The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
Volume 31 , Issue 12
Showing 1-18 articles out of 18 articles from the selected issue
  • PRODUCTION, IN VITRO BIOLOGICAL ACTIVITY, MICROBIOLOGICAL ASSAYS AND TAXONOMY OF THE PRODUCING MICROORGANISM
    L. J. HANKA, A. DIETZ, S. A. GERPHEIDE, S. L. KUENTZEL, D. G. MARTIN
    1978 Volume 31 Issue 12 Pages 1211-1217
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    A new antitumor antibiotic is produced in fermentation liquors of Streptomyces zelensis sp.n. The antibiotic is biologically active at extremely low concentrations. At 40 pg/ml, it inhibited 90% of the growth of L1210 cells in culture in tube dilution assays. The minimal inhibitory concentrations against Gram-positive bacteria is between 1-10 ng/ml, while these values for Gram-negative bacteria and fungi are mostly under 1 μg/ml. A microbiological assay with Bacillus subtilis can detect concentrations of 1-2 ng/ml.
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  • I. TAXONOMY, FERMENTATION AND PARTIAL PURIFICATION
    N. J. PALLERONI, K. E. REICHELT, D. MUELLER, R. EPPS, B. TABENKIN, D. ...
    1978 Volume 31 Issue 12 Pages 1218-1225
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    A taxonomic study of Streptomyces X-14077 (NRRL 8144), which produces a water-soluble purple-red pigment complex, revealed it to be a new species which has been named Streptomyces echinoruber sp. nov. The pigment complex was produced in deep culture fermentation and isolated by solvent extraction and concentration. The major pigment component, rubrolone, has low toxicity and may have potential as a food coloring agent. It appears to be devoid of antibiotic activity.
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  • II. CHEMISTRY AND STRUCTURE ELUCIDATION
    W. SCHÜEP, J. F. BLOUNT, T. H. WILLIAMS, A. STEMPEL
    1978 Volume 31 Issue 12 Pages 1226-1232
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Streptomyces echinoruber sp. nov. produces several red pigments. The major component, rubrolone, has been identified as 8(R), 9(R), 10(S), 10a(R)-tetrahydro-9, 10, 1Oa, 11-tetrahydroxy-3, 8-dimethyl-l-propyl-6aH(S)-pyrano[2'', 3'': 5', 4]furo[2', 3': 5, 6]azuleno[2, 3-c]pyridine-5, 13-di one (1) by single crystal X-ray analysis of a suitable derivative. A second pigment, B, is probably structurally closely related.
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  • TETSURO YAMASAKI, TSUTOMU TSUCHIYA, SUMIO UMEZAWA
    1978 Volume 31 Issue 12 Pages 1233-1237
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    A key protected streptidine derivative (3) useful for the synthesis of antibiotics of streptomycin series was prepared by hydrolysis of an acylated dihydrostreptomycin (DHSM) derivative (2), and it was condensed with a protected dihydrostreptobiosaminyl chloride (5) to give two condensation products (6 and 7). By deblocking, 6 was led to DHSM and 7 to a biologically inactive isomer (8) of DHSM. From the PMR spectrum of 4-O-mesyl derivative (4) of 3, the benzyloxycarbonyl and acetyl groups were concluded to be attached to the end nitrogens of the guanidine groups.
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  • NALINEE ASWAPOKEE, HAROLD C. NEU
    1978 Volume 31 Issue 12 Pages 1238-1244
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    CP-45, 899 [3, 3-dimethyl-7-oxo-4-thia-1-azabicyclo(3, 2, 0)heptane-2-carboxylic acid, 4, 4-dioxide, [2S-(2α, 5α)]] has low intrinsic activity against most Gram-positive cocci, Enterobacteriaceae and Pseudomonas . It inhibits Neisseria at concentrations of 0.1-6.2 μg/ml. The combination of CP-45, 899 and ampicillin inhibited Staphylococcus aureus and Enterobacteria-ceae resistant to ampicillin by virtue of β-lactamase activity. Combination of CP-45, 899 and cephalothin was synergistic less often, and CP-45, 899 did not act synergistically with carbenicillin or ticarcillin against Pseudomonas resistant to these agents. CP-45, 899 acted synergistically with ampicillin against Bacteroides. Synergy of CP-45, 899 and ampicillin was demonstrated at varying concentrations suggesting that it may significantly enlarge the antibacterial activity of ampicillin against resistant bacteria.
