Proc R Soc Lond B Biol Sci, 1980 Oct 15, 209(1177), 473 - 87 Electrostatic components of drug-receptor recognition . II . The DNA-binding antibiotic actinomycin; Dean PM et al.; The semiempirical molecular orbital method PCILO has been used to study the electronic charge distribution and conformation of the antibiotic actinomycin . Molecular electrostatic potential fields have been constructed in three-dimensional space round the molecule and displayed stereoscopically together with contour maps in the orthogonal planes relative to that of the chromophore . It was found that the drug has a considerable dipole moment and that the electrostatic fields can be separated into two large regions; an area of positive potential surrounds the chromophore and one of negative potential is directed away from the peptide rings . In this and the preceding paper these observations are discussed with respect to drug-receptor recognition phenomena . Pattern-matching of complementary electrostatic fields between the drug and polynucleotide receptor can be discerned. J Antibiot (Tokyo), 1980 Oct, 33(10), 1107 - 13 New anticoccidial antibiotics, WS-5995 A and B . I . Isolation and characterization; Ikushima H et al.; WS-5995 A, B and C are produced by a new strain of Streptomyces designated Streptomyces auranticolor . These antibiotics were purified by solvent extraction followed by chromatography on silica gel and then crystallized . WS-5995 A (C19H12O6, m.p., 289 approximately 291 degrees C) and WS-5995 B (C19H14O6, sublimation at 300 degrees C) protect chickens from infection with Eimeria tenella, a species of coccidia, which produces morbidity or mortality in chickens . WS-5995 C (C19H14O 7, m.p . 288 approximately 290 degrees C), a biologically inactive component, was found to be converted to WS-5995 A on treatment with trifluoroacetic anhydride. J Antibiot (Tokyo), 1980 Oct, 33(10), 1103 - 6 Streptomyces auranticolor Sp . Nov., a new anticoccidial antibiotics producer; Ikushima H et al.; A new species of Streptomyces is described and designated Streptomyces auranticolor (FERM-P No . 5365) which produces new anticoccidial antibiotics, designated as WS-5995 A and WS-5995 B . The organism is characterized by gray spore mass color, spiral spore chain with smooth spores, non-chromogenic reaction, soluble pigment, and carbon utilization characteristics . It differs from previously described streptomycetes on the basis of carbon utilization, and pigment production. J Antibiot (Tokyo), 1980 Oct, 33(10), 1098 - 102 BBM-928, a new antitumor antibiotic complex . II . Taxonomic studies on the producing organism; Tomita K et al.; An actinomycete strain No . G455-101 isolated from a soil sample collected in Luzon Island, Philippines produced a new antitumor antibiotic complex BBM-928 . The organism was determined to be a new species of the genus Actinomadura and designated Actinomadura luzonensis nov . sp . The type strain, No . G455-101, has been deposited under the number ATCC 31491. Antimicrob Agents Chemother, 1980 Oct, 18(4), 586 - 92 Permeabilizing and hemolytic action of large and small polyene antibiotics on human erythrocytes; Brajtburg J et al.; The effects of large polyenes (heptaenes and the "degenerate heptaene" nystatin) on human erythrocytes were found to occur in three separate stages . Stage I was a reversible increase in cell membrane permeability to monovalent cations and occurred at low antibiotic concentrations . At intermediate antibiotic concentrations, an irreversible increase in cell membrane permeability to cations (stage II) occurred, which then led to swelling of cells and hemolysis (stage III) . Hemolysis could be prevented by sucrose, mannitol, or melezitose, but stages I and II still occurred under these conditions . The effects of the small polyenes (pentaenes and a tetraene) occurred in only one stage . Changes in cell membrane permeability (stages I and II) were not noted before hemolysis (stage III) even in the presence of carbohydrate . Carbohydrates gave only weak, transient protection from the hemolytic action of small polyenes, probably because the membrane damage induced by these antibiotics was more extensive than that induced by the large polyenes . In the presence of sucrose, large polyenes were able to inhibit the hemolytic action of small polyenes, implying that both antibiotics have the same binding sites. J Reprod Med, 1980 Oct, 25(4), 173 - 7 Premature rupture of the membranes: maternal and neonatal infectious morbidity related to betamethasone and antibiotic therapy; Miller JM Jr et al.; A retrospective study of patients delivering in 1976-77 at Duke University Medical Center was performed to assess the impact of betamethasone and prophylactic antibiotics on infectious morbidity in mothers with premature rupture of the membranes (PROM) at 26 to 34 weeks' gestation and in their neonates . Ninety-five records were reviewed for evidence of maternal and neonatal infection and perinatal mortality . Betamethasone had no impact on maternal or neonatal infection . Antibiotics given concurrently with betamethasone significantly reduced the incidence of maternal and/or neonatal infection (18.0% vs . 0) . Perinatal mortality increased when the duration of the latent period was 72 hours and greater because of factors other than infection. J Clin Pathol, 1980 Oct, 33(10), 995 - 1001 Light-scattering methods for antibiotic sensitivity tests; Murray J et al.; The total intensity of light scattered in the angular range 30 degrees-130 degrees by a suspension of bacteria can be used as the basis of a method of antibiotic sensitivity testing . A procedure is given in which the bacteria are incubated in the presence of antibiotic, as a test, and in its absence, as a control, for 60 minutes . An incubation time of 90 minutes gives slightly more reliable results . With this increased incubation time it is necessary to measure the intensity of scattered light only at a single fixed angle or, at most, a few angles . Measuring the angular dependence of the scattered intensity does not allow the incubation period to be reduced. Antibiotiki, 1980 Oct, 25(10), 764 - 9 {Carminomycin induction of single-stranded DNA breaks in the normal and tumorous cells of mice administered the antibiotic intravenously}; Trenin AS; The effect of carminomycin administered intravenously to albino mice on the sedimentation character of the ascitic cell DNA of mouse lymphadenosis NK/Li, as well as the cells of the lungs, kidneys, liver, heart and spleen in alkaline sucrose gradients was studied . It was found that carminomycin in a dose of 3.5 mg/kg (LD50) induced DNA single-strand breaks in the cells of the lungs, kidneys, liver and heart . At the same time the single-strand breaks were not detected in the tumor cells NK/Li and the cells of the spleen . The results are indicative of correlation between sensitivity of the cells to carminomycin and a decreased capacity of the antibiotic for induction of single-strand breaks in DNA . Probably, the cell ability for DNA repair is an important factor defining the antitumor selective effect of carminomycin . Induction of the single-strand breaks reflects the role of the excision repair in healing the damages induced by carminomycin. Antimicrob Agents Chemother, 1980 Oct, 18(4), 506 - 10 Enzymatic method for rapid and sensitive determination of beta-lactam antibiotics; Frere JM et al.; A rapid and sensitive procedure for the estimation of beta-lactam antibiotics is described which makes use of the ability of these antibiotics to inactivate the R39 DD-carboxypeptidase . Depending on the values of the kinetic parameters which govern the reaction, the antibiotics fall into two groups . The lower limit for the quantitative estimation of the antibiotics of groups I and II is about 5 and 50 pmol/ml, respectively . The procedure has been adopted to biological fluids such as human sera and cows' milk. J Antibiot (Tokyo), 1980 Oct, 33(10), 1183 - 92 Mutual pro-drugs of beta-lactam antibiotics and beta-lactamase inhibitors; Baltzer B et al.; The principle of combining a beta-lactam antibiotic with a beta-lactamase inhibitor in a single molecule functioning as pro-drug for the two active components is illustrated by the linked esters 3 and 4 in which ampicillin and mecillinam, respectively, are combined with the beta-lactamase inhibitor penicillanic acid sulfone . It is shown that in man these esters are excellently absorbed from the gastro-intestinal tract and after absorption hydrolyzed with simultaneous liberation of the active components . As a result high blood and tissue levels of antibiotic and beta-lactamase inhibitor in a balanced ratio are attained . The advantages of "mutual pro-drugs" over simple combinations are discussed. J Med Chem, 1980 Oct, 23(10), 1144 - 8 Structure-activity relationships of pyrrole amidine antiviral antibiotics . 2 . Preparation of mono- and tripyrrole derivatives of congocidine; Bialer M et al.; Representatives of three types of congocidine (1) analogues were synthesized . These were tested for cytotoxicity, inhibition of herpes simplex virus (HSV) replication in cultured cells, and effects on the synthesis of HS DNA in isolated nuclei in vitro, as well as on DNA synthesis by purified HSV DNA polymerase . All synthesized tripyrrole derivatives of congocidine were less cytotoxic and more active than the parent drug in all the three ant iviral tests. JAMA, 1980 Sep 19, 244(12), 1353 - 4 Antibiotic activity in surgical incisions . The basis of prophylaxis in selected operations; Polk HC Jr et al.; Perioperative antibiotic administration to produce systemic effects reduces the frequency of operative wound infection in selected procedures . Controlled clinical trials now indicate that cephalothin sodium may not be effective in this role, whereas cephaloridine and cefazolin sodium have been beneficial . Review of estimates of incisional antibiotic concentrations taken during prospective patient studies display patterns compatible with these data . EAch drug reaches acceptable incisional concentrations, which are relatively well maintained for cephaloridine and cefazolin; cephalothin disappears from human incisions so rapidly as to provide little wound protection in operations lasting more than one hour. Experientia, 1980 Sep 15, 36(9), 1025 - 7 The structure of a novel antitumor antibiotic, saframycin A; Arai T et al.; A structure is assigned to saframycin A, a novel antitumor antibiotic from Streptomyces lavendulae No . 314, on the basis of 13C NMR-spectral data. Biochem J, 1980 Sep 15, 190(3), 765 - 70 Ribosomal resistance to the 12,13-epoxytrichothecene antibiotics in the producing organism Myrothecium verrucaria; Hobden AN et al.; An extract of Myrothecium verrucaria, a fungus which produces a range of 12,13-epoxytrichothecene toxins, was found to be resistant to T-2 toxin, one of its products . The epoxytrichothecenes are inhibitors of eukaryotic protein synthesis and normally bind to the 60S ribosomal subunit so as to inhibit peptidyltransferase activity . Ribosomes from M . verrucaria contain 60S subunits which are not subject to inhibition by T-2 toxin and are also resistant to certain other drugs such as anisomycin and homoharringtonine, but not sparsomycin or cycloheximide. Experientia, 1980 Sep 15, 36(9), 1051 - 2 Antibiotic bioassay by flow microcalorimetry; Beezer AE et al.; A rapid, sensitive microcalorimetric bioassay of good reproducibility has been developed for the antibiotics penicillin-G, carbenicillin, ampicillin and cefoxitin . The use of growing organisms as responding agents allows discussion of the results for systems which may involve biological fluids. Farmakol Toksikol, 1980 Sep-Oct, 43(5), 536 - 40 {Effect of preliminary antibiotic administration on the course of ether anesthesia}; Batrak GE et al.; The effect of pretreatment with benzylpenicillin, tetracycline hydrochloride and streptomycin sulfate on the course of either anesthesia was studied in experiments on animals . Benzylpenicillin and tetracyclin hydrochloride neither significantly changed the reactivity of the mouse body nor affected the course of ether anesthesia . Administration of streptomycin sulfate to mice and dogs was attended by the reduced function of the central nervous system . The course of ether anesthesia changed accordingly . The reaction of the animals who had been pretreated with streptomycin sulfate was determined by the species features . In white mice, the antibiotic increased the resistance to the toxic effect of ether while in the dogs, it decreased, on the contrary, the body resistance under anesthesia, thereby accelerating the animals' death. J Antibiot (Tokyo), 1980 Sep, 33(9), 998 - 1004 The structure of lienomycin, a pentaene macrolide antitumor antibiotic . II . The location of the pentaene chromophore and of six isolated double bonds . The complete structure of the antibiotic; Pawlak J et al.; The locations of the isolated double bonds and of the pentaene chromophore in lienomycin (I) were established by chemical