The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
Volume 29, Issue 2
Displaying 1-17 of 17 articles from this issue
  • II. ISOLATION AND CHARACTERIZATION
    HIROSHI FUKASE, TORU HASEGAWA, KAZUNORI HATANO, HIDESUKE IWASAKI, MASA ...
    1976 Volume 29 Issue 2 Pages 113-120
    Published: 1976
    Released on J-STAGE: April 12, 2006
    JOURNAL FREE ACCESS
    Two new species of Streptomyces, S. heteromorphus and S. panayensis, were found to produce a new antibiotic named C-2801X together with cephamycins A and B. The antibiotics were separated from each other by column chromatography on Amberlite XAD-2 and isolated in pure form as mono-sodium salts. C-2801X mono-sodium salt has a molecular formula C25H28N3O12SNa, and exhibits antibacterial activity against Gram-positive and Gram-negative bacteria including those insensitive to cephamycins A and B. From its physicochemical and biological properties, C-2801X was considered to be a new cephamycin-type antibiotic.
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  • DONALD R. BRANNON, JAMES A. MABE, DAVID S. FUKUDA
    1976 Volume 29 Issue 2 Pages 121-124
    Published: 1976
    Released on J-STAGE: April 12, 2006
    JOURNAL FREE ACCESS
    Bacteria and actinomycetes were screened for esterase enzymes capable of removing the para-nitrobenzyl ester from cephalosporins. An esterase preparation from Bacillus subtilis was used to prepare cephalexin and 7-ADCA from the corresponding para-nitrobenzyl esters.
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  • F. KNAUSEDER, E. BRANDL
    1976 Volume 29 Issue 2 Pages 125-131
    Published: 1976
    Released on J-STAGE: April 12, 2006
    JOURNAL FREE ACCESS
    Derivatives of pleuromutilin, formed during the fermentation of pleuromutilin. were isolated and their structure determined. 14-Acetyl-mutilin and mutilin as well as different unsaturated fatty acid esters of pleuromutilin were identified. The proportion of each derivative formed depends to a considerable degree on the conditions of the fermentation process. The possible biosynthetic pathways are shown.
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  • K. RIEDL
    1976 Volume 29 Issue 2 Pages 132-139
    Published: 1976
    Released on J-STAGE: April 12, 2006
    JOURNAL FREE ACCESS
    A number of derivatives of pleuromutilin (I) and of its degradation product, mutilin (II), was prepared. The new monotosylation product of pleuromutilin (IIIc) served as the key substance for modification of the glycolic acid side chain. From the pleuromutilin monosuccinate (IIIk) water-soluble salts were obtained, among them the crystallized diethylaminoethanol salt that was investigated more closely. Some of the pleuromutilin derivatives showed antimicrobial activity.
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  • R.T. TESTA, B.C. TILLEY
    1976 Volume 29 Issue 2 Pages 140-146
    Published: 1976
    Released on J-STAGE: April 12, 2006
    JOURNAL FREE ACCESS
    Utilizing a paromamine-producing mutant of Micromonospora purpurea blocked in the production of gentamicin, bioconversion of various minor gentamicin components into the gentamicin C complex was demonstrated. The compounds tested Were structurally related to the gentamicin C's and are found as minor components in the gentamicin fermentation. Based upon the bioconversions detected, a branched pathway for the biosynthesis of the gentamicin C components is proposed.
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  • I. 19-O-SUBSTITUTED DAMAVARICIN C
    KAZUYA SASAKI, TAKANOBU NAITO, TOSHIYUKI SATOMI, KAZUKIYO ONODERA
    1976 Volume 29 Issue 2 Pages 147-154
    Published: 1976
    Released on J-STAGE: April 12, 2006
    JOURNAL FREE ACCESS
    A number of derivatives of pleuromutilin (I) and of its degradation product, mutilin (II), was prepared. The new monotosylation product of pleuromutilin (IIIc) served as the key substance for modification of the glycolic acid side chain. From the pleuromutilin monosuccinate (IIIk) water-soluble salts were obtained, among them the crystallized diethylaminoethanol salt that was investigated more closely. Some of the pleuromutilin derivatives showed antimicrobial activity.
