonstrated in 18 of 20 children in both treatment groups . Cure rates, recurrences and persistent middle ear effusions were not significantly different in the 2 study groups during a 3-month follow-up . It was concluded that cefixime is clinically effective and well tolerated in the treatment of children with acute otitis media.

Drugs, 1991, 42 Suppl 4, 10 - 3
Single dose oral administration of cefixime 400mg in the treatment of acute uncomplicated cystitis and gonorrhoea; Asbach HW; A placebo-controlled prospective randomised double-blind study was performed in 80 consecutive female outpatients with acute cystitis . Single dose oral antibiotic treatment was successful in 89.4% of patients treated with cefixime 400mg or ofloxacin 200mg and in 84.2% of those receiving cotrimoxazole (160/800mg) . Bacteriuria was eradicated in 26.3% of patients in the placebo group . Two noncomparative clinical trials involving a total of 43 male patients with acute gonococcal urethritis reported a 100% cure rate after administration of a single 400mg dose of cefixime . Such single dose regimens offer the advantages of reduced expense, good tolerability, minimal alteration of normal bacterial flora, and the potential for improved patient compliance, compared with multiple dose antibacterial therapy.

Lab Delo, 1991, (7), 64 - 6
{A method of determining the content of antibiotics in tears and liquid media of the eye}; Somov EE et al.; The authors have developed a simple highly accurate method for measuring antibiotic concentrations in liquid media of the eye . It is based on the ability of antibacterial drugs to diffuse in agar medium . The studies may be carried out at any bacteriologic laboratory.

Adv Exp Med Biol, 1991, 288, 245 - 53
The effects of ethanol, tumor necrosis factor, and granulocyte colony-stimulating factor on lung antibacterial defenses; Nelson S et al.; In summary, evidence is emerging indicating that alcohol-abusing hosts are seriously undermined by profound disturbances in cytokine production and activity . These alterations likely play a critical role in the development and clinical sequelae of their immunosuppressed status . Recombinant technology currently provides the clinician with the potential to immunologically reconstitute and restore host defenses in these hosts . While the ultimate role of these agents in patients will require extensive clinical investigations into their multiple biologic effects and interactions, cytokines, when properly employed, will likely have a major impact on the prevention and treatment of many life-threatening diseases . For the first time, we possess the potential to regulate essential functions of the host defense system which may prevent the development and mitigate the severity of infections in these and other immunocompromised hosts.

Folia Microbiol (Praha), 1991, 36(6), 538 - 41
Streptomyces species producing the streptovaricin complex; Vesselinova N et al.; Morphological, cultural and physiological-biochemical properties of Streptomyces sp . strain 1000 and its antibiotic production were investigated . Antibiotics 1011 (identical with the streptovaricin complex) and 1012 (with antibacterial action) were isolated from the cultural broth of this strain . The overproducing natural variant 1011 was isolated from the population of a strain producing antibiotic 1011 at a concentration of 1000 mg/L (activity of the parent strain represents 41 mg/L only) . Comparative taxonomical characteristic of Streptomyces sp . strain 1000 with strains from S . spectabilis showed that the strain 1000 differed in some properties and antibiotic production being considered as a new variant of S . spectabilis . The strain shows an expressed antibiotic activity against G+ as well as G- bacterial and yeasts.

Ter Arkh, 1991, 63(11), 135 - 8
{The overdiagnosis of bacterial endocarditis}; Demin AA et al.; The diagnosis of bacterial endocarditis (BE) is analyzed in 255 patients . After examination, the diagnosis of BE was verified but in 92 patients (36.1%) . Of these, BE was overdiagnosed in 163 patients (63.9%) . The main causes of the overdiagnosis were body temperature rise in 134 patients (52.6%), heart murmur in 163 patients (63.9%), and positive hemoculture in 57 patients (22.3%) . Three cases of BE overdiagnosis are provided . Exaggeration of the specificity of body temperature rise in patients with heart murmur often leads to BE overdiagnosis . Mitral valve prolapse is one of the predisposing BE factors . At the same time it is a cause of overdiagnosis of BE in patients with fever, BE overdiagnosis often results in unbased long-term antibacterial therapy, while other causes of the symptoms are not considered . Ineffectiveness of antibacterial treatment (no clinical improvement, continuous or recurrent fever) points to the necessity of further diagnostic search.

Arch Inst Pasteur Madagascar, 1991, 59(1), 9 - 23
{Preliminary study of the prevalence of Helicobacter pylori in Tananarive, Madagascar and the antibacterial activity in vitro of 13 Malagasy medicinal plants on this germ}; Cassel-Beraud AM et al.; Helicobacter pylori infection has been studied in 60 patients who were suffering from either a peptic ulcer disease or a gastritis complaint . Helicobacter pylori was searched in antral biopsy specimens using standard bacteriological methods (Gram-staining urea-test, culture) and histological staining techniques (hematoxylin-eosin-saffron, undifferentiated Giemsa) . The culture was successful in 40 cases . The antibacterial activity of 13 malagasy medicinal plants has been tested versus Helicobacter pylori using disc method on agar culture . For five extracts, we observed an anti-Helicobacter pylori activity which would deserve further investigations.

Zh Nevropatol Psikhiatr Im S S Korsakova, 1991, 91(6), 16 - 8
{Convulsive conditions in somatic pathology of infectious etiology in children with perinatal brain injury}; Bondyrev AI et al.; Convulsive conditions account for 69.8% out of the total number of patients admitted to the department of intensive care of the children's neurological hospital . In 25.3% (348 children) they first developed in the presence of somatic pathology of the infectious inflammatory genesis in children with perinatal brain injury . Acute somatic pathology (acute respiratory diseases, pneumonia, intestinal infections) dominated (n = 318) . In all the children, convulsive seizures occurred in hyperthermia largely in early childhood . Apparently, in the majority of cases, perinatal injury alone was insufficient to precipitate seizures . However, the combined perinatal brain injury and an infectious disease form favourable conditions for the appearance of convulsive conditions in children . Therefore, to prevent them, of importance is the prophylaxis of both perinatal pathology and infectious diseases . The patients with convulsive conditions should be given combined treatment including anticonvulsants, antiinflammatory, antibacterial, detoxication and other drugs.

Yao Xue Xue Bao, 1991, 26(4), 299 - 302
{Syntheses of 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-{(4-P-nitrobenzol)-1- piperazinyl} quinoline-3-carboxylic acid and its analogues}; Chen HC et al.; Syntheses of thirteen new compounds of 1-ethyl-6-flouro-1, 4-dihydro-4-oxo-7-{(4-p-nitrobenzoyl)1-piperazinyl} quinoline-3-carboxylic acid and its analogues are reported . The structures were determined by IR, 1HNMR and elemental analysis . Four compounds have been subjected to antibacterial activity tests in vitro . Compound I1 was shown to have significant activity.

Crit Rev Biochem Mol Biol, 1991, 26(3-4), 335 - 75
DNA gyrase: structure and function; Reece RJ et al.; DNA gyrase is an essential bacterial enzyme that catalyzes the ATP-dependent negative super-coiling of double-stranded closed-circular DNA . Gyrase belongs to a class of enzymes known as topoisomerases that are involved in the control of topological transitions of DNA . The mechanism by which gyrase is able to influence the topological state of DNA molecules is of inherent interest from an enzymological standpoint . In addition, much attention has been focused on DNA gyrase as the intracellular target of a number of antibacterial agents as a paradigm for other DNA topoisomerases . In this review we summarize the current knowledge concerning DNA gyrase by addressing a wide range of aspects of the study of this enzyme.

