Antimicrobial

J Clin Pharmacol, 1978 Oct, 18(10), 491 - 9
Cinoxacin: pharmacokinetics and the effect of probenecid; Israel KS et al.; Cinoxacin is a new synthetic organic antibacterial compound which has a serum half-life of approximately 1 hour . Most of the drug is eliminated in man by the kidney, primarily as unchanged drug . The renal clearance of cinoxacin is slightly greater than the usually accepted value for the average glomerular filtration rate, which suggests that it is probably filtered and is also secreted by the tubule . Results after pretreatment with probenecid further suggest secretion of the drug.

J Antibiot (Tokyo), 1978 Oct, 31(10), 945 - 8
The isolation and characterization of rubradirin B; Hoeksema H et al.; Rubradirin B, C40H33N3O15, was separated from other components of the rubradirin complex by chromatographic and crystallization procedures . The spectrum of antibacterial activity is similar to that of rubradirin, but the antibiotic is less active.

Appl Environ Microbiol, 1978 Oct, 36(4), 577 - 83
Isolation, purification, and antibiotic activity of o-methoxycinnamaldehyde from cinnamon; Morozumi S; o-Methoxycinnamaldehyde has been isolated and purified from powdered cinnamon . The compound inhibits the growth and toxin production of mycotoxin-producing fungi . The substance completely inhibited the growth of Aspergillus parasiticus and A . flavus at 100 microgram/ml and A . ochraceus and A . versicolor at 200 microgram/ml . It inhibited the production of aflatoxin B1 by over 90% at 6.25 microgram/ml, ochratoxin A at 25 microgram/ml, and sterigmatocystin at 50 microgram/ml . The substance also displayed a strong inhibitory effect on the growth of five dermatophytoses species, e.g., Microsporum canis (minimum inhibitory concentration, 3.12 to 6.25 microgram/ml) . However, no antibacterial effect was observed at concentrations as high as 50 microgram/ml.

J Bone Joint Surg Am, 1978 Oct, 60(7), 871 - 81
Treatment of orthopaedic infections with electrically generated silver ions . A preliminary report; Becker RO et al.; Electrically generated silver ions have been shown previously to be a potent antibacterial agent with an exceptionally broad spectrum as indicated by in vitro testing . The present study reports on clinical experience using electrically generated silver ions as adjunctive treatment in the management of chronic osteomyelitis . Fourteen patients had fifteen treatment attempts: thirteen for chronic osteomyelitis of the tibia, one for acute and chronic pyarthrosis and osteomyelitis of the knee, and one for a chronically draining sinus after total hip replacement . Wound debridement, silver ion iontophoresis, and subsequent wound care (usually provided by the patient) resulted in control of the infection in twelve of the fifteen treatment attempts and in healing of the non-union after follow-up ranging from three to thirty-six months . The other three attempts led to two partial and one complete failure.

Ric Clin Lab, 1978 Oct-Dec, 8(4), 211 - 31
Human lysozyme (origin and distribution in health and disease); Reitamo S et al.; Histochemical and in particular immunoperoxidase techniques have extended our knowledge about the cellular distribution of LZM . The enzyme has been detected in: 1 . granulocytes, which synthesize LZM in bone marrow; 2 . cells of the mononuclear phagocytic system, which synthesize LZM continuously; 3 . various exocrine glands, whose LZM is probably in part synthesized locally and in part derived from blood; 4 . cartilage, which probably synthesizes LZM and 5 . the kidney, in which LZM is serum-derived . In pathological conditions, such as inflammation and neoplasia, most LZM-positive cells at the site of disease are either granulocytes or members of the mono-nuclear phagocytic system . A notable exception are the metaplastic Paneth cells that occur along the gastrointestinal tract in inflammation and neoplasia . LZM is an antibacterial agent, but evidence is accumulating which suggests that the enzyme might have other functions as well.

Urology, 1978 Oct, 12(4), 411 - 5
Heparin as antibacterial agent in rabbit bladder; Hanno PM et al.; Previous studies performed in our laboratory indicated that the primary antibacterial defense mechanism of the rabbit bladder is the antiadsorptive action of the surface mucopolysaccharide . The increased bacterial adsorption that occurs when the bladder is denuded of this layer was prevented by the instillation of heparin . Additional studies showed that the protective effect of heparin is inhibited by protamine, a further indication that the bladder's "antiadherence factor" is a mucopolysaccharide . Small amounts of heparin, applied directly to the mucoprotein-deficient bladder or to the surface of the inoculated bacteria, produced a statistically significant reduction in bacterial adsorption.

Immun Infekt, 1978 Oct, 6(5), 180 - 93
{The present situation of antibacterial resistance (author's transl)}; Wagner WH; The various types of bacterial resistance (natural species resistance, chromosomal and plasmidic resistance) and their mechanisms are described . Thereafter, a survey on the resistance is given using investigations from different sources . The distribution of resistant strains dependent on the geographical location and the situation of the patients (ambulatory--hospitalized) is described, and the development of resistant strains in dependance of time is analyzed . Finally, the phenomena of resistance against aminoglycoside and beta-lactam antibiotics are explained in more detail.

J Antibiot (Tokyo), 1978 Oct, 31(10), 991 - 6
1- and 3-deamidino derivatives of dihydrostreptomycin and some 1-N-acyl derivatives; Usui T et al.; 1-Deamidino-, 3-deamidino- and 1,3-di(deamidino)dihydrostreptomycin (1, 2, 3) were prepared by treatment of dihydrostreptomycin (DHSM) with ammonia at 100 degrees C . The 3-guanidino group of DHSM is suggested to be more important than the 1-guanidino group for the antibacterial activity of DHSM . 1-N-{(S)-4-Amino-2-hydroxybutyryl) and 1-N-{(S)-4-guanidino-2-hydroxybutyryl} derivatives (4, 6) of 1-deamidinodihydrostreptomycin were futher prepared.

Chem Biol Interact, 1978 Sep, 22(2-3), 167 - 83
Effects of halogenated antibacterials on the erythrocyte membrane; Miller TL et al.; The influence of halogenated antibacterials on membrane structure and function was investigated using the human erythrocyte membrane as a model . Measurements of hemolysis in isotonic solution, altered membrane permeability, and stabilization against hypotonic hemolysis resulting from exposure of erythrocytes to halogenated antibacterials served as criteria of membrane-related effects . The hemolytic potency of the compounds studied differed widely, decreasing in the order hexachlorophene (HCP) greater than 2,2'-methylenebis(3,5-dichlorophenol) (3,5-TCP) greater than 2,2'-methylenebis(3,4-dichlorophenol) (3,4-TCP) approximately equal to 2,2'-methylenebis(4,6-dichlorophenol) (4,6-TCP) greater than 2,2'-methylenebis(4-chlorophenol) (DCP) greater than 3,4'-tribromosalicylanilide (TBS) approximately equal to 3,3',4',5-tetrachlorosalicylanilide (TCSA) . Each of the antibacterials tested stabilized the erythrocyte against hypotonic hemolysis, although there were marked differences in the concentrations required to afford maximum stabilization as well as in the extent of protection . The observed order of protective effectiveness was HCP greater than 3,4-TCP greater than 4,6-TCP greater than DCP approximately equal to TCS greater than TBS . As shown by measurements of the first-order rate constant for K+ efflux, the permeability of the erythrocyte membrane to K+ was increased upon exposure to the antibacterials, with the effect of HCP greater than 3,4-TCP greater than 4,6-TCP approximately equal to 3,4-TCP greater than DCP approximately equal to TCS greater than TBS . These results indicate that halogenated antibacterials are capable of perturbing mammalian membranes, a feature which may account in part for their mammalian toxicity.

Tijdschr Diergeneeskd, 1978 Sep 1, 103(17), 899 - 906
{Nalidixic acid intoxication in two pregnant bitches (author's transl)}; Solleveld HA et al.; To ensure prolonged survival, dogs with cyclic neutropenia should be protected against bacterial infection of exogenous or endogenous origin, particularly during the neutropenic episodes . One of the methods available to minimize the risk of infection in these dogs, is selective decontamination of the gastrointestinal tract by using antibiotics and/or chemotherapeutic agents, in conjunction with housing in a laminar-flow cabinet . Two pregnant bitches, some of the offspring of which were expected to be homozygous for the cyclic neutropenia allele, were decontaminated with nalidixic acid . Fourteen days after initiation of the antibacterial treatment, the two dogs died . Jaundice and seizures had been apparent in both animals prior to death . Histopathological examination revealed changes primarily in the liver, which were consistent with toxic hepatic necrosis and were characterized by severe centrilobular haemorrhage and disappearance of hepatocytes . Multiple haemorrhages were observed in other organs . Further clinical investigation in two other dogs strongly suggested that nalidixic acid was the cause of death in the two pregnant bitches.

J Pharm Sci, 1978 Sep, 67(9), 1336 - 8
Selenium heterocycles XXII: Synthesis and antibacterial antifungal activities of arylsulfonyl-1,2,3-selenadiazoles; Lalezari I et al.; Series of 4-arylsulfonylmethyl-1,2,3-selenadiazoles, 4-(1-arylsulfonylethyl)-1,2,3-selenadiazoles, and 4-alkyl (or aryl)-5-arylsulfonyl-1,2,3-selenadiazoles were synthesized . 4-(3-Pyridyl)-5-phenylsulfonyl-1,2,3-selenadiazole exhibited the highest activity of growth inhibition against some bacteria and fungi.

Rev Cubana Med Trop, 1978 Sep-Dec, 30(3), 167 - 73
{Preparation and evaluation of antibacterial activity of partial fractions of Vallesia antillana Wood}; Rojas Hernandez NM et al.; A study on the antibacterial properties of alkaloidal fractions of Vallesia antillana Wood, a Cuban plant belonging to the Apocynaceae family, is performed for the first time . Four partial fractions from bark of stems were prepared according to a classical extraction of total alkaloids and a partial fractionation of these, with the use of tartaric acid and ethyl ether and by a pH gradient with values of 2.5, 5.0, 7.0 and alkaline one . Data from thin layer chromatography on the alkaloidal content of different fractions are added and an assessment of antibacterial activity was made; for this, a method of sections in agar medium with bacterial species of human clinical interest was used; inhibitory halos found within 24 hours of incubation at 37 degrees C are reported in millimeters.

J Dent Res, 1978 Sep-Oct, 57(9-10), 922 - 6
Inhibition and killing of oral bacteria by silver ions generated with low intensity direct current; Thibodeau EA et al.; Silver cations generated by passing low intensity direct current through pure silver electrodes were found to be sufficiently antibacterial to cause sterilization of samples of infected dentin . The optimal procedure involved a 5 microA current applied for 20 minutes with the anode then left in contact with the sample . Minimal inhibitory concentrations of electrically generated silver ions for representative oral bacteria were essentially equal to those for silver ions added as nitrate or fluoride salts, and medium constituents, including sodium thioglycolate, antagonized antibacterial action . A major advantage to the use of the electrode method is that it allows for continuous, focal application of antibacterial silver cations.

J Antibiot (Tokyo), 1978 Sep, 31(9), 906 - 10
Effects of polymyxin antibiotics on iodohippurate accumulation in rabbit renal cortical slices; Milman N et al.; The in vitro effects of polymyxin antibiotics on 0-125I-hippurate (OIH) accumulation in rabbit renal cortical slices were studied using incubation media with pH ranging from 6.9 to 7.9 and containing polymyxin B sulfate, colistin sulfate, sodium colistimethate and antibacterially inactive N-succinyl colistin in concentrations ranging from 1 to 2,000 microgram base/ml . Polymyxin B, colistin and colistimethate depressed OIH accumulation significantly in concentrations greater than or equal to 300 microgram/ml . The effects on accumulation were clearly pH-dependent and most pronounced at alkaline pH . N-Succinyl colistin had only a marginal influence on accumulation, even in high concentrations . Colistimethate produced a significantly smaller decrease in accumulation at all pH values than both polymyxin B and colistin . The results suggest that the presence of free amino groups is necessary to obtain a decrease in accumulation and correlate with the known in vivo nephrotoxicity of these antibiotics.

Am J Physiol, 1978 Sep, 235(3), C103 - 8
Reactive forms of oxygen and chemiluminescence in phagocytizing rabbit alveolar macrophages; Miles PR et al.; Chemiluminescence (CL), superoxide anion (O2-) production, and particle uptake were measured to determine the role of antibacterial substances in the chemiluminescent response associated with phagocytosis in rabbit alveolar macrophages (AM) . Exposure of AM to zymosan particles induced both CL and the production of extracellular O2- . CL is inhibited by superoxide dismutase, an enzyme which catalyzes the conversion of O2- to hydrogen peroxide (H2O2), by catalase, an enzyme which destroys H2O2, and by the hydroxyl radical (.OH) scavengers, benzoate and ethanol . Superoxide dismutase and catalase probably exert their effects in the extracellular fluid . CL can also be produced by the addition of NaO2 or H2O2 to zymosan in a noncellular system . The chemiluminescent response occurs before particle uptake is complete, which also indicates that CL occurs in the extracellular fluid . These results suggest that CL induced by zymosan in AM is due to the extracellular reaction between various reactive forms of oxygen and zymosan.

Gastroenterology, 1978 Sep, 75(3), 445 - 9
Endotoxin and the liver . III . Modification of acute carbon tetrachloride injury by polymyxin b--an antiendotoxin; Nolan JP et al.; Previous work suggests that endotoxin of enteric origin may contribute to both acute and chronic liver injury by other agents . In particular, evidence exists that endotoxin tolerance modifies biochemical and histological evidence of carbon tetrachloride hepatotoxicity . The present study was undertaken to ascertain whether another method of modifying endotoxicity would protect against carbon tetrachloride (CCl4) damage as well . The antibiotic polymyxin B (PB) has unique antiendotoxin properties not shared by gentamicin sulfate, an antibiotic with a similar antibacterial spectrum . In groups of rats pretreated with either PB, gentamicin, or diluent, the LD100 of an oral dose of CCl4 was reduced by PB to an LD50, but the gentamicin pretreatment was without effect . When a sublethal dose of CCl4 was administered, both the SGOT and SGPT values were significantly lower in the PB group of rats . This biochemical protection was mirrored in the striking lack of histological liver necrosis in these animals, protection not shared by the gentamicin group or controls . The incidence of endotoxemia 24 hr after CCl4 as detected by lead acetate enhancement was also reduced by PB pretreatment . These findings further support the contention that endotoxins from the gut may be major contributors to the extent of liver injury induced by an unrelated toxin.

Br J Dermatol, 1978 Aug, 99(2), 117 - 37
The pathogenesis of miliaria rubra . Role of the resident microflora; Holzle E et al.; Anhidrosis was induced in volunteers by covering the skin with an impermeable plastic film . The degree of sweat suppression and miliaria after a thermal stimulus was directly proportional to the increase in the density of resident aerobic bacteria, notably cocci . No anhidrosis resulted when antibacterial substances were used to prevent the expansion of the microflora . Histological study showed a PAS-positive diastase resistant amorphous mass deep within the acrosyringium after 2 days of occlusion, accompanied by a periductal dermal infiltration of leukocytes . After another 2 days the duct became clogged by an amalgam of degenerating leukocytes . This impaction sloughed after about 3 weeks as a result of epidermal renewal . Colonies of bacteria were never found within the ducts . It is postulated that cocci secrete a toxin which injures luminal cells and precipitates a cast within the lumen . Infiltration by leukocytes creates an impaction which completely obstructs the passage of sweat for several weeks.

Br J Surg, 1978 Aug, 65(8), 560 - 4
Primary suture of the perineal wound following rectal excision for imflammatory bowel disease; Marks CG et al.; Delay in healing of the perineal wound is a major cause of disability in patients after excision of the rectum . The outcome of primary suture in 76 patients treated at St Mark's Hospital between 1967 and 1976 was correlated with a number of factors describing the patients, their preparation for surgery and details of surgical technique and management . The perineal wound healed by first intention in 33 patients . The remaining 43 patients regarded as failures included 7 with delayed breakdown after initial healing . The results showed that women fared better than men . Excision of the rectum following colectomy and ileostomy was associated with failure of the perineal wound to heal in 9 out of 10 patients . Treatments with peroperative ampicillin and topical antibacterial agents were both correlated significantly with success . Preoperative sepsis and operative contamination were followed by perineal sepsis and wound breakdown on 16 out of 21 occasions . Discriminant analysis showed that topical and peroperative antibacterial treatments, sex, preoperative sepsis and finally ACTH were the most important variables in descending order of importance . The prediction of success and failure by this procedure was 72.4 per cent correct.

J Infect Dis, 1978 Aug, 138(2), 125 - 33
Antibacterial functions of macrophages in experimental protein-calorie malnutrition . I . Description of the model, morphologic observations, and macrophage surface IgG receptors; Keusch GT et al.; An experimental protein-calorie malnutrition was produced in weanling Sprague-Dawley rats . The model resembles human malnutrition with respect to weight loss, inanition, angular stomatitis, anemia, lymphopenia, hypoproteinemia with hypoalbuminemia, and marked thymic involution . In addition, systemic invasion by gram-negative rods was documented . However, no edema was produced, and animals did not survive for longer than six weeks on the protein-deficient diet . One percent glycogen was found to be a satisfactory nonprotein stimulus for induction of a peritoneal exudate consisting primarily of young macrophages . Electron microscopy showed that morphologic events of phagocytosis and degranulation proceeded normally in macrophages from protein-deficient animals . In addition, cell surface receptors for IgG were preserved under these experimental conditions . These data indicate that weanling rats may be employed as a small animal model for servere, fulminant protein-calorie malnutrition in humans.

Antibiotiki, 1978 Aug, 23(8), 675 - 6
{Search for new antitumor antibiotics in the bleomycin group}; Gauze GF et al.; The culture of Penicillium avellaneum 444 and its bleomycin resistant variant may serve a rather valuable specific test for detecting organisms producing new antitumor antibiotics of the bleomycin group . The organisms producing antitumor antibiotics of the group of anthracyclines (rubomycin and carminomycin), actinomycins and other chemical groups do not inhibit the growth of these test-organisms . Such tests are also resistant to the effect of antibacterial antibiotics.

Wien Klin Wochenschr, 1978 Jul 14, 90(14), 506 - 9
{Application of acerbine, a mixture of organic acids containing propylene glycol as lotion or ointment in paediatric surgery (author's transl)}; Geley L; Acerbine has been available for clinical trial since three years ago . Promotion of epithelialization, as well as antiphlogistic, antibacterial and fungicidal actions have been attributed to this preparation . This paper presents a critical appraisal of our own results with Acerbine; initial scepsis was soon dispelled by the evident efficacy of this preparation, both in the form of a lotion and ointment, and its wide scope of application . Moreover, our own studies revealed an excellent effect on keloids, which became smoother and visibly paler . A very good prophylactic and curative effect was observed in respect to all types of skin transplantation . So far Acerbine has been successfully applied in 117 patients who have completed their course of treatment . Acerbine is being currently employed in the case of 16 further patients who are still in hospital . No untoward side effects were recorded . Our findings confirm the opinion of other authors that hospitalization is shortened by the use of this preparation . The availability, more recently, of the new preparation in form of an ointment enables treatment to be continued on an ambulant basis or at home in many cases . Certain new fiies . The results of further explorative investigations into these aspects are under review at present.

Antibiotiki, 1978 Jul, 23(7), 642 - 4
{Effect of inhalatory therapy with antibacterial preparations on the fungal-yeastlike flora of the respiratory tracts in pulmonary tuberculosis}; Kulik NM et al.; A total of 254 patients with various forms of the lung tuberculosis were examined on the presence of the yeast-like flora; 130 patients out of them (the main group) were subjected to complex antibacterial therapy including inhalation with antitubercle drugs and 124 patients (control) were not treated with inhalation . On acceptance to the stationary the fungal flora was registered in 22.4% of the patients including 20.9% of the males and 29.2% of the females . The fungi were found more often in old patients (33.3%), patients with diseases of long duration (29.7%) and patients with fibrous cavernous tuberculosis of the lungs (27.1%) . It was shown that the local treatment of the patients suffering from the lung tuberculosis with antitubercle drugs including streptomycin had no significant effect on either the period of the fungi carrying (22.3% before the treatment and 21.5% after the treatment, P less than 0.05), or development of the fungal diseases (1.9% in the main group and 1.6% in the control group, P greater than 0.05).

Proc Natl Acad Sci U S A, 1978 Jul, 75(7), 3173 - 7
Oxygen-mediated heterogeneity of apo-low-density lipoprotein; Schuh J et al.; Mild oxidation of human serum low-density lipoprotein (LDL) converts the apoprotein from a nearly homogeneous component of high apparent molecular weight to a mixture of apparently lower molecular weight polypeptide components, as characterized by sodium dodecyl sulfate/polyacrylamide gel electrophoresis . This protein alteration, which correlates temporally with increases in the formation of lipid oxidation products and in the fluorescence of the apoprotein, is markedly reduced when oxygen is excluded or when EDTA or the free-radical-scavenging antioxidants, butylated hydroxytoluene or propyl gallate, are added . The conversion thus appears to be due to a reaction between the protein moiety and auto-oxidizing lipid . The presence of the antibacterial agent sodium azide markedly accelerates the oxidation, suggesting that it should only be used with caution in lipid-containing solutions.

J Med Chem, 1978 Jul, 21(7), 639 - 43
Folate antagonists . 12 . Antimalarial and antibacterial effects of 2,4-diamino-6-{(aralkyl and alicyclid)thio-, sulfinyl-, and sulfonyl}quinazolines; Elslager EF et al.; A series of 2,4-diamino-6-{(aralkyl and alicyclic)thio-, sulfinyl-, and sulfonyl}quinazolines was prepared via condensation of 5-chloro-2-nitrobenzonitrile or 5,6-dichloro-2-nitrobenzonitrile with the appropriate aralkyl or alicyclic thiopseudourea, reduction of the resulting 2-nitro-5-{(aralkyl or alicyclic)thio}benzonitrile with stannous chloride to the amine, and cyclization with chloroformamidine hydrochloride . Oxidation was effected with hydrogen peroxide or the bromine complex of 1,4-diazabicyclo{2.2.2}octane . These analogues when examined for suppressive activity against drug-sensitive lines of Plasmodium berghei in mice were not as active as 2,4-diamino-6-{3,4-dichlorobenzyl)amino}quinazoline (Ia).

Arch Ophthalmol, 1978 Jul, 96(7), 1262 - 4
Efficacy of penicillin G, cefazolin, and gentamicin in M-K medium at 4 degrees C; Baum J et al.; Corneal-scleral shells are routinely stored in McCarey-Kaufman (M-K) medium at 4 degrees C . Antibiotics are added to the medium to suppress bacterial growth . We examined the antibacterial activity of penicillin G potassium, 100 microgram/ml, cefazolin sodium, 100 microgram/ml, and gentamicin sulfate, 20 microgram/ml against test organisms in M-K medium at 4 degrees, 23 degrees, and 37 degrees C for periods up to 18 hours . Within the limits of the experimental conditions, none of the antibiotics used could be relied on to sterilize an inoculum of sensitive bacteria in M-K medium at 4 degrees C, the recommended storage temperature.

Arthritis Rheum, 1978 Jul-Aug, 21(6), 681 - 9
Hematologic and serologic studies in 6-sulfanilamidoindazole arthritis; Miller ML et al.; 6-sulfanilamidoindazole (6-SAI), an antibacterial sulfonamide, is known to cause an acute, self-limited inflammatory reaction in the hind paws of older rats . Administration of 6-SAI results in hyperfibrinogenemia which precedes the onset of clinical arthritis . The hyperfibrinogenemia is associated with the prolongation of dilute blood clot lysis times, appearance of heparin-precipitable fibrinogen, elevations in fibrin degradation products, and complement titers and serum electrophoretic pattern changes that consist of decreased albumin concentrations and increased beta globulin concentrations . Alterations in 6-SAI medicated young rats are less marked and require higher doses.

Vet Rec, 1978 Jun 17, 102(24), 523 - 4
Distribution of trimethoprim/sulphadiazine in plasma, tissue and synovial fluids; Piercy DW; The subcutaneous implantation of tissue cages was used to study the distribution of trimethorprim and sulphadiazine into tissue (interstitial) fluid in calves, sheep and dogs over a 24-hour period . After oral dosing there was good gastrointestinal absorption of both antibacterial agents in dogs but only of the sulphonamide in sheep . The concentration of trimethoprim in tissue fluid peaked at five to seven hours after administration when it exceeded the plasma concentration . Sulphadiazine persisted in the plasma for longer than trimethoprim, but distribution into tissue fluid was slower . The findings show that reliance on plasma concentration curves alone in determinations of bioavailability of chemotherapeutic agents may lead to false interpretations.

Can Med Assoc J, 1978 Jun 10, 118(11), 1395 - 8
Use of a topical antibiotic spray in vaginal surgery; Wright VC et al.; During vaginal hysterectomy with or without colporrhaphy a topical aerosol spray containing neomycin sulfate, polymyxin B sulfate and zinc bacitracin was used in 50 patients to decrease the change of postoperative pelvic infection; a placebo spray was used in another 50 patients . All patients were treated preoperatively with povidone iodine and postoperatively with nitrofurantoin and an antibacterial irrigating solution for the bladder if catheter drainage was necessary . The frequency of postoperative pelvic infection was 16% in the group sprayed with the antibiotic combination and 34% in the group sprayed with the placebo, a significant difference (P less than 0.05).

