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 distinctiv