degradation of I followed by MS and 1H NMR examination of the products . The complete structure of the antibiotic is proposed. J Antibiot (Tokyo), 1980 Sep, 33(9), 989 - 97 The structure of lienomycin, a pentaene macrolide antitumor antibiotic . I . The structure of the carbon skeleton and the location of functionalities; Pawlak J et al.; The structure of a novel type of pentaene macrolide named lienomycin (I) was established by selected chemical transformations of I followed by MS examination of the products . This report provides evidence on the structure of the carbon skeleton of I and on the location of functionalities. J Antibiot (Tokyo), 1980 Sep, 33(9), 979 - 88 Studies on the ionophorous antibiotics . XXVI . The assignments of the 13C-NMR spectra of lonomycin A and mutalomycin; Seto H et al.; All resonances observed in the 13C-nmr spectra of the polyether antibiotics lonomycin A and mutalomycin have been assigned by the aid of biosynthetic method, selective proton decoupling as well as comparison with structurally related compounds. J Antibiot (Tokyo), 1980 Sep, 33(9), 967 - 78 Papulacandins, a new family of antibiotics with antifungal activity . Structures of papulacandins A, B, C and D; Traxler P et al.; The structures of the papulacandins A, B, C and D, new antibiotics of Papularia sphaerosperma have been established by means of spectral analysis and degradation reactions . Base catalysed hydrolysis of the main product papulacandin B (1) gave two new hydroxylated long-chain unsaturated fatty acids 5 and 6 along with a hitherto unknown spirocyclic diglycoside 7 . The structure of 7 was determined by further degradation reactions . The positions of attachment of the two fatty acids to the spirocyclic diglycoside 7 through ester-bonds were established by selective base catalysed hydrolysis of 1 and spectral analysis of 1 and some derivatives and degradation products thereof . The structures of papulacandin A (2), papulacandin C (3) and papulacandin D (4) were determined in an analogous way. J Antibiot (Tokyo), 1980 Sep, 33(9), 961 - 6 New antibiotics, carbazomycins A and B . II . Structural elucidation; Sakano K et al.; The structures of carbazomycins A and B are elucidated to be 3,4-dimethoxy-1,2-dimethylcarbazole and 4-hydroxy-3-methoxy-1,2-dimethylcarbazole, respectively . Further, 13C-chemical shifts of carbazomycins and their derivatives are assigned simultaneously. Br J Pharmacol, 1980 Sep, 70(1), 25 - 40 Interaction between synthetic analogues of quinoxaline antibiotics and nucleic acids: role of the disulphide cross-bridge and D-amino acid centres in des-N-tetramethyl-triostin A; Fox KR et al.; 1 {Ala3, Ala7} TANDEM is an analogue of des-N-tetramethyl-triostin A (TANDEM) in which both L-Cys residues of the octapeptide ring are replaced by L-Ala; accordingly it lacks the disulphide cross-bridge which limits the conformational flexibility of TANDEM . 2 In {L-Ser1} TANDEM the configuration of one of the serine residues is inverted, altering the disposition of one of the quinoxaline chromophores with respect to the peptide ring . 3 Both compounds interact weakly but detectably with natural DNAs as judged by spectral shifts and increases in the thermal denaturation ('melting') temperature Tm . They also raise the Tm of poly rA . poly rU . 4 Binding isotherms determined by solvent partition analysis with {Ala3, Ala7} TANDEM yield association constants of about 10(3) M-1 for its interaction with natural DNAs . A Scatchard plot for binding to poly(dA-dT) determined by solvent partition and spectrophotometric methods shows marked evidence of cooperativity with an intrinsic association constant 1.9 x 10(4) M-1, 8.7 nucleotides per binding site, and cooperativity parameter 15 . 5 Binding of {Ala3, Ala7} TANDEM to short rod-like fragments of poly(dA-dT) increases their contour length by almost the theoretical amount expected for an ideal process of bifunctional intercalation . 6 No effect of either compound on the winding of the DNA helix could be detected in sedimentation experiments with closed circular duplex PM2 DNA . 7 It is concluded that the cross-bridge of TANDEM greatly stabilizes its binding to DNA, most probably via entropic factors, but is not the only structural feature that influences its AT sequence-selectivity . The consequences of epimerising one of the D-Ser residues appear as disastrous as epimerising both . 8 The experimental details for the synthesis of {Ala3, Ala7} TANDEM and {L-Ser1} TANDEM are given in an appendix to this paper. Plast Reconstr Surg, 1980 Sep, 66(3), 356 - 60 Antibiotic iontophoresis for the management of burned ear chondritis; Greminger RF et al.; A total of 11 ears in 8 patients were treated with iontophoresis utilizing either gentamicin sulfate or potassium penicillin . All patients experienced rapid healing with little or no deformity. J Biochem (Tokyo), 1980 Sep, 88(3), 689 - 93 Estimation of the in vivo translational activity of rat liver mitochondria without use of an antibiotic; Kitagawa Y et al.; In order to estimate the in vivo translational activity of mitochondria without using cycloheximide, we developed a selective separation procedure for the mitochondrial translation products . The effects of cycloheximide and isotopic dilution kinetics on the precursor leucine pool indicate that the pH 11.5 insoluble mitochondrial fraction is greatly enriched in mitochondrial translation products. Antibiotiki, 1980 Sep, 25(9), 690 - 1 {Use of antibiotics for preventing suppurative inflammatory complications in scleroplastic operations for myopic disease}; Savinykh VI; Sodium or potassium benzylpenicillin in a dose of 200000 units 6 times a day and streptomycin sulfate in a dose of 0.5 g twice a day were used intramuscularly during the postoperative period for prevention of purulent inflammatory complications in 172 out of 187 patients with myopic disease subjected to scleroplastic operations performed according to the methods of Shevelev-Kertin, N . N . Pivovarov and V . I . Savinykh . The antibiotic use decreased the period of the inpatient treatment from 28+/-2 to 14+/-2 days and lowered the levels of tenonitis and edema of the eye mucosa . No purulent dissolution of the orbital tissues was observed in the patients. Antibiotiki, 1980 Sep, 25(9), 673 - 5 {Effect of antibiotic therapy on the functional state of the adrenal cortex in mice under irradiation}; Lebedev VG et al.; Therapeutic efficacy of ampicillin on mice subjected to total irradiation with gamma-rays in a dose of 850 Gy and the effect of the antibiotic therapy on adrenocortical function in the irradiated animals were studied . It was found that the daily use of ampicillin over a period of the 3rd to the 10th day after the irradiation increased the survival rate of the animals by 30 per cent against 100 per cent death of the animals in the control group . An increase in the average life span of the irradiated animals in the test group was observed . The levels of corticosterone in the peripheral blood plasma of the irradiated animals in the test group was observed . The levels of corticosterone in the peripheral blood plasma of the irradiated animals not treated with the antibiotic markedly increased by the 6th and 10th day after the irradiation . The therapeutic use of ampicillin resulted in a significant decrease in the hormone level by the 10th day after the irradiation as compared to that in the control animals . Normalization of adrenocortical function in the animals treated with ampicillin promotes an increase in the rate of recovery from radiation injury. Antibiotiki, 1980 Sep, 25(9), 669 - 73 {Effect of polyene antibiotics on the increase in specific resistance due to inactivated antiviral vaccines}; Vil'ner LM et al.; The capacity of polyenic antibiotics, such as water soluble forms of amphotericin B, mycoheptin, nystatin and levorin to stimulate immunogenicity and interferonogenic activity of inactivated antiviral vaccines was shown . The protective effect of the vaccine against rabies or forest-spring encephalitis in albino mice was more pronounced on its two-fold use in combination with the antibiotic than that on its use alone . The most significant results were obtained with highly diluted vaccines supplemented with amphotericin B . In this case the resistance index was 2 times higher than on vaccination without amphotericin B . In comparative assays of 4 various lots of vaccines against rabies the ED50 of every inactivated vaccine corresponded to thrice as low levels of the antirabies antigen than on vaccination without the polyen . The problems of the mode of action of the polyenic antibiotics and antiviral inactivated vaccines used in combination are discussed. Surg Gynecol Obstet, 1980 Sep, 151(3), 404 - 6 The selective use of systemic antibiotics in the treatment of burns; Wilkins TJ et al.; For the past ten years, we have followed a conservative program in using systemic antibiotics for the treatment of significant burns . Prophylactic antibiotics are not used except for scalds . Antibiotics are given selectively at the time of operation and, otherwise, are reserved for the treatment of specific infections . It has been unusual for a patient with a burn severity index, compatible with survival, to die of uncontrolled sepsis . Resistant bacteria and fungi have not been a problem . We attribute this to the selective use of antibiotics. Biol Bull Acad Sci USSR, 1980 Sep-Oct, 7(5), 400 - 7 Effect of antibiotics on fatty acid composition of strains of E . coli K12 carrying R-plasmids; Andreev LV et al.; A dynamic approach was employed for a study of the reaction of the fatty acid pool of sensitive and resistant strains of E . coli K12 in response to the introduction of antibiotics . Bacteria whose resistance is controlled by plasmids exhibited a specific reaction - a reversible increase in the concentration of cis-9,10-methyl-enehexadecanoic acid . Strains of E . coli K12 (C600, J53, CSH-2) carrying plasmids RP4, R6K, R1 drd 19, pMB9, R386, RP1, RtS-1, were studied. Ann Surg, 1980 Sep, 192(3), 356 - 64 Prophylactic antibiotics in vascular surgery . Topical, systemic, or both? Pitt HA, Postier RG, MacGowan AW, Frank LW, Surmak AJ, Sitzman JV, Bouchier-Hayes D. A prospective, randomized, blinded study was performed to determine whether prophylactic antibiotics would reduce the incidence of infection in peripheral vascular surgery and whether the route of antibiotic administration was important . Patients undergoing a vascular procedure with a groin incision were allocated to one of four groups with respect to prophylactic antibiotics . Group I received no antibiotic . Group II had topical cephradine instilled in their incisions prior to closure . Group III received a 24-hour perioperative course of intravenous cephradine, and Group IV received both topical and intravenous cephradine . Groin and abdominal incisional infections were significantly reduced (p < 0.01) among patients who received prophylactic antibiotics by either the topical, systemic, or combined routes of administration . No significant differences were noted among the three antibiotic groups . Profundoplasty, femoral embolectomy, and femoral aneurysm repair were each associated with an increased incidence of infection (p < 0.01) . Other risk factors were only important in patients not receiving antibiotics . Either intraoperative topical antibiotics or perioperative systemic antibiotics prevent infection in peripheral vascular surgery, but antibiotic administration by both routes is unnecessary. Antibiotiki, 1980 Sep, 25(9), 643 - 7 {Variability of a Cephalosporium acremonium culture for 2 quantitative traits: antibiotic formation and proteolytic activity}; Shuvalova IA et al.; Exposure of Cephalosporium acremonium, strain 1435, to N-nitrozo-N-methylbiuret resulted in a changed variation coefficient with respect to two quantitative features--the antibiotic production and proteolytic activity . Correlation between the variation coefficient and mutagen exposure time was different for every feature . Positive correlation was found in variation with respect to the antibiotic production and proteolytic activity in populations of various Cephalosporium acremonium strains chosen with regard to one or two of the above features . The level and form of the correlation in variation of the above features in populations changed during selection . Selection according to the two quantitative features resulted in an increased correlation coefficient. Antibiotiki, 1980 Sep, 25(9), 680 - 3 {Increase in the sensitivity and a simplification of the method for the separate determination of antibiotic activities in combined preparations (oletetrin) by using media with a varying pH value}; Makarova RA et al.; An agar-diffusion method for determination of oleandomycin and tetracycline low levels in solutions of the drug combination was developed . The medhod may be used for investigation of oletetrin absorption and distribution in humans and animals . It provides high accuracy in separate determination of oleandomycin and tetracycline activity in solutions of the drugs at a ratio of 1 : 2 . The same test-culture, Bac . subtilis, variant L2 is used for the assay of tetracycline and oleandomycin activity . The only differences are in the values of pH and the buffer solution and the standards. Biokhimiia, 1980 Sep, 45(9), 1682 - 4 {Effect of the polycationic antibiotic polymyxin B on the respiratory activity of rat liver mitochondria}; Kapitanova NG et al.; the mechanism of the effect of the peptide antibiotic polymixin B on respiration of rat liver mitochondria was studied . It was shown that polymixin B at concentrations of (1,6--2,0) . 