The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
Volume 32 , Issue 11
Showing 1-22 articles out of 22 articles from the selected issue
  • I. TAXONOMY, ISOLATION AND CHARACTERIZATION
    JIRO ITOH, SHINJI MIYADOH, SAEKO TAKAHASI, SHOICHI AMANO, NORIO EZAKI, ...
    1979 Volume 32 Issue 11 Pages 1089-1095
    Published: 1979
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The two new antibiotics, BN-227 and BN-227-F, were isolated from the fermentation broth of Pseudomonas sp. BN-227. BN-227 has a molecular formula C7H9NO3, and melts at 115°C. BN-227-F has a molecular formula C21H24N3O9Fe, and melts at 156°C. BN-227-F is a chelate compound consisting of three similar ligands (antibiotic BN-227) and ferric ion. The two antibiotics have antimicrobial activity against Gram-positive and Gram-negative bacteria.
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  • W. R. BARKER, C. CALLAGHAN, L. HILL, D. NOBLE, P. ACRED, P. B. HARPER, ...
    1979 Volume 32 Issue 11 Pages 1096-1103
    Published: 1979
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Antibiotic G1549, isolated from culture broth of Pseudomonas alcaligenes, is a new cyclic hydroxamic acid with a 1-hydroxy-2(1H)-pyridinone structure that complexes with metals. The structure of G1549 is suggested to be 1-hydroxy-5-methoxy-6-methyl-2(1H)-pyridinone. In vitro, G1549 and its copper and ferric complexes show moderate activity against Gram-positive bacteria, fungi and Trichomonas vaginalis. Topical application of G1549 and its copper and ferric complexes protect guinea pigs against cutaneous infection with Microsporum canis. The compounds, however, have some systemic toxicity in mice.
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  • ROLF G. WERNER, KARL-RICHARD APPEL, WALTER M. A. MERK
    1979 Volume 32 Issue 11 Pages 1104-1111
    Published: 1979
    Released: April 12, 2006
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    In a screening program for antibiotics which were antagonized by cysteine, a strain, which was characterized as Ustilago sp., was found to produce a new quinone antibiotic, gunacin. The molecular weight M+=348.084 determined by mass spectroscopy, corresponds to a molecular formula of C17H16O8. Further spectroscopic data prove that gunacin is a new antibiotic. The antibiotic possesses a good inhibitory effect against mycoplasmas and Gram-positive bacteria including multi-resistant strains. It also possesses a weak activity against Gram-negative bacteria with the exception of Proteus vulgaris, which is more strongly inhibited. The main activity against fungi is found against Trichophyton mentagrophytes. Gunacin shows an inhibition of the DNA synthesis in vivo, is antagonized by mercapto compounds and possesses an acute toxicity of LD50=16 mg/kg i.p. and LD50=12 mg/kg i.v. in mice. Against HeLa-cell the antibiotic shows an ED50=12.11 μg/ml. Thirty five μg/ml of gunacin induces 1, 063 interferon units.
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  • OUDEMANSIN, AN ANTIFUNGAL ANTIBIOTIC FROM OUDEMANSIELLA MUCIDA (SCHRADER ex FR.) HOEHNEL (AGARICALES)
    TIMM ANKE, HANS JÜRGEN HECHT, GEORGS CHRAMM, WOLFGANG STEGLICH
    1979 Volume 32 Issue 11 Pages 1112-1117
    Published: 1979
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    From mycelial cultures of Oudemansiella mucida a crystalline optically active antibiotic, oudemansin (2), has been isolated; its structure is closely related to strobilurin A (1). The relative configuration of oudemansin have been determined by X-ray analysis. The antibiotic exhibits strong antifungal properties and inhibits respiration in fungi, cells of the ascitic form of EHRLICH carcinoma, and rat liver mitochondria.
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  • MIEKO TAKEUCHI, HIRONOBU IINUMA, TOMIO TAKEUCHI, HAMAO UMEZAWA, KAYOKO ...
    1979 Volume 32 Issue 11 Pages 1118-1124
    Published: 1979
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    2-Amino-5-methyl-5-hexenoic acid (AMHA), a new methionine analog, was isolated from a fermentation broth of Streptomyces sp. MF374-C4 based on its reversal of the effect of N-methyl-N'-nitro-N-nitrosoguanidine (MNNG) in a test system that determines the size of growth zones of revertants (His+) of Salmonella typhimurium TA 1535. AMHA also inhibited growth of the tester strain in a synthetic medium. These AMHA activities were abolished by methionine. The incidence of spontaneous streptomycin-resistant mutations of Escherichia coli K12 was not decreased by AMHA at concentrations where cell growth was partially inhibited. AMHA inhibited protein synthesis but not DNA or RNA synthesis in S. typhimurium TA1535 and E. coli K-12. The analog inhibited formation of methionyl-tRNA but not of valyl-tRNA in a cell-free system of E. coli, and supported ATP-PPi exchange in the cell-free system. At concentrations where it inhibited cell growth, AMHA decreased the number of foci, induced by ROUS sarcoma virus, on cultured sheets of chick-embryo fibroblasts. The effects of AMHA on focus formation and on the cell growth were overcome by methionine.
