J Antibiot (Tokyo), 1984 Jul, 37(7), 706 - 11 A new antitumor antibiotic, kazusamycin; Umezawa I et al.; A new antibiotic kazusamycin, was isolated from the culture broth of Streptomyces sp . No . 81-484, which shows antitumor activity against experimental murine tumors . This antibiotic did not possess antibacterial activity against Gram-positive and Gram-negative bacteria, but showed strong cytotoxic activity against HeLa cells in vitro . The chemical and physico-chemical properties of kazusamycin suggest that the molecular formula of this antibiotic is C33H48O7 (MW 556). Mikrobiyol Bul, 1984 Jul, 18(3), 154 - 9 {Antibacterial effect of cefoperazone}; Ozbal Y et al.; Seven hundreds fifty three strains of pathogen microorganisms were investigated for in-vitro sensitivity of cefoperazone and of some other wide spectrum antibiotics . Cefoperazone has found to have very wide spectrum of inhibition against frequently isolated microorganisms from clinical specimens. Antibiotiki, 1984 Jul, 29(7), 510 - 2 {Mechanism of action of ectericide on opportunistic microbes}; Dikii IL et al.; Ectericide is a product of cod-liver oil oxidation (lower fatty acids, organic peroxides and aldehydes) . Its antibacterial activity is based on the capacity for partial disintegration and extraction of the structural lipopolysaccharide of the microbial cell without any significant effect on the quantitative content of the structural proteins and nucleotides. Ann Surg, 1984 Jul, 200(1), 29 - 39 Antibiotic trials in intra-abdominal infections . A critical evaluation of study design and outcome reporting; Solomkin JS et al.; The introduction of several new antibiotics, including cephalosporins and ureido-penicillins, has been a stimulus for clinical trials with these agents for intra-abdominal infection . Despite marked differences in antibacterial spectra, substantial differences in treatment results have not been documented . We reviewed published trials of antibiotic therapy for intra-abdominal infection to determine factors in study design that might impair identification of clinically important differences between regimens . Sixteen articles were identified that provided sufficient numbers of cases and data for analysis . Eight were prospective comparative trials, the remainder "single-armed" studies . The mortality rate was 3.5%, and the overall success rate was 84% for aminoglycoside plus clindamycin (range 52%-96%), 89% (range 83%-93%) for aminoglycoside plus metronidazole, and 93% (range 61%-95%) for cephalosporin-based regimens . Several defects in study design were identified . (1) Exclusionary criteria employed generally prevented enrollment of seriously ill patients or infections associated with high failure rates: Patients were excluded if even mild renal impairment was present or if antibiotic therapy had been recently administered, thereby excluding patients with postoperative or recurrent infections . Several studies allowed entry of contaminated but not infected patients . (2) Criteria used for reporting infectious diagnosis, premorbid health status, severity of infection, and outcome were nonuniform, and few studies provided such information . (3) Despite the small number of treatment failures, data reported did not allow determination of the basis for failure . For example, only four studies provided information on the operations performed upon treatment failures . Whether treatment failures were due to inadequate antibiotic therapy could therefore not be determined . Enrollment of a variety of low mortality infections precluded demonstration of any differences in regimens . Use of stratified randomization, stratifying for site of infection and severity of infection, and inclusion of greater numbers of patients would increase the likelihood of identifying differences between regimens . Such study design would likely require a multicenter trial to enroll sufficient numbers of cases for statistical analysis. Ann Intern Med, 1984 Jul, 101(1), 92 - 104 The neurotoxicity of antibacterial agents; Snavely SR et al.; Commonly used antibacterial agents may be associated with various neurotoxic reactions . Central nervous system toxicities include seizure disorders, encephalopathy, bulging fontanelles, and neuropsychiatric symptoms . These abnormalities have been associated with the use of the penicillins, cephalosporins, sulfonamides, tetracyclines, chloramphenicol, colistin, aminoglycosides, metronidazole, isoniazid, rifampin, ethionamide, cycloserine, and dapsone . Cranial nerve toxicities, such as myopia, optic neuritis, deafness, vertigo, and tinnitus, have been associated with the use of erythromycin, sulfonamides, tetracyclines, chloramphenicol, colistin, aminoglycosides, vancomycin, isoniazid, and ethambutol . Peripheral nerve symptoms consisting of paresthesias, motor weakness, or sensory impairment have been associated with the use of the penicillins, sulfonamides, chloramphenicol, colistin, metronidazole, isoniazid, ethionamide, and dapsone . Neuromuscular blockade has been associated with the use of the tetracyclines, polymyxins, lincomycin, clindamycin, and aminoglycosides . Management generally consists of supportive therapy and immediate discontinuation of therapy with the offending drug. ASDC J Dent Child, 1984 Jul-Aug, 51(4), 274 - 6 Desensitization of dentin by resin impregnation: a clinical and light-microscopic investigation; Nordenvall KJ et al.; Desensitization of dentin by resin impregnation and the pulpal effect of impregnation procedures were studied in fifty-one pairs of contralateral exposures located on cuspal tips of young premolars . One surface in each pair was impregnated . Pretreatment consisted of etching, antibacterial cleaning and desiccation . Concise Enamel Bond was used for impregnation . Excess was removed or reduced before polymerization . The sensitivity to probing and compressed air was tested after seven to eighteen days . The impregnated surface was less sensitive than the untreated one in forty-one pairs . No difference was reported by nine patients . Twenty-nine impregnated and three untreated surfaces were insensitive to testing . In most histologically examined teeth, impregnated or not, a local, slight inflammation was seen in the pulp horn . Microorganisms usually penetrated some dentinal tubules . Resin impregnation as applied in the present study could reduce or eliminate the sensitivity of exposed dentin, but did not prevent infectious irritation of the pulp. Schweiz Med Wochenschr, 1984 Jun 23, 114(25), 932 - 4 {Efficacy of the immunostimulant Broncho-Vaxom}; Ahrens J et al.; In a 6-month placebo-controlled double-blind multicenter study in 230 patients with recurrent respiratory tract infections, the therapeutic efficacy of Broncho-Vaxom was demonstrated by comparing infection incidence and severity as well as antibacterial medication . Investigators and patients agreed that Broncho-Vaxom exerts a significantly greater protective effect than placebo . Reports of side effects were more frequent with placebo as compared to Broncho-Vaxom. Handchir Mikrochir Plast Chir, 1984 Jun, 16(2), 135 - 8 {Hidradenitis suppurativa--treatment with myocutaneous island flap or the traditional method}; Gorkisch K et al.; Inflammations of the apocrine sweat glands are characterized by painful, nodose and often superficially phlogistic infiltrates with a tendency towards abscess-formation and fistulation . These foci of inflammation are situated particularly in the armpit as well as the anal and genital region . The failure of conservative therapy--e.g., application of antibacterial ointments, red light, short-wave therapy or irradiation--is followed by a surgical intervention which involves excising the abscess cavity and leaving the wound open for secondary closure by granulation . The resultant scar is an impairment both functionally and cosmetically, particularly in the axilla; and, in many cases, a new focus of inflammation eventually develops in the immediate vicinity . For multiple occurrence of sudoriparous abscesses in the axilla with undermining of the surrounding cutaneous soft tissue mantle and fistulation, we therefore suggest the following therapeutic concept as an alternative to conventional methods: radical removal of the focus of inflammation far into the healthy tissue with concomitant excision of all sweat glands in the affected area and coverage of the resultant defect with a partial myocutaneous island flap from the latissimus dorsi muscle. Antimicrob Agents Chemother, 1984 Jun, 25(6), 735 - 41 Antibiotic action on phagocytosed bacteria measured by a new method for determining viable bacteria; Vosbeck K et al.; Antibiotics such as rifampin that act on phagocytosed bacteria have clinical advantages . The investigation of such intraphagocytic activity of antibiotics is, however, hampered by the time-consuming and cumbersome procedures necessary for enumerating viable bacteria . We have developed a semiautomatic biophotometric method for this purpose that permits the processing of relatively large numbers of samples . Using this method with Staphyloccus aureus Wood 46 as a test organism, we studied the dose dependence of the activities of a number of antibiotics against intraphagocytic bacteria . We could confirm the very good intracellular activity of rifampin . Its activity at low concentrations was slightly better against intracellular than against extracellular bacteria . In contrast, clindamycin and erythromycin, both of which have been reported to accumulate within phagocytes, did not exhibit a correspondingly enhanced intracellular activity, erythromycin being active intracellularly only at high concentrations . Clindamycin and vancomycin were effective against intracellular organisms, but only at relatively high concentrations owing to their low bactericidal activity against S . aureus Wood 46 . Penicillin G, ampicillin, gentamicin, and streptomycin exhibited no useful intracellular activity . These results demonstrate that radioactive accumulation studies of antibacterial agents are not sufficient to show intracellular activity . Intracellular activity must be demonstrated in a functional test, preferably with graded concentrations of the test substance. Am J Vet Res, 1984 Jun, 45(6), 1148 - 50 Serum erythromycin concentration in sheep fed two diets; Wilson RC et al.; Serum erythromycin concentrations following a single IV injection (12.5 mg/kg) were compared in 6 sheep during feeding of a grass hay diet and a concentrate diet . The concentrate diet resulted in a mean decrease of at least 1 pH unit in forestomach fluid, but did not significantly alter either the serum drug concentrations or half-life . Variable antibacterial activity was present in forestomach fluid as early as 1 or 2 hours after injection . This study indicates that ion-trapping in forestomach fluid as a result of normal dietary changes does not require therapeutic dosage adjustment. Pathol Biol (Paris), 1984 Jun, 32(5 Pt 2), 516 - 9 {Pefloxacine: diffusion into bronchial mucus}; Morel C et al.; Pefloxacin is a new quinolone with significant in vitro antibacterial activity and a broad spectrum . It was included in an extensive study of antibiotic diffusion into bronchial mucus . Pefloxacin was given to 35 patients divided into five groups according to the timing of sputum sampling . Plasma specimens were taken simultaneously . Pefloxacin was measured by microbiological assay . Mean pefloxacin concentrations in bronchial mucus was high, exceeding 5 mg/l . Concentrations on the first and third days were similar . The ratio of mucus concentrations to plasma concentrations was high in each case, around or often above 1 . These findings show that diffusion of pefloxacin into bronchial mucus is outstanding. Vestn Khir Im I I Grek, 1984 Jun, 132(6), 51 - 5 {Surgical treatment of tuberculosis of non-pulmonary localization}; Petrov IN et al.; Experiments in 86 rabbits and observation of 360 patients have shown the antibacterial therapy to be of limited use for the treatment of non-pulmonary tuberculosis . It was found that the antibacterial therapy failed to result in healing the caseous-destructive foci and to cure turebculosis of kidneys, bones, joints, female genitals and lymph nodes . It is considered to be a reason for surgical procedures according to principles of the focal surgery on non-pulmonary tuberculosis elaborated by P . G . Kornev and his school. Can J Microbiol, 1984 Jun, 30(6), 730 - 8 Directed biosynthesis of novel derivatives of echinomycin . II . Purification and structure elucidation; Gauvreau D et al.; New antibiotics produced by Streptomyces echinatus A8331 cultured in the presence of heterocyclic aromatic acids can be separated and purified by high-performance liquid chromatography using reversed phase columns . Natural quinoxaline antibiotics and certain quinoline derivatives can also be efficiently separated in normal phase systems . Details of purification procedures are described together with experiments to characterise the new antibiotics by field desorption mass spectrometry and proton magnetic resonance . Mono- and bis-substituted derivatives of echinomycin containing the following replacement chromophores have been isolated: 7-chloroquinoxaline-2-carbonyl, thieno{3,2-b}pyridine-5-carbonyl, and 6-methylquinoline-2-carbonyl . With a 6-methylquinoline-2-carboxylic acid precursor the analogues containing one or two replacement chromophores are each separable into two distinct components . One of the bis-substituted 6-methylquinoline products appears inactive in an antibacterial assay and behaves as a triostin analogue, presumably an immediate precursor of the corresponding