Ciba Found Symp, 1978 Jun 6-8, (65), 285 - 94
The lactoperoxidase-thiocyanate-hydrogen peroxide antibacterium system; Reiter B; Lactoperoxidase present in various secretions oxidizes thiocyanate (SCN-) in the presence of H2O2 to an unstable oxidation product--hypothiocyanite (OSCN-), which is bactericidal for enteric pathogens including multiple antibiotic resistant strains of E . coli . The system damages the inner membrane causing leakage and cessation of uptake of nutrient, leading eventually to death of the organisms and lysis . The possible involvement of O2- and 1O2 is discussed.

Farmaco {Sci}, 1978 Jun, 33(6), 438 - 52
{Reactions of potassium salts and methyl esters of some aroylhydrazino-carbodithioic acids}; Mazzone G et al.; In continuation of previous research designed to obtain compounds of pharmacological interest, the following substances were prepared, from the potassium salts (I-III) and from the methyl esters (IV-VI) of some aroylhydrazinocarbodithioic acids, derivatives of 1,3,4-oxadiazole (VII-XV), of 3-aminorhodanine (XVI-XVIII), of 1,2,4-triazole (XIX-XXI), of 7H-(1,2,4)-triazol{3,4-b} {1,3,4} thiadiazine (XXII-XXIV) and of 1,3,4-thiadiazole (XXV-XXX) . The compounds have present in the molecule a nucleus and radical which have produced marked biological activity in other series of compounds . To date some of the above compounds have shown antibacterial, antimycotic and antimitotic activity.

J Antibiot (Tokyo), 1978 Jun, 31(6), 561 - 9
Diastereomeric 7-ureidoacetyl cephalosporins . II . 7beta {{{(Aminocarbonyl) amino}-2-thienylacetyl} amino}-7-methoxy-3-{{(1-methyl-1H-tetrazol-5-yl) thio} methyl}-8-oxo-5-thia-1-azabicyclo {4.2.0} oct-2-ene-2-carboxylic acid; Applegate HE et al.; The synthesis and antibacterial activity in vitro of 7-methoxylated cephalosporins having a thienylureidoacetyl or a thienylglycyl C-7 side-chain are described . Acylation of 7 beta-amino-7-methoxycephems with a novel 2-aminooxazolone hydrochloride under neutral conditions gave the thienylureidoacetyl derivatives in good yield with retention of configuration . 7 beta-{{D-{(Aminocarbonyl)amino}-2-thienylacetyl}amino}-7-methoxy-3-{{(1-methyl-1H-tetrazol-5-yl)thio} methyl}-8-oxo-5-thia-1-azabicyclo{4.2.0}oct-2-ene-2-carboxylic acid sodium salt (SQ 14,359) was found to have a broad-spectrum of antibacterial activity in vitro, particularly against beta-lactamase-producing organisms.

Arch Intern Med, 1978 Jun, 138(6), 925 - 7
Mucormycosis . A complication of critical care; Agger WA et al.; Lethal nosocomial mucormycosis developed in three previously well individuals while they were receiving intensive care for acute hemorrhagic pancreatitis, for cardiogenic shock, and for a ruptured intra-abdominal aortic aneurysm . In two cases, the condition was first seen as progressive cavitary pneumonia refractory to antibacterial therapy; Mucoraceae was identified in all three patients only at autopsy . Each patient had received large doses of corticosteroids and broad-spectrum antibiotics, and all had suffered from respiratory failure, acute renal failure with acidosis, and severe hyperglycemia in association with total parenteral nutrition . Mucoraceae should be regarded as an additional nosocomial pathogen in the setting of advanced life-support care.

Zentralbl Bakteriol {Orig B}, 1978 Jun, 166(6), 528 - 39
Studies on the mode of action of phenylmercuric borate on Escherichia coli . II . Biochemical localization and inhibition of some metabolic activities; Cortat M; The biochemical localization of phenylmercuric borate (PHB) on Escherichia coli shows that this disinfectant associates essentially with proteins . Protein electrophoresis demonstrates that each protein contains PHB, and that SH groups play a very important role in its fixation . The quantity of PHB able to associate with proteins is so large that many other electron donor groups must react with it . Moreover, it appears that concentration of PHB on cytoplasmic membrane results rather from the privileged position of this structure than from special physicochemical properties . The great reactivity of PHB towards proteins leads to numerous inhibitions and confers upon this antibacterial drug a very complex mode of action . Four important metabolic activities have been tested in the presence of PHB, namely: respiration, protein-synthesis, RNA synthesis and DNA synthesis . These four metabolic functions are rapidly and totally inhibited at low concentrations of PHB . The complexity of the mode of action of PHB makes the adaptation of bacteria to this disinfectant more difficult . In addition, in the case of plasmid dependent resistence, PHB, with its complexe mode of action, does not favour such a selection in opposition to the antibiotics which generally have a more specific mode of action.

Oral Surg Oral Med Oral Pathol, 1978 Jun, 45(6), 947 - 54
The bactericidal potential of various endodontic materials for primary teeth; Cox ST Jr et al.; An in vitro study of the bactericidal or bacteriostatic effects of several pulp therapy compounds and their components on selected bacterial commonly isolated from infected primary teeth was undertaken . It was determined that zinc oxide had no inhibitory effects on E . coli, Staph . aureus, and Strep . viridans; however, the addition of eugenol to this system retarded the growth of only the grampositive organisms . The inclusion of zinc acetate as a setting accelerator inhibited both gram-positive and gram-negative bacteria . Also the inhibitory effects on these three organisms could be greatly enhanced by the addition of formocresol or paraformaldehyde to the zinc oxide--eugenol--zinc acetate system . It was also noted that Sargenti's N-2 paste was apparently no more effective in retarding growth of these organisms than the mixtures . Only the lead tetroxide and hydorcortisone present in the N-2 paste was toxic to the Staph . aureus but not to E . coli or to Strep . viridans . The other heavy metals in N-2 apparently have no antibacterial activity in the manner in which they were tested . This evidence suggests, but is not conclusive, that zinc oxide--eugenol--zinc acetate, with or without formaldehyde-containing compounds, may be effective in the elimination of bacteria from pulpotomized primary teeth . Therefore, the addition of highly cytotoxic chemicals which will remain sealed in a root canal and be active for extended periods of time may not be necessary for successful treatment.

J Infect Dis, 1978 Jun, 137(6), 830 - 4
Probenecid and the antibacterial activity of cephradine in vivo; Kunst MW et al.; The influence of probenecid on the concentrations in blood and antibacterial efficacy of cephradine was studied in experimentally infected mice . An infection was induced by injection of 5 X 10(6) Escherichia coli into the thighs of irradiated, granulocytopenic mice . Probenecid was given 1 hr later, just before the administration of cephradine . The control animals received only the vehicle . Concentrations of cephradine in blood were determined for 2 hr; the antibacterial activity was estimated from bacterial counts made in the homogenized individual thighs . The blood concentrations of cephradine were 1.77 times higher in the probenecid-treated animals than in the controls . The potency ratio for doses was 2.41, the potency ratio for the areas under the drug concentration in blood vs . time curves was 1.34, and that for the peak blood concentrations was 1.43.

Am J Med, 1978 Jun, 64(6), 933 - 6
Acidosis of synovial fluid correlates with synovial fluid leukocytosis; Ward TT et al.; The antibacterial activity of aminoglycoside antibiotics is significantly reduced by lowering the pH of the incubation medium . Since gram-negative septic arthritis responds poorly to aminoglycoside antibiotic therapy, we sought to determine whether synovial fluid acidosis contributes to this poor outcome . Synovial fluid samples from 22 patients with various forms of acute and chronic arthritis were examined for white blood cell count and pH . A close correlation (r = -0.92, p is less than 0.001) between an increasing white blood cell count and a decreasing pH was demonstrated . Since septic arthritis is associated with high white blood cell counts, in synovial fluid, the resultant low pH may contribute to the poor response to gram-negative septic arthritis treated with aminoglycoside antibiotics.

Science, 1978 May 26, 200(4344), 902 - 7
Immunization against infectious disease; Mortimer EA Jr; Mortality and morbidity from infectious diseases in the United States have declined more than 90 percent since 1900 . Factors believed to be responsible for this decline include changes in the natural history of disease, sanitation, quarantine measures, control of nonhuman vectors, antibacterial drugs, and immunization . The contributions of each of these factors differ among the various infectious diseases; except for smallpox and diphtheria control, immunization had little effect until after World War II . The success of present and future immunization programs is endangered by public and physician complacency and by complex legal and ethical problems related to informed consent and responsibility for rare, vaccine-related injury.

J Antibiot (Tokyo), 1978 May, 31(5), 441 - 50
Modification of seldomycin factor 5 at C-3'; Carney RE et al.; Attempted removal of the 3'-hydroxyl group of seldomycin factor 5 via displacement of a sulfonate ester has led to 3'-epi-seldomycin factor 5 . Removal of the hydroxyl group has been effected by the Barton procedure . The antibacterial activity of 3'-epi- and 3'-deoxyseldomycin factor 5 against various aminoglycoside-resistant strains is discussed.

J Pharm Sci, 1978 May, 67(5), 706 - 9
Electronic structure--activity relationships of antibacterial acridines; Singh P et al.; The antibacterial activity of a series of amino- and fluorinated acridines was studied in the framework of their electronic structures . To calculate the electronic structure, a simple Huckel molecular orbital theory was used . A statistical regression analysis revealed linear correlations between the activity and the electronic indexes, particularly the electron density at the ring nitrogen.

South Med J, 1978 May, 71(5), 512 - 5
Treatment of Nocardia asteroides infection with trimethoprim-sulfamethoxazole; Cook FV et al.; Although sulfonamide therapy has reduced the case fatality rate in infection due to Nocardia asteroides from nearly 100% to 25% to 45% there remains a need for a still more effective chemotherapeutic regimen . We describe three cases of serious infection due to N asteroides treated successfully with trimethoprim-sulfamethoxazole (TMP-SMX) and review an additional 15 cases from the world literature . Trimethoprim and sulfamethoxazole exhibit a synergistic interaction in vitro against N asteroides, and the agent reaches antibacterial concentrations in blood, lung, and the central nervous system . Clinical results have been satisfactory in the limited number of patients treated to date.

J Med Chem, 1978 May, 21(5), 493 - 5
Mitomycin antibiotics . Synthesis of 7-methoxy-1-(N-pyrrolidino)mitosene and its methiodide; Mott J et al.; 7-Methoxy-1-(N-pyrrolidino)mitosene and its methiodide were synthesized . The latter compound was a potential bifunctional alkylating agent because of its two good leaving groups appropriately situated with respect to the indoloquinone chromophore . However, it was inactive in bacteriophage induction and P388 murine leukemia assays . Both compounds showed antibacterial activity in culture, and the former compound was very weakly active in inducing lysogenic bacteriophage.

Pharmazie, 1978 Apr, 33(4), 196 - 8
Studies in potential organo-fluorine antibacterial agents . Part 1: Synthesis and antibacterial activity of some fluorinated arylsulfonylthiosemicarbazides and Arylsulfonylhydrazones; Joshi KC et al.; A series of fluorinated arylsulfonylthiosemicarbazides and arylsulfonylhydrazones has been synthesized . A representative number of the synthesized compounds have been screened for their antibacterial activity but none of the compounds showed significant activity.

Pharmazie, 1978 Apr, 33(4), 184 - 5
The scope of the reactions of hydrazines and hydrazones . Part 4: Trisubstituted pyrazoles of possible hypoglycemic and antibacterial activity; Soliman R et al.; Condensation of ethyl 2,4-dioxo-6-phenyl hex-5-enoate (1) with 4-substituted sulphamyl phenylhydrazines (2) led to 1-aryl-3-ethoxycarbonyl-5-styrylpyrazoles (3) which on hydrolysis gave 1-aryl-5-styrylpyrazole-3-carboxylic acids (4) and upon permanganate oxidation gave 1-aryl-3-ethoxycarbonylpyrazole-5-carboxylic acids (5) . Similar condensation of hydralazine (6) with (1) gave the corresponding pyrazole (7) which on hydrolysis gave the acid 8.

J Cell Sci, 1978 Apr, 30, 21 - 35
Ultrastructural localization of cationic proteins in human polymorphonuclear leukocytes; Brown WJ et al.; The present investigation is concerned with the use of the post-formalin ammoniacal silver reaction to detect the arginine-rich cationic proteins in human polymorphonuclear leukocytes at the ultrastructural level . These proteins appear to function as neutral proteases in antibacterial action and as mediators of inflammation . Originally, the ammoniacal silver reaction relied upon primary fixation in dilute formalin which prevented optimum fixation of tissues . This study shows that by using the proper sequence of glutaraldehyde fixation and the ammoniacal silver solution in conjunction with osmium tetroxide treatment, better fixation of the tissue and localization of the ammoniacal silver reaction can be achieved . Also, the ammoniacal silver reaction in human polymorphonuclear leukocytes is exclusively located in the large, crystalline cytoplasmic granules of eosiniphils . All other cytoplasmic granules of neutrophils, eosinophils, and basophils were found to be devoid of the ammoniacal silver reaction product . These results are contrary to previously published experimental data . Possible explanations for this discrepancy are discussed.

Antibiotiki, 1978 Apr, 23(4), 317 - 21
{Experimental studies to set hygienic standards for benzylpenicillin in the air of a work area}; Shteinberg GB et al.; The character and level of benzylpenicillin toxic effect was studied in accordance with the methodic instruction for performance of the experiments on toxicological estimation and hygienic norms of antibiotics in the air of working areas in production premises . It was shown that the antibiotic was of low toxicity under conditions of a single exposure, did not cumulate and had no local irritating and resorbing effect . It was shown to be an allergen . Prolonged inhalation of benzylpenicillin in a concentration of 14 mg/m3 resulted in reversible changes in the function of the kidneys and liver of the animals, their sensitization and development of pronounced dysbacteriosis of the mouth and intestine mucosa . In a concentration of 1 mg/m3 benzylpenicillin had no general toxic and sensitizing effect but induced reversible changes in the normal autoflora . This allowed the authors to consider the above concentration to be maximum with respect to the antibacterial effect . On the basis of the experiments the maximum permissible norm (MPN) of the aerosol of benzylpenicillin disintegration was recommended at the level of 0.1 mg/m3.

Am J Vet Res, 1978 Apr, 39(4), 633 - 8
Hemostatic function in swine as influenced by warfarin and an oral antibacterial combination; Osweiler GD; Pertinent literature on naturally occurring hemorrhagic diseases in poultry and livestock were reviewed and compared with reports on recent outbreaks of a hemorrhagic syndrome in swine . Epizootiologic, clinical, and hematologic data from porcine hemorrhagic disease suggest vitamin K-responsive hypoprothrombinemia . In weanling pigs, the toxicity of warfarin was compared with that in swine given tylosin and sulfamethazine antibacterial combination versus those given warfarin only . Toxicosis was induced in weanling swine fed warfarin daily at dose level of 0.055 mg/kg of body weight . Approximately 5 days after feeding was started, signs of poisoning appeared: lameness, anorexia, subcutaneous hematomata, melena, and periarticular enlargement . Administration of warfarin at dose level of 0.017 mg/kg did not cause clinical toxicosis, and 0.028 mg/kg produced significant increases in one-stage prothrombin time (OSPT) and activated partial thromboplastin time (APTT), but no evidence of clinical bleeding . When tylosin-sulfamethazine antibacterial combination was fed at normal and high dose levels concurrently with warfarin at dose level of 0.017 mg/kg of body weight, increase of clotting time, OPST, or APTT did not occur due to antibacterial influence . The antibacterial combination fed alone did not produce changes in clotting time, OSPT, APTT, fibrinogen, total protein, differential leukocyte count, or packed cell volume.

J Parasitol, 1978 Apr, 64(2), 193 - 7
Evidence that sulfisoxazole, an antibacterial sulfonamide, can adversely affect the development of Brugia pahangi in Aedes aegypti mosquitoes; Jaffe JJ et al.; The average number of infective larvae recovered from Brugia pahangi-infected Aedes aegypti was approximately one-half that recovered from the controls after the former group of infected mosquitoes had ingested a 1.0% solution of sulfisoxazole diolamine (SXZ) in 10% sucrose-water for 4 consecutive days, beginning 4 days after infection . Most of the filarial larvae from the SXZ-treated mosquitoes were small and sluggish compared with those from the controls . There was no increased mortality of mosquitoes that ingested 1.0% SXZ in sugar-water for 4 days . Average filarial larval burdens were not decreased in mosquitoes that ingested a solution of 10(-6) M methotrexate (MTX), a potent dihydrofolate reductase inhibitor, in sugar-water for 4 days, beginning 4 days after infection . The distributional pattern of larval burdens in mosquitoes that ingested combined 1.0% SXZ and 10(-6) M MTX in sugar-water for 4 days closely resembled that seen in mosquitoes that had imbibed 1.0% SXZ only . Average filarial larval burdens were not decreased in mosquitoes with 4-day-old B . pahangi infections that fed upon jirds which received intraperitoneal injections of SXZ (2 g/kg) and MTX (1 mh/kh), alone and in combination, 1 hr previously . Survival of the mosquitoes that fed upon the drug-treated hosts was unaffected, as was the hatchability of their eggs and subsequent growth and development of the mosquito larvae.

Zh Mikrobiol Epidemiol Immunobiol, 1978 Apr, (4), 31 - 7
{Natural antibodies (isohemagglutinins, heterophilic, antierythrocytic and antibacterial) in children with congenital immunologic deficiency syndromes}; Krizon SS et al.; Examination of 30 patients with immunodeficient diseases showed that the system of natural antibodies was considerably changed depending on the form and the extent of deficiency of the immune system: in agammaglobuinemia the antibodies under study were almost completely absent, and in immunological insufficiency with ataxia-teleangiectasis the production of antibacterial antibodies proved to be sharply decreased . The data obtained can be used both for the diagnosis of immunodeficiencies and for control of the restoration of the immunological competence after a number of therapeutic measures, particularly after the transplantation of the thymus-sternum complex.

Ann Microbiol (Paris), 1978 Apr, 129(3), 265 - 84
Morphological mutants of Escherichia coli: nature of the permeability barrier in mon and envC cells; Starkova Z et al.; Morphological mon mutants and a chain-forming envC mutant of Escherichia coli K12 are hypersensitive to detergents and to various other antibacterial agents . Electron microscopy shows that the cytoplasmic membrane of growing mon and envC cells is dissolved by detergents, and that the cytoplasm dissociates into two parts of unequal density . The mutant envC is sensitive to actinomycin D and to rifampicin, is lysed by lysozyme in the absence of EDTA, and releases alkaline phosphatase in the absence of osomotic shock, indicating a gross perturbation of its outer membrane.

J Pharm Pharmacol, 1978 Apr, 30(4), 236 - 9
The effect of various topical antibiotic and antibacterial agents on the middle and inner ear of the guinea-pig; Parker FL et al.; The topical application of antibiotics and anti-inflammatory agents is used to reduce inflammation of the middle ear mucosa and irradicate infection . Many of the antibiotic and anti-inflammatory preparations so used contain compounds known to be or are potentially ototoxic . Eighteen antibiotic, antibacterial, antifungal and anti-inflammatory compounds and four commonly used solvents were screened for the absence of ototoxicity and inflammation to the middle ear mucosa . All compounds were injected intra-tympanically and sensory hair cells loss recorded graphically . Inflammation of the middle ear mucosa was assessed macroscopically . Of the 18 compounds only three, penicillin, carbenicillin and nystatin were free of hair cell toxicity and inflammatory effects on the middle ear mucosa . Only one of the commonly used solvents was free of side effects.

J Pharm Sci, 1978 Mar, 67(3), 413 - 5
S-(4-Chlorophenyl) 3-aryl-3-hydroxypropanethioates as antibacterial agents; Snyder HR Jr et al.; A series of S-(4-chlorophenyl) 3-aryl-3-hydroxypropanethioates was prepared and shown to have in vitro activity against several selected bacterial species.

Antibiotiki, 1978 Mar, 23(3), 273 - 5
{Antibacterial therapy of liver abscesses of varying etiology}; Aliev VM; The investigation of microbial flora and its sensitivity in 196 patients with the kidney abscesses of various etiology showed expediency of the use of aminoglycosides, ampicillin and lincomycin . The local use of colloid iodine promoted rapid inhibition of the microbial flora . The dynamic observations showed an increase in the number of gramnegative pathogens by the 7th--10th day of the treatment . Rational surgical intervention, the antibiotic use with control of the microbial flora sensitivity, specific chemotherapy provided a decrease in the lethality up to 6.7 per cent.

Antibiotiki, 1978 Mar, 23(3), 250 - 3
{Tetracycline hydrochloride complex formation with collagen}; Rudenko TG et al.; The quantitative indices and regularities of tetracycline hydrochloride binding with colelagen in the process of complex formation were studied in vitro . It was found that tetracycline-interacted with collagen . The amount of the antibiotic bound depended on its initial concentration in the mixture and the aggregate state of the protein: the amount of tetracycline hydrochloride absorbed by dissloved collagen was 10 times higher than that absorbed by polymerized collagen . The antibiotic bound with collagen did not lose its specific antibacterial activity.

J Pharm Sci, 1978 Mar, 67(3), 380 - 3
Differences in antibacterial activity of benzalkonium chloride; Richards RM et al.; Benzalkonium solutions obtained from different manufacturers were shown to have different activities . This difference in activity was related to the composition of the benzalkonium chloride . The potential seriousness of this situation is emphasized, and a recommendation is made that the official monographs on benzalkonium chloride be amended appropriately, noting the apparently superior antibacterial activity of the tetradecyl (C14) homolog.

Antimicrob Agents Chemother, 1978 Mar, 13(3), 479 - 83
Activity of flumequine against Escherichia coli: in vitro comparison with nalidixic and oxolinic acids; Greenwood D; The in vitro activity of the new antibacterial agent, flumequine, against Escherichia coli was compared with those of oxolinic acid and nalidixic acid . As judged by turbidimetric criteria, flumequine was considerably more active than nalidixic acid and slightly less active than oxolinic acid against both nalidixic acid-susceptible and -resistant strains . Resistance to all three drugs could be easily induced in vitro . The comparative efficacy of flumequine, oxolinic acid, and nalidixic acid was also tested in an in vitro model of the treatment of bacterial cystitis . In this system, suppression of bacterial growth was obtained with markedly lower concentrations of flumequine and oxolinic acid than of nalidixic acid, but prevention of the emergence of bacterial populations that exhibited increased resistance to these compounds depended on the maintenance of adequate drug levels.

Farmaco {Sci}, 1978 Feb, 33(2), 142 - 7
Antibacterial activity and chemical reactivity of sulphanylamides . Rate constants of alkaline hydrolysis of N4-acetylsulphanylamides; Albasini A et al.; The alkaline deacylation rate constants of a collection of N4-acetylderivatives of acidic and non-acidic sulphonamides (SA) clearly show a definite trend due to the intramolecular effects induced by the different substitutions on the N1 nitrogen . The rate constant is interpreted as a reactivity index of the corresponding non-acetylated compound, and is found to be strictly correlated with the electron-availability of the p-amino group; thus providing an interesting correlation with the antibacterial activity of these drugs . Moreover, the reported experiments corroborate early predictions that the greatest reactivity of the p-amino group pertains to p-aminobenzoate (PAB) in the series of chemically related compounds, and that SA anions show the highest chemical and electronic resemblance to the essential metabolite (PAB); thus the high antibacterial activity of SA anions correctly corresponds to its close resemblance to the metabolite.

Am J Vet Res, 1978 Feb, 39(2), 347 - 9
Relative efficacy of two oxytetracycline formulations and doxycycline in the treatment of acute anaplasmosis in splenectomized calves; Kuttler KL et al.; The efficacy of 3 antibiotic formulations was measured in the treatment of artificially induced anaplasmosis in the early stages of an ascending parasitemia (1% to 4%) in 23 splenectomized calves . Group 1, consisting of 5 calves, served as nontreated controls . Four calves (group 2) were treated 1 time with 10 mg of oxytetracycline (T-50)/kg of body weight IM; 5 calves (group 3) were treated 3 times with 10 mg of T-50/kg IM; 5 calves (group 4) were treated 1 time with 20 mg of an experimental oxytetracycline (T-200)/kg IM; and 4 calves (group 5) were treated 1 time with 10 mg of a synthetically derived antibacterial agent, doxycycline (D-100)/kg IM . All control calves died and 1 of 4 calves died that was treated 1 time with T-50 . Other deaths did not occur . All treatments were effective in moderating the infective process, but T-50 given 3 times and T-200 given 1 time were markedly more effective than T-50 and D-100 given 1 time . There appeared to be little or no difference in therapeutic efficacy between T-50 and D-100 given 1 time and between T-50 given 3 times and T-200 given 1 time.

J Med Chem, 1978 Feb, 21(2), 221 - 5
Chemical modification of 1,4-diamino-1,4-dideoxy-3-O-(4-deoxy-4-propionamido-alpha-D-glucopyranosyl)-D-glucitol; Ponpipom MM et al.; Chemical modification of the 4'-N position of 1,4-diamino-1,4-dideoxy-3-O-(4-deoxy-4-propionamido-alpha-D-glucopyranosyl)-D-glucitol (GlA1) in the form of 4'-N-acyl analogues, e.g., 3, led to no significant potency enhancement . The n-propylamino analogue 4 was more active against gram-positive bacteria but was less act vs . gram-negative bacteria . The intrinsic activity of the 6'-chloro analogue 15 like the antibiotic GlA1 was not high, but the antibacterial spectrum was broad with moderate activity against most resistant organisms.