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  • II. CHEMICAL DEGRADATIONS OF 14C-LABELLED CLAVULANIC ACID
    IRENE STIRLING, S. W. ELSON
    1979 Volume 32 Issue 11 Pages 1125-1129
    Published: 1979
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Two chemical degradations of clavulanic acid are described which are useful for locating label in 14C-clavulanate. In the first, the β-hydroxyethylidene side chain of pbromobenzyl clavulanate is removed by ozonolysis to give pbromobenzyl (2R, 5R)-3, 7-dioxo-4-oxa-1-azabicyclo [3.2.0] heptane-2-carboxylate. The second involves the reaction of pbromobenzyl clavulanate with dibenzylamine in methanol, to isolate the three β-lactam carbons as methyl trans3-(N, Ndibenzyl)amino acrylate. These techniques were used to degrade clavulanic acid derived from fermentations fed with 2-14C-acetate or universally 14C-labelled glycerol. The amount of label retained in the degradation products was in agreement with the distribution of 13C in clavulanic acid derived from 2-13C-acetate, or 1, 3-13C2-glycerol, as observed by 13C-NMR.
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  • IV. IN VITRO SYNERGISM BETWEEN NEOVIRIDOGRISEIN II AND THE ANTIBIOTICS OF THE MIKAMYCIN A GROUP
    YASUSHI OKUMURA, MICHIKO SAKAMOTO, TOMOKO TAKEI, TOMOYUKI ISHIKURA, YA ...
    1979 Volume 32 Issue 11 Pages 1130-1136
    Published: 1979
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Neoviridogrisein II is a homologue of viridogriscin in which the hydroxyproline residue is replaced by proline. Neoviridogrisein II proved to be more active than the parent antibiotic against Gram-positive bacteria and Mycoplasma species. When neoviridogrisein II or viridogrisein was combined with griseoviridin, a non-peptidyl macrocyclic lactone, synergism was observed: maximum synergistic effect was observed for a combination ratio that depended on the test bacterium used. Neoviridogrisein II also exerted synergism when combined with mikamycin A and A-2315A.
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  • TAKASHI YAMAGUCHI, YOSHINORI KYOTANI, ISAMU WATANABE, SEIICHI SATO, YO ...
    1979 Volume 32 Issue 11 Pages 1137-1146
    Published: 1979
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    2-Deoxy-4-N-glycyl-6-O-(α-nebrosaminyl)fortamine (21) and 3-de-O-methyl-2-deoxy-4-N-glycyl-6-O-(α-nebrosaminyl)fortamine (27) were prepared starting from lividamine. The syntheses include four key steps, that is, transformation of 2-deoxystreptamine moiety of lividamine to 4-N, 3-O-didemethyl-2-deoxyfortamine, selective 4-N-methylation of the new aminocyclitol moiety, selective attachment of a glycyl residue to the methylamino group at C-4 and selective amination at C-6'.
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  • JEFFREY W. WILLIAMS, DEXTER B. NORTHROP
    1979 Volume 32 Issue 11 Pages 1147-1154
    Published: 1979
    Released: April 12, 2006
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    Gentamicin acetyltransferase I will catalyze acyl transfer from chloroacetylcoenzyme A to form 3-N-chloroacetylgentamicin. This product can be linked to coenzyme A to form a multisubstrate analog by nucleophilic displacement of the chlorine by the sulfur of coenzyme A. The analog can be purified by selective binding to cationic and anionic ion exchange resins. Kinetic analysis of a time-dependent onset and reversal of inhibition of gentamicin acetyltransferase I by the purified multisubstrate analog yields an inhibition constant of 5-20×10-10M. The inhibitor does not potentiate antibiotic activity against resistant Escherichia coli. Nevertheless, the effectiveness of the tight-binding between the enzyme and the multisubstrate analog demonstrates that inhibitors of resistance can be designed and prepared by specific enzymatic synthesis.
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  • SYNTHESIS AND BIOLOGICAL PROPERTIES OF THE ACETOXYMETHYL ESTER OF CEFAMANDOLE
    WALTER E. WRIGHT, WILLIAM J. WHEELER, VERLE D. LINE, JUDITH ANN FROGGE ...