10(-3) M inhibits mitochondrial respiration in state 3 and 3u irrespective of the oxidation substrate used and activates oxygen consumption in state 4 at lower concentrations . It is assumed that the antibiotic affects mitochondrial respiration by changing the ionic permeability of the membranes. J Gen Microbiol, 1980 Sep, 120(1), 95 - 104 Resistance to the antibiotics viomycin and capreomycin in the Streptomyces species which produce them; Skinner RH et al.; Viomycin capreomycin, antibiotics produced by Streptomyces vinaceus and S . capreolus respectively, are potent inhibitors of bacterial protein synthesis . Although these organisms are highly tolerant of their own products in vivo, their ribosomes are fully sensitive to the action of the drugs in vitro . However, they processes novel, antibiotic-inactivating enzymes (viomycin phosphotransferase, capreomycin phosphotransferase, capreomycin acetyltransferase) which, in addition to possible biosynthetic roles, may contribute to the resistances observed in vivo. J Antibiot (Tokyo), 1980 Sep, 33(9), 1048 - 53 Effects of several anthracycline antitumor antibiotics on the transcriptional activity of isolated nucleoli; DuVernay VH et al.; The class II anthracycline antitumor antibiotics musettamycin, rudolfomycin, aclacinomycin and marcellomycin, which were shown in earlier studies to preferentially inhibit the synthesis of nucleolar RNA in intact tumor cells, were studied in an isolated nucleolar transcriptional assay . Their effects were compared with those of the nucleolar non-selective anthracyclines adriamycin, carminomycin and pyrromycin, as well as with the 10-descarbomethoxy-analogs of marcellomycin and rudolfomycin . The isolated nucleolar transcriptional assay was found to have linear activity for 30 minutes at 30 degrees C . At increasing concentrations of alpha-amanatin up to 200 micrograms/ml, the maximum degree of inhibition of transcriptional activity was found to be 6 approximately 7% . The ranking of nucleolar RNA synthesis inhibitory potencies of the class I and II anthracyclines and the 10-descarbomethoxy-analogs obtained previously in intact cells was reproduced in the isolated nucleoli assay system described here . Thus, evidence for the use of this assay as a screen for nucleolar active antitumor agents is presented. Mycopathologia, 1980 Aug 29, 72(1), 13 - 9 Antifungal antibiotic sensitivity testing: use of Autobac 1 for standardization purposes; Seguela JP et al.; The authors used a semi-automatic device, Pfizer Autobac 1, to standardize antifungal antibiotic sensitivity testing . The first trials gave quite satisfying results for true (polyene) antibiotics, but more questionable results were obtained for imidazole derivatives and 5-fluorocytosine. Biochim Biophys Acta, 1980 Aug 4, 600(2), 585 - 9 The influence of the fatty acid composition of Acholeplasma laidlawii membranes on the growth inhibitory activity of narasin, a polyether ionophorous antibiotic; Smith CK 2nd et al.; Narasin, apolyether ionophorous antibiotic capable of acting as a transmembrane carrier of cations, has a growth inhibitory effect on Acholeplasma laidlawii, permitting only 20% survival when present as 0.1 micrograms/ml in an undefined growth nutrient or fatty acid-deficient nutrient supplemented only with palmitic acid . When A . laidlawii is propagated in fatty acid-deficient nutrient supplemented with linoleic acid, however, the organisms become 40 times more sensitive to the growth inhibitory effect of this antibiotic . The actual fatty acid composition of the membranes would indicate that a higher degree of unsaturation enhances ionophore activity. Chirurg, 1980 Aug, 51(8), 519 - 23 {Results of therapy combining peritoneal lavage and local application of antibiotics in 250 patients with acute perforating appendicitis}; Duyzings JW et al.; Since 1967, 2480 appendectomies have been performed at the St . Lucas Hospital (Amsterdam) and the St . Annadal Hospital (Maastricht), of which 250 were for perforated appendicitis . A so-called 'combined method' of treatment was used in all these cases: during the operation saline was used to lavage the peritoneal cavity with the patients in the reverse-Trendelenburg position . Antibiotics were left in the peritoneal cavity . No intraperitoneal drainage was performed, but the wound was drained for 5 days . Postoperative treatment consisted of nasogastric suction and parenteral antibiotics for 5 days in combination with anticoagulation . With thus combined approach one death was seen in 250 cases . There were 20 cases of wound infection (8%), 7 pelvic abscesses (2.8%), and 2 retroperitoneal abscesses . No thromboembolic complications were seen because of the use of routine anticoagulation . For 191 patients (77%), total hospitalization was less than 14 days . This method of treatment is compared with recent reports in literature. J Reprod Med, 1980 Aug, 25(2), 63 - 6 C-reactive protein in the evaluation of antibiotic therapy for pelvic infection; Angerman NS et al.; C-reactive protein (CRP), an acute-phase reactant not found in normal serum, has previously been shown, by qualitative assay, to differentiate inflammatory from noninflammatory pelvic pathology . In this study, quantitative measures of serum CRP were obtained concomitantly with white blood counts (WBC) and erythrocyte sedimentation rates (ESR) in patients being treated for pelvic infection . CRP levels and their changes, which were not known to physicians treating the patients, accurately indicated those patients who would need supplementary antibiotics to achieve remission . WBC levels were misleading in over half the patients, and the ESR bore no relationship to the clinical situation . The data suggest that CRP may be used to assess the efficacy of antibiotic therapy in pelvic infection . Our successful use of single-agent therapy in most cases also suggests that the use of multiple antibiotics is unnecessary and that CRP levels can indicate when additional antibiotics are appropriate. Antibiotiki, 1980 Aug, 25(8), 615 - 9 {Modern antibiotics in the clinical picture of infectious diseases}; Bilibin AF et al.; The number of various chemotherapeutics including antibiotics used in combined treatment of patients with various infectious diseases is rather significant . Recently some new valuable drugs have been recommended . Still, in spite of definite achievements in treatment of patients with infectious diseases there are some difficulties and problems mainly connected with therapy of patients with sepsis, chronic typhoid fever bacterial carriers and some other patients. Antibiotiki, 1980 Aug, 25(8), 566 - 71 {Inactivation mechanism of polyene antibiotics . The change in the functional component of levorin during inactivation}; Bronov LV et al.; The inactivation process of levorin, a polyenic antibiotic was studied in the presence of oxygen . It was found that the biological activity did not sufficiently correlate with the optical density of the antibiotic solution . This indicates that destruction of the double bonds was not the only process resulting in the biological activity loss . In this connection methods for qualitative determination of the levorin main functional groups, i.e . aromatic and aliphatic amines and carbonyl groups were developed . The methods were used for the control of the changes in these functional groups on levorin inactivation . It was found that the inactivation level was directly proportional to the amount of the oxygen absorbed, 1 molecule of oxygen being required for inactivation of 2 levorin molecules . The number of the carbonyl groups and aromatic amines did not change during the inactivation process . In the first stages of inactivation the biological activity was directly proportional to the level of amino sugars . If the heptaen chromophore is not absorbed, 3 double bonds remain in inactivated levorin. Acta Ophthalmol (Copenh), 1980 Aug, 58(4), 567 - 75 Bacterial flora in relation to cataract extraction . V . Effects of topical antibiotics on the preoperative conjunctival flora; Fahmy JA; In a randomized study comprising 60 patients, six different prophylactic regimens were evaluated for their effectiveness in eradicating bacteria on the conjunctivas before surgery . Gentamicin sulfate ophthalmic solution was the only antibiotic able to eliminate bacteria in almost all of the examined patients . The other drugs (chloramphenicol solution, oxytetracycline-polymyxin B ointment, sulphamethizole, bacitracin-neomycin and ristocetin-polymyxin B solutions) were not effective, although most of the isolated strains were sensitive to the respective antibiotics, probably because of the short treatment period (18 h) . The problem of prophylactic therapy of ophthalmology is discussed, and some guide lines are given. J Antibiot (Tokyo), 1980 Aug, 33(8), 895 - 9 Have deoxystreptamine aminoglycoside antibiotics the same binding site on bacterial ribosomes? Le Goffic F, Capmau ML, Tangy F, Caminade E. (3H) Tobramycin was used as a probe to determine the relationship between the structure of aminoglycoside antibiotics and their ability to remove this drug from its higher affinity binding site on the ribosome . The dissacharide moieties (neamine, tobramine, gentamine) appeared to have a common binding site, whereas the kanosamine, garosamine and ribose moieties determined the specificity of this binding . Amikacin and butikacin behaved in an anomalous manner in spite of their close structural relationship to tobramycin. J Gen Microbiol, 1980 Aug, 119(Pt 2), 397 - 404 Co-synthesis of penicillin following treatment of mutants of Aspergillus nidulans impaired in antibiotic production with lytic enzymes; Makins JF et al.; Mycelia from four mutants of Aspergillus nidulans impaired in penicillin production at separate genetic loci were treated with an enzyme complex capable of lysine cell walls, then mixed in all possible paired combinations and grown in osmotically buffered penicillin production media, containing 2-deoxyglucose and an unrefined mixture of polyoxins to prevent cell wall regeneration . The culture filtrates were assayed after 6 d and significant penicillin yields were observed in four of the six possible combinations . None of these pairs produced penicillin when grown together as normal mycelium, suggesting that intermediates of the penicillin biosynthetic pathway unable to diffuse from untreated mycelium could do so from enzyme-treated mycelium when cell wall regeneration was inhibited . A general method is thus available for examining biochemical pathways with mutants accumulating intermediates unable to cross the cell wall barrier. Antibiotiki, 1980 Aug, 25(8), 595 - 606 {Ability of vancomycin-group antibiotics to induce or to inhibit thrombocyte agglutination}; Rak K et al.; The effect of 4 vancomycin antibiotics on factor VIII-dependent agglutination of thrombocytes was studied . Significant similarity, both quantitative and qualitative, between ristocetin and ristomycin was found . In this connection ristomycin may be used for determination of the so-called ristocetin cofactor . Actinoidin and vancomycin inhibited agglutination of platelets induced by ristocetin or ristomycin in platelet-enriched plasma with citrate or EDTA the same as in the system contaning platelets treated with formalin and did not inhibit agglutination induced by the bovine factor VIII . The 4 antibiotics induced precipitation of the plasma protein . Vancomycin was most active and actinoidin ws lest active in this respect . Ristocetin and ristomycin also possessed such capacity, the effect of the latter being higher . Actinoidin and vancomycin did not prevent the immediate effect of light absorption increasing due to addition of ristocetin or ristomycin to fixed platelets in concentrations completely inhibiting agglutination of platelets in the presence of the protein cofactor . Inhibition of this direct effect of ristocetin and ristomycin was observd only at higher concentrations, which indicated that this effect was not probably associated with agglutination . The results of the study on various ristomycin derivatives showed that methylated carboxylic groups and free hydroxyls of phenol may play the main role in ristomycin binding with the thrombocytic membrane and/or protein cofactor. Can J Microbiol, 1980 Aug, 26(8), 874 - 80 Regulatory control of 3-deoxy-D-arabino-heptulosonic