J Pharm Sci, 1978 Feb, 67(2), 281 - 2
Synthesis and antibacterial evaluation of 2-(substituted phenylureido)-4-thiocyanatobenzothiazoles; Alaimo RJ et al.; The synthesis and antibacterial evaluation of a number of 2-(substituted phenylureido)-4-thiocyanatobenzothiazoles are described . The more active compounds against the test organisms in vitro generally were those substituted with halogens on the phenyl and benzothiazole rings.

J Med Chem, 1978 Feb, 21(2), 189 - 93
Semisynthetic aminoglycoside antibacterials . 6 . Synthesis of sisomicin, Antibiotic G-52, and novel 6'-substituted analogues of sisomicin from aminoglycoside 66-40C; Davies DH et al.; The discovery of aminoglycoside 66-40C, a novel dimeric, unsaturated imine produced by Micromonospora inyoensis, afforded a versatile intermediate for the synthesis of a variety of sisomicin analogues modified at the 6' position . The conversion of 66-40C into sisomicin, antibiotic G-52, and a series of novel 6'-substituted analogues of sisomicin is described, and the biological activity of the products is discussed.

J Dairy Res, 1978 Feb, 45(1), 109 - 18
Antibacterial effect of the lactoperoxidase system on psychotrophic bacteria in milk; Bjorck L; Activation of the antibacterial lactoperoxidase system in milk, i.e . increasing the thiocyanate concentration to 0.25 mM and adding an equimolar amount of H2O2, results in a substantial reduction of the bacterial flora and prevents the multiplication of psychrotrophic bacteria for up to 5 d . This treatment has no effect on the physico-chemical properties of milk and does not lead to the accumulation of resistant bacteria . The practical application of the lactoperoxidase system in prolonging the storage period of raw milk at low temperatures is discussed.

Infect Immun, 1978 Feb, 19(2), 510 - 4
Humoral bactericidal systems: antibacterial potential of serum from young animals; Skarnes RC; The antibacterial potential of fresh serum obtained from young animals during a pre-antibody period of development was assessed against two smooth and two rough strains of gram-negative bacteria . The bactericidal capacity of serum from 3- to 4-week-old guinea pigs and 4- to 5-week-old rabbits was compared with that of serum from adults . Serum from young animals was deficient in natural antibodies, and in conventional dilution assays the bactericidal action was unimpressive, especially against the smooth strains . However, when decimal increments of bacteria were incubated in fresh undiluted serum, killing of both smooth and rough strains proved substantial . This finding may have particular meaning in the very young animal when natural antibodies are at ebb: cellular defense mechanisms may function less efficiently at this time and effect a greater reliance on humoral antibacterial systems.

J Dent Res, 1978 Feb, 57(2), 171 - 4
Antibacterial activity of tooth-colored dental restorative materials; Orstavik D et al.; The antibacterial activity of dental restorative materials (12 resin based and one silicate) was tested in vitro against 5 species of bacteria . When fresh, all materials inhibited growth in pour plates of at least one bacterial strain . After storage in saline for 24 hours, the antibacterial activity was markedly reduced . There was a wide variation among the materials in the extent of their antibacterial activity . The bacterial strains apparently differed in their susceptibility to the antibacterial activity of the materials.

Aktuelle Gerontol, 1978 Feb, 8(2), 85 - 91
Natural antibody level in old age; Batory G et al.; Antibacterial antibodies were determined with a passive hemagglutination micromethod using the Boivin extract of eight different strains of bacteria . Correlation between antibody values of different specificities and between the summarized titer values and individual antibody titers were found . A significant decrease in the average of the summarized titer values was observed especially for persons over 70 . The possibility of genetic regulation of normal antibody levels is suggested . The question whether the decrease in agglutinating antibody level in old age is due to the decreased activity of the corresponding immunocompetent cells or is secondary to other changes occuring in old age, is discussed.

Ann Rech Vet, 1978, 9(2), 287 - 94
The effect of trypsin and chymotrypsin on the antibacterial activity of complement, antibodies, and lactoferrin and transferrin in bovine colostrum; Brock JH et al.; The effect of trypsin and chymotrypsin on antibacterial factors in bovine colostrum has been studied . Endogenous complement in colostrum was extremely sensitive to both enzymes . IgM was attacked by chymotrypsin but not by trypsin . Trypsin slowly attacked IgG1, causing loss of biological activity due to cleavage of both light and heavy chains . IgG1 was only very slightly attacked by chymotrypsin . Lactoferrin and transferrin in the iron-free state were both susceptible to proteolysis, but the iron saturated forms were more resistant and tended to give rise to stable iron-binding fragments.

Chemotherapy, 1978, 24(6), 360 - 3
In vitro antibiotic sensitivity of Moraxella species; Rosenthal SL et al.; Minimal inhibitory concentrations of 17 antibacterial agents for 34 Moraxella strains were determined using a plate dilution method . A strain of Moraxella nonliquefaciens was found which produced beta-lactamase and was resistant to ampicillin and carbenicillin but not to cephalothin . Several strains were relatively resistant to erythromycin and sulfisoxazole . Disk sensitivity tests could be used to reliably predict penicillin and erythromycin resistance but not sulfisoxazole resistance.

Acta Obstet Gynecol Scand, 1978, 57(4), 337 - 48
Ultrastructure and variations of human cervical mucus during pregnancy and the menopause; Chretien FC; Ultrastructural aspect and variations of cervical mucus have been studied by scanning electron microscopy in 58 pregnant and 29 menopausal women . In both groups, a striking tightening of the ultrastructural glycoprotein framework was demonstrated . The phenomenon appears to occur very rapidly at the beginning of pregnancy while patients near the menopause show more variable patterns . The results are compared to the known evolution of cervical mucus ultrastructure during the ovarian cycle and discussed from a rheological point of view . Particular attention was paid to the eventual antibacterial role of cervical mucus in pregnancy, which was found to be very plausible.

Infection, 1978, 6(4), 171 - 4
The concentration of thiamphenicol in severely diseased human kidneys; Plomp TA et al.; The concentration of thiamphenicol in serum and renal tissue was determined in 17 patients with severly diseased kidneys after an intravenous injection of 1000 mg of the drug . Two hours after the administration the renal tissue concentrations ranged in patients with hydronephrotic kidneys from 38.0-63.5 microgram/g, in patients with cirrhotic kidneys from 17.9-42.7 microgram/g, in patients with pyonephrosis from 9.8-17.6 microgram/g and in patients with renal carcinoma from 37.7-64.2 microgram/g . The patient with the renal sarcoma had a level of 138.7 microgram/g . At the same time the serum concentration ranged from 4.6-15.2 microgram/ml . The highest renal tissue/serum concentration ratios of thiamphenicol were observed in patients with hydronephrotic kidneys and renal tumours, the lowest in cases of pyonephrosis . The influence of severe renal disease on the renal tissue/serum concentration ratios of thiamphenicol is discussed . The high renal tissue levels of thiamphenicol in patients with severely diseased kidneys fulfill an important condition for the antibacterial chemotherapy of kidney infections.

Chemotherapy, 1978, 24(3), 121 - 33
Pharmacokinetics of cephalosporin antibiotics: protein-binding considerations; Singhvi SM et al.; The therapeutic activity of antibiotics depends on several factors including absorption, elimination kinetics, distribution in the body, minimal inhibitory concentrations (MIC), stability against enzymes, and plasma-protein binding . Some of these factors are interrelated, for example, the extent of protein binding of an antibiotic influences its elimination kinetics, distribution into tissues, MIC, and antibacterial activity . To evaluate the potential efficacy of an antibiotic, it is important to know the extent of its binding to plasma proteins especially since the protein-bound fraction of the antibiotic is devoid of antibacterial activity . Cephalosporins are a new class of broad-spectrum antibiotics that bind to plasma proteins in different degrees . Reported values for protein binding range from 6% for cephradine to 92% for cefazolin . The effects of protein binding of some of the commonly used cephalosporins on antibacterial activity and several pharmacokinetic parameters are discussed in this communication.

Vestn Khir Im I I Grek, 1978 Jan, 120(1), 70 - 2
{Diagnosis and treatment of subphrenic abscess}; Parakhnoiak VI et al.; The clinical picture of subphrenic abscess taking place against the background of the treatment with modern antibacterial drugs has changed essentially, which requires a complex solution of the problem of the timely abscess diagnosis . The antistaphylococcal plasma and gamma globulin applied together with other methods of intense therapy proved to be the most effective after the dissection of the abscess.

Infection, 1978, 6(1), 23 - 8
Assays of cephalosporin antibiotics administered prophylactically in open heart surgery . Determination of serum and tissue levels before, during and after cardiopulmonary bypass; Eigel P et al.; Twenty-eight patients who underwent open-heart surgery were divided into three groups, each of which received a different antibiotic from the cephalosporin series (cephalotin, cefazolin or cefamandole) in order to prevent infection . All antibiotics were given via intravenous infusion in a dosage of 2 g prior to surgery . To clarify the question of antibacterial activity under operative conditions with the cardiopulmonary bypass, the serum and tissue levels were determined before, during and after the surgical procedure . The effectiveness of the cephalosporins against bacteria most frequently encountered in open-heart surgery was demonstrated and substantiated by the serum and tissue concentrations . It became apparent that, in view of the favorable serum and tissue levels during and after the cardiopulmonary bypass, cefamandole should be considered the antibiotic of choice in preventing infections during open-heart surgery.

J Antibiot (Tokyo), 1978 Jan, 31(1), 43 - 54
Chemical modification of some gentamicins and sisomicin at the 3''-position; Nagabhurshan TL et al.; Chemical and photochemical oxidative methods of de-N-methylation of some gentamicins and sisomicins at the 3''-position are described . Selective acetylation of gentamicins and sisomicins at the 1, 3, 2' and 6' and of gentamicin B at the 1, 3, and 6'positions are achieved by treatment of the free bases with carbon dioxide prior to acetylation . De-N-methylation of the above selectively blocked gentamicins and sisomicins followed by re-alkylation at the 3''-position and de-N-protection gives a series of 3''-N-alkyl analogues . The in vitro antibacterial properties of the new derivatives of gentamicins and sisomicins are given.

J Pediatr, 1978 Jan, 92(1), 131 - 4
Oral antibiotic therapy for skeletal infections of children . I . Antibiotic concentrations in suppurative synovial fluid; Nelson JD et al.; To evaluate the feasibility of oral antibiotic treatment for pyogenic arthritis, one or more oral doses of antibiotics were substituted for the drugs being used for parenteral therapy . Synovial fluid and serum specimens obtained at randomized times after an oral dose of ampicillin, cephalexin, cloxacillin, dicloxacillin, or penicillin G were assayed for antibiotic content and antibacterial activity . Seventy specimens from 21 infants and children were studied . Peak synovial fluid concentrations were greater than 60% of peak serum concentrations with all drugs tested and there was adequate inhibitory activity against bacteria commonly causing arthritis . The degree of antibiotic binding to serum protein had no apparent effect on the degree of penetration into pyogenic synovial fluid.

Chemotherapy, 1978, 24(1), 17 - 23
Tri-minocycline: a minocycline complex for parenteral use . I . Antibacterial activity and toxicity data; Kahan IL et al.; Aqueous solutions of tri-minocycline (equivalent to 20--50 mg/ml minocycline HCl) and preconstituted ready-for-use injections were prepared at the pH of blood; these exert high antibiotic activities equal to those of the parent substance . The chloroform/water distribution coefficients of tri-minocycline in the different types of injections were somewhat lower, but in the same order of magnitude as that of the parent substance . The MIC values of tri-minocycline proved to be very low and the LD50 values very high, their separation covering more than 3 orders of magnitude.

Arzneimittelforschung, 1978, 28(9), 1602 - 4
{Experimental studies on topic application of amikacin to the eye (author's transl)}; Krasemann C et al.; The compatibility of amikacin as well as its penetration into the different tissues of the eye were studied experimentally in rabbits . Amikacin is well tolerated, both when applying drops and subonjunctival injections . When 1% solution of amikacin is dropped into the eye, antibacterially effective concentrations are achieved in the cornea and in the aqueous humour . There was only minimum penetration in the cornea found after subconjunctival injection . No amikacin was found in the vitreous body, neither when applying drops nor subconjuctival injections.

Arzneimittelforschung, 1978, 28(8a), 1466 - 70
Pharmacological properties of lidamidine hydrochloride (WHR-1142A), a novel antidiarrheal agent; Mir GN et al.; 1-(2',6'-Dimethylphenyl)-3-amidinourea hydrochloride (WHR-1142A, lidamidine hydrochloride), a potent, unique antidiarrheal agent, was tested for other pharmacological properties . It inhibited gastric acid secretion in both 4-h and 22-h pylorus-ligated rats and reduced mortality and gastric ulcer severity in the latter test . WHR-1142A also exhibited local anesthetic activity in the rabbit corneal reflex and guinea pig intradermal wheal tests and reverisbly blocked conduction in isolated frog nerves . Low doses of WHR-1142A increased plasma glucose concentration in fasted mice and rats and prolonged the hyperglycemia in response to a glucose meal . WHR-1142A showed mild diuretic activity but had no anti-inflammatory or antibacterial activity . The acute oral LD50 of WHR-1142A was 260 (208,328) mg/kg in male mice, 267 (212,336) mg/kg in male rats and 160 130,197) mg/kg in female rats.

J Int Med Res, 1978, 6(2), 94 - 101
Antibacterial activity of sisomicin; Rossi A et al.; A study of the in vitro antibacterial activity of a new aminoglycoside, sisomicin, is reported . The results show no significant differences between the activity of sisomicin and gentamicin.

Infection, 1978, 6(4), 166 - 70
Cefazolin and cephradine: relationship between serum concentrations and tissue contents in mice; Kunst MW et al.; The relationship between serum concentrations and tissue levels of various doses of cefazolin and cephradine was determined in experimentally infected mice . An infection was induced by injection of 5 X 10(6) Escherichia coli into the right hind leg, antibiotics were administered 1 h later . At 15-minute intervals mice were killed by exsanguination after a blood sample was taken, and the infected thigh was taken out and homogenized . The total amount of antibiotic per gram thigh muscle tissue was calculated on the basis of the concentration in the supernatant of the homogenate . From the parallel course between blood concentrations and total tissue contents it may be concluded that the thigh was easily accessible for both cephalosporins . The ratio between the total tissue content and the free serum concentrations was the same for both antibiotics despite the difference in protein binding between cefazolin and cephradine in mouse serum . This implies that the discrepancy between the relative antibacterial activity of the cephalosporins in vitro and in vivo found in earlier experiments cannot be explained by differences in accessibility of the tissue.

Infection, 1978, 6(3), 140 - 3
Indications, interpretation and applications of antibiotic assays; Yourassowsky E; Routine monitoring of serum levels is imperative when antibiotics are given to patients with impairment of renal function . Other desirable indications include: need for assessment of adequate aminoglycoside levels in the initial management of severe infection; chloramphenicol therapy; need for control of bioavailability of new drugs or of new derivatives of known compounds; specific clinical situations (unexplained therapeutic failure, assessment of the oral use of antibiotics as an adequate therapy in patient with severe infections; appraisal of the innocuity of topical antibiotics in burned patients or in patients with liver or renal insufficiency) . The serum antibacterial test is highly recommended for assessing the adequency of antibiotic therapy in patients with bacterial endocarditis and in infected patients with impaired host resistance such as those with leukopenia . Control of initial treatment in any severe infection, osteomyelitis (particularly when combined antibiotics are used) and tuberculosis are other indications of this test . Any attempt to correlate the results yielded by antibiotic assays with in-vivo effectiveness must take into account the patient himself and the several unknown factors which, in each individual case, can affect the ultimate result of the antibiotic therapy, such as antibiotic delivery to tissues, drug binding to cellular debris, intracellular penetration of the antibiotic, etc.

Antibiot Chemother, 1978, 23, 21 - 5
Yeast mutants with distorted cell membranes as a detection system for antitumor antibiotics; Gause GF et al.; Yeast mutants with distorted cell membranes, which are selectively inhibited by anticancer antibiotics and are not affected by antibacterial antibiotics, could be of considerable interest as test organisms . They could be used for the isolation of active antitumor substances from complex mixtures of natural compounds.

J Clin Pathol, 1978 Jan, 31(1), 12 - 5
Specific and non-specific resistance to aminoglycosides in Escherichia coli; Mawer SL et al.; The turbidimetric responses of a strain of Escherichia coli K12 to gentamicin and tobramycin were investigated . Both agents showed antibacterial activity below the conventionally measured minimum inhibitory concentration, but exposure to such subinhibitory concentrations of either agent generated a bacterial population which was able to grow in previously inhibitory concentrations at a rate equivalent to that of the parent culture . The increase in resistance was non-specific in that both aminoglycosides were equally affected, and was unstable on multiple passage in drug-free broth . The response to tobramycin was unaffected by the presence of an R factor conferring gentamicin resistance, but exposure of the R factor bearing strain to gentamicin caused a concomitant increase in the resistance to tobramycin, apparently by a non-specific adaptive mechanism similar to that observed with the parent strain . It is suggested that prior treatment of a gentamicin-resistant organism with gentamicin (as may occur during blind therapy) may adversely affect the subsequent response to other aminoglycosides.

Scand J Infect Dis Suppl, 1978, (14), 177 - 85
Antibiotics in bone tissues . Methodological and practical aspects; Dornbusch K; With regard to determination of antibiotic levels in bone, variance in results may be obtained as a consequence of type of the bones involved, degree of penetration of the drug used and of assay method performed . Measurements of antibacterial activity in bone from patients undergoing orthopaedic surgery were performed after preoperative treatment with doxycycline, lincomycin, clindamycin or cefuroxime . In performing the assay by the agar diffusion method, after extraction of the bone specimens in buffer according to classical systems, the concentrations of doxycyline were in the range of 0.05--0.6 microgram/g, clindamycin 0.4--4.9 microgram/g, lincomycin 1.7--2.9 microgram/g and of cefuroxine about 0.4 microgram/g . After electrophoresis in agarose-gel and followed by microbiological assay higher levels of these drugs were estimated possibly as a consequence of a diminution in the binding capacity of bone.

Scand J Infect Dis Suppl, 1978, (14), 118 - 24
The tissue cage model in the distribution of antibacterial agents; Chisholm GD; Developments in the measurement of interstitial tissue fluid using the tissue cage model are described . The design and physical characteristics of tissue cages are examined and evidence is presented to show that the fluid contained within these cages is representative of interstitial tissue fluid . The distribution of a variety of antibacterial agents into tissue cage fluid is examined and shows that this technique is a reliable experimental model for the study of drug distribution . The results also show that some antibacterial agents may never, normally, distribute into the tissue fluid and that the use of tissue homogenates, especially the kidney, is unreliable as a guide to the tissue concentration of a drug.

Scand J Infect Dis Suppl, 1978, (13), 37 - 46
On the pharmacokinetics of cephalosporin antibiotics; Andersson KE; A review is given on the pharmacokinetic characteristics of some cephalosporin antibiotics . The use of the pharmacokinetic parameters serum concentration, serum protein binding, serum half life, and apparent volume of distribution as a basis for the selection of the clinically most effective cephalosporin derivative is discussed . It is concluded that these parameters must be used in conjunction with data on tissue distribution to specialized sites, and with information on antibacterial activity and toxicity.

J Dent Res, 1978 Jan, 57(1), 43 - 7
Alterations in lactoferrin in salivary gland disease; Tabak L et al.; During the active phase of chronic recurrent parotitis there is a marked elevation in the parotid concentration of lactoferrin (Lf), and iron-binding glycoprotein with antibacterial properties . The Lf concentration decreases during the recovery period, but still remains above normal levels . The changes of Lf in parotitis parallel recent findings in mastitis and pancreatitis . Elevations in Lf were also noted in five of six subjects with Sjogren's disease, but not in subjects with sarcoidosis, diabetes or "dry mouth" without sialographic changes . The source of the Lf has not been determined; it could arise in part from disrupting polymorphonuclear leucocytes and in part from epithelial cells that synthesize Lf in the salivary glands . Inflammatory stimulation of Lf synthesis would suggest a basic protective mechanism in exocrine glands and should be fully explored.

Microbios, 1978, 21(85-86), 135 - 52
Cell composition and drug resistance in Escherichia coli; Hugo WB et al.; Resistance of micro-organisms to antibacterial drugs which cannot be attributed to a genetic change may often be traced to phenotypic changes in cell composition caused by differing growth conditions . To investigate an aspect of this attribute E . coli NCTC 86 was grown on a simple synthetic media containing alanine or cystine and, as a control, in nutrient broth . Cells grown on the media containing alanine and cystine showed a depleted total extractable lipid and phospholipid content . Phosphatidylethanolamine was notably reduced in both cases . Electrophoretic studies revealed a reduction in the surface lipid of cells grown on the simple synthetic media, while electron microscopy revealed defects in the cell wall of the cells grown on alanine . The total protein content of cells grown on alanine was reduced, whereas cells grown on the cystine showed an enhanced total carbohydrate content . Lipopolysaccharide synthesis was possibly also affected as judged by 2-keto-3-desoxy-D-manno-octonic aid content . The action of p-tertiary amylphenol, cetrimide and polymyxin B sulphate, showed that cells grown on the media containing alanine were most susceptible to the action of the phenol and cetrimide, whilst cells grown on the media containing cystine were most resistant to the action of polymyxin.

J Int Med Res, 1978, 6(1), 72 - 7
The effectiveness of topical antibacterials in acne: a double-blind clinical study; Franz E et al.; In a double-blind study, three groups of patients with mild to moderate acne were treated for eight weeks with topical acne creams containing the antibacterials triclosan or triclosan plus propylene phenoxetol . The formula without antibacterials served as the control . Total-face lesion counts, evaluation of the overall degree of inflammation of the lesions, and patient self-assessment showed the added efficacy of the antibacterials when incorporated into the control.

Folia Microbiol (Praha), 1978, 23(6), 438 - 43
Eurotium (Aspergillus) repens metabolites and their biological activity; Podojil M et al.; Eurotium repens mycelium cultivated under static conditions was used to isolate and identify metabolities--echinulin, physcion, erythroglaucin, flavoglaucin and asperentin; the filtrate of the culture yielded asperentin 8-methylether . The broadest biological activity spectrum was displayed by asperentin which had antibacterial and antifungal effects and, at a concentration of 86 microgram/ml, caused 50% mor7 tality in Artemia saline larvae . The highest cytotoxicity towards HeLa cells was found in physcion which caused 50% growth inhibition at a concentration of 0.1 microgram/ml.

Acta Microbiol Pol, 1978, 27(1), 63 - 71
Primary production and extracellular release by phytoplankton in some lakes of the Masurian Lake District, Poland; Chrost RJ et al.; The primary production and extracellular release by phytoplankton were measured at different depths of Mikolajskie Lake, Rynskie Lake and Beldany Lake (Masurian Lake District, Poland) . The release of dissolved organic compounds was found to be related to the rates of primary production . The percentage of extracellular release (PER) of organic matter in the photic zone showed an inverse relationship with particulate production and chlorophyll alpha concentration . The highest PER was determined in the epilimnion of the studied lakes, where also increased release was observed . The higher release of algal products of photosynthesis in the photic zone than in the profundal is probably caused by the inhibition of physiological activity of bacteria by antibacterial substances produced by algae . The substances released by algae in the profundal are taken up by aquatic bacteria which explains the lower release and PER measured.

Ann Anesthesiol Fr, 1978, 19(11-12), 909 - 13
{Postoperative peritoneal irrigation in generalized peritonitis treated in an intensive care unit}; Manelli JC et al.; Over a period of four years, 16 patients with generalized peritonitis have been treated by postoperative peritoneal irrigation in an Intensive Care Unit . The majority of cases involved postoperative peritonitis accompanied by severe visceral failure . The irrigation liquid, containing an antibacterial agent, was perfused for between one and eleven days at a high flow rate (mean 16.5 I) . The overall mortality in the series was extremely high (75 p . 100), and even greater (85 p . 100) if only the cases of postoperative peritonitis were considered . Anatomical examination of the peritoneum, performed on reintervention or at autopsy, revealed an abnormally high incidence of residual abscesses . These are responsable for the continuation or recurrence of infection, and explain the high mortality . These observations, combined with the frequent occurrence of local or general complications, led the authors to reject peritoneal irrigation in postoperative peritonitis in the presence of severe visceral failure, and to use it, in selected cases, only for periods not exceeding 48 hours.

Biochemistry, 1977 Dec 13, 16(25), 5573 - 8
Neocarzinostatin: effect of modification of side chain amino and carboxyl groups on chemical and biological properties; Samy TS; The antitumor protein neocarzinostatin (NCS), isolated from Streptomyces carzinostaticus, is a single chain polypeptide with 109 amino acid residues . Complete acylation of the amino groups (alanine-1 and lysine-20) was observed when NCS was allowed to react with 3-(4-hydroxyphenyl)-propionic acid N-hydroxysuccinimide ester at pH 8.5 . Since the ensuing bis{(alanine-1, lysine-20)-3-(4-hydroxyphenyl)}-propionamide NCS was fully active in antibacterial potency and in the inhibition of growth of leukemic (CCRF-CEM) cells in vitro, it appears that the two amino groups in the protein are not essential for biological activity . Radiolabeled NCS was prepared by using a tritiated or 125I-labeled acylating agent . Since the CD spectra of native and bis(alanine-1, lysine-20)-amino modified NCS were indistinguishable, there is presumably no change in the native conformation of the protein due to acylation . Reaction of NCS with ammonium chloride in the presence of 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide at pH 4.75 converted all the 10 carboxyl groups into carboxamides and produced a protein derivative of basic character . This modification caused a change in the native conformation of the protein accompanied by a loss in biological inhibitory activities.