echinomycin derivative. Acta Pathol Microbiol Immunol Scand {B}, 1984 Jun, 92(3), 181 - 2 Septicaemia in granulocytopenic patients caused by multiresistant diphtheroid rods . A study of two cases; Dibb WL et al.; Two cases of septicaemia in granulocytopenic patients are reported . Both were caused by multiresistant aerobic (JK-group) diphtheroid rods . The bacterial isolates were resistant to all commonly used antibacterial agents but showed good sensitivity to vancomycin and rifampicin . These agents should be included in the routine sensitivity testing of such isolates and diphtheroids should always be reported by the routine laboratory for granulocytopenic patients. Vestn Khir Im I I Grek, 1984 Jun, 132(6), 10 - 4 {Elimination of a stable residual pleural cavity with an antibacterial fibrin filling}; Chepcheruk GS et al.; A simple, effective and safe method is proposed to liquidate a persistent residual pleural cavity by a biological filling prepared ex tempore from a solution of fibrinogen with antibacterial drugs . The method was used in 24 patients after pleura empyema . The method of filling is described as well as the conditions for a successful use of the new means of liquidation of the residual pleural cavity and prevention of recurrent pleura empyemas. Pathol Biol (Paris), 1984 Jun, 32(5 Pt 2), 570 - 2 {Pharmacokinetics and antibacterial activity of ticarcillin in 11 patients with cystic fibrosis}; de Meirleire F et al.; We studied the pharmacokinetics of ticarcillin in cystic fibrosis patients . Concentrations of ticarcillin were assayed in serum and sputum samples from 11 children . We found that antibiotic serum concentrations were consistent with those reported in the literature . Ticarcillin half-life was shorter in patients than in controls . No direct correlation was found between concentrations in serum and those in sputum . Among six children with P . aeruginosa infection, ticarcillin levels in sputum were sufficient to eliminate P . aeruginosa in 50% of cases. J Antibiot (Tokyo), 1984 Jun, 37(6), 627 - 34 Semisynthesis of A23187 (calcimycin) analogs . II . Introduction of a methyl group on the benzoxazole ring; Prudhomme M et al.; Semisynthesis of two demethylamino A23187 with a methyl group in the 4- or 5-position on the benzene ring were carried out via the cleavage of A23187 oxazole ring and rebuilding of modified benzoxazoles . These compounds were shown to release Ca++ and MG++ from mitochondria and to keep part the antibacterial activity of the natural metabolite. J Med Chem, 1984 Jun, 27(6), 717 - 26 Inhibition of arabinose 5-phosphate isomerase . An approach to the inhibition of bacterial lipopolysaccharide biosynthesis; Bigham EC et al.; Arabinose 5-phosphate ( A5P ) isomerase is a key enzyme in the biosynthesis of lipopolysaccharide, an essential component of the outer membrane of Gram-negative bacteria . The mechanism of the isomerase is envisioned to involve an enediol intermediate . A series of compounds, which are analogues of the substrates or intermediate, were tested as inhibitors of A5P isomerase with the belief that a good inhibitor would stop bacterial growth or render the cells more susceptible to other antibiotics or natural defenses . In a series of phosphorylated sugars, the order of isomerase inhibitory activity was as follows: aldonic acids greater than alditols greater than aldoses . Nonphosphorylated sugars were much less inhibitory . The best inhibitor was erythronic acid 4-phosphate (54), which had Km/Ki = 29 . None of the compounds displayed antibacterial activity in vitro. J Pharm Sci, 1984 Jun, 73(6), 803 - 8 Some effects of 1-(2,4-Dichlorophenyl)-4-dimethylamino-methyl-1-nonen-3-one hydrochloride on Escherichia coli GK-19; Khachatourians GG et al.; 1-(2,4-Dichlorophenyl)-4-dimethylaminomethyl-1-nonen-3-one hydrochloride (Id) was shown to inhibit the growth of Escherichia coli GK-19 at a concentration of 50 micrograms/mL in a medium of pH 6.5 . Maximal antibacterial activity was found during the logarithmic growth phases rather than at the early stationary phase . Electron microscopy revealed that Id caused lysis, and inhibition of respiration and retardation of RNA and protein syntheses occurred in the bacteria with this compound at 50 micrograms/mL. Pathol Biol (Paris), 1984 May, 32(5), 381 - 3 {Antibiotic sensitivity of strains of Brucella}; Shir Y et al.; The susceptibility of 31 strains of Brucella to various antibiotics was investigated by agar dilution technique . When tested with inocula ranging from 10(4) to 10(6) bacteria/ml, all strains were susceptible to tetracycline, chloramphenicol, streptomycin and gentamicin . More than 25% were resistant to the combination trimethoprim-sulfamethoxazole . With this combination, the maximal antibacterial effect was obtained at a trimethoprim/sulfamethoxazole ratio of 1:19 . In 90% of the strains, stable mutants, highly resistant to rifampicin (CMI greater than or equal to 1024 micrograms/ml) were detected . The mutation rate was about 10-7. Mod Vet Pract, 1984 May, 65(5), A19 - 22 Transtracheal aspiration in the horse: a photo essay; Krpan MK; Transtracheal aspiration is used to obtain samples for culture and cytologic examination of respiratory tract secretions and exudates . A 15-cm-long area of the ventral midcervical region is surgically prepared, a small site infiltrated SC with 2-3 ml lidocaine, and a stab incision made in the skin . A trocar with cannula is inserted through the incision and annular ligament into the trachea and the trocar removed . An 8-Fr polypropylene catheter is inserted about 35-40 cm down the trachea and attached to a 30-ml syringe, containing 20 ml sterile saline, with a 3-way stopcock . The saline is rapidly injected and a 3- to 4-ml sample is aspirated after the horse coughs and as the catheter is slowly withdrawn . The catheter and cannula are withdrawn, the area covered with antibacterial ointment and gauze sponges, and elastic tape applied . Complications are rare but include SC emphysema or infection, pneumomediastinum and cartilage ring damage. Arch Surg, 1984 May, 119(5), 601 - 5 Improved treatment of the Stevens-Johnson syndrome; Marvin JA et al.; The Stevens-Johnson syndrome (SJS), a disease resulting in greater than 30% body surface area epidermal and mucosal desquamation, is reported to have a mortality of greater than 50% . Recommended treatment has included steroids, prophylactic antibiotics, nutritional support, and application of topical antibacterials . Since the lesions represent only epidermal loss without dermal necrosis, rapid reepithelialization should occur if the dermis is protected from desiccation with a biological dressing . Five nonburned patients with severe SJS were treated in the University of Washington burn center, Seattle, with urgent operative debridement of their wounds and application of porcine xenograft immediately after admission . Steroid administration was stopped . Antibiotics were used only for culture-proved infections . All patients completely re-epithelialized within a mean of 18 days . There was one death, a 9-year-old boy who was completely re-epithelialized when sudden fatal sepsis that originated from a ventriculovenous shunt placed when he was an infant developed . In this group of patients, rapid wound closure with xenograft and supportive care permitted rapid reepithelialization and decreased mortality and morbidity. Surg Gynecol Obstet, 1984 May, 158(5), 431 - 6 The most indolent ulcers of the skin treated with porcine xenografts and silver ions; Ersek RA et al.; Cutaneous ulcers associated with Hansen's disease have long been recognized as among the most indolent of all ulcers . We have successfully treated such ulcers with porcine xenograft, achieving healing in ulcers which had been present for as much as three decades . These results suggest that this regimen may be applicable to other cutaneous ulcers wherever skin is missing . The newly available antibacterial effects of silver-impregnated porcine xenografts should have the result of increasing the effectiveness of the treatment still further. J Antimicrob Chemother, 1984 May, 13(5), 423 - 7 In-vitro antibacterial activity of Sch 25393, a fluorinated analogue of thiamphenicol; Marca G et al.; The in-vitro antibacterial activity of a fluorinated analogue of thiamphenicol, Sch 25393, has been evaluated in comparison with chloramphenicol and thiamphenicol . The substitution of an hydroxyl group at position 3 and of two atoms of chlorine with fluorine in the acyl side-chain improves remarkably the antibacterial activity of the compound against strains resistant to chloramphenicol and thiamphenicol because of the production of acetyltransferases, but not against strains resistant because of non-enzymatic mechanisms of resistance . Although itself resistant to the enzymatic inactivation, Sch 25393 is unable to inhibit the acetylation of chloramphenicol and thiamphenicol. Diabetes Care, 1984 May-Jun, 7 Suppl 1, 3 - 7 Sulfonylureas: background and development of the field; Levine R; This paper traces the growth of the field from the incidental finding of the hypoglycemic "side effect" of certain antibacterial sulfonamides and sulfonylureas (1942), to the establishment of islet beta cell stimulation and insulin release as a major mechanism of action of these drugs (1946), to the more recent findings that additional effects exist on the level of cell metabolism and its regulation by hormones . These changing concepts of mechanism have influenced the clinical uses of these drugs. Mutat Res, 1984 May, 133(3), 199 - 244 Testing of chemicals for genetic activity with Saccharomyces cerevisiae: a report of the U.S . Environmental Protection Agency Gene-Tox Program; Zimmermann FK et al.; The yeast Saccharomyces cerevisiae is a unicellular fungus that can be cultured as a stable haploid or a stable diploid . Diploid cultures can be induced to undergo meiosis in a synchronous fashion under well-defined conditions . Consequently, yeasts can be used to study genetic effects both in mitotic and in meiotic cells . Haploid strains have been used to study the induction of point mutations . In addition to point mutation induction, diploid strains have been used for studying mitotic recombination, which is the expression of the cellular repair activities induced by inflicted damage . Chromosomal malsegregation in mitotic and meiotic cells can also be studied in appropriately marked strains . Yeast has a considerable potential for endogenous activation, provided the tests are performed with appropriate cells . Exogenous activation has been achieved with S9 rodent liver in test tubes as well as in the host-mediated assay, where cells are injected into rodents . Yeast cells can be recovered from various organs and tested for induced genetic effects . The most commonly used genetic end point has been mitotic recombination either as mitotic crossing-over or mitotic gene conversion . A number of different strains are used by different authors . This also applies to haploid strains used for monitoring induction of point mutations . Mitotic chromosome malsegregation has been studied mainly with strain D6 and meiotic malsegregation with strain DIS13 . Data were available on tests with 492 chemicals, of which 249 were positive, as reported in 173 articles or reports . The genetic test/carcinogenicity accuracy was 0.74, based on the carcinogen listing established in the Gene-Tox Program . The yeast tests supplement the bacterial tests for detecting agents that act via radical formation, antibacterial drugs, and other chemicals interfering with chromosome segregation and recombination processes. J Antimicrob Chemother, 1984 May, 13 Suppl B, 9 - 23 Investigations into the mechanism of action of the antibacterial agent norfloxacin; Crumplin GC et al.; Examination of the mechanism of action of norfloxacin upon susceptible strains of Escherichia coli K12 has shown that the drug exerts a potent bactericidal effect resulting from the inhibition of the A subunit of the essential enzyme DNA gyrase . It is also shown that the use of norfloxacin can reduce the total number of bacteria at the site of an infection as well as having significant effects upon the metabolism of treated cells in the interim period between the loss of viability and cell-lysis . These effects may provide a clue to a previously unsuspected mechanism of providing symptomatic relief which functions in parallel with the elimination of viable pathogenic bacteria. Antibiotiki, 1984 Apr, 29(4), 291 - 5 {Antibacterial therapy of peritonitis}; Tsatsanidi KN et al.; The microbiological assay of the exudate provided isolation of anaerobic pathogens in 48 (64 per cent) out of 75 patients with peritonitis . All the patients were subjected to antibacterial therapy with antibiotics and chemotherapeutic drugs active against aerobic and anaerobic pathogens. Antimicrob Agents Chemother, 1984 Apr, 25(4), 458 - 62 Disposition of phosphomycin in patients with pleural effusion; Lastra CF et al.; The pharmacokinetics of phosphomycin were studied in seven patients with pleural effusion of varied etiologies . All patients received a single intravenous bolus of 30 mg of antibiotic per kg . Phosphomycin levels in plasma and pleural fluid were determined simultaneously . Antibiotic levels in plasma followed a two-compartment open kinetic model . In the pleural fluid, maximum concentrations of phosphomycin, 42.63 +/- 16.03 micrograms/ml (mean +/- standard deviation), were reached at 3.69 +/- 1.08 h after administration of the antibiotic . The disappearance constant of the antibiotic from the pleural fluid was significantly smaller (0.16 +/- 0.06 h-1) than