acid 7-phosphate synthetase in Streptomyces antibioticus; Murphy MF et al.; Streptomyces antibioticus possesses a tryptophan-inhibitable 3-deoxy-D-arabino-heptulosonic acid 7-phosphate (DAHP) synthetase whose synthesis is also repressed by L-tryptophan . Studies of the DAHP synthetase obtained by ammonium sulfate fractionation of a crude extract derived from S . Antibioticus revealed that the enzymic activity was only partially inhibited by tryptophan . Inhibition of the DAHP synthetase activity was strongly pH dependent at values below 7.0 . A number of tryptophan analogues was noted to inhibit the enzyme; by contrast, other aromatic amino acid end products failed to affect DAHP synthetase activity . Chorismic acid, a key intermediate in aromatic amino acid biosynthesis, was ineffective as an inhibitor when used alone; however, if supplied with L-tryptophan, a further reduction of DAHP synthetase activity (15--25%) was routinely observed. Br Med J, 1980 Jul 12, 281(6233), 111 - 2 Antibiotics in surgical treatment of acute abscesses; Blick PW et al.; A four-way, double-blind, prospective trial of treatment of abscesses by incision, curettage, and primary closure with and without antibiotic cover (clindamycin injection before operation or capsules after operation, or both) was conducted . There was no appreciable difference in mean healing time between the patients given both the antibiotic injection and the antibiotic capsules and those given the injection and placebo capsules, whereas healing times in those given the placebo injection and antibiotic capsules or placebo only were appreciably longer . Four of the patients who were not given the antibiotic injection developed bacteraemia; one patient who was given the antibiotic injection also developed a bacteraemia, but this was caused by clindamycin-resistant bacteria . These results show that a single injection of an effective antibiotic before operation is sufficient to protect the patient against bacteraemia and permit optimum healing. Br J Dermatol, 1980 Jul, 103(1), 51 - 9 Neutrophil chemotaxis in the presence of antibiotics: a re-evaluation using an agarose technique; Gange RW; Neutrophil chemotaxis in the presence of tetracycline and clindamycin was evaluated using an agarose technique . No significant inhibition of chemotaxis by these antibiotics could be demonstrated, in contrast to previously reported findings using the Boyden chamber technique for measurement of chemotaxis . Both agents caused a minor increase in movement towards a P . acnes derived chemotactic factor . Some reduction of chemokinesis by high concentrations of tetracycline was noted . No effect of the drugs upon generation of chemotactic activity from whole serum could be demonstrated . Normal cell movement occurred in the absence of extracellular calcium and magnesium, in contrast to reported findings using the Boyden chamber. Can J Surg, 1980 Jul, 23(4), 366 - 9, 372 Use of a topical triple-antibiotic spray to reduce morbidity from pelvic infection after gynecologic operations; Wright VC et al.; To study the effect of a topical antibiotic spray in reducing postoperative morbidity when used during surgery, a randomized, double-blind study was done on 150 women who had a vaginal hysterectomy with or without colporrhaphy . The spray contained neomycin sulfate, polymyxin B sulfate and zinc bacitracin and was used in 75 patients; a placebo spray was used in the other 75 patients . The antibiotic spray significantly (P < 0.01) decreased the frequency of pelvic infections postoperatively--14.7% in the antibiotic group compared with 37.3% in the placebo group. J Biomed Mater Res, 1980 Jul, 14(4), 487 - 97 Interaction of the absorbable hemostatic agent (IP760) with aminoglycosidic antibiotics; Boyle VJ; The linear, crosslinked amylose-succinate hemostatic agent, IP760, has been evaluated for its interaction with aminoglycosidic antibiotics . The highly structured polymer appears to act as a cationic exchange resin which binds the basic aminoglycosides . Binding of these agents to IP760 is reversed by increased pH and/or increased ionic strength . Dialysis experiments demonstrated that 85 and 90% of the bound gentamicin was released at pH 7.5 and 8.0, respectively, over a period of 36 hr . Formation of the IP760-antibiotic complexes suggests potential medicinal use for hemostatis and slow release of the antibiotic for prophylaxis of postsurgical contamination or infection J Dairy Sci, 1980 Jul, 63(7), 1134 - 7 Sensitivities to antibiotics and seasonal occurrence of mastitis pathogens; Bishop JR et al.; In a 2-yr survey of the Clemson University's dairy herd, each sample of mastitic milk was cultured, and mastitis pathogens were isolated . Causative organisms then were subjected to disc assay of sensitivity to antibiotics . Antibiotics were penicillin, streptomycin, erythromycin, oxytetracycline, cephalothin (cephalosporin), ampicillin and novobiocin . The more widely used antibiotics--penicillin, streptomycin, and erythromycin--were relatively ineffective for bacterial sensitivity in vitro, whereas bacterial sensitivity in vitro for oxytetracycline and cephalothin was considerably more . These results also were true in vivo in treatment of animals in the University herd . Incidence of mastitis under our conditions of weather, housing, and management increased greatly during summer months with less increase during winter months. Drugs, 1980 Jul, 20(1), 57 - 68 Adverse antibiotic drug interactions; Bint AJ et al.; There is enormous potential for drug interactions in patients who, today, often receive many drugs . Antibiotics are prominent amongst the groups of drugs commonly prescribed . Many interactions take place at the absorption stage . Antacids and antidiarrhoeal preparations, in particular, can delay and reduce the absorption of antibiotics such as tetracyclines and clindamycin, by combining with them in the gastrointestinal tract to form chelates or complexes . Other drugs can affect gastric motility, which in turn often controls the rate at which antibiotics are absorbed . Some broad spectrum antibiotics can alter the bacterial flora of the gut which may be related to malabsorption states . The potentiation of toxic side effects of one drug by another is a common type of interaction . Antibiotics which are implicated in this type of interaction are those which themselves possess some toxicity such as aminoglycosides, some cephalosporins, tetracyclines and colistin . Some of the most important adverse interactions with antibiotics are those which involve other drugs which have a low toxicity/efficacy ratio . These include anticoagulants such as warfarin, anticonvulsants such as phenytoin and phenobarbitone and oral antidiabetic drugs like tolbutamide . Risk of interaction arises when the metabolism of these drugs is inhibited by liver microsomal enzyme inhibitors such as some sulphonamides and chloramphenicol, or is enhanced by enzyme inducers such as rifampicin. Ann Intern Med, 1980 Jul, 93(1), 1 - 8 Antibiotic therapy in Lyme disease; Steere AC et al.; We studied antibiotic efficacy in 113 patients with erythema chronicum migrans, the first manifestation of Lyme disease . Erythema chronicum migrans and its associated symptoms resolved faster in patients given penicillin or tetracycline (median duration, 4 and 2 days, respectively) than in untreated patients (10 days; P less than 0.001 and P = 0.005, respectively) . Erythromycin had no significant effect . Although the frequency of subsequent neurologic and cardiac abnormalities was similar in all four groups, significantly fewer patients given penicillin developed arthritis than did untreated patients (P = 0.001) . Among 15 patients with arthritis who were followed for at least 29 months, the total duration of joint involvement was shorter in penicillin-treated patients (median, 4 weeks) than in untreated patients (17 weeks; P = 0.019) . Although the clinical manifestations of the disease may fluctuate in frequency from year to year and influence apparent antibiotic effect, we conclude that penicillin therapy shortens the duration of erythema chronicum migrans and may prevent or attenuate subsequent arthritis. Minerva Med, 1980 Jun 30, 71(26), 1873 - 8 {The use of a new antibiotic for local administration in burns}; Giuliani V et al.; A new antibiotic already available on the market (meclocyclin) was experimented on 27 patients aged 45 days to 66 yr with burns due to various causes . Tolerance was excellent in all cases and the average hospital stay was 16 days . Two ointments (one containing meclocyclin, the other containing a different bacteriostatic) were applied on symmetrical sites . The results were practically the same . The meclocyclin ointment can be regarded as preferable, however, owing to its excellent tolerance, and non-absorption into the circulation, so that sensitisation cannot occur even during protracted administration . Another ointment, containing meclocyclin and fluochinolone, was also used in the presence of hypertrophic or keloid pathological scars . Useful results were obtained with regard to both the extent of the damaged areas and the functional limitations sometimes observed . Treatment in these cases, however, was sometimes prolonged for months. Biochemistry, 1980 Jun 24, 19(13), 3069 - 73 Mechanism of the antibiotic action of alpha-dehydrobiotin; Piffeteau A et al.; alpha-Dehydrobiotin, a naturally occurring biotin analogue, exhibits antibiotic properties {Hanka, L . J., Reineke, L . M., & Martin, D . G.(1969) J . Bacteriol . 100, 42--46} . It is shown in this paper that in addition to its activity as corepressor of the transcription of the biotin locus {Guha, A., Saturen, Y., & Szybalski, W . (1971) J . Mol . Biol . 56, 53--62} alpha-dehydrobiotin acts at the enzyme level . The synthesis of specifically tritiated alpha-dehydrobiotin has been achieved . By use of this labeled compound and a biotin-department strain of Escherichia coli, it has been demonstrated that alpha-dehydrobiotin can be linked covalently to proteins without further transformation . The fixation of biotin to apocarboxylases is inhibited irreversibly after preincubation with alpha-dehydrobiotin . This strongly supports the hypothesis that alpha-dehydrobiotin can be specifically linked to apocarboxylases in place of biotin and leads to carboxylases that are inactive . Thus, the antibiotic properties of alpha-dehydrobiotin would be partly due to the fact that it compete with biotin for the fixation on the apocarboxylases, producing irreversibly inactive enzymes. Biochim Biophys Acta, 1980 Jun 20, 599(1), 280 - 93 Interaction between phospholipid bilayer membranes and the polyene antibiotic amphotericin B: lipid state and cholesterol content dependence; Bolard J et al.; The interaction between amphotericin B and egg yolk phosphatidylcholine, dimyristoyl (DMPC) and dipalmitoyl phosphatidylcholine (DPPC) phospholipid bilayer vesicles has been monitored by the circular dichroism (CD) spectra of amphotericin B at a 1 . 10(-5) M concentration . This method has revealed that amphotericin B may be present in a number of different forms depending on the time elapsed after the mixing, the cholesterol content of the vesicles and the vesicles' physical state . Some striking features of these CD detected species are the following: with egg yolk phosphatidylcholine and a molar cholesterol percentage lower than 25, at 25 degrees C several forms are coexistent, their amount is time-dependent; with dipalmitoyl or dimyristoyl phosphatidylcholines without cholesterol or with a cholesterol molar percentage lower than 25, in the gel state, a form different from the former appears very rapidly; with egg yolk phosphatidylcholine, DMPC and DPPC at a molar cholesterol percentage between 25 and 50 a new form is monitored, identical in the three cases and observed in the liquid crystalline state as well as in the gel state . In the case of the three phospholipids without cholesterol a definite interaction with the antibiotic is observed but with different characteristics according to the nature of lipid . With amphotericin B 'Fungizone' the same species are monitored but their appearance is much slower . Two explanations are proposed for the origin of the discrepancies between CD and electronic absorption. Gann, 1980 Jun, 71(3), 308 - 12 Antitumor effect of a new antibiotic, neothramycin; Hisamatsu T et al.; A new anthramycin-group antitumor antibiotic, neothramycin, isolated from a Streptomyces culture, showed activity against experimental tumors such as lymphocytic leukemia P388 ascites sarcoma-180, hepatoma AH130, Walker carcinosarcoma-256 and mouse mammary adenocarcinoma (CCMT) . In particular, the tumor growth inhibition ratio was as high as 96% when neothramycin was injected intraperitoneally at a daily dose of 2 mg/kg into Wistar strain rats previously inoculated with Walker carcinosarcoma-256 by the subcutaneous route . Successive intraperitoneal injections of the compound were more effective than