Antimicrobial

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 appeared to reflect on the therapeutic effects of both drugs.

Int J Clin Pharmacol Ther Toxicol, 1983 Dec, 21(12), 605 - 10
Cefotaxime in the treatment of lower respiratory tract infections; Beumer HM et al.; The effect of cefotaxime in treatment of lower respiratory tract infections was evaluated in 23 patients . Because of its high efficacy, low potential for adverse reactions, and convenient dosage, cefotaxime was found to be an effective antibacterial choice in the treatment of this troublesome condition.

J Med Chem, 1983 Dec, 26(12), 1753 - 60
Folate antagonists . 20 . Synthesis and antitumor and antimalarial properties of trimetrexate and related 6-{(phenylamino)methyl}-2,4-quinazolinediamines; Elslager EF et al.; A series of 6-{(arylamino)methyl}-2,4-quinazolinediamines have been prepared by catalytic hydrogenation of the requisite 2,4-diamino-6-quinazolinecarbonitriles in the presence of the appropriate benzenamine . Formylation, acetylation, and nitrosation provided N omega derivatives of these compounds . A variety of the compounds exhibited potent antimalarial, antibacterial, and antitumor activity . In particular, 5-methyl-6-{{(3,4,5-trimethoxyphenyl)-amino}methyl}-2, 4-quinazolinediamine (trimetrexate, 15) has shown a broad spectrum of antitumor effects and is undergoing preclinical toxicology evaluation prior to trial in man.

Boll Ist Sieroter Milan, 1983 Nov 30, 62(5), 417 - 9
Effect of protein concentration and blood clots on the "in vitro" anti-Pseudomonas aeruginosa activity of cefoperazone; Frongillo RF et al.; The effect of the protein content in the medium and blood clots on the anti-Pseudomonas aeruginosa activity of cefoperazone was studied and its activity against strains of the bacteria in the blood clots investigated . Medium protein content, blood clots and the localization of the microorganism all appeared to effect the antibacterial activity of cefoperazone: the therapeutic implications of these findings are briefly discussed.

Boll Soc Ital Biol Sper, 1983 Nov 30, 59(11), 1674 - 7
{In vitro activity of beta-lactam antibiotics and their sensitivity to beta-lactamase}; Esposito S et al.; beta-lactamase production was evaluated by chromogenic cephalosporin 87/312 in 116 E . coli isolated from clinical sources . Such test revealed beta-lactamase production in 54 strains out of 116 (46%): MICs of eight beta-lactam antibiotics (Ampicillin, Piperacillin, Cefazoline, Cephaloridine, Cephalexine, Cefuroxime, Cefotaxime, Cefotaxime) were determined using a miniaturized dilution broth method . Cefotaxime and Ceftriaxome and Ceftriaxone showed the highest antibacterial activity . All beta-lactamases produced by E . coli strains under examination were isolated and purified by ultrasonic disruption and high speed centrifugation . Sensitivity of the eight antibiotics to purified beta-lactamases was assessed by a spectrophotometric method that utilizes the velocity of cytochrome c reduction . The sensitivity to beta-lactamases was reflected in the in vitro activity of the antibiotics as assessed by the determination of the MICs.

Pharmazie, 1983 Nov, 38(11), 752 - 4
{The effect of new quaternary ammonium compounds on bacteria and fungi . 5: Synthesis of 3-methyl-n-alkylthiomethylpyridinium-, 1-methyl-3-n-alkylthiomethylimidazolium- and 1-ethyl-3-n-alkylthioimidazolinium chloride}; Pernak J et al.; Synthesis of some chlorides indicated in headline and their antibacterial properties was described . Synthesis of quaternary pyridine and imidazoline chlorides was performed by reaction of chloromethyl-n-alkylthioether with 3-methylpyridine or 1-methyl- and 1-ethylimidazole . Antibacterial properties of obtained compounds was tested on 13 strains of bacteria and fungi . Chlorides with dodecyl radical indicated the best antibacterial activity.

Methods Find Exp Clin Pharmacol, 1983 Nov, 5(9), 595 - 600
Ethanol-cephalosporin antibiotic interactions: an animal model for the detection of disulfiram (Antabuse)-like effects; Fromtling RA et al.; Disulfiram (Antabuse)-like reactions occurring in patients undergoing antibacterial therapy with certain cephalosporin antibiotics, and after ingestion of ethanol, are well documented . A murine model is described which may prove useful in the detection of compounds likely to produce this effect . Eight cephem compounds (moxalactam, cefamandole, cefmetazole, cefonicid, cefmenoxime, cefoperazone, cefotiam, ceforanide) each carrying an N-methyltetrazolethiol substituent in the 3-position of the dihydrothiazine ring of the parent antibiotic were capable of inducing a disulfiram-like reaction in the test animals . Evidence is presented which strongly suggests a direct relationship between N-methyltetrazolethiol and related heterocyclic thiols and the ability to induce this reaction.

Isr J Med Sci, 1983 Nov, 19(11), 1009 - 15
Comparison between the combination of azlocillin-gentamicin and ampicillin-gentamicin in the treatment of a nursery population; Fogel D et al.; Newborn, and particularly premature infants are prone to life-threatening infections . The combination of ampicillin-gentamicin (AM-G) has been used extensively in neonatal intensive care units (NICU) . Because resistant bacteria emerged, a new drug--an acylureidopenicillin, azlocillin, with a wide antibacterial spectrum--has been developed . A prospective randomized study was performed in order to evaluate the combination of AM-G vs . azlocillin-gentamicin (AZ-G) . Thirty neonates received AM-G and 28 received AZ-G . Definite infection was found in 15 AM-G patients and in 10 AZ-G patients . In these patients, the antibiotic regimen was changed in six of the AM-G and in one of the AZ-G patients . In each of the two treatment groups, one very-low-birth-weight baby died due to overwhelming sepsis . In vitro sensitivity to AZ-G was higher than to AM-G, according to azlocillin blood levels obtained . Infants weighting less than 2,350 g had lower clearance and volume of distribution than did infants weighing greater than 2,350 g . The serum half-life was approximately the same in both groups . It appears to be that in the NICU, the combination of AZ-G may be more effective than the AM-G combination.

J Thorac Cardiovasc Surg, 1983 Nov, 86(5), 785 - 7
Pericardial injury by antibacterial irrigants; Kratz JM et al.; We injected antibacterial solutions into rabbit pericardium to investigate tissue injury . Povidone-iodine was the only irrigant found to cause substantial damage . These data lend experimental support to recent clinical observations that suggest a causal relation between pericardial irrigation with povidone-iodine and the later development of constrictive pericarditis.

Proc Natl Acad Sci U S A, 1983 Nov, 80(21), 6475 - 9
Solid-phase synthesis of cecropin A and related peptides; Andreu D et al.; Cecropin A, a 37-residue antibacterial peptide amide, was synthesized by the solid-phase method . It was shown to be homogeneous and totally indistinguishable from natural cecropin A by chemical and physical criteria, as well as by its antibacterial activity against several Gram-positive and Gram-negative organisms . The synthetic material was also used to establish unambiguously that the carboxyl-terminal blocking group of natural cecropin A is a primary amide as tentatively proposed earlier . The role of the amino terminus of cecropin A in antibacterial activity was investigated by the synthesis of two analogs.

Infect Control, 1983 Nov-Dec, 4(6), 448 - 51
Environmental factors contributing to antibiotic resistance; Phillips I; The genetic determinants of antibiotic resistance originate as a result of random events, affected only by those physical and chemical agents that stimulate mutation . It is the selection and spread, within and between species, of new genetic material that is influenced by environmental factors, though the intrinsic antibiotic resistance of many opportunistic pathogens remains to be explained . Depending on the frequency of genetic change, the biochemical resistance mechanism, the efficiency of selection (including access of antibiotic to relevant bacteria), and the opportunity for person-to-person spread, resistance may present in a number of ways . The use of an antibiotic in any individual may give rise to resistance, among pathogens or normal flora, to that antibiotic alone, to some or all members of its class, or to additional unrelated antibacterials, or to the acquisition of new bacteria, from a variety of sources (humans, animals, inanimate environment) . A resistant organism may occasionally have other advantages that enable it to spread in the absence of the initial selective agents . In the absence of controlled experiments, which are difficult or perhaps impossible, the only evidence of the truth of these hypotheses comes from the clinical use of antibiotics . A wise observer will conclude that the emergence of resistance is a rare event in an individual patient, but is commoner but by no means universal in populations, especially those that are closed . He will note the reports of diminished resistance in the presence of increased usage . The role of academic infection control is to explain all the phenomena observed, and to formulate methods for identifying and countering the actual as opposed to the imagined hazards.

Infection, 1983 Nov-Dec, 11(6), 336 - 9
{Antibacterial concentrations in serum and tooth-jawbone tissue following perioperative administration of propicillin}; Wagner W et al.; Antibacterial Concentrations in Serum and Dental Tissues after Preoperative Application of Propicillin . After resecting radicular and follicular cysts in the jaws, the serum, bone, capsule and fluid of the cysts from 40 patients were studied for their propicillin concentration . The patients received 1 Mega unit (0.7 g) propicillin orally as oblong tablets one or two hours before surgery . One or two hours after the application of propicillin, the distribution coefficients between serum and the three tissues were 0.78 and 0.87 for the spongious bone, 0.07 and 0.06 for the cyst capsule and 0.14 and 0.08 for the cyst fluid . The mean concentrations in all three tissues were distinctly above the MICs of the bacteria most frequently isolated from the mouth for at least two hours.

J Antibiot (Tokyo), 1983 Nov, 36(11), 1516 - 24
Synthesis and antibacterial activity of triazole and isoxazole derivatives of ampicillin; Yasuda N et al.; In order to improve the antibacterial activity of ampicillin, new penicillin derivatives having a 1-aryltriazole-4-carboxamide group or a 5-arylisoxazole-3-carboxamide group at the alpha-position of benzylpenicillin or p-hydroxybenzylpenicillin were synthesized . Some compounds in these series were found to possess high activity against Pseudomonas and other Gram-negative bacteria . In addition, structure-activity relationships, especially the effect of the hydrophobic character of the compounds on activity, were investigated.

J Antibiot (Tokyo), 1983 Nov, 36(11), 1495 - 501
Novel rifamycins . III . Synthesis and antibacterial activity of 3-amidino- and of 4-aminoimidazolo{4,5-c}rifamycin derivatives; Marsili L et al.; A number of semisynthetic rifamycin derivatives modified at position 3 and/or 4, belonging to general structures 2 and 4 (see Scheme 1), have been obtained . The synthesis and the biological activities of the new compounds are described . Compounds 4p and 4q display very good antimycobacterial activity in mice.

Antimicrob Agents Chemother, 1983 Nov, 24(5), 742 - 9
Enhanced activity of streptomycin and chloramphenicol against intracellular Escherichia coli in the J774 macrophage cell line mediated by liposome delivery; Stevenson M et al.; Streptomycin and chloramphenicol were entrapped within large neutral or anionic unilamellar vesicles of egg phosphatidylcholine prepared by an ether injection method . Both antibiotics in liposomal form were inactive against Escherichia coli in a simple tube dilution assay . A comparison was made of the activities of the free and liposomal forms of the antibiotics against E . coli located within the macrophages of the J774.2 murine cell line . The apparent intracellular antibacterial activity of both antibiotics was increased more than 10-fold by entrapment in neutral liposomes and in the case of chloramphenicol in anionic liposomes containing phosphatidylserine . Anionic liposomes containing phosphatidic acid were much less effective carriers than neutral liposomes for either antibiotic in this in vitro system . Incubation at 4 degrees C of cells with liposomes containing antibiotic or carboxyfluorescein inhibited intracellular antibacterial activity and cell-associated fluorescence . The high intracellular activity of the liposomal antibiotics is consistent with their phagocytic uptake by the macrophages followed by intracellular liposomal degradation and antibiotic release . Liposomal modification of cellular uptake and intracellular distribution of antibiotics may be used to extend the activity of existing and new agents against intracellular infection of the reticuloendothelial system.

Rev Infect Dis, 1983 Nov-Dec, 5(6), 1078 - 92
Hydrolytic enzymes of alveolar macrophages; Goldstein E; Hydrolytic enzymes are major constituents of alveolar macrophages, which in recent years have been shown to be involved in many aspects of the inflammatory response in addition to their better-known role in bactericidal processes . This review summarizes the general properties, physiologic function, cellular physiology, and clinical associations of four important hydrolytic enzymes of alveolar macrophages--lysozyme, elastase, plasminogen activator, and collagenase--with particular attention to the relationship of these enzymes to the pathophysiology of lung disease . The information reviewed shows that much is known about the biochemistry of these enzymes, that each is produced in greater quantity when alveolar macrophages are stimulated, that each has a distinctive physiologic role in the inflammatory process, and that they function as part of the overall pulmonary antibacterial defense system . Studies of the pathophysiologic effects consequent to the elaboration of excess quantities of these enzymes by stimulated macrophages show that some hydrolytic enzymes injure the lung by attacking normal as well as inflammatory tissue sites that are susceptible to degradation . Such damage is normally limited by enzymatic inhibitors, like alpha-antitrypsin, but the inactivating capacity of the inhibitors can be overwhelmed and in these instances excess enzyme contributes to the development of emphysema . This newer understanding of the pathophysiologic role of hydrolytic enzymes may lead to therapeutically beneficial methods for modulating the pulmonary inflammatory response.

J Antibiot (Tokyo), 1983 Nov, 36(11), 1502 - 6
LM 427, a new spiropiperidylrifamycin: in vitro and in vivo studies; Della Bruna C et al.; The spiropiperidylrifamycin LM 427 (4-deoxo-3,4-{2-spiro-N-isobutyl-4-piperidyl}-(1H)-imidazo-(2,5-dihydro) rifamycin S) displays a broad spectrum of potent antibacterial activity in vitro . In vivo it is particularly effective in the therapy of experimental tubercular infections of mice . Three schedules of treatment were employed and the best results were obtained when intermittent administrations were used (ED50 of LM 427; 7 times lower than rifampicin) . LM 427 is well distributed in tissues of mice and rats, with lung concentrations 10 to 20 times higher than plasma levels.

Int J Pept Protein Res, 1983 Nov, 22(5), 573 - 81
Studies of peptide antibiotics . XLIV . Syntheses and biological activities of gramicidin S analogs containing delta-hydroxy-L-norvaline or glycine; Yonezawa H et al.; The antibiotic gramicidin S (GS) has the structure of cyclo (-L-Val1-L-Orn2-L-Leu3-D-Phe4-L-Pro5-L-Val1'-L-Orn2'-L-Leu3'-D-Phe4'-L-Pro5'-) and is basic in character . Five GS analogs including {Gly1,1'}-GS and the neutral {L-Hnv2,2'}-GS (Hnv represents delta-hydroxynorvaline) were synthesized by the solid-phase method to evaluate the role of L-Val1,1' and L-Orn2,2' residues in GS . The hybrid analogs {( Gly1}-GS and {L-Hnv2}-GS) and {D-Tyr4,4'}-GS showed high antibacterial activities, whereas {Gly1,1'}-GS and {L-Hnv2,2'}-GS possessed no activity . Inhibitory effects by these analogs for the adsorption of 14C-labeled GS on cells of bacteria sensitive to GS were determined . The structure-activity relationship of GS is discussed on the basis of the results on these GS analogs.

Gan To Kagaku Ryoho, 1983 Nov, 10(11), 2382 - 8
{Sensitivity to bleomycin of human cultured tumor cells and analysis of related factors}; Urade M et al.; Several types of human cultured tumor cells were tested for the sensitivity to BLM, an effective antitumor antibiotic for epidermoid (squamous cell) carcinomas . Three cell lines (HeLa, KB, Hepd) derived from epidermoid carcinomas were very sensitive to BLM under concentrations tested, whereas BLM-resistant HeLa cells (HeLa-BLMr), neoplastic cells derived from salivary glands (HPA, HSG), malignant fibrous histiocytoma (MFH) and melanoma (MEC) were much less sensitive to BLM than epidermoid carcinoma cell lines under the same conditions . To investigate the possible mechanism of BLM resistance, these cell lines, namely HeLa, HeLa-BLMr, HSG and MEC, were examined for i) BLM permeability into cells by using 3H-PEP which was a new derivative of BLM, ii) BLM-inactivating activity in cell extracts by bioassay for antibacterial activity with B . subtilis PCI 219 strain, and iii) DNA repair activity after UV irradiation . Consequently, as compared with BLM-sensitive HeLa cells, BLM less sensitive HeLa-BLMr, HSG and MEC cells showed 34%, 50% and 39% reduction per 10(6) cells in BLM permeability, 1.6-, 5.6- and 4.7-fold increase per mg protein in BLM inactivating activity, and 24.5-, one and 8-fold enhancement in DNA repair activity, respectively . Therefore, it was indicated that above three factors at least were involved in the BLM sensitivity of human tumor cells.