    1979 Volume 32 Issue 11 Pages 1155-1160
    Published: 1979
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The synthesis of the acetoxymethyl (AOM) ester of cefamandole (CM) is described. The sparingly soluble ester is shown to be well absorbed orally by mice, but only when administered in solution in a partially non-aqueous vehicle, 50% propylene glycol. Neither the ester in aqueous suspension nor the sodium salt of CM in solution is well absorbed orally. The rate of oral absorption of the ester from solution is very rapid as shown by the early peak time and
    shape of the plasma level curve. Oral bioavailability from solution is at least 60% and is apparently limited only by hydrolysis or precipitation of a variable portion of the ester dose in the intestinal lumen prior to absorption.
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  • JOSEPH V. URI, PAUL ACTOR, IHOR ZAJAC, DONALD H. PITKIN, LILLIAN PHILL ...
    1979 Volume 32 Issue 11 Pages 1161-1167
    Published: 1979
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Three cephalosporins with 7-(2-hydroxyiminophenylacetamido) side chains (SK&F 79433, 80000 and 80303), differing in their 3-substituents, exhibited similar broad-spectrum antibacterial activity in vitro against strains of Staphylococcus aureus, Streptococcus faecalis and various Gram-negative bacilli. All three were active in vivo (s.c., mouse) against S. aureus, Esclrerichia coli or Klebsiella pnemnoniae, but they differed significantly in serum pharmacokinetic profiles. SK&F 80303 produced high and extremely prolonged serum levels and protected mice when administered up to 24 hours prior to challenge with β-lactamase-producing S. aureus or K. pneumoniae NS. It was resistant to hydrolysis by β-lactamases from S. aureus, and variably so to β-lactamases from E. coli strains. SK&F 80303 was bacteriolytic to logarithmically growing S. aureus, E. coli, Proteus mirabilis, K. pneumoniae and Enterobacter cloacae (partially).SK&F 80303 illustrates further the effect of the 3-sulfoalkyltetrazole substituent on the pharmacokinetic properties of cephalosporins. Its combined biological properties make it a possible candidate for therapeutic and long-term prophylactic use.
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  • GOHTA MASUDA, TARO YAJIMA, KISHIO NAKAMURA, TOKUO YANAGISHITA, HARUKUN ...
    1979 Volume 32 Issue 11 Pages 1168-1173
    Published: 1979
    Released: April 12, 2006
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    Comparative bactericidal activities were determined utilizing a relatively large number of test strains, in both agar and broth media, with special reference to the time of exposure of the bacteria to certain β-lactam antibiotics. It was apparent that the activities increase with time. The concentrations producing a 99.9% kill with cephalothin for Escherichia coli, Klebsiella sp., and carbenicillin for Pseudomonas aeruginosa were higher in broth than in agar. In contrast, those of benzylpenicillin for α-streptococcus( non-enterococcal) were higher in agar than in broth. If the bactericidal concentrations with 3-hour or 6-hour exposuret o antibiotics were used as the criterion, these concentrations of carbenicillin for P. aeruginosa, and benzylpenicillin for α-streptococcus were, in particular, unusually high compared with the conventionally determined bacteriostatic concentrations( MICs).
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  • NICHOLAS DELIHAS, ELIZABETH BAGLEY, CAROL PROKOP, DANIEL WEXLER
    1979 Volume 32 Issue 11 Pages 1174-1180
    Published: 1979
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Incubation of streptomycin (SM)** with [32P]5'-ribonucleotides at pH 7.0 produces fractions that migrate towards the cathode in high voltage electrophoresis (HVE) separations at pH 3.5. SM appears to interact with pG, pA and pC but not with pU. The appearance of these [32P]-labeled fractions is dependent on incubation time and SM concentration. Incubation of nucleotides with dihydrostreptomycin (DSM) or SM reduced with sodium cyanoborohydride (NaBH3CN) at pH 5.0, does not produce detectable changes in [32P] nucleotide mobility on HVE; however, incubation with SM reduced with NaBH3CN at pH 7.0 does produce [32P]-labeled fractions migrating with a net positive charge. Elution of [32P]-labeled material migrating towards the cathode from SM-5'-nucleotide incubations and re-electrophoresis results in nucleotides migrating with pG, pA and pC markers. These data indicate a reversible interaction between the SM-streptose aldehyde and amino-group containing nucleotides. This type of interaction may form an additional binding site for SM to RNA, relative to DSM.
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  • KAZUO YAMAMOTO, FRANKLIN HUTCHINSON
    1979 Volume 32 Issue 11 Pages 1181-1185
    Published: 1979
    Released: April 12, 2006
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    The effect of bleomycin on the colony forming ability of Escherichia coli K12 strains in exponential growth at 37°C was not affected by introducing recAl3, lexAl, polAl and uvrA6 mutations. For cells starved for amino acids, wild type strains became ten-fold more resistant to bleomycin, but again introducing lexAl, polAl and uvrA6 strains did not change the effect on colony forming ability; however, starved recA13 cells were now four-fold more sensitive. Strains with recA13, lexA1 and polAl mutations were always more sensitive than wild type to gamma rays under the same conditions as used for the bleomycin treatment. It is suggested that bleomycin-induced lesions may be concentrated in that part of the bacterial genomes at the cell wall, near the replication forks.