a single injection with the P388 system. Res Commun Chem Pathol Pharmacol, 1980 Jun, 28(3), 497 - 504 Embryotoxicity and teratogenicity of the anthracycline antibiotic carminomycin in mice; Damjanov I et al.; Carminomycin, a new antitumor anthracycline antibiotic, has embryolethal, embryotoxic and teratogenic effects during early postimplantation stages of development in mice . These effects depend on the dose and route of administration and the gestational age of the exposed embryos. Antibiotiki, 1980 Jun, 25(6), 440 - 4 {Surface activity of polyene antibiotics}; Etingova NI; The surface activity properties of polyenic antibiotics, such as amphotericin B, mycoheptin, levorin and nystatin were studied . The critical concentrations for the mycella formation were determined and the values of the polyenic antibiotic surface activity at various temperatures were estimated . It was found that the process of the mycella formation of polyenic antibiotics was defined by a positive change in the entropy . A thermodynamic analysis of the process of the mycella formation of the polyenic antibiotics in aqueous solutions was performed. Nippon Heikatsukin Gakkai Zasshi, 1980 Jun, 16(2), 93 - 7 {Effects of some kinds of antibiotics on the electrical and mechanical activities of guinea-pig taenia coli (author's transl)}; Nakai Y; Effects of some kinds of antibiotics on the electrical and mechanical activities of guinea-pig taenia coli were investigated . The sucrose gap method was used for measurement of electrical activity and simultaneously isometric tension was recorded . Both cephalothin (2.4 mM) and lincomycin (2.2 mM) did not cause any effect on the spontaneous electrical and mechanical activities . Chloramphenicol (3.1 mM) completely abolished the spontaneous spike discharges and relaxed the smooth muscle in a short time, while clindamycin (2.2 mM) took a long time to produce an effect as same as chloramphenicol . Both chloramphenicol and clindamycin abolished the stimulus-induced spikes and Sr-spikes . All of these responses were reversible by washing out with normal Krebs solution . These results suggest that chloramphenicol and clindamycin may inhibit Ca2+ influx through the Ca2+ channels across the smooth muscle cell membrane. J Antibiot (Tokyo), 1980 Jun, 33(6), 591 - 9 Characterization of aromatic heptaene macrolide antibiotics by high performance liquid chromatography; Mechlinski W et al.; High performance liquid chromatographic (HPLC) procedures were utilized for the rapid and efficient separation and characterization of the aromatic heptaene macrolide group of antifungal antibiotics . The instrument utilized a 350 nm phosphor converted ultraviolet detector and a mu Bondapak C18 column packing . Optimum resolution of eleven commercial aromatic heptaene macrolide preparations was obtained with solvent systems consisting of mixtures of acetonitrile and 0.05 M aqueous sodium citrate buffer, pH 5.3 . The presence of two distinct types of aromatic heptaene macrolides with numerous well-defined individual components has been established. Antibiotiki, 1980 Jun, 25(6), 411 - 5 {Action of antibiotics on the growth and metabolic processes of streptomycetes and Nocardia}; Toropova EG et al.; New experimental data on the effect of novobiocin, ristomycin and nystatin on growth and metabolism of Streptomycetes and Nocardia are presented . The study of the organisms producing other antibiotics showed that they were tens, hundreds and even thousands times more sensitive to the tested biologically active compounds than the organisms producing these compounds . The protein synthesis and antibiotic biosynthesis proved to be most sensitive out of the processes studied . The findings showed that during their evolution the antibiotic-producing organisms have developed definite protective mechanisms which enable them to resist relatively high concentrations of their own metabolites (antibiotics) . This ensures them in their struggle for existence. Antibiotiki, 1980 Jun, 25(6), 403 - 7 {Biosynthesis of the antibiotic, grizin, by prototrophic revertants of Streptomyces griseus biochemical mutants}; Kuklin VV et al.; Spontaneous and nitrosomethylbiuret-induced prototrophic revertants of various biochemical mutants of Str . griseus producing grisin, a streptothricin antibiotic, were isolated . The antibiotic production level of the revertants was studied . It was found that most of the prototrophic revertants synthesized much higher amounts of grisin than the initial biochemical mutants . It was also shown that a number of the prototrophic revertants of the methionine- and arginine-dependent mutants synthesized 20-23% higher amounts of grisin as compared to the control. J Pharm Pharmacol, 1980 Jun, 32(6), 394 - 8 The use of liposomes as a model for drug absorption: beta-lactam antibiotics; Kimura T et al.; Liposomes were prepared from egg phosphatidylcholine-cholesterol-diacetylphosphate (80:20:5) and total lipid extracts of rat intestinal mucosa, and the permeabilty of the liposomal membrane to eight beta-lactam antibiotics was studied by using a dynamic dialysis method . Although all the antibiotics used here are ionized and poorly lipid-soluble at pH 6.5, some of them are orally active and efficiently absorbed from the small intestine . The release rate constants from the aqueous dispersion of drug-entrapped liposomes were approximately in the order of their absorbability . Intestinal lipid liposomes were more permeable to the antibiotics than egg lecithin liposomes and the release rate constants for the drugs from intestinal lipid liposomes were strongly correlative with their absorption rate constants, except for cephalothin and ampicilin, the deviations of which could be explained by their surface activity . It is suggested that lipid components of the intestinal mucosa and the bilayer structure may play an important role in the absorption process of the antibiotics . The validity of liposomes as a model for the intestinal absorption of drugs is also discussed. Minerva Med, 1980 May 19, 71(20), 1453 - 8 {Effect of antibiotics on spontaneous and direct migration of human leukocytes . Preliminary findings}; De Simone C et al.; Like other human blood cells, neutrophiles can travel enter tissues spontaneously . This apparently casual journeying is arrested in the presence of infection and they migrate to the site of the lesion . Experiments in vitro have shown that tetracycline, rifamycin, chloramphenicol, and cefuroxine inhibit such migration . In the present paper, it is demonstrated that ampicillin and tauglycolcillin, a new semi-synthetic penicillin, exert no significant influence on either direct or spontaneous neutrophile migration. Philos Trans R Soc Lond B Biol Sci, 1980 May 16, 289(1036), 169 - 72 Recent biosynthetic studies on beta-lactam antibiotics; Baldwin JE et al.; Recent experimental observations on the cell-free formation of penicillins and cephalosporins in protoplast lysates from C . acremonium are described . Conversion of radiolabelled penicillin N into deacetoxycephalosporin C is described . A proposal is made about the general types of mechanism involved in these conversions. Experientia, 1980 May 15, 36(5), 550 - 2 The effect of two new peptide antibiotics, the hypelcins, on mitochondrial function; Takaishi Y et al.; The action on mitochondria of 3 peptide antibiotics, hypelcin-A, hypelcin-B, and alamethicin, was examined . The results showed that they are unique uncouplers of oxidative phosphorylation, with the same mechanism of action. Z Kardiol, 1980 May, 69(5), 329 - 33 {The treatment of digitalis poisoning with antibiotics (author's transl)}; Hess T et al.; Digitalis intoxication occurs frequently and proves fatal in 5-10% of all cases . Treatment is limited to symptomatic measures . Glycoside-specific antibodies offer a new way of treatment of digitalis intoxication . In our experiments with cats, they were found to be highly effective in reversing digoxin-induced arrhythmias . Specific antibodies have previously been employed in a patient with suicidal digoxin intoxication . We report a case of nonsuicidal Lanatosid-C intoxication treated with F(ab')2-fragments of digoxin-specific antibodies from the sheep . The treatment was successful and without side-effects . Serum concentration of free digoxin and total digoxin measured during and after treatment showed a decrease of free and a sharp raise in total digoxin . For clinical use, antibody fragments are superior to intact antibodies . Problems and possible indications concerning the treatment of digitalis intoxication with antibodies are briefly discussed. Antimicrob Agents Chemother, 1980 May, 17(5), 779 - 83 Concentrations of various antibiotics in serum and fluids accumulated in diffusion chambers implanted in various sites in rabbits; Georgopoulos A et al.; Diffusion chambers with Millipore membranes were implanted in soft tissue, kidneys, and peritoneal and pleural cavities of rabbits . Single doses of azlocillin, cefazolin, and gentamicin were injected intramuscularly and ampicillin was administered orally 2--5 weeks after implantation . The concentrations of the respective drugs in simultaneously collected samples of fluid from each diffusion chamber were measured and compared with concentrations found at the same time in serum . All chambers were tolerated well, and the method proved to be effective for collecting data on the distribution of drugs throughout the body. Antibiotiki, 1980 May, 25(5), 383 - 7 {Clinical manifestations and the ways to prevent antibiotic allergy in nonspecific pulmonary pathology}; Gurin NG; Retrospective analysis of 555 cases with nonspecific pulmonary pathology was performed . Certain allergic reactions to antibiotics were revealed in 172 (30.8%) patients, while the physicians recorded such reactions only in 65 (11.7%) patients . Allergy to 2 or more drugs was more frequent . Antibiotic intolerance was mainly evident from the temperature increase (44%), skin eruption (22%), development or aggravation of the bronchospastic syndrome (12.2%), Quincke's edema (69%), blood eosinophilia (6.9%) and sometimes other reactions . The bronchospastic syndrome was largely observed in patients treated with antibiotic inhalations . Clinical manifestations of antibiotic allergy were concomitant in most cases . The temperature increase, skin eruptions and blood eosinophilia may be considered as the early manifestations of the allergy, while impairment of the bronchial patency as the late manifestation . Intolerance of antibiotics significantly lowers their efficiency . Rational use of antibiotics, due regard for the history of allergic reactions and in vitro tests for antibiotic susceptibility are important measures in prevention of allergic reactions to antibiotics. Ann Microbiol (Paris), 1980 May-Jun, 131(3), 271 - 83 {Use of Autobac system in the study of the bacteriostatic effect of combinations of antibiotics (author's transl)}; Darbas H et al.; After determining the LSI80 (light scattering index 80) concentration X and Y of two antibiotics for a given bacteria by an automated light scatter photometric method, we use the same process to test the bacteriostatic effect of all the combinations between the values 2X, X, X/2, X/4, X/8 and 2Y, Y, Y/2, Y/4, Y/8 . The results read on the light scatter photometer are interpreted: --approximatealy by means of a simplified schematic diagram; --more precisely by drawing three curves: we begin with two inhibiton curves in order to determine the LSI50 concentrations (CLSI50) of each antibiotic, isolted and in the presence of defined concentrations of the complementary antibiotic; then from these CLSI50 we draw the bacteriostatic effect curve of the combination . When the LSI50 effect of the combination occurs with less than 50% of the CLSI50 of each isolated antibiotic, the combination is synergistic . It is antagonist if the bacteriostase is obtained with more than 100% of the CLSI50 of each isolated antibiotic . The intermediate percentages determine the indifferent effects . The additive effects come to an equilateral hyperbola passing through the points 50%-50%, 25%-75% . The Autobac system allows inoculum standardization, very simplified handlihg and automatic reading . It takes only 9 h to handle the complete process, including the determinations of the CLSI80 and the study of the combination . There is a high correlation between the results obtained and those given by the Patte and Chabbert "carre method". Vestn Khir Im I I Grek, 1980 May, 124(5), 57 - 61 {Value of antibiotics in treated acute cholecystitis in elderly patients}; Sovtsov SA; The treatment of 673 patients with acute cholecystitis aged 70 and more was analyzed . Half of the patients were treated with antibiotics . Under study were 110 antibioticograms of bile of the operated patients . In 71% Escherichia coli was found sensible to tetracycline, chloramphenicol, monomycin and kanamycin . The results of the investigation show that use of antibiotics of the tetracycline order for the treatment of acute cholecystitic results in decreased mortality of patients aged 70 and older. Arch Esp Urol, 1980 May-Jun, 33(3), 261 - 6 {Local antibiotic therapy in the treatment of chronic bacterial prostatitis}; Muntanola P et al.; In view of the great incidence of bacterial prostatitis and the small number of antibiotics which reach significant levels in the prostate gland, we have used Baert's local antibiotherapy on 24 patients suffering from chronic, bacterial prostatitis and in whom, previous treatment with trimethoprim-sulphamethoxazol had failed . 