the elimination constant determined from the levels of drug in plasma (0.73 +/- 0.26 h-1) . Phosphomycin persisted in antibacterial concentrations in the pleural fluid for a considerable period of time . The low accessibility of phosphomycin observed in one of the patients in the study, with a maximum concentration value of 2.16 micrograms of phosphomycin per ml of pleural fluid, could be due to the existence of pachypleuritis in that patient; this was later confirmed in clinical and histological studies done after the research described here. Farmaco {Sci}, 1984 Apr, 39(4), 305 - 15 {Derivatives of lithocholic acid with antibacterial and antifungal activity . IV}; Bellini AM et al.; A series of N-substituted amides of litocholic acid and some N-substituted derivatives of 3 alpha-hydroxy-24-amino-5 beta- cholane were prepared and their in vitro antibacterial and antifungal activity determined against a variety of gram-positive and gram-negative strains and two kinds of mycetes . Some of the tested compounds showed an interesting activity against gram-positive strains and mycetes . Scand J Dent Res, 1984 Apr, 92(2), 161 - 4 In vivo antibacterial effect of tin on the oral microflora; Attramadal A et al.; The antibacterial effect of oral rinses with stannous fluoride and stannous chloride solutions, and of the use of a toothpaste containing stannous fluoride and stannous pyrophosphate was tested by recording the bacterial viable counts on the oral mucous membrane . Stannous chloride had no antibacterial effect, while stannous fluoride drastically reduced the viable counts up to 4 h . Calculations demonstrated that 25% of the tin content in 10 ml rinsing solutions was retained in the mouth, and analyses showed a raised tin level in saliva up to 4 h after rinsing or toothbrushing . It is suggested that most of the retained tin is bound to the oral mucosa. Scand J Dent Res, 1984 Apr, 92(2), 109 - 19 Antibacterial properties of human lysozyme toward Fusobacterium nucleatum Fev1; Vasstrand EN et al.; Human lysozyme in physiologic concentrations (17-50 micrograms/ml) had apparently no effects on growth rate and viability of exponentially growing Fusobacterium nucleatum Fev1 cells, but cells in the stationary phase were affected . When grown in the presence of active lysozyme about 70% of the cells in late exponential phase (24-h culture) were able to form colonies, compared to about 100% in the control culture . About 24 h later the colony forming abilities were about 5% and 20%, respectively . Addition of lysozyme to suspensions of cells taken from any growth phase did not lead to any significant decrease in turbidity, that is, no more than 10% decrease at 650 nm . Control cells treated with acridine orange fluoresced with a uniform bright orange color, while the lysozyme treated stationary phase cells fluoresced more faintly . Intracellular granules were more preponderant in the latter cells . When incubated with the hydrophobic probe 8-anilinonaphthalene-1-sulfonic acid (ANS), lysozyme exposed cells gave approximately 20% higher fluorescence intensity than the control cells . Changes in the ultrastructure of the lysozyme treated cells were best studied in the transmission electron microscope using ultrathin sectioned preparations . The peptidoglycan layer became disorganized and apparently dissolved and the ordered structure of the cell wall had disappeared in zones . The cells, however, still retained their form, and only a few per cent had lost their cellular content . This explains why the turbidity of the solution did not change significantly. Vestn Khir Im I I Grek, 1984 Apr, 132(4), 14 - 9 {Local hemostasis in surgical practice}; Asoian GA et al.; Results of experimental and clinical investigations of a new local highly effective hemostatic drug " Gelplastan " are presented . Gelplastan was found to increase blood coagulation, to have strong adhesive and prolonged antibacterial properties . It is well resolved in the tissues, is biologically intact, has no side effects. Br J Obstet Gynaecol, 1984 Apr, 91(4), 342 - 8 Antibacterial activity in human amniotic fluid: relationship to zinc and phosphate; Scane TM et al.; Antibacterial activity, tested with B . subtilis, was present in all 44 human amniotic fluids at between 36 and 42 weeks of pregnancy and was unrelated to gestational age within these limits, or to maternal age or parity . High-molecular-weight (beta-lysin) activity, present in all samples, was directly related to concentration of bound zinc, but not to that of free zinc . Low-molecular-weight antibacterial activity (less than 1000 Daltons) was only present in nine specimens, but sub-threshold concentrations were demonstrable by concentrating the ultrafiltrates in more than half of the remaining specimens . Low-molecular-weight activity in the ultrafiltrates was directly related to the concentration of bound zinc in the original amniotic fluid . Neither high- nor low-molecular-weight antibacterial activities were associated with amniotic fluid phosphate levels. Antibiotiki, 1984 Apr, 29(4), 295 - 9 {Antibacterial therapy of cholecystocholangitis in viral hepatitis}; Andreichin MA et al.; The chemotherapy of cholecystocholangitis in patients with virus hepatitis was estimated . Antibiotics, furagin and pathogenetic drugs were used for the treatment . The antibiotics were chosen with regard to their sensitivity to the bile microflora . This resulted in sanation of the bile ducts . Furagin was less effective . The use of the pathogenetic drugs alone was ineffective in the majority of patients. Antibiotiki, 1984 Apr, 29(4), 286 - 91 {Intralymphatic administration of antibiotics in the complex treatment of suppurative complications in patients with neurosurgical pathology}; Shcherbakova EG et al.; The efficacy of endolymphatic route of gentamicin and ceporin administration was studied in 89 patients with neurosurgical pathological processes complicated by acute pneumonia (80 patients) and meningoencephalitis (9 patients) usually after ineffective antibiotic therapy according to the routine methods . The antibiotics were used in accordance with the antibiograms of the causative agents isolated from the bronchial tree or CSF . The endolymphatic use of gentamicin or ceporin once a day in doses of 80 mg or 1 g respectively provided rapid sanation and arresting of the inflammatory foci, lowering of the intoxication level, more rapid promotion of the positive time course of the clinico-roentgenological and laboratory indices and decreasing of the recovery periods by 1.5-2 times in 86 per cent of the patients with pneumonia . The endolymphatic administration of gentamicin in a dose of 80 mg twice a day or ceporin in a dose of 1 g twice a day allowed one to maintain the antibiotic therapeutic levels in the cerebrospinal fluid and to obtain satisfactory clinical results in the combined treatment of meningoencephalitis . The endolymphatic administration of the drugs was well tolerated by the patients and no adverse reactions were observed . This route of administration of antibiotics and in particular broad spectrum antibiotics may be recommended for urgent antibacterial therapy of especially severe neurosurgical patients with pyo-inflammatory complications and patients who did not respond to the routine antibiotic therapy. Minerva Med, 1984 Mar 10, 75(9-10), 457 - 62 {Use of high-dose lysozyme in the treatment of herpes zoster and flat warts}; Cavicchini S; Lysozyme is a natural enzyme with antiviral, antibacterial and immunomodulating+ action . This drug has several dermatological applications particularly in the therapy of some viral skin diseases as herpes zoster, viral warts and aphthous stomatitis . In this work the Author has valued the efficacy of high dosage lysozyme in the treatment of 30 patients with herpes zoster infection and in 10 patients affected with viral plane warts . The good results obtained in this clinical trial confirm those reported in previous papers and denote the usefulness of this therapy. Am J Med, 1984 Mar, 76(3), 450 - 7 Can antibacterial therapy be discontinued in persistently febrile granulocytopenic cancer patients? Joshi JH, Schimpff SC, Tenney JH, Newman KA, de Jongh CA. It has been suggested that empiric broad-spectrum antibiotics, instituted for fever in the presence of granulocytopenia, should continue to be administered, even when infection is not demonstrable, to those patients who remain persistently febrile and granulocytopenic . Therefore, the consequences of discontinuing antibiotics when the presence of infection is doubted in this setting were evaluated . In 16 (3.7 percent) of 429 episodes of fever and granulocytopenia for which empiric antibiotic therapy was instituted, after approximately four days, persistence of both fever and granulocytopenia was found, and yet infection was prospectively classified at that time as "doubtful." The initial empiric antibiotic regimen was therefore discontinued after a mean of 4.8 (median 5.0) days . Discontinuation of antibiotics proved appropriate for half of the patients; eight patients received no systemic therapeutic antibiotics with no evidence of infection during a period of at least two weeks . The other eight patients had antibacterial antibiotics reinstituted within a mean of 2.4 days; six infections were subsequently demonstrable . Six of these eight patients also required or were believed to require antifungal therapy with intravenous amphotericin B for presumed fungal infections . Patients with relapsed leukemia or lymphoma and those with a likelihood of continued profound granulocytopenia (counts below 100/microliters) or both were the ones who tended to require reinstitution of antibiotics . Discontinuation of antibiotics when infection was considered doubtful despite persistence of both fever and granulocytopenia was, therefore, successful in eight of 16 patients . Reinstitution of antibiotics was required in the eight remaining patients . No definite rule appears to be applicable to all patients. Mol Pharmacol, 1984 Mar, 25(2), 281 - 6 Nuclear magnetic resonance studies on the interaction of avoparcin with model receptors of bacterial cell walls; Fesik SW et al.; On the basis of nuclear Overhauser enhancement and 1H chemical shift data obtained in aqueous solution, a model is proposed for the interaction of beta-avoparcin and epi-beta-avoparcin with acetyl-D-alanyl-D-alanine (Ac-D-Ala-D-Ala) and diacetyl-L-lysyl-D-alanyl-D-alanine (Ac2-L-Lys-D-Ala-D-Ala) . For the beta-avoparcin: Ac2-L-Lys-D-Ala-Ala complex, the COOH-terminal end of the tripeptide is located near the NH2 terminus of the antibiotic with the tripeptide extending across the peptide backbone of beta-avoparcin toward its COOH-terminal end . In our proposed structure, the three amino acid residues of the peptide span the entire length of the antibiotic, and the aliphatic side chain of the lysine residue extends over the D-ring of beta-avoparcin . The structure of the epi-beta-avoparcin:Ac2-L-Lys-D-Ala-D-Ala complex was found to be similar to the beta-avoparcin complex at the binding site for the lysine residue at the COOH-terminal end of the antibiotic, but differed in the interactions at the NH2 terminus . These results are consistent with the similarities in the COOH-terminal conformations and the differences in conformations at the NH2 terminus found for beta-avoparcin and epi-beta-avoparcin which were described in the preceding paper {Fesik, S . W., I . M . Armitage, G . A . Ellestad, and W . J . McGahren, Mol . Pharmacol . 25:275-280 (1984)} . The association constants (measured by UV methods) for both beta-avoparcin:peptide complexes were greater than those measured for epi-beta-avoparcin and correlated with their differences in antibacterial activity . Epi-beta-avoparcin exhibited no measurable binding to the dipeptide: however, a significant affinity was measured for the tripeptide, indicating that the interactions with the NH2 terminus of the antibiotics provide binding energy for the antibiotic peptide complex but that the COOH-terminal end of the antibiotics also plays an important role in the binding interaction . These results are interesting in light of the similarities in the structural and conformational features at the COOH terminus for all of the glycopeptide antibiotics. Mol Pharmacol, 1984 Mar, 25(2), 275 - 80 Nuclear magnetic resonance studies on the antibiotic avoparcin, Conformational properties in relation to antibacterial activity; Fesik SW et al.; Avoparcin is a commercially important glycopeptide antibiotic which is active against Gram-positive bacteria . Recently, beta-avoparcin, the major component of the avoparcin mixture, and several other analogues have been structurally characterized and tested for their antibacterial activity . Varying degrees of activity were observed for only minor structural differences . For example, beta-avoparcin and epi-beta-avoparcin, which differ only in the stereochemistry at position 1' of the NH2-terminal phenylsarcosine subunit, exhibit a 10- to 100-fold difference in antibacterial activity . Following the supposition that the conformational properties of these molecules may explain the differences in their antibacterial activity, we have analyzed the conformations of beta-avoparcin, epi-beta-avoparcin, and other avoparcin analogues in aqueous solutions using NMR methods . On the basis of an analysis of the 1H chemical shifts, 1H-1H nuclear Overhauser enhancement data, and pH titration experiments, it was concluded that the conformations of all of the analogues are similar at the COOH terminus . However, for beta-avoparcin and epi-beta-avoparcin, conformational differences were observed in the NH2-terminal region of the molecules . In this paper, we present a detailed description of the over-all conformations of these two glycopeptides as deduced from an in-depth analysis of their corresponding 1H NMR spectra and discuss the possible relationships this may have with their markedly different antibacterial activities. J Antibiot (Tokyo), 1984 Mar, 37(3), 191 - 9 Chicamycin, a new antitumor antibiotic . I . Production, isolation and properties; Konishi M et al.; Chicamycin is a new antitumor antibiotic produced by a strain of Streptomyces albus, No . J576 -99 . The antibiotic is extractable into organic solvents from the fermentation broth and is obtained in two active forms, chicamycins A and B, depending upon the isolation procedure used . Chicamycin A is not a natural antibiotic but the methanol adduct of naturally produced chicamycin B . Both forms of the antibiotic have weak antibacterial activity against some Gram-positive and acid-fast bacteria . They inhibit the growth of experimental tumors such as P388 mouse leukemia. J Med Chem, 1984 Mar, 27(3), 292 - 301 Pyridonecarboxylic acids as antibacterial agents . 