J Pharm Pharmacol, 1983 Nov, 35(11), 712 - 7
Mechanisms of antibacterial formaldehyde delivery from noxythiolin and other 'masked-formaldehyde' compounds; Gidley MJ et al.; Formaldehyde release in aqueous solutions of noxythiolin (N-methyl-N'-hydroxymethyl thiourea) has been monitored by nuclear magnetic resonance (n.m.r.) spectroscopy . The results suggest that antibacterial activity in such solutions resides mainly in the free formaldehyde . N.m.r . spectroscopy also demonstrated slow C-N bond rotation in noxythiolin and N-methylthiourea, with delta G of ca 15 kcal mol-1 (63 kJ mol-1) . N-Hydroxymethyl imidazole is marginally more effective than corresponding hydrated formaldehyde solutions, an effect which is attributed to more rapid turnover of unhydrated formaldehyde as detected by saturation transfer n.m.r . spectroscopy . These observations are combined with the known delivery of lethal iminium ions, R2N+ = CH2, by compounds of the form R2NCH2X (X = OH, NR2; R is alkyl) to suggest a single consistent explanation of the antibacterial properties of a wide range of masked formaldehyde compounds.

Pathology, 1983 Oct, 15(4), 457 - 62
Disinfection of human heart valve allografts with antibiotics in low concentration; Strickett MG et al.; Antibiotic disinfection of allograft heart valves is now an established procedure . A new low-concentration, broad-spectrum mixture of antibiotics was formulated and used successfully to disinfect 58 of 60 human aortic and pulmonary valves after 48 h exposure at 4 degrees C . The antibiotics included were cefoxitin 240 mcg/ml, lincomycin 120 mcg/ml, polymyxin B 100 mcg/ml, vancomycin 50 mcg/ml and amphotericin B 25 mcg/ml . Microorganisms isolated from experimental tissue and from clinical valves before treatment were tested for sensitivity to these antibiotics and were found to be sensitive to one or more . One isolate of Pseudomonas spp . showed decreased sensitivity to polymyxin B, and was found to have a minimum bactericidal concentration of 70 mcg/ml . Results indicated this antibiotic mixture had superior antibacterial efficiency to that in routine clinical use for the past 13 yr.

Jpn J Antibiot, 1983 Oct, 36(10), 2921 - 4
{Ototoxicity of micronomicin sulfate--audiometric assessment}; Hohzawa K et al.; Micronomicin sulfate (MCR) is a new aminoglycoside antibiotic, and its antibacterial spectrum is similar to that of gentamicin (GM) . According to the animal test, MCR has less ototoxicity than other aminoglycoside antibiotics such as GM . To check its clinical ototoxicity, MCR was given intramuscularly to 20 patients at dose of 120--240 mg/day, respectively for 2--8 days, and audiometry was carried out before and after administration of MCR . No evident change was detected between the preadministration hearing levels and the postadministration hearing levels . These data suggest that MCR is sufficiently safe in ototoxicity within dose of 120 mg/day for 4 days.

Lepr India, 1983 Oct, 55(4), 714 - 8
The effect of clofazimine on liver function tests in lepra reaction (ENL); Bulakh PM et al.; Twenty patients with suspected DDS resistance and repeated attacks of lepra reactions were selected for the study . Clofazimine was administered in different doses over a period of 12 months . Elevated levels of transaminases and Alkaline phosphatase prior therapy attained values to near normalcy . Progressive fall in serum Bilirubin and Proteins with normal A/G ratio at the end of therapy was also observed . Clofazimine by its anti-inflammatory and antibacterial action could inhibit the process of liver damage and happened to have minimal deleterious effect on liver by studying the liver function tests.

Vestn Khir Im I I Grek, 1983 Oct, 131(10), 44 - 6
{Ultrasonic cavitation in the treatment of lactation suppurative mastitis}; Romashov FN et al.; Clinical assessment of the efficiency of the method of ultrasound cavitation in the liquid medium of tomicid has shown a pronounced antibacterial effect in addition to stimulation of reparative-regenerating processes as compared with traditional methods of treatment . The proposed method allowed wide use of secondary sutures . It resulted in two-times shortening the treatment of the patients at the hospital.

Antimicrob Agents Chemother, 1983 Oct, 24(4), 486 - 93
Agar disk elution method for susceptibility testing of Mycobacterium marinum and Mycobacterium fortuitum complex to sulfonamides and antibiotics; Stone MS et al.; An agar disk elution method using round well plates, supplemented Mueller-Hinton agar, and commercial drug disks is described for susceptibility testing of Mycobacterium marinum and the rapidly growing mycobacteria to antibiotics and sulfonamides . By this method, 14 of 14 strains of M . marinum were susceptible to rifampin, doxycycline, minocycline, and trimethoprim-sulfamethoxazole . Identical results were obtained with Middlebrook 7H10 agar and drugs prepared from standard powders . With 58 isolates of Mycobacterium fortuitum and Mycobacterium chelonei, this method had a 92% correlation with broth minimal inhibitory concentration determinations for cefoxitin and greater than 98% for doxycycline, kanamycin, amikacin, and the sulfonamides . Sixty-nine percent of isolates of M . chelonei susceptible to amikacin on supplemented Mueller-Hinton agar were resistant on 7H10 agar, and 15 of 16 M . chelonei isolates susceptible to erythromycin in broth were resistant by disk elution when an endpoint of no growth was used with either agar . The agar disk elution method offers a practical method for testing of most antibacterial agents against these mycobacterial species.

J Antibiot (Tokyo), 1983 Oct, 36(10), 1245 - 51
SQ 28,332, a new monobactam produced by a Flexibacter sp . Taxonomy, fermentation, isolation, structure determination and biological properties; Singh PD et al.; A new monobactam SQ 28,332 has been isolated from fermentations of a Flexibacter sp . and the structure 3 was deduced from its spectroscopic properties . SQ 28,332 exhibits weak antibacterial activity.

Int J Clin Pharmacol Ther Toxicol, 1983 Oct, 21(10), 511 - 3
Empiric antibiotic therapy with an amikacin-carbenicillin-cefoxitin combination in granulocytopenic febrile patients--a clinical report; Fernandez-Ranada J et al.; The authors report 57 febrile episodes in 36 patients with leukemia and lymphoma . Patients with less than 1000 granulocytes and fever above 38.5 degrees C were included in this empirical antibacterial protocol (15 mg amikacin/kg/day/iv, 500 mg carbenicillin/kg/day/iv, 200 mg cefoxitin/kg/day/iv) . The criteria for diagnosis of infection were those widely accepted {Schimpff et al . 1971} . Microbiologic documentation of infection was performed in 33.4% of febrile episodes . Antibacterial therapy induced an improvement in 75.1% of cases . Clinical response often occurred in the presence of profound granulocytopenia (in 72% of episodes) . Therapy failure was higher in pneumonia (46%) and lower in fever of unknown origin (21%).

Appl Environ Microbiol, 1983 Oct, 46(4), 925 - 9
Novel method for selective isolation of actinomycetes; Hirsch CF et al.; A new technique for the selective isolation of actinomycetes from natural mixed microbial populations is described . A nutrient agar medium was overlaid with a 0.22- to 0.45-microns-pore cellulose ester membrane filter, and the surface of the filter was inoculated . During incubation, the branched mycelia of the actinomycetes penetrated the filter pores to the underlying agar medium, whereas growth of nonactinomycete bacteria was restricted to the filter surface . The membrane filter was removed, and the agar medium was reincubated to allow the development of the isolated actinomycete colonies . This procedure selects actinomycetes on the basis of their characteristic mycelial mode of growth, offers a general method for their selective isolation, and does not rely on the use of special nutrient media or of antibacterial antibiotics.

Scand J Dent Res, 1983 Oct, 91(5), 351 - 5
Effect of topical application of stannous fluoride, stannous chloride and stannous tartrate on rat caries; Rolla G et al.; Topical application of 10 mM aqueous solutions of stannous fluoride inhibited caries in rats to a higher degree than 20 mM sodium fluoride, although the difference was not statistically significant . Furthermore, stannous fluoride reduced the number of Strep . mutans in plaque significantly; stannous ions have an antibacterial effect . Stannous chloride and stannous tartrate did not reduce caries in the rats, probably because of the low concentrations of available stannous ions in these solutions at low pH . The high concentration of stannous ions in solutions of stannous fluoride is probably partly due to the reduced hydroxide formation resulting from the buffering effect of HF formed at low pH in this solution.

J Trauma, 1983 Oct, 23(10), 878 - 81
The effect of 5% mafenide acetate solution on bacterial control in infected rat burns; Murphy RC et al.; Mafenide acetate is commonly available as a 10% cream and has been shown to be effective in the prevention and control of burn wound sepsis . The high osmolarity of the cream has been implicated in the pain upon application and the neoeschar formation often seen with its use . Mafenide acetate as a 5% solution has a lower osmolarity, and clinical trials with this agent have shown it to be both well accepted by patients and effective in wound preparation . Information concerning its antibacterial efficacy in comparison with other agents, however, has been lacking . Utilizing the Walker burn model, we have found the 5% mafenide acetate solution used as gauze soaks to be equal to mafenide acetate cream and better than silver sulfadiazine in attaining bacterial control of this experimental burn wound in the rat . The 5% solution provided prompt decrease in bacterial counts to less than 10(5) bacteria per gram of tissue in a majority of wounds by 48 hours of treatment . In addition, such wounds showed no evidence of neoeschar formation . In light of the efficient bacterial control and rapid preparation of the wound for grafting seen in this model, more extensive clinical use of the 5% mafenide acetate solution appears justified.

J Clin Microbiol, 1983 Oct, 18(4), 759 - 64
Routine use of BACTEC 16B bottles to remove antibacterial and antitumor agents from blood cultures of cancer patients; Hopfer RL et al.; A total of 1,764 paired sets of BACTEC 6B and 16B blood culture bottles were collected from patients for analysis . The majority of the patients were receiving antibiotic therapy at the time the blood specimens were collected . A total of 126 isolates were considered clinically significant . Of these, 58 grew in both 6B and 16B bottles, 25 grew only in 6B bottles, and 43 grew only in 16B bottles . In both bottles, the same amount of time was required to detect a positive culture . In 18 patients, septicemias were detected in the 16B bottles that were not detected in the 6B bottles . In seven patients, microorganisms were detected in the 6B bottles that were not detected in the 16B bottles . Interestingly, the antibiotic therapy was changed for only 4 of the 18 patients whose septicemias were detected only in the 16B bottles . Finally, an in vitro study showed that certain chemotherapeutic agents can cause the inhibition of growth of several microorganisms when tested in 6B bottles . These inhibitory effects were reduced or eliminated when the same organism-drug combinations were tested in 16B bottles.

Antimicrob Agents Chemother, 1983 Oct, 24(4), 522 - 8
Phosphonopeptides as substrates for peptide transport systems and peptidases of Escherichia coli; Atherton FR et al.; Peptide transport and peptidase susceptibility of the antibacterial agent alafosfalin and other phosphonopeptides have been characterized in Escherichia coli . Phosphonodipeptides were accumulated by a process which appeared to involve multiple permeases; saturation was not achieved even at concentrations of 128 microM . Competition studies showed that these compounds had only a low affinity for the system transporting phosphonooligopeptides and were rapidly taken up by and were inhibitory to E . coli mutants unable to transport the toxic peptide triornithine . Phosphonodipeptides containing D-residues were not appreciably transported . By contrast, phosphonooligopeptides were generally transported by a distinct saturable permease system for which they had a high affinity . This system was identical to that utilized by triornithine . Phosphonooligopeptides with simple monoalkyl substituents at the amino terminus were also transported except in the case of a t-butyl substituent . The oligopeptide permease was also able to transport certain derivatives which contained some residues having D rather than L stereochemistry . Intracellular metabolism of phosphonooligopeptides was initiated almost exclusively by hydrolysis from the N terminus by an L-specific peptidase . This initial hydrolytic activity was unaffected by the aminopeptidase inhibitor bestatin, unlike the final hydrolysis step which yields L-1-aminoethylphosphonic acid from the phosphonodipeptide intermediate.

Pediatrics, 1983 Oct, 72(4), 560 - 2
Transfusion-acquired Plasmodium malariae infection in two premature infants; Piccoli DA et al.; Several diseases can be transmitted to infants via transfusion . The risk of acquiring an infection via transfusion is greatly increased in sick premature infants because they receive frequent transfusions . The full-term infant is not fully competent immunologically, and the premature infant is even less able to deal with infection . Ideally, the transfusion of infected blood, especially into immunoincompetent recipients, should not occur . However, because screening for malaria in nonendemic regions is not practical, physicians caring for sick premature babies should consider transfusion-acquired malaria as a possible cause of illness, especially when there is no response to antibacterial therapy.

Jpn J Antibiot, 1983 Oct, 36(10), 2693 - 710
{Clinical effect of a cephalosporin derivative, cefotiam, on otorhinolaryngologic infections}; Baba S et al.; CTM was administered at dose levels of 1 to 3 g a day to 77 cases of otorhinolaryngological infections, and the following results were obtained: The effect of the drug was determined in 75 cases . The responders were 3 out of 5 (60.0%) in acute suppurative otitis media, 4 out of 11 (36.4%) in chronic suppurative otitis media, 39 out of 43 (90.7%) in tonsillitis and peritonsillar abscess and 12 out of 16 (75.0%) in other diseases, a total of 58 out of 75 cases (77.3%) . The bacteriological effect of CTM was evaluated in 53 cases, and bacterial eradication was demonstrated in 41 cases (77.4%) . Also, its antibacterial potency was 2 to 4 times superior in comparison to that of CEZ against isolated bacteria in which MICs were measurable . Side effects which were neither severe nor specific were recognized in 3 out of 77 cases (3.9%) . In the cases with abnormal laboratory values, none was determinable to be attributed to CTM.

J Antibiot (Tokyo), 1983 Sep, 36(9), 1144 - 9
A new antitumor antibiotic, awamycin; Umezawa I et al.; A new antibiotic, awamycin, was isolated from the culture broth of Streptomyces sp . No . 80-217 . It appeared to belong to the quinone indicator group from results of physicochemical studies and has the empirical formula C38H49NO12S . This antibiotic possessed antibacterial and antitumor activities against Gram-positive bacteria and experimental murine tumors . The antibiotic also showed direct cytotoxic activity against HeLa cells in vitro.

J Antibiot (Tokyo), 1983 Sep, 36(9), 1201 - 4
Synthesis and biological evaluation of a 4-fluoromethyl monobactam analog; Skotnicki JS et al.; The synthesis and in vitro antibacterial activity of (+/-)(cis)-3-{2-(2-aminothiazol-4-yl)-(Z)-2-methoxyiminoacetamido}- 4-fluoromethyl-2-oxo-1-azetidinesulfonic acid, potassium salt are presented.

J Antibiot (Tokyo), 1983 Sep, 36(9), 1205 - 10
Synthetic cephalosporins . The synthesis and antibacterial activities of 7-{2-(2-(amino-1,3,4-thiadiazol-5-yl)acetamido}-cephalosporins; Sakagami K et al.; Synthesis and antibacterial activities of 7-{2-(2-amino-1,3,4-thiadiazol-5-yl)acetamido}-cephalosporins and their derivatives having the methoxyimino group at the 2-position of the 7-acyl moiety are described . These compounds are of interest as structural analogues of potent antibiotics, 7-{2-(2-aminothiazol-4-yl)acetamido}cephalosporins . 7-{2-(2-Amino-1,3,4-thiadiazol-5-yl)acetamido}cephalosporins showed comparable activity with cefazolin . Introduction of methoxyimino group to the 7-side chain resulted in a lowering of activity.

J Antibiot (Tokyo), 1983 Sep, 36(9), 1109 - 17
Northienamycin and 8-epi-thienamycin, new carbapenems from Streptomyces cattleya; Wilson KE et al.; Two new carbapenem antibiotics, northienamycin and 8-epi-thienamycin have been isolated from culture broth of Streptomyces cattleya grown under conditions for thienamycin production . The isolation, structure elucidation and in vitro antibacterial spectra of the new carbapenems are reported . In addition, comparison of the in vitro potency of the corresponding formamidine derivatives to that of MK787 is presented.

Bull Eur Physiopathol Respir, 1983 Sep-Oct, 19(5), 453 - 8
{Proteins of bronchial secretions in mucoviscidosis . Role of infection}; Jacquot J et al.; The protein composition of sputum collected by a protected method in 17 children with cystic fibrosis (CF) was analysed . The severity of the disease was assessed using the Shwachman score and the degree of bronchial superinfection was determined by a quantitative cyto-bacteriological study . The main proteins with antibacterial activity (IgA, IgG, IgM, lysozyme and lactoferrin) or reflecting the degree of bronchial inflammation (serumalbumin and alpha 1-antitrypsin) were determined by immunological methods . In the presence of severe superinfection (11 cases out of 17), the concentrations of antibacterial activity proteins are unchanged . On the other hand, the bronchial superinfection is accompanied by a marked local inflammation . In sputa, the increased concentrations of serum-derived proteins are closely correlated to the severity of the disease . This study confirms the importance of bronchial inflammation in CF.