Arch Toxicol, 1991, 65(6), 495 - 9
Important role of oxygen metabolites in quinolone antibacterial agent-induced cutaneous phototoxicity in mice; Wagai N et al.; We investigated whether or not the generation of reactive oxygens and toxic photoproducts participated in the cutaneous phototoxicity mechanisms induced by the quinolone derivatives, ofloxacin (OFLX), enoxacin, lomefloxacin, ciprofloxacin and DR-3355 (the s-isomer of OFLX) in a mouse model . Pretreatment of Balb/c mice with allopurinol, soybean trypsin inhibitor, catalase and beta-carotene gave significant protection against ear swelling reactions induced by oral administration of quinolones and following ultraviolet-A (UVA) irradiation . Pretreatment with diethyldithiocarbamate augmented the swelling . No swelling was observed with direct injection into the auricle of UVA-pretreated photoproducts of the quinolones . These results showed that cutaneous phototoxicity did not depend on the generation of toxic photoproducts and suggested that oxygen metabolites generated in the xanthine oxidase pathway participated in the toxicity.

Chemotherapy, 1991, 37 Suppl 1, 2 - 13
Ofloxacin, a bactericidal antibacterial; Smith JT; Ofloxacin, like other 4-quinolones, is unusual among front line drugs available to treat bacterial infections since it affects bacterial DNA synthesis, rather than cell wall or protein synthesis . The 4-quinolones are also unusual because even for serious infections they can be given orally . Most unusually transferable resistance mediated by plasmids does not affect the 4-quinolone antibacterials . Thus the only way that bacteria can resist these drugs is by chromosomal mutation . However, when mutants gain resistance, they can also lose pathogenicity, and even should mutants remain pathogenic then their resistance cannot transfer to other bacteria by conjugation.

J Biol Chem, 1990 Dec 25, 265(36), 22493 - 8
Insect immunity . Characterization of a Drosophila cDNA encoding a novel member of the diptericin family of immune peptides; Wicker C et al.; Drosophila shows an immune response when challenged by injection of low doses of bacteria . To date, the molecules involved in this immune reaction have remained elusive, with the exception of cecropins (4-kDa antibacterial peptides initially isolated from the moth Hyalophora cecropia) for which three closely related genes have been characterized recently . We report the molecular cloning and sequencing of a cDNA from a library of immune Drosophila which encodes a novel member of the family of diptericins (9-kDa antibacterial peptides initially isolated from the fly Phormia terranovae) . Transcripts for the Drosophila diptericin are detected 2 h after injection of bacteria . They are apparently derived from a single gene mapping at position 56 A on the right arm of the second chromosome . We discuss the existence of a distant relationship between the diptericins and two other groups of anti-bacterial insect proteins, the attacins, and the sarcotoxins II.

Science, 1990 Dec 21, 250(4988), 1729 - 32
Hemolin: an insect-immune protein belonging to the immunoglobulin superfamily; Sun SC et al.; Insects have an efficient defense system against infections . Their antibacterial immune proteins have been well characterized . However, the molecular mechanisms by which insects recognize foreignness are not yet known . Data are presented showing that hemolin (previously named P4), a bacteria-inducible hemolymph protein of the giant silk moth Hyalophora cecropia, belongs to the immunoglobulin superfamily . Functional analyses indicate that hemolin is one of the first hemolymph components to bind to the bacterial surface, taking part in a protein complex formation that is likely to initiate the immune response.

Biochem J, 1990 Dec 15, 272(3), 633 - 6
Production of recombinant sarcotoxin IA in Bombyx mori cells; Yamada K et al.; A cDNA for sarcotoxin IA, an antibacterial protein of Sarcophaga peregrina (fleshfly), was inserted into a silkworm baculovirus vector and expressed in Bm-N cells, a line of Bombyx mori cells . When a cysteine proteinase inhibitor, p-chloromercuribenzenesulphonic acid, was present in the culture medium, a significant amount of recombinant sarcotoxin IA accumulated, but without this reagent the product seemed to be degraded in this system . The C-terminus of the recombinant sarcotoxin IA seemed to be glycine, not amidated arginine as found in authentic sarcotoxin IA . Probably, Bm-N cells lack the C-terminal alpha-amidation enzyme.

Onderstepoort J Vet Res, 1990 Dec, 57(4), 239 - 41
Failure of an Actinomyces pyogenes vaccine to protect sheep against an intravenous challenge; Hunter P et al.; The immunity conferred by an A . pyogenes bacterin-toxoid was evaluated in sheep, using an intravenous challenge system . Three sheep were vaccinated and 3 served as controls . The vaccinated sheep were not protected against pyogenic conditions . High antitoxin levels were induced by vaccination but could not be associated with protection against infection . Antibacterial antibody levels elicited with initial vaccination dropped progressively with the 2nd and 3rd vaccinations . Nevertheless, these antibodies did not seem to be necessary for protection against A . pyogenes conditions.

J Antibiot (Tokyo), 1990 Dec, 43(12), 1513 - 8
The kapurimycins, new antitumor antibiotics produced by Streptomyces . Producing organism, fermentation, isolation and biological activities; Hara M et al.; As a result of screening for antitumor agents from actinomycetes, the kepurimycins were isolated from Streptomyces sp . DO-115 . The antibiotics were produced in a fermentation medium supplemented with high porous polymer resin which adsorbs antibiotics and results in an increase of titer . The active complex was isolated from the polymer resin by a solvent extraction procedure and was separated by column chromatography, into two minor and one major component, named A1, A2 and A3 . The kepurimycins were active against bacteria, particularly Gram-positive organisms, and were cytotoxic to HeLa S3 human cerivical cancer cells and T24 human bladder carcinoma cells in vitro . Among the individual components of the kapurimycins, kapurimycin A3 exhibited the strongest antibacterial and cytotoxic activities . It showed a potent antitumor activity against murine leukemia P388 in vivo.

Br J Ophthalmol, 1990 Dec, 74(12), 734 - 8
Randomised single blind trial to compare the toxicity of subconjunctival gentamicin and cefuroxime in cataract surgery; Jenkins CD et al.; Comparatively little attention has been paid to the conjunctival toxicity of antibiotics administered at the time of cataract surgery . We have observed the effect of subconjunctival gentamicin and cefuroxime injection, using colour photography in a randomised single blind trial of 121 patients undergoing routine cataract surgery . Our results suggest that a hyperaemic eye is likely to occur about twice as often in patients injected with gentamicin (p less than 0.001) . Gentamicin is associated with more pain postoperatively (p less than 0.05) . Significant manifestations of gentamicin toxicity are conjunctival oedema and capillary closure . Cefuroxime has some theoretical advantages over gentamicin in its antibacterial spectrum.