2 . Synthesis and structure-activity relationships of 1,6,7-trisubstituted 1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acids, including enoxacin, a new antibacterial agent; Matsumoto J et al.; The title compounds having nitro, amino, cyano, chloro, or fluoro as the C-6 substituent were prepared . Introduction of the chloro and cyano groups at C-6 was accomplished by the Sandmeyer reaction of 6-amino-1,8-naphthyridine derivatives 9 via their 6-diazonium salts . The reaction was extended to the synthesis of the 6-fluoro analogues, involving the Balz-Schiemann reaction of the diazonium tetrafluoroborate . Furthermore, a series of the 1-ethyl, 1-vinyl, 1-(2-fluoroethyl), and 1-(difluoromethyl) analogues of 7-substituted 6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acids was prepared . 1-Pyrrolidinyl and, particularly, N-substituted or unsubstituted 1-piperazinyl groups were introduced as the C-7 variants . As a result of this study, 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-1, 8-naphthyridine-3-carboxylic acid (named enoxacin, originally AT-2266) was found to show the most broad and potent in vitro antibacterial activity, an excellent in vivo efficacy on systemic infections, and a weak acute toxicity . Structure-activity relationships of compounds with variations of substituents at C-1, C-6, and C-7 are also discussed. Jpn J Antibiot, 1984 Mar, 37(3), 512 - 23 {Laboratory and clinical studies of ceftazidime in the pediatric field}; Nishimura T et al.; The authors have carried out the laboratory and clinical studies of ceftazidime ( CAZ ) and obtained the following results . The antibacterial activities of CAZ against the clinical isolates of S . aureus, E . coli, K . pneumoniae, E . cloacae, E . aerogenes, S . marcescens, C . freundii and P . aeruginosa were measured by the plate dilution method with inoculum size of 10(6) cells/ml . The susceptibility distribution of S . aureus to CAZ ranged from 3.13 to 100 micrograms/ml, and the peak of distribution was 12.5 micrograms/ml . The peak of susceptibility distribution of E . coli, K . pneumoniae and E . cloacae was 0.2 micrograms/ml, and the distribution of E . aerogenes ranged from 0.1 to 100 micrograms/ml and that of S . marcescens, from 0.05 to 3.13 micrograms /ml . The growth of 92% of P . aeruginosa was inhibited at the concentration of 3.13 micrograms/ml or lower . For pharmacokinetic study, CAZ was given in a single dose of 10 mg/kg by intravenous administration for 5 minutes in 1 child and by drip infusion for 30 minutes in 2 children . After intravenous administration of CAZ , the serum level got to the peak of 41.0 micrograms/ml at 15 minutes, and was 1.0 micrograms /ml at 6 hours . Half-life time was 1.30 hours . With drip infusion of CAZ , the mean peak serum level was 52.45 +/- 2.05 micrograms/ml on completion of the infusion, and 1.05 +/- 0.05 micrograms/ml at 6 hours . Half-life time was 1.30 hours . CAZ was effective in 9 cases out of 11 cases with bacterial infection . No side effect was observed except for elevation of serum GOT and GPT in 1 case and eosinophilia in 1 case. Jpn J Antibiot, 1984 Mar, 37(3), 485 - 9 {Fundamental and clinical studies on ceftazidime in the field of paediatrics}; Nakamura T et al.; Ceftazidime (CAZ), a new cephem antibiotic for injection, was used in the field of paediatrics, and the following results were obtained . Antibacterial activity of CAZ was high against Gram-negative rods including P . aeruginosa, but slightly low against Gram-positive cocci . Absorption and excretion of CAZ were rapid, and 90% or more was excreted at 6 hours after administration . The clinical efficacy was excellent or good in all the 4 cases treated with CAZ, and no side effects were observed. Jpn J Antibiot, 1984 Mar, 37(3), 423 - 59 {Fundamental and clinical studies on ceftazidime in the field of pediatrics}; Toyonaga Y et al.; Fundamental and clinical studies were carried out on ceftazidime ( CAZ ), a newly synthesized cephalosporin C antibiotic ( CEPs ) . The antibacterial activity of CAZ was compared with those of CER, CEZ, CMZ and CPZ against clinical isolates of S . aureus . S . pyogenes . E . coli, K . pneumoniae and P . mirabilis, and with those of GM and CFS against P . aeruginosa . Against S . aureus, the antibacterial activity of CER was highest, followed by that of CEZ . The peak MIC after inoculation of 100-fold dilution was 0.10 microgram/ml with CER and 0.78 microgram/ml with CEZ . But in view of the peak MIC of 6.25 micrograms/ml, the antibacterial activity of CAZ was inferior to that of CPZ by about 2 tubes . This was not surprising, because CAZ was one of the antibiotics in the fifth group of CEPs . The CEPs in the fifth group naturally show high antibacterial activity against S . pyogenes . CAZ , as expected, inhibited the growth of all the strains at the concentration of 0.10 microgram/ml at the inoculation of 100-fold dilution . In the gut bacterial flora such as E . coli, K . pneumoniae and P . mirabilis, CAZ showed the results almost equal to those of other CEPs in the fifth group; the peak MICs of CAZ were 0.20 approximately 0.39, 0.20 approximately 0.39, 0.10 microgram/ml, respectively, at the inoculation of 100-fold dilution, which was good results . In P . mirabilis with the undiluted inoculation, the result of CAZ was slightly inferior to those of the other CEPs in the fifth group previously reported; however, CAZ was prone to be affected by inoculum size, and with the inoculation of 100-fold dilution, MIC of CAZ turned to be as low as 0.10 microgram/ml . Against P . aeruginosa, CAZ showed the activity comparable to that of CFS, the antibiotic considered to have the highest antibacterial activity of all CEPs used in Japan . This finding is in accordance with the findings reported by other authors . The peak MICs of CAZ were 3.13, 12.5 microgram/ml at the inoculation of undiluted solution, and from 1.56 to 3.13 microgram/ml at the inoculation of 100-fold dilution, which were the results equal to, or even better than those of GM . The change in blood levels of CAZ was studied by one shot intravenous injection and 1 hour intravenous drip infusion.(ABSTRACT TRUNCATED AT 400 WORDS) J Antimicrob Chemother, 1984 Mar, 13(3), 227 - 36 The in-vitro activity of metronidazole against strains of Escherichia coli with impaired DNA repair systems; Jackson D et al.; The minimal inhibitory concentration (MIC) of metronidazole was lower for strains of Escherichia coli with lesions in their DNA repair systems than for their parent strains . The viable numbers of all strains of E . coli tested were considerably reduced by metronidazole, even at sub-MIC levels, and the effect was greater when DNA repair lesions were more severe . In addition, metronidazole caused cell elongation of E . coli and slowly disappeared from the medium upon incubation with the bacterium . The drug-induced decrease in viable numbers of E . coli was followed by an increase . Most cells in this 'recovery' population were found to be anaerogenic and were relatively unaffected by subsequent exposure to metronidazole . The results show that E . coli consumes and is susceptible to metronidazole, under anaerobic conditions . DNA damage is involved in the antibacterial action of the drug, and E . coli resistant to the drug can be obtained readily in in-vitro incubations. Farmaco {Sci}, 1984 Mar, 39(3), 265 - 72 {Furazan sulfanilamides}; Tironi C et al.; Synthesis and antibacterial activity against Escherichia coli of a series of furazan sulfanilamides are reported . A structural activity relationship for these derivatives is also briefly discussed. Eur J Cancer Clin Oncol, 1984 Mar, 20(3), 397 - 403 Role of mononuclear phagocyte function in endotoxin-induced tumor necrosis; Bloksma N et al.; The temporal susceptibility of tumors to induction of necrosis and regression by endotoxin was investigated further with a focus on the role of the putative mediator, tumor necrosis factor (TNF) . Production of this factor was shown earlier to require prior activation of the mononuclear phagocytic system (MPS) . Transplants of Meth A sarcoma or MOPC315 plasmacytoma had no consistent effect on parameters of MPS function such as hepatosplenomegaly, carbon clearance and non-specific antibacterial resistance at times that they were sensitive to induction of necrosis . Moreover, TNF, quantified by its necrotizing and regressing activity in vivo, could not be detected in the serum of tumor hosts after a necrotizing dose of endotoxin, while much smaller volumes of serum with TNF (TNS) of appropriately treated donor mice showed activity . As repeated incubation of TNS with Meth A cells at 37 degrees C hardly removed its in vivo activity against Meth A, immediate absorption of produced TNF to the tumor cell mass seems a less likely cause . Cytostatic activity, another property attributed to TNF, was hardly increased in post-endotoxin tumor host serum, while TNS is highly cytostatic . It is concluded that induction of tumor necrosis is not dependent on MPS activation . A role of TNF as mediator of the effects of endotoxin still remains uncertain . Furthermore, the present and other data suggest that TNF, like endotoxin, probably acts by an indirect mechanism against tumors in vivo. Am J Med, 1984 Mar, 76(3), 436 - 49 Approaching the controversies in antibacterial management of cancer patients; Pizzo PA et al.; The principles for management of infectious complications in cancer patients are continuing to evolve . The critical element includes the prompt institution of broad-spectrum antibiotic(s) empirically when granulocytopenic patients become febrile and continuation and modification of the regimen in patients with persistent fever and granulocytopenia . The view is presented that antibiotics provide systemic prophylaxis as well as therapy in persistently granulocytopenic patients and that they should be continued until all signs of infection have cleared or the granulocyte count has recovered . Such aggressive therapy, supplemented by continued evaluation and monitoring of the patient, can significantly reduce infection-relation morbidity and mortality. Mod Vet Pract . 1984 Feb;65(2):115. Hepatitis in a dog given sulfadiazine-trimethoprim and cyclophosphamide; Anderson WI et al.; Vomiting, diarrhea, icterus and elevated serum alkaline phosphatase, SGPT and serum bilirubin levels occurred in a 12-year-old Basenji on sulfadiazine-trimethoprim and cyclophosphamide therapy . After use of the antibacterial drug was discontinued, the dog returned to normal with no further evidence of hepatocellular damage. Pharmazie, 1984 Feb, 39(2), 84 - 91 Synthesis, antibacterial and antifungal activity of 4-hydroxycoumarin derivatives, analogues of novobiocin; Patonay T et al.; 3-Acylamino-, -arylsulfonylamino-, -(N'-arylureido)-, -arylideneamino- and -arylcarbamoyl-4-hydroxycoumarins have been synthesized and tested for antibacterial and antifungal activity . 3-Arylcarbamoyl-4-hydroxycoumarins have been shown to possess significant activity against Gram-positive bacteria; 3-acylamino-4-hydroxycoumarins have moderate antibacterial and antifungal effects whereas the additional compounds are inactive. J Antibiot (Tokyo), 1984 Feb, 37(2), 150 - 8 Synthesis of pseudotrisaccharides related to ribostamycin; Girodeau JM et al.; The three protected sisamine derivatives 2i, 2j and 3, with a free 5-hydroxyl group, have been synthesized . Glycosylation at the 5 position with various pentofuranose derivatives yielded after deprotection of the 6a approximately i ribostamycin related aminoglycoside . These pseudotrisaccharides showed only low antibacterial activities with respect to the parent compounds. Farmaco {Sci}, 1984 Feb, 39(2), 95 - 109 Researches on antibacterial and antifungal agents . II - Synthesis of 1-ethyl-1,4-dihydro-4-oxo-7-(1-pyrrolidinyl)quinoline-3-carboxylic acid, a novel highly active, broad-spectrum antibacterial agent related to piromidic acid; Corelli F et al.; The synthesis and antibacterial activities of 1-ethyl-1,4-dihydro-4-oxo-7-(1-pyrrolidinyl)quinoline-3-carboxylic acid are reported . The new analog of nalidixic acid has been prepared by standard procedure starting from 1-(3-aminophenyl)pyrrole; it showed a broad spectrum of antibacterial activity and exhibited much higher activity than nalidixic, pipemidic and piromidic acids . The synthesis of 1-ethyl-1,4-dihydro-4-oxo-8-(1-pyrrolyl)quinoline-3-carboxylic acid is also described; this acid was inactive when tested as antibacterial agent. Antimicrob Agents Chemother, 1984 Feb, 25(2), 226 - 33 Side chain modifications in lankacidin group antibiotics; McFarland JW et al.; Novel N-acyl analogs of lankacidin may be prepared from 3-isocyanatolankone diformate {7,13-bis(formyloxy)-2-isocyanato-1,4,10,19-tetramethyl-16- oxabicyclo{13.2.2.