J Med Chem, 1977 Dec, 20(12), 1665 - 8
3-(3-Substituted prop-1-enyl)cephalosporins; Beeby PJ et al.; The synthesis of cephalosporin derivatives possessing a 3-substituted prop-1-enyl group at the 3 position is described . This was achieved using the reaction of vinylmagnesium chloride with the 3-formyl derivatives 1 to give a vinylcarbinol which readily underwent allylic rearrangements to give the desired side chains . The new derivatives exhibited potent in vitro and in vivo antibacterial activity.

Inflammation, 1977 Dec, 2(4), 295 - 307
Steroids, aspirin, and inflammation; Katler E et al.; The ability of adrenal corticosteroids to both both suppress inflammation and compromise host defenses has been well documented . Recently, a series of in vitro and in vivo experiments, based on our new knowledge of the cell biology of inflammation and the biochemistry of the phagocytic cell itself, has provided new insights into the mechanism of steroid action in the inflammatory process . Evidence is presented that pharmacologic doses of steroids are capable of inhibiting each of the steps in phagocytic-micro-organism interaction: chemotaxis, recognition and opsonization, phagocytosis, membrane fusion, and degranulation . In addition, steroid alteration of the postphagocytic superoxide production, hydrogen peroxide generation, and prostaglandin and thromboxane synthesis is described . The antiinflammatory effects of aspirin and indomethacin can be explained almost entirely by virtue of their ability to inhibit cyclooxygenase, this preventing the transformation of arachidonic acid to both prostaglandins and thromboxanes . The cortisol-induced inhibition of endoperoxides, prostaglandins, and thromboxanes (at a site proximal to the release of arachidonic acid) may well explain those antiinflammatory actions that cortisone shares with aspirin . However, patients treated with nonsteroidal antiinflammatory agents effectively combat infections . In contrast, corticosteroids have more profound effects, as can be seen by the inhibition of superoxide production, with the subsequent decrease in hydrogen peroxide generation and the diminution in release of the antibacterial lysosomal hydrolases within the phagocytic vacuole . Thus, corticosteroids interfere with the killing of microorganisms . This new understanding of the pharmacologic action of cortisol on phagocytic cells explains, we believe, how glucocorticoids alleviate inflammation while, at the same time, they permit multiplication of the offending microorganism within the phagocyte.

Nord Vet Med, 1977 Dec, 29(12), 533 - 8
Studies of the pathogenesis of enteric E . coli infections in weaned pigs . The significance of the milk of the dam in preventing the disease; Svendsen J et al.; Milk from sows whose progeny developed post weaning E . coli diarrhoea (PWD milk) and from sows which were immunized by intramuscular vaccination using a homologous strain of E . coli (immune milk) were tested in ligated segments of pig intestine . The results showed that PWD milk neutralized the enterotoxigenic, fluid accumulating capacity of the lysate of the disease-causing E . coli pathogen . A similar effect was seen by using immune milk (Table I) . Neither PWD milk nor immune milk contained sufficient antibacterial activity to neutralize the fluid accumulating capacity of live cultures of E . coli O149:K91, while such activity was contained in immune serum . It is concluded that milk from sows whose progeny developed PWD contains antibodies capable of neutralizing the enterotoxigenic effects of the homologous E . coli organisms . It is suggested that the presence in milk from these sows of antibody-mediated activity against enteropathogenic E . coli organisms may be instrumental in preventing the disease in the progeny during the suckling period and consequently, when this protective milk supply stops at weaning, the disease may develop in susceptible animals, mainly because their own production of specific E . coli antibodies is insufficient to prevent PWD.

J Med Chem, 1977 Dec, 20(12), 1592 - 4
Studies of antitumor agents . 1 . Resolution of racemic 1-(tetrahydro-2-furanyl)-k-fluorouracil into the R and S isomers and examination of the biological activities of the isomers; Yasumoto M et al.; 1-(Tetrahydro-2-furanyl)-5-fluorouracil (Thf-FU), which is named Ftorafur or FT-207 and is used clinically as an antitumor agent, was conveniently synthesized by condensation of the trimethylsilyl derivative of 5-fluorouracil with 2-acetoxytetrahydrofuran using NaI as a catalyst . This optically inactive Thf-FU was resolved into optically active (R)-(+)- and (S)-(-)-Thf-FU in high optical purity and excellent yield by formation of diastereoisomers with brucine . 13C NMR data were obtained on Thf-FU and related compounds and the antibacterial activities and in vivo antitumor activities of these isomers were tested . The degradations of these isomers to 5-fluorouracil by liver microsomes were also examined . No significant differences were found in any of these properties of these isomers.

Farmaco {Sci}, 1977 Dec, 32(12), 909 - 22
Structure-activity correlations for antibacterial 1,5-benzodiazepine derivatives on gram-positive cells; Grieco C et al.; The antibacterial activity of a set of 1,5-benzodiazepine derivatives against Staph, aureus and Strep, pyogenes has been correlated with structural features of the compounds examined . It is shown by means of substituent constants and regression analysis that the lipophilic character of the molecule is the most important factor in determining its activity . Electronic and steric effects appear to be quite important.

J Dent Res, 1977 Dec, 56(12), 1599 - 602
Alkylamine salts and amides: in vitro inhibition of S mutans 6715; Warner VD et al.; Our studies with the salts and amides of alkylamines have shown that the undecylenate salts have significant in vitro activity against S mutans No 6715, suggesting that these agents are worthy of additional evaluation . The attempt to increase activity by combining undecylenic acid with the alkylamines was not successful; however, better attachment to tooth surfaces and/or retention during washing did occur . Our results suggest that the free amino group of alkylamines and the free acid group of undecylenic acid are required for these two classes of agents to demonstrate antibacterial activity.

Drugs, 1977 Dec, 14(6), 401 - 19
Vitamin A acid: a review of its pharmacological properties and therapeutic use in the topical treatment of acne vulgaris; Heel RC et al.; Vitamin A acid (retinoic acid: tretinoin) is a vitamin A derivative used in the topical treatment of acne . It acts by 'unseating' comedones, improvement developing slowly over a period of 2 to 3 or more months, and is also said to prevent the formation of new lesions . About three-quarters of patients with acne vulgaris benefit from treatment . In controlled studies, results achieved after a 3 to 4 months course of treatment were superior to those with sulphur-resorcinol-salicylic acid . When compared with benzoyl peroxide, results were variable and appear to depend on the length of treatment, the types of formulations used, and the concentrations compared . Application of vitamin A acid should be continued until the patient has been free of new lesions for several months . Further continued application at a less frequent interval or using a less active dosage form may help to prevent exacerbations of acne . A systemic antibacterial agent such as tetracycline can be given as well as in patients with moderate to severe lesions . Vitamin A acid is used in conjunction with gentle washing (to remove surface oil) but should be applied to a dry skin to avoid unnecessary irritation . Patient education and encouragement are crucial during the initial phase of treatment when microcomedones may be converted to pustules prior to desquamation.

J Pharm Pharmacol, 1977 Dec, 29(12), 717 - 22
Loss of antibacterial preservatives from contact lens solutions during storage; Richardson NE et al.; The preservative content of 34 commercially available contact lens solutions has been determined . Over half of the solutions contained less than 90% of the stated preservative content . Storage tests conducted at 40 degrees, using both simulated and commercially available contact lens solutions in plastics containers of the type used to present these products showed that thiomersal and chlorbutol appeared to be sorbed by these containers in contrast to benzalkonium chloride and chlorhexidine gluconate which interacted mainly by a surface adsorption process . The extent of any interactions was dependent upon the type of plastics material used to fabricate the container.

C R Acad Sci Hebd Seances Acad Sci D, 1977 Nov 14, 285(13), 1215 - 7
{Description of some simple tests allowing the distinction between bacteriocins sensu stricto and other antibacterial agents produced by bacteria}; Hamon Y et al.; In contrast with other antibacterial agents produced by bacteria, the bacteriocins of Gram -- bacteria (briefly: cins G--) are characterized by their primary lethal action, their inactivation by trypsin, their resistance to pH 2 (in the crude state) and insensitivity to DNase I after treatment with 7 M urea . Only 4 among 26 studied cins G + have the 4 above-cited properties and share most properties of cines G--.

J Pharm Sci, 1977 Nov, 66(11), 1607 - 11
N-Glucopyranosyl-5-aralkylidenerhodanines: synthesis and antibacterial and antiviral activities; Foye WO et al.; A series N-(2,3,4,6-tetra-O-acetyl-beta-D-glucopyranosyl)-5-aralkylidenerhodanines was synthesized, and the acetyl groups were removed to give N-beta-D-glucopyranosyl-5-aralkylidenerhodanies without cleavage of the rhodanine ring by means of acid hydrolysis . Alkaline hydrolysis with ammonia in methanol resulted in cleavage to N-glucosylthiourea, providing evidence for N-glycoside formation . A number of the rhodanine derivatives, especially those with nitro or chloro groups in the aromatic ring, showed antibacterial activity . N-beta-D-Glucopyranosyl-5-(4-nitrobenzylidene) rhodanine showed antiviral activity by inhibition of viral RNA synthesis . Some effect on blood sugar levels also was observed with several rhodanines.

J Med Chem, 1977 Nov, 20(11), 1445 - 8
Antibacterial halogenoacetyl derivatives of amino acids and simple peptides; Goodacre J et al.; The vital role of D-alanine and L-lysine in the peptidoglycan crosslinking process in the bacterial cell wall prompted preparation of various small peptides incorporating these amino acids . N-Iodoacetyl or -bromoacetyl derivatives of the peptides were then prepared in the hope that they would serve as active-site-directed irreversible inhibitors of cell wall transpeptidases . Certain of the halogenoacetyl dipeptide esters, but not the corresponding free acids, showed slight antistaphylococcal activity . Subsequent structural variation showed that inclusion of C-alanine or L-lysine was not necessary, since antibacterial activity was at least as good when the dipeptide unite was replaced by glycylglycine or by an omega-aminoalkanoic acid . It was concluded that the observed antibacterial activity was probably not due to specific inhibition of a cell wall transpeptidase.

Acta Otolaryngol, 1977 Nov-Dec, 84(5-6), 440 - 5
Maxillary sinusitis . Effects of treatment on the local antibacterial defence; Carenfelt C; Low levels of immunoglobulins and complement in purulent antral secretion might jeopardize the local antibacterial defence . To evaluate whether or not antibiotic treatment and antral drainage influence the local content of immunoglobulins and complement, samples of secretion were analysed both prior to drainage and 1-2 days after drainage . In those patients requiring repeated drainage for their recovery, the local concentration of IgA and IgG was significantly lower in the secretion obtained prior to drainage than the local concentration found in patients who recovered after the initial drainage . It was also demonstrated that after drainage, the level of IgA, IgG and the complement factors C3 and C4 increased significantly, whereas the proteolytic activity in the secretion usually decreased.

J Antibiot (Tokyo), 1977 Oct, 30(10), 843 - 6
Synthesis and antibacterial activities of 1-N {(S)-omega-amino-2-hydroxyalkyl} kanamycin A derivatives; Richardson K et al.; Four 1-N-aminohydroxy-alkyl derivatives of kanamycin A were prepared and their in vitro activities against aminoglycoside-sensitive and aminoglycoside-resistant organisms were compared with amikacin . 1-N-{(S)-4-Amino-2-hydroxybutyl} kanamycin A (Fig . 1, compound 2, code no . UK-18,892) was equipotent to amikacin in all these tests and in mouse protection studies.

J Antibiot (Tokyo), 1977 Oct, 30(10), 836 - 42
The aminoglycoside antibiotics . I . Synthesis and biological evaluation of an analog of gentamicin; Sitrin RD et al.; The synthesis of 2-deoxy-4-O-(2,6-diamino-2,3,4,6-tetradeoxy-alpha-D-erythrohexopyranosyl)-6-O-(3-deoxy-3-methylamino-alpha-D-xylopyranosyl)-D-streptamine (1), an analog of gentamicin A, from diideoxyneamine and methyl 3-methylamino-3-deoxy-beta-D-xylopyranoside is described . The product was characterized by its 13C nmr spectrum and was found to exhibit broad spectrum antibacterial activity.

J Antibiot (Tokyo), 1977 Oct, 30(10), 779 - 88
Tallysomycin, a new antitumor antibiotic complex related to bleomycin . I . Production, isolation and properties; Kawaguchi H et al.; The unusual actinomycetes strain No . E465-94 produced a complex of new glycopeptide antibiotics tallysomycin, which was separated by CM-Sephadex chromatography into two major components, A (C68H107N21O27S2) and B (C62H95N19O26S2) . They were isolated first in a copper-chelated form and showed physico-chemical properties similar to those of the bleomycin-group of antibiotics . Tallysomycin exhibited broad antibacterial and antifungal activity, and was highly active in vivo against bacterial infections in mice . Tallysomycins A and B demonstrated potent activity in the prophage induction of lysogenic bacteria.

Arch Dis Child, 1977 Oct, 52(10), 778 - 81
Intramuscular iron-dextran and susceptibility of neonates to bacterial infections . In vitro studies; Becroft DM et al.; An increased incidence of E . coli sepsis has been observed in neonates given intramuscular iron-dextran for prevention of iron deficiency . Mechanisms for this apparent effect on susceptibility to infection were investigated by comparing phagocytic and antibacterial functions in paired samples of venous blood from 7 infants, median age 5 days, before and after iron-dextran . Post-treatment sera had increased inhibitory effects on leucocyte chemotaxis and markedly reduced bacteriostatic effects agaainst E . coli . The clinical relevance of the effects on chemotaxis is uncertain . The reduction in serum bacteriostasis is similar to that observed in other forms of hyperferraemia not associated with saturation of transferrin, and is a likely cause of the increased susceptibility to infection in vivo . We consider that prophylactic treatment with parenteral iron-dextran is contraindicated in early infancy.

Surg Clin North Am, 1977 Oct, 57(5), 1089 - 1102
The diabetic foot: an alternative approach to major amputation; Robson MC et al.; Of the complications of diabetes mellitus, none is more devastating than gangrene of the foot and the threat of leg amputation . The pathophysiology of vascular insufficiency, neurotrophic changes, and infection leading to this gangrene have been reviewed . Based on this pathophysiology, an approach for conservative surgery of the diabetic foot has been outlined . Using known principles of wound healing and the management of soft tissue infection, obviously necrotic or infected tissue is debrided and the wound managed conservatively . The use of debriding adjuncts such as the pulsating jet lavage, topical antibacterials, and biologic dressings are suggested to control the infection so that the wounds can be closed with either skin grafts or local flaps . This method can result in salvage of many feet and the maintenance of biped ambulation since the outlook for the diabetic with a major amputation is markedly different from the nondiabetic amputee.

J Med Chem, 1977 Oct, 20(10), 1287 - 91
Synthesis and antibacterial activity of some derivatives of tolypomycinone . Relationship between structure and activity in ansamycins; Bellomo P et al.; 3-Aminotolypomycinoes and 3,16-diamino-16,17-dihydrotolypomycinones are formed by the addition of primary and secondary amines to tolypomycinone, obtained by mild hydrolysis of the antibiotic tolypomycin Y.3-Amino-16,17-dihydrotolypomycinones are formed by the addition of primary and secondary amines to 16,17-dihydrotolypomycinone . In vitro microbiological tests showed high antibacterial activity in compounds obtained by the addition of primary amines, which must be unbranched in the alpha position to the nitrogen atom to position 3 of the naphthoquinone ring . The relationship between structure and activity is described, and evidence is presented that hydrogen bonding between the amino NH bonded to C3 and the amide CO of tolypomycinone is very important for biological activity.

J Periodontol, 1977 Oct, 48(10), 646 - 9
Prolongation of antibacterial activity of chlorhexidine adsorbed to teeth . Effect of sulfates; Turesky S et al.; The results suggest that the effectiveness of sulfates in prolonging the antibacterial activity of teeth treated with chlorhexidine gluconate is related to the acidity and concentration of the sulfate solutions . The acidity may contribute to the effectiveness by modifying the tooth surface for enhanced reaction with sulfate ions . It is suggested that during the priming process bonded crystals of calcium sulfate develop which become transformed by treatment with chlorhexidine gluconate to relatively insoluble chlorhexidine sulfate.

Arch Dermatol, 1977 Oct, 113(10), 1390 - 1
Topical clindamycin in acne vulgaris . Safety and stability; Algra RJ et al.; Eighteen patients with acne vulgaris used a hydroalcoholic solution of clindamycin hydrochloride topically . Serum samples were obtained and assayed for clindamycin; no evidence for systemic absorption was found . The clindamycin capsules used in this preparation contained insoluble fillers that may be removed by filtration without loss of in vitro antibacterial activity . This solution is stable for at least six months.

J Antibiot (Tokyo), 1977 Sep, 30(9), 705 - 13
Cephalosporins . III . 7-(O-Aminomethylphenylacetamido)cephalosporanic acids with bicyclic heteroaromatics in the C-3 side chain; Naito T et al.; Bicyclic heteroaromatic thiols with a bridge-head nitrogen atom were used for nucleophilic substitution of 7-ACA at the C-3 acetoxy function followed by N-acylation of the 7-amino group with o-aminomethylphenylacetic acid to afford a series of new cephalosporins (24) with potent antibacterial activity against gram-positive and gram-negative organisms . The most active member of this series was 7-(o-aminomethylphenylacetamido)-3-(tetrazolo-{4,5-b}pyridazin-6-ylthiomethyl)-3-cephem-4-carboxylic acid (BB-S 226) (24e) with antibacterial activity superior activity superior to cephalothin and cefazolin.

J Antibiot (Tokyo), 1977 Sep, 30(9), 698 - 704
Cephalosporins . II . 7-(O-Aminomethyl-phnylacetamido) cephalosporanic acids with six membered heterocycles in the C-3 side chain; Naito T et al.; 7-(o-Aminomethylphenylacetamido)cephalosporanic acids with six-membered heterocycles in the C-3 side chain were prepared by nucleophillic substitution of 7-ACA at the C-3 acetoxy group followed by N-acylation of the 7-amino group . The 7-side chain acid, o-aminomethylphenylacetic acid (5), was prepared by two new convenient routes, which involved Schmidt reaction of indanone (2) followed by cleavage of the lactam ring or reduction of o-cyanophenylacetic acid (10) starting from o-nitrotoluene . The antibacterial activity of the cephalosporins in this series depends on the heterocycle in the C-3 side chain . In general pyridazines gave cephalosporin derivatives possessing better activity than those with a pyridine or pyrimidine ring . The most active member of the new cephalosporins was 7-(o-aminomethylphenylacetamido)-3-(6-hydroxypyridazin-3-ylthilmethyl)-3-cephem-4-carboxylic acid (BB-S 150) (1g) which has in vitro antibacterial activity superior to cephalothin and cefazolin against both gram-negative and gram-positive organisms . The in vitro activity of BB-S 150 determined in mice was superior to cephalothin and comparable to cefazolin.

Vestn Khir Im I I Grek, 1977 Sep, 119(9), 12 - 4
{Puncture method of treating amebic abscesses of the liver}; Tikhii AT; In surgical treatment of hepatic amebic abscesses by means of extensive dissection and drainage the postoperative lethality remains high . The literature data and the author's own observations on 30 patients, who underwent puncture of amebic abscess of the liver together with specific and antibacterial therapy, which resulted in their recovery, permit to consider paracentensis as a method of choice, when there are no complications, such as a purulent discharge into the adjoining organs and tissues, which calls for surgical intervention.

Antibiotiki, 1977 Sep, 22(9), 829 - 32
{Methodological bases for the hygienic standardization of antibiotics}; Shteinberg GB et al.; For determination of the maximum permissible concentrations of antibiotics it is necessary to develop some specific approaches conditioned by the peculiarities of the biological effect of antibiotics in addition to the use of the general principles of the hygienic rationing of the factors of the production environment . It is advised to determine the thresholds of the specific antibacterial and allergen effect of antibiotics in the acute experiment in addition to the threshold of the general toxic effect.

Nord Vet Med, 1977 Sep, 29(9), 369 - 75
Effect of vaccination of sows with Bordetella bronchiseptica on the incidence of atrophic rhinitis in swine; Pedersen KB et al.; Vaccination of pregnant sows with Bordetella bronchiseptica was performed in an SPF herd with clinical atrophic rhinitis . Agglutinins against the organism were induced in serum and colostrum by the vaccination . The antibody titres were generally higher in colostrum than in corresponding serum samples . The frequency at slaughter of turbinate atrophy (+, ++, +++) was lower among pigs from vaccinated sows (11%) than in pigs borne by unvaccinated sows (20%) . In the control group a lower daily weight gain was observed in pigs with turbinate atrophy than in pigs with normal noses . The mean daily weight gain in pigs with turbinate atrophy borne by vaccinated sows was slightly lower than in pigs without atrophy of conchae, but the difference was not significant . A specific immunological prophylaxis might be an alternative to antibacterial treatment in herds where atrophic rhinitis is aetiologically related to B . bronchiseptica infection.

J Pharm Sci, 1977 Sep, 66(9), 1312 - 6
Thermal decomposition of amorphous beta-lactam antibacterials; Pikal MJ et al.; Thermal decomposition rates for amorphous samples of penicillin G potassium, cephalothin sodium, cefamandole sodium, and cefamandole nafate were determined as a function of water content and temperature . Even when rigorously dry, amorphous cephalosporins were at least one order of magnitude less stable than the corresponding unsolvated crystalline form . Absorbed water generally increased both the number of decomposition products and the net decomposition rate . Reaction kinetics were usually apparent first order, but an anomalously high effective reaction order was observed in several systems . Nonlinear Arrhenius plots were observed, and a qualitative model based on molecular relaxation in glayses is proposed . Although decomposition rates at 25 degrees were small for dry samples, even slight decomposition produced visually detectable changes . Thus, the unsolvated crystalline form was noticeably more stable, even at 25 degrees.

J Pharm Sci, 1977 Sep, 66(9), 1239 - 41
Smooth muscle relaxant properties and vasomotor actions of 2-amino-1-p-nitrophenylpropane-1,3-diol; Banerjee S et al.; Experiments with the guinea pig ileum, trachea, and vas deferens, the rat fundal strip, the rabbit jejunum and aortic strip, and the toad heart indicated that 2-amino-1-p-nitrophenylpropane-1,3-diol, the hydrolytic product of chloramphenicol, inhibited smooth muscles . Its action was direct and not through any mediators . After intravenous administration, the compound produced vasodepression followed by an overshooting rise of blood pressure . Vasodepression was not mediated by adrenergic, cholinergic, or histaminergic mechanisms . Hypertension was a sympathomimetic effect . Muscle relaxant and cardiovascular effects of the compound were similar to those of chloramphenicol, although it had no antibacterial effect.

J Antibiot (Tokyo), 1977 Sep, 30(9), 736 - 42
Uptake of 2'-amino-2'-deoxyguanosine by Escherichia coli and its competition by guanosine; Nakanishi T et al.; The antibacterial activity of a new nucleoside antibiotic, 2'-amino-2'-deoxyguanosine (2AG), is reversed by guanosine and other purine nucleosides . 2AG is apparently taken up by E . coli by a mechanism different from that of guanosine; guanosine inhibits this uptake non-competitively . Insensitive E . coli strains and the resistant mutant obtained from the sensitive strain also took up 2AG.

Mutat Res, 1977 Sep, 44(3), 327 - 35
Testing the mutagenic potency of chemical substances in a linear host-mediated assay (LIHMA); Lorenz RJ et al.; Instead of comparing "mutation frequencies" as used in the conventional host-mediated assay (HMA), a modified concept of measuring mutagenic potency is introduced by using a number of time intervals for taking samples . Regression analysis methods can then be applied to the numbers of mutant bacteria (reversions) . Not only the mutagenic but also an additional antibacterial potency of a compound can be detected and estimated in the sam assay . It is demonstrated that interference of (undetected) antibacterial activity with the mutagenic activity may lead to misclassification of a substance concening its mutagenicity in the conventional HMA . This kind of erroneous assessment will be avoided by the LIHMA . Another advantage of the LIHMA over the conventiona HMA is that regression analysis also allows estimation of the sensitivity and reliability of the assay . The calculative procedure may be programmed on desk computers and is then most suitable for laboratories where large numbers of substances have to be examined routinely . A numerical is given using results obtained with nitrosoguanidine.

Dtsch Zahnarztl Z, 1977 Sep, 32(9), 755 - 6
{The effect of amyloglucosidase and glucoseoxydase containing toothpastes on plaque formation and gingivitis}; Rotgans J et al.; Earlier studies showed that an antibacterial lactoperoxydase system in the saliva is activated by the application of a hydrogen paroxide-generating combination of enzymes: amyloglucosidase and glucose oxydase . The object of the present study was to investigate the effect of these enzymes in a test and control group of 29 subjects . The results showed the plaque-inhibiting effect of the enzyme paste . An influence on the gingiva could not be demonstrated.

Antibiotiki, 1977 Sep, 22(9), 798 - 803
{Clinical biological possibilities of the early detection of the side effects of antibiotics}; Marshak AM et al.; The study of the dynamics of biogenic amines in the blood of patients provided to a certain extent determination of the possible thread of the drug complications . In this respect the serotonin level was of special significance . As for the reaction of leucocyte agglomeration it may be used before the treatment if there is a doubt in the tolerance of the antibacterial drug prescribed . Increased serotonin blood levels in this case also serve a confirmation of the thread of the possible allergic or toxic reaction in the patient.