J Oral Rehabil, 1983 Sep, 10(5), 373 - 81
Antibacterial and mechanical properties of restorative materials combined with chlorhexidines; Jedrychowski JR et al.; Chorhexidine gluconate or chlorhexidine dihydrochloride were added to a composite resin and a glass ionomer restorative material in concentrations of 0, 1, 2, 3, 5, and 10% by weight . Antibacterial activity was measured by inhibition of growth of S . viridans, S . pyogenes, S . mutans, L . acidophilus, and E . coli, for 4 days . Compressive, tensile, and restorative material-enamel adhesive shear strength tests were performed . The addition of chlorhexidine gluconate or chlorhexidine dihydrochloride increased the antibacterial activity of the composite resin and the glass ionomer restorative material and changed the mechanical properties of the restorative materials . The addition of chlorhexidine dihydrochloride resulted in mechanical properties closest to controls.

J Hand Surg {Am}, 1983 Sep, 8(5 Pt 2), 785 - 8
The management of acute thermal injuries to the upper extremity; Madden JW et al.; In summary, although thermal injuries of the upper extremity can produce permanent functional compromise, intelligent management of burns of the hands and fingers can produce fully functional and cosmetically acceptable hands . When the dorsal aspects of the hands alone are injured by thermal insult, the immediate excision of the burned tissue and replacement by split-thickness skin grafts will produce functional and esthetically satisfying results . Should immediate excision and grafting be contraindicated because of massive burns of the body, management by application of topical antibacterial agents and dressings is possible . With this treatment, carefully supervised exercises are mandatory . Revisions of hypertrophic and contracted scars can be done at a later date . The stiff and painful hand is not the direct consequence of thermally destroyed skin, but is due instead to the metabolic and biologic complications of unhealed burn wounds . It follows, therefore, that the burn illness should preferably be terminated by prompt excision of the eschar and wound closure by the application of split-thickness skin grafts.

J Antibiot (Tokyo), 1983 Sep, 36(9), 1136 - 43
The fermentation, isolation and characterization of a macromolecular peptide antibiotic: AN-3; Miyashiro S et al.; A new macromolecular peptide antibiotic, named AN-3, was isolated from the culture broth of Streptomyces albulus . From 19 liters of culture broth containing AN-3 with 90 units/ml activity, a 400 mg sample with a specific activity of 109 units/mg was obtained . Purified AN-3 gave a single band on polyacrylamide gel electrophoresis . AN-3 was a basic polypeptide with a molecular weight of 12,000 approximately 12,500 and an isoelectric point of pH 7.6 . It showed a peak of absorption at 280 nm and seemed to have no nonprotein chromophoric component . It was soluble in water but insoluble in ethanol, butanol and acetone, and was stable at pH 4 approximately 9 but unstable at pH2 . AN-3 had no antibacterial activity against Gram-positive and Gram-negative bacteria so far as tested . But, it showed a strong inhibitory effect on a macromolecule permeable mutant of Escherichia coli . It was not mutagenic . It appeared to inhibit synthesis of DNA and RNA without affecting DNA itself . It also inhibited the in vitro cell growth of L1210 and its ED50 was 5 micrograms/ml . AN-3 had antitumor activity against Lewis lung carcinoma in mouse in vivo.

J Urol, 1983 Sep, 130(3), 495 - 7
Ceftazidime, an open randomized comparison of 3 dosages for genitourinary infections; Childs SJ et al.; Ceftazidime, a new beta-lactamase resistant aminothiazo-oyl cephalosporin with a broad spectrum of antibacterial activity against gram-positive and gram-negative bacteria, including Pseudomonas species, was evaluated clinically for efficacy and safety at 3 dosage levels in patients with acute genitourinary tract infection . Sixty patients with infections, including cystitis, pyelonephritis, epididymitis and prostatitis, were assigned randomly to 1 of the 3 dosage regimens: 250, 500 or 1,000 mg . administered intramuscularly every 12 hours . Patients were evaluated bacteriologically and clinically during the course of treatment and after treatment . All patients became asymptomatic and showed clinical improvement or cure within 48 to 72 hours regardless of dosage . Bacteriological success, namely eradication of the pathogen during therapy with no recurrence of superinfection during followup, was attained in 95 per cent of the patients with uncomplicated infections and in 61 per cent of those with complicated infections . Superinfections accounted for most of the noncures, particularly with the 250 mg . regimen . The difference in success rates between the 250 mg . dosage, and the 500 mg . and 1 gm . dosages in patients with complicated infections was statistically significant . Injections were well tolerated without significant side effects . No clinically important variations in laboratory tests were observed . The results indicate that ceftazidime is a useful third generation cephalosporin for complicated and uncomplicated genitourinary infections but it is recommended that the 250 mg . dosage not be used in patients with complicated infections.

J Clin Chem Clin Biochem, 1983 Sep, 21(9), 545 - 53
Determinants of the production of active oxygen species by granulocytes and macrophages; Karnovsky ML et al.; Under certain conditions, phagocytic leukocytes generate considerable quantities of superoxide and hydrogen peroxide, as well as small quantities of hydroxyl radical and singlet oxygen . These activated forms of oxygen are involved in the antibacterial, antiparasitic and antitumour functions of the cells . Important factors in the production of the different oxygen species are the nature of the stimulant and the animal species from which the cells are derived; in addition, macrophages exist in various metabolically modulated states within the organism . The oxidases involved in this process are localized in the leukocyte plasmalemma, where they catalyse the oxidation of reduced pyridine nucleotides; a cytochrome may also be involved in the electron transport . Other oxidases are also present in certain species; for example, guinea pig cells contain aldehyde oxidase . Active forms of oxygen can attack bacteria and other foreign bodies inside the phagocytic vacuole or outside the cell . Peroxidase may play a critical role, chiefly in granulocytes . In this kind of multienzyme system, it is self evident that different genetic defects can lead to the same phenotypic end results, e.g . Chronic Granulomatous Disease in children, and other biochemical disorders.

Am J Med, 1983 Aug 29, 75(2A), 54 - 9
Amdinocillin pharmacokinetics . Simultaneous administration with cephalothin and cerebrospinal fluid penetration; Gambertoglio JG et al.; In the treatment of serious infections, combinations of beta-lactam antibiotics are being utilized in order to avoid aminoglycoside toxicity and to achieve antibacterial synergy . The pharmacokinetic disposition of amdinocillin and cephalothin was determined, when administered alone or in combination to healthy volunteers, as well as the penetration of amdinocillin into human cerebrospinal fluid . Six subjects received, on separate occasions, single intravenous doses of amdinocillin 10 mg/kg, cephalothin 15 mg/kg, or a combination of the two in the same doses . The elimination half-lives of amdinocillin and cephalothin are increased when these drugs are given simultaneously, compared with when they are administered alone . However, no significant differences were observed . When they were given in combination, no significant changes in plasma clearance, renal clearance, or steady-state volume of distribution were found . Eight patients undergoing lumbar puncture for various neurologic disorders without inflamed meninges received a single dose of 10 mg/kg amdinocillin intravenously . One to two hours later, simultaneous plasma and cerebrospinal fluid samples were obtained . The concentration of amdinocillin in the cerebrospinal fluid ranged from approximately 1 to 10 percent of concomitant plasma concentrations . Thus, amdinocillin penetrates in the cerebrospinal fluid in marginal amounts in the absence of meningeal inflammation.

J Med Chem, 1983 Aug, 26(8), 1122 - 6
Synthesis and antibacterial activity of some 3-{(alkylthio)methyl}quinoxaline 1-oxide derivatives; Dirlam JP et al.; Some 3-{(alkylthio)methyl}quinoxaline 1-oxide derivatives (1) have been synthesized and screened for antibacterial activity . 2-Acetyl-3-{(methylsulfonyl)methyl}quinoxaline 1-oxide (7a) was found to possess good in vitro activity against some pathogens important to veterinary medicine including Treponema hyodysenteriae, a causative agent in swine dysentery . In an in vivo experiment, this compound (7a) completely protected pigs against a swine dysentery challenge over a 21-day period.

Chir Ital, 1983 Aug, 35(4), 484 - 8
{Prevention of infection in thyroid surgery}; Sussi PL et al.; The Authors remark the clear infections are rare in thyroid surgery, whereas rather frequent are the light phlogistic forms, appearing through thermal movement, slight oedema and reddening of the cutaneous wound, drainage emergency point and upper cutaneous edge, which may make the postoperative course unideal . They report the observations done on 25 patients who underwent operation of thyroidectomy after preparation of skin, the evening before operation, with detergent and antiseptic solution containing cetrimide and chlorexidin, followed by dressing with alcoholic solution of quaternary ammonium salts . The patients were immediately treated before and after 8 and 16 hours from operation with amoxicillin . The results obtained confirm the validness of proximate antibacterial chemoprophylaxis in this surgery too.

Jpn J Antibiot, 1983 Aug, 36(8), 2081 - 92
{Clinical evaluation of latamoxef, an oxacephem antibiotic with special reference to transport of latamoxef into the lung tissues and prevention of postoperative infections after thoracotomy}; Imaizumi M et al.; There are few clinical reports about concentration of latamoxef (LMOX) in lung tissues . At present, clinically, we report a concentration of LMOX in serum and lung tissues on 21 patients of chest disease and a study of the administration schedule of LMOX for prophylaxis of postoperative infections on 31 operated patients with chest disease . Our results are the followings: The peak concentration of LMOX in serum is 77.4 micrograms/ml at 1 hour after starting drip infusion of LMOX 1 g . The concentration of LMOX in lung tissues is from 25% to 50% of serum level . LMOX is more useful to prophylaxis of postoperative infections after thoracotomy than cephalothin, especially in case of administration of LMOX just before operation . No side effects of LMOX are noted in our cases . LMOX has wide antibacterial activity against various clinical isolates and is useful to treatment of postoperative infections.

Jpn J Antibiot, 1983 Aug, 36(8), 2077 - 80
{Transfer of piperacillin into the body water and gallbladder tissue in cholestasis}; Kitou M et al.; Acute inflammation becomes severe and the risk of perforation of the gallbladder increases every time gall stone colic occurs in patients with cholelithiasis . In the surgical treatment for these patients, interval operation is said to be preferable to emergency operation in the acute stage . Furthermore, the flow of bile into gallbladder is blocked by incarceration of stones at the neck of the gallbladder and other causes in the acute stage . In this case, therefore, how an antibacterial agent in blood moves to the gallbladder wall is important in suppressing infections of the gallbladder wall . We divided 15 patients with cholelithiasis into cases positive for cholecystogram and negative cases and made a comparative study of piperacillin (PIPC) levels after intravenous drip infusion . PIPC level in bile in the gallbladder was very low in the cases negative for cholecystogram compared with the positive cases . However, no definite difference in levels of the gallbladder tissue was observed between positive for cholecystogram and negative cases . Accordingly, it is concluded that administration of PIPC is not ineffective even in severe cholecystitis in which transference of an antibacterial agent from bile can hardly be expected.

Jpn J Antibiot, 1983 Aug, 36(8), 2103 - 8
{Evaluation of in vitro antibacterial potencies of oral antibiotics against sputum isolates}; Yamada H et al.; Susceptibility of 162 sputum isolates to oral antibiotics was measured by an agar dilution method . The sputum isolates included S . pneumoniae 25 strains, S . aureus 30 strains, H . influenzae 37 strains, K . pneumoniae 51 strains and E . coli 19 strains . Minimal inhibitory concentration (MIC) values of cefaclor (CCL), cephalexin (CEX), ampicillin (ABPC) and minocycline (MINO) were measured for each strains . Eighty percent of S . pneumoniae strains were inhibited at 0.024 to 0.05 micrograms/ml of ABPC, 0.39 to 0.78 micrograms/ml of CCL, and 1.56 to 3.13 micrograms/ml of CEX and MINO . ABPC, CCL and CEX were considered to be effective clinically when they were used with the usual dosage . However, about 30% of strains were resistant to the usual dosage of orally administrated MINO . Eighty percent of S . aureus strains were inhibited at 0.20 to 0.39 microgram/ml of MINO and 3.13 to 6.25 micrograms/ml of the other 3 drugs . MINO is the most effective with the usual dosage . Twenty to 40% of strains showed resistance to CCL, CEX and ABPC . Eighty percent of H . influenzae strains were inhibited at 0.39 micrograms/ml of ABPC, 0.78 to 1.56 micrograms/ml of MINO, 3.13 micrograms/ml of CCL and 12.5 to 25 micrograms/ml of CEX . ABPC should be selected as the first choice antibiotic . However, there were 2 ABPC-resistant strains that were highly susceptible to CCL . Eighty percent of K . pneumoniae strains were inhibited at 0.39 to 0.78 micrograms/ml of CCL, 3.13 to 6.25 micrograms/ml of MINO and CEX, and 12.5 to 25 micrograms/ml of ABPC . CCL seemed to be only effective oral antibiotic for K . pneumoniae infection.(ABSTRACT TRUNCATED AT 250 WORDS)

Obstet Gynecol, 1983 Aug, 62(2), 137 - 44
Prematurity: infection as an etiologic factor; Minkoff H; Preterm delivery accounts for a substantial percentage of perinatal mortality and morbidity . A large body of evidence suggests that perinatal infections may play an etiologic role in preterm rupture of membranes and preterm labor . The interaction between a patient's vaginal flora and her local defense mechanisms (antibacterial activity of amniotic fluid and cervical mucus) may help determine who delivers prematurely . The evidence implicating infection as a cause of labor is reviewed, and the organisms which may be responsible are identified . Potential avenues of investigation and intervention are outlined which would delineate the role of infections in preterm delivery and lead to a means of preventing some preterm deliveries caused by infection.

J Antibiot (Tokyo), 1983 Aug, 36(8), 1007 - 12
Configuration of the methoxyimino group and penetration ability of cefotaxime and its structural analogues; Costa A et al.; Among the different mechanisms by which bacteria are resistant to beta-lactam antibiotics, three are of major interest: production of beta-lactamase, modifications of the target penicillin-binding proteins (PBPs) and decreased permeability . Cefotaxime (CTX) is a recently synthesized cephalosporin derivative, active against beta-lactamase producing Gram-negative bacteria and possessing in the acylamino side chain a methoxyimino group in the syn-configuration . It has been compared for affinity to PBPs and penetration ability with its isomer possessing the same group in the anti-configuration and the corresponding demethoxyimino derivative . The anti-isomer, although resistant to beta-lactamase, is devoid of antibacterial activity (MIC for Escherichia coli higher than 500 micrograms/ml) . The affinities of CTX and its analogues for the PBPs of several strains of E . coli have been determined in vivo and in vitro by competition experiments using intact cells and bacterial envelopes, respectively . Only minor differences in the affinity for the target PBPs were detected in vitro . However, in vivo studies proved that the 50% saturating concentrations for the PBPs were more than 100-fold higher for the anti-isomer than for CTX . The reported results suggest that a very simple structural modification of the CTX molecule greatly decreases the penetration ability of the antibiotic through the outer cell layers, thus dramatically affecting its antibacterial properties.

Acta Odontol Scand, 1983 Aug, 41(4), 227 - 40
Ultrastructural study of induced keratinization in sulcular gingival epithelium in rhesus monkeys; Kristoffersen EK et al.; Gingival sulcular epithelium--which in primates normally does not keratinize--can be induced to undergo keratinization by prolonged intensive antibacterial therapy . Three months before biopsy the teeth of two adult male rhesus monkeys were scaled and polished, and for 5 days the monkeys were given intravenous injections of 75 mg Achromycin daily . Their teeth were subsequently subjected to daily cleaning and polishing . The presumably in-situ-keratinized sulcular epithelium was examined by transmission electron microscopy . It was also compared with oral gingival epithelium from the same two animals and with oral and sulcular epithelium from a rhesus monkey that had not been exposed to local or systemic antibacterial therapy . The results confirmed earlier histological studies, which have shown that under the conditions described the sulcular epithelium becomes parakeratinized . In addition, several other ultrastructural changes were observed, some of which suggest that the treatment given may result in the formation of a more efficient permeability barrier in the sulcular area . The possible clinical significance of such a barrier is briefly discussed.

Klin Wochenschr, 1983 Aug 1, 61(15), 723 - 36
The biological properties of immunoglobulin G and its split products {F(ab')2 and Fab}; Sedlacek HH et al.; Antibodies of the IgG class possess antibacterial, antiviral and toxin neutralizing properties and for this reason are administered prophylactically and therapeutically . In the case of the immunoglobulin preparations commercially available for i.v . application a basic distinction must be made between unsplit immunoglobulins and those antibody preparations obtained by enzymatic digestion, such as F(ab')2 or Fab antibodies . This survey deals with the largely experimental evidence describing the biological properties of these preparations . Administration of antibodies in the presence of the corresponding antigens leads to the formation of immune complexes in the organism . These immune complexes can activate, either directly or indirectly, the cellular and humoral systems which are involved in phagocytosis and the elimination of antigens, in the regulation of the body's own antibody production and in inflammatory reactions . As a result of their inability to interact with Fc receptors, immune complexes with F(ab')2 or F(ab) antibodies appear to be less active in the release of inflammation mediators from leucocytes and thrombocytes than immune complexes with unsplit immunoglobulins . These, on the other hand, can antigen-specifically and non-antigen-specifically suppress the immune system which is not the case for immune complexes with F(ab')2 or Fab antibodies . There are indications that these split products also occur in vivo due to the action of tissue and leucocyte proteases . Unlike Fab preparations, F(ab')2 antibodies have antibacterial and antiviral potencies similar to unsplit immunoglobulins, which is probably due to the ability of F(ab')2 molecules to activate complement, not by the classical but by the alternative pathway . Like Fab preparations, F(ab')2 molecules appear to be superior to unsplit IgG in the elimination of haptens . On account of the relatively long period of time unsplit immunoglobulins remain in the blood, they are well suited for prophylactic treatment and substitution over longer periods . The extent to which indications, obtained predominantly from experimental studies, of a reduced release of inflammation mediators, a lack of immune suppression and a lack of augmentation of IgG catabolism would advocate the use of F(ab')2 split products, especially for therapeutic purposes, can only be ascertained after prospective and comparative studies have been carried out.