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  • I. 7-(β-KETOACYLAMINO)CEPHALOSPORINS
    MITSUO NUMATA, MASAYOSHI YAMAOKA, ISAO MINAMIDA, MASAAKI KURITANI, YOS ...
    1978 Volume 31 Issue 12 Pages 1245-1251
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The synthesis and antimicrobial profile of a series of 7-(β-ketoacylamino)cephalosporins (1) bearing an acetoxymethyl or a heterocyclicthiomethyl group at the 3-position are described. Of this series, 3-[[(1-methyl-1H-tetrazol-5-yl)thio]methyl]-7-(3-oxobutyrylamino)ceph-3-em-4-
    carboxylic acid (11) showed moderate antibacterial activities in in vitro and in vivo tests.
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  • II. FURTHER MODIFICATIONS OF 7-(3-OXOBUTYRYLAMINO)- CEPHALOSPORINS
    MITSUO NUMATA, ISAO MINAMIDA, MASAYOSHI YAMAOKA, MITSURU SHIRAISHI, TO ...
    1978 Volume 31 Issue 12 Pages 1252-1261
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    New cephalosporins modified in the acyl part of 7-(3'-oxobutyrylamino)cephalosporins (1), which have been described in the preceding paper, were synthesized by thiolation at the 2'-or the 4'-position, or by transforming the 3'-oxo group into a 3'-imino group. The most active compound in vitro was 3-[[(1-methyl-1 H-tetrazol-5-yl)thio]methyl]-7-(4-methylthio-3-oxobutyrylamino)ceph-3-em-4-carboxylic acid (7c), which showed superior in vitro activity against Gram-positive and Gram-negative bacteria compared to the parent cephalosporin (1b) with the same 3-substituent. The ED50 value for 7c, however, was essentially equal to that of 1b in mice infected with Escherichia coli O-111.
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  • CHEMISTRY AND STRUCTURE-ACTIVITY RELATIONSHIPS
    MITSUO NUMATA, ISAO MINAMIDA, MASAYOSHI YAMAOKA, MITSURU SHIRAISHI, TO ...
    1978 Volume 31 Issue 12 Pages 1262-1271
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The synthesis and the in vitro and in vivo antimicrobial activities of a series of 7-[2-(2-aminothiazol-4-yl)acetamido]cephalosporins (1) having varied 3-substituents, such as methyl, hydroxymethyl, acetoxymethyl, pyridiniomethyl and heterocyclicthiomethyls, are described. The derivatives having five membered heterocyclicthiomethyls exhibited strong inhibitory
    activities against Gram-negative organisms including some strains of Escherichia coli and Proteus morganii which are insensitive to cefazolin and cephaloridine. Pronounced activities were noted with 7-[2-(2-aminothiazol-4-yl)-acetamido]-3-[[[1-(2-dimethylaminoethyl)-1H-tetrazol-5-yl]thio]methyl]ceph-3-em-4-carboxylic acid (1y; SCE-963).
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  • KANJI TSUCHIYA, MASAHIRO KONDO, YASUO KITA, YUMIKO NOJI, MARIKO TAKEUC ...
    1978 Volume 31 Issue 12 Pages 1272-1282
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    A single dose of 20 mg/kg of SCE-963 [7β-[2-(aminothiazol-4-yl)acetamido]-3-[[[1-(2-dimethylaminoethyl)-1H-tetrazol-5-yl]thio]methyl]ceph-3-em-4-carboxylic acid] was administered subcutaneously to mice, intramuscularly to rats, rabbits and dogs. Plasma and tissue levels of SCE-963 reached a peak in 15-30 minutes after administration. In mice, rats and dogs, SCE-963 was distributed at high concentration in the descending order in the kidney, liver, plasma, lung and spleen, and in rabbits, in the kidney, plasma, lung, liver and spleen. The SCE-963 levels in the liver of mice, rats and dogs were higher than those of cefazolin, cephaloridine and cephalothin. The plasma and tissue levels of SCE-963 in mice and rats diminished rapidly, but those in rabbits and dogs declined gradually. SCE-963 was mainly excreted in the urine. The rate of excretion of SCE-963 in the bile was two to three times higher than that of cefazolin.