Chirurg, 1977 Sep, 48(9), 604 - 6
{Modified agar diffusion test for direct testing of the effectiveness of released antibiotics from bone cements}; Stubner G et al.; A modified agar-diffusion method is used to test the bactericidal efficacy of antibacterial substances (model substance: Gentamicin) that have been mixed with Palacos osseous cement . Holes of a diameter slightly larger than the diameter of the cylindric Palacos test block are cut from the agar plate . The remaining space (inner wall of the hole--edge of the test body) is filled with various eluate media . The release of active antibacterial substances from polymethylmetacrylates can thereby be determined under nearly physiologic conditions at varying pHs by direct antibacterial testing.

J Med Chem, 1977 Aug, 20(8), 1086 - 90
Structure--activity relationships in cephalosporins prepared from penicillins . 2 . Analogues of cephalexin substituted in the 3-methyl group; Brain EG et al.; A previously outlined general procedure for preparing various 3-substituted cephalosporins from the penicillin nucleus has been used, with modifications where required, to prepare a series of analogues of cephalexin with various substituents in the 3-methyl group . The 3-substituents most conducive to broad-spectrum antibacterial activity were 3-pyridylmethyl and m- or p-carboxybenzyl . The compounds were only poorly absorbed by the oral route in mice, but the 3-(carboxybenzyl) compounds gave more prolonged useful serum levels than the usual cephalosporins.

J Med Chem, 1977 Aug, 20(8), 1082 - 5
Structure--activity relationships in cephalosporins prepared from penicillins . 1 . 7beta-Acylamino derivatives of 3-benzyl- and 3-(3-pyridylmethyl)ceph-3-em-4-carboxylic acids; Brain EG et al.; tert-Butyl 7beta-aminoceph-3-em-4-carboxylates carrying either benzyl or 3-pyridylmethyl substituents at position 3 have been prepared by a multistep modification of the penicillin nucleus . Acylation of either amine, followed by deprotection, gave a range of new cephalosporins . The relationship between structure and antibacterial activity is discussed . D-Phenylglycine proved to be a preferred side chain in both series.

Ann Surg, 1977 Aug, 186(2), 136 - 9
Multiple mycotic aneurysms due to Candida endocarditis; Collins GJ Jr et al.; Candida endocarditis is a serious condition which should be suspected in any patient with signs and symptoms compatible with bacterial endocarditis when cultures are negative . It should be managed by a medical-surgical approach which combines resection of all infected heart tissue and repair of any preexisting heart defects with appropriate antifungal therapy . Mycotic aneurysms should be treated by ligation of the vessel above and below the aneurysm, resection of the aneurysm, and implementation of appropriate antifungal or antibacterial therapy . Revascularization is not always necessary . When required, an extra-anatomic approach is preferable to placing a graft through the bed of the aneurysm.

J Bone Joint Surg Br, 1977 Aug, 59(3), 302 - 7
Antibacterial activity of antibiotics in acrylic bone cement; Picknell B et al.; The release of various penicillins and other antibiotics from two brands of polymerised bone cement has been studied in vitro and in vivo in mice . Bone cement plugs containing antibiotics demonstrated antibacterial activity as a result of diffusion of antibiotic from the plugs into the surrounding medium . With all antibiotics tested, from 2-5 to 10 per cent of the antibiotic in the cement was released in vitro in active form within twenty-four hours . Most of the activity appeared within three hours of the start of the test, but in some cases low levels of activity were detected after four days . Antibiotic cement plugs implanted in mice and rats produced low concentrations of antibiotic in the blood up to two hours after implantation, but activity was seldom detected subsequently . In general, penicillins and non-penicillin antibiotics showed similar diffusion characteristics, and the pattern of release in vitro and in vivo was consistent with the leaching of antibiotic from, or near, the surface of the bone cement.

Antibiotiki, 1977 Aug, 22(8), 753 - 6
{Results of using an accelerated method of determining microbial flora sensitivity to antibacterial preparations in the surgical clinic}; Lunacharskaia TV; Express diagnosis using 2,3,5-triphenyltetrasolium chloride as the redox indicator provided in most tests rapid and sufficiently precise determination of the microbial flora sensitivity to antibacterial drugs permitting to start in time the antibiotic therapy of the patients . For rapid response it proved to be useful to incubate beforehand the test material taken from surgical patients within 16 to 18 hours and to increase the indicator concentration up to 2--3 per cent.

Antibiotiki, 1977 Aug, 22(8), 704 - 8
{Spheroplast bacteriocin from strains of the causative agent of pseudotuberculosis and its identification by the antibacterial activity spectrum and the morphology of the inhibition zones}; Gramotina LI; Capacity for production of bactericin was found in the spheroplasts of the strains of the rodent pseudotuberculosis microbe . The author named it as pseudotuberculocin . The bacteriocin production was not detected in the initial strains of the pseudotuberculosis microbe . Pseudotuberculocin differed in the antibacterial spectrum and morphology of the growth inhibition zones formed on the plates with the indicator strains from the pesticins produced by the strains of the plaque microbe of the marmot and sandword varieties respectively and the cultures of the plaque microbe from the Transcaucasian Upland, as well as from pesticins of the spheroplasts of these strains . Production of a pesticin differing from pesticins of the rod-like forms of these strains by an ability to inhibit the growth of the homologous indicators was shown in the spheroplasts of the plaque microbe of the marmot and sandword varieties . Sensitivity of the plaque microbe strains of the marmot and sandword varieties to the pesticins of the plaque microbe strains and pseudotuberculocin was noted . With an account of the difference in the activity of the tested pesticins and pseudotuberculocin against the strains of the Frederic collection it is recommended to use this property for identifications of pesticins and pseudotuberculocin.

J Pharm Sci, 1977 Aug, 66(8), 1204 - 6
Imidazo{4,5-f}quinolines III: Antibacterial 7-methyl-9-(substituted arylamino)imidazo{4,5-f}quinolines; Synder HR Jr et al.; A series of 7-methyl-9-(substituted arylamino)imidazo{4,5-f}quinolines was prepared and screened against four varieties of bacteria . The compounds possessed antibacterial activity against both Gram-positive and Gram-negative organisms.

J Pharm Sci, 1977 Aug, 66(8), 1108 - 11
Spectrophotometric determination of cephapirin, a cephalosporin antibacterial; Bodnar JE et al.; A simple and specific method for the quantitative determination of cephapirin, a cephalosporin antibacterial, in finished bulk and dosage forms is reported . The method is based on reproducible degradation under controlled conditions to an unidentified species, which is measured spectrophotometrically at 375 nm . The procedure can be performed manually on a short series of samples in about 15 min or can be automated for large runs . Precursors and related substances show minimal interference . The coefficient of variation of the automated system is about 1% within days and 1.3% among days.

Z Gesamte Inn Med, 1977 Jul 15, 32(14), Suppl 219 - 22
{Antibacterial combination therapy}; Tauchnitz C; Reasons for the use of antibacterial combinations are synergistic effects and delayed development of bacterial resistance . On the basis of numerous experiments in vitro the opinion is supported that a clinically useful synergism depends on the addition of an aminoglycoside, the second compound being either one of the penicillins or cephalosporins, or a polymyxin, or a bacteriostatic agent like tetracycline, macrolide, and lincomycine . The decrease of MBC and MIC values varies according to the species and strains of bacteria and in dependence on the components of antibiotic combinations . Combination therapy with antibacterial synergism is indicated in life-threatening infections and in order to suppress bacterial persistences . Combinations with antagonistic effects should be avoided . The use of multiple antibiotics for broader spectrum only is not supported.

J Antibiot (Tokyo), 1977 Jul, 30(7), 533 - 40
Fortimicins A and B, new aminoglycoside antibiotics . I . Producing organism, fermentation and biological properties of fortimicins; Nara T et al.; A culture of Micromonospora species MK-70 was found to produce two new antibiotics, fortimicins A and B . Antibacterial and paper chromatographic data on an eluate from IRC-50 treatment of fermentation beers indicated that fortimicins A and B are new antibiotics with broad-spectrum, basic and water-soluble properties . Fortimicin A exhibited potent, unique, broad-spectrum antibacterial activity against Gram-positive and negative bacteria both in vitro and in vivo, while fortimicin B was only weakly active.

Ann Sclavo, 1977 Jul-Aug, 19(4), 876 - 80
{The demonstration of antibacteric power in a blood sample taken for blood culture . Preliminary note . (author's transl)}; Rigoli E; To identify a possible "false" negative blood culture from a patient not declearing antibiotic treatment, we propose a "Residual Antibiotic Power" test (PAR-test) on the same blood sample to be rum in parallel with the blood culture . Hence we propose using B . stearothermophilus var . calidolactis, which we have found very sensitive to the common antibiotics used in Human Medicine . Suggested technique: agar+germ with an absorbent paper disc soaked with the sample, incubated for 3 hours at 60 degrees C, to give an easy test reading.

Arzneimittelforschung, 1977 Jul, 27(7), 1396 - 9
Derivatives of N,N-bis(alpha, alpha, alpha-trifluoro-m-tolyl)amine; Yale HL et al.; Amongst a series of novel derivatives of N,N-bis-(alpha, alpha, alpha-trifluoro-m-tolyl)amine, several were found to possess antiinflammatory, hypotensive, antibacterial and antifungal activity . The synthesis of these compounds is described and their biological properties are discussed.

Arzneimittelforschung, 1977 Jul, 27(7), 1393 - 4
Antibacterial and anthelminthic properties of visnaginone and khellinone derivatives; Ismail E et al.; The compounds tested, derivatives of visnaginone and khellinone, showed antibacterial activity on gram negative and gram positive micro-organisms . Some of the compounds possess an antibacterial activity on some pathogenic bacteria, i.e . Brucella abortus, for which there is no remedy as yet . All the chalcones tested were inactive except Ib, which showed antiparasitic broad spectrum.

Cancer Treat Rep, 1977 Jul, 61(4), 591 - 5
Detection and microbiologic assays of antimetabolites; Hanka LJ; The biochemical considerations applicable in the detection of new antimetabolites are very similar to those used in developing microbiologic assays for these drugs . An in vitro system for detection of antimetabolites was developed based on different sensitivities to such drugs of bacteria cultivated in complex versus completely synthetic media . A number of new antimetabolites of amino acids, vitamins, and purines or pyrimidines were isolated and microbiologic assays for these drugs were developed . As an example of the technology utilized and possibilities available, an assay for cytosine arabinoside was described . It can detect 0.5-microgram/ml concentrations of this drug even in the presence of other antitumor or antibacterial antibiotics.

Ann Microbiol (Paris), 1977 Jul, 128B(1), 73 - 80
{Bacterial cytostimulation by different effectors: purified antibacterial antibodies, concanavalin A and lipopolysaccharide (author's transl)}; Schirmann-Marotel J; The rate of growth of Gram- bacterial strains may be stimulated by various effectors: antibacterial antibodies, concanavalin A and specific lipopolysaccharide . Purification of the stimulating antibodies is brought about by saline dissociation of the bacteria-antibodies complex . Antibodies accountable for the cytostimulation would appear to be specific of the bacterial lipopolysaccharide.

Tohoku J Exp Med, 1977 Jul, 122(3), 299 - 300
Antibacterial activity detected in duodenal juice; Umenai T et al.; Antibacterial activity could be detected in bacterium-negative duodenal juice from 3 patients, whereas it was not detected in bacterium-positive duodenal juice from other 3 patients . The follow-up study revealed that appearance of the activity in duodenal juice was just coincident with disappearance of bacteria in duodenal juice . The activity was not influenced by pH of the duodenal juice . These results seem to suggest that some antibacterial activity, different from that of pH, in duodenal juice regulates in some way proliferation of the upper gastrointestinal flora.

Arch Dis Child, 1977 Jun, 52(6), 501 - 3
Acute bacterial maningitis in childhood: aspects of prehospital care in 687 cases; Goldacre MJ; Some basic features of the prehospital management of children with acute bacterial meningitis were ascertained by a retrospective review of case notes . A diagnosis of intracranial infection was considered in 63% of general practitioners' referral letters and was more often considered for older than younger children . 47% of children had received antibacterial chemotherapy before hospital admission . Such treatment did not appear to have jeopardized the outcome . The possibility of delay in the admission of children to hospital at weekends is discussed.

Infect Immun, 1977 Jun, 16(3), 938 - 46
Gastrointestinal antibody responses in axenic mice to topically administered Escherichia coli; Ebersole JL et al.; Immunoglobulin levels were determined in gastrointestinal secretions of both conventional and axenic mice, as was the stability of the immunoglobulin classes in these secretions . Axenic animals were then administered nonviable Escherichia coli O111:B4 by topical application into the oral cavity . Immunoglobulin (Ig) A, IgG1, AND IgG2 were detected in the gastrointestinal secretions, with an apparent gradation in stability (IgA greater than IgG1 greater than IgG2) under the conditions investigated . Specific antibodies (IgA and IgG) to both the somatic and the flagellar antigens of E . coli were demonstrated . The time course of the responses to the polysaccharide and protein antigens suggested that a secondary response to lipolysaccharide was being observed in the secretions . Examination of the autoclaved diet fed to the germfree animals indicated the presence of antigenically intact polysaccharide materials (i.e., lipopolysaccharides), whereas antigenic bacterial proteins were uniformly undetectable . Therefore, endotoxin in the diet was apparently causing a primary type of sensitization in the mice, whereas the active oral immunization regimen induced a secondary antibacterial response in the secretions.

Antibiotiki, 1977 Jun, 22(6), 564 - 7
{Use of aminoglycosides and other antibacterial preparations in gastroenterology}; Saksen EF et al.; Kanamycin and monomycin were used in the treatment of 945 severe surgical patients . Examination of antibiograms showed that the microflora of the patients was moderately and highly sensitive . The antibotic blood levels defined the tactics of the drug administration rate and route . The antibiotic treatment was accompanied by complex therapy for increasing the host protective forces . The antibiotic treatment was well tolerated by the patients . No impairements of the kidneys or the VIII pair of the cranial nerve were observed . Allergic reactions in the form of urticaria were registered in several patients.

Cutis, 1977 Jun, 19(6), 852 - 4
Old drug--in a new system--revisited; Olansky S; Sodium sulfacetamide, penetrating antibacterial, in combination with hydrocortisone and sulfur, has enjoyed twenty years of remarkable safety, with outstanding efficacy and patient acceptance, in the prescription treatment of pustular acne and severe, refractory seborrheic dermatitis . Recently, this combination has been reported to be highly effective concomitant therapy for perioral dermatitis . Almost paradoxically, it achieves these desired goals without the excessive erythema and discomforting irritation associated with retinoic acid and benzoyl peroxide.

J Pharm Sci, 1977 Jun, 66(6), 861 - 6
Physicochemical properties of beta-lactam antibacterials: deuterium solvent isotope effect on penicillin G degradation rate; Yamana T et al.; To obtain kinetic evidence on the degradation mechanism of penicillin in aqueous solution, degradation rates of penicillin G in water and deuterium oxide were measured in the pH (pD) range of 4-10 . The solvent isotope effect (kH2O/kD2O) of 1.53 below pH (pD) 6 supports the mechanism of water-catalyzed rearrangement of undissociated penicillin G to benzylpenicillenic acid . The spontaneous degradation at neutral pH (pD) and the hydroxide-ion-catalyzed degradation in the alkaline pH (pD) range progress with a deuterium solvent isotope effect (kH2O/kD2O) of 4.5 and 0.59, respectively . This finding indicates the mechanisms of general base-catalyzed hydrolysis by water in the neutral pH range and of nucleophilic attack of the hydroxide ion on the beta-lactam in the alkaline pH range . No significant side-chain dependency was observed in the reaction of penicillins with bases . The solvent isotope studies led to the conclusion that penicillin degradation is catalyzed by a series of bases via general base-catalyzed and nucleophilic mechanisms, depending on their basicity.

Aust Fam Physician, 1977 May, 6(5), 486 - 95
The rational use of antibiotics in general practice; Steele TW et al.; Many antibiotics produce serious adverse effects which, though uncommon, may be lethal or carry a high morbidity . This article provides a rational basis for the choice of antibiotics in common infections involving various anatomical sites . Short notes on the more useful antibacterial agents, dosage, major side effects and contraindications are included.

Anesth Analg, 1977 May-Jun, 56(3), 338 - 45
Cardiovascular effects of atropine sulfate preparations in vagotomized dogs under halothane anesthesia; Reitan JA et al.; The cardiovascular effects of 3 preparations of atropine sulfate were studied acutely in open-chest, vagotomized dogs under endotracheal halothane anesthesia . Indices of myocardial performance (LVdp/dt/CPIP and maximum ascending aortic blood acceleration) showed insignificant changes when varying doses of IV atropine (0.04 mg/kg and 0.04 mg/kg) were given . However, mean ascending aortic pressure fell by 20 percent following the larger doses of 2 commercial preparations containing antibacterial preservatives, and only 9 percent following a "pure" (USP) atropine preparation . Calculated changes in systemic vascular resistance closely followed actual pressure values . These results indicate that atropine, even in large doses, causes little or no depression of ventricular function independently of its chronotropic action . However, atropine does cause a fall in blood pressure, seemingly due to peripheral vasodilation, particularly in commercial preparations containing preservatives.

Urology, 1977 May, 9(5), 526 - 33
Role of urothelial surface mucoprotein in intrinsic bladder defense; Shrom SH et al.; To implicate further the surface mucoprotein as the factor responsible for preventing bacterial attachment to the bladder mucosa, rabbit urothelium was severely disrupted and allowed to regenerate for varying periods of time . Quantitative measurements of the attachment of 14C-labeled Escherichia coli were correlated with the histologic presence of the surface mucoprotein . Control levels of bacterial attachment were observed only when the PAS-positive layer had regenerated, further supporting the role of this layer in the bladder's antibacterial defense.

J Med Microbiol, 1977 May, 10(2), 151 - 60
Determination of antibacterial antibodies in serum by immunoradiometric assays; Hambleton P et al.; When used to determine immunopurified antibacterial globulins in saline-phosphate buffer, the detection sensitivities of direct competitive and indirect immunoradiometric assays were respectively 25 and 2 ng . Normal human and rabbit sera interfered in both types of assay, markedly decreasing sensitivity and precision . Various pre-treatments of sera and modifications of reaction conditions substantially decreased interference in the competitive assay without affecting the activity of added antibody, but they had only marginal effects in the indirect assay . When serum samples taken from rabbits after vaccination with the Live Vaccine strain of Francisella tularensis were tested with the two assays and agglutination tests, newly synthesised circulating antibody was usually detected earlier by the competitive assay than by the other methods.

J Periodontol, 1977 May, 48(5), 282 - 4
An in vivo comparison of chlorhexidine and picloxydine mouthrinses: a possible association between chemical structure and antiplaque activity; Newcomb GM et al.; A double blind clinical trial was conducted in which both the plaque-inhibiting ability and the in vivo effects on the oral flora of chlorhexidine and picloxydine mouthwashes was compared . While picloxydine in higher concentration suppressed the oral flora more effectively than chlorhexidine, the latter agent inhibited plaque development to a much greater extent . This lack of correlation between antibacterial and antiplaque activity can be related to structural differences between these two bis-biguanides.

J Antibiot (Tokyo), 1977 May, 30(5), 409 - 15
Studies of binding C3-substitute rifamycins to human and bovine serum albumin; Assandri A et al.; The interactions of a series of C3-substituted rifamycins with human and bovine serum albumins were studied in order to find possible correlations between the degree of binding and the structural features of the various molecules . The results obtained indicate some of the physicochemical properties and, therefore, of the structural requirements which appear to determine or influence the bonding mechanisms of this series of rifamycins . Two types of interaction were found to exist, ionic and hydrophobic types . The findings suggest that the inhibition by protein of the antibacterial activities of these antibiotics depends on the type of bonding mechanism rather than the degree of binding.

Antibiotiki, 1977 Apr, 22(4), 344 - 8
{Effect of semi-synthetic penicillins and cephaloridine on indices of immunologic reactivity and protein metabolism during treatment of puerperal infection}; Kulikova NN et al.; The effect of semisynthetic penicillins, such as methicillin and oxacillin and cephalosporins, such as cephaloridin of immunity and protein metabolism was studied on 63 patients with postnatal mastitis and endomyometritis . It was shown that the above antibiotics had no significant effect on the immunological reactivity and protein metabolism . However, lower titers of alpha-antitoxin, lysine levels and C-reactive protein content were registered in the mastitis patients treated with cephaloridin . Therefore, while recomending antibacterial drugs their effect on the immunity and protein metabolism should be taken into account and from this point of view semisynthetic penicillins are preferable in treatment of mastitis patients and semisynthetic penicillins and cephaloridin are preferable in treatment of endomyometritis patients.

Appl Environ Microbiol, 1977 Apr, 33(4), 996 - 7
Production and antibacterial activity of malforming C, a toxic metabolite of Aspergillus niger; Kobbe B et al.; The production of the new mycotoxin malformin C by a solid substrate fermentation is described . Malformin C is highly toxic (mean lethal dose = 0.9 mg/kg) and exerts antibacterial activity against a variety of gram-positive and gram-negative organisms.

Farmaco {Sci}, 1977 Apr, 32(4), 261 - 9
Synthetic analogs of natural prenylated and chromene chalcones; Lupi A et al.; A number of synthetic analogs of the prenylated and chromene chalcones isolated from lonchocarpus neuroscapha (Leguminosae) were obtained by condensation of prenylated acetophenones with substituted benzaldehydes . The antibacterial activity of these products was studied and correlated with their structure.

J Pharm Sci, 1977 Apr, 66(4), 597 - 8
Polarographic study of new antibacterial isoxazolium salts: 2,3-dialkyl-5-arylisoxazolium perchlorates; Omar NM et al.; The polarographic reduction of new antibacterial 2,3-dialkyl-5-arylisoxazolium salts is described . The electrode process involves an irreversible two-electron transfer and is pH independent within the 6.0-10.0 range . In more acidic media, hydrogen waves are observed; at higher pH values, a chemical degradation of the isoxazolium salt proceeds . Values of the half-wave potential of the salts are dependent on the polar contribution of the 5-aryl substituents in terms of the Hammett equation . The in vitro minimum inhibitory concentrations of these compounds are best correlated with Hansch PI values.

Plast Reconstr Surg, 1977 Apr, 59(4), 551 - 4
Conservative management of the ulcerated diabetic foot; Robson MC et al.; Four cases are presented of the conservative treatment of the diabetic foot . Using the known principles of wound healing and of management of soft tissue infection, the obviously necrotic or infected tissue was debrided and the wounds were managed conservatively . The use of such debriding adjuncts as a pulsating jet lavage, topical antibacterials, and biological dressings, has controlled infections--so that the foot wounds could be closed then with sking grafts or local flaps . This resulted in the salvage of these feet, with maintenance of biped ambulation.

J Med Chem, 1977 Apr, 20(4), 557 - 60
Nitrones . 7 . alpha-Quinoxalinyl-N-substituted nitrone 1,4-dioxides; Kim HK et al.; A series of alpha-quinoxalinyl-N-substitute nitrone 1,4-dioxides has been synthesize and evaluated as antibacterial and antiprotozoal agents . Structure-activity relationships are discussed . Of the compounds tested, alpha-(3-methyl-2-quinoxalinyl)-N-methylnitrone 1,4-dioxide (2) was the most active agent in vivo against the gram-negative and the gram-positive organisms.

J Med Chem, 1977 Apr, 20(4), 560 - 3
Beta-Lactam antibiotics derived from nitrogen heterocyclic acetic acids . 1 . Penicillin derivatives; Studies on aculeacin . I . Isolation and characterization of aculeacin A; Aculeacin A, a new antifungal antibiotic was isolated from the mycelial cake of Aspergillus aculeatus M-4214 . The antibiotic is a white amorphous powder soluble in lower alcohols and hardly soluble in other organic solvents or water . Aculeacin A gave palmitic acid and five ninhydrin-positive products including theonine, hydroxyproline upon acid hydrolysis . The antibiotic showed a potent activity against molds and yeasts, but exhibited no antibacterial activity . Aculeacin A has relatively low toxicity in mice.

Am Rev Respir Dis, 1977 Apr, 115(4), 601 - 7
The relationship between nicotinamide adenine dinucleotide concentration and antibacterial activity of isoniazid in Mycobacterium tuberculosis; Jackett PS et al.; The relationship between the antibacterial effect of isoniazid and the intracellular concentration of nicotinamide adenine dinucleotide (NAD) was investigated in Mycobacterium tuberculosis strain H37Rv given continuous and pulsed exposures to the drug . Depletion of NAD to a plateau value occurred rapidly during exposure, and recovery after a pulse of isoniazid was also rapid . It seemed unlikely that NAD depletion was the direct cause of the antibacterial activity because (1) insufficient depletion occurred at low isoniazid concentrations; (2) antibacterial activity, but not NAD depletion, was proportional to the product of isoniazid concentration and the exposure period; and (3) NAD depletion was not related to antibacterial activity in cultures of differing physiologic state.

Mutat Res, 1977 Apr, 48(2), 195 - 203
Effect of DNA Repair systems on antibacterial and mutagenic activity of an antitumor protein, neocarzinostatin; Tatsumi K et al.; Antibacterial and mutagenic effects of an antitumor protein, neocarzinostatin (NCS), on isogenic strains of Escherichia coli with normal or defective DNA repair systems were studied . Growth of the strains lacking recA gene was inhibited by NCS with much lower concentration than in the case of those possessing it, while the "differential inhibition for growth" (DIG) between the strains uvrA+ and uvrA- was not seen . NCS induces mutation in recA+ strains but not significantly in recA-, while no such difference of mutagenesis was noticed between the strains uvrA+ and uvrA- . These results suggest that NCS produces hardly excisable DNA damage which is repaired by an error-prone recombination process.