}nonadeca-3,5,9,11-tetraen-17,18-dione} . Of seven such analogs evaluated in vitro only homolankacidin diformate showed significant activity . However, in a cell-free system two of the inactive analogs inhibited polypeptide synthesis as well as did lankacidin itself or erythromycin . Antibacterial activity, therefore, is a function of the ability of a congener to penetrate the bacterial cell membrane in addition to its intrinsic activity . Similarly, lankacidinol is as potent as lankacidin or erythromycin as an inhibitor of bacterial polypeptide synthesis in a cell-free system . This intrinsic activity is expressed as potent antibacterial activity against growing gram-positive cultures in O(2')-acyl derivatives with the proper lipophilicity. Res Commun Chem Pathol Pharmacol, 1984 Feb, 43(2), 235 - 49 Inhibition of bacterial plasmid replication by stereoselective binding by tricyclic psychopharmacons; Molnar J et al.; Several dibenzazepines, thioxanthene, and phenothiazine stereoisomers were studied for their abilities to inhibit plasmid replication, intracellular transfer of R-plasmid, bacterial ATP-ase, and mouse serum cholinesterase isoenzyme . Partially saturated derivative of desipramine inhibited plasmid replication and transfer, but the fully saturated derivative was inactive . The inhibition of plasmid curing and transfer patterns did not correlate with the inhibition of ATP-ase and cholinesterase . Trans-clopenthixol was more effective in plasmid elimination than the cis-isomer . On the other hand, the cis-isomer inhibited ATP-ase and cholinesterase more than the trans-isomer . The levo- and dextro-methoxytrimeprazine also inhibited plasmid replication and enzyme activity . We believe that the tricyclic configuration of the drugs tested for stereospecific binding to bacterial receptors is more important than its side chain orientation . We believe that there is a similarity between bacterial receptor sites and neural receptor sites . Therefore, this model may be useful in the study of neuropharmacological agents as potential antibacterial agents. South Med J, 1984 Feb, 77(2), 204 - 14 Emergent burn care; Harvey JS et al.; The estimated 32,600,000 fires that occur annually in the United States produce over 300,000 injuries and 7,500 deaths . Ten percent of hospitalized burn victims die as a direct result of the burn . Initial evaluation and management of the burn patient are critical . The history should include the burn source, time of injury, burn environment, and combustible products . The burn size is best estimated by the Lund and Browder chart, and the burn depth is determined by clinical criteria . Pulmonary involvement and circumferential thoracic or extremity burns require detection and aggressive treatment to maintain organ viability . Hospitalization is usually necessary for adults with burns larger than 10% of the total body surface area (TBSA) or children with burns larger than 5% of TBSA . Major burns, those of 25% or more of TBSA or of 10% or more of full thickness, should be considered for treatment at a burn center, as well as children or elderly victims with burns of greater than 10% TBSA . Lactated Ringer's solution, infused at 4 ml/kg/% TBSA, is generally advocated for initial fluid restoration . After the acute phase (48 hours), replacement of evaporative and hypermetabolic fluid loss is necessary . These losses may constitute 3 to 5 liters per day for a 40% to 70% TBSA burn . Blood transfusion is often required because of persistent loss of red blood cells (8% per day for about ten days) . Many electrolyte abnormalities may occur in the first two weeks . Pulmonary injury commonly is lethal . Circumoral burns, oropharyngeal burns, and carbonaceous sputum are indicative of inhalation injury, but arterial blood gas determinations, fiberoptic bronchoscopy, and xenon lung scans are useful for confirming the diagnosis . Humidified oxygen, intubation, positive-pressure ventilation, and pulmonary toilet are the mainstays of therapy for inhalation injury . Wound care is initially directed at preservation of vital function by escharotomy, if restrictive eschar impairs ventilatory or circulatory function . Antibacterial agents may be applied to the burn, but invasive sepsis, defined as greater than 10(5) organisms per gram of tissue with invasion of subjacent viable tissue, requires systemic antibiotic therapy . Wound debridement is done by daily hydrotherapy, tangential excision, chemicals, primary excision, and grafting, tailoring the technique to the individual burn.(ABSTRACT TRUNCATED AT 400 WORDS) Jpn J Antibiot, 1984 Feb, 37(2), 267 - 78 {Susceptibility of clinical isolates to cefotaxime . Comparison to new antibiotics latamoxef, cefoperazone, and ceftizoxime}; Asari S et al.; Susceptibilities of 372 strains of bacteria to cefotaxime (CTX) were determined based on the inhibition zone diameter obtained by the single-disc method . Four categories were assessed . Susceptibility of clinical isolated to CTX and 3 other antibiotics . Against most strains, CTX showed higher antibacterial activity than other drugs in the low concentration, especially for S . aureus, S . pneumoniae, S . agalactiae, E . coli and P . morganii . Susceptibility of strains isolated from different clinical materials . CTX showed the highest antibacterial activity against most strains isolated from pus, blood and cerebrospinal fluid and showed higher activity against strains isolated from other materials, too . Susceptibility of clinical isolates in 7 different fields . CTX was shown to have uniformly higher antibacterial activity than other drugs against isolates from such fields as internal medicine, pediatrics, surgery, urology, obstetrics & gynecology, dermatology and otorhinolaryngology . CTX showed the highest antibacterial activity in dermatology . Susceptibility of all clinical isolates . CTX showed the highest antibacterial activity against isolated pathogenic 352 strains (except for P . aeruginosa of 20 strains). Am J Surg, 1984 Feb, 147(2), 205 - 9 Noncovalent bonding of penicillin and cefazolin to dacron; Harvey RA et al.; Dacron grafts treated with the surfactant, benzalkonium chloride or TDMAC bind significant quantities of penicillin-14C or cefazolin-14C . The treated grafts showed strong antibacterial activity which indicated that bound radioactivity corresponds to the reversible adsorption of biologically active molecules . Bound penicillin-14C or cefazolin-14C slowly dissociates when the grafts are placed in a surgically prepared muscle pouch in the rat . This slow release of antibiotic produces therapeutic levels of antibiotic in the adjacent tissue . Binding can also be achieved by in situ irrigation of surfactant treated grafts with antibiotic or by injection of the antibiotic. Chemioterapia, 1984 Feb, 3(1), 25 - 32 Comparative experimental antibacterial activity of ceftriaxone (Ro 13-9904); Bohni E; The in vitro activity of new cephalosporins, oxacephems and penicillins against pathogens involved in respiratory and gastrointestinal tract infections is practically equivalent . However, in experimental infections with the same pathogens the superior efficacy of ceftriaxone over all comparative cephems and penicillins, expressed in low 50% effective doses after multiple and particularly after single dosage schedules, and caused by a longer maintenance of blood and tissue levels can be demonstrated . Although mice have an altered pharmacokinetics these experimental results reflect the observed clinical advantage of ceftriaxone in human infections: long plasma half-life, low dosage and single daily administration. Biochemistry, 1984 Jan 31, 23(3), 508 - 14 Formaldehyde metabolism by Escherichia coli . In vivo carbon, deuterium, and two-dimensional NMR observations of multiple detoxifying pathways; Hunter BK et al.; 13C NMR has been used to demonstrate the metabolism of dilute solutions of labeled formaldehyde by Escherichia coli to methanol, formate, carbon dioxide, and several other unidentified metabolites which contain labeled CH2 groups . Aeration of bacterial suspensions within the spectrometer dramatically increased the rate of oxidation to formate and carbon dioxide . Deoxygenation with nitrogen gas virtually abolished all metabolism, as did the exposure of bacteria to very high formaldehyde concentrations . Deuterium NMR of whole cells in deuterium-depleted water further demonstrated the conversion of formaldehyde-d2 to methanol-d2, ruling out a formaldehyde dismutase as an important species . Two-dimensional proton-carbon chemical shift correlation was used to reveal the chemical shifts of the protons attached to 13C labels in metabolites . The results indicate that formaldehyde is efficiently detoxified by the bacterial cell through a route or routes which do not appear to involve tetrahydrofolate . This detoxification may be in competition with the lethal antibacterial processes associated with formaldehyde. Dev Comp Immunol, 1984 Spring, 8(2), 283 - 91 Identification of hemagglutinating protein and bactericidal activity in the hemolymph of adult Sarcophaga peregrina on injury of the body wall; Kubo T et al.; When the body wall of adult Sarcophaga peregrina (flesh-fly) was injured with a hypodermic needle, hemagglutinating activity and antibacterial activity were induced in the hemolymph simultaneously . The hemagglutinating activity was shown to be due to the same lectin that was found previously in the hemolymph of injured larvae . Thus, larval and adult Sarcophaga respond in the same way to injury of the body wall. Indian J Med Sci, 1984 Jan, 38(1), 1 - 2 Povidone-iodine (Betadine) as prophylaxis against wound infection in abdominal tubal ligation; Khanna A et al.; PIP: Povidone-iodine solution was used for this prospective study by including 100 patients who underwent abdominal tubal ligation by a small, vertical, suprapubic incision . In the test group of 50 patients a thin layer of povidone-iodine (5%) was painted over the skin around the incision and it was left as such for 5 minutes . Then part preparation was done by savalon and spirit . A layer of povidone (5%) was instilled in the wound . The wound was cleanded with spirit and then a povidone-iodine (5%) soaked gauge piece was applied and dressings were done . No postoperative antibiotics were given . In the 50-patient group, a similar procedure was performed but without povidone-iodine . Postoperative antibiotics were given to these patients until the stitches were removed . The wound was opened after 48 hours in both groups and then checked at 48-hour intervals . If the wound showed any evidence of infection, the dressing was done at 24-hour intervals . In cases of infected wounds, povidone-iodine (5%) ointment dressing was done in the test group; dressing was done by other antibacterial ointments in the control group . The wound infection rate was comparable in both groups . 4 of 50 (87%) test group patients had wound infection in the form of stitch abscess and serious discharge, which was rapidly controlled by povidone-iodine dressing in 3 days time on average . 3 of 50 (6%) control group patients had wound infection, which was controlled by local dressing in 4-5 days on average . There was no statistically significant difference between the 2 groups . It is concluded that povidone-iodine solution is preferable to routine use of postoperative antibiotics in minor operations . It is well tolerated with no untoward reactions and is an inexpensive modality for preventing infection . Ann Immunol (Paris), 1984 Jan-Feb, 135C(1), 107 - 15 Regulatory idiotopes, parallel sets and internal image of the antigen within the polyfructosan-A48 idiotypic network; Bona CA et al.; The study of the A48 idiotype anti-beta 2----6-polyfructosan immune response was used as a tool to investigate the various postulates of the immune network theory . The results of this study have shown: that only certain idiotopes, designated as regulatory idiotopes, play a role in idiotype-regulated immune responses; that some of the A48 idiotopes were expressed on a myeloma protein with unknown binding activity (MOPC173) and on MOPC167, a phosphorylcholine-binding myeloma protein; that one out of six monoclonal antiidiotypic antibodies tested carried the internal image of the antigen and could elicit an antibacterial levan immune response in mice treated at birth with bacterial levan or polyclonal anti-A48Id antibodies. Antimicrob Agents Chemother, 1984 Jan, 25(1), 134 - 6 Antibacterial properties of tuftsin and its analogs; Blok-Perkowska D et al.; The antibacterial properties of tuftsin and its 11 analogs on 20 bacterial strains were investigated . Tuftsin showed a definite antibacterial effect at a minimal effective concentration of 62.5 micrograms/ml . All analogs were either less effective or lacked any activity . The bacteria used included some highly pathogenic organisms. J Antibiot (Tokyo), 1984 Jan, 37(1), 57 - 62 Syntheses and biological activities of new carbapenem derivatives; Shiozaki M et al.; 3-beta-Alanyloxymethyl, 3-glycyloxymethyl and 3-methyl derivatives of 6-(1-hydroxyethyl)-carbapenems, (VIIa, VIIb and VIII), and 3-methyl-6-(1-hydroxyethyl)carbapenam (IX) were synthesized from 3-(1-tert-butyldimethylsilyloxyethyl)-4-(3-chloro-2-oxopropyl) -2-azetidinone (I) . The antibacterial activities of these compounds proved that the delta 2 double bond was essential for the appearance of bioactivity, whereas the amino group on the C-3 side chain was not necessary. J Int Med Res, 1984, 12(1), 30 - 4 Alkalinisation in the management of cystitis; Spooner JB; A study is described in which 205 women aged 18 to 60 years presenting with symptoms of cystitis and for whom there was no clear clinical evidence of a bacterial infection were treated with a 48-hour course of sodium citrate in the form of Cymalon granules . Significant bacteriuria was present in forty-three (21.3%) of the 202 patients for whom assessment was possible . Continuing or assumed bacteriuria was evident in twenty-one patients after treatment for whom an antibacterial agent was indicated . The average pre-treatment symptom score was higher for those with initial bacteriuria, than those without . In patients with persisting bacteriuria, symptom severity remained unchanged or worsened . In patients with pre-treatment bacteriuria whose symptoms improved, the bacteriuria was cleared . In those patients who were abacteriuric initially, symptoms were relieved in about 80% of cases . It is concluded that a 48-hour course of sodium citrate can provide good symptomatic relief for most women with cystitis for whom there is no definite clinical evidence of a bacterial infection . Failure to respond adequately is very suggestive evidence of persisting bacteriuria for which a course of antibacterial therapy is indicated. J Med Chem, 1984 Jan, 27(1), 63 - 6 Electronic structures of cephalosporins and penicillins . 