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  • COMPARISON OF A STRAIN CARRYING AN R-FACTOR AND THE PARENT STRAIN
    SUSUMU HORIKAWA, HIROSHI OGAWARA
    1978 Volume 31 Issue 12 Pages 1283-1291
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Membrane-bound penicillin-binding proteins of an Escherichia coil carrying an R factor which mediated the resistance to penicillins were examined by slab gel electrophoresis and fluorography using β-lactamase inhibitors such as methicillin, clavulanic acid and MC-696-SY2-A, and by affinity chromatography. By fluorography, it appeared that the penicillin-binding proteins of the strain carrying the R factor could not be distinguished from those of the parent strain. In both strains, methicillin had a preferential affinity for penicillin-binding proteins 2 and 3, clavulanic acid for 2 and 4, and MC-696-SY2-A for 1A at the concentration which was needed to inhibit about 75-80% of β-lactamase activity of the membrane fraction from a strain carrying
    an R factor. This with other facts indicates that MC-696-SY2-A has a unique character in the binding to penicillin-binding proteins. By affinity chromatography using cephalexin-CH-Sepharose 4B column, two major cephalexin-binding proteins were detected. Their molecular weights were found to be 110, 000 and 32, 000, respectively. These two proteins corresponded to penicillin-binding proteins 1 and 5/6. From these results it was suggested that the R factor had no influence on the penicillin-binding proteins in the E. coli strain examined.
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  • CORRELATION BETWEEN THE AFFINITIES OF CEFOXITIN TO PENICILLINBINDING PROTEINS AND ITS RATES OF INHIBITION OF THE RESPECTIVE PENICILLIN-SENSITIVE REACTIONS IN E. COLI
    MICHIO MATSUHASHI, SHIGEO TAMAKI
    1978 Volume 31 Issue 12 Pages 1292-1295
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The affinities of cefoxitin, a cephamycin antibiotic, to penicillin-binding proteins of Escherichia coil were reexamined using a recently developed method for separating penicillin-binding proteins. The inhibitions by this antibiotic of four measurable penicillin-sensitive enzymatic reactions, the reactions of D-alanine carboxypeptidases IA and IB, cross-bridge formation and concomitant release of D-alanine, were also measured. An approximate correlation was found between the affinities of cefoxitin to the penicillin-binding proteins responsible for these reactions and its rates of inhibition of the respective penicillin-sensitive reactions.
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  • EVALUATION OF THE STABILITY OF ANTIMICROBIALS IN WILKENS-CHALGREN BROTH AND THE EFFECT OF MEDIA PREREDUCTION
    PATRICK R. MURRAY, JUDY L. CHRISTMAN
    1978 Volume 31 Issue 12 Pages 1296-1298
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The stability of eight antimicrobial agents in WILKENS-CHALGREN broth was evaluated. The activities of only carbenicillin and benzyl penicillin were significantly decreased after storage for eight weeks at -20°C. Anaerobic reduction of the susceptibility testing broth prior to inoculation was found to be unnecessary.
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  • TAKAKO KATO, SATONORI KURASHIGE, Y. A. CHABBERT, SUSUMU MITSUHASHI
    1978 Volume 31 Issue 12 Pages 1299-1303
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Microorganisms were plated on agar plates containing various concentrations of an antimicrobial drug and inhibition of growth was determined at each drug concentration. The ID50 value and the gradient of the line were calculated by the least square method. When 200-800 bacterial cells were inoculated on an agar plate, growth inhibition corresponded linearly with the log concentration of a drug within the range of 5-95% inhibition. The ID50 value and the gradient obtained were reproducible and reliable using microorganisms at stationary phase of growth with all tested bacterial species and all tested antimicrobial agents. It was found that the ID50 values of drugs were more reproducible and may be more reliable than the MIC (minimum inhibitory concentration) values of the drugs.
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  • JOSEPH V. URI, PAUL ACTOR, JERRY A. WEISBACH
    1978 Volume 31 Issue 12 Pages 1304-1305
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • TETSU AKIYAMA, KENJI TANAKA, NOBUO TANAKA, YOSHIAKI NONOMURA
    1978 Volume 31 Issue 12 Pages 1306-1309
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • YUKIO SUGIURA, TAKANOBU KIKUCHI
    1978 Volume 31 Issue 12 Pages 1310-1312
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • KOICHI OGATA, MOTOHIRO MATSUURA, HIROSHI IRIE, TAMIO UENO, YOSHIKI TAN ...
    1978 Volume 31 Issue 12 Pages 1313-1315
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • INTERACTION OF BLEOMYCIN WITH NUCLEIC ACIDS, PREFERENTIAL BINDING TO GUANINE BASE AND ELECTROSTATIC EFFECT OF THE TERMINAL AMINE
    HIROSHI KASAI, HIROSHI NAGANAWA, TOMOHISA TAKITA, HAMAO UMEZAWA
    1978 Volume 31 Issue 12 Pages 1316-1320
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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