Minerva Med, 1983 Jul 14, 74(28-29), 1765 - 70
{Piperacillin: microbiological and clinical studies}; Soranzo ML et al.; A microbiological and clinical study of the action of piperacillin is presented . The drug showed an excellent in vitro antibacterial action on gram positive and gram negative microorganisms . Its in vitro action on Ps . aeruginosa (70.8% of strains inhibited) was also extremely interesting, making it the second most effective of the antibiotics tested after polymyxin B and colistin, polypeptides unsuitable for clinical use . In vivo, the administration of piperacillin achieved a clinical and bacteriological cure in 35 out of 40 patients and a clinical cure in 2 out of 40 . It was only therapeutically unsuccessful in 3 cases . It is concluded that its microbiological, kinetic and tolerance features make piperacillin suitable for a wide range of therapeutic purposes.

Cornell Vet, 1983 Jul, 73(3), 225 - 39
Growth, cultural characteristics, and antibacterial sensitivity of Leptospira interrogans serovar hardjo; Ellinghausen HC Jr; Nutrient requirements of Leptospira interrogans serovar hardjo were investigated using a 1% bovine serum albumin (BSA) medium, supplemented separately with polysorbates (Tweens) 80, 60, 40, 20, NH4Cl, and vitamins thiamine and cyanocobalamin (vitamin B12) . L . hardjo was tested in vitro against 30 antibacterial compounds incorporated into semisolid medium (0.2% agar) at 3 compound concentrations . Growth was superior in polysorbate 80 (oleic acid rich) and polysorbate 40 (palmitic rich) media . A linear growth response to vitamin B12 could be shown . Hamster isolates all required thiamine and vitamin B12 for growth . The antibacterial compounds could be classed as: 100% bacteriocidal, bacteriocidal at the 2 highest concentrations, bacteriocidal at only 1 concentration, and completely noninhibitory . The tetracyclines were strongly bacteriocidal . The comparative growth rates of hamster isolates were much reduced when compared to the type strain hardjoprajitno . These studies were performed acknowledging that the polysorbates were mixtures of fatty acids . Nephelometry was used as an accepted method to monitor the synthesis of leptospiral cell mass.

Jpn J Antibiot, 1983 Jul, 36(7), 1615 - 20
{Antibacterial peptides (18) . Synthesis and antibacterial activity of alpha-acyltetrapeptides containing basic amino acids (7)}; Kurihara T et al.; Three kinds of (formula; see text) were synthesized to investigate the relationship between the chemical structure and the antibacterial activities by acylation of the corresponding tetrapeptides . Acyl chlorides of (+)-6-Methyloctanoic acid (a component of colistin) and two kinds of other organic acid were employed as acylating agents . It was proved that one of three, (formula; see text) shows antibacterial activity against four kinds of Gram-negative bacteria and against Gram-positive bacteria, but that the other only have weak antibacterial activity.

Vestn Khir Im I I Grek, 1983 Jul, 131(7), 3 - 10
{Major trends in the treatment of patients with septic shock}; Lytkin MI et al.; The authors formulate main tasks to be solved which will result in successful treatment of septic shock in the surgical clinic . Choice of the methods affecting the septic focus is determined including measures from the rational systemic antibacterial therapy to interventions on the focus with its ablation or draining . The infusive and medicamentous programs are formulated, debatable questions in the treatment of such patients are discussed on the basis of the personal experience: the application of vasoactive drugs, corticosteroids, heparin.

J Antimicrob Chemother, 1983 Jul, 12(1), 39 - 45
Pharmacokinetics of N-formimidoyl thienamycin and influence of a renal dipeptidase inhibitor in experimental meningitis; Washburn DE et al.; We studied the pharmacokinetics of N-formimidoyl thienamycin with and without a renal dipeptidase inhibitor in plasma and cerebrospinal fluid (CSF) of rabbits . Thienamycin reached a maximal concentration of 0.6 +/- 0.06 mg/l in the CSF of normal rabbits . When the meninges were inflamed, the mean CSF concentration of N-formimidoyl thienamycin was 3.2 +/- 1.5 mg/l, five times higher than in normal rabbits . This concentration would kill most bacteria that cause meningitis . The renal dipeptidase inhibitor alone had no detectable antibacterial activity . When administered with N-formimidoyl thienamycin, it exerted only minor effects on the pharmacokinetics in either plasma or CSF of normal or infected rabbits.

J Antibiot (Tokyo), 1983 Jul, 36(7), 846 - 54
Studies on beta-lactam antibiotics . VII . Effect on antibacterial activity of the oxime O-substituents with various functional groups in the 7 beta-{(Z)-2-(2-amino-4-thiazolyl)-2-oxyiminoacetamido}cephalosporins; Takasugi H et al.; The synthesis and in vitro activity of the 7-{O-substituted oxyiminoacetamido}cephalosporins (I) without substitution at 3-position of a cephem nucleus are described . Effect of changing the oxime O-substituents (R1) with various functional groups in the 7-acyl residue on antibacterial activity was examined . Against Gram-positive bacteria, cephems with hydrophilic functions in the R1 moiety such as hydroxyethyl, aminoethyl and carboxymethyl groups showed decrease of the activity, while cephems with lipophilic functions such as cyanomethyl, methylthiomethyl and halogenoethyl groups exhibited increase of the activity . However, influence of the substituents (R1) on activity against Gram-negative bacteria was observed to be relatively independent of the nature of their functional groups.

Sem Hop, 1983 Jun 30, 59(26), 1977 - 80
{The French experience with moxalactam in pneumology}; Leng B et al.; Twenty-nine patients, aged 19 to 87, were treated for an infection of the lower respiratory tract (pneumonia, bronchopneumonia, bronchitis, pulmonary abscess, pleuritis) due to a pathogen with in vitro sensitivity to the antibiotic (pneumococcus, hemophilus, anaerobic organisms . . .) . Patients were given Moxalactam as the only antibacterial treatment . In most instances, excellent results (24 successes, i.e . 84% of cases) were recorded with two daily intramuscular injections of 1 g each . Biologic tolerance was satisfactory . Possible clinical side-effects are rashes and local pain during the injection . We conclude that Moxalactam is very effective in severe lower respiratory tract infections, with a daily dosage of 30 mg/kg.

Pharm Weekbl Sci, 1983 Jun 24, 5(3), 81 - 7
Antibacterial drugs and their interference with the biogenesis of mitochondria in animal and human cells; Kroon AM et al.; Mitochondrial RNA and protein synthesis in mammalian cells is sensitive to inhibition by a variety of antibiotics which are used in medical practice . In spite of the intrinsic sensitivity of the synthetic processes to these drugs it appears that inhibition in intact cells and living organisms is not observed in all cases because the cellular membranes may act as barriers which prevent the antibiotics from reaching their intramitochondrial targets . This holds for the rifamycins, the lincomycins and a number of macrolides, but not for chloramphenicol and its analogues . Some of the toxic side-effects of the latter antibiotics can be related to their antimitochondrial action . For the tetracyclines selectivity in permeability exists in the sense that some cell types are permeable and other are not . The hypothesis is developed that the deliberate inhibition of mitochondrial protein synthesis in vivo may lead to cell proliferation arrest and offer a device in combined modality treatments of malignant growths . This hypothesis is supported by the results of two studies with experimental tumour models in rats and by retrospective and prospective clinical data.

Biochem J, 1983 Jun 1, 211(3), 727 - 34
Purification and characterization of an antibacterial protein from haemolymph of Sarcophaga peregrina (flesh-fly) larvae; Okada M et al.; Three antibacterial proteins were induced when the body wall of Sarcophaga peregrina (flesh-fly) larvae was injured with a hypodermic needle . These proteins were separated and one was purified to homogeneity . The molecular weight of the purified protein was 5000 and its amino acid composition was similar to that of cecropins, which are antibacterial proteins in Hyalophora cecropia (cecropia moth) pupae . This protein was found to have bactericidal activity and to be effective at a concentration of 0.1 micrograms/ml against certain Gram-negative and Gram-positive bacteria.

J Pharm Sci, 1983 Jun, 72(6), 705 - 7
NMR studies and GC analysis of the antibacterial agent taurolidine; Knight BI et al.; The NMR spectrum of taurolidine in deuterium oxide was compared with spectra obtained from model experiments with amines and formaldehyde . Head-space analysis combined with capillary GC showed that there was less than 0.004% free formaldehyde present in 2% solutions of taurolidine . This value is comparable to the concentration of formaldehyde found when the taurolidine solutions were injected directly onto GC columns.

J Clin Microbiol, 1983 Jun, 17(6), 1156 - 8
Comparison of the antibacterial spectra of cephalexin and cefaclor with those of cephalothin and newer cephalosporins: reevaluation of the class representative concept of susceptibility testing; Preston DA et al.; The validity of the class representative concept for in vitro susceptibility testing of older cephalosporins was reevaluated . Two oral cephalosporins, cephalexin and cefaclor, were compared with the established cephalosporin class representative, cephalothin, by using reference microdilution minimal inhibitory concentrations of 528 isolates of a wide variety of gram-positive and gram-negative bacterial pathogens . For each comparison, there were only 15 (2.8%) random major and very major interpretive discrepancies . Additional comparisons confirmed the need to test second-generation (cefamandole) and third-generation (cefotaxime) cephalosporins separately . These results provide reasonable assurance that the use of cephalothin as an in vitro predictor of qualitative bacterial susceptibility to these two oral cephalosporins remains an acceptable alternative to testing each antibiotic individually.

J Appl Bacteriol, 1983 Jun, 54(3), 409 - 16
A selective and indicative medium for groups of Penicillium viridicatum producing different mycotoxins in cereals; Frisvad JC; A medium, pentachloronitrobenzene-rose bengal-yeast extract-sucrose agar (PRYES), for the isolation of moulds occurring during storage of cereals has been developed and compared with other selective media . The basal medium is yeast extract agar containing 15% sucrose (w/v) . In addition to the sucrose content further selective measures include the addition of antibacterial antibiotics chloramphenicol and chlortetracycline (50 mg/l), the fungicides rose bengal (25 mg/l each), and pentachloronitrobenzene (1 g/l) and a low incubation temperature (20 degrees C) . Members of the Mucorales were completely inhibited, and fast-growing species of other moulds were slightly inhibited, allowing important storage moulds to develop . The important ochratoxin A and citrinin-producing Penicillium viridicatum group II was indicated by a typical violet brown reverse on PRYES . Producers of xanthomegnin and viomellein (P . viridicatum group I and P . aurantiogriseum) were indicated on PRYES by their yellow reverse and obverse colours . The medium was used for screening 40 samples of barley, and moulds with the characteristic colours were all identified as the species mentioned above.

J Med Chem, 1983 Jun, 26(6), 891 - 5
3'-Amino-2',3'-dideoxyribonucleosides of some pyrimidines: synthesis and biological activities; Krenitsky TA et al.; 3'-Amino-2',3'-dideoxyribonucleosides of thymine, uracil, and 5-iodouracil (1-3) were synthesized from the corresponding 2'-deoxyribonucleosides via the threo-3'-chloro and the erythro-3'-azido derivatives . Corresponding aminonucleosides of 5-bromouracil, 5-chlorouracil, and 5-fluorouracil (4-6) were synthesized enzymatically with 3'-amino-2',3'-dideoxythymidine as the aminopentosyl donor and thymidine phosphorylase (EC 2.4.2.4) as the catalyst . 3'-Amino-2',3'-dideoxycytidine (7) was synthesized by amination of the 3'-azido precursor of 3'-amino-2',3'-dideoxyuridine . The biological activity of 3'-amino-2',3'-dideoxy-5-fluorouridine (6) was notable among this group of aminonucleosides . It had an ED50 of 10 microM against adenovirus and was not appreciably cytotoxic to mammalian cells in culture . It also had activity against some Gram-positive bacteria but not against a variety of Gram-negative bacteria . The other aminonucleosides (1-5 and 7) lacked or exhibited weak antiviral and antibacterial activities . The only compounds in this group that were appreciably toxic to mammalian cells in culture were the thymidine and deoxycytidine analogues (1 and 7).

J Infect Dis, 1983 Jun, 147(6), 1011 - 7
Bactericidal and opsonic activity of ascitic fluid from cirrhotic and noncirrhotic patients; Akalin HE et al.; Cirrhotic patients with ascites are highly susceptible to spontaneous bacterial peritonitis . Patients with ascites due to causes other than cirrhosis very seldom develop peritonitis . The antibacterial activity of these ascitic fluids is not known . The present study was undertaken to evaluate the bactericidal and opsonic activity in ascitic fluid from patients with and without cirrhosis and in normal (nonascitic) peritoneal fluid . Normal peritoneal fluids of 20 control subjects and ascitic fluids of 22 patients with noncirrhotic ascites all had normal bactericidal activity . The bactericidal activity of ascitic fluid was diminished in all 25 patients with cirrhosis (P less than 0.00005 by Fisher's exact test) . Similar results were found when opsonic activity was evaluated . Complement and immunoglobulin concentrations in cirrhotic ascites were significantly lower than those in the other two groups . The present study demonstrates that noncirrhotic ascitic fluid has antibacterial activity similar to normal peritoneal fluid, whereas cirrhotic ascitic fluid has a marked reduction of both bactericidal and opsonic activities . These defects may explain the high incidence of peritonitis in cirrhotic patients.

Obstet Gynecol, 1983 Jun, 61(6), 757 - 60
Necrotizing fasciitis and progressive bacterial synergistic gangrene of the vulva; Meltzer RM; Necrotizing fasciitis and progressive bacterial synergistic gangrene are two infrequently reported diseases in the gynecologic literature . The author reports 2 cases highlighting the many similarities and some important differences between these clinical entities . Diabetes mellitus and arteriosclerosis predispose women to both diseases . Aggressive antibacterial and surgical treatment is imperative.

Arch Ophthalmol, 1983 Jun, 101(6), 958 - 60
Antibacterial effect of cyanoacrylate glue; Eiferman RA et al.; Enbucrilate (butyl-2-cyanoacrylate; Histoacryl {West Germany}, no comparable US product) is a tissue adhesive used in the management of corneal perforations that may have a therapeutic value in suppressing selective pathogens isolated, from corneal infections . In three patients with confirmed corneal infections, varying degrees of inhibition were observed . Bacteriostatic activity was most pronounced against gram-positive microorganisms, and no activity was observed against gram-negative organisms . It appears that this chemical adhesive provided an ancillary means of promoting healing of corneal perforations.

Vestn Khir Im I I Grek, 1983 Jun, 130(6), 58 - 63
{Regional infusion and superselective embolization in organ-preserving surgical treatment of kidney diseases}; Shapkin AG et al.; The authors describe the method of regional continuous infusion into the renal artery of antibacterial cocktails used in 8 patients (cavernous tuberculosis of the kidney in 4 patients, purulent injury of the parenchyma in 4 patients) and the method of superselective embolization of the renal artery branches before the organ-preserving operation performed in 2 patients.

J Cell Biol, 1983 Jun, 96(6), 1651 - 61
A novel type of cytoplasmic granule in bovine neutrophils; Gennaro R et al.; We obtained cell preparations containing greater than 95% neutrophils from freshly drawn bovine blood . The cells were suspended in sucrose and disrupted in a Dounce homogenizer, and the postnuclear supernate was fractionated by zonal differential sedimentation and by isopycnic equilibration . The subcellular fractions were characterized biochemically by testing for marker enzymes and other constituents known to occur in azurophil and specific granules of other species, and by electrophoretic analysis of extracts of the particulate material . In addition, each fraction was examined by random-sampling electron microscopy . We found that bovine neutrophils contain in addition to azurophil and specific granules a third type of granule, not known to occur in neutrophils of other species . These novel granules are larger, denser, and considerably more numerous than the two other types . Except for lactoferrin, they lack the characteristic constituents of azurophil granules (peroxidase, acid hydrolases, and neutral proteinases) and of specific granules (vitamin B12-binding protein) . Instead, they contain a group of highly cationic proteins not found in the other granules, and they are the exclusive stores of powerful oxygen-independent bactericidal agents . We studied the fate of the large granules in bovine neutrophils exposed to opsonized particles, the ionophore A 23187, or phorbol myristate acetate . The appearance in the cell-free media of antibacterial activity and of the characteristic highly cationic proteins as revealed by electrophoresis was monitored and compared with the release of azurophil and specific granule markers . In addition, changes of the relative size of the large granule compartment induced by phagocytosis were assessed by morphometry . The results show that exocytosis of the large granules occurs following both phagocytosis and exposure to soluble stimuli . Like the specific granules, the large granules appear to be discharged by true secretion under conditions where the azurophil granules are fully retained.