J Am Acad Dermatol, 1990 Dec, 23(6 Pt 1), 1039 - 58
Toxic epidermal necrolysis (Lyell syndrome); Roujeau JC et al.; Toxic epidermal necrolysis is perhaps the most formidable disease encountered by dermatologists . Uncommon but not rare, toxic epidermal necrolysis occurs in 60 to 70 persons per year in France . It remains as puzzling a disorder as it was 34 years ago, when described by Lyell . Whether or not toxic epidermal necrolysis is the most severe form of erythema multiforme is still the subject of discussion . The physiopathologic events that lead to this rapidly extensive necrosis of the epidermis are not understood . Indirect evidence suggests a hypersensitivity reaction, but the search for potential immunologic mechanisms has resulted in little data to support this hypothesis . Accumulated clinical evidence points to drugs as the most important, if not the only, cause of toxic epidermal necrolysis . Sulfonamides, especially long-acting forms, anticonvulsants, nonsteroidal anti-inflammatory agents, and certain antibiotics are associated with most cases of toxic epidermal necrolysis . Many other drugs have been implicated in isolated case reports . All organs may be involved either by the same process of destruction of the epithelium as observed in the epidermis or by the same systemic consequences of "acute skin failure" as seen in patients with widespread burns . Sepsis is the most important complication and cause of death . Approximately 20% to 30% of all patients with toxic epidermal necrolysis die . Elderly patients and patients with extensive lesions have a higher mortality rate . Surviving patients completely heal in 3 to 4 weeks, but up to 50% will have residual, potentially disabling ocular lesions . The prognosis is improved by adequate therapy, as provided in burn units, that is, aggressive fluid replacement, nutritional support, and a coherent antibacterial policy . Corticosteroids, advocated by some in high doses to halt the "hypersensitivity" process, have been shown in several studies to be detrimental and should be avoided.

Toxicol Lett, 1990 Dec, 54(2-3), 299 - 308
Phototoxic potential of quinolone antibacterial agents in Balb/c mice; Wagai N et al.; The phototoxic potentials of quinolone antibacterial agents were investigated in Balb/c strain mice . The mice were orally administered nalidixic acid (NA), enoxacin (ENX), ofloxacin (OFLX), ciprofloxacin (CPFX), lomefloxacin (LMFX) and DR-3355 (s-isomer of OFLX), and immediately exposed to ultraviolet-A (UVA) for 4 h (21.6 joules/cm2) . The ears were examined for overt damage, as a major phototoxic parameter, 0, 24 and 48 h after irradiation ended . At doses of 200 mg/kg, LMFX, NA and ENX caused marked cutaneous phototoxic reactions on the ears, whereas CPFX, OFLX and DR-3355 caused none . At 800 mg/kg, however, CPFX, OFLX and DR-3355 also caused phototoxic reactions on the ears . These phototoxic changes were characterized grossly by erythema, and histopathologically by edema and infiltration of inflammatory cells, especially neutrophils, into the connective tissue surrounding the cartilage . The 50% erythema-inducing doses of LMFX, ENX, NA, OFLX, DR-3355 and CPFX were calculated at 19, 102, 143, 553, 619 and 741 mg/kg, respectively . Thus, the phototoxic potencies of the quinolones tested were: LMFX greater than ENX, NA greater than OFLX, DR-3355, CPFX.

Am J Obstet Gynecol, 1990 Dec, 163(6 Pt 2), 2153 - 9
Interactions with oral contraceptives; Fotherby K; The interaction of a range of different factors with the pharmacologic activity of oral contraceptives is reviewed . Pharmacokinetic interactions with oral contraceptives may occur (1) during absorption and extrahepatic circulation, (2) by interfering with protein binding, and (3) during hepatic metabolism . The hepatic mixed function oxidase system, which is mainly responsible for the metabolism of oral contraceptives, is affected by several different factors and is easily induced . Nutrition affects the activity of many drugs, but information regarding oral contraceptives is meager . Both pharmacokinetic and pharmacodynamic interactions, which may be synergistic or antagonistic, between the estrogen and gestagen components of oral contraceptives, are important, but there is no correlation between the rate of metabolism of the two components . Evidence suggests that some anticonvulsant, antibiotic, and antibacterial drugs may reduce the efficacy of oral contraceptives . Instances of interactions of other therapeutic agents are reported infrequently . The incidence of serious interactions is low and does not appear to have been reduced with low-dose oral contraceptives, probably because of large intersubject variability in the pharmacokinetics of oral contraceptivesPIP: Pharmacokinetic interactions between oral contraceptives (OCs) and other drugs and nutrients may occur during absorption and extrahepatic circulation, through interference with protein binding, and during hepatic metabolism . However, the most significant locus of drug interaction is the mixed function oxidase system of the liver endoplasmic reticulum . Increased activity of the mixed function oxidase system produced by other drugs tends to reduce the half-life of elimination of sex steroids and consequently of their serum concentrations and biological effect . At the same time, OC administration generally has an inhibitory effect on the metabolism of other drugs and consequent reductions in their pharmacologic activity . The rate of drug metabolism will vary according to genetic and environmental factors such as diet, alcohol use, smoking, and pathologic conditions . Although the influence of nutrition on the absorption and bioavailability of contraceptive steroids has not yet researched adequately, high-protein diets appear to stimulate the activity of the hepatic drug-oxidizing system and increase the metabolism of other drugs . Pharmacokinetic and pharmacodynamic interactions between the estrogen and gestogen components of OCs may be synergistic or antagonistic, but no correlation has been found between the rate of metabolism of the 2 steroids as reflected in their elimination half-lives . Despite evidence that some anticonvulsant, antibiotic, and antibacterial drugs reduce the efficacy of OCs, this interaction is severe enough to lead to OC failure in less than 5% of cases . It can be postulated that women in whom drug interactions lead to contraceptive failure are fast metabolizers or have liver enzyme systems especially susceptible to induction .

Mol Cell Biol, 1990 Dec, 10(12), 6114 - 22
Analysis of a gene cluster for sarcotoxin II, a group of antibacterial proteins of Sarcophaga peregrina; Kanai A et al.; Sarcotoxin II is a group of antibacterial proteins of Sarcophaga peregrina (flesh fly) with related primary structures . We have cloned three genes in this family . These genes formed a tandem array with about 2-kb intervals, and one of them was present in the opposite strand . The putative amino acid sequences of the proteins encoded by these genes were very similar except for a deletion in one of them . All of the genes were found to be activated transiently in the same way when the larval body wall was injured, suggesting that the encoded proteins are acute-phase-responsive proteins for protecting the insect from bacterial infection.

Oral Surg Oral Med Oral Pathol, 1990 Dec, 70(6), 748 - 55
Oral melanotic macules in patients infected with human immunodeficiency virus; Ficarra G et al.; A group of 217 patients seropositive for human immunodeficiency virus (HIV) were studied for 2 years, during which time pigmented lesions of the oral mucosa developed in 14 (6.4%) of them . The lesions were well circumscribed in some cases and diffuse in others . In some patients the macules enlarged or recurred after surgical excision . In two patients the macules appeared during the administration of zidovudine . Clinical and laboratory evidence of adrenal insufficiency was not detected in any of the patients examined . The histologic appearances were those of melanotic macules . No ultrastructural alterations of the melanocytes were observed . Two of these macules also contained Epstein-Barr virus, and in one case normal oral mucosa was examined and also contained Epstein-Barr virus in the epithelial cells . As a control group we examined 180 health care workers who did not belong to any risk category, and 30 intravenous drug abusers who tested seronegative to HIV . Oral melanotic pigmentation was found in eight of the control subjects (3.6%) . The difference was not statistically significant (p = 0.3097) . Our study shows that oral macules do not occur more frequently in HIV-infected patients . However, the clinical behavior of these lesions appears to be different during the course of HIV infection . In some HIV-infected patients the cause of the macules might relate to the administration of zidovudine and antifungal or antibacterial drugs . In others the cause remains unknown and could be due to multiple factors.