95.9% of sterilizations of prostate liquid growths were obtained six months after the treatment. Antimicrob Agents Chemother, 1980 May, 17(5), 861 - 4 Effect of fatty acids on action of polyene antibiotics; Iannitelli RC et al.; Fatty acids cause a decrease in the absorption spectra of the antifungal polyene macrolide antibiotics nystatin, filipin, candicidin, and amphotericin B . For nystatin, filipin, and candicidin, this decrease in absorption could be correlated with the activity of the fatty acids in protecting the yeast Saccharomyces cerevisiae against the action of these antibiotics . With amphotericin B a correlation was observed between the decrease in absorption caused by certain derivatives of fatty acids and the protective action of these derivatives against the activity of amphotericin B on yeast . It is concluded that, like the sterols, fatty acids also interact with the polyene antibiotics and thereby reduce their effective concentrations. Antibiotiki, 1980 May, 25(5), 375 - 81 {Experimental study of a new method of endolymphatic antibiotic administration and a trial of its clinical use}; Shcherbakova EG et al.; A new procedure for antibiotic administration via endolymphatic route was developed . Experiments performed on 34 dogs revealed differences in the pharmacokinetics of gentamicin in the central lymph after its administration in a dose of 4 mg/kg via endolymphatic and intramuscular routes: the maximum levels of 590 and 23 mg/kg were determined in 15 and 45 minutes respectively . In 1 hour the concentrations decreased to 17 and 10 mg/kg . When gentamicin was administered endolymphatically it remained in the lymph and blood in concentrations of 0.2 and 0.8 mg/kg respectively for 24 hours . The kinetics of gentamicin in the blood serum within the first 6 hours after its administration by both routes did not differ significantly . After endolymphatic administration high concentrations of gentamicin (56-36 mg/g) were determined in the paraaortal and retroperitoneal lymph nodes in 10-24 hours . Within the period of the 4th to the 13th day its concentrations of at least 5 mg/g were detected . The changes in the structure of the lymph nodes observed 18-48 hours after the antibiotic endolymphatic administration were reversible and returned to normal by the 96th hour . The first experience with the clinical use of the endolymphatic route of gentamicin administration showed its high efficacy in 84.8% of the patients with severe purulent inflammatory diseases of the organs of the abdominal cavity . The antibiotic was used in a dose of 80 mg once a day . The treatment course consisted of 5-6 infusions . Perspectives of the further experimental and clinical investigation of the procedure are indicated . Endolymphatic administration of antibiotics makes it possible to increase the efficacy of antibiotic therapy of a number of severe inflammatory infections. Obstet Gynecol, 1980 May, 55(5 Suppl), 128S - 138S Therapeutic considerations in the use of antibiotics in renal insufficiency; Whelton A; Virtually all antibiotics are excreted in part or in total by the kidneys . Therefore in various degrees of renal function impairment, systemic drug accumulation with dose-related toxicity may take place unless a readjustment is made in standard drug dosing principles . Good clinical practice dictates that the physician have some familiarity with the drug dosing changes that are necessary when patients with renal failure require antibiotic therapy . Correlation of the patient's renal function status with the selected antibiotic is the first step, after which drug dosing tables and nomograms serve as an immediate and practical guide to safe and effective therapy . Antibiotic dosing regimens in renal failure should always be monitored by analysis of serum drug levels when available to the clinician, as this is the best confirmation of safe and effective therapy . This review contains detailed metabolic and pharmacokinetic information that may be used as an additional clinical resource for the antibiotic therapy of patients with renal insufficiency. Minerva Stomatol, 1980 May-Jun, 29(3), 163 - 82 {Fractures with loss of substance of the middle and upper third of the face: nosographic classification, surgical indications and the prevention of meningeal infections with the new antibiotic, cefuroxime}; Torrielli F et al.; Reference is made to considerable personal experience acquired in the treatment of craniofacial fractures, particularly those affecting the upper third of the face . An account is given of the anatomical and surgical features of the naso-ethmoid-frontal and temporo-orbito-sphenoid areas--now recognised as within the domain of maxillofacial surgery--and their symptomatologies . Particular attention is directed to the question of liquorrhoea and the possibility of ascendent infections of the meninges . Reduction is favoured with respect to the former, since forward and upward repositioning often leads to the regression of ethmoidal liquorrhoea . Exclusion of the frontal sinus is regarded as a "categorical imperative" as far as meningeal infection is concerned, and support is also given for its prevention with antibiotics . A personal preference is expressed for cefuroxim, a new antibiotic with particular potency and marked diffusibility within the cerebrospinal fluid. J Antibiot (Tokyo), 1980 Apr, 33(4), 377 - 82 Studies on antibiotics BN-227 and BN-227-F, new antibiotics . II . Chemical structure of antibiotics BN-227 and BN-227-F; Itoh J et al.; The structure of a new antibiotic BN-227 was determined as I by physico-chemical methods . The X-ray analysis also suggested the structure of I . The structure of antibiotic BN-227-F was determined as II . The antibiotic BN-227-F was prepared by addition of a solution of ferric chloride to antibiotic BN-227. J Antibiot (Tokyo), 1980 Apr, 33(4), 364 - 76 Mycinamicins, new macrolide antibiotics . I . Taxonomy, production, isolation, characterization and properties; Satoi S et al.; Mycinamicins, novel macrolide antibiotics were obtained from the culture broth of Micromonospora grisseorubida sp . nov . Isolation of five components, mycinamicins I, II, III, IV and V, was accomplished by silica gel adsorption or partition chromatography . Mycinsmicin I and II exhibit a strong UV absorption peak at 218 nm and have a shoulder at 240 nm . Mycinamicin III, IV and V show strong UV absorption peaks at 215 nm and around 280 nm . From their physicochemical and biological properties, the mycinamicins are classified as new macrolide antibiotics. Antibiotiki, 1980 Apr, 25(4), 266 - 7 {Method of determining the concentration of the antibiotic nisin}; Baranova IP et al.; To accelerate determination of nizin concentrations by the agar-diffusion method it is suggested that Twin-80 be added to the agar . For making the media composition more simple, agarized phosphate buffer, pH 5.0, or agarized water, pH 7.0, is recommended to be used for the lower layer. South Med J, 1980 Apr, 73(4), 533 - 4 Successful treatment of empyema with thoracocenteses and intrapleural antibiotics; Mittapalli MR; Daily thoracocentesis and treatment with an appropriate antibiotic instilled into the pleural space, continued until the returns are clear, may still have a significant role in the treatment of empyema, thereby avoiding the discomforts and disadvantages of chest tube insertion. South Med J, 1980 Apr, 73(4), 444 - 7 Antibiotic-associated colitis: a persistent clinical problem; Davidson ED et al.; Examination of this series of 19 patients with antibiotic-associated pseudomembranous colitis revealed that most of the patients were given the antibiotics for trivial reasons . Many different antibiotics were identified as being related to the development of colitis . There were three deaths in this series; two of the 15 patients treated medically and one of the four treated surgically . The efficacy of all diagnostic procedures and medical therapies are discussed, and the role of surgery in treating patients with toxic state, sepsis, or perforation is presented. J Antibiot (Tokyo), 1980 Apr, 33(4), 441 - 6 Antibiotics that specifically block translation in virus-infected cells; Lacal JC et al.; Several antibiotics including anthelmycin, blasticidin S, destomycin A, gougerotin, hygromycin B and edeine complex, known to powerfully block translation in cell-free systems, did neither inhibit protein synthesis in intact mouse L and 3T6 cells, nor in hamster BHK 21 cells, due to failure to cross the cell plasma membrane . However, after viral infection, these antibiotics exhibited a marked blockade of translation, that is related to the permeability changes induced by viral infection . The inhibition of protein synthesis by hygromycin B in virus-infected cells was studied over the time course of infection, both in encephalomyocarditis virus-infected mouse L cells and in Semliki forest virus-infected hamster BHK cells . We have observed that the entry of hygromycin B into virus-infected cells parallels the inhibition of cellular protein synthesis, i.e., the cells became permeable to this antibiotic at the time the shut-off of host translation occurred . A marked inhibition of picornavirus RNA synthesis by hygromycin B was also noticed, likely as a consequence of the inhibition of the viral replicase synthesis . Finally, a reduction in the virus yield by treatment of virus-infected cells with several antibiotics is also described . All these observations are considered in the context of the interference of viral infection with cellular functions and the potential use of inhibitors non-permeable to normal cells as antiviral agents. Biochim Biophys Acta, 1980 Mar 28, 607(1), 171 - 80 Conformational analysis of nucleoside and nucleotide antibiotics prossessing five-membered base rings . A comparison of the glycosyl barrier for purine, pyrimidine and imidazole rings; Vijayaiakshmi KS et al.; The preferred conformations of the nucleosides comprising five-membered base rings viz., ribavirin, tetrazole, showdomycin and pyrazomycin and their 5'-nucleoside monophosphates have been explored by semiempirical potential energy calculations . The nature of the substituents on the five-membered base ring has been found to influence significantly the favoured glycosyl conformation and the hydrogen bonding between the base and the sugar . In the absence of any such hydrogen bonding, the imidazole nucleosides expectedly exhibit nearly 'free' rotation around the glycosyl bond for the commonly found C(3') endo and C(2') endo sugar ring conformations, thus increasing the probability of anti in equilibrium high-anti in equilibrium syn conformational interconversions as compared to common purine and pyrimidine nucleosides . However, the C(2') exo pucker imparts a high-energy barrier to glycosyl rotation, locking the base in the high-anti region . The conformation behaviour is significantly modified in the nucleoside 5'-monophosphates . The additional attractive interactions between the carboxamide and the phosphate groups favour the syn glycosyl conformation in the 5'-monophosphates of ribavirin as well as pyrazomycin smaller to guanosine 5'-monophosphate whereas the anti conformation is strongly favoured for the 5'-nucleotides of tetrazole and showdomycin similar to other common purine and pyrimidine nucleotides . The conformational properties of five-membered base ring nucleosides have a strong resemblance to purine nucleosides . Molecular modelling studies reveal that only the anti or high anti-glycosyl conformations of ribavirin can mimic the inosine base . It is suggested that experiments on the configurational isomers of ribavirin, viz., aravirin and cycloaravirin would conclusively establish the conformational specificity and biological function of ribavirin and analogues. Br Med J, 1980 Mar 22, 280(6217), 836 - 8 Family trends in psychotropic and antibiotic prescribing in general practice; Howie JG et al.; A ten-year retrospective study of the consultations of 50 families with a city general practice was used to test the hypothesis that mothers who receive an excess of psychotropic drugs have children who receive an excess of psychotropic drugs have children who receive an excess of antibiotics for episodes of acute respiratory illness . The children of the 10 mothers classed as high psychotropic users were seen twice as often with acute respiratory illness and received twice as many antibiotics as the children of the mothers who had received no psychotropic medication . The association between high psychotropic and high antibiotic use was not linked in time, and indeed the time of highest antibiotic use coincided with the time when the mother received fewest psychotropic prescriptions . It is suggested that at many of these consultations the mother rather than the child should have been treated as the patient. Biochemistry, 1980 Mar 4, 19(5), 865 - 70 Interaction of elongation factor Tu with the ribosome . A study using the antibiotic kirromycin; Sander G et al.; Elongation factor Tu (EF-Tu) dependent GTP hydrolysis normally requires the presence of ribosomes and aminoacyl-tRNA (aa-tRNA) . In the presence of the antibiotic kirromycin, the factor alone displays a GTPase activity that is enhanced by ribosomes and/or aa-tRNA {Wolf, H., Chinali, G., & Parmeggiani, A . (1974) Proc . Natl . Acad . Sci . U.S.A . 