Int J Lepr Other Mycobact Dis, 1983 Jun, 51(2), 225 - 34
The interpretation of the ultrastructure of mycobacterial cells in transmission electron microscopy of ultrathin sections; Silva MT et al.; In the present report the authors discuss several aspects of the ultrastructure of mycobacterial cells as seen by transmission electron microscopy of ultrathin sections that are relevant in the characterization of normal versus altered bacteria . The importance of the use of adequate fixation conditions is stressed and illustrated with examples showing that normal, but inadequately fixed, mycobacterial cells may exhibit micromorphological alterations similar to those typical of cells affected in several situations such as autolysis, heterolysis, and antibacterial treatments.

Infect Immun, 1983 Jun, 40(3), 967 - 76
Inhibition of neutrophil function by fluid phase C3b of complement; Ogle JD et al.; A high-molecular-weight fragment of C3 was isolated from normal human serum by column chromatography, was generated by incubation of serum at 37 degrees C with inulin, and was produced from highly purified C3 by limited digestion with trypsin . This product was shown to inhibit the antibacterial function of neutrophils by using Escherichia coli O75 as the main test organism . The inhibitor reacted with anti-C3b and anti-C3c, but not with anti-C3B (anti-native C3) or anti-C3a . The manner of preparation of the inhibitor, the sodium dodecyl sulfate-polyacrylamide gel electrophoresis pattern, and the amino acid composition of the inhibitor indicated that it was fluid phase C3b . The inhibitor of neutrophil function (fluid phase C3b) was shown to bind to C3b receptors or acceptors on sheep erythrocytes in a model system.

Antibiotiki, 1983 May, 28(5), 358 - 62
{Antibacterial prevention of suppurative complications after operations on the large intestine}; Kuzin MI et al.; The data on comparative study of complications after operations on the large intestine are presented . During the preoperative period, 62 patients of the control group were treated with phthalylsulfathiazole, nevigramon and nystatin . Thirty-nine patients of the test group were treated with metronidazole and kanamycin monosulfate . Kanamycin monosulfate was used 3 days before the operation in a dose of 0.5 g orally 4 times a day whereas metronidazole in a dose of 0.5 g 3 times a day . The last doses of the drugs were administered 4-5 hours before the operation . After the operations the patients were treated with kanamycin sulfate for 3-5 days in a daily dose of 2 g intramuscularly . The number of the postoperative suppurative complications decreased from 22 to 5 per cent . No lethal outcomes were registered in the test group . The number of lethal outcomes in the control group amounted to 8 per cent.

J Antimicrob Chemother, 1983 May, 11(5), 481 - 4
Temocillin elimination in patients with varying degrees of renal failure; Wright N et al.; Temocillin is a new penicillin combining activity against Gram-positive organisms, beta-lactamase stability and an exceptionally long half-life . In patients with normal renal function the half-life was approximately 4-6 h and this increased to 30 h in patients with severe renal failure . It is suggested that unlike other penicillins this compound may give adequate antibacterial concentration with once daily dosing in subjects with normal renal function; this will certainly require reduction in subjects with severely impaired renal function.

J Antimicrob Chemother, 1983 May, 11(5), 427 - 33
The fractional inhibitory concentration (FIC) index as a measure of synergy; Hall MJ et al.; The value of the FIC index as a predictor of synergy has been investigated using the antibacterial agents alafosfalin and cephalexin combined together with themselves in fully blind experiments . Under the conditions used, even weak interaction (FIC index 0.5-0.99) proved to be statistically highly significant . The use of such fully controlled blind studies would greatly enhance the credibility of many of the claims of synergy published in the literature . The representation of results as average isobolograms is only of value with combinations which show moderate to strong interaction.

HNO, 1983 May, 31(5), 180 - 2
{Bremen nose ointment--a new boric acid-free nasal ointment}; Maiwald J et al.; Drug treatment containing boric acid, has not been permitted with the exception of ophthalmological preparations, since 1.6.1981 . Attention is brought to possible complications during treatment with the well-known boric acid containing Wittmaack'sche Nasensalbe . In preparing a new unguent for the nose we took Chlorhexidindiacetat as an antiseptic . The antibacterial and toxicological features of Chlorhexidindiacetat are mentioned . Different therapeutical possibilities of this new nose unguent are listed.

Tijdschr Diergeneeskd, 1983 May 1, 108(9), 350 - 8
{Treatment of bacterial infections in commercial poultry}; Goren E; Several aspects of antibacterial drug therapy in poultry are reviewed and field as well as experimental findings are reported . The relatively very brief elimination half-life of antibacterial agents in poultry and the fact that the entire flock is treated orally during a short period accounts for the fact that a satisfactory therapeutic effect is only achieved in a limited number of systemic diseases . In view of the findings reported, a re-assessment of possibilities and limitations of antibacterial therapy in this field is recommended.

Arch Ophthalmol, 1983 May, 101(5), 764 - 5
Chemical preparation of the eye in ophthalmic surgery . II . Effectiveness of mild silver protein solution; Isenberg S et al.; Although a mild silver protein solution (Argyrol) has been used for a number of years and is still used by many ophthalmic surgeons, its efficiency as an antibacterial agent on the conjunctiva has not been scientifically evaluated as part of the preoperative chemical preparation of the eye . We studied the effectiveness of a mild silver protein solution on the conjunctival flora of 32 patients in a masked fashion . By bacteriologic analysis, the mild silver protein solution was found to be no more effective in reducing the number of species and colonies in the treated eye than in the untreated eye . While the mild silver protein solution does stain mucus and other debris on the eye to facilitate irrigation, this study did not demonstrate a significant bactericidal effect.

Jpn J Antibiot, 1983 May, 36(5), 939 - 55
{Fundamental and clinical studies of T-1982 (cefbuperazone) in the field of obstetrics and gynecology}; Cho N et al.; T-1982 (cefbuperazone), a new cephamycin antibiotic, was studied for its MICs against clinical isolates, transfer into uterine tissues and clinical efficacy in the field of obstetrics and gynecology . The following results were obtained . The MICs of T-1982 were measured against 397 strains of 13 species . In antibacterial activity, T-1982 was equal to CTT but inferior to CMZ against Gram-positive bacteria . Against Gram-negative bacteria, T-1982 was superior to CEZ and other cephamycin antibiotics, i.e . CMZ and CTT . The activity of T-1982 was almost equal to that of CMZ and superior to that of CTT against B . fragilis . T-1982 concentrations in various uterine tissues attained the peaks of 16.8-35.9 micrograms/g at 34 minutes after intravenous administration of 1 g, the tissue/serum ratios being 34-72% . The tissue concentrations were about 3-4 micrograms/g even at 5-5.5 hours after administration . T-1982 was intravenously administered at a dose of 1 g twice daily to 5 cases with obstetrical and gynecological infections . All the cases responded to the therapy . Elevated GOT and GPT were observed in 1 case, but they returned to normal on 8 days after the therapy.

Zh Vopr Neirokhir Im N N Burdenko, 1983 May-Jun, (3), 26 - 9
{Surgical treatment of bedsores with blind suture and active drainage in spinal cord lesions}; Livshits AV et al.; Operations were performed on 32 patients for persistent bedsores of different localization . The operative technique included plastic surgery of the bedsore with prolonged irrigation of the postoperative wound with solutions of antibacterial agents . In 75% of cases the wound healed by first intention, in 85% the bedsores healed within one month . The operative technique described may be recommended for use on a wide scale in patients with injury to the spinal cord.

Hautarzt, 1983 May, 34(5), 203 - 8
{Antibacterial treatment of bacteria-abundant leprosy}; Klokke AH; A historic introduction reviews the start of DDS (diaminodiphenylsulphone) therapy in leprosy, stressing the fact that, far after the start of combined therapy in tuberculosis, leprosy continued to be treated with monotherapy of DDS . Reports about resistance of M . leprae to DDS initiated a review of policy . A complete breakthrough toward combined therapy started after 1962, when Shepard introduced mousefootpad inoculation of M . leprae to be used for therapeutic trials . Full attention is given to Freerksen's trial in Malta where combined treatment with rifampicin, INH, prothionamide, and DDS were given for 2 years only to all patients, while at resurvey after 4 years no relapse was found . The applicability of short-term combined therapy for endemic areas is discussed.

J Med Chem, 1983 May, 26(5), 667 - 73
2,4-diamino-5-benzylpyrimidines and analogues as antibacterial agents . 6 . A one-step synthesis of new trimethoprim derivatives and activity analysis by molecular modeling; Stuart A et al.; A new route to 2,4-diamino-5-(4-hydroxybenzyl)pyrimidines has been developed that involves the condensation of 2,4-diamino-5-(hydroxymethyl)pyrimidine with phenols in acidic medium . The use of phenol and its 2,6-dialkyl derivatives produces 5-(4-hydroxybenzyl)pyrimidines exclusively . However, 2,6-dimethoxyphenol produces a mixture of 5-(3-hydroxy-2,4-dimethoxybenzyl)- and 5-(4-hydroxy-3,5-dimethoxybenzyl)pyrimidines . The phenolic condensation has been used to prepare a series of alkyl-substituted 5-(4-hydroxybenzyl)- and 5-(4-alkoxybenzyl)pyrimidines . The use of 1,2,3-trimethoxybenzene in place of a phenol produces 2,4-diamino-5-(2,3,4-trimethoxybenzyl)pyrimidine, a trimethoprim isomer with low antibacterial activity . The use of molecular models of several of the new ortho-substituted derivatives in the active site of dihydrofolate reductase has provided a rational explanation for their activities relative to trimethoprim.

Jpn J Antibiot, 1983 May, 36(5), 1133 - 6
{Transportation of cefotiam from serum to lung tissue}; Shimizu N et al.; Thirteen patients who were performed radical lobectomy for the disease of the chest, were administered of cefotiam (CTM) 1.0 g for an hour by intravenous drip infusion during their operation . The concentration of CTM in serum and lung tissue were determined . CTM showed very high concentration in lung tissue and very high concentration ratio of lung tissue to serum concentration for several hours . These results suggested that CTM will be useful agent for the prevention and treatment of pulmonary infection, since CTMsh owed also very potent antibacterial activity against Gram-positive and Gram-negative bacteria.

J Histochem Cytochem, 1983 May, 31(5), 601 - 7
Observations on the cytochemistry of the hemocytes of an insect, Galleria mellonella; Chain BM et al.; A number of cytochemical parameters of the hemocytes of larval Galleria mellonella, an insect frequently used as a model by comparative cellular immunologists, are described . Cytochemical methods were used to quantify hemocyte granule-associated components, the results are compared to those obtained for leukocytes from higher animals . Granulocytes contained a population of nonlysosomal granules rich in mucopolysaccharide not seen in plasmatocytes . The numbers and dimensions of these granules showed a positive correlation to cell size, probably reflecting a developmental sequence in granulocyte maturation . Both granulocytes and plasmatocytes had other granules containing the typical lysosomal enzymes, acid phosphatase, beta-glucuronidase, esterase, and lysozyme . The nonlysosomal enzyme alkaline phosphatase was not found in Galleria hemocytes; it is also absent from vertebrate monocytes, macrophages, and immature polymorphonuclear leukocytes . Insect hemocytes appear to lack certain components of antibacterial systems typical of mammalian blood cells, such as H2O2-generating systems, cationic proteins, and myeloperoxidase . The bactericidal mechanisms of hemocytes probably involve lysozyme, as well as other biologically active cellular and humoral factors unique to insects.

J Infect Dis, 1983 May, 147(5), 882 - 9
Antibacterial mechanisms of antibody to mannose-sensitive pili of Escherichia coli; Weinstein R et al.; To identify mechanisms whereby antibody to mannose-sensitive pili of Escherichia coli might enhance host defenses, we evaluated the activity of antibody to pili in four antibacterial immune processes . Antiserum to pili and Fab' fragments of IgG antibody to pili inhibited the ability of homologous piliated organisms to adhere to buccal epithelial cells . However, this antiserum did not enhance intravascular clearance, complement-dependent bacteriolysis, or opsonophagocytosis . The addition of antiserum to pili to polymorphonuclear leukocytes and piliated E . coli reduced the rate of killing from 52% to 5% . The addition of complement restored the rate to 52%, but this was much less than the 99% rate achieved with polymorphonuclear leukocytes and either fresh serum or antibody to the whole bacteria . These observations suggest that the principal anti-bacterial property of antibody to mannose-sensitive pili of E . coli is inhibition of bacterial attachment . Whether the anti-opsonic effect of antibody to pili is detrimental to host defense remains to be determined.

Farmaco {Sci}, 1983 Apr, 38(4), 219 - 31
Researches on antibacterial and antifungal agents . I . Analogs of nalidixic acid with a pyrrole moiety; Corelli F et al.; The synthesis and antibacterial activities of 4-hydroxyquinoline-3-carboxylic acid and 1,4-dihydro-1-ethyl-4-oxoquinoline-3-carboxylic acid containing a pyrrole or 2,5-dimethylpyrrole group at 6 position are reported . Reaction of 1-(4-aminophenyl)pyrrole or 2,5-dimethyl-1-(4-aminophenyl)-pyrrole with ethoxymethylenemalonate diethyl ester (EMME) afforded the related pyrroleanilinomethylenemalonates, which were subjected to thermal cyclization to give the required quinoline derivatives . These compounds on ethylation furnished at last the quinolonecarboxylic analogs of nalidixic acid.

J Med Chem, 1983 Apr, 26(4), 469 - 75
Structure-activity relationships of synthetic antibiotic analogues of anisomycin; Hall SS et al.; A general synthetic sequence was used to synthesize a series of analogues of anisomycin, and the biological activities of the new synthetic analogues as antiprotozoals, antifungals, and antibacterials were evaluated . The synthetic antibiotics included 3 beta-acetoxy-4 alpha-hydroxy-2 beta-(p-methylbenzyl)pyrrolidine (1b), 3 beta-acetoxy-2 beta-benzyl-4 alpha-hydroxypyrrolidine (1c), 3 beta-acetoxy-4 alpha-hydroxy-2 beta-(m-methoxybenzyl)pyrrolidine (1d), 3 beta-acetoxy-4 alpha-hydroxy-2 beta-(o-methoxybenzyl)pyrrolidine (1e), 3 beta-acetoxy-4 alpha-hydroxy-2 beta-(alpha-methyl-p-methoxybenzyl)pyrrolidine (1f), and 3 beta-acetoxy-4 alpha-hydroxy-2 beta-(alpha-phenyl-p-methoxybenzyl)pyrrolidine (1g) . The anisomycin analogues showed activity against protozoa and fungi, but this activity was restricted primarily to the p-methylbenzyl and benzyl analogues 1b and 1c . The activities dropped dramatically as the methoxy substituent was moved to the meta or ortho positions of the benzyl group (1d and 1e) or a methyl or phenyl group was attached at the alpha-benzyl carbon (1f and 1g).

Z Kinderchir, 1983 Apr, 38 Suppl, 16 - 8
{Comparative in vitro tests of silver sulphadiazine and zinc sulfadiazine swabs on burn patients}; Youssef S et al.; The antibacterial effect of silver sulphadiazine is compared with that of zinc sulphadiazine in three in vitro tests with 14 different bacterial colonies . Our results demonstrate that silver sulphadiazine is more efficient than zinc sulphadiazine as an antibacterial agent . As the local application of zinc promotes and accelerates wound healing, we suggest to apply first silver sulphadiazine and then zinc sulphadiazine in combined local therapy of burn wounds.

Antibiotiki, 1983 Apr, 28(4), 250 - 4
{Standardization of the nutrient medium for determining the biological activity of a number of antibiotics by the diffusion-in-agar method}; Bershteein EM et al.; The possibility of using 2 variants of a unified nutrient medium containing no Hottinger's broth for determination of the biological activity of a large number of antibacterial antibiotics was shown . The medium provided satisfactory reproducibility of the results . It contained yeast extract as a source of nitrogen . The medium was selected with the method of the fractional factor experiment . Clear inhibition growth zones and the slope of the dose-response curve were used as the criteria for estimation of the optimal medium . The described nutrient medium allowed a 2-time increase in the sensitivity of the method used for determination of the biological activity of neomycin, monomycin, streptomycin, oxytetracycline, chlortetracycline and erythromycin.