Am J Gastroenterol, 1990 Dec, 85(12), 1545 - 51
Drug therapy for Helicobacter pylori infection: problems and pitfalls; Glupczynski Y et al.; Antibacterial chemotherapy against Helicobacter pylori is currently being assessed by open or randomized controlled clinical studies for its efficacy in eradicating this bacterium from the stomach of patients with gastritis or gastroduodenal ulcer . Whereas there is presently no "optimal" agent and treatment scheme, the combination of some antibiotics (metronidazole, tinidazole, amoxicillin) with bismuth salts proves definitely superior in vivo to either of these agents administered alone . Several reasons have been proposed, to explain the clinical failure after treatment: insufficient concentration of active drugs in gastric mucus, instability of some agents at an acidic pH, inappropriate formulation of drug, insufficient duration of treatment, and variable compliance of patients . Recently, it has appeared from several clinical trials that H . pylori may rapidly acquire resistance to some antibiotics, and that this event might also account for clinical failure . A critical review of the literature on H . pylori treatment indicates that association of bismuth and antibiotics or of antibiotics alone both may efficiently reduce the risk of emergence of resistance and improve the therapeutic outcome . Guidelines of treatment are suggested in order to avoid the future misuse of antibiotics that would increase selection of antibiotic-resistant H . pylori and negatively affect the ecology of the gastric microflora . Likewise, an accurate definition of a subset of patients with H . pylori who really will require treatment needs to be rapidly established.

Kanagawa Shigaku, 1990 Dec, 25(3), 369 - 73
{Basic investigation of saliva SIgA}; Yoshida N et al.; Saliva, which contributes to maintaining health in the oral environment, is affected by the physiological functions of the organism and their condition . Dental caries and periodontosis, both of which are oral diseases with frequent occurrence, require the presence of bacteria to occur . SIgA (secretory IgA), an immune globulin that is found in large quantities in substances secreted during salivation, has an antibacterial action . Thus, in conducting a basic investigation on the relationship between these factors, the author investigated what effect the speed of saliva secretion, a physiological factor of the saliva component, has on the SIgA value . Results showed that, regarding the relationship between the salivary SIgA value and the speed of salivary secretion, a negative correlation exists although this is weak in terms of relevance . The fact that the correlation displayed a tendency toward scattering indicates a need to pay attention when measuring the elements in the saliva to those factors that evidently have an effect on the composition of the saliva.

Higashi Nippon Shigaku Zasshi, 1990 Dec, 9(2), 23 - 32
{Drug information in recent 5 volumes of the Year Book of Dentistry}; Sakata K et al.; The Year Book of Dentistry appears annually, providing a review of dental articles . We surveyed the abstracts of the recent 5 volumes of the Year Book of Dentistry, from 1985 to 1989 . Two hundred and eighty articles were abstracted in each volume, divided into about 13 categories . The proportion of abstracts concerned with drugs and drug therapies (here termed drug information) was almost 20% in all volumes . Most of the drug information appeared under the heading "Oral Medicine and Oral Pathology" (63%) . The original articles for the abstracts were from many journals, but 70% of the drug information articles were from JADA, Oral Surgery, and 10 other journals . The classification of the drugs in the drug information were: drugs for dental treatment, antibacterials, antiinflammatories, hemostatics, anesthetics, and others . Oral manifestations of systemic diseases or side effects of drugs used for these diseases were also abstracted . There were numerous articles of systemic diseases, due to dental treatments, including infective, hematologic diseases.

Ortop Travmatol Protez, 1990 Dec, (12), 48 - 51
{Extracorporeal connection of heterologous spleen (ECHS) in the combined intensive therapy of sepsis}; Krasovskii OIu et al.; Biohemosorption by means of extracorporeal connection of heterogeneous spleen renders not only powerful detoxic action, but intensive immunomodulation action as well . Swine spleen used for biohemosorption possess high bacterisorptive and immunomodulating potential . The cases of persistent course of disease, development of antibacterial therapy, grave condition of a patient serve as an indication for application of extracoproreal connection of heterogeneous spleen within the complex of intensive therapy . During 1989 in the hospital were treated 9 patients with osteomyelitis and extensive suppurative foci of soft tissues of the locomotor apparatus, complicated by severe sepsis . Those patients were applied to totally II extracorporeal connections of heterogeneous spleen and 8 biohemosorptions by means of heterogeneous spleen sections . In general, intensive therapy with application of extracorporeal connection of heterogeneous spleen was effective enough . All patients with no exception left hospital in satisfactory condition in 28-56 days after the beginning of treatment.

J Chemother, 1990 Dec, 2(6), 368 - 70
Enhancement of in-vitro activity of ofloxacin and gentamicin by rat serum; Miglioli PA et al.; Normal rat serum shows antibacterial activity because of the presence of endogenous substances . The aim of this research was to study some aspects of the interaction between this biological fluid and some antibiotics, in order to demonstrate possible synergistic activity . Serum is able to lower the minimum inhibitory concentration of gentamicin and ofloxacin against some Gram-negative microorganisms . This can be explained by the presence of lysozyme, antibodies, beta-lysin and other complementary factors that are able to cooperate with these antibiotics.

Chem Pharm Bull (Tokyo), 1990 Dec, 38(12), 3359 - 65
Fluorinated pyrido{2,3-c}pyridazines . II . Synthesis and antibacterial activity of 1,7-disubstituted 6-fluoro-4(1H)-oxopyrido{2,3-c}pyridazine-3- carboxylic acids; Miyamoto T et al.; Chemical modification of pyridonecarboxylic acid antibacterials with a 1,8-naphthyridine ring, such as enoxacin and tosufloxacin, to their 2-aza derivatives was studied . A new series of 1,7-disubstituted 6-fluoro-4(1H)-oxopyrido{2,3-c}pridazine-3-carboxylic acids (25-27) was prepared by a route involving either alkylation of ethyl 6-fluoro-4(1H)-oxo-7-(p-tolylthio)pyrido{2,3-c}pyridazine-3-carbox ylate (7) or intramolecular cyclization of ethyl 2-(2,6-dichloro-5-fluoronicotinoyl)-2-{2-(p-fluorophenyl)hydraz ono}acetate, (20), followed by displacement reaction with cyclic amines at C-7; the N-1 substituent in these compounds included of ethyl, 2-fluoroethyl and p-fluorophenyl groups, and the C-7 functional group comprised variously-substituted piperazines and pyrrolidines . Antibacterial activities of these compounds were markedly inferior to those of enoxacin and tosufloxacin.