71, 4910-4914} . Using this system, we have found the following: (1) the 50S ribosomal subunit can substitute the 70S ribosome; (2) the 50S CsCl core a, b, and c particles {Sander, G., Marsh, R . C., Voigt, J., & Parmeggiani, A . (1975) Biochemistry 14, 1805-1814}, lacking an increasing number of proteins, can induce ca . 65, 45, and 25%, respectively, of the EF-Tu-kirromycin GTPase activity of control 50S subunits, in the presence of 30S subunits and aa-tRNA; (3) addition of proteins L7/L12 with L10, but not of proteins L7/L12 free from L10, restored the activity of all the 50S CsCl cores in the EF-Tu-kirromycin-dependent GTPase to 70-90% of the control; (4) proteins L7/L12, with or without contaminating L10, did not induce any EF-Tu-dependent GTPase activity, in contrast to a recent report {Donner, D., Villems, R., Liljas, A., & Kurland, C . G . (1978) Proc . Natl . Acad . Sci . U.S.A . 75, 3192-3195}, whether EF-Ts and/or kirromycin were present or not. Pol J Pharmacol Pharm, 1980 Mar-Apr, 32(2), 217 - 24 Toxicological studies on the new veterinary antibiotic turimycin; Hartl A et al.; The acute toxicity of turimycin investigated in several animal species and following different routes of administration is low . In mice the LD50 values range from 320 mk/kg after iv injection up to more than 3000 mg/kg when administered orally . When lethal or sublethal doses of turimycin were given, animals either developed clonic convulsions and died within 24 hr, or recovered completely . The main pharmacological effect of turimycin is a reversible, dose dependent decrease in the blood pressure after intravenous injection of 10 to 15 mg/kg in cats and dogs . This may be due to the negative inotropic and chronotropic effect on heart muscle (isolated atria of guinea-pigs) and to the spasmolytic effect on the smooth muscle (rat ileum) . A temporary decrease of the renal filtration rate after administration of turimycin is probably caused by its influence on the blood pressure . In rats the hexobarbital sleeping time was increased after repeated administration of higher doses of turimycin . In a chronic study on dogs oral doses of 50 and 125 mg/kg of turimycin, given in capsules daily for 12 months, produced no functional or histopathological abnormalities. Res Commun Chem Pathol Pharmacol, 1980 Mar, 27(3), 521 - 31 Alterations of mitochondrial respiration induced by aminoglycoside antibiotics; Weinberg JM et al.; In vitro gentamicin treatment stimulates State 4 mitochondrial respiration and inhibits State 3 and DNP-uncoupled respiration . These effects are qualitatively similar in both hepatic and renal mitochondria . Threshold gentamicin concentrations for these effects were between 1 and 2 mM for renal mitochondria while hepatic mitochondria were slightly more sensitive . Neomycin, kanamycin, and streptomycin had effects qualitatively similar to those of gentamicin on State 4, State 3, and DNP-uncoupled respiration . The potency of the aminoglycosides in producing these effects strongly correlated with the number of ionizable amino groups present on the aminoglycoside molecule suggesting that cationic charge is an important molecular determinant of aminoglycoside-induced mitochondrial toxicity. J Pharm Sci, 1980 Mar, 69(3), 354 - 6 Serum protein binding alterations of selected cephalosporin antibiotics by fatty acids and their derivatives; Pitkin DH et al.; Saturated fatty acids containing 10--14 carbon atoms were more potent inhibitors of serum protein binding than those containing shorter or longer carbon chains . Introduction of unsaturation into chains containing 16 or 18 carbons increased their inhibitory potency . Triglycerides and fatty acid esters, chlorides, thiols, and amides had no inhibitory activity . When inhibition was observed, it was concentration dependent and occurred when the molar ratio of fatty acid to protein equaled or exceeded three . The change in percent serum protein binding in the presence of an effective inhibitor was the greatest with cephalosporins that were most highly bound in the absence of an inhibitor. J Antibiot (Tokyo), 1980 Mar, 33(3), 280 - 3 FR-900137, a new antibiotic . II . Structure determination of FR-900137; Kuroda Y et al.; The structure of FR-900137, a new antibiotic produced by a new strain of Streptomyces has been established as methyl hydrogen N1-methyl N2-(L)-leucyl phosphorohydrazidate on the basis of spectroscopic and chemical evidence. J Antibiot (Tokyo), 1980 Mar, 33(3), 267 - 71 FR-900148, a new antibiotic . II . Structure determination of FR-900148; Kuroda Y et al.; The structure of FR-900148, a new antibiotic produced by a strain of Streptomyces xanthocidicus, has been established as 1-N-valyl-3-chloro-2,5-dihydro-5-oxo-1H-pyrrole-2-carboxylic acid on the basis of spectroscopic and chemical evidence. Clin Orthop, 1980 Mar-Apr, (147), 167 - 9 The effect of previous surgery, operating room environment, and preventive antibiotics on postoperative infection following total hip arthroplasty; Nelson JP et al.; In 711 consecutive total hip arthroplasty operations, approximately 80% of patients were followed one to 7 years . Per priman operations outnumbered hips having had previous operations 511 to 200 . The incidence of infection was higher in the hips having had previous operations (1.6 vs 3.5%) . The overall incidence of deep infection was 16/711, or 23% . Analysis of the influences of operating room environment and preventative antibiotics revealed that there was a marked decrease in the attack rate of deep infection (7.6 vs 0.6%) when the Clean Room, personnel-isolator system, and preventative antibiotics were used . Reduced intraoperative wound bacterial contamination is accompanied by a reduced incidence of sepsis. Gastroenterology, 1980 Mar, 78(3), 431 - 4 Symptomatic relapse after oral vancomycin therapy of antibiotic-associated pseudomembranous colitis; Bartlett JG et al.; Twenty patients with antimicrobiol-associated diarrhea had a symptomatic relapse after oral vancomycin therapy . All patients had stool examinations which implicated C . difficile as the causative agent, and 16 had pseudomembranous colitis . Clinical courses were characterized by resolution of symptoms with recurrence of diarrhea at 4--21 days after vancomycin was discontinued . Studies of stools collected sequentially showed that vancomycin failed to eliminate C . difficile despite susceptibility to this agent with in vitro testing . A review of our records shows the incidence os symptomatic relapse is approximately 14% . This experience emphasizes the importance of adequate follow-up in patients treated with oral vancomycin for antibiotic-associated diarrhea or colitis due to C . difficile. J Antibiot (Tokyo), 1980 Mar, 33(3), 310 - 6 A novel method for evaluating the outer membrane permeability to beta-lactamase-stable beta-lactam antibiotics; Kojo H et al.; A novel method is described which allows estimation of the outer membrane permeability to beta-lactamase-stable beta-lactams by determining antibiotic concentrations in the periplasm . The method is based on measurement of the inhibiting activity of beta-lactamase-stable beta-lactams on the hydrolysis of a substrate by periplasmic beta-lactamase . Application of the method to carbenicillin revealed that the high level of resistance to carbenicillin of an Escherichia coli strain acquiring the plasmid encoding ampicillin resistance resulted from the poor ability of carbenicillin to penetrate the outer membrane of E . coli. Br Med J, 1980 Feb 2, 280(6210), 275 - 7 Rational use of antibiotic therapy after appendicectomy; Pinto DJ et al.; A prospective randomised trial was carried out on 263 patients admitted for appendicectomy . In those patients with normal or inflamed appendix only, wound sepsis occurred in five (5%) of the 96 patients receiving metronidazole compared with seven (7%) of the 91 controls . In patients with gangrenous or perforated appendices, however, 15 of the 32 patients (47%) receiving ampicillin and five (16%) of 31 patients receiving metronidazole developed a wound infection (p less than 0.025) . Therapeutic courses of metronidazole significantly reduced wound sepsis rate in those with gangrenous or perforated appendices . Together with another antibiotic it should form part of the management of such patients, but antibiotics are unlikely to reduce further the low rate of wound infection in patients with normal or inflamed appendices. Poult Sci, 1980 Feb, 59(2), 268 - 73 Compatibility and anticoccidial activity of lasalocid in combination with roxarsone and antibiotics against Eimeria mixed infection in chicks; Schildknecht EG et al.; Lasalocid at the concentration of .0075% (68 g/ton) with and without roxarsone 45.4 g/ton was fed in combination with the growth promotants bacitracin methylene disalicylate 200 g/ton, bambermycins 2 g/ton, lincomycin 4 g/ton, nosiheptide 2.5 g/ton, zinc bacitracin 200 g/ton g/ton, and virginiamycin 20 g/ton exhibited a high degree of anticoccidial activity against mixed Eimeria infection in chickens in 9 day challenged battery trials . In these short term challenge trials chicks fed lasalocid, and the lasalocid growth promotant combinations, performed significantly better (P < .05) for growth and anticoccidial efficacy than those fed the growth promotants alone, and the infected, unmedicated controls . In almost all instances, the lasalocid-roxarsone-antibiotic combinations allowed for numerical increases in gains, improvement in feed conversion, and numerical decreases in lesions (in some cases, statistically significant (P < .05) over chicks fed lasalocid alone and/or the lasalocid antibiotic combination . The growth promotants did not interfere with the anticoccidial activity of lasalocid . The growth promotants fed alone exhibited no anticoccidial activity . However, when roxarsone was combined with the antibiotics, the combination resulted in numerically improved performance, reduced mortality, and in most instances, statistically significant decreases in lesions (P .05) over the infected, unmedicated control. Chirurg, 1980 Feb, 51(2), 106 - 9 {Orthograde intestinal irrigation as a preoperative intestinal preparation . Reduction of the intestinal flora using antibiotics}; Huk I et al.; Whole gut irrigation is a now a well-established method of preoperative bowel preparation . Additional reduction of bacterial content is desirable . The influence of neomycin/bacitracin and clindamycin as well as the combination, as admixture to the whole gut irrigation, on the flora of the large intestine, was therefore investigated in a prospective controlled study . While neomycin/bacitracin caused only a reduction of aerobic, and clindamycin of the anaerobic bacteriae, the combination resulted in a nearly total eradication of detectable bacterial content at the time of operation. J Antibiot (Tokyo), 1980 Feb, 33(2), 205 - 12 Macbecins I and II, new antitumor antibiotics . II . Isolation and characterization; Muroi M et al.; New antitumor antibiotics, macbecins I and II, were isolated from the culture broth of Nocardia sp . No . C-14919 . Macbecins I and II belong to the ansamycin group and have a benzoquinone and hydroquinone nucleus, respectively . Both showed antitumor activity against murine leukemia P 388 in vivo. J Antibiot (Tokyo), 1980 Feb, 33(2), 144 - 56 Studies on the ionophorous antibiotics . XXV . The assignments of the 13C-NMR spectra of dianemycin and lenoremycin; Mizoue K et al.; All the resonances observed in the 13C-NMR spectra of polyether antibiotics, dianemycin and lenoremycin (Ro 21-6150) have been assigned by the aid of selective proton decoupling experiments, T1 value measurements and biosynthetic methods as well as comparison to model compounds such as monensin, nigericin, etheromycin and carriomycin. J Antibiot (Tokyo), 1980 Feb, 33(2), 132 - 6 FR-900130, a novel amino acid antibiotic . II . Isolation and structure elucidation of the acetyl derivative of FR-900130; Kuroda Y et al.; FR-900130 is a new antibiotic having an acetylene moiety and is very unstable in aqueous solution . The antibiotic was isolated as the acetyl derivative by