Lepr India, 1983 Apr, 55(2), 265 - 77
Clofazimine in lepra (ENL) reaction, one year clinical trial; Burte NP et al.; Twenty patients of lepromatous leprosy with lepra reaction and suspected dapsone resistance were treated with tapering doses of clofazimine . Clinical assessment was carried out every week . Bacteriological examination was carried out every six month . Fifteen patients became reaction free at the end of three months and severity and frequency of reactions was reduced in other patients . Nerve tenderness, arthralgia, nodular eruptions and all other signs and symptoms except anaesthesia showed complete recovery in fifteen patients and severity of the reactions was reduced in others . Gynaecomastia regressed in two out of three patients within nine months . In a majority of patients, the BI and MI was reduced at the end of 3 months, and further reduced after 6 months, and in one case both BI and MI became negative . Clinical and bacteriological improvement is attributed to the antibacterial effect of clofazimine while reduction in incidence of (ENL) reactions was attributed to anti-inflammatory effect of clofazimine . Regression of gynaecomastia may be due to either improvement of involvement of testes or liver or both . Apart from dyschromia clofazimine did not produce any severe side effects or toxicity.

Clin Obstet Gynaecol, 1983 Apr, 10(1), 37 - 64
Host defence mechanisms in obstetrics and gynaecology; Larsen B; The host possesses a variety of defence mechanisms which operate in concert to prevent infection or alter the course of an infective process . The majority of infectious diseases in the gynaecological patient arise at the mucosal surfaces . Mucosal surface pathogens must compete with organisms which are members of the normal flora and with local immunity . In the surgical patient infection usually arises as a result of disruption of anatomical barriers and implantation of organisms from the host's own flora in deeper tissues . Inflammatory and phagocytic reactions provide protection in this setting but their effectiveness may be perturbed by such features of the surgical procedure as leaving devitalized tissue or excessive amounts of suture in the operative site, or by inadequate haemostasis . The pregnant patient appears to have increased phagocytic activity and certain humoral antibacterial factors are also increased . She may have slight alterations in humoral immunity and evidence for altered cell-mediated immunity is provided . Further investigation of host defence in obstetrical and gynaecological patients may produce better methods for identifying defects in resistance to infectious processes and the development of the means for augmenting the natural defences of the host.

Jpn J Antibiot, 1983 Apr, 36(4), 678 - 88
{Antibacterial activity of cefotiam against clinical isolates in the field of obstetrics and gynecology}; Deguchi K; Antibacterial activity of cefotiam (CTM) against clinically isolated organisms in the field of obstetrics and gynecology was discussed as follows: In the point of view of the MICs peak, CTM was 1-fold worse than CEZ against Gram-positive bacteria, while, in the case of the concentration of CTM required to inhibit the growth of 80% or 90% of the total number of tested Gram-positive organism, antibacterial activity of CTM was approximately identical with that of CEZ, CMZ or SBPC . CTM against E . coli, K, pneumoniae, P . Mirabilis was 16-32-fold more effective than CEZ and 4-16-fold than CMZ . Against indole-positive organisms with CEZ was no effective, CTM was considerably effective . But antibacterial activity of CTM against B . fragilis was insufficient . However, in the case that no spore forming anaerobic organism involved in infectious disease, it is said that existence of aerobic organism is important . As E . coli is representative of aerobic organism, CTM with potent antibacterial activity against this organism is seemed to be effective antibiotic for the gynecological infection.

Bull Eur Physiopathol Respir, 1983 Mar-Apr, 19(2), 173 - 8
The participation of antiviral immune mechanisms in alveolar macrophage dysfunction during viral pneumonia; Jakab GJ et al.; Virus infections transiently suppress pulmonary antibacterial defenses by causing dysfunctions in the alveolar macrophage phagocytic system . This impairment of pulmonary bactericidal activity is not associated in time with virus proliferation, but rather with the period of time of rapidly declining virus titers and the expression of the antiviral immune response in the lungs . This temporal relationship suggests that the impairment of pulmonary bactericidal activity might be secondary to the antiviral immune response rather than a direct effect of virus replication . Immune depletion of mice during the course of influenza virus pneumonia ameliorated the virus-induced bactericidal defect and prevented bacterial multiplication in the lungs . In contrast, immune reconstitution reestablished the alveolar macrophage phagocytic defect . These data indicate that virus-induced suppression of pulmonary antibacterial defenses may be, in part, immunologically mediated.

Bull Eur Physiopathol Respir, 1983 Mar-Apr, 19(2), 131 - 6
{Interactions between complement system and bacterial walls}; Colomb MG et al.; The complement system is involved in the antibacterial defence either with a delay, following the specific antibody response, or immediately through a direct interaction between complement components and the bacterial cell wall . Several gram- bacteria initiate the classical pathway through direct interaction between C1 and the lipid A of the lipopolysaccharides; this activation depends upon the structure, the accessibility and the state of polymerization of the lipopolysaccharides . Gram+ and gram- bacteria are able to activate the alternative pathway through a covalent C3b binding . Capsules appear to prevent activation due to their high content of sialic acid, which probably accounts for the virulence . As targets, bacteria may undergo opsonization mainly by C3b, or lysis through transmembrane channels formed by terminal components from C5b to C9.

J Antibiot (Tokyo), 1983 Mar, 36(3), 250 - 5
Role of the 1-amino group in aminocyclitol antibiotics: synthesis of 1-deaminogentamicin C2; Philippe M et al.; The synthesis of 1-deaminogentamicin C2 described here, uses 3,2',6',3"-tetrakis-N-tert-butoxycarbonylgentamicin C2 (2) as intermediate . N-Formylation of 2 followed by per-O-acetylation and dehydration furnished the isocyanide 5 . Radical-induced deamination of the latter using tri-n-butylstannane and removal of the protecting groups afforded the target 1-deaminogentamicin C2 (7) . Its in vitro antibacterial activity is less than that of the parent gentamicin C2 . The behaviour of 7 towards aminoglycoside-inactivating enzymes was also examined; interestingly, it was found to be neither substrate nor inhibitor for such enzymes . These results strongly suggest that the substitution pattern of the 1-position determines the biological properties of the aminoglycoside antibiotics.

J Antibiot (Tokyo), 1983 Mar, 36(3), 267 - 75
3-amino-3-demethoxyfortimicin A and the C-2 epimeric-2-amino-3-O-demethyl-2-deoxyfortimicins A; Tadanier J et al.; Selective reactions of 3-O-demethyl-3-O-methanesulfonyl-4-N, 5-O-methylenefortimicin derivatives have been used as the key steps in the syntheses of 3-amino-3-demethoxyfortimicin A and the C-2 epimeric 2-amino-3-O-demethyl-2-deoxyfortimicins A . In vitro antibacterial activities of the new fortimicin derivatives are reported.

J Antibiot (Tokyo), 1983 Mar, 36(3), 256 - 66
3-O-demethyl-2,3-di-epi-fortimicins and 3-O-demethyl-3-epi-fortimicins; Tadanier J et al.; Syntheses of the 3-O-demethyl-2,3-di-epi-fortimicins A and B and the 3-O-demethyl-3-epi-fortimicins A and B have been accomplished in processes the key steps of which were solvolyses of 4-N-acetyl-3-O-demethyl-3-O-methanesulfonylfortimicin derivatives . Antibacterial activities of the new antibiotics are reported.

J Antibiot (Tokyo), 1983 Mar, 36(3), 229 - 41
Synthesis and biological activity of 7 beta-(2-amino-2-carboxy)-ethylthioacetamido-7 alpha-methoxycephalosporin derivatives; Iwamatsu K et al.; C-7 and C-3 substituents of a new antibiotic SF-1623 were chemically modified to improve the bioactivity, and substituent effect at C-7 and C-3 was examined on the basis of MIC and ED50 values against selected bacteria . Among a large number of derivatives, MT-141 possessing 2-D-2-amino-2-carboxyethylthioacetamido residue at C-7 and N-methyltetrazolyl-thiomethyl residue at C-3 showed a high order of antibacterial activity in vitro and especially in vivo.

Gastroenterology, 1983 Mar, 84(3), 483 - 9
Role of bacteria in gastric ulceration produced by indomethacin in the rat: cytoprotective action of antibiotics; Satoh H et al.; Indomethacin produces mucosal lesions in both the gastric antrum and small intestine in rats refed for 1 h after a 24-h fast . This study was designed to determine the role of bacteria in the formation of the antral lesions . A mixture of antibiotics (bacitracin, neomycin, and polymyxin B) prevented the antral lesions as well as intestinal lesions . The antibiotics also decreased the gastric corpus lesions induced by indomethacin in the fasted rat . Under a germ-free condition, indomethacin did not produce severe lesions in the small intestine of the refed rat but provoked many lesions in the antrum of the refed rat and in the corpus of the fasted rat . Corpus lesions induced by indomethacin in the fasted rat were decreased markedly by neomycin and slightly by polymyxin B, but not by bacitracin . Corpus lesions produced by an absolute ethanol, however, were prevented by each of the antibiotics . The inhibitory effect of neomycin on the corpus lesions was not blocked by pretreatment with indomethacin . In pylorus-ligated rats, neomycin did not decrease gastric acid secretion . The concentration of nonprotein sulfhydryls in the gastric mucosa was not altered by the treatment with neomycin . The antibiotic solutions were hypotonic . It is concluded that (a) bacteria are not important in the formation of antral and corpus lesions induced by indomethacin, and (b) antibiotics prevent gastric ulceration not by its antibacterial action, but by a "cytoprotective" action . The mechanism is unknown, but it may be different from that of antisecretory drugs, prostaglandins, mild irritants, hypertonic solutions, and sulfhydryl compounds.

J Prosthet Dent, 1983 Mar, 49(3), 331 - 6
Protective effect of polystyrene liners for composite resin restorations; Brannstrom M et al.; The main purpose of lining cavities before insertion of composite resin restorations is to prevent bacterial contamination at the cavity walls . A thin film of polystyrene liner dissolved in ethyl acetate applied to all surfaces by compressed air provided good protection against bacteria on cavity walls under composite resin restorations . An antibacterial primer in an alcohol solution applied prior to the liner may improve this protection . This procedure had no detectable injurious effect on the pulp.

Oral Surg Oral Med Oral Pathol, 1983 Mar, 55(3), 307 - 12
Bacteriologic evaluation of the effect of 0.5 percent sodium hypochlorite in endodontic therapy; Bystrom A et al.; The antibacterial effect of 0.5 percent sodium hypochlorite solution as root canal irrigant was studied in fifteen single-rooted teeth . Each tooth was treated at five appointments, and the presence of bacteria in the root canal was studied on each occasion . No antibacterial intracanal dressings were used between the appointments . When 0.5 percent hypochlorite was used no bacteria could be recovered from twelve of fifteen root canals at the fifth appointment . This should be compared with eight of fifteen root canals when saline solution was used as irrigant . These results suggest that 0.5 percent sodium hypochlorite solution is more effective than saline solution as a root canal irrigant.

Jpn J Antibiot, 1983 Mar, 36(3), 487 - 99
{Clinical evaluation of BRL 25000 (clavulanic acid-amoxicillin) in the fields of obstetrics and gynecology}; Kishida H et al.; BRL 25000 was administered to 37 cases with infections in the fields of obstetrics and gynecology, and the following results were obtained . The drug was administered to 17 cases with adnexitis, 13 cases with intrauterine infection and 7 cases with parametritis and/or inflammation of pelvic dead space, etc . The percentage of efficacy (excellent and good) was 74.3% . Of 7 cases where no therapeutic effect was obtained with other drugs, the percentage of efficacy was 57.1% . Antibacterial effect of BRL 25000 was studied in terms of percentage of eradication (including replacement) of clinical isolates . A high percentage of eradication (94.4% or 17/18) was obtained . Among all clinical isolates, 37.9% or 11/29 were beta-lactamase producing organisms . Eradication or replacement by BRL 25000 was noted in all these 9 strains, and BRL 25000 was proved to have a high efficacy also against penicillin or cephalosporin resistant organisms . No abnormality was noted in any patient in hematological, hepatic and renal function before and after administration of BRL 25000 . As adverse reaction, diarrhea was found in 1 of 37 cases (2.7%), but it reduced after off-dose.

Bull Eur Physiopathol Respir, 1983 Mar-Apr, 19(2), 123 - 30
{The role of lactotransferrin in the molecular mechanisms of antibacterial defense}; Spik G et al.; Lactotransferrin is involved in the antibacterial defence of the host by virtue of its reversible iron-binding capacity . On the one hand, it participates in different molecular mechanisms displayed by immunocompetent cells which are known to synthesize or recognize the lactotransferrin . For instance, 1) during inflammation, apolactotransferrin released by the neutrophils captures the iron from serotransferrin which is accumulated by the macrophages, by means of their lactotransferrin membrane receptors; 2) lactotransferrin is an important component in the microbicidal activity of neutrophils by regulating the hydroxyl radical production; 3) lactotransferrin acts as a regulator of myelopoiesis by modulating activity of the colony stimulating factors; 4) lactotransferrin could be involved in the control mechanism of lymphoid cell migration . On the other hand, lactotransferrin participates to the non-specific local secretory immunity by being involved in antibacterial mechanisms together with secretory immunoglobulins sIgA and lysozyme . The different aspects of the participation of the lactotransferrin in the cellular and secretory mechanisms of antibacterial defence of the host show that the lactotransferrin plays a predominant role in the local immunity of any mucosa.

Am J Trop Med Hyg, 1983 Mar, 32(2), 221 - 5
Effects of antibiotics on Plasmodium falciparum in vitro; Geary TG et al.; Evidence from in vivo experiments and clinical reports in humans has indicated that some antibiotics demonstrate antimalarial activity . Twelve antibiotics have been tested against Plasmodium falciparum in vitro, including cycloheximide, streptomycin, erythromycin, tetracycline, chloramphenicol, clindamycin, actinomycin D, rifampin, nalidixic acid, penicillin G, chlorhexidine, and isoniazid . Inhibitory effects obtained at various drug concentrations in vitro were compared to drug levels reported to be effective against bacteria in vivo . Several antibacterial drugs, including erythromycin, chloramphenicol, clindamycin, rifampin and tetracycline, demonstrated significant antiparasitic effects at concentrations within or near those observed during therapy in vivo; the potency of erythromycin and tetracycline was greater at 96 hours of exposure than at 48 hours.

J Antibiot (Tokyo), 1983 Mar, 36(3), 242 - 9
Synthesis and antibacterial activity of 6- and 7-{2-(5-carboxyimidazole-4-carboxamido)phenylacetamido}-penicillins and cephalosporins; Yasuda N et al.; The synthesis and antibacterial activity of a series of beta-lactam antibiotics having a 5-carboxyimidazole-4-carbonyl group attached through an amide linkage to ampicillin, cephaloglycin or their analogs are described . Some compounds of this series were found to possess high activity against Pseudomonas and other Gram-negative bacteria.

Wien Med Wochenschr, 1983 Feb 15, 133(3), 73 - 83
{Preventable side effects of chemotherapy}; Lenzhofer R et al.; During the last years antineoplastic chemotherapy provided the possibility to cure many patients suffering from a malignant tumor and to improve their quality of life . Like every powerful remedy cytostatic drugs show side effects, which must be taken into consideration . Advantages and risks of cancer chemotherapy have to be considered carefully in each individual treatment schedule . The definition of the upper limit of therapeutic risk for each individual patient in order to avoid life-threatening situations is of principal importance . This can be accomplished by introduction of methods which can measure actual functional conditions and by the definition of a threshold-level in order to establish contraindication . Paul Ehrlich introduced the term "therapeutic index" in antibacterial chemotherapy . This term should express the ratio between risk and benefit of a drug and its application in the still very young field of antineoplastic chemotherapy should be considered . Since every treatment of a patient with cytostatic drugs represents a very significant interference with the patient's life, very strict indication- and and contraindication-criteria have to be applied.

Science, 1983 Feb 11, 219(4585), 709 - 14
New applications of microbial products; Demain AL; Microbial secondary metabolites are now being used for applications other than as antibacterial, antifungal, and antitumor agents . These applications include use against parasites (coccidia, helminths) and insects as well as for animal and plant growth stimulation, immunosuppression, uterocontraction, and other pharmacological activities . Further applications are possible in various areas of pharmacology and agriculture, a development catalyzed by the use of simple enzyme assays for screening prior to testing in intact animals or in the field.

Antimicrob Agents Chemother, 1983 Feb, 23(2), 221 - 31
Preparation and DNA-binding properties of substituted triostin antibiotics; Cornish A et al.; Novel derivatives of the triostin group of antibiotics were prepared by supplementing cultures of the producing organism Streptomyces triostinicus with a variety of aromatic carboxylic acids . Five new antibiotics, each having both the natural quinoxaline chromophores replaced by a substituted ring system, were purified to homogeneity and characterized by high-pressure liquid chromatography and nuclear magnetic resonance . Their antibacterial activities and DNA-binding properties were investigated . Addition of a halogen atom at position 6 of the quinoxaline ring or an amino group at position 3 had little effect on either the biological activity or the DNA-binding characteristics . The bis-3-amino derivative is fluorescent, and its fluorescence is strongly quenched by calf thymus DNA and polydeoxyguanylate-polydeoxycytidylate but not by polydeoxyadenylate-polydeoxythymidylate, suggesting that it binds preferentially to guanosine-cytosine-rich sequences in natural DNA . Binding constants for the bis-6-chloro and bis-3-amino derivatives do not differ greatly from those of unsubstituted triostin A . The analogs having two quinoline chromophores or a chlorine atom in position 7 of the quinoxaline ring display little or no detectable antibacterial activity, in marked contrast to the other congeners . Bis-7-chloro-triostin A binds conspicuously more tightly to polydeoxyadenylate-polydeoxythymidylate than to any other polynucleotide tested.