DICP, 1990 Dec, 24(12), 1220 - 5
A nationwide survey of antibiotic prescribing patterns and clinical outcomes in patients with bacterial pneumonia; Grasela TH Jr et al.; Antibiotic prescribing information was prospectively collected on 1822 hospitalized patients treated for suspected or documented bacterial pneumonia . Antibacterial therapy with a single antibiotic was employed in more than 50 percent of the patients, with cefazolin, cefuroxime, ampicillin, and ceftriaxone sodium representing the most commonly employed agents . Combination therapy using two antibiotics was employed in approximately 30 percent of patients with the aminoglycosides, particularly gentamicin, used extensively . A satisfactory outcome was achieved in approximately 80 percent of patients with a community- or institutional-acquired pneumonia; only 66 percent of nosocomial pneumonias had a satisfactory outcome . An important observation was the apparently common practice of switching patients to an oral antibiotic regimen after an average of seven days of antibiotics and subsequently discharging the patient . No difference was observed in the patterns of clinical response or duration of therapy for culture-positive versus culture-negative patients . The results of this surveillance program can serve as a basis for comparison of institution-specific drug utilization evaluation programs.

Vrach Delo, 1990 Dec, (12), 44 - 6
{The use of enterosorption in pulmonary tuberculosis patients with side effects from antibacterial preparations}; Cherkasov VA et al.; Data are reported on 66 tubercular patients . In 59 of them enterosorption along with traditional treatment were used to control side-effects of antibacterial treatment, correction of liver function, reduction of tubercular intoxication . The obtained results indicate efficiency of enterosorption that removes during a short time period the side-effect allowing to treat efficiently the main disease.

Klin Med (Mosk), 1990 Dec, 68(12), 52 - 3
{Acute intestinal infection caused by Escherichia coli}; Dolidze ID et al.; Clinical manifestations and autopsy findings on 23 patients who died of acute sepsis of Escherichia coli origin lead the authors to the conclusion on polymorphic clinical run of the disease . It varies with premorbid background (food intoxication, acute respiratory disease in decompensated diabetes mellitus, chronic somatic disorders) and risk factors (inadequate antibacterial therapy, nervous strain, fatigue) . Inadequate antibacterial therapy promoting dysbacteriosis aggravated preexisting pathomorphological shifts in the intestine likely after toxic infection, diabetes-specific foci, contributed to the onset of intestinal sepsis.

J Rheumatol, 1990 Dec, 17(12), 1704 - 6
Intraarticular osmic acid in postinfectious arthritis persisting after treated bacterial arthritis; Jarvinen P et al.; We describe 4 patients successfully treated with intraarticular osmic acid for post-infectious arthritis persisting after apparent eradication of bacteria from the infected joint . In addition the bactericidal effect of osmic acid in vitro is demonstrated . We conclude that treatment with osmic acid carries no risk of iatrogenic infection; on the contrary, an antibacterial effect seems likely.

Bioessays, 1990 Dec, 12(12), 601 - 6
Selective reminiscences of beta-lactam antibiotics: early research on penicillin and cephalosporins; Abraham E; The discovery, made in Oxford, that crude penicillin could cure systemic and life-threatening bacterial infections was followed by attempts to purify penicillin, to determine its structure and then to produce it by total chemical synthesis . The beta-lactam structure of the molecule, first proposed in October 1943, was a source of controversy until 1945 . However, no useful chemical synthesis was achieved and fermentation became the commercial source of the antibiotic . In 1953, one of the products of a Cephalosporium sp . from Sardinia was shown to be a new and hydrophilic penicillin (penicillin N) . This was contaminated with a substance having the same side-chain but a characteristic absorption spectrum . The latter, cephalosporin C, showed antibacterial activity but was not inactivated by a penicillinase . The determination of its beta-lactam structure and isolation of its nucleus enabled pharmaceutical companies to produce many semisynthetic cephalosporins . A new tripeptide was later found to be an intermediate in the biosynthesis of both penicillin N and cephalosporin C, and this was followed by the complete elucidation of the biosynthetic pathways leading to these compounds and to benzylpenicillin.

Yakugaku Zasshi, 1990 Dec, 110(12), 908 - 15
{Studies on FK482 (Cefdinir) . IV . Synthesis and structure-activity relationships of 7 beta-{(Z)-2-(2-aminothiazol-4-yl)-2-hydroxyiminoacetamido}- 3-substituted cephalosporin derivatives}; Inamoto Y et al.; The synthesis of 7 beta-{(Z)-2-(aminothiazol-4-yl)-2-hydroxyiminoacetamido} cephalosporins (Ia-i) modified at the C-3 position of a cephem nucleus and the effect of the C-3 substituents on the antibacterial activity and oral absorbability are discussed . The cephems (Ie, h and i) having a C-3 substituent such as 1-propenyl, ethylthio and vinylthio group as well as FK482 (cefdinir) exhibited excellent antibacterial activities against both gram-positive and gram-negative bacteria . However, those compounds showed poor absorption rate after oral administration in rats . It is concluded that the vinyl moiety at the 3-position is necessary to display fairly oral absorptivity in a series of 7 beta-{(Z)-(2-aminothiazol-4-yl)-2-hydroxyiminoacetamido}c eph ems.

J Antimicrob Chemother, 1990 Dec, 26 Suppl F, 131 - 44
Mechanisms of resistance to the 4-quinolone antibacterial agents; Crumplin GC; Because of the close structural relationship of the fluorinated 4-quinolones to the parent compound nalidixic acid the mechanism of resistance is often perceived to be the same . However, it is clear that whilst the mechanism of resistance to fluorinated 4-quinolones is essentially the same, strains that are selected as resistant to nalidixic acid generally retain sensitivity to the newer agents . A number of mutations in the chromosome of Escherichia coli have been identified and these are described . These mutations affect the interaction of quinolones with their presumed targets (DNA gyrases) and the transport of quinolones through the cell membrane . A small number of other mutations giving rise to low-level resistance to nalidixic acid, which affect neither gyrase nor membrane function, are also recognized . Despite the recognition of these mutations, the practical application of this information is hampered by lack of knowledge of the normal uptake mechanisms, the processes involved in selection and maintenance of resistance, the relationship of resistance to pathogenicity and the frequency of occurrence of these mutations.

J Biol Response Mod, 1990 Dec, 9(6), 576 - 83
Effects of granulocyte colony-stimulating factor on hematopoietic injury induced by anticancer drugs in mice; Mizushima Y et al.; The in vivo effects of the subcutaneous administration of the granulocyte colony-stimulating factor (G-CSF) on chemotherapy-induced hematopoietic injury were evaluated in BALB/c mice . Mice treated with chemotherapeutic drugs were injected once a day for up to 12 days with 2 micrograms of recombinant human G-CSF, and following this, bone marrow cellularity, spleen weight, and peripheral blood cell counts were measured 24 h after cessation of the G-CSF treatment . Treatment of normal mice had minimal effect on the elevation of the white blood cell (WBC) count or on the hosts' resistance to K . pneumoniae infection . Spleen weight was significantly higher in normal mice treated with G-CSF, and the platelet counts were slightly lower . In mice treated with cyclophosphamide (150 mg/kg), G-CSF treatment caused an elevation of WBC and an enhancement of antibacterial resistance . Variable amounts of an accelerated recovery of neutrophils by G-CSF treatment was also observed in nimustine hydrochloride (50 mg/kg)-, mitomycin c (MMC) (8 mg/kg)-, or vindesine sulfate (VDS) (4 mg/kg)-treated mice . A significant decrease in PLT counts was observed in MMC- or VDS-treated hosts given G-CSF . These results indicate that administration of G-CSF may facilitate hematopoietic recovery in chemotherapy-treated cancer patients and that it may help them to increase their resistance to life-threatening infection . Conversely, treatment with G-CSF and chemotherapeutic drugs may cause a more severe thrombocytopenia than is observed with only chemotherapy treatment.