15 . Inductive effect of the 3-position side chain in cephalosporins; Boyd DB; Induction appears to be the primary means by which the side chain at position 3 of the cephem nucleus influences the chemical reactivity of the beta-lactam ring . In vitro antibacterial activity data suggest that when the cephalosporin is in the active site of the target bacterial enzymes, the presence of a leaving group in the side chain can promote inhibition. J Clin Microbiol, 1984 Jan, 19(1), 1 - 3 Stability of antibiotics bound to polytetrafluoroethylene with cationic surfactants; Donetz AP et al.; This study evaluated the effect of prolonged storage and sterilization on the noncovalent bonding of penicillin to polytetrafluoroethylene grafts . The surfactant tridodecylmethylammonium chloride was unaffected by prolonged storage or sterilization, and its ability to bind penicillin remained constant for as long as 3 months . Steam or ethylene oxide sterilization markedly diminished the antibacterial activity of bound penicillin . However, the antibacterial properties of penicillin remained constant for up to 12 weeks when the grafts were stored at either 4 degrees C or room temperature . Thus, the bonding process appears to increase the stability of the antibiotic, and the data presented suggest that vascular prostheses can be treated with a surfactant, sterilized, and stored for at least 3 months . Grafts can then be treated with an antibiotic in the operating room, washed, and implanted. Pharmacol Res Commun, 1984 Jan, 16(1), 21 - 9 Antipyretic and antibacterial actions of Teucrium polium (L.); Autore G et al.; The antipyretic and antibacterial activities of the ethanolic extract of the flowering tops of Teucrium polium (L.) were been studied . The extract was effective against both yeast and carrageenin pyrexia in rats . It also exhibited a marked antibacterial action against both gram positive and gram negative organisms and was found to be non toxic in acute studies. Scand J Infect Dis Suppl, 1984, 42, 135 - 42 Treatment with beta-lactam antibiotics in skin and soft tissue infections; Hedstrom SA; Beta-lactam antibiotics are highly effective against most bacteria causing skin and soft tissue infections . Good tissue penetration further makes beta-lactam antibiotics useful against skin and soft tissue infections . Drugs with a narrow spectrum should be among the first choice . Broader spectrum beta-lactam antibiotics may be needed in reduced bacterial susceptibility . Low molecular weight compounds (monobactams, penems, penicillinase inhibitors) in addition to their high antibacterial effect have shown excellent tissue penetration . In easy and moderately severe anaerobic infections not treatable with conventional oral beta-lactam antibiotics, other oral antibacterial agents (e.g . clindamycin, metronidazole) may be used rather than the parenteral recent acyl-ureidopenicillins or cephalosporins . Due to long duration of skin and soft tissue levels of drugs, it is unnecessary to administer beta-lactam antibiotics more than 2 or 3 times a day . Normal dosage schedules can be employed except in severely compromised elimination when decreased doses may be recommended or in immuno-compromised hosts and other risk patients who may require a 2- or 3-fold increase. Acta Neurol Scand Suppl, 1984, 100, 77 - 87 Some toxic effects of lead, other metals and antibacterial agents on the nervous system--animal experiment models; Olson L et al.; Modern man is chronically exposed to lead levels in the biosphere, several times higher than the natural level that once existed . There is much concern about the possible adverse effects of this population-wide low-level lead exposure, particularly on the developing organism, where the central nervous system may be a primary target for lead . We have developed animal test systems which permit temporal and spatial discrimination of possible effects of lead and other potentially neurotoxic agents in the environment on the developing central nervous system, as well as on different types of peripheral nerves in the adult individual . In one experimental design, defined areas of the fetal rat brain are grafted to the anterior chamber of the eye of adult rat recipients which are exposed to lead (1% PbAc in drinking water) . Such grafts will become vascularized from the host iris and continue their development in oculo . Thus the grafted brain tissue and the host brain will share circulation and therefore be exposed to exactly the same amounts of lead simultaneously . Studies of cerebellar grafts revealed that although there was a normal gross cytological development in the presence of lead, there was a severe, permanent impairment of the spontaneous discharge rates of the grafted Purkinje neurons as observed with electrophysiological techniques long after cessation of the lead treatment . The host Purkinje neurons were not affected . A similar, although less dramatic, impairment of cerebellar function could then be demonstrated in intact animals when newborn rats were given lead (8 mg PbAc/kg i.p.) during the first 20 days of life and then studied as adults . In other areas of the fetal central nervous system grafted to the eye, lead caused disturbed growth (substantia nigra, cortex cerebri) . A screening technique for potentially harmful effects on autonomic and sensory nerve terminals in adult rats makes use of intraocular injections of agents to be tested . Morphological and histochemical changes of the innervation apparatus of the iris are then studied in iris whole-mount preparations . Lead causes an adrenergic hyperinnervation of the iris . Computer-based image analysis revealed severe degenerative effects by hexachlorophene and chlorhexidine . These studies demonstrate the usefulness of the intraocular grafts and the intraocular injection technique and the need to apply both structural and functional techniques in order to detect possible neurotoxic actions of xenobiotics . The techniques have revealed hitherto unknown toxic actions of lead on cerebellar function. Scand J Gastroenterol Suppl, 1984, 90, 29 - 34 Penetration of antibiotics to tissues and infected foci; Bergan T et al.; There is proportionality between the area under the curve of concentrations in serum and the area under the curve in tissues and other extravascular foci of the body . A high peak area under the serum curve - PAUC - establishes high extravascular concentration levels in tissues, operation areas and infected sites . Most antibiotics are able to produce satisfactory antibacterial levels in interstitial tissue fluid regardless of serum protein binding . Binding to components of interstitial space, like alpha 1-globulin, inhibits the establishment of the concentrations . Administration of a prophylactic agent by infusion 1 h before an operation suffices to produce anti-bacterial levels in wound tissues to inhibit growth of susceptible bacteria contaminating it during the operation. Ciba Found Symp, 1984, 102, 40 - 51 Plant-plant interactions; Bell EA; Higher plants show three types of biochemical adaptation which enable them to combat pathogenic organisms in the form of lower plants . Firstly they may synthesize antibacterial or antifungal compounds in concentrations that prevent the invasion of the higher plant by the bacteria or fungi . Secondly they may synthesize such compounds in less than adequate amounts for defence in healthy tissues but respond to invasion by increasing the synthesis; and, thirdly, they may respond to invasion by synthesizing antibacterial or antifungal compounds de novo . Higher plants also show biochemical adaptations that enable them to compete with individuals of the same or different higher plant species . These include the synthesis of volatile and water-soluble phytotoxins which suppress the germination, growth, or both, of competitors. J Inorg Biochem, 1984 Jan, 20(1), 79 - 86 Ligational behavior of a novel biologically active donor toward Cu(II) and Ni(II) ions and potentiation of its antibacterial activity by chelation with metal ions; Ghosh S et al.; The chelating behavior of a new multidentate ligand with tuberculostatic activity toward Cu(II) and Ni(II) ions has been studied . This ligand 3-(2-carboxyhydrazine)phenylimino-2-oximobutane(H2C POB) is found to chelate the above metal ions in both its keto and enol forms . The probable structures of all the complexes and the location of the bonding sites have been established through magnetic and spectroscopic (infrared, electronic) studies . The Cu(II) complex of the enol form exhibits subnormal magnetic moment at room temperature, indicating the probable existence of some sort of super exchange phenomenon in the system . The ligand itself and a few of its Cu(II) complexes have been found to exert powerful in vitro antibacterial activity toward some tuberculosis mycobacteria, such as Mycobacterium flae, Mycobacterium smegmatis, and Mycobacterium H37Rv. Polim Med, 1984, 14(1-4), 55 - 60 {Treatment of varicose ulcers with Codogard of Polish production}; Stryga W et al.; Synthetic skin CODOGARD produced by the Research and Development Centre of the Knitting Industry in Lodz was applied in 125 cases of the shank varicose ulcer treated in the Clinic of General Surgery of the Warsaw Medical Academy . Two different types of CODOGARD were used for evaluation: the first one without antibacterial dripping, and the second one with antibacterial dropping Sterinol . On the basis of achieved results it was established that CODOGARD was a successful medicine for the crus varicose ulcer . It causes faster cleaning away of the pus . It was observed that CODOGARD with Sterinol dripping was more effective . Taking into account the fact that the application of CODOGARD is easy, it should be widely used in surgical out patient's departments. Ann Med Interne (Paris), 1984, 135(7), 512 - 8 {Evaluation of the biliary passage of beta-lactam antibiotics}; Brogard JM et al.; The present study is devoted to the biliary excretion of some beta-lactam antibiotics (6 derived from the penicillin group: Penicillin G, Ampicillin, Metampicillin, Carbenicillin, Mezlocillin, Apalcillin and 9 from the cephalosporin group: Cephalothin, Cephaloridine, Cephacetrile, Cefalexin, Cefazolin, Cefamandole, Cefuroxime, Cefaclor and Ceftizoxime) . The biliary excretion of these antibiotics was assessed by 4 different procedures: 1) experimental study of their biliary elimination by a perfused isolated rabbit liver; 2) in humans, by evaluation of their passage: a) in aspirated duodenal fluid, b) in bile collected by external biliary drainage, c) and in bile obtained by puncture of the main bile duct and the gall bladder during surgery . The results of these different investigations were concordant and showed that the biliary excretion of Metampicillin, Apalcillin and Mezlocillin was definitely higher than that of the other studied beta-lactams; on account of their suitable antibacterial spectrum, these 3 derivatives should be used in preference for the treatment of biliary infection. Ter Arkh, 1984, 56(9), 87 - 90 {Sanitation bronchoscopy in the treatment of nonspecific lung diseases}; Ermakov EV et al.; The authors provide the results of application of sanitation bronchoscopy in patients with nonspecific lung diseases . Differential (depending on the disease etiology, endobronchitis pattern, immunity) application of antibacterial drugs, bacteriophages, immunity and regeneration stimulants substantially improves the disease course and prognosis . As compared to the control group, the main group patients manifested a more rapid positive dynamics of the immunological parameters. Sabouraudia, 1984, 22(5), 433 - 8 Imported penicilliosis marneffei in the United States: report of a second human infection; Pautler KB et al.; The first natural infection due to Penicillium marneffei in a human was reported in the United States in 1973 . We describe a second case of penicilliosis marneffei that was diagnosed in Florida . In both instances, the patients had a history of travel in Southeast Asia where P . marneffei is endemic . The Florida patient had recurrent episodes of hemoptysis attributed