J Antibiot (Tokyo), 1983 Feb, 36(2), 147 - 54
Synthesis and antibacterial activity of asparagine derivatives of aminobenzylpenicillin; Wagatsuma M et al.; In order to improve the antibacterial activity of aminobenzylpenicillin, penicillin derivatives having an asparagine moiety in the 6-acyl side chain (11a approximately g, 12a, b, f, g) were synthesized . The structure-activity relationship of new penicillins, N4-alkyl-asparaginylaminobenzylpenicillins, was investigated . N4-Methyl-D-asparaginylamoxicillin (11a), TA-058, was found to possess a broad spectrum of antibacterial activity against Gram-positive and Gram-negative bacteria . In acute toxicity, TA-058 showed good tolerance in mice (LD50 greater than 10 g/kg, i.v.).

J Med Chem, 1983 Feb, 26(2), 259 - 64
beta-Lactam antibiotics: geometrical requirements for antibacterial activities; Cohen NC; Recent observations reveal deficiencies in the accepted theory rationalizing the biological activities of the beta-lactam antibiotics, since a study of strained carbapenem beta-lactams has shown that the observed antibacterial activities do not correlate either with the pyramidal character of the beta-lactam nitrogen atom or with the ease of base hydrolysis of the lactam amide bond . The contradiction can be reconciled by an analysis of the three-dimensional (3-D) features of a set of the representative active and inactive beta-lactam structures, which shows that highly specific 3-D recognition sites may exist in the enzymes in their recognition of the antibiotics . The identification of the geometrical requirements for antibacterial activity also reveals how it could be possible to restore antibiotic activities to inactive structures, up to now considered as devoid of any therapeutic interest.

Jpn J Antibiot, 1983 Feb, 36(2), 433 - 51
{Clinical studies of long acting amoxicillin in oral surgery}; Shiiki K et al.; Clinical studies with long acting amoxicillin (L-AMPC) have been carried out and the following results were obtained . 1 . Forty-two patients with acute bacterial infections in the oral region were administrated orally L-AMPC at a daily dose of 1 gram . The clinical results obtained were classified as excellent in 3 cases, good in 28 cases, and the overall efficacy was 75.6% . 2 . The antibacterial activity of AMPC was determined for 66 strains isolated from patients with oral infections . Of the strains tested, Gram positive cocci showed high sensitivity with MIC's less than 1.56 mcg/ml, while the sensitivity of PC resistance strains of S . aureus, K . pneumoniae and P . vulgaris was lower . 3 . There was 1 case of transaminase elevation in the laboratory finding . 4 . Five patients reported the following side effects, eruption 3, diarrhea 2, nausea 1, anorexia 1 and malaise 1 . From the results of the present study, it is considered that L-AMPC is a useful antibiotic in the treatment of acute bacterial infections in oral region.

Br J Exp Pathol, 1983 Feb, 64(1), 15 - 24
Muscle regeneration and transplantation enhanced by bone marrow cells; Meyer S et al.; This work was undertaken in an attempt to improve the usually poor results of muscle regeneration and grafting in cases of muscle injury . Since bone marrow cells markedly increase myogenic growth in vitro (in Millipore diffusion chambers), we added autogenous and isologous bone marrow cells to minced muscle grafts or to sites of excised muscle in rats . In each case the opposite side was left without added marrow cells, to serve as a control . The results showed that addition of bone marrow produces more extensive muscle regeneration with little fibrosis . The myogenesis-stimulating and antibacterial properties of bone marrow cells warrant further study, aiming towards clinical application of the method.

Tijdschr Diergeneeskd, 1983 Feb 1, 108(3), 103 - 6
{The litter - Aspergillus - mastitis}; Overgoor GH et al.; A number of cases of bovine mastitis caused by Aspergillus fumigatus are reported . The animals showed considerably swollen hard quarters associated with the production of large quantities of watery secretion and symptoms of systemic disease . Both intramammary and systemic treatment with several antibacterial agents failed to produce any improvement, nor did an antimycotic administered by intramammary route result in improvement . Severe mastitis marked by mycotic lesions was observed on slaughter, and the causative agent was found to be present again . Contamination had apparently originated from the litter (sawdust), and infection resulting from intramammary treatment could not be ruled out . The role pf predisposing factors and the fact that Aspergillus is common fungus in various types of litter are stressed.

Jpn J Antibiot, 1983 Feb, 36(2), 249 - 59
{Antibacterial action of cefoperazone and piperacillin against Escherichia coli}; Obana Y et al.; A study of the antibacterial action of cefoperazone (CPZ) and piperacillin (PIPC) against E . coli demonstrated clear differences between these 2 drugs . CPZ showed higher bactericidal and lytic activity which was dose dependent and not greatly influenced by inoculum size . In contrast, the activity of PIPC was strongly influenced by inoculum size and showed high bactericidal activity only against a low inoculum size . The activity of CPZ was not related to the pH of the culture medium, whereas PIPC showed increased activity in an acid medium . In a study of the drug sensitive phase of a synchronous culture, CPZ was highly effective during the period of cell division showing strong bactericidal activity at that time . The bactericidal action of CPZ was inhibited by the addition of chloramphenicol . In contrast, PIPC which by itself demonstrated only weak bactericidal activity was not effective during the period of cell division . Although CPZ and PIPC both activate autolysin activity, CPZ was more active in this regard.

Padiatr Padol, 1983, 18(3), 281 - 9
{Clinical experiences with intravenous immunoglobulin therapy of infectious diseases in infancy and childhood}; Gyarmati E et al.; In 26 infants with severe sepsis antibacterial therapy was supplemented by the intravenous administration of immunoglobulins (Endobulin, Immuno AG, Vienna) . Such therapy was indicated in 6 patients by the appearance of granulocytopenia during the treatment of their underlying disease, in 14 children by their very young age which was less than 2 years, and in 6 children by the failure of antibacterial therapy to produce the desired effect . Depending on the clinical picture of sepsis different organ manifestations were seen, purulent meningitis (10 cases) and pneumonia (9 cases) being the most frequent . In 24 patients immunoglobulin therapy led to complete recovery . In all 7 cases of purulent meningitis, the simultaneous administration of antibiotics and immunoglobulins was effective.

Antibiotiki, 1983 Jan, 28(1), 23 - 6
{Effectiveness of liposome-incorporated streptomycin in experimental tuberculosis in mice}; Vladimirskii MA et al.; The chemotherapeutic efficacy of streptomycin incorporated into liposomes was studied on mice with experimental tuberculosis . Streptomycin incorporated into liposomes was prepared with the detergent method using purified egg lecithin, sodium cholate and streptomycin sulfate . The level of streptomycin incorporation into liposomes was 250-399 micrograms of streptomycin base per 1 mg lecithin . The size of the liposome was determined by electron microscopy . It was 40-80 nm . BALB/c and (CBA X C57B1(6)) F1 mice infected with M . tuberculosis H37Rv (0.1 mg of half-moist mass per mouse, intravenously) were used in the experiments . It was shown that the liposome-incorporated streptomycin injected intravenously on the 3rd or the 4th day (20 or 25 mg/kg) or 3 times on the 4th, 7th and 10th or the 12th days (50 or 67.5 mg/kg a day) after the infection inhibited the growth of M . tuberculosis in the spleen tissue, while analogous doses of streptomycin solution had no such an effect . With respect to the lung tissue, the antibacterial effect of the liposome-incorporated streptomycin was not potentiated . When the liposome-incorporated streptomycin was administered 3 times, the life-span of the animals was increased and the loss of the body weight was retarded as compared to the results of an analogous treatment course with the use of streptomycin solution . The acute toxicity of intravenous streptomycin incorporated into liposomes was lower as compared to that of streptomycin solution.

Farmaco {Sci}, 1983 Jan, 38(1), 3 - 8
Preliminary pharmacobiological study of new steroidal sapogenins; Gonzalez AG et al.; The chemotherapeutic study of a limited series of steroidal sapogenins from several endemic species of the flora of the Canary Islands is presented here . On the whole, they possess a very weak antibacterial activity, a slight antifungal effect and one of them, vespertilin, displays interesting cytostatic activity (ID50 = 5 micrograms/ml) . A pharmacodynamic screening carried out on this product mainly revealed very slight toxicity, antihistaminic activity and a light tranquilizing effect . The data obtained justify further research.

Arch Immunol Ther Exp (Warsz), 1983, 31(5), 631 - 40
Biological evaluation of Wratizolin penetration from ointments to the skin; Inglot AD et al.; The degree of Wratizolin penetration to the skin from ointments prepared in 6 different media was determined . Experiments were carried out in mice and guinea pigs using: a) method determining the decrement of cytotoxic and antibacterial activity of the tested ointment contacted with the skin, b) biological tests to check the presence-of the drug in tissue extracts . Absorption of Wratizolin appeared dependent upon the kind of base ointment . The preparation penetrated well when suspended in polyethylene glycol base ointment (PEG).

J Antibiot (Tokyo), 1983 Jan, 36(1), 36 - 41
Studies on beta-lactam antibiotics . VI . Effect on antibacterial activity of alpha-substituents in the 2-(2-amino-4-thiazolyl)acetyl side chain of a cephalosporin nucleus; Takasugi H et al.; Synthesis and in vitro antibacterial activity of semisynthetic cephalosporins (I) having an alpha-substituted 2-(2-amino-4-thiazolyl)acetyl side chain at the 7-position were described.

J Cell Biochem, 1983, 23(1-4), 47 - 56
Killing of Giardia lamblia trophozoites by normal human milk; Gillin FD et al.; The clinical course of giardiasis is variable, and serum antibodies do not appear to be protective . We propose that natural factors either produced by intestinal tissue, transported into the intestine, or ingested (ie, by breast-fed babies) might promote resistance to this disease . Human milk is very rich in secretory IgA (S-IgA) antibodies, as well as nonspecific antibacterial factors (eg, lactoferrin, lysozyme) . Previous studies showed that Giardia lamblia trophozoites were killed by nonimmune human milk (NHM) in a time- and concentration-dependent manner . Removal of greater than 99% of the S-IgA from NHM did not decrease its Giardia-cidal activity . Thus, the killing was not antibody dependent . This is the first demonstration of nonimmune antiparasitic defenses in human milk . The present studies show that in the presence of NHM, trophozoites lost motility, swelled, and lysed . The Giardia-cidal activity (GCA) may be specific to human milk, since unheated cow's and goat's milk were virtually devoid of activity . Much, but not all, of the GCA was lost when NHM was heated or reacted with diisopropylfluorophosphate (DIFP), a specific esterase inhibitor . Activity of the major human milk lipase (BSL, bile salt-stimulated lipase, a fatty acid esterase) was lost after heat or DIFP treatment and was absent from cow's or goat's milk . The parasites were also killed by pure BSL . These studies suggest that BSL may be a heat-labile Giardia-cidal component of NHM.

Acta Otorhinolaryngol Belg, 1983, 37(4), 589 - 94
Bacterial invasion of the sinus mucosa; Lundberg C; Pathohistological examinations show that bacterial infection of the sinus mucosa starts in the mucosal secretion, spreads out to the glandular cells, which are the points of least resistance, and only reaches the deeper mucosal layer when the normal arrangement of the epithelial cells and the basal membrane are broken up . Hence treatment of sinus infection starts with the restauration of the mucosa defence system and when using antibiotics it is essential that antibacterial active concentrations are established both in sinus mucosa and sinus secretion.

Folia Microbiol (Praha), 1983, 28(5), 386 - 96
A new antifungal antibiotic produced by Streptomyces galbus; Paul AK et al.; A streptomycete producing an antibiotic having antifungal and antibacterial activity was isolated from a soil sample of West Bengal . It was characterized and identified as Streptomyces galbus . The antibiotic was isolated from the fermented broth by treatment with activated charcoal and purified by chromatography on alumina and paper . It is a colourless, odourless, hygroscopic, amorphous compound . Although homogeneous by paper and thin-layer chromatography, the possibility of the presence of two components was indicated by gel filtration . Its physico-chemical characteristics and UV-absorption spectrum suggest a non-polyenic nature . It is active against a wide variety of fungi and bacteria . It has some phytotoxic effect, but is relatively non-toxic to rats.

EMBO J, 1983, 2(4), 571 - 6
Insect immunity . Attacins, a family of antibacterial proteins from Hyalophora cecropia; Hultmark D et al.; Six closely related antibacterial proteins, attacins A-F, were isolated from the hemolymph of immunized pupae of the Cecropia moth, Hyalophora cecropia . Chromatofocusing separated attacins A-F, with isoelectric points between 5.7 and 8.3 . Immunological experiments show that the attacins constitute antibacterially active forms of the previously isolated inducible immune protein P5 . Their mol . wts., 20-23 K, are similar to that of protein P5, but significantly lower than 28 K found for preP5 synthesized in vitro (see accompanying paper) . The six attacins can be divided into two groups according to their amino acid composition and amino-terminal sequences, attacins A-D constitute a basic group and attacins E and F an acidic one . Within each group the forms are very similar . The attacins efficiently killed Escherichia coli and two other Gram-negative bacteria isolated from the gut of a silk worm but they did not act on other Gram-positive and Gram-negative bacteria tested . Only growing cells of E . coli were attacked; cells suspended in phosphate buffer were inert . Besides the cecropins and lysozyme, the attacins represent a third class of antibacterial proteins in the humoral immune system of H . cecropia.

Infection, 1983, 11 Suppl 2, S112 - 8
Antibacterial defence mechanisms; Hahn H; Pathogenic bacteria fall into two groups with regard to their fate within phagocytes: extracellular bacteria are promptly killed after phagocytosis and facultative intracellular bacteria are resistant to intracellular killing unless macrophages are activated . Extracellular bacteria cause purulent infections, and facultative intracellular bacteria granulomatous ones . Humoral immune mechanisms (antibody, complement) deal mainly with extracellular bacteria, while cellular immune mechanisms (T cells, macrophages) deal with facultative intracellular bacteria . The specific and nonspecific factors and their interactions are discussed with respect to their role in the buildup of an effective antibacterial defence.

Wien Klin Wochenschr Suppl, 1983, 142, 15 - 7
{Antibacterial chemotherapy in impaired renal function}; Zazgornik J; In the antibacterial chemotherapy in patients with chronic renal diseases several principles should be considered . Highly nephrotoxic or ototoxic antibiotics are not to be used in patients with chronic renal failure . The dosage ought to be reduced adequately to the degree of damage of renal function . The degree of reduction of renal function is to be evaluated by estimation of endogenous creatinine clearance or by estimation of serum creatinine level . The first dose of an antibacterial drug ought to be the same as in persons with good renal function . Additional doses should be reduced or the interval between the doses prolonged . It is necessary to monitor kidney function and possible side effects.

J Med, 1983, 14(3), 193 - 202
Treatment of febrile granuloycytopenic cancer patients receiving antineoplastic therapy with a combination of carbenicillin, cefazolin and gentamicin; Halpern J et al.; A three drug regimen of carbenicillin, cefazolin and gentamicin was used for the treatment of patients with solid tumors, who developed fever while granulocytopenic following chemotherapy . Thirty-five (8%) of 426 cancer patients receiving various combinations of antineoplastic chemotherapy qualified for the antibiotic treatment . Nine patients (26%) had bacteriologically confirmed infections, all with gram negative microorganisms . Twenty-four patients (69%) recovered and eleven (31%) died . All deaths occurred within five days of antibiotic therapy; in patients who recovered, the fever subsided within six days . Mortality was not influenced by the presence of a positive bacterial culture, age, or the cytotoxic agents used . It was, however, strongly related to metastatic spread: nine out of 14 patients with liver metastases (64%) died from the infection, while only two of 11 patients (18%) with other metastatic sites failed to respond to the antibacterial therapy . No death occurred in 10 patients who had local disease or received adjuvant therapy . This combined antibiotic therapy was as effective as reported for other combinations, with no serious side effects.

Arch Oral Biol, 1983, 28(6), 545 - 8
Isolation and serological typing of ureaplasma in human saliva; Watanabe T et al.; Ureaplasmas were detected in the saliva of 3.5 per cent (12/342) of subjects . A total of 60 isolated strains did not revert to bacterial forms on repeated subculture in antibacterial agent-free media, failed to grow in serum-free media, were inhibited by digitonin and hydrolysed urea but not glucose or arginine . Twenty-five strains were divided into serotypes: I (5), II (3), III (5), IV (4) and VI (8 strains) . Ureaplasmas of serotype I, II, III, IV and VI were harboured by 2, 1, 1, 1 and 3 subjects respectively and the remaining 4 subjects harboured 2 different serotypes . Ureaplasma-positive subjects were young and middle-aged and, except for 1 subject with mandibular arthrosis, suffered from periodontitis, pericoronitis, gingivitis and maxillary sinusitis . These accounted for only 6.1 per cent (11/180) of the series of subjects examined.