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  • NOBUO TANAKA, MANABU ISEKI, TOSHIO MIYOSHI, HATSUO AOKI, HIROSHI IMANA ...
    1976 Volume 29 Issue 2 Pages 155-168
    Published: 1976
    Released on J-STAGE: April 12, 2006
    JOURNAL FREE ACCESS
    Microscopic examination of cultures of Escherichia coli exposed to bicyclomycin revealed elongated or spheroplast-like cells. At the lethal level, bicyclomycin was shown to inhibit the synthesis of RNA and protein in the growing cells of E. coli 15 THU, whereas DNA and lipid synthesis were not significantly affected. However, the antibiotic did not block RNA and protein synthesis in vitro.
    Bicyclomycin was observed to inhibit the synthesis of envelope proteins more markedly than that of cytoplasmic proteins. The synthesis of two major envelope proteins was more sensitive to bicyclomycin than that of the other envelope proteins. One (peak I), which was inhibited to the greatest extent, seemed to be identical with a bound form of lipoprotein, and the other (peak V) with a free form of lipoprotein. Bicyclomycin exhibited inhibitory effects on the exclusive biosynthesis of the lipoprotein in histidine-starved cells of E. coli 15 THU. The biosynthesis of the bound form of lipoprotein was more profoundly inhibited by bicyclomycin than that of the free form.
    These results indicate that the primary action of bicyclomycin may be due to the interference with the biosynthesis of lipoprotein, and its assembly to peptidoglycan.
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  • MEGUMI KONO, KOJI O'HARA
    1976 Volume 29 Issue 2 Pages 169-175
    Published: 1976
    Released on J-STAGE: April 12, 2006
    JOURNAL FREE ACCESS
    Three clinical isolates, K-Ps 94, K-Ps 97 and K-Ps 102, of Pseudomonas aeruginosa having R factor and showing MIC of more than 51, 200 mcg/ml to streptomycin (SM), were examined for mechanisms of SM-resistance. Among the strains, K-Ps 94 and K-Ps 102 had R factor conferring SM-resistance. In K-Ps 94, the mechanism of SM-resistance was mainly owing to SM-phosphorylating enzyme and also owing to decreased permeability by an R factor, kR94. In K-Ps 97, it was considered to be due to SM-adenylylating enzyme by the chromosomal gene but not R factor, kR97. In K-Ps 102, the reduced permeability of the cell membrane to SM by an R factor, kR102, and the reduced affinity of the ribosome to the drug by the chromosomal gene contributed to the mechanisms of SM-resistance.
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  • MEGUMI KONO, KOJI O'HARA
    1976 Volume 29 Issue 2 Pages 176-180
    Published: 1976
    Released on J-STAGE: April 12, 2006
    JOURNAL FREE ACCESS
    The chloramphenicol (CP)-resistance mechanism of five-drug-resistant R factor (kR102) of Pseudomonas aeruginosa K-Ps 102 derived from a clinical specimen was investigated. Neither inactivation by acetyltransferase of CP nor induced resistance by CP was recognized. Reduced affinity of the ribosome to the drug was not seen in the result of incorporation experiment of 14C-valine by phage f2 RNA and ribosome of K-Ps 102. However, on spheroplasts by glycine treatment, remarkable increase of CP susceptibility was observed. From the above evidence, it was considered that the
    CP-resistance barrier controlled by kR102 factor would be in the cell wall and the surface layer of cytoplasma and that the mechanism of CP-resistance was possibly by decreased membrane permeability of CP. However, the susceptibility to CP of the susceptible strain still increased by the formation of spheroplasts. Consequently, it was considered that R factor might be controlling the function of membrane permeability of the cells.