ion-exchange resin and adsorption chromatography . The structure has been determined to be L-2-amino-3-butynoic acid by spectral data of its derivatives. Br J Surg, 1980 Feb, 67(2), 140 - 1 The delayed treatment of wounds of the hand and forearm under antibiotic cover; Morgan WJ et al.; In wounds of the hand and forearm treated within 4 h of injury, prophylactic clindamycin, in a dose of 150 mg 6-hourly for 5 days, did not reduce the infection rate . In wounds treated after 4 h the infection rate was reduced, but not significantly so . There was a significant reduction in the infection rate comparing all wounds treated within 4 h with those treated after 4 h . Early treatment of wounds is more important than prophylactic antibiotics, although these may have a part to play where late treatment is unavoidable. J Pharm Sci, 1980 Feb, 69(2), 229 - 30 13C-NMR spectroscopy of three tetracycline antibiotics: minocycline hydrochloride, meclocycline, and rolitetracycline; Mazzola EP et al.; 13C-NMR data and spectral assignments are presented for tetracycline antibiotics minocycline hydrochloride, meclocycline, and rolitetracycline. Antibiotiki, 1980 Feb, 25(2), 126 - 9 {Comparative study of rifampicin distribution in the body of pregnant and nonpregnant white rats exposed to the antibiotic by inhalation}; Zel'tser IZ et al.; When rifampicin was administered to albino rats in the form of inhalations, it was absorbed by the blood and penetrated into various organs, the levels of the antibiotic in the biosubstrates being dependent on its concentration in the inhalation air . Rifampicin distribution in the gravid animals was mainly of the same character as that in the nongravid rats . However, when the animals were exposed to the antibiotic effect during the whole period of the gravidity, a significant increase in the antibiotic levels in the blood and internal organs was observed. J Histochem Cytochem, 1980 Feb, 28(2), 161 - 8 Evaluation of the polyene antibiotic filipin as a cytochemical probe for membrane cholesterol; Robinson JM et al.; Distribution of the filipin-cholesterol complexes has been studied by freeze-fractures techniques . While filipin-cholesterol complexes are formed in fixed as well as unfixed cells, the distribution of the complexes varies with fixation . Furthermore, filipin induces dramatic rearrangement of intramembrane particles in unfixed, but not in fixed, cells . Examination of thin sections of filipin-treated cells shows that filipin alone induces substantial cellular damage, while filipin treatment simultaneous to fixation or following fixation does not cause noticeable damage . For filipin to be an effective cytochemical probe of membrane structure, cellular damage must be minimized; this is best achieved by treating cells with filipin following glutaraldehyde fixation. Cutis, 1980 Feb, 25(2), 216 - 8, 220 Topical antibiotic therapy of acne: laboratory investigation of vehicles, various antibiotics, and stability characteristics; Stoughton RB et al.; A new vehicle preparation has proved effective in enhancing the penetration of antibiotics . The vehicle seems to maintain stability of the incorporated antibiotic. Anaesth Intensive Care, 1980 Feb, 8(1), 34 - 8 Antibiotics--their administration, choice and prophylactic use; Goodwin CS; A wider range of antibiotics is now available with the advent of two new cephalosporins--cefamandole and cefuroxime, and the first cephamycin--cefoxitin . These drugs may be particularly useful in the treatment of septicaemia, and when combined with ticarcillin are effective against nearly all pathogens . Cefuroxime can be given intramuscularly . Intravenous cotrimoxazole must be given in large doses to achieve therapeutic concentrations in the cerebrospinal fluid . The correct use of antibiotics for prophylaxis demands an accurate knowledge of the organisms likely to cause infection and the most efficient way of using the antibiotics to prevent that infection . There is little argument about the need for prophylaxis to prevent recurrent rheumatic heart disease or tetanus from a contaminated wound . However, in the various areas of surgery a wide range of antibiotics is used not always as a result of controlled trials having proved their value . Non-surgical situations for prophylaxis are briefly reviewed. Antibiotiki, 1980 Feb, 25(2), 121 - 6 {Possibility of reversing the action of the membranotropic antibiotic, gramicidin S, on bacteria}; Bulgakov VG et al.; The study on the possibility of eliminating gramicidin S from the bacterial cells which had adsorbed it showed that a part of the labeled antibiotic bound by the bacteria may be washed out with buffer or salines . When the cells which had adsorbed gramicidin S were treated with lecithin emulsion, a significant part of the bound antibiotic was transferred to the lecithin liposomes . This turned the gramicidin S effect to the cells: significant but not complete reduction of the membrane barrier properties and dehydrogenase reactivation . Elimination of gramicidin S also reduced the colony forming capacity in a part of the cells. Methods Find Exp Clin Pharmacol, 1980 Feb, 2(1), 45 - 51 Neuromuscular blocking activity of aminoglycoside antibiotics; Paradelis AG et al.; The aminoglycoside antibiotics possess neuromuscular blocking activity; the potency of those antibiotics tested appears to be as follows: gentamicin greater than streptomycin greater than amikacin greater than sisomicin greater than kanamycin = tobramycin greater than kanendomycin = dibekacin . The neuromuscular blockade produced by these antibiotics is not reversed by neostigmine, whereas it is reversed by calcium . Calcium not only has the ability to restore the neuromuscular transmission but also to exert protective action against the neuromuscular blocking activity of aminoglycoside antibiotics; these antibiotics are also potentially capable of interacting with non-depolarizing muscle relaxant drugs (d-tubocurarine, pancuronium) or propranolol, a beta-adrenergic receptor blocking agent . This interaction results in respiratory depression and/or prolonged apnoea . Our findings lead to the assumption that amino-glycoside antibiotics are involved in the process of acetylcholine release by nerve impulses, antagonizing calcium ions. Arch Microbiol, 1980 Feb, 124(2-3), 229 - 32 In vitro degradation of guanosine 3',5'-bis(diphosphate) {ppGpp} by the spoT gene product {ppGppase} from auxotrophic strains of Escherichia coli: effects of various antibiotics and drugs; Richter D; The enzyme specifically hydrolyzing guanosine 3',5'-bis(diphosphate) {ppGpp} has been isolated from the ribosomal fraction of Escherichia coli; it released pyrophosphate from the 3'-position of ppGpp . The effects of various drugs and antibiotics known to interfere with protein and/or RNA synthesis were investigated in the ppGpp degrading reaction . It was determined that tetracycline, chlorotetracycline, and thiostrepton strongly inhibited the reaction, whereas levallorphan gave a moderate inhibition . Only the tetracycline-mediated inhibition could be reversed by manganese ions . Oxytetracycline, rifampicin, fusidic acid, kirromycin, streptomycin, puromycin, chloramphenicol, and morphine did not inhibit the decay reaction. S Afr Med J, 1980 Jan 26, 57(4), 114 - 6 {Antibiotic peritoneal lavage in acute peritonitis resulting from septic abortion or a ruptured pyosalpinx}; Nel H; An analysis is given of 16 patients who presented with acute peritonitis during the years 1976-1978 and who were treated by means of antibiotic peritoneal lavage . The history and technique of peritoneal laage are discussed. Biochim Biophys Acta, 1980 Jan 25, 595(2), 277 - 90 Selective release of non-electrolytes from liposomes upon perturbation of bilayers by temperature change or polyene antibiotics; Oku N et al.; A new system for assaying the permeability characteristics of liposomes was established using Amicon cells equipped with a membrane filter (pore size, 0.3 micrometer) . In this system, damage of liposomes during the assay procedure was negligible . Changes in permeability to non-electrolytes, such as glucose (Mr 180), sucrose (Mr 342), inulin (Mr 5000) and dextran (Mr 75000), induced by perturbation of the bilayers were examined with this system . The following results were obtained on the barrier properties of multilamellar liposomes modified by various treatments . 1 . Amphotericin B and nystatin did not cause any change in permeability to glucose of egg yolk phosphatidylcholine liposomes prepared in physiological saline and containing trace amounts of radioactive markers in their aqueous compartments . Both antibiotics, however, induced nonspecific release of glucose, sucrose, inulin and dextran from liposomes that contained 0.3 M glucose in their aqueous compartments . These antibiotics first seem to form pores through which small ions can permeate; Na+ and Cl- can enter the liposomes through these pores, whereas glucose in the liposomes cannot pass out . As a result, the liposomes become swollen with consequent severe disruption of their membranes . 2 . Filipin and digitonin disrupted the membrane structures, resulting in release of large molecules such as dextran even in the absence of an osmotic mechanism . 3 . Perturbation of the phase equilibrium by temperature change resulted in formation of 'pores' . The penetration of cations and anions through these 'pores' was apparently much faster than that of glucose, since when liposomes swollen in 0.3 M glucose were incubated in salt solution they were disrupted by an osmotic mechanism releasing not only glucose but also dextran . Most of the 'pores' were not large enough to allow passage of large non-electrolytes, such as inulin and dextran, since no appreciable amounts of these markers were released from liposomes under conditions where there should be no osmotic gradient . 4 . At a temperature well above the phase transition temperature, egg yolk phosphatidylcholine liposomes exhibited specific release of glucose . This process did not involve an osmotic gradient, indicating that it was mainly due to diffusion of the solutes through the bilayers. Can Med Assoc J, 1980 Jan 12, 122(1), 49 - 52 Antibiotic misuse in a pediatric teaching hospital; Schollenberg E et al.; Antibiotic use at a pediatric teaching hospital was reviewed for a month . A total of 188 courses of therapy were evaluated with respect to choice of antibiotic, dosage and necessity of treatment . Errors in therapy were noted in 30% of the medical orders and 63% of the surgical orders . The most frequent error, unnecessary therapy, was found in 13% and 45% of the medical and surgical orders respectively . Error rates were highest for the most frequently ordered antibiotics, notably the penicillins . The magnitude of the problem appeared to be similar to that previously reported from general ana adult hospitals . The difficulties with solutions such as educational programs and compulsory consultation are discussed. Arch Otorhinolaryngol, 1980, 229(3-4), 255 - 9 Occurrence of non-ototoxic antibiotic (cephazolin) in the inner ear; Tachibana M et al.; Cephazolin, a non-ototoxic antibiotic, and kanamycin, an ototoxic antibiotic, were administered to the guinea pig systemically and their tissue concentration was measured . Not only kanamycin but also cephazolin did occur in the inner ear as well as in the kidney and other tissues . Therefore, it is most likely that the accumulation of an antibiotic inside the inner ear forms only a sine qua non for its ototoxicity . The mechanism of the ototoxicity should exist in the antibiotic-vulnerable cells (hair cells) themselves. Arch Otorhinolaryngol, 1980, 226(3), 129 - 33 Supra-normal sensitivity to ototoxic antibiotic of the developing rat cochlea; Carlier E et al.; A period of increased sensitivity to the ototoxic antibiotic amikacin was found in the cochlea of the developing rat . Starting either at birth, 10 or 30 days of age, rat were injected i.p . daily with 200 mg/kg of amikacine for 10 days . Only in the group injected with drug from 10 to 20 days of age was there evidence of a substantial (40-100 dB) permanent threshold shift (PTS) . To characterize the period of supra-normal sensitivity more precisely, independent groups of pups were injected with 50 mg/kg of amikacin from 10 to 20, 15 to 25, 20 to 30, and 30 to 40 days of age . Only those pups injeced from 10 to 20 or 15 to 25 days of age showed PTS (30-60 dB) . These data, taken together with those on rat cochlear maturation indicate that the sensitive period to ototoxicity starts at the age of onset of cochlear function (around day 10) and ends few days after the cochlea shows adult-like characteristics (3rd postnatal week). Zentralbl Gynakol, 1980, 102(12), 659 - 63 {Prophylactic antibiotics in Cesarean section (author's transl)}; Schulze G; Report of maternal infections by 498 abdominal deliveries in the years 1968--1975 . Three groups of patients were analyzed retrospectively: 1 . group: patients without antibiotics; 2 . gr