J Biol Chem, 1990 Nov 25, 265(33), 20496 - 505
Evidence for a common mechanism of action for antitumor and antibacterial agents that inhibit type II DNA topoisomerases; Huff AC et al.; Numerous antitumor and antibacterial agents inhibit type II DNA topoisomerases, yielding, in each case, a complex of enzyme covalently bound to cleaved DNA . We are investigating the mechanism of inhibitor action by using the type II DNA topoisomerase of bacteriophage T4 as a model . The T4 topoisomerase is the target of antitumor agent 4'-(9-acridinylamino)-methanesulfon-m-anisidide (m-AMSA) in T4-infected Escherichia coli . Two m-AMSA-resistant phage strains were previously isolated, one with a point mutation in topoisomerase subunit gene 39 and the other with a point mutation in topoisomerase subunit gene 52 . We report here that the wild-type T4 topoisomerase is inhibited by six additional antitumor agents that also inhibit the mammalian type II topoisomerase: ellipticine, 9-OH-ellipticine, 2-me-9-OH-ellipticinium acetate, mitoxantrone diacetate, teniposide, and etoposide . Further, one or both of the m-AMSA-resistance mutations alters the enzyme sensitivity to each of these agents, conferring either cross-resistance or enhanced sensitivity . Finally, the gene 39 mutation confers on T4 topoisomerase a DNA gyrase-like sensitivity to the gyrase inhibitor oxolinic acid, thus establishing a direct link between the mechanism of action of the anti-bacterial quinolones and that of the antitumor agents . These results strongly suggest that diverse inhibitors of type II topoisomerases share a common binding site and a common mechanism of action, both of which are apparently conserved in the evolution of the type II DNA topoisomerases . Alterations in DNA cleavage site specificity caused by either the inhibitors or the m-AMSA-resistance mutations favor the proposal that the inhibitor binding site is composed of both protein and DNA.

J Appl Bacteriol, 1990 Nov, 69(5), 701 - 4
A note on the antibacterial properties of 3-(3'-isocyanocyclopent-2'-enylidene)propionic acid in the ovine rumen; Brewer D et al.; The concentration of 3-(3'-isocyanocyclopent-2'-enylidene)propionic acid after introduction into the ovine rumen declined by 50% during 30 min . Its antibacterial activity in the rumen could be demonstrated by the decline in numbers of cellulolytic rumen bacteria from about 10(6)/ml to about 10(2)/ml.

Cell Tissue Kinet, 1990 Nov, 23(6), 637 - 49
Haemopoietic stem cells: spleen colony-forming cells are normally actively proliferating; Necas E et al.; The haemopoietic stem cells forming spleen colonies (CFU-S) had on average 30 to 40% of cells engaged in the DNA synthesis in normal mice continuously over 4 years . A majority of experiments aimed at the suppression of the CFU-S proliferation, which included suppression of the T-lymphocytes by means of cyclosporin A or by adult thymectomy, administration of antibacterial and antifungal agents and maintainance of mice in a sterile environment, suppression of antibody-producing cells by a successive administration of the bacterial lipopolysaccharide and cyclophosphamide and attempts to increase the total number of CFU-S in the body through massive transfusions of bone marrow cells or by grafting plugs of the bone marrow under the kidney capsulae, have not been sufficiently effective . A transient suppression of CFU-S proliferation occurred during recovery of the haemopoietic tissue from damage caused by cyclophosphamide . The results support the view that changes in CFU-S numbers and in the proportion of them in DNA synthesis may be positively correlated when CFU-S numbers fluctuate physiologically about their normal values . The failure to manipulate the CFU-S proliferation rate easily suggests that proliferation of these cells may not be under a strong 'switch on - switch off' control.

J Antibiot (Tokyo), 1990 Nov, 43(11), 1441 - 9
Synthesis and biological properties of 1-oxapenems; Murakami M et al.; Several 2-substituted oxapenems, 1a, 1b and 1c, bearing the hydroxyethyl side-chain at 6 alpha were synthesized in a highly stereoselective manner starting from the commercially available 3 alpha-hydroxyethyl-4 beta-acetoxyazetidinone (5) . The stability, in vitro antibacterial activity, and beta-lactamase inhibitory properties of these oxapenems were examined . The 2-isopropyl penem 1c had considerable stability as shown by its t1/2 of 200 minutes in pH 7.0 buffer solution and at 37 degrees C, while the other two 1a and 1b were labile . Interestingly, the antibacterial activity of these compounds paralleled their stability and thus penem 1c showed appreciable MICs, whereas the other two were virtually inactive . All three penems inhibited certain cephalosporinases strongly, but penicillinases only weakly . Thus, the inhibitory spectrum was similar to that for epi-thienamycin B and not the spectrum for clavulanic acid.

Arch Intern Med, 1990 Nov, 150(11), 2258 - 64
Empiric treatment of fungal infections in the neutropenic host . Review of the literature and guidelines for use; Sugar AM; Persistent fever that is refractory to broad-spectrum antibacterials is common in neutropenic patients undergoing induction chemotherapy of acute leukemia . Clinical experience suggests that many of these patients are infected with fungi . Until recently, data supporting the role of empiric antifungal therapy in this setting were limited to small groups of patients or postmortem reports . Evolving evidence in larger patient populations supports data from smaller series: febrile neutropenic patients who have failed to respond to a 4- to 7-day course of broad-spectrum antibacterials may benefit from the early initiation of antifungal therapy . Patients with fungal colonization or pulmonary infiltrates and adult patients who have not received previous fungal prophylaxis may especially benefit from the early use of antifungal drugs . Amphotericin B has been the "gold standard" for empiric antifungal therapy, although the newer azoles may be useful in certain situations.

J Dent Res, 1990 Nov, 69(11), 1724 - 30
mRNAs for PRPs, statherin, and histatins in von Ebner's gland tissues; Azen EA et al.; A search was made for expression of genes for proline-rich proteins (PRPs) and other salivary-type proteins, including statherin and histatins, in taste-bud tissues of mice and primates because of previous genetic findings in mice (Azen et al., 1986) that Prp and taste genes for certain bitter substances are either the same or closely linked . Taste-bud tissues and other tissues were tested for specific mRNAs with labeled DNA probes by Northern blotting and in situ hybridization . It was found that PRP mRNAs were present in von Ebner's glands of mice and macaques, and that there was a much greater degree of PRP mRNA induction in mouse parotid (16-fold) than in von Ebner's gland (two-fold) after in vivo isoproterenol stimulation . This difference may be due, in part, to differences in autonomic nerve innervation . Statherin and histatin mRNAs were found in macaque taste-bud tissues containing von Ebner's gland, and statherin protein was found in human von Ebner's gland by immunohistochemistry . The finding of PRP gene expression in von Ebner's gland, whose secretions have been suggested to play a role in taste stimulation, adds further support to a possible function of PRPs in bitter tasting . The possible functions of statherin and histatins in von Ebner's gland secretions may be related to statherin's regulation of salivary calcium and histatins' antibacterial and antifungal properties.