Arzneimittelforschung, 1983, 33(3), 470 - 2
{N-Formimidoyl-thienamycin in Animal Studies}; Ritzerfeld W; The beta-lactam antibiotic thienamycin is rather unstable and is metabolized in man by renal dehydropeptidase-I . The derivatives of the antibiotic, especially N-formimidoyl-thienamycin (MK-0787) are reported to be more resistant . The antibacterial activity of N-formimidoyl-thienamycin was tested by means of the infection- and therapy model of the acute, occlusive pyelonephritis in rats . Cefotaxime was used as control agent . Even with a low dosage a clear anti-bacterial activity was proved with the E . coli- as well as especially with the Pseudomonas pyelonephritis . In our tests N-formimidoyl-thienamycin was more potent than cefotaxime.

J Antimicrob Chemother, 1983 Jan, 11 Suppl, 37 - 43
Susceptibility of bacterial pathogens to cefotetan judged by MIC and disc tests; Grimm H; The activity of cefotetan was tested against 683 bacterial strains by measuring the minimum inhibitory concentrations . Comparisons were made with cefoxitin, cefotaxime, moxalactam, cefoperazone and piperacillin . In addition, a regression line analysis was made with cefotetan discs (30 micrograms) using the ICS technique . Cefotetan was noted to have a broader spectrum of activity than cefoxitin and its antibacterial activity was comparable to that of cefotaxime and moxalactam . According to the regression line analysis a cefotetan inhibition zone diameter of greater than or equal 19 mm is interpreted as sensitive in agar diffusion tests.

J Antimicrob Chemother, 1983 Jan, 11 Suppl, 169 - 77
The interactions of {14C}cefotetan with penicillin binding proteins of a wide variety of Gram-positive and gram-negative species; Nolan RD et al.; Membrane preparations were made from a number of Gram-positive and Gram-negative bacterial strains . The ability of the membrane-bound penicillin-binding proteins (PBP) in these preparations to bind {14C}cefotetan has been studied . Increasing amounts of unlabelled benzylpenicillin were added and subsequently {14C}cefotetan was introduced to determine its ability to bind to additional proteins or to displace the pre-bound benzylpenicillin . In the Gram-positive series some quantitative binding differences between the two labelled compounds could be seen . However, in the majority of Gram-negative organisms tested cefotetan exhibited greatest affinity for PBP 3 and none for PBP 2 . No new PBPs were detected using {14C}cefotetan, suggesting that the compound exerts its antibacterial effect by a mechanism similar to the other cephamycins . The high minimal inhibitory concentrations (MICs) of cefotetan found for the Gram-positive genera tested are reflected in only one organism by the failure to bind of some of its PBPs . In the majority of cases, permeability is assumed to play the dominant role in the relatively low sensitivity of these organisms to cefotetan.

Scand J Prim Health Care, 1983, 1(1), 20 - 4
Prescription of antibacterial drugs for treatment of bronchitis and pneumonia in general practice in Denmark; Mabeck CE; Phenoxymethyl penicillin is the drug of choice in the treatment of acute respiratory tract infection . The widespread use of a broadspectrum antibiotic indicates that practitioners use such a preparation in the absence of a proper microbiological diagnosis . A relatively high proportion of patients were treated with erythromycin . This may reflect the widespread misconception of allergy to penicillin among patients and doctors . Too many prescriptions for antibacterial drugs seem to be based on telephone contact.

Comp Immunol Microbiol Infect Dis, 1983, 6(4), 273 - 80
Heme-iron and ecology of Escherichia coli within the porcine gut; Maisi P et al.; Growth of Escherichia coli was followed in sow whey by a turbidometric technique . Heme-iron clearly promoted bacterial growth, therefore free heme would be dangerous in small intestine by enhancing bacterial growth: duodenal brush border membrane (BBM) was seen to bind heme-iron, thus abolishing the growth promoting effect of this form of iron . Scatchard analysis of heme-binding onto BBM showed that heme became bound by a specific mechanism (KD approximately equal to 10(-7) M) as well as non-specifically . The absorption system for iron within the enterocytes should be considered an important antibacterial system within the gut.

Microbios, 1983, 37(149-150), 139 - 49
Local anaesthetics as antibacterial agents: effects on cellular respiration and the leakage of cytoplasmic constituents; Fazly Bazaz BS et al.; The effect of four local anaesthetics, amethocaine and procaine (esters) and cinchocaine and lignocaine (amides), on the respiration and dehydrogenase activity of E . coli has been studied . Cells were suspended in either a chemically defined medium or in 0.2 M phosphate buffer (pH 6.4) . Substrates included: glucose, succinate, malate and lactate . Further studies on the release of cellular constituents (pentoses and inorganic phosphate) are included and indicated that some local anaesthetics, at high concentrations, inhibit autolysis . Results are discussed in terms of the action of local anaesthetics on membrane integrity and its significance in enzyme action . A novel method for the detection of inorganic phosphate by differential pulse voltammetry and its application to studies of drug induced leakage of intracellular materials is described.

Gynecol Obstet Invest, 1983, 15(1), 26 - 32
Antibacterial activity in amniotic fluid from west virginia women; Larsen B et al.; Amniotic fluids from women in West Virginia were evaluated for the presence of antibacterial activity by a bioassay technique . 41% of 32 third trimester samples were inhibitory . Evaluation of additional test organisms emphasized differences in susceptibility of various bacterial strains; two isolates of Escherichia coli were found which were more sensitive to the phosphate-sensitive antibacterial system of amniotic fluid than in the initial test organism . The stated prevalence of inhibition may therefore be considered a conservative estimate.

Scand J Infect Dis, 1983, 15(1), 91 - 6
The antibacterial activity of combinations of mecillinam and ampicillin in vitro and in normal and granulopenic mice; van der Voet GB et al.; The antibacterial activity of mecillinam and ampicillin, alone and in combination, against Escherichia coli was quantitated and compared in vitro and in vivo . Minimum inhibitory concentrations (MICs) were determined for both antibiotics individually and combined . Two-hour growth curves were established in vitro . A quadratic fit to these growth curves provided quantitative concentration-dependent growth characteristics . The antibacterial activity in vivo was determined by applying a short-term thigh muscle infection model to normal and irradiated granulopenic mice . The effects in vivo were also quantitated as dose-dependent or concentration-dependent parameters . Mecillinam showed activity in vitro, but none in vivo . Combinations of mecillinam with ampicillin showed a strong potentiation, as judged from MICs and from short-term experiments in vitro and in the normal and irradiated granulopenic mice . The potentiating activity in vivo was not influenced by host factors (i.e . granulocytes) . However, the degree of potentiation indicated by the MICs led to strong overestimation of the effect of the combination of the two antibiotics on short-term in vitro growth . Furthermore, the combined activity in vitro overestimated the potentiating effect of the two antibiotics in vivo.

Jpn J Antibiot, 1983 Jan, 36(1), 117 - 23
{Study of cefotaxime on stability to beta-lactamases and affinity to penicillin-binding proteins}; Inoue M et al.; Cefotaxime (CTX) was compared with other cephems concerning stability to beta-lactamases and affinity to penicillin-binding proteins of Escherichia coli JE1011 . The results are summarized as follows . 1 . CTX showed potent activity against bacteria whose resistance is mediated by plasmids on chromosomal genes . 2 . The antibacterial activity of CTX was not influenced by the transfer of 25 different plasmids to E . coli ML1410 . 3 . CTX was stable to typical cephalosporinases (CSases) . This compound was slightly hydrolyzed by cefuroximases (CXases) . 4 . There was no difference between CTX and other cephems in the affinity to beta-lactamases . 5 . CTX showed high affinity to the 1A, 1Bs and 3 fractions of penicillin-binding proteins of E . coli JE1011.

Arzneimittelforschung, 1983, 33(1), 88 - 90
{Mezlocillin: a penicillin from the acylureido series . Synthesis and chemical properties}; Konig HB et al.; Mezlocillin, 6-{D-2-(2-Oxo-3-mesyl-imidazolidine-1-carboxamido)- 2-phenylacetamido}-penicillanic acid, is a new semisynthetic acylureido-penicillin with a broad spectrum of antibacterial activity . The synthesis of mezlocillin from ampicillin and from 6-aminopenicillanic acid and the physicochemical properties are described . Mezlocillin is cleaved by penicillinase to the penicilloate which is degraded further by acids to the penilloate.

Comp Immunol Microbiol Infect Dis, 1983, 6(4), 301 - 12
Experimental study of antibiotic-induced immunosuppression in mice . II . Th, Ts and NC cell involvement; Voiculescu C et al.; In penicillin(pen), streptomycin(str), kanamycin(kan) and tetracycline(tet)-treated CBA/J adult mice, no difference was noticed as concerned spleen T "helper" (Th) cell activity, as studied by means of response to PHA of X-irradiated/whole T fraction cell mixtures in vitro . On the contrary, in erythromycin(erm), colistin(col) and chloramphenicol(chl)-treated groups, Th cell activity was significantly decreased . On the other hand, spleen T "suppressor" (Ts) cell activity (assayed by response to PHA of mixtures containing pre-incubated with Concanavalin A and whole T cells, respectively) was augmented in samples arising from chl-treated group . These results are also supported by experiments testing Th or Ts soluble factors, induced in spleen T cells belonging to each antibiotic-treated group and purified by affinity chromatography (Concanavalin A-Sepharose 4B columns) . Thus, it was confirmed both Th cell deficiency in erm, col or chl-groups, and Ts cell augmentation in chl-group . As regards spleen "natural cytotoxic" (NC) cell activity, as tested in a xenogeneic "target" cell substrate, a diminished cytotoxic capacity manifested chl-group-derived NC cells, possibly by richness in own "non-specific suppressor" (NSS) cells . NC cell samples in vitro supplemented with NSS cells arising from suckling mouse spleens and a lower cytotoxic activity, in a larger extent in chl-group-derived NC cells, as compared to other groups . The pre-incubation of control-group-NC cells with several antibiotic preparations in vitro was followed by decrease of the cytotoxic values in erm, col and chl-samples, suggesting a drug-induced NC receptor "masking", that prevented "target" cell recognition in mice--II . In the case of NSS addition in vitro, as strong inhibition of the cytotoximity occurred in chl-treated NC cells derived from the control group, that proves a possible chloramphenicol-induced immunodepression by potentiation of NSS inhibitory effect on NC cells . Based upon data from the present work, as well as from the previous work, the authors suggest a classification of several mechanisms by which the antibacterial antibiotics can act as immunosuppressive.

Comp Immunol Microbiol Infect Dis, 1983, 6(4), 291 - 9
Experimental study of antibiotic-induced immunosuppression in mice . 1 . Humoral and cell-mediated immune responsiveness related to in vivo antibiotic treatment; Voiculescu C et al.; By using CBA/J mice as responders, the immunodepressive effect of seven antibacterial chemotherapeutic agents was tested, i.e . penicillin (pen), streptomycin (str), erythromycin (erm), kanamycin (kan), tetracycline (tet), colistin (col) and chloramphenicol (chl) . Lymphocytotoxicity power, as well as the ability of each drug to influence secondary humoral (against sheep red blood cells or diphtheria anatoxin) or cell-mediated (against PPD and Coxsackie A9 virus) immunity were searched . Erm, col and chl markedly depressed humoral and cell-mediated immune responsiveness in vitro after in vivo treatment with non-cytotoxical amounts . The Th lymphocyte supplementation of B reactive spleen cell population recovered the immune capacity in col and chl in vivo-treated groups, but not in erm-treated group.

Arzneimittelforschung, 1983, 33(4), 571 - 4
{Antibacterial activity of the combination of cefoperazone piperacillin}; Kruger E et al.; The effect of the combination cefoperazone plus piperacillin was tested against 131 clinical isolates of gram-positive and gram-negative bacteria by checkerboard titration and by determining the serum bactericidal activity . The interaction was synergistic against 9% of the strains in vitro and partially synergistic against 48% . In the serum bactericidal tests bactericidal titers higher than 1:8 were obtained with the combination one hour after administration . No antagonism was observed either in the in vitro tests or in tests of serum bactericidal activity.

Jpn J Antibiot, 1983 Jan, 36(1), 1 - 15
{Laboratory and clinical studies on latamoxef in the field of obstetrics and gynecology}; Takase Z et al.; Latamoxef (LMOX) is a new antibiotic synthesized by Shionogi Research Laboratory . Chemically LMOX is especially unique with a sulfur atom replacing the oxygen atom in the 1 position of the conventional cephalosporin nucleus, and in addition, this antibiotic has a cephamycin-like structure . The antibacterial activity of LMOX shows high potency against Gram-negative bacteria, but tends to be weak against Gram-positive bacteria . The tissue levels of LMOX in humans after intravenous injection of 1 g were examined . The levels in uterine and adnexa uteri tissue at 1 hour after administration were 25.4 and 27.4 micrograms/g respectively . LMOX was administered to 147 cases in infections of obstetric and gynecological field . The clinical effect according to disease was 94.6% for intrauterine infections, 95.0% for adnexitis, 87.0% intrapelvic infections, and 100% for external genital organ infections, making a total of 92.5% . The rate of occurrence of side effects or abnormal laboratory findings was similar to or slightly less than that seen with other beta-lactam antibiotics.

Wien Klin Wochenschr Suppl, 1983, 144, 3 - 31
{Selective toxicity of cytostatic agents: studies on the cardiotoxicity of doxorubicin, its pathogenesis and contraindications}; Lenzhofer R; In the past few years the medical treatment of malignant diseases has steadily increased in scope and importance . However, the tumor regimens described in the textbooks still are rather schematic recommendations, which are inadequately tailored to the needs of the individual case . Current tumor therapy is based on the results of the statistical analysis using empirical data collected in randomized trials . While patients can today be given a statistical value which expresses their computed chance of a cure versus that of a defined population, there is still no generally valid method which could serve as a rational basis for individualized counselling . But cytostatic chemotherapy has yet another major shortcoming: the collective assessment of toxicity, which is related to one of the basic properties of cytostatic drugs, i.e . their extremely low therapeutic index . Many of the side effects of cytostatics may cause severe irreversible, at times even fatal, organ dysfunction . Consequently, the definition of the therapeutic risks involved on the basis of an objective identification of potential organ toxicity is a major challenge . "Surgery without a knife", as K.H . Spitzy has called chemotherapy, should be subjected to objective criteria for its indications and contraindications so that patients can truly benefit from what are become increasingly aggressive measures . The principle of weighing the benefits desired in the individual case against the potential risks involved in a specific treatment, which Paul Ehrlich postulated for antibacterial chemotherapy, should also be applied to cytostatic chemotherapy with a view to facilitating the decision for or against therapy in borderline cases . The present contribution which is designed to shed light on the cardiotoxicity of doxorubicin should be interpreted in light of this situation . Pathogenetic aspects and animal experiments on drug-induced lipid peroxidation will be discussed and clinical trials on both acute and chronic doxorubicin cardiotoxicity will be reviewed . Special attention will be paid to the tolerable risks of this special form of toxicity and cardiologic methods currently available for patient monitoring will be critically assessed . In summary, the studies produced the following results: A . Pathogenesis Treatment of C 57 B1 mice with doxorubicin increases the production of malonic dialdehyde in the myocardium . Enhanced malonic dialdehyde production can largely be suppressed by the additional administration of anti-oxidants (tocopherol, glutathione, cysteamine, cysteine).(ABSTRACT TRUNCATED AT 400 WORDS)

Biochem J, 1983 Jan 1, 209(1), 183 - 8
Inhibition of reverse transcriptases by seminalplasmin; Reddy ES et al.; Seminalplasmin, an antibacterial protein present in bovine seminal plasma, is shown to be a potent inhibitor of reverse transcriptases (RNA-dependent DNA nucleotidyltransferases) . Seminalplasmin inhibits RNA-directed, hybrid-directed, and DNA-directed DNA-polymerizing activities of purified reverse transcriptase from avian myeloblastosis virus and from crude viral lysates of several retroviruses by binding to the enzyme, at least in the case of avian myeloblastosis virus . Seminalplasmin does not inhibit significantly DNA synthesis either by Escherichia coli DNA polymerase I, or a mammalian alpha-DNA polymerase . The presence of seminalplasmin in the seminal fluid could provide protection to the male and/or the female reproductive tract against retroviruses.

J Antibiot (Tokyo), 1983 Jan, 36(1), 47 - 53
Quaternary heterocyclylamino beta-lactams . II . The in vitro antibacterial properties of L-640,876, a new type of beta-lactam antibiotic; Koupal LR et al.; A new semisynthetic cephalosporin antibiotic designated 7-beta-(1-benzylpyridinium-4-yl)-amino-3-{( (1-methyl-1H-tetrazol-5-yl) thio}methyl)ceph-3-em-4-carboxylate (L-640,876) was compared for antibacterial activity in vitro with mecillinam, cefoxitin and cefotaxime . The antibacterial spectrum of L-640,876 and the effect of culture medium composition and inoculum size on activity are most similar to those of mecillinam . In some cases the inoculum effect on MICs correlated with instability of the compound to certain beta-lactamases and in others to the presence of ionized compounds such as sodium chloride in the medium . On balance, L-640,876 was superior to mecillinam in potency and breadth of spectrum.

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