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  • FRITZ REUSSER
    1979 Volume 32 Issue 11 Pages 1186-1192
    Published: 1979
    Released: April 12, 2006
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    The antibiotic rubradirin is structurally related to the ansamycin family of antibiotics. Most members of this group act as specific inhibitors of bacterial RNAP*. Rubradirin and its aglycone possess diverging modes of action. Rubradirin inhibits ribosomal functions related to the peptide chain initiation process. It does not inhibit RNAP. By contrast the aglycone of rubradirin retains moderate inhibitory activity towards ribosomal functions but acts essentially as an extremely potent inhibitor of RNAP.
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  • J. M. PATTERSON, M. R. OLINGER, J. F. HOLLAND, L. L. BIEBER
    1979 Volume 32 Issue 11 Pages 1193-1200
    Published: 1979
    Released: April 12, 2006
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    The effect of salts, small neutral molecules, detergents, and organic solvents on the interaction of filipin and pimaricin with cholesterol was investigated using fluorometric techniques. The salts and small molecules, at concentrations of 0.5 mM-100 mM, showed no effect on the interaction of filipin with cholesterol. The interaction of pimaricin with cholesterol was slightly decreased in the presence of 100 mM MgCl2 or CaCl2. The detergents sodium deoxycholate and lauryl sulfate altered the fluorescence properties of the polyenes and precluded the interaction of the polyenes with cholesterol. The organic solvents dimethylformamide, ethanol, acetone, and iso-propanol when present at 0.1-1% (v/v) did not affect the fluorescence properties of pimaricin or the pimaricin-cholesterol complex. However, these solvents changed the fluorescence properties of filipin as well as its capacity to interact with cholesterol. These data indicate that low concentrations of some organic solvents and detergents can affect the fluorescence properties of these polyenes in a manner not directly related to the interaction of the polyene with sterol. Light scattering experiments indicate that the different solvents used to solubilize cholesterol produce suspensions of varying size when injected into the aqueous solutions. The extent of the subsequent interaction with the polyene antibiotic correlates with the light scattering properties of these suspensions.
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  • KANKI KOMIYAMA, IWAO UMEZAWA, TAKEHISA AKIYAMA, TOJU HATA
    1979 Volume 32 Issue 11 Pages 1201-1206
    Published: 1979
    Released: April 12, 2006
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    Sporamycin showed a remarkable tumor regressive activity against sarcoma-180 with a single 5 mg/kg dose of intravenous administration. This antitumor effect on tumor and host animals was examined immunologically. As the results:
    (1) When sarcoma-180 tumor cells were used as an antigen macrophage migration inhibition reaction by spleen cells derived from the tumor-bearing mice treated with sporamycin was positive at day 7-14 after the medication and was negative thereafter.
    (2) The delayed hypersensitivity tested by the foot-pad reaction was positive in tumor-bearing mice treated with sporamycin, and no decrease of foot pad reaction was observed, whereas this reaction decreased remarkably in non-treated tumor-bearing mice.
    (3) Sarcoma-180 tumor cells were mixed with spleen cells derived from sporamycin-treated mice, and were inoculated into normal dd mice. The growth of tumor cells was inhibited markedly, but no inhibition of tumor growth was observed in case of spleen cells derived from non-treated tumor bearing mice.
    (4) Combined treatment of sporamycin with PS-K, an immunopotentiator, showed a remarkable synergistic effect.
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  • JOSEPH V. URI, PAUL ACTOR
    1979 Volume 32 Issue 11 Pages 1207-1209
    Published: 1979
    Released: April 12, 2006
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  • MOTOO SAITO, IKUTOSHI MATSUURA, HIROSHI OKAZAKI
    1979 Volume 32 Issue 11 Pages 1210-1212
    Published: 1979
    Released: April 12, 2006
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  • ASHIT K. GANGULY, AJAY K. BOSE, NICHOLAS F. CAPPUCCINO
    1979 Volume 32 Issue 11 Pages 1213-1216
    Published: 1979
    Released: April 12, 2006
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  • SADAO MIYAMURA, KAIO KOIZUMI, YOJI NAKAGAWA
    1979 Volume 32 Issue 11 Pages 1217-1218
    Published: 1979
    Released: April 12, 2006
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  • TADAZUMI KOMIYAMA, TOSHIKAZU OKI, TAIJI INUI
    1979 Volume 32 Issue 11 Pages 1219-1222
    Published: 1979
    Released: April 12, 2006
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