J Infect Dis, 1977 Apr, 135(4), 623 - 32
Virulence-associated acquisition of iron in mammalian serum by Escherichia coli; Kochan I et al.; Effects of iron on the growth of avirulent and virulent strains of Escherichia coli were tested in mice and in mammalian sera . Infection of the animals with iron increased mortality rates in mice infected with the avirulent strain to levels found in mice infected with the virulent strain . In vitro experiments showed that bacteria deprived of iron in bovine or human sera or milk or in chicken egg white stopped miltiplication and died in a very short time . These antibacterial effects were neutralized effectively with the addition of exogenous iron or the iron-binding bacterial product, enterochelin . In contrast to avirulent bacteria, which were effectively inhibited in mammalian serum, virulent bacteria were able to obtain iron and multiply . The ability of virulent bacteria to grow in mammalian serum is being attributed to the presence of iron-binding enterochelin and lipopolysaccharide in large amounts on the cell walls of virulent bacteria.

Am J Obstet Gynecol, 1977 Mar 15, 127(6), 603 - 8
Bacterial growth inhibition by amniotic fluid . VII . The effect of zinc supplementation on bacterial inhibitory activity of amniotic fluids from gestation of 20 weeks; Schlievert P et al.; Twenty human amniotic fluids obtained from gestations of 20 weeks' duration supported bacterial growth . Nine of the 20 fluids could be made inhibitory by adjusting the phosphate to zinc ratios of the fluids to less than 200 mug per milliliter . These fluids contained the phosphate-sensitive bacterial inhibitor previously, but the fluids contained sufficient phosphate to inactivate the antibacterial system . The remaining 11 amniotic fluids did not contain the peptide component of the phosphate-sensitive bacterial inhibitor and could not be made inhibitory by adjusting the phosphate to zinc ratio to less than 200 mug per milliliter . The data obtained suggested synthesis of the peptide component may occur at a gestational age of approximately 20 weeks . The peptide may indirectly be detected in fluids by determining whether antibacterial activity is obtained when the phosphate to zinc ratio of the fluids is adjusted to less than 200 mug per milliliter.

J Infect Dis, 1977 Mar, 135 Suppl, S69 - 73
Bacteremia due to Bacteroidacceae: a review of 92 cases; Mathias RG et al.; The clinical courses of 92 patients who had bacteremia due to Bacteroidaceae were reviewed . The overall mortality rate was 21% (19 patients) . There was no significant difference between mortality rates when patients were grouped by anticipated clinical course of underlying disease (nonfatal, ultimately fatal, and rapidly fatal) and when they were grouped by type of antibacterial therapy (appropriate, including clindamycin, chloramphenicol, lincomycin, and carbenicillin; or inappropriate, signifying no antibiotic treatment or treatment with antibiotics other than the four listed above) . However, there was a correlation between recovery of the patient and portal of entry of the infectious agent; patients whose source of infection was the gastrointestinal tract had a mortality rate of 29% (17 of 58 patients), whereas there were no deaths among the 26 women whose presumed source of bacteremia was the genital tract . Increasing age appeared to be an important factor as well; 17 of 19 deaths occurred in patients who were older than 40 years . There was no significant difference between the mortality rate of patients who were treated with clindamycin (15%, eight of 52 patients) and that of patients who were treated with chloramphenicol (44%, four of nine).

Chirurg, 1977 Mar, 48(3), 180 - 3
{Comparative studies on preoperative skin disinfection}; Hiller U et al.; The antibacterial effects of Sepso-tincture, Kodan, Dibromol, and 70% ethanol as disinfectants were compared on the skin of 34 patients of the first surgical department of the general hospital in Hamburg-Barmbek . Special attention was paid to the regeneration of microorganisms in relation to time . The result was that the tested substances showed an almost equal effect after 2 min . However, after 10, and 60 min the tests showed considerable divergencies . In comparison, therefore, with the other substances, it could be proved that the least regeneration of microorganisms was observed after application of Sepso-tincture (significance after 10 min: P less than 0.01, after 60 min: P less than 0.05).

J Antibiot (Tokyo), 1977 Mar, 30(3), 244 - 51
Feedback inhibition of the synthesis of an antibiotic: aurodox (X-5108); Liu C et al.; The effect of aurodox on its own biosynthesis by Streptomyces goldiniensis was studied . It was found that addition of exogenous aurodox inhibits further accumulation of aurodox by the antibiotic-producing culture . Both long term fermentation studies with aurodox-14C and precursor incorporation studies over short time periods indicated that aurodox synthesis was regulated by feedback inhibition . The concentration of aurodox required to completely block further synthesis of the antibiotic was about 400 microng/ml . This is the same as the maximum concentration of aurodox normally accumulated by the culture used in this study . Antibiotic synthesis was inhibited not only by aurodox but also by some structural analogs of aurodox including several having no antibacterial activity . This effect was immediate and readily reversible, indicating that it could be due to inhibition of an enzyme(s) involved in the biosynthesis of aurodox.

Antibiotiki, 1977 Mar, 22(3), 239 - 42
{Properties of a collagen and monomycin complex}; Rudenko TG et al.; The prolonged effect of a single application of a collagen-monomycin sponge was studied experimentally on albino rats on a model of a skin flat wound . The monomycin levels in the blood and tissues in the area of the sponge application for 14 days were determined by the biological method . The therapeutically effective concentration of monomycin, i.e . 3.8 gemma/ml was maintained in the general blood flow for 2 weeks . During this period the local antibiotic concentration was almost 5 times higher . The toxic effect of the collagen-monomycin complex was studied on rabbits and albino rats for 2 months with respect to the indices of the protein metabolism and the content of residual nitrogen and urea . The activity of cholinestrerase and the content of histamine in the blood were determined . No significant changes in the studied tests were observed during the period of the chronic experiment . The microstructure of the organs of the test animals did not differ from that of the intact animals . The collagen-monomycin complex had a prolonged antibacterial effect and was not toxic with respect to the the test animal.

Antibiotiki, 1977 Mar, 22(3), 216 - 9
{Simplified liquid nutrient media for controlling antibiotic activity, the spectrum of their antibacterial action and the sensitivity of microorganisms}; Semenov SM et al.; Beaf-peptone broth and some of its modifications, one of which is a simple and in expensive one to a leser extent binding to antibiotics, such as penicillin, oxytetracycline and streptomycin and providing sufficient growth of the test microbes were used to determine the antibiotic activity with the methods of serial dilutions . The simple modification was recommended for practical use . The MIC of the antibiotics in the above simple medium was less than that in the control . The results of the antibiotic activity determination on both media coincided.

Arch Orthop Unfallchir, 1977 Feb 28, 87(2), 117 - 28
{Hydraulic problems in so-called antibacterial suction-drainage of surgical infections and osteomyelitic cavities (author's transl)}; Boda A; 1 . Suction-drainage should only be employed when there is a closed space enabling free flow of the irrigation fluid . 2 . The drainage of the irrigation fluid must be ensured . 3 . Positioning of the perforated drain is more important than the actual length of the perforated segment of the drain . Enlargment of the holes in the drain may prevent it from clogging and not so much an increase in the number of holes . 4 . The irrigation system must be simple and not be complicated by Y-tubes . 5 . Wound closure should be water-tight for the construction of a closed drainage system.

S Afr Med J, 1977 Feb 26, 51(9), 276 - 9
Bone cement and antibiotics; Ger E et al.; Antibiotics of various kinds were added to the powdered polymer of methylmethacrylate in a concentration of 1 g antibiotic/40 g cement, prior to the addition of the liquid monomer . Specimens were subjected to mechanical testing by loading them in direct compression on a 20-ton Instron Universal Testing Machine, and load deflection curves were recorded . It was found that the addition of antibiotics does have an effect on the mechanical strength of the cement--the loss was small, less than 10% for both the compressive strength and the elastic modulus, provided the antibiotic was in powder form . Liquid antibiotics resulted in a greater loss of the compressive strength of the mixtures, but specimens tended to be less porous . In vitro studies of the antibiotic properties of the mixtures demonstrated potent antibacterial activity in all the antibiotics tested, except chloramphenicol . Possible clinical applications are discussed . Further in vivo studies are needed before widespread clinical use can be advocated.

Med Klin, 1977 Feb 22, Spec No, suppl 33 - 7
{Vibravenös in infections of the biliary and respiratory tracts (author's transl)}; Wickschrath H; The clinical results of a European Vibravenos multicentre trial are reported as far as 227 patients with infections of the biliary tract and 185 patients with infections of the respiratory tract--mainly pneumonia--are concerned . In 203 of the 227 cases with biliary tract infections (=90%) and in 142 of the 185 cases with respiratory tract infections (=77%) the overall clinical result was good or very good . Toleration of Vibravenos was usually very good, only 4 patients had to be withdrawn from the trial because of side effects: in 3 cases an allergic skin reaction or pruritus occurred and in 1 patient local phlebitis developed at the injection site . Bacteriological tests performed on 71 patients showed that after broad usage doxycycline has an excellent antibacterial activity.

J Antibiot (Tokyo), 1977 Feb, 30(2), 129 - 31
Nucleosides . CVI . Syntheses of 1-N-methyl-5-(beta-D-ribofuranosyl)uracil (1-N-methyl-phi-uridine) and its identity with a metabolite elaborated by Streptomyces platensis var . clarensis; Reichman U et al.; Very recently, 1-N-methyl-psi-uridine was isolated from the culture filtrate of Streptomyces platensis var . clarensis along with an antibacterial and antiviral antibiotic, U-44590 . We achieved chemical syntheses of 1-N-methyl-psi-uridine by selective methylation of psi-uridine in two different routes and established the identity of the synthetic nucleoside with the natural product.

J Pediatr Surg, 1977 Feb, 12(1), 55 - 61
The antibacterial effects of impregnated silastic and its possible applications in surgery; Bayston R; We have made an in vitro preliminary study of the feasibility of incorporating suitable antibacterial agents with medical grade silicone rubber ("Silastic") with reference to the immediate and sustained effects in simulated conditions of use . The results are encouraging and further work is planned . The possible applications of such impregnated Silastic in clinical conditions involving implants of various kinds is discussed.

Arzneimittelforschung, 1977 Feb, 27(2A), 286 - 8
{Dose finding in antibacterial chemotherapy (author's transl)}; Metzger K; The therapy of bacterial infections is considered against the background of the relations existing within the system bacteria-man-chemical substance . The experimental conditions and the difficulties are discussed which are encountered in the determination of in vitro values and their transfer into therapy . On this background the basic equation of chemotherapy is discussed . The factors are given which reduce the strict validity of this basic equation and lead to the introduction of a safety factor when making a dose proposal.

Arzneimittelforschung, 1977 Feb, 27(2), 343 - 52
New broad-spectrum alkylthio cephalosporins; Nannini G et al.; A series of 7-substituted alkyl-thio-acylaminocephalosporins with the following general formula were prepared and tested for in vitro antibacterial activity: (formula: see text) . We tried in our research to find any relationship between antibacterial activity and pharmacokinetic properties on the one hand, and chemical structure on the other . The most interesting products were also studied for their in vivo antibacterial activity in experimental acute systemic infections in the mouse.

Farmaco {Sci}, 1977 Feb, 32(2), 92 - 105
{Pyrazole sulfanilamides . XV . Nitroderivatives of 1-phenyl-4-sulfanilamidopyrazole}; Alberti C et al.; The research on the change of antibacterial activity due to the introduction of a nitro group in the benzene nucleus linked at the heterocyclic nitrogen of N-phenylsulfanilamidopyrazoles is continued with the preparation of 1-(2'-nitrophenyl)-4-sulfanilamidopyrazole (IIa: -NO2 in 2'; R=-H), 1-(3'-nitrophenyl)-4-sulfanilamidopyrazole (IIb: -NO2 in 3'; R=-H) and 1-(4'-nitrophenyl)-4-sulfanilamidopyrazole (IIc: -NO2 in 4'; R=-H) . By analogy with the results obtained for the derivatives of 4-sulfanilamidopyrazole (I) previously prepared, enhancement of the bacteriostatic activity in vitro against S . aureus and E . coli, have been observed in almost all the cases, especially with 1-(3-nitrophenyl)-4-sulfanilamidopyrazole (IIb).

J Clin Periodontol, 1977 Feb, 4(1), 62 - 8
Some antibacterial properties of periodontal dressings; Haugen E et al.; Three commercial periodontal dressings were tested for antibacterial activity against salivary microorganisms after having been stored dry or in liquid for 1 and 2 days . Inhibition of growth of mixed salivary flora was evaluated on blood agar dishes . Also, the ability of Strep . mutans to colonize the surface of the dressings was tested . The surface contact test indicated antibacterial activity against salivary microorganisms by freshly made Coe-pak and Wondrpak . Some activity could also be observed after 2 days' storage in about half the experiments . The initial bacteriostatic effect of Peripac was limited to the setting phase . The plaque accumulation test revealed single cells only on the surfaces of Coe-pak and Wondrpak whereas Peripac seemed to be colonized by the test bacteria.

Immunology, 1977 Feb, 32(2), 207 - 13
The effect of trypsin and chymotrypsin on the bactericidal activity and specific antibody activity of bovine colostrum; Brock JH et al.; Digestion of bovine colostral whey with trypsin or chymotrypsin caused a progressive loss of the complement-mediated bactericidal activity of naturally-occurring colostral antibodies of E . coli 0111 . Bactericidal activity was associated primarily with IgG1 immunoglobulin and to a lesser extent with IgM . Chymotrypsin preferentially attacked IgM, destroying its antibacterial activity and producing an apparent decrease in its mol wt . Trypsin preferentially attacked IgG1, but loss of antibacterial activity was in this case not accompanied by a decrease in molecular weight . Using colostral whey with antiperoxidase activity it was shown that the kinetics of loss of specific antibody activity were similar to those of loss of bactericidal activity . It is therefore suggested that trypsin may cause a loss of specific antibody activity of colostral IgG1 without cleaving the immunoglobulin molecule.

Plast Reconstr Surg, 1977 Feb, 59(2), 216 - 22
Iodinated silicone-an antibacterial alloplastic material; Morain WD et al.; Iodine is readily miscible in silicones and will pass freely into and out of this material at highly predictable and constant rates . Iodinated silicone is thus an effective, controlled-rate delivery system for molecular iodine . This delivery system was shown to produce bacteriostatic and bactericidal effects in vitro, and at least bacteriostatic effects in vivo . Iodinated silicone produced a protective effect against the morbidity of infection in the mouse.

Polim Med, 1977, 7(1), 19 - 26
{Surgical plastic materials with prolonged antibacterial activity}; Shalimov AA et al.; Sulphonation and further treatment with geomycine of surgical plastic articles (arterial prostheses, surgical threads) allowed to receive materials with prolongated surface antibacterial activity . The results of experiments on 200 animals proved the modified threads and prostheses to protect the bacteriostatic effect in surgical wounds within 2 to 10 days' period . The healing of implants was uncomplicated . The high antibacterial activity of these materials (500-1000 bacteriostatic doses) stands the radiosterilization and normal keeping conditions.

Chemotherapy, 1977, 23(4), 213 - 26
Biliary excretion of ampicillin: experimental and clinical study; Brogard JM et al.; The biliary excretion of ampicillin was studied in various conditions . Using an isolated perfused rabbit liver preparation, 4.1% of the amount of ampicillin added to the circulating blood (10 mg) was recovered in the bile where the maximum antibiotic activity (mean: 104 +/- microng/ml) was 4 times higher than in the serum (mean: 24.1 +/- 3.4 microng/ml) . In man, provided with T-tube drain, the oral or intravenous administration of 500 mg ampicillin resulted in a biliary excretion of 0.10% of the administered dose . The biliary concentrations thus obtained equalled or exceeded for several hours the minimal inhibitory concentration of the organisms included in the antibacterila spectrum of ampicillin justifying thus the use of this antibiotic in the treatment of biliary tract infections . Per-operatory assays showed that in patients with gallbladder disease or with cystic duct obstruction, ampicillin levels in the gallbladder bile were markedly lower than in the common duct bile.

Anaesthesia, 1977 Jan, 32(1), 69 - 70
A comparison of the antibacterial properties of six local analgesic agents; Zaidi S et al.; The effect of six local analgesic drugs on bacterial growth is reported . Amethocaine proved to be the only effective antibacterial agent.

Mutat Res, 1977 Jan, 42(1), 109 - 15
Study on cytological effects of carofur -- a new mutagen; Vig BK et al.; Chinese hamster cells (line V-79) and human leukocytes in vitro and mice of the CBA strain were treated with carofur (also called nifurprazinum), an antibacterial agent of pharmaceutical importance . At concentrations as low as 20 ppm, the in vitro treatments of cells of Chinese hamster and human lymphocytes expressed chromosome aberrations, almost exclusively of deletion type . This effect resembles that of fluorodeoxyuridine but may not necessarily reflect the same basic mechanism involved . When Chinese hamster cells were treated with 5 ppm or more of carofur for 24 hr, a 3-fold increase in the frequency of somatic sister chromatid exchanges was observed . An interesting phenomenon of "centromeric association" was observed in the bone marrow cells of mice treated with carofur, where the centromeres of the acrocentric chromosomes were oriented towards each other in groups of 2's or more.

Antibiotiki, 1977 Jan, 22(1), 54 - 6
{Lincomycin concentration in human serum and pulmonary tissue}; Farago E et al.; Lincomycin levels in the blood serum and lung tissue were determined in 17 patients after surgical operations because of the lung diseases, the drug being administered in a dose of 500 mg . In 45 to 330 minutes after administration of the antibiotic its concentration in the blood serum and lung tissue was 4.6 +/- 10 lambda/ml(average 7.7 lambda/ml) and 1.4-8 lambda/gm (average 4.4 lambda/gm) respectively . The lincomycin level in the lung tissue amounted to 61 per cent of that in the blood setum . The concentration of lincomycin the lung tissue was several times higher than the minimum level necessary for inhibition of the strains included in the antibiotic antibacterial spectrum . Therefore, lincomycin is an important drug in the treatment of infections of the respiratory tract.

Scand J Infect Dis, 1977, 9(1), 46 - 54
Use of electrophoresis in the identification and quantitation of antibiotics administered in combinations; Carlstrom A et al.; The investigation presents a method of electrophoretic separation of antibacterial drugs which are used in combinations in clinical medicine . Subsequent to electrophoresis in agarose gel, a microbiological assay was performed . This technique permitted the determination of the concentrations of beta-lactam antibiotics, rifampicin, and clindamycin in the presence of aminoglycosides . In therapeutic combinations of fusidic acid and clindamycin, the concentrations of each drug could be determined.

Jpn J Antibiot, 1977 Jan, 30(1), 124 - 7
{Clinical experience with amoxicillin (Pasetocin) in urology (author's transl)}; Sakaguchi H; Amoxicillin, a synthetic penicillin with a broad antibacterial spectrum, was administed in a daily dose of 1.0 g (in potency) to 47 patients who came to the department of urology (6 patients in whom the antibiotic was used for the prevention of infections included) . The results are summarized in the following . 1 . The patients with urological infections who were treated with amoxicillin included 20 patients with acute cystitis, 1 with acute urethritis, 18 with chronic prostatitis, 1 with epididymitis, 1 with pyelonephritis and 6 patients in whom the antibiotic was used for the prevention of infections . Amoxicillin was remarkably effective in 27 patients (58.7%), effective in 7 patients (15.2%), but ineffective in 12 patients (26.1%), with the overall effectiveness of 73.9% . The therapy was withdrawn in one patient because of side effects . 2 . A patient with acute cystitis showed eruption which was probably associated with allergic reaction to penicillin, and the administration was discontinued . Other side effects worth mentioning were not observed.

J Antibiot (Tokyo), 1977 Jan, 30(1), 98 - 105
Mutational biosynthesis by idiotrophs of Micromonospora purpurea . II . Conversion of non-amino containing cyclitols to aminoglycoside antibiotics; Daum SJ et al.; A mutant of Micromonospora purpurea, which produces the gentamicin complex only when 2-deoxystreptamine is added to the fermentation medium, produces a new antibiotic complex, 2-hydroxygentamicin, when streptamine or 2,4,6/3,5-pentahydroxycyclohexanone is added to the fermentation medium . This mutant also produces the gentamicin complex when 2,4/3,5-tetrahydroxycyclohexanone is added to the fermentation medium . The C1 and C2 components of 2-hydroxygentamicin have broad spectrum in vitro antibacterial activity similar to the gentamicin C1 and C2 components, but with greater activity against some gentamicin-resistant strains.

J Antibiot (Tokyo), 1977 Jan, 30(1), 17 - 24
A new aminoglycoside antibiotic complex--the seldomycins . I . Taxonomy, fermentation and antibacterial properties; Nara T et al.; A soil isolate named Streptomyces hofunensis sp . nov . was found to produce seldomycin factors 1, 2, 3 and 5, new aminoglycoside antibiotics . Taxonomy of the producing organism, a study of cultural conditions for seldomycin production, and antibacterial activity of seldomycins are reported . Seldomycin factor 5 was the most active both in vitro and in vivo against gram-positive and negative bacteria.

J Med Chem, 1977 Jan, 20(1), 173 - 5
Synthesis of cephalosporin-4-aldehydes; Beeby PJ; The first reported synthesis of cephalosporin-4-aldehyde derivatives has been achieved via Moffatt oxidation of the corresponding 4-hydroxymethylcephalosporins . The aldehyde 1 was converted into a number of polar derivatives, in particular the acrylic acid derivative 13 which is the 4-vinylogue of sodium cephalothin . None of the new cephalosporin derivatives possessed useful antibacterial activity.

J Med Chem, 1977 Jan, 20(1), 138 - 41
Mitomycin antibiotics . Synthesis and activity of 1,2-disubstituted mitosenes; Taylor WG et al.; cis-1-Acetamido-2-acetoxy-7-methoxy-N-methylmitosene was prepared in 11 steps from 7-methoxy-6-methyl-2,3-dihydro-1H-pyrrolo{1,2-a}indol-1-one by a route involving bromination of the pyrrolidineenamine or trimethylsilyl enol ether of starting material, displacement of bromide by acetate, oxime formation, and reductive acetylation, followed by elaboration of the quinone and methyl carbamate functions according to previously established methods . An unsubstituted carbamate could not be prepared . The mitosene thus synthesized differs from previously reported 1,2-disubstituted mitosenes, which are derived from the solvolysis of mitomycins, in that it has the opposite arrangement of oxygen and nitrogen substituents at the 1 and 2 positions . It showed antibacterial activities in disk-plate assays superior to those of cis-diacetylapomitomycin A and equivalent to those of certain 1-substituted mitosenes; however, it was less active than mitomycin A in these assays . It was inactive in inducing lambda-bacteriophage in Escherichia coli and inactive against P388 leukemia in mice . In contrast, certain 1-substituted mitosenes were active in prophage induction and 2b and mitomycin A were active in both assays.

Chemotherapy, 1977, 23(1), 7 - 10
Intravenous co-trimoxazole ("Bactrim") in the treatment of acute pyelonephritis; Bailey RR; Patients with acute pyelonephritis may be extremely ill and have a complicating septicaemia . This may necessitate the parenteral administration of an appropriate antibacterial agent . This paper reports the use of intravenous co-trimoxazole in two young women with severe acute pyelonephritis . 101 ml of co-trimoxazole (800 mg sulphamethoxazole and 160 mg trimethoprim) was added to 500 ml of 5% dextrose in water and infused over a 90-min period . This treatment was given every 12 h for five doses, before switching to oral co-trimoxazole . The treatment was clinically and bacteriologically successful and no side effects were noted.

Arzneimittelforschung, 1977, 27(11), 2035 - 8
Reactions of hydroxybenzofurans . VI . Syntheses of benzofuran chalcones, hydrazones and pyrazolines of potential biological activity; Hishmat OH et al.; Condensation of 5-acetyl-6-methoxy- (I) and 6-acetyl-5-methoxy-2,3-diphenylbenzofuran (II) with aromatic aldehydes gave the chalcones IIIa--f and IVa--f, respectively . Reaction of the chalcones IIIa--f and IVa--f with hydrazine hydrate-acetic acid mixture yielded the corresponding N-acetyl pyrazolines Va--f and VIa--f . The chalcones IIIa--f and IVa--f reacted with phenylhydrazine in ethanol to yield the corresponding phenylhydrazones VIIa--f and VIIIa--f . The latter hydrazones cyclize easily with boiling glacial acetic acid to the corresponding pyrazoline derivatives (IXa--f and Xa--f) . The antibacterial activity of the chalcones and pyrazolines was investigated.

Arzneimittelforschung, 1977, 27(4), 889 - 90
Biological properties and clinical application of propolis . I . Some physico-chemical properties of propolis; Scheller S et al.; The presence of 19 elements has been shown in the ethanol extracts of propolis (EEP) . Three fractions have been obtained by filtration through a structural gel that did not show an initial antibacterial activity when investigated separately . Fractions 2 and 3 joined together have regained this activity . EEP solutions maintain their anitbacterial activity in acidic or neutral pH . Insensitivity of EEP solutions on temperautre of 75 degrees C for 30 min has been found.

