The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
Volume 29 , Issue 1
Showing 1-20 articles out of 20 articles from the selected issue
  • NAOKI TSUJI, MASAAKI KOBAYASHI, KAZUO NAGASHIMA, YOSHIHARU WAKISAKA, K ...
    1976 Volume 29 Issue 1 Pages 1-6
    Published: 1976
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    A new antibiotic, trichostatin, was isolated from the metabolites of strains of Streptomyces hygroscopicus. It is active against trichophytons and some fungi. The structure was determined to be a derivative of a primary hydroxamic acid by chemical and spectroscopic evidences.
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  • NAOKI TSUJI, MASAAKI KOBAYASHI, YOSHIHARU WAKISAKA, YOSHIMI KAWAMURA, ...
    1976 Volume 29 Issue 1 Pages 7-9
    Published: 1976
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    New antibiotics, griseusins A and B were isolated from a strain of Streptomyces griseus. Both antibiotics have a 5-hydroxy-1, 4-naphthoquinone chromophore and their molecular formulae were determined to be C22H20O10 and C22H22O10, respectively. The griseusins are active against gram-positive bacteria.
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  • NAOKI TSUJI, KAZUO NAGASHIMA, MASAAKI KOBAYASHI, YOSHIHARU WAKISAKA, Y ...
    1976 Volume 29 Issue 1 Pages 10-14
    Published: 1976
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Two new antibiotics, A-218 and K-41, were isolated from strains identified as Streptomyces hygroscopicus. The antibiotics are characterized as polycyclic polyether compounds and are active against gram-positive bacteria.
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  • SADAFUMI OMURA, MICHINORI SHIBATA, SADAO MACHIDA, JIRO SAWADA, NOBORU ...
    1976 Volume 29 Issue 1 Pages 15-20
    Published: 1976
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    A new polyether antibiotic, lonomycin, was isolated from the culture of Streptomyces ribosidificus strain TM-481. The antibiotic obtained as a sodium salt is a colorless prism having a molecular formula of C44H75O14Na (M.W. 850), m.p. 188-189°C, and has no absorption maxima in the ultraviolet region. The infrared and NMR spectra of the antibiotic suggest the presence of a carboxyl and four methoxyl groups. Lonomycin shows antimicrobial activity against gram-positive bacteria.
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  • CHAO-MIN LIU, RALPH Jr. EVANS, LUCY FERN, THERON HERMANN, EDWARD JENKI ...
    1976 Volume 29 Issue 1 Pages 21-28
    Published: 1976
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    A new polyether antibiotic, Ro 21-6150, has been isolated from culture broths of Streptomyces hygroscopicus, strain X-14563. Ro 21-6150 has ionophore properties and is active in vitro against gram-positive bacteria.
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  • CYNTHIA H. O'CALLAGHAN, R. B. SYKES, D. M. RYAN, R. D. FOORD, P. W. MU ...
    1976 Volume 29 Issue 1 Pages 29-37
    Published: 1976
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    βCefuroxime is a new broad spectrum cephalosporin antibiotic for administration by injection. It is stable to most β-lactamases. It is active against gram-positive organisms, including penicillinase-producing staphylococci, and has wide activity against gram-negative bacilli including Enterobacter and many strains of indole-positive Proteus spp. The substance is also highly active against Haemophilus influenzae and Neisseria gonorrhoeae. Studies on human volunteers showed that it produced high, long-lasting blood levels with virtually complete recovery of unchanged antibiotic in the urine. No evidence of toxicity due to cefuroxime was found. Slight, short-lived pain followed intramuscular injection, and the compound was well tolerated intravenously.
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  • JAMES P. SCANNELL, DAVID L. PRUESS, HELEN A. AX, ABRAHAM JACOBY, MARTH ...
    1976 Volume 29 Issue 1 Pages 38-43
    Published: 1976
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    A novel amino acid, L-2-amino-4-(2-aminoethoxy)-butanoic acid, was isolated from a fermentation broth of Streptomyces sp. X-11, 085. It was shown to be identical with the chemical reduction product of an antimetabolite antibiotic, L-2-amino-4-(2-aminoethoxy)-trans-3-butenoic acid, a co-product in the fermentation. Addition of the title compound to the fermentation led to an enhanced yield of the antimetabolitesuggesting that the saturated amino acid serves as a precursor for the antimetabolite.
    A de novo chemical synthesis and enzymatic resolution of the title compound are also reported.
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  • INA HAUPT, EDITH SCHUHMANN, RUDOLF GEUTHER, HEINZ THRUM
    1976 Volume 29 Issue 1 Pages 44-49
    Published: 1976
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The action of the polyene macrolide antibiotics mycotrienin, pimaricin, lucensomycin, tetramycin, rimocidin, nystatin, filipin, lagosin, pentaene antibiotic 2814P, flavomycoin, flavofungin, hexaene antibiotic 5001P, and candicidin, including perhydro derivatives of them, on wall-less stable protoplast type L-form and normal rod form cells of E. coli W 1655F+ was studied. No inhibition of the normal rod form cells was detected. In contrast to these results the growth of the L-form cells was inhibited by all of the substances tested, with the exception of pimaricin.
    Further experiments have shown that the differences in sensitivity of normal and L-form cells cannot be explained by differences in sterol content, the target site of polyene antibiotics in sensitive eukaryotic cells. According to our results