to bronchitis and bronchiectasis . In spite of therapy with various antibacterial antibiotics for tuberculosis, the granulomatous lesions in the left upper lobe of the lungs persisted . The diagnosis of penicilliosis marneffei was established by isolating and identifying the dimorphic species of Penicillium, P . marneffei . The histopathologic features of the lung tissue included granulomata with central areas of necrosis and neutrophilic infiltration with many yeast-like, tissue-form cells of P . marneffei, which multiplied by a fission rather than a budding process. Folia Microbiol (Praha), 1984, 29(5), 375 - 84 Mechanisms of antibacterial immunity of mucous membranes; Franek J et al.; A survey based on both literary data and the authors own results, concerning the mechanisms of sIgA-mediated antibacterial immunity, is presented . Secretory IgA is characterized as a specific component of the immune system of mucous membranes, which can recognize harmful bacterial and distinguish them from indigenous microflora physiologically colonizing the mucous membranes, to fix them to the mucous membrane surface and to direct further factors, such as mucin, lysozyme, etc . (which form the effector component of the mucous membrane immunity system) for their final inactivation and neutralization. Surv Synth Pathol Res, 1984, 3(2), 119 - 30 Antibacterial monoclonal antibodies and the dawn of a new era in the control of infection; Macario AJ et al.; Literature reports concerned with monoclonal antibodies against bacteria, or their toxins, which are pathogens for man and animals were surveyed . These antibodies have important potential uses in human and veterinary pathology and medicine . They are likely to become key elements in a fast progression toward a more complete understanding and control of infectious diseases and of toxin poisoning . A new area of bacteriology relevant to sanitary engineering is also being advanced with the help of antibacterial monoclonal antibodies . This area involves bacteria that produce the biofuel methane, along with other molecules of nutritional value, through a process which brings about the recycling of organic wastes and thereby limits or controls microbial contamination of soil and water. Am Rev Respir Dis, 1984 Jan, 129(1), 76 - 81 Alterations in the antibacterial properties of rabbit pulmonary macrophages exposed to wood smoke; Fick RB Jr et al.; We studied the local response of the bronchoalveolar cell population after acute exposure to smoke from pyrolysis of Douglas fir wood . Cell viability experiments and function of the pulmonary macrophages were assessed, including adherence to surfaces, bacterial phagocytosis, and the intracellular bactericidal process . The smoke-exposed group (n=23) when compared with control animals (n=15) produced a significantly greater total cell yield (p less than 0.01) on bronchoalveolar lavage . There was no increase in the percentage of polymorphonuclear leukocytes . As carboxyhemoglobin levels increased, macrophage adherence to glass decreased (r = -0.79, p = 0.0001) . Pulmonary macrophages from exposed animals were 33% less adherent at 120 min in vitro; however, these nonadherent smoke-exposed macrophages remained viable (55 to 78% viable by trypan blue dye exclusion) . Both the phagocytic rate (361 14C cpm/unit time) and the maximal number of bacteria associated (at 60 min) with the exposed macrophages were significantly less than in the sham-exposed animals (uptake = 672 14C cpm/time, p less than 0.002 for each) . The antibacterial properties of pulmonary macrophages are adversely affected by exposure to wood pyrolysis. Microbios, 1984, 41(165-166), 139 - 47 A study of the activity of soft soaps prepared from a homologous series of saturated fatty acids against cells of Escherichia coli NCTC 9001; Lamikanra A et al.; Soaps were prepared by direct neutralization of a homologous series of fatty acids with potassium hydroxide, the acids used being lauric, myristic palmitic and stearic acids . The antibacterial activity of these soaps were studied using Escherichia coli as the test organism . From the various phenomena examined it can be concluded that all the soaps used had a measure of antibacterial activity, the order of this activity being myristate, laurate, palmitate, and stearate . The antibacterial activity of both the palmitate and the stearate can only be described as marginal. Microbios, 1984, 41(163), 15 - 22 Binding of some polyhexamethylene biguanides to the cell envelope of Escherichia coli ATCC 8739; Broxton P et al.; Absorption and antibacterial action of some polyhexamethylene biguanides upon Escherichia coli has been investigated . An amine-ended-dimer (AED) (n = 2), a polydisperse mixture sold by ICI Limited as the active ingredient of vantocil IB (PHMB) (n = 5.5), and a high molecular weight fraction of PHMB (HMW, n greater than or equal to 10) were used . Bactericidal activity was determined over a range of pH (5-9) . Similarly, adsorption of drug to the cell surface, indicated by changes in electrophoretic mobility, and overall drug absorption by the cells were determined . Maximal activity occurred at pH 6 for PHMB and HMW and at pH 5 for AED . This corresponded to minimal surface adsorption and maximal distribution of drug to the underlying cytoplasm and cytoplasmic membrane . Uptake of drug corresponded to high affinity isotherms and indicated a rapid transfer of biocide into the cells following their initial interaction at the surface. Gynecol Obstet Invest, 1984, 18(2), 100 - 4 Critical assessment of antibacterial properties of human amniotic fluid; Larsen B et al.; A low molecular weight fraction of human amniotic fluid was found to be rapidly bactericidal for Escherichia coli ATCC 33908 . Incubation in an atmosphere of CO2 but not N2 diminished the antibacterial effect suggesting that loss of CO2 and change in pH may be partly responsible for the observed antibacterial activity of the low molecular weight fraction of amniotic fluid . Incubation in pH 8.5 buffers did not duplicate the rapid killing of bacteria observed in the low molecular weight fraction of amniotic fluid, suggesting that elevated pH and an antibacterial factor from amniotic fluid act synergistically . The pH change in amniotic fluid which occurs in room atmosphere may account for some of the antibacterial effect which has been reported for amniotic fluid incubated aerobically. Clin Ther, 1984, 6(5), 669 - 76 Clinical efficacy of cefoperazone in obstetric and gynecologic infections; Ling FW et al.; Compared with second-generation cephalosporins, cefoperazone, a third-generation cephalosporin, has demonstrated an extended antibacterial spectrum . In addition, it has a long serum half-life and requires only twice-a-day administration . In this study, 66 patients with clinically diagnosed obstetric and gynecologic infections were treated with cefoperazone, and 61 were evaluated for efficacy . An overall cure rate of 93% (57 patients) was achieved . In view of the excellent clinical response and convenience of twice-a-day administration, we conclude that cefoperazone is a clinically useful single agent for the initial empirical treatment of patients with obstetric and gynecologic infections. Microbios, 1984, 41(160), 107 - 15 Factors affecting the entry of antibiotics into Escherichia coli; Clark D; Factors affecting the entry into Escherichia coli of diverse antibacterial agents, especially beta-lactams were investigated . Agents of greater than a critical molecular weight (approximately 600 Daltons) penetrated extremely poorly . However, there was little correlation between penetrative ability and molecular weight for substances below the critical size . Within classes of related antibiotics (e.g . cephalosporins) penetrative ability was highly dependent on hydrophobicity . The relationship was parabolic rather than linear in nature . The proposal that the envelope of E . coli preferentially excludes hydrophobic molecules is to some extent an artefact arising from pre-selection of the agents used . For unrelated antibiotics hydrophobic nature was a poor guide to penetrative ability . A rather empirical property, diffusion ability through agar, was found to show good inverse correlation with penetrative ability for many unrelated antibiotics. Ann Biol Clin (Paris), 1984, 42(1), 61 - 70 {Effector mechanisms of IgA}; Vaerman JP; Like all immunoglobulins (Ig), IgA has a double function: recognition of the antigen, situated in the Fab alpha fragments, and effector functions which allow elimination of the antigen (Ag), carried by the Fc alpha fragment . Secretory IgA ( IgAs ) is the principal Ig of external secretions and mucosae and has a different structure and composition from serum IgA . Its external function of protection against various forms of bacterial and viral aggression has been well established . Its general mechanism is "the immune exclusion of antigens" i.e . prevention of the penetration of the Ag into the organism by confining them to external secretions followed by elimination . The elimination of bacteria is facilitated by the immobilization and agglutination by IgA . Sometimes, with the aid of lysozyme, IgAs can be bacteriolytic . Antibacterial IgAs have a bacteriostatic function in synergy with lactoferrin and/or transferrin; they even reduce the bacterial production of siderophores . IgAs can inhibit bacterial adhesion to epithelial cells and can increase their adherence to mucus . The neutralization of viruses by IgA is due to inhibition of the first stage of infection, attachment and intracellular penetration of the virus . The same mechanism is involved in the neutralization of bacterial toxins . IgAs also decrease intestinal absorption of foreign proteins in the diet . It has been reported that antibacterial IgAs can cause certain bacteria to lose a plasmid which determines their infectivity . IgAs are able to protect themselves by neutralizing IgA1-proteases secreted by certain bacteria found on mucosal surfaces . Plasma IgA has a limited internal action compared to IgM or IgG . It is generally accepted that IgA barely activates complement (C) by the classical pathway and minimally opsonizes Ag for mono- and polymorphonuclear phagocytes . Antibacterial IgA are not bactericidal in the presence of complement and do not facilitate the phagocytosis of the bacteria to which they are attached . Certain unfavourable effector functions have even been described, such as a specific inhibition of complement fixation and bacterial lysis by IgM and IgG . Some IgA may non-specifically inhibit neutrophil chemotaxis as well as their bactericidal and phagocytic activities . It is difficult to believe that IgA, the second Ig (in quantity) in human serum, is simply useless or even harmful.(ABSTRACT TRUNCATED AT 400 WORDS) J Antibiot (Tokyo), 1984 Jan, 37(1), 27 - 32 The fermentation, isolation and characterization of a macromolecular peptide antibiotic: AN-1; Miyashiro S et al.; A new macromolecular peptide antibiotic, named AN-1, was isolated from the culture broth of Streptomyces albus AJ9003 . From 18 liters of culture broth (110 units/ml activity) a 300 mg sample of AN-1 was obtained with a specific activity of 1,160 units/mg was obtained . AN-1 is a basic polypeptide with a molecular weight of 12,000, isoelectric point of pH 8.3, and gives a single band on SDS polyacrylamide gel electrophoresis . It is soluble in water but insoluble in ethanol, butanol and acetone . It was stable at pH 6 approximately 9 but very unstable at pH 2 . The UV absorption spectrum shows a maximum at 280 nm . AN-1 had no antibacterial activity against the Gram-positive and Gram-negative bacteria tested, but shows strong inhibitory activity toward Escherichia coli MP2, a macromolecule permeable mutant . In addition to being highly mutagenic, AN-1 inhibits the in vitro cell growth of L1210 (ED50 0.41 micrograms/ml) . However, AN-1 had no antitumor activity against mouse leukemia L1210 or Lewis lung carcinoma in mouse. J Antibiot (Tokyo), 1984 Jan, 37(1), 20 - 6 The fermentation, isolation and characterization of macromolecular peptide antibiotics: AN-7A, -7B and -7D; Miyashiro S et al.; A group of new macromolecular peptide antibiotics, named AN-7, was isolated from the culture broth of Streptomyces griseoincarnatus AJ9424 . AN-7 was fractionated into three different components, A, B and D . From 18 liters of culture broth (78 units/ml), 10 mg of AN-7A with a specific activity of 2,053 units/mg, 9 mg of AN-7B (1,167 units/mg) and 11 mg of AN-7D (6,225 units/mg) were obtained . All of these samples gave single bands on polyacrylamide gel electrophoresis . They are acidic polypeptides with molecular weights ranging from 12,400 to 13,000 . Their UV absorption spectra showed maxima peaks at 280 nm and shoulders at 290 nm . Each AN-7 component has a nonprotein chromophoric component . AN-7A, -7B and -7D have no antibacterial activity against the Gram-negative bacteria tested but strongly inhibit the growth of Gram-positive bacteria and Escherichia coli MP2, a macromolecule permeable mutant strain . The AN-7 components are mutagenic . These antibiotics inhibit the in vitro growth of L1210 cells (ED50 0.13 approximately 0.18 micrograms/ml) . AN-7A, -7B and -7D also inhibit the growth of L1210 cells in mice. Scand J Infect Dis Suppl, 1984, 42, 38 - 49 Basic design of beta-lactam antibiotics: penams and analogues and monocyclic beta-lactams; Ekstrom B; Improved microbiological and chemical techniques have resulted in the development of a range of new beta-lactam antibiotics with valuable clinical properties . The work on semi-synthetic penicillins demonstrated that by