J Hyg Epidemiol Microbiol Immunol, 1977, 21(4), 454 - 9
Pathogenesis of diphtheria carrier state from the immunological point of view; Kostyukova NN et al.; Results of a comparative investigation of diphtheria antitoxin and type-specific antibacterial antibodes in 264 carriers of diphtherial bacteria, 41 diphtheria patients and 263 non-infected subjects are presented . A high level of antitoxin did not prevent the development of toxigenic-strain carrier state . A basically similar immunological antibacterial response was observed in patients with manifest forms of diphtheria and in carriers of toxigenic strains; such a response could not as yet be detected in carriers of non-toxigenic strains . It has been suggested that the infectious process in the toxigenic-strain carrier state is due to factors of the virulence responsible for infectivity and invasiveness of the diphtherial microbe . The toxin plays no pathogenic role in carrier state.

Folia Microbiol (Praha), 1977, 22(4), 269 - 74
Antibiotic activity of pyrenomycetes under submerged conditions; Bandre TR et al.; Twenty-three pyrenomycete species were tested for antibiotic activity in submerged cultures . When they were screened against bacteria and fungi, 15 showed positive results . Among these, Eutypa acharii, Diaporthe pustulata, Melanconis flavovirens and Camarops microspora were quite promising against bacteria and/or fungi . An antibacterial antibiotic from Camarops microspora was partially purified and characterized.

Bull Eur Physiopathol Respir, 1977 Jan-Feb, 13(1), 27 - 46
{Secretory IgA and the antibacterial defenses of the respiratory tract (author's transl)}; Michel FB et al.; The secretory IgA (IgA S) in bronchial mucus is produced by cells which are derived, at least in part, from the BALT (Bronchus Associated Lymphoid Tissue) . The physico-chemical characteristics of IgA S (the amino-acid structure of the alpha chain, the secretory component and the J chain) explain three properties of this antibody which enable it to play its part as the first line of defense on the surface of the mucus, namely its resistance to proteolysis, its adherence and its ability to penetrate mucus . The role of IgA S in the antibacterial defense of the respiratory tract has been in doubt for some time because it does not follow the usual processes of antibacterial action, having neither opsonising nor lytic activity . It is thought at present that IgA S exerts its action in an individual way, more directly and peculiar to the secretory immune-apparatus . It acts by 1) causing agglutination of bacteria and by inhibiting their adsorption on the mucous membranes, 2) inhibiting bacterial reproduction and 3) by inactivating bacterial toxins . The combination of these three processes produces a surface defense system which inhibits bacterial penetration of the mucus . Despite the uncertainties which still exist, it is essential that the fundamental immunological data should be included in the complex picture of the mechanisms of defense of the respiratory tract.

Appl Environ Microbiol, 1977 Jan, 33(1), 211 - 2
Production of cyclopiazonic acid by Aspergillus flavus Link; Luk KC et al.; Production of cyclopiazonic acid by Aspergillus flavus is reported for the first time . A procedure for its production by agitated solid substrate fermentation on red wheat is described along with the isolation procedure and physical and chemical properties of this indole derivative . The compound has been found to exert antibacterial activity.

Semin Perinatol, 1977 Jan, 1(1), 59 - 70
Amniotic fluid antibacterial mechanisms: newer concepts; Schlievert P et al.; In this review the factors present in human amniotic fluid that may function to inhibit bacterial growth have been examined . It appears that several potential antibacterial systems are present . Lysozyme and B-lysin may significantly contribute to the killing of gram-positive bacteria . Whether or not the remaining antibacterial systems function to inhibit gram-positive organisms remains to be determined . The phosphate-sensitive bacterial inhibitor recently described in our laboratory may represent the primary defense mechanism against gram-negative bacteria in amniotic fluid . Studies are warranted to ascertain whether this antibacterial system also inhibits gram-positive bacteria . The phosphate-sensitive bacterial inhibitor is quite different from other bacterial inhibitors in at least three respects . The system is very sensitive to the ubiquitous phosphate anion . The reason for this sensitivity is unknown and is difficult to explain phylogenetically, since phosphates are present virtually everywhere . To our knowledge this is the first antibacterial system of human origin which has been shown to require a metal cation as an integral part of the bactericidal effect . The peptide component of the phosphate-sensitive bacterial inhibitor is also unique in that it is of the molecular size of antibiotics or hormones . Additionally, the peptide does not appear to contain any unusual amino acids to explain its antibacterial activity . The mechanism of bacterial destruction of the phosphate-sensitive bacterial inhibitor, and its relation to the other antibacterial systems in amniotic fluid, remain to be elucidated.

Microbiol Immunol, 1977, 21(9), 481 - 94
Effect of dihydroxymethyl furatrizine on cell division of Escherichia coli; Iida K et al.; Antibacterial activities of 3-di(hydroxymethyl) amino-6{2-(5-nitro-2-furyl)vinyl}-1,2,4-triazine, (dihydroxymethyl furatrizine) were investigated using mutant strains of Escherichia coli lacking repair systems for DNA damage, i.e . polA, uvrA, uvrA, uvrC, recA, recB, recC and uvrArecA . All of the mutant strains were more sensitive to the drug than the parent sgrains, as was the case with the sensitivity to UV-irradiation . These results indicate that the drug acts lethally on sensitive bacteria by damaging their DNA, and parts of the damaged DNA are repaired by excision and recombinational repair systems . Filamentous cell formation was induced in all strains except the uvrArecA strain by sublethal concentration of the drug, as well as by UV-irradiation . It is possible that the occurrence of the short period of "unbalanced growth" induced by such DNA damaging agents leads to filament formation . In the cells of the double mutant, filament formation was induced by the drug but not by UV-irradiation, and the majority of the filamentous cells formed were multinucleated . This suggests that, in this double mutant, the drug directly reacts with the septation mechinery of the cell envelope, resulting in filament formation . This hypothesis is supported by the electron microscopic observations that septation is interrupted in the filamentous cells induced by the drug.

Scand J Plast Reconstr Surg, 1977, 11(1), 33 - 7
Antibacterial effect of biological dressings in the treatment of infected wounds; Bartholdson L et al.; Human cadaver split skin preserved in a special transport medium (Histocon; Histo-Lab . Ltd., Goteborg, Sweden) and porcine split skin (Skintec; Genetic Lab . Inc., Minneapolis, USA), were used in thirteen patients with infected wounds . Cadaver skin made it possible to reduce applications of wound dressing to two or three times a week without aggravation of infection and made the wound bed suitable for autografting . Skintec was less reliable in these respects . The two biological dressings had equal pain reducing properties . Leukocyte agglutinins, attributable to the treatment with cadaver skin did not appear . Because of retained histological and histochemical characteristics in the preserved cadaver skin it was preferred to Skintec . A regimen consisting of initial wound toilet, antibiotic treatment, skin changing every second or third day finally made permanent skin grafting possible . Secondary gains were a reduce in nursing and dressing routine as compared to saline dressings.

Scand J Infect Dis, 1977, 9(3), 204 - 6
The effect of eight antibacterial agents on the elimination of 32P-labelled Escherichia coli by rat polymorphonuclear cells; Melby K; The effect of 8 antibacterial agents on the elimination of 32P-labelled Escherichia coli from rat polymorphonuclear cells was studied . None of the drugs tested had a detectable influence on the expulsion of labelled products from the cells being exposed to the various drugs during the elimination phase.

Biochimie, 1977, 59(1), 59 - 63
Stability of 70S ribosomes in relation to misreading and antibacterial activity of aminoglycosides; Cousin MA et al.; The anomeric aminoglycosides, RU 21886 and RU 23468, which both have a 2-deoxystreptamine residue, stabilize 70S ribosomes to similar extents at low magnesium ion concentrations . Only RU 21886, however, has marked antibacterial and bactericidal activity and gives rise to a high level of misreading in cell-free protein synthesizing systems . It would thus appear that the ability to stabilize the association of the two ribosomal subunits does not necessarily lead to errors in translation.

Bull Eur Physiopathol Respir, 1977 Jan-Feb, 13(1), 83 - 94
{Kinetics of pulmonary defense in deep lung (author's transl)}; Arnoux B et al.; The association of different experimental methods using radioactive particulate aerosols with bronchial washing and morphometric techniques reveals the importance of alveolar macrophages in antibacterial defense and the interest of their quantitative evaluation . The study of the kinetics of pulmonary phagocytic systems has shown a "capillary compartment", which consists of a reserve of monocytes which are temporarily present in the lung and in transit through it . This reserve represents 4.6% (sigma=1.4) of the cells from deep in the lung and is much larger than the systemic monocytic pool . 0.5% of these monocytes are in a phase of DNA synthesis . This capillary compartment must be clearly separated from interstitial phagocytes, the number of which is insignificant under physiological conditions . The phagocytic relay by polynuclear elements appears during bacterial aggression and is interdependent with macrophagic population . The particularities of the immune defenses of the distal parts of the lung are stressed especially in comparison with systemic defenses.

Bull Eur Physiopathol Respir, 1977 Jan-Feb, 13(1), 57 - 67
Role of the alveolar macrophage in pulmonary bacterial defense; Goldstein E et al.; This review concerns the role of the alveolar macrophage as part of the coordinated mucociliary, macrophge and immune bacterial defense mechanisms of the lung . Alveolar macrophages are end-stage phagocytes that are derived from two precursor sources; an uncommitted pleuripotential hematopoietic stem cell, and a committed differentiated pulmonary precursor which can renew itself, as well as mature into functional alveolar macrophages . Sufficient numbers of alveolar macrophages are distributed throughout the lungs to ensure their proximity to any bacteria that penetrates alveolar regions . Studies with rodents have shown that these alveolar macrophages ingest, inactivate, and degrade inhaled microorganisms within eight hours of their entrance into alveolar regions . The biochemical mechanisms responsible for this antibacterial function involve the elaboration of chemotactic factors consequent to the interaction of bacteria, antibody, and complement, and the presence of bactericidal substances within the macrophage itself . Normally, these cellular mechanisms enable the alveolar macrophage system to maintain the lungs bacteria-free . However, if macrophage function is impaired due to pollutant or viral exposure, the host-parasite balance is upset and bacterial proliferation ensues . In such circumstances, polymorphonuclear leucocytes and additional macrophages enter the area of bacterial proliferation to produce the classical inflammatory reaction of pneumonia.

Scand J Infect Dis, 1977, 9(1), 9 - 12
The effect of eight antibacterial agents on the phagocytosis of 32P-labelled Escherichia coli by rat polymorphonuclear cells; Melby K et al.; Using 32P-labelled Escherichia coli, the effect of 8 antibacterial agents on the ability of rat polymorphonuclear cells to ingest the labelled bacteria was studied with and without serum present during the ingestion phase . No impairment of ingestion was observed when testing gentamicin, cephalothin and trimethoprim . High doses of oxytetracycline, doxycycline, colistin, erythromycin and chloramphenicol seemed to impair ingestion . The effect was most pronounced when applying 100 mug/ml of doxycycline: the ingestive capability was reduced to 25% without serum and 24% with serum present compared to untreated controls . 83 mug/ml of colistin reduced theingestion to 39% without serum present, this effect being totally eliminated when serum was present during the ingestion phase.

J Pharm Sci, 1977 Jan, 66(1), 88 - 92
Antibacterial structure-activity relationships obtained with resistant microorganisms I: Inhibition of R-factor resistant Escherichia coli by tetracyclines; Miller GH et al.; Aparent partition coefficients and inhibitory activities against sensitive and resistant Escherichia coli were determined for 14 tetracyclines . The difference in the kinetics of inhibition of the two organisms is discussed in terms of their permeabilities . The partition coefficients were determined in an octanol-buffer system . Values for eight compounds were in general agreement with the literature; values for the remaining six compounds had not been reported previously . Growth of the organisms was determined by a single-point turbidimetric method in the presence and absence of tetracyclines . Inhibitory activities were obtained by a kinetic treatment . Derived rate constants for the sensitive organism were linearly related to antibiotic concentration . For the resistant organism and 12 compounds, the derived rate constants and antibiotic concentration were related in a manner typical of saturation kinetics . These inhibitory activities were related to the partition coefficients, while activities against the sensitive strain were not . These findings suggest that activity against the resistant strain is permeability controlled but that activity against the sensitive strain has a different rate-determining step.

Phys Ther, 1977 Jan, 57(1), 16 - 23
Management of the burned hand; Newmeyer WL et al.; Current concepts in the management of acute and chronic injury to hands due to thermal burns are presented . A review of relevant functional anatomy and its alteration by the burn process is outlined . The maintenance of wrist extension, metacarpophalangeal flexion, and an open thumb web is critical in the acute phase . The physical therapist, using splints and regular exercise, is the key person in maintaining this position . The use of antibacterial agents, surgical debridement, and skin grafting is discussed . Surgical methods of reconstruction in chronic burns, the long-term role of the physical therapist, and the use of compression garments to minimize scar are stressed.

J Med, 1977, 8(3-4), 177 - 89
In vivo investigation of antibacterial ointments; Tabernero E et al.; The clinically used topical antibiotic ointments, gentamicin 0.1%, oxytetracycline 3% w/polymyxin 0.1% and chloramphenicol 2% and an experimental preparation, 10-undecen-1-yl thiopseudourea iodide (AHR-1911) were studied for anti-infective action applied externally on the skin of mice inoculated subcutaneously with S . aureus and E . coli . In both infections statistically significant difference was encountered between curative and "clinical" healing rate in the case of the less effective preparations and/or dosages . The method appears suitable to establish and to compare the in vivo activity of ointments . This is not directly related to that of the aqueous drug solutions . AHR-1911, a powerful inhibitor of nucleic acid and protein synthesis, showed a bimodal action, with maximal effectiveness at 0.12-0.25% concentration, due presumably to the anti-inflammatory effect of higher concentrations . Direct evidence for the absorption of the drug from the application site was obtained using 14C labeled AHR-1911.

Zahn Mund Kieferheilkd Zentralbl, 1977, 65(8), 851 - 8
{Biological testing of pulp-preserving agents on the pulp of rat molars}; Gangler P et al.; The effects of calxyl, ZOE, zinc oxide without eugenol, and zinc oxide with an antibacterial substance (glutaraldehyde) were tested on perforated molar pulps of rats . All of the substances tested were found to lead to the same initial reactions (acute inflammation and partial necrosis) . Calxyl and ZOE yielded unfavorable results . There was a negligible tendency of the pulp toward hard tissue demarcation . Zinc oxide without eugenol improved the formation by the pulp of secondary tin . - The use of glutaraldehyde resulted in a less pronounced spread of inflammation as well as in the formation of new hard tissue in one half of the cases . Molars of rats are particularly suitable for biologically examining the local toxicity of pulpal protectives and the regeneration of the pulp . The results presented in this paper are discussed from the point of view of pulp-preserving therapy and of avoiding invasion by germs.

Acta Microbiol Acad Sci Hung, 1977, 24(1), 1 - 6
Antibacterial effect, plasmid curing activity and chemical structure of some tricyclic compounds; Molnar J et al.; Diethazine, amitriptyline and imipramine showed bacteriostatic and bactericidal effect on different bacteria . Chlorpromazine sulphoxide and fluorescein were ineffective even at 1000 microgram/ml . The antibacterial compounds deleted at 40-70% frequency the F'lac plasmid of Escherichia coli K12 LE-140.

Jpn J Antibiot, 1977 Jan, 30(1), 1 - 6
{Bacteriological evaluation of clindamycin-2-phosphate (author's transl)}; Ono H et al.; Clindamycin-2-phosphate, a newly developed injectable antibiotic, was bacteriologically evaluated in comparison with the parent compound, clindamycin . Clindamycin-2-phosphate has a rather weak antibacterial activity . However, it is metabolized into clindamycin in vivo . And this parent compound shows strong activity against both gram-positive bacteria and gram-negative cocci . In vitro studies demonstrated that clindamycin-2-phosphate and clindamycin are affected by the pH of the medium used--the antibacterial activity becomes stronger as the medium is made more alkaline--while they are little affected by the size of the inoculum . In mice with experimental infections, clindamycin-2-phosphate showed about the same therapeutical effect as clindamycin in contrast with the former's inferior in vitro activity as compared with the latter.

J Antibiot (Tokyo), 1977 Jan, 30(1), 59 - 65
Chemical modification of coriolin B; Takeuchi T et al.; Several derivatives of 5-ketocoriolin B (8, 11, 12) chemically modified at C-8 have been synthesized . These derivatives showed antitumor and antibacterial activity of the same degree as 5-ketocoriolin B (4) and diketocoriolin B (5) which were the most active members of the known coriolin group antibiotics . These derivatives were more stable than 4 and 5 in acidic or alkaline solution.

Br J Surg, 1976 Dec, 63(12), 978 - 80
Noxytiolin and peritoneal adhesion formation; Gilmore OJ et al.; Clinical and experimental studies have suggested that intraperitoneal noxytiolin prevents adhesion formation . A reliable experimental animal model was therefore established and the effect of noxytiolin on adhesion formation was evaluated in a controlled trial using 80 rats . All 40 rats given Ringer solution developed adhesions, whereas in 7 out of 40 given noxytiolin no adhesions were found (P less than 0-02) . Noxytiolin reduced both the total and the mean number of adhesions formed (P less than 0-2) and their mean length of attachment (P less than 0-05) . The anti-adhesive effect of noxytiolin may be due to its anticoagulant, cytotoxic or antibacterial properties.

Contact Dermatitis, 1976 Dec, 2(6), 301 - 4
Allergic contact dermatitis and conjunctivitis to corticosteroids; Alani SD et al.; This is a report of two patients suspected of having allergic dermato-conjunctivitis due to corticosteroids . Both were tested with the constituents of the ointments they were using, that is, corticosteroids, antibacterial agents, preservatives, and other active ingredients of the ointment bases . Both patients showed positive allergic patch test reactions to the respective corticosteroid betamethasone valerate, and one to hydrocortisone, neomycin, and a rubber additive . The importance of routine patch testing in ophthalmic practice to detect sensitizers in cases of allergy is mentioned . Hydrocortisone (25%) in petrolatum is recommended for patch testing.

Antibiotiki, 1976 Dec, 21(12), 1059 - 62
{New producer of cephamycin C, Streptomyces filipinensis var . cephamycini var . nov.}; Gauze GF et al.; An actinomycetes strain 3016 was isolated from a soil sample on a selective medium with actinomycin as a result of directed screening of organisms producing beta-lactam antibiotics . The culture fluid of the isolate contained an antibacterial anibiotic identical to cephamycin C . Description of the strain is presented . It is a representative of new variety of streptomyces filipinensis var . cephamycini var . nov . The results of the study of the chemical properties of antibiotic 3016 and its identification with cephamycin C are also presented.

J Urol, 1976 Dec, 116(6), 757 - 8
Forty years of transurethral prostatic resections; Perrin P et al.; The 4 consecutive series of transurethral prostatic resections compared were done by the senior authors during a period of nearly 40 years: 420 cases in 1937 to 1938, 520 cases in 1940 to 1945, 480 cases in 1950 to 1955 and 270 cases in 1972 to 1973 . The most notable improvements in the recent series are the fewer patients with temperatures more than 100 degrees (69 virsus 29 per cent) and the improved mortality rate (5.5 verus 0.7 per cent) . In our opinion these improvements are owing to antibacterial medication, improved instruments, more skillful performance of the operation, the use of isotonic irrigating fluid and improved postoperative care.

Antibiotiki, 1976 Dec, 21(12), 1116 - 21
{Etiopathogenetic approach to the treatment of viral-bacterial pneumonias}; Nekliudova LI et al.; The efficacy of aerosols of leukocytal interferon used in complex with antibacterial and other medicamentous agents was studied during influenza epidemic in 1975 due to Port-Chalmers virus of influenza A with increased numbers of viral-bacterial pneumonia . The viral-sta-phylococcal etiology of the infection was confirmed in 80 per cent of the cases under stationary conditions . Various microorganism and most often Staph aureus were isolated in addition to the viruses from the patient's sputum and washings and their antibioticograms were determined . The studies showed that the complex treatment of the patients with virologically and serologically confirmed diagnosis of the disease resulted in decreased duration of the disease, less pronounced intoxication and more rapid resorption of the changes in the lung tissue.

Tijdschr Diergeneeskd, 1976 Dec 1, 101(23), 1291 - 7
{Antibiotic sensitivity tests (author's transl)}; Devriese L; Sensitivity to antibacterial agents may be studied using quantitative dilution tests and qualitative diffusion tests . There is a strongly felt need for standardized testing methods . Currently, the so-called Bauer-Kirby method appears to be the most suitable test, also for use in veterinary medicine . When this technique is adopted, results are classifid as "sensitive", "resistant" and "showing diminished sensitivity" . Interpretations are based on pharmacological, bacteriological and clinical criteria . In some situations, in vitro results have not been sufficiently tested in the field . This would appear to be particularly so in local conditions and treatment.

Clin Exp Immunol, 1976 Dec, 26(3), 463 - 8
Neutrophilic granulocytes in acute bacterial infection . Sequential studies on lysozyme, myeloperoxidase and lactoferrin; Hansen NE et al.; The changes in intraneutrophilic and plasma concentrations of the three antibacterial proteins lysozyme, lactoferrin, and myeloperoxidase were studied sequentially during acute bacterial infection in nine patients . Intraneutrophilic concentrations of the three proteins were decreased by more than 50% during the 1st week of infection, followed by a slow increase over the following 2 weeks . Nadir values coincided with maximal toxic granulation of the neutrophils . The data suggest that neutrophilic granulocytes are deficient during early bacterial infection, possibly because of deficient synthesis of antibacterial proteins in the bone marrow, and that neutrophil toxic granulation is the visual counterpart of this defect . The plasma concentrations of the three proteins showed considerable differences: whereas plasma lysozyme did not show any sequential changes, plasma myeloperoxidase was high at the start of infection and quickly decreased towards normal values, and plasma lactoferrin, high in the first samples, showed a secondary peak 1 week after onset of disease, before normalization was seen . These differences may result from differences in the signals are specific for the individual antibacterial protein and not for the different types of neutrophil granules.

Cancer Res, 1976 Dec, 36(12), 4378 - 81
Radioimmunoassay of neocarzinostatin, an antitumor protein; Samy TS et al.; Antibodies directed toward the antitumor protein neocarzinostatin (NCS) have been produced in a rabbit by immunization with a highly purified NCS preparation . The antiserum was monospecific and reversed the antibacterial activity of NCS against Sarcina lutea . It cross-reacted with chemically modified derivatives of NCS and mitomalcin but failed to cross-react with macromomycin . A radioimmunoassay procedure has been developed utilizing the antiserum and a biologically active 125I-labeled derivative of NCS . The lower limit of detection by this radioimmunoassay, which involves a double antibody technique for the separation of antibody-bound and free antigen, was 1 X 10(-13) mole . The sensitivity of the assay is such that serum levels of NCS can be determined accurately after administration of the drug to rats at a single dose of 2 mg/kg . Since NCS is now undergoing clinical trial, the radioimmunoassay of the drug will be a valuable tool in clinical pharmacological studies.

J Clin Periodontol, 1976 Nov, 3(4), 195 - 9
The effect of two commercial antibacterial mouthrinses on plaque growth in vivo; Saxen L et al.; An experimental study was designed to compare the claimed antibacterial effect of Betadine and Blend-a-med Fluid with the known plaque growth inhibiting effect of a 0.2% aqueous solution of chlorhexidine digluconate (Hibitane) . Before the test perios for 5 days . During the following week they cleaned their teeth mechanically with toothbrush and toothpicks . For the third week the students were divided into three experimental groups . Following closely the manufacturers' recommendations, one group rinsed their mouths four times daily with 10 ml of Betadine, one group every 2 hours with a glassful of water containing 5-8 drops of Blend-a-med Fluid, and the control group twice daily with 10 ml of the 0.2% chlorhexidine solution . Mechanical cleaning of the teeth was not allowed during the experimental week . The Plaque Index scorings decreased significantly from the end of the no-hygiene to the end of the mechanical cleaning period . During the experimental period a further decrease of the mean P1I scores returned to the level recorded after the no-hygiene period . As neither Betadine nor Blend-a-med Fluid proved able to prevent plaque growth in vivo, there seems to be no indication for their use in treatment of gingivitis.

Vopr Neirokhir, 1976 Nov-Dec, (6), 29 - 34
{Clinico-immunologic periods of spinal cord injuries}; Kaplan AE; A clinical and immunological periodicity of spinal cord injuries is introduced, comprising 5 periods . The periodicity is based on a study of the indices of a specific and non-specific immunological reactivity of 150 persons with vertebral column traumas accompanied by spinal cord injuries studied after different periods following the trauma and compared with the clinical data and results of similar examinations in the controls . The clinical and immunological periodicity plays an important role in the panning of rational therapy, in the evaluation of bacteriuria and the principles of antibacterial therapy, as well as for the exaluation of the neurodynamics of the injured spinal cord.

Farmaco {Sci}, 1976 Nov, 31(11), 824 - 44
{Correlative analysis of chemical structure - biological activity using Hansch's method: principles and development of the method}; Grieco C et al.; The basic principles and developments on which the Hansch multiple parameter approach depends are described . A correlation analysis on the antibacterial activity of 2-Y-4-(X-phenyl)-3H-1,5-benzodiazepines is discussed . The use of indicator varioables is shown to greatly increase one's ability to formulate quantitative structure-activity relationships . This approach allows one to carry out objective studies of massive amounts of chemical and biological data.

Farmaco {Sci}, 1976 Nov, 31(11), 791 - 6
Dimeric hydrazones of 3-formylrifamycin SV:synthesis, antibacterial activity and other biological properties; Cricchio R; The synthesis of some dimeric hydrazones of 3-formylrifamycin SV is described . The chemical and physical characteristics, the antibacterial activity and other biolgoical properties of the new derivatives are reported.