Antibiot Khimioter, 1990 Nov, 35(11), 44 - 7
{Sandoglobulin immunocorrection in trauma}; Belotskii SM et al.; Twenty one patients with the long-term compression syndrome (LCS) and 12 patients with burns treated with sandoglobulin in combination with antibacterial therapy were followed up . The control groups included 14 and 18 patients, respectively . All the patients had wound infections . Increased or lowered respiratory burst of peripheral blood neutrophils and lowered contents of active T-lymphocytes were detected in the majority of the patients . The patients had also an increased respiratory burst of tissue homogenate in the primary focus . Sandoglobulin decreased the periods of normalization of the immunological indices, body temperature and leukogram shifts to the right . The most pronounced effect of the drug was recorded before radical operations, i.e . in the presence of acute microbial toxemia or in patients with severe and extended burns . The procedure of immunological monitoring developed by the authors rapidly estimates the indications to the use of sandoglobulin alone or in combination with other immunomodulators.

Am Rev Respir Dis, 1990 Nov, 142(5), 1068 - 72
The lavage fluid from a patient with alveolar proteinosis inhibits the in vitro chemiluminescence response and arachidonic acid metabolism of normal guinea pig alveolar macrophages; Carre PC et al.; Pulmonary alveolar proteinosis is characterized by the accumulation of a lipoproteinaceous material within the alveoli of the lung . It is well established that patients with pulmonary alveolar proteinosis have a high incidence of complicating pulmonary infections possibly resulting from defects of antibacterial functions of alveolar macrophages . Moreover, for unclear reasons, an inflammatory response in the airways is frequently absent . In order to investigate the role of the lipoproteinaceous material in these two patterns, we tested the in vitro effects of a lavage fluid from a human pulmonary alveolar proteinosis on the secretion of reactive oxygen intermediates and arachidonic acid metabolites by normal guinea pig alveolar macrophages . After incubation with the lipoproteinaceous material, the luminol-enhanced chemiluminescence of zymosan-triggered alveolar macrophages was reduced in a dose-dependent fashion . The lipoproteinaceous material similarly reduced the chemiluminescence response in a cell-free xanthine-xanthine oxidase system generating superoxide anions . This latter observation suggests that the lipoproteinaceous material acts as a scavenger for superoxide anions produced by alveolar macrophages . Its purified protein or phospholipid fractions also resulted in a general inhibition of the secretion of arachidonic acid metabolites by alveolar macrophages challenged in vitro with zymosan . Our results suggest that the alveolar filling material of pulmonary alveolar proteinosis may inhibit the action of antibacterial and/or proinflammatory agents produced by alveolar macrophages . We speculate that such effects of the lipoproteinaceous material may play a role in vivo in the high incidence of pulmonary infections and in the absence of discernible interstitial or intraalveolar inflammation seen in pulmonary alveolar proteinosis.

Int Endod J, 1990 Nov, 23(6), 283 - 97
Review of calcium hydroxide; Foreman PC et al.; Calcium hydroxide is a material which has been used for a variety of purposes since its introduction into dentistry in the early part of the twentieth century . In its pure form, the substance has a high pH, and its dental use relates chiefly to its ability to stimulate mineralization, and also to its antibacterial properties . A range of products has been formulated with different therapeutic actions, the effects of which are partially dependent upon the tissue to which they are applied . The material is reviewed under the following general headings: biochemical actions; dental formulation; uses.

Pathologica, 1990 Nov-Dec, 82(1082), 707 - 17
{Helicobacter pylori and gastro-duodenal pathology}; Villani L et al.; Helicobacter Pylori (HP) were found in 878 (73%) of 1205 patients undergoing upper G-I endoscopy with multiple biopsies for gastroduodenal diseases . HP were present in similar percentages among patients with active (89%) or healed (81%) peptic ulcer as well as in non ulcerous dyspeptics affected with gastritis (85%) . 96% of active chronic gastritis were infected by HP as compared with 55% of quiescent gastritis . Antral gastritis was more frequently active in patients with ulcer diseases (76%) than in dyspeptic and asyntomatic patients (50%) . Healed gastric and duodenal ulcers showed decreased incidence of active antral gastritis (69) as compared with active ulcers . Conversely body gastritis was more frequently active in healed (37%) than in overt (18%) duodenal ulcers . 95 histologically normal stomachs as well as 9 cases exhibiting type A gastritis were devoid of HP . High rates of infection were found in 610 cases of chronic gastritis without atrophy as well as in 151 atrophic antral (type B) gastritis . Cytoplasmic vacuolization and swelling of foveolar-superficial cells with adhering bacteria, micropapillae and microerosions were commonly found in HP-infected mucosa . In 16 of 19 children with type B chronic gastritis antibacterial therapy eradicated HP . This was followed by resolution or striking improvement of gastritis and disappearance of epithelial lesions.

Eur Respir J, 1990 Nov, 3(10), 1206 - 16
Subclinical alveolitis in immunological systemic disorders . Transition between health and disease?
Wallaert B, Dugas M, Dansin E, Perez T, Marquette CH, Ramon P, Tonnel AB, Voisin C.
A subclinical inflammatory alveolitis as assessed by BAL cell analysis may be present in a high proportion of symptomless patients with immunological systemic disorders and with normal chest roentgenogram . Subclinical alveolitis can be characterized by the relative proportions of the different cell populations comprising the alveolitis and by the activated state of the cells . Thus, subclinical alveolitis can be classified into two major groups: lymphocyte and neutrophil alveolitis . Lymphocyte alveolitis is frequently found in patients with extrathoracic granulomatosis (Crohn's disease, primary biliary cirrhosis, extrathoracic sarcoidosis) or with some collagen vascular diseases (Sjogren's syndrome, rheumatoid arthritis, systemic lupus erythematosus) . Neutrophil alveolitis is a main finding in collagen vascular diseases, especially progressive systemic sclerosis, dermatopolymyositis and mixed connective tissue disease . In addition, alveolar macrophages may be spontaneously activated and release various mediators that could be relevant to the pathogenesis of interstitial lung disease . On the other hand, some other alveolar macrophage functions (antibacterial activity may be severely impaired in some diseases, for example systemic lupus erythematosus) . Alveolar inflammation is associated with an increase in the permeability of the alveolar membrane responsible for an increased influx of blood proteins in the alveolar spaces . Although subclinical inflammation may also be detected by high resolution computed tomography (HRCT) scan and/or lung permeability scintigraphic studies, the significance and prognostic value remains unclear and clearly differs according to both the disease and the pattern of alveolitis.

J Nat Prod, 1990 Nov-Dec, 53(6), 1615 - 8
A new polyhalogenated monoterpene from the red alga Plocamium cartilagineum; Konig GM et al.; From a sample of the red alga Plocamium cartilagineum, four polyhalogenated monoterpenes {1-4} were isolated and characterized with (3R*, 4R*)-1-bromo-7-chloromethyl-3,4-dichloro-3-methyl-1E,5E,7-octatrie ne {1} being a new compound . Also reported are antifungal, antibacterial, and molluscicidal activities, as well as the brine shrimp toxicity of these metabolites.