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  • DOROTHY STEWART, GERALD P. BODEY
    1976 Volume 29 Issue 2 Pages 181-186
    Published: 1976
    Released on J-STAGE: April 12, 2006
    JOURNAL FREE ACCESS
    The in vitro activity of cephalexin, cephaloridine, cephalothin, cephapirin, cefoxitin, cephamycin C, cephradine, cephacetrile and cefazolin was determined against 443 isolates of bacteria. At a concentration of 12.5 μg/ml, all of the cephalosporins inhibited more than 60% of the isolates of Klebsiella pneumoniae. At the same concentration, cephalexin, cephaloridine, cephalothin, cephapirin, cephamycin C and cefazolin inhibited more than 90% of isolates of Proteus mirabilis. All of the cephalosporins except cephalothin and cephapirin inhibited over 60% of isolates of
    Escherichia coli at a concentration of 12.5 μg/ml. Cefoxitin was the most active cephalosporin against gram-negative bacilli. There were substantial differences in the activity of cephalosporins against gram-positive cocci. Cephaloridine was the most active cephalosporin against these organisms. There was considerable fluctuation in the proportion of isolates of gram-negative bacilli susceptible to these cephalosporins from year to year, but there was no evidence to suggest that the number of resistant isolates was increasing.
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  • KOJI FURUNO, KUNIO ANDO, SHIGEO SUZUKI, KOZO HIRATA
    1976 Volume 29 Issue 2 Pages 187-194
    Published: 1976
    Released on J-STAGE: April 12, 2006
    JOURNAL FREE ACCESS
    Dehydrated rats regularly develop acute renal failure following single injection of aminoglycoside antibiotics combined with dextran or of antibiotics only. Oral administration of 2, 5-di-O-acetyl-D-glucaro-1, 4-6, 3-dilactone protected rats against renal failure induced by kanamycin-dextran. The protective effect was prevalent among D-glucarates, and also to other saccharic acid, hexauronic acids and hexaaldonic acids, although to a lesser degree, but not to a hexaaldose, sugar alcohols, substances in the TCA cycle and other acidic compounds. D-Glucarates were effective against renal damage induced by peptide antibiotics as well as various aminoglycoside antibiotics. Dose-responses were observed in the protective effect of D-glucarates. With a D-glucarate
    of a fixed size of dose, approximately the same degree of protection was obtained against renal damages induced by different basic antibiotics despite large disparities in administration doses of different antibiotics. D-Glucarates had the ability to prevent renal damage but not to cure it. Rats excreted acidic urine when they were spared from renal lesions by monosaccharides. The reduction effect of D-glucarates against nephrotoxicity of basic antibiotics was discussed.
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  • LLOYD E. MCDANIEL
    1976 Volume 29 Issue 2 Pages 195-196
    Published: 1976
    Released on J-STAGE: April 12, 2006
    JOURNAL FREE ACCESS
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  • LEONARD FALKOWSKI, JERZY GOLIK, JAN ZIELINSKI, EDWARD BOROWSKI
    1976 Volume 29 Issue 2 Pages 197-198
    Published: 1976
    Released on J-STAGE: April 12, 2006
    JOURNAL FREE ACCESS
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  • THE INTRAMOLECULAR ALDOL CONDENSATION OF 19-O-ACETONYLDAMAVARICIN C AND ITS ANALOGS
    KAZUYA SASAKI, TAKANOBU NAITO, TOSHIYUKI SATOMI, YOSHIO MOMOKI
    1976 Volume 29 Issue 2 Pages 199-200
    Published: 1976
    Released on J-STAGE: April 12, 2006
    JOURNAL FREE ACCESS
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  • KENNETH L. Jr. RINEHART, FREDERICK J. ANTOSZ, PRABHAKAR V. DESHMUKH, K ...
    1976 Volume 29 Issue 2 Pages 201-203
    Published: 1976
    Released on J-STAGE: April 12, 2006
    JOURNAL FREE ACCESS
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  • YUJI MATSUHASHI, TSUTOMU SAWA, TOMIO TAKEUCHI, HAMAO UMEZAWA
    1976 Volume 29 Issue 2 Pages 204-207
    Published: 1976
    Released on J-STAGE: April 12, 2006
    JOURNAL FREE ACCESS
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  • SHINICHI KONDO, KATSUHARU IINUMA, KENZABURO YOSHIDA, KAZUTERU YOKOSE, ...
    1976 Volume 29 Issue 2 Pages 208-211
    Published: 1976
    Released on J-STAGE: April 12, 2006
    JOURNAL FREE ACCESS
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