Ann Clin Lab Sci, 1976 Nov-Dec, 6(6), 540 - 4
Elution of filtered granulocytes for transfusion; Morse EE et al.; Functional and clinical transfusion studies were carried out on granulocytes eluted from nylon filters using ACD Saline solutions and 20% CPD Plasma ACD Saline solutions . Although the average volume of blood and total number of granulocytes filtered were the same, the yield of granulocytes eluted form the filters was 20% greater when 20% CPD plasma was in the eluting solution . Function studies indicated that while the antibacterial capacity of the saline eluted granulocytes was equivalent to that of plasma eluted cells, chemotactic activity was markedly reduced after 24 hours storage in the saline eluted cells . Clinical studies post transfusion also suggest better response from plasma eluted granulocytes.

Can J Microbiol, 1976 Nov, 22(11), 1612 - 9
Antibacterial activity of marine violet-pigmented Alteromonas with special reference to the production of brominated compounds; Gauthier MJ et al.; The synthesis of several types of antibiotics was investigated in four strains of violet-pigmented bacteria belonging to the species Alteromonas luteo-violaceus . Two of the strains simultaneously produce an antibiotic polyanionic polysaccharide, weakly bound to the cells and diffusing throughout the medium, and two intracellular brominated bactericidal substances . The third strain only synthesizes the polyanionic antibiotic . The fourth one is totally inactive . The macromolecular antibiotic, probably responsible for the autointoxication of the bacteria in their cultures, acts at the respiratory level; it induces an increase of oxygen uptake and the production of peroxides by test bacteria . Thus, its activity is inhibited by catalase and peroxidase.

J Immunol, 1976 Nov, 117(5 Pt.2), 2042 - 4
Lack of antibody activity directed against the most common human bacteria in human myeloma protein; Pillot J et al.; The fact that sera of germ-free animals contain very little Ig suggests that most Ig probably correspond to antibacterial antibodies . We have detected an antibacterial activity against 40 bacterial strains, pathogenic and nonpathogenic, in 85 M-component of human origin . This work has been conducted by indirect immunofluorescence withipure labeled antibodies . The reasons for which indirect immunofluorescence seems to be the best technique for this kind of research are discussed . No activity whatsoever could be detected . The reasons of this lack of activity remain to be explained.

Infect Immun, 1976 Nov, 14(5), 1156 - 66
Isolation of a low-molecular-weight antibacterial system from human amniotic fluid; Schlievert P et al.; A low-molecular-weight antibacterial system has been isolated from human amniotic fluid . The bacterial inhibitor requires the metal cation zinc and a peptide with a molecular weight of 630 . The peptide component was purified using ultrafiltration, gel filtration, and ion-exchange chromatography . It can be inactivated by digestion with carboxypeptidase . The amino acid composition of the peptide is: 3 glutamine-glutamic acid, 2 glycine, and 1 lysine . Removal of zinc from the peptide has been shown to remove bacterial inhibitory activity.

Schweiz Med Wochenschr, 1976 Oct 30, 106(44), 1489 - 98
{The importance of clinical observations for medical research}; Koller F; Medical progress owes a great deal to the fundamental medical sciences and to the application of chemistry, physics and mathematics to medical problems . However, clinical observations and investigations are still of decisive importance in any field of medicine . By a feed-back mechanism they may even stimulate and fertilize fundamental medical sciences . Thus, our knowledge of the blood coagulation mechanism has been considerably enlarged by clinical analysis of hereditary bleeding disorders . - Chemotherapy of neoplastic diseases started from clinical observations during World War I (production of leucopenia by sulfur mustard gas) . - Surgical procedures and their consequences have contributed greatly to our knowledge of thyroid function, of the segmental anatomy of the lung, and of the conduction system of the heart . - Observations of side effects of drugs have often enlarged or completely changed their primary clinical indications: from antibacterial sulfonamides, anti-diabetic, antihypertensive and powerful diuretic drugs have been developed, and from histaminics the modern neuroleptics and antidepressants . - Fundamental immunology has been enormously activated by clinical transplantation of kidney and bone marrow . Selective immunological defects in men, real experiments of nature, contributed much to our knowledge of the various types of allergic response . The quality of clinical investigations, particularly of controlled clinical trials, has been considerably improved during the last two decades . Although it is an applied science the reliability of its results is to-day comparable with that of "pure" natural sciences . However, medicine is more than a natural science: examples of outstanding scientists who at the same time were great and human physicians are presented.

Med Klin, 1976 Oct 29, 71(44), 1903 - 6
{Urethritis syndrome and atypical germ flora of the exterior female genitalia (author's transl)}; Hofstetter A et al.; A positive microbiological evidence could be obtained 54 times from the smear of the exterior genitals of 80 women suffering from complaints that were caused by urethritis, criteria of the examinations being sterile catheter specimen, negative cystoscopical findings, and missing indications to anatomical changes in the urethral region . Cytological examinations of these cases with regard to the vaginal epithelium had the following results:Group I:6 times; group II: 37 times; group IIW:8 times; group IIId: once; group IVa:twice . The cytological tests were carried out according to the method of papanicolaou as modified by Soost . Furthermore, we could state the following degrees of purity: Degree I: 8 times; degree II:16 times; degree III: 30 times . The cytological examinations of the urethral epithelium demonstrated, in 52 cases, an increased appearance of "nude" completely exposed epithelial cell nuclei--a fact corresponding to a degenerative autolysis (according to Wied) . In the 26 women with missing atypical germ flora within the region of the exterior genitals, exclusively groups I (according to Papanicolaou and Soost) and degrees of purity I were stated . These persons also demonstrated remarkably grave psychical disturbances, especially in the intimate regions . In the cases of positive microbiological evidence, the following measures have proved satisfactory: Vaginal hygienization combined with a directly aimed antibacterial therapy, and the prescription of preparations containing lactic acid . A transitory discontinuation of contraceptives is being discussed . Our examination results are emphasizing the necessity of an analysis of the germ flora in cases of complaints arising from urethritis . Also psychical disturbances must be taken into consideration in cases of missing urological and gynaecological criteria of evidence.

Science, 1976 Oct 29, 194(4264), 533 - 5
Antibacterial synergism: a proposal for chemotherapeutic potentiation between trimethoprim and sulfamethoxazole; Poe M; Sulfamethoxazole and other sulfa drugs are moderately potent inhibitors of Escherichia coli dihydrofolate reductase . They also significantly potentiate the inhibition of this enzyme by trimethoprim . The molecular basis for inhibition potentiation is the simultaneous binding of trimethoprim and sulfa by the enzyme . This potentiation may explain the synergism observed when these drugs are used in antibacterial chemotherapy.

Z Gesamte Inn Med, 1976 Oct 15, 31(20), 828 - 34
{The cephalosporins and their clinical value}; Tauchnitz C; Up to now cephalothin was the only parenteral and cephalexin the only oral cephalosporin for clinical use in the GDR . The paper deals with several newer cephalosporins . Of these cephazolin shows some advantages, especially in antibacterial activity and serum levels . There is no metabolization and a better local tolerability compared with cephalothin . Cephapirin has no and cephacetril only inessential advantages . The antibacterial activity of the also well tolerated cephradin is less than that of cephalothin . Certain favourable pharmacokinetic properties such as high lymph and tissue levels, related to serum levels, slight protein binding, high distribution volume and a better stability against beta-lactamases lead to a superiority over cephalothin and diminish the disadvantages compared with cephazolin . The oral form of cephradin very equals to cephalexin.

Vestn Khir Im I I Grek, 1976 Oct, 117(10), 64 - 8
{Experience with treating complicated forms of abscessing pneumonia in children}; Pipiia VI et al.; Under observation were 157 patients with different forms of abscessing pneumonias . Pleural complicaitons were noted in 113 patients (about 60%) . The complex treatment was employed in all patients (intensive antibacterial therapy, immunotherapy, bacteriophage, administration of protein preparations, vitamin-therapy, fresh blood transfusion, artery system and by means of percutaneous catheterization of th subclavian vein . The results of the treatment are described.

J Antibiot (Tokyo), 1976 Oct, 29(10), 1007 - 14
Antibiotics produced by Streptomyces ficellus II . Feldamycin and nojirimycin; Argoudelis AD et al.; Feldamycin, a new antibacterial agent, and nojirimycin, a previously described antibiotic have been isolated from cultures of Streptomyces ficellus . Feldamycin, C17H25N7O5, is an amphoteric compound which inhibits a variety of bacteria in vitro but is found to be ineffective in the treatment of experimental bacterial infections in mice . Nojirimycin (5-amino-5-deoxy-D-glucose) has been isolated previously from cultures of several species of streptomycetes.

Biotechnol Bioeng, 1976 Oct, 18(10), 1463 - 72
An immobilized two-enzyme system for the activation of the lactoperoxidase antibacterial system in milk; Bjorck L; Lactoperoxidase catalyzes the oxidation of thiocyanate by hydrogen peroxide and an intermediary product is formed with antibacterial properties . The components of this system, with the exception of hydrogen peroxide, are present in milk . H2O2 may be introduced by means of enzymatic generation and thus make the system complete . A two-enzyme system consisting of beta-galactosidase and glucose oxidase has been developed for this purpose . The coupled enzyme reaction is shown to work with high efficiency at the neutral pH of milk although the enzymes as such, particularly lactases suitable for immobilization, have optimal activities at much lower pH values . The results indicate that the lactoperoxidase system may in this way be employed to inactivate bacteria present in milk.

Proc Natl Acad Sci U S A, 1976 Oct, 73(10), 3386 - 90
Nitrofurans, a group of synthetic antibiotics, with a new mode of action: discrimination of specific messenger RNA classes; Herrlich P et al.; Nitrofurans, a class of antibacterial drugs in extensive use, interferes with gene expression in a highly specific manner . While in the low dose range (0.5-25 mug/ml), 5-nitro-2-furfurylidene-1-aminohydantoin has no effect on transcription, it inhibits specifically the expression of one class of genes in translation . The specific inhibition concerns the inducible genes . The inhibition of messenger RNA expression occurs at the initiation step . The action of nitrofurans, thus, indicates heterogeneity in the population of mRNA molecules and in the translational machinery and suggests the possibility of selective translational control.

Gut, 1976 Oct, 17(10), 801 - 11
Cholangiography in the jaundiced patient; Elias E; Though local practice will reflect the previously acquired expertise of the operators, it seems reasonable to employ a minimum of percutaneous transhepatic cholangiography, and, ideally, this in combination with ERCP for preoperative cholangiography in patients with cholestatic jaundice . Few cases will defy both techniques . The morbidity is well known and if properly anticipated can be reduced to a minimum by judicious use of antibacterial agents and early surgical intervention when appropriate . Grey-scale ultrasonography by indicating the diameter of the bile ducts enables one to select percutaneous transhepatic cholangiography for dilated ducts and ERCP for non-dilated ducts with an almost 100% success rate for the former and only slightly less for the latter in experienced hands.

MMW Munch Med Wochenschr, 1976 Sep 24, 118(39), 1253 - 4
{Treatment of inflammatory diseases of the mouth and throat with Larypront in ENT practice (author's transl)}; Reinecke M; Treatment of inflammations of the oral and pharyngeal cavities (glossitis, pharyngitis, pharyngolaryngitis, tonsillitis) in 60 patients with Larypront Throat Tablets alone, without administration of systemic antibiotics, gave very good results in 49 cases (81.6%) with complete regression of the complaints in 3-4 days . In 11 patients with acute pharyngitis and tonsillitis without demonstrable effect, systemic antibiotic therapy had to be added because of radiologically demonstrable acute sinusitis or increasing antibacterial infection . Side effects were not seen with the use of Larypront in any case.

Antibiotiki, 1976 Sep, 21(9), 779 - 84
{New species of Actinomadura coeruleoviolacea sp . nov . and its antagonistic properties}; Preobrazhenskaia TP et al.; Eight strains of actinomycetes isolated from soil samples were described as representatives of Actinomadura coeruleoviolacea sp.nov . The species was characterized by straight and sometimes branching short chains of spores, smooth spores, blue aerial mycellium and violet soluble pigment . All the strains showed antibacterial activity when cultivated in liquid media . The pigment differed from all known pigments . It is probably a new natural compound.

Thromb Haemost, 1976 Aug 31, 36(1), 115 - 26
Bleeding in uremic patients after carbenicillin; Andrassy K et al.; Hemorrhagic diathesis was observed in patients with renal insufficiency after carbenicillin at serum levels greater than 300 mug/ml . Normal coagulation factors (F . I, II, V, VII, VIII, X), normal PTT, normal platelet counts, negative ethanol gelation test (fibrin monomers) were found as well as a prolongation of thromboplastin time (Quick), thrombin time, reptilase time and thrombin coagulase time . Platelet function was disturbed . In addition, the plasmatic system was involved: inhibition of fibrinogen-fibrin conversion (Belitser assay) and enhanced antithrombin III activity; in vivo the latter was ascribed to a heparin-like activity . In vitro, abnormal III was seen: however an enhanced antithrombin III activity in vitro was not found with carbenicillin and various penicillin derivatives . This study demonstrates that carbenicillin, in addition to its known effect on platelet function, also disturbs the plasmatic coagulation system . This additional effect of carbenicillin is clinically important since protamin chloride effectively blocks bleeding without interfering with antibacterial activity . Both penicillin and penicillin derivatives have been shown to interfere with hemostasis and to cause clinically manifest hemorrhagic diathesis (Fleming and Fish 1947, Lurie et al . 1970a, b, McClure et al . 1970, Yudis et al . 1972, Demos 1971, Waisbren et al . 1971) . Carbenicillin interferes with ADP-, collagen- or thrombin-induced platelet aggregation and with the release reaction both in vivo (McClure et al . 1970, Cazenae et al . 1973) and in vitro (McClure et al . 1970, Cazenave et al . 1973) . In addition Lurie and colleagues (1970b) concluded that an inhibition of the conversion of fibrinogen to fibrin is involved although no experimental details were given . Later Brown and colleagues (1974) concluded that carbenicillin at usual dose levels "only affects the platelet component of hemostasis and has little effect on fibrin formation or other phases of coagulation in patients with normal renal function".

Am J Obstet Gynecol, 1976 Aug 1, 125(7), 906 - 10
Bacterial growth inhibition by amniotic fluid . VI . Evidence for a zinc-peptide antibacterial system; Schlievert PS et al.; The zinc bacterial inhibitory activity of amniotic fluid is dependent on the presence of a second, organic component contained in amniotic fluid . The second component is heat stable, resists proteolytic digestion, and is present in amniotic fluid throughout pregnancy . Further, the component may be a peptide with a molecular weight of less than 5,000 daltons . Phosphate reversal of amniotic fluid inhibitory activity may result from interference with the organic component rather than zinc.

Johns Hopkins Med J, 1976 Aug, 139(2), 51 - 9
Whipple's disease: demonstration by immunofluorescence of similar bacterial antigens in macrophages from three cases; Keren DF et al.; Although it is widely accepted that Whipple's disease is caused by microorganisms, there is little agreement as to the exact nature of those microbes . Several different types of bacteria have been reported from patients with Whipple's disease causing some workers to speculate that Whipple's disease may be due to a variety of microorganisms . Using an indirect immunofluorescence technique, we have demonstrated bacterial antigens in the granules of the foamy macrophages from three patients with Whipple's disease . The macrophages in each case stained with several types of antibacterial grouping sera . Jejunal biopsies from three normal subjects and one from a patient with celiac-like disease did not show significant reactions with any of the antisera . When these same antisera were reacted with homologous and heterologous bacteria, numerous cross-reactions were seen . However, each organism only reacted with certain antisera resulting in a distinctive pattern of reaction which could identify it . Therefore, if a different organism was present in each case of Whipple's disease, the antisera should give dissimilar reactions from case to case, but if the same type of microbe was present in each case, a similar pattern of reaction should be seen . In fact, the reactions were remarkably similar from case to case . These results suggest that a single, antigenically definable microorganism is present in the jejunal tissue of patients with Whipple's disease.

Vet Rec, 1976 Jul 24, 99(4), 61 - 4
The selection of antibiotics; Sanford J; The usefulness of an antibiotic depends not only upon its antibacterial potency and spectrum but also on the prevalence of resistant organisms and the extent and severity of the adverse reactions to which it may give rise . Variations in formulation of the same compound are reflected in differences in bioavailability . These may be intentional, as in the development of long-acting preparations, but may also be unexpected following differences in drug purity, content and gastro-intestinal absorption . Individual and species differences in treated animals also result in variations in bioavailability . The merits of combination products of two or more antibiotics are often equivocal and some combinations are definitely disadvantageous . Practical rules for the selection and use of antibiotics emphasise the need for full doses of effective compounds used for limited periods with monitoring of patterns of sensitivity so that problems of large-scale resistance can be avoided.

Arch Otorhinolaryngol, 1976 Jul 20, 212(3), 203 - 11
A clinical study on the ototoxic effects of tobramycin; Lehmann W et al.; In a clinical, prospective, non-randomized study, tobramycin has shown its high antibacterial activity in Gram-negative bacillary infections . The incidence of ototoxic side effects was very low: none of 18 patients studied before, at the end and 9 months after completion of tobramycin therapy showed any change in pure tone audiograms . Five of these 18 patients had renal impairment: 3 of them developed subjective and objective evidence of vestibular dysfunction, as demonstrated by caloric vestibulometry . However, these bilateral vestibular lesions all proved to be reversible a few weeks after cessation of therapy . Despite the low incidence and the reversibility of the ototoxic side effects, it seems advisable to monitor patients on long-duration tobramycin therapy for signs of vestibular dysfunction, particularly in cases of renal insufficiency.

Eur J Biochem, 1976 Jul 15, 66(3), 597 - 606
Paromomycin and dihydrostreptomycin binding to Escherichia coli ribosomes; Lando D et al.; Paromomycin binds specifically to a single type of binding site on the 70-S streptomycin-sensitive Escherichia coli ribosome . This site is different from that of dihydrostreptomycin since paromomycin binds to streptomycin-resistant ribosomes and sine dihydrostreptomycin does not compete for paromomycin binding . Paromomycin binding, unlike dihydrostreptomycin binding, is independent of changes in ribosome concentration but influenced by magnesium ion concentration . Moreover, paromomycin does not bind to the 30-S subunit of the streptomycin-sensitive ribosome, except in the presence of dihydrostreptomycin, which probably induces the conformational changes necessary for a paromomycin binding site . This induction does not occur with streptomycin-resistant ribosomes . Neither antibiotic binds to the 50-S subunit . In general, binding of the one antibiotic increases the number of sites available for binding of the other . Both antibiotics exhibit marked non-specific binding at high antibiotic/ribosome ratios . Competition studies have enabled the classification of other aminoglycosides according to their ability to compete for the paromomycin and dihydrostreptomycin binding sites . Derivatives structurally related to paromomycin compete for its binding, the degree of competition being related to antibacterial activity, but do not compete for dihydrostreptomycin binding; they, on the contrary, increase the number of dihydrostreptomycin binding sites . Neither gentamicin nor kanamycin derivatives, which induce a high level of misreading, nor kasugamycin and spectinomycin, which do not induce misreading, compete for paromomycin or dihydrostreptomycin binding sites . Other sites may be involved in the binding of these aminoglycosides and in inducing misreading.

Dtsch Zahnarztl Z, 1976 Jul, 31(7), 566 - 70
{Primary healing of intraoral bone defects under the effect of local and general antibacterial prophylaxis}; Handtmann S et al.; On the basis of 4,700 cases, experience is reported which has been gained over 15 years with a method developed in Tubingen for the primary filling of intraoral bone defects which are big and/or especially jeoplardized by infection . To find an optimum antibacterial prophylaxis for undisturbed primary healing, the operative removal of a lower wisdom tooth is used as an example to compare groups of cases in which either only local prophylaxis of additional general prophylaxis was applied . Comparison of the results with the findings of other authors shows that local implantation of antibacterial substances is superior to an exclusively antibiotic general therapy and that the best results may be expected by simultaneous implantation and general therapy . The findings also cast a light on the importance of exact technical skills in the treatment of wounds and on the considerable influence of the type of gelatine sponge on the stabilization of blood coagulation.

Ann Sclavo, 1976 Jul-Aug, 18(4), 590 - 600
{Experimental studies on the antibacterial activity of the association cephaloridine-dicloxacilline (author's transl)}; Ripa S et al.; A study on the efficiency of the association cephaloridine-dicloxacilline in the ratio 2:1 has been carried out . Both in vitro and in vivo the antibacterial activity shown by the association is higher than that merely additive of the single components and is due to positive interaction.

J Antibiot (Tokyo), 1976 Jul, 29(7), 692 - 5
Alborixin, a new antibiotic ionophore: taxonomy, isolation and biological properties; Delhomme C et al.; Alborixin is an ionophorous antibiotic of the nigericin group isolated from cultures of a strain of Streptomyces albus . It is active against Gram-postive bacteria and is coccidiostatic, but it is very toxic . The antibacterial principle was extracted with organic solvent from the mycelium, isolated in crystalline form and named alborixin.

HNO, 1976 Jul, 24(7), 242 - 4
{Experiences with polyethylene ventilation tubes in children with recurrent middle ear inflammation (author's transl)}; Kortekangas AE et al.; Middle-ear ventilation tubes (of the Sheehy modification) were placed in 401 ears of 209 children under 16 years of age as treatment for recurrent middle-ear infection . The same procedure was later required in 26% of the cases studied because of further recurrence of middle-ear infection . In four per cent of all patients studied, the ventilating tube failed to cure middle ear disease in spite of controlled concomitant antibacterial therapy . In these cases, an early extrusion of the tube was commonly found . Among all patients, the tube was spontaneously extruded in 76 per cent of the ears, whereas the intubation time was longer than half a year in 53 per cent of the cases . No complications from insertion of the ventilation tubes was seen in the present series of patients . The tympanic membrane was found to be normal in 71 per cent of all cases when follow-up examination was obtained three months after completion in intubation . However, a permanent tympanic membrane perforation was found in five ears (1% of patients) . The present study has confirmed the usefulness of middle-ear ventilation tubes, particularly in patients with recurrent middle-ear infections.

Antibiotiki, 1976 Jul, 21(7), 636 - 42
{Effect of the prolonged use of streptomycin as well as streptomycin in combination with tubazid on the bioelectrical activity of the brain in experimental tuberculosis}; Aksel'rod LB et al.; The effect of streptomycin used alone and in combination with tubazid on the brain electric activity was studied in chronic experiments on rabbits with tuberculosis . The electrocorticographical investigations showed that the antibacterial treatment lowered the spontaneous electric activity and reactive capacity of the cortex . It was evident from a narrow amplitude of the main rythm, coefficient and energy of synchronization on rythmic photostimulation and paroxysmal activity withing the theta range . With the account of the high therapeutic effect of the antibacterial treatment evident from minimum affection of the organs with tuberculosis, the above changes in the electrocorticogrammes should be attributed to the neurotropic effect of the drug and not to tuberculosis intoxication.

South Med J, 1976 Jul, 69(7), 902 - 4
Septic arthritis and Reiter's syndrome in sickle cell disorders: case reports and implications for management; Palmer DW et al.; Two patients with sickle cell disorders developed gram-negative septic arthritis and responded poorly to conventional managment . Unfavorable factors included (1) confusion with the nonseptic arthropathy of a sickle crisis; (2) impaired articular perfusion, perhaps related to local sickling; (3) conversion of an infecting organism to an L-form in the presence of cell-wall inhibitors; and (4) interference with cultures and antibacterial titrations of synovial fluid caused by intro-articular administration of antibiotics . Prolonged treatment with very high doses of antibiotics was required to eradicate infection in both patients . Because sickling and local hypoxia apparently interfere with defenses against infection, anemia should be corrected by transfusion . One patient had had Reiter's syndrome; the dysenteric form of this disease may be a cause of arthritis in some sicklemic patients.

J Am Dent Assoc, 1976 Jul, 93(1), 105 - 10
Long-term study of pulp capping in monkeys with three agents; McWalter GM et al.; The pulps of 40 permanent teeth of two monkeys were mechanically exposed and contaminated with adjacent saliva or plaque for 3 to 5 1/2 hours . The pulps were then capped with either Keflin (an antibiotic), Durelon (a polycarboxylate cement), or Dycal (a calcium hydroxide compound) . Varnish and then amalgam were inserted . Each monkey received at least one dose of Procion red H-8BS vital dye . The teeth were extracted from one monkey 23 months after capping and from the other monkey 29 months after capping . Serial, decalcified, 7 mum-thick paraffin sections were prepared . Alternate slides were stained with hematoxylin ane eosin . Unstained sections were examined for Procion labeling, and selected slides were stained by the Brown-Brenn method for bacteria . Of 13 teeth capped with Keflin, only 4 responded satisfactorily . All of the Dycal and Durelon-capped pulps were successful at both time intervals . All of the Dycal-capped pulps showed complete bridging and no inflammation or pulp obliteration . Bridging was complete in only three of the Durelon-capped pulps . The findings of this study support the findings in our previous study3 and further substantiate the effectiveness of Dycal as a pulp-capping agent . The often-repeated claim that calcium hydroxide compounds exert a persistent stimulating effect on the pulp resulting in its eventual obliteration was not supported . Durelon is not recommended for pulp capping since the material apparently lacks an antibacterial effect and does not stimulate reparative dentinogenesis at the exposure site . The low rate of satisfactory responses of pulps capped with Keflin, as used, precludes its use of pulp capping.

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