alteration of the side chain in the 6-position of the penam structure it was possible to significantly affect the antibacterial activity of the compounds and their stability against degradation by acids and beta-lactamases . Esterification of the carboxyl group in the 3-position may improve the pharmacokinetic properties of the compounds whereas substitution in the bicyclic penam structure may give compounds with strong inhibitory action against beta-lactamases . Penems are available by chemical synthesis and may have potent antibacterial activity and good stability against beta-lactamases . Carbapenems can be obtained microbiologically and chemically . The latter, include compounds which have high and broad antibacterial activity as well as those which are potent inhibitors of beta-lactamases . Many of the compounds are, however, chemically rather labile and may also be degraded by a dehydropeptidase present in the kidneys . Clavulanic acid is a microbial oxapenam with modest antibacterial activity but potent inhibitory activity against beta-lactamases . Two types of monocyclic beta-lactams with antibacterial properties, the nocardicins and the monobactams, have so far been found to be produced by microorganisms . They have modest in vitro activity, but at least in case of the monobactams it has been possible to obtain compounds by chemical derivatization with high activity against Gram-negative bacteria and with high stability against beta-lactamases. Ter Arkh, 1984, 56(10), 10 - 4 {Chronic nonspecific lung diseases, immunological deficiency and the means of its correction}; Chuchalin AG et al.; Ninety-eight patients with different patterns of chronic nonspecific pulmonary diseases (CNPD) were examined for thymus-dependent immunity . The clinical manifestations of T lymphocyte dysfunction included a torpid recurrent inflammatory process in the respiratory system, respiratory viral infections, short-term efficacy of antibacterial drugs . The patients demonstrated a decrease in the number of T lymphocytes, in production of immune interferon, and in secretion of serum thymic humoral factor . Application of tactivin, a new immunomodulator, is an effective approach to correction of the disorders enumerated . The drug has a beneficial effect on inflammatory process, reduces the symptoms of virus-induced intoxication . Administration of repeated tactivin treatment made it possible to shorten the time of repeated tactivin treatment made it possible to shorten the time of staying at hospital, to reduce the frequency of CNPD relapses from 80 to 36% within the period from 2 months to 1.5 years . This permits recommending the drug during resistance to antibiotic therapy. Avian Dis, 1984 Jan-Mar, 28(1), 238 - 43 Swollen-head syndrome in broiler chickens; Morley AJ et al.; Swollen-head syndrome is a disease seen in broiler chickens between 4 and 6 weeks of age in Southern Africa . It appears to be caused by a mixed coronavirus and Escherichia coli infection . The coronavirus appears to be of a hitherto unrecorded serotype . The disease is controlled by an attenuated live-virus vaccine and antibacterial medication. Ciba Found Symp, 1984, 102, 204 - 18 Bacterial resistance to antibiotics; Datta N; Effective antibacterial drugs have been available for nearly 50 years . After the introduction of each new such drug, whether chemically synthesized or a naturally occurring antibiotic, bacterial resistance to it has emerged . The genetic mechanisms by which bacteria have acquired resistance were quite unexpected; a new evolutionary pathways has been revealed . Although some antibiotic resistance has resulted from mutational changes in structural proteins--targets for the drugs' action--most has resulted from the acquisition of new, ready-made genes from an external source--that is, from another bacterium . Vectors of the resistance genes are plasmids--heritable DNA molecules that are transmissible between bacterial cells . Plasmids without antibiotic-resistance genes are common in all kinds of bacteria . Resistance plasmids have resulted from the insertion of new DNA sequences into previously existing plasmids . Thus, the spread of antibiotic resistance is at three levels: bacteria between people or animals; plasmids between bacteria; and transposable genes between plasmids. Trans Am Ophthalmol Soc, 1984, 82, 75 - 91 Norfloxacin and silver norfloxacin in the treatment of Pseudomonas corneal ulcer in the rabbit; Darrell RW et al.; Norfloxacin is a new synthetic antibiotic with a broad spectrum of activity against gram-positive and gram-negative bacteria, and is more effective than the aminoglycosides against P aeruginosa . In this study norfloxacin was particularly effective in treatment of P aeruginosa infection of the rabbit cornea, and caused no toxicity in normal rabbit eyes after prolonged administration . The addition of silver to norfloxacin enhances its antipseudomonal activity, and broadens its spectrum to include antifungal activity . In this study, silver norfloxacin appears to be the most effective antibiotic against P aeruginosa corneal ulcer in the rabbit . Because of its broad antibacterial spectrum, silver norfloxacin may be useful in the initial treatment of bacterial corneal ulcer before the identity of the bacteria is known . Because of its low toxicity in topical administration, and its antifungal and antibacterial activity, silver norfloxacin may be helpful in prophylaxis against infection in chronic corneal ulcers. Acta Microbiol Hung, 1984, 31(3), 179 - 85 Absorption of viruses into oral lymphocytes and decreased antibacterial activity of oral polymorphonuclear leukocytes; Ongradi J et al.; Antibacterial activity of the oral polymorphonuclear leukocytes and in vitro virus absorption by oral lymphocytes was studied in two patient groups and in controls . A slight decrease of phagocytosis was observed in those control cases and periodontitis patients where orolymphocytes and oral epithelial cells had absorbed viruses, but in the same subjects the bactericidal effect was significantly weaker . Periodontosis patients with a defect of polymorphonuclear cells did not exhibit such a difference . As in similar subjects the antibacterial activity was more frequently weak when their orolymphocytes carried latent viruses, the results suggest that certain individuals are prone to carry latent viruses in their lymphocytes . Lymphokines released from these carrier cells and concentrated locally might damage phagocytic leukocytes, resulting in serious local inflammation. Comp Biochem Physiol B, 1984, 78(1), 15 - 20 The occurrence and production of avidin: a new conception of the high-affinity biotin-binding protein; Elo HA et al.; The production of avidin, a high-affinity biotin-binding egg-white protein, is not restricted to the avian, amphibian and reptilian oviducts . In the acute phase of inflammation, avidin is synthesized and secreted by various injured tissues in the domestic fowl, both male and female . Also in other avian species and a lizard, injured tissues produce an avidin-like biotin-binding factor . The non-oviductal production of avidin in domestic fowl has a great variety of inducers, for example acute inflammation caused by mechanical or thermal tissue injury, septic bacterial infection and (toxic) drugs, and even retrovirus-induced cell transformation . In culture, chicken embryo fibroblasts and yolk sac macrophages synthesize and secrete avidin . Besides the albumen, avidin may act as an antibacterial protein also in the tissues. J Ethnopharmacol, 1983 Dec, 9(2-3), 261 - 72 Physiological effects of cabbage with reference to its potential as a dietary cancer-inhibitor and its use in ancient medicine; Albert-Puleo M; Interest in the potential of cabbage and other Brassica species as possible dietary cancer-inhibitors has been expressed . Preliminary data in support of this include the following: dietary cabbage has been reported to enhance the aromatic hydrocarbon hydroxylase (AHH) microsomal enzyme system and increase the rate of metabolism of certain drugs and carcinogens and to affect chemically-induced tumor formation . Bacterial studies also indicate that cabbage has demutagenic activity in the Ames assay . Cabbage has also been reported to have a protective effect against radiation exposure . In addition, cabbage has been shown to have a variable ability to induce goiter formation in otherwise healthy laboratory animals . Other effects discussed in the literature include an affect on blood sugar, gastric secretion and antibacterial activity . Reference is made to claims found in ancient herbal literature regarding cabbage's alleged therapeutic benefit in putatively cancerous conditions. Jpn J Antibiot, 1983 Dec, 36(12), 3349 - 54 {Antibacterial peptides (XX) . Synthesis and antibacterial activity of alpha-acyltetrapeptides containing basic amino acids (IX)}; Ito H et al.; In order to compare the antibacterial activity with Acyl-Lys-Lys(Thr)-Glu-OH (I), already reported, 3 kinds of Acyl-Lys-Lys(Glu)-Thr-OH (9a - c) and corresponding tetrapeptide (10), which were exchanged Thr for Glu on I, were synthesized by dicyclohexylcarbodiimide method . It was proved the (+)-6-methyloctanoyl-Lys-Lys(Glu)-Thr-OH (9a) shows antibacterial activity against 5 kinds of Gram-negative bacteria and against 2 kinds of Gram-positive bacteria, but that the others (9b), (9c), only have the weak one, and that tetrapeptide has against Gram-positive bacteria; and that those compounds have almost the same one as Acyl-Lys-Lys(Thr)-Glu-OH (I) has. Tropenmed Parasitol, 1983 Dec, 34(4), 229 - 32 A selective liquid medium for primary isolation of South American Leishmanias; Palomino JC et al.; A selective liquid medium for direct isolation of Leishmania spp . from mucocutaneous lesions is described . Minimal inhibitory concentrations and synergy studies were performed and used to select 5-fluorocytosine as an antimycotic agent which inhibits contaminating fungi without an adverse effect on the parasite thus permitting its isolation from contaminated lesions . Penicillin-Streptomycin were included as antibacterial agents . Isolations have been obtained from biopsy material in an average of 5.6 days from 11 of 15 patients with mucous lesions. J Antibiot (Tokyo), 1983 Dec, 36(12), 1683 - 90 Epimerization and stereochemistry of avoparcin; Ellestad GA et al.; The epimerization of avoparcin entities is discussed in some detail . The absolute stereochemistry of avoparcin is now known since the N-methyl terminal amino acid of the aglycone has been isolated and shown to exhibit negative optical rotation and hence has the R-configuration . The same amino acid has been isolated from an epimerized solution of avoparcin and found to have positive rotation and hence the S-configuration . A comparison is made of the CD curves of beta-avoparcin and epi-beta-avoparcin . Some discussion on the effect of protonation of the terminal N-methyl group on the antibacterial activity of avoparcin is included. J Antibiot (Tokyo), 1983 Dec, 36(12), 1659 - 63 Fusidane antibiotics produced by dermatophytes; Perry MJ et al.; Isolates of Microsporum canis, Microsporum gypseum and Epidermophyton floccosum were observed to produce antibacterial activities under cross-resistance to fusidic acid . The activity from E . floccosum was shown to be due to fusidic acid, diketofusidic acid and 3-ketofusidic acid . Possible contributions of these antibiotics to microbial interaction during dermatophytosis is discussed. Vestn Khir Im I I Grek, 1983 Dec, 131(12), 97 - 101 {Effect of drainage of the thoracic duct with lymphosorption on the lymphocyte number in the blood and lymph}; Kochnev OS et al.; Having studied the amount and quality of lymphocytes in the blood and lymph of 48 patients the authors have established that loss of great amount of small lymphocytes during the three-days drainage of the thoracic lymph duct was completely compensated at the expense of reserve populations . Drainage prolonged up to 5-6 days results in exhaustion of the circulating pool of small lymphocytes and changes in immune reactivity . The latter however are not followed by a sharply decreased antibacterial resistance of the organism. Antibiotiki, 1983 Dec, 28(12), 908 - 11 {Comparative sensitivity of the main causative agents of suppurative infection to antibacterial preparations and their combinations}; Makarenkova RV et al.; Sensitivity of 492 microbial strains to 9 antibacterial drugs and their double combinations was studied . The MTC was determined with the method of serial dilutions in an apparatus MIC-2000 (Austria) . The apparatus provides determination of the MTC simultaneously to 12 antibiotics in 8 dilutions or to 8 antibiotics in 12 dilutions. Jpn J Antibiot, 1983 Dec, 36(12), 3444 - 9 {In vivo antibacterial activity of cefoperazone in intraperitoneal infections in mice}; Minami S et al.; The in vivo antibacterial activity of cefoperazone (CPZ) against systemic infections was studied in comparison with that of cefotiam (CTM) using beta-lactamase non-producing bacteria and producing bacteria . In vitro antibacterial activity of CPZ against Gram-positive bacteria was slightly inferior to that of CTM, but there was no significant difference between their in vivo activities . On the other hand, the therapeutic effect of CPZ against Gram-negative bacteria was nearly parallel to in vitro antibacterial activity and particularly was superior to that of CTM against cephalosporinase (CSase) producing bacteria . The ascitic levels of CPZ in mice infected with CSase producing bacteria were persisted longer, but those of CTM disappeared quickly after administration . This result ap