Chem Pharm Bull (Tokyo), 1990 Nov, 38(11), 3031 - 4
Lignified materials as potential medicinal resources . III . Diversity of biological activity and possible molecular species involved; Oh-hara T et al.; Diverse biological activities of hot-water and alkali extracts of lignified materials were reviewed and the molecular species involved are discussed . Materials tested included pine cone of Pinus parviflora SIEB . et Zucc., wood chips of slash pine, Douglas fir, and tallow wood, and two basidiocarps, in addition to their partially degraded preparations and commercial lignins . As a tentative conclusion, the lignin structure of these extracts might be responsible for the potent stimulation of granulocytic cell iodination, inhibition of viral infection and/or proliferation in vitro, and inactivation of viral ribonucleic acid (RNA)-dependent RNA polymerase and (adenosine diphosphate-ribose)n glycohydrolase . Other activities displayed by some of these extracts, such as antibacterial and antitumor activities, induction of hemolytic plaque-forming-cells in mice, and stimulation of deoxyribonucleic acid synthesis of isolated splenocytes, remain to be investigated.

J Antimicrob Chemother, 1990 Nov, 26(5), 659 - 66
In-vitro and in-vivo activity of DR-3355, an optically active isomer of ofloxacin; Tanaka M et al.; DR-3355 {S-(-)-ofloxacin}, an optically active isomer of ofloxacin, showed a broad spectrum of antibacterial activity against both Gram-positive and Gram-negative bacteria and was generally twice as potent as ofloxacin and considerably more active than DR-3354 {R-(+)-ofloxacin} . The activity of DR-3355 was largely unaffected by the type of culture medium, inoculum size and addition of human serum, but decreased under acidic condition at pH 6.0 . The protective effect of orally administered DR-3355 in experimental infections in mice with various bacterial pathogens was superior to those of ofloxacin and ciprofloxacin.

J Antimicrob Chemother, 1990 Nov, 26 Suppl C, 1 - 8
Cefodizime, a new 2-aminothiazolyl cephalosporin: physicochemical properties, toxicology and structure-activity relationships; Bryskier A et al.; Cefodizime is a 2-aminothiazolyl cephalosporin for parenteral use . Cefodizime has a bisubstituted thiothiazole moiety in position 3 of the cephem nucleus . The presence of this moiety does not alter the in-vitro antibacterial activity, or safety in animal studies, which are similar to those of cefotaxime, but results in an apparent long elimination half-life in rodents and dogs, and in novel immunological properties.

J Hosp Infect, 1990 Nov, 16(4), 331 - 8
An in-use evaluation of decontamination of polypropylene versus steel bedpans; Block C et al.; A prospective cross-over study in three different wards has demonstrated the lack of effect of two disinfectants compared with a detergent when added to the washing cycle of automatic bedpan washers that employ hot water centrally supplied at 60 degrees C . An unexpected and potentially important finding was that polypropylene pans were much more effectively cleaned and decontaminated than their stainless steel counterparts . The role, if any, of bedpans in the epidemiology of nosocomial infections remains a mystery . The continued absence of information clearly incriminating these ubiquitous devices in the transmission of potential pathogens, or of genes encoding antibacterial drug resistance, raises questions as to whether extensive efforts to achieve a high degree of decontamination of bedpans are necessary at all.

J Pharm Sci, 1990 Nov, 79(11), 1023 - 8
Protonation equilibria of quinolone antibacterials; Takacs-Novak K et al.; The acid-base properties of seven antibacterial 7-piperazinyl fluoroquinolone derivatives were studied by potentiometry and UV and NMR spectroscopy . These molecules contain two proton-binding sites of similar basicity, namely, the piperazine amino and the carboxylate groups, as proven by 1H NMR spectroscopy . The basicities are quantitated at the molecular level in terms of macroconstants, and also at the submolecular level in terms of microconstants . The microconstants are then used to calculate the concentration of the positive, zwitterionic, neutral, and negatively charged species (microspeciation) . The zwitterionic forms always predominate over their neutral protonation isomers, but the zwitterionic:neutral concentration ratio is considerably different for the examined fluoroquinolone derivatives.

Agric Biol Chem, 1990 Nov, 54(11), 2883 - 7
New pyrrolobenzodiazepine antibiotics, RK-1441A and B . II . Isolation and structure; Osada H et al.; Antibacteriophage antibiotics, RK-1441A and B, related to neothramycin were isolated from the culture broth of Streptomyces sp . and their structures were deduced from spectroscopic analyses . The structure of RK-1441A was 8,11-dihydroxy-3,7-dimethoxy-5-oxo-1H-pyrrolo{2,1-c:1,4}benzodiazepine . RK-1441B is a tautomeric mixture at C-3 of the structure, 3,8,11-trihydroxy-7-methoxy-5-oxo-1H-pyrrolo{2,1-c:1,4}benzodiazepine.

J Chromatogr, 1990 Oct 19, 519(1), 125 - 36
Determination of minor impurities in temafloxacin hydrochloride by high-performance liquid chromatography; Elrod L Jr et al.; Minor impurities in the antibacterial agent temafloxacin hydrochloride were determined using high-performance liquid chromatography . Manufacturing impurities and degradation products were separated using a reversed-phase system with gradient elution . Detector response was linear for the individual impurities to approximately 50 micrograms/ml which represents 2.5% of the drug concentration . The procedure provides quantitation of impurities to approximately the 0.05% level with precision (relative standard deviations) of 4.7% to 29% in typical bulk drug lots . A variety of reversed-phase columns were evaluated for the assay method with optimum resolution achieved using a 5-microns Nucleosil C18 packing.

FEBS Lett, 1990 Oct 15, 272(1-2), 200 - 4
Amino acid sequence of CAP37, a human neutrophil granule-derived antibacterial and monocyte-specific chemotactic glycoprotein structurally similar to neutrophil elastase; Pohl J et al.; We report the amino acid sequence of CAP37, a human neutrophil granule protein with antibacterial and monocyte-specific chemotactic activity . CAP37 is a single-chain protein consisting of 222 amino acid residues . It has three N-glycosylation sites, at Asn residues 100, 114 and 145 . Some species of CAP37 are glycosylated at all three sites; some at Asn-114 alone, others at Asn-114 and Asn-110 or Asn-145 . CAP37 has 45% sequence identity to human neutrophil elastase, and 30-37% identity to several other granule serine proteinases . Despite these similarities, CAP37 is not a serine proteinase because the active site residues serine and histidine are replaced.

J Immunol, 1990 Oct 15, 145(8), 2539 - 44
Monoclonal antibodies against an HLA-B27-derived peptide react with an epitope present on bacterial proteins; Raybourne RB et al.; The role of molecular mimicry in the spondyloarthropathies was investigated with respect to the epitopes involved . mAb were produced against a synthetic peptide whose sequence was derived from a polymorphic region of the HLA-B27 molecule (amino acids 63-83) . Two antibodies (J7F2 and H2B6) were selected for study on the basis of their ability to react with bacterial envelope proteins (ELISA) and B27-positive cells (immunofluorescence) . J7F2 reacted preferentially with B27-positive cells and neither antibody reacted with MHC class I negative cells . Based on SDS-PAGE blot analysis of bacterial envelope proteins, the pattern of reactivity for both antibodies (against 36- and 19-kDa proteins) was the same as that for a third monoclonal produced against bacterial envelope and reactive with B27-positive cells . This apparent epitope similarity was investigated by using synthetic peptides to inhibit binding of the monoclonals . The B27 synthetic peptide and a smaller peptide derived from it were efficient inhibitors of antipeptide and antibacterial antibody binding to bacterial Ag and B27-positive cells . These studies provide insight into the molecular basis of cross-reactivity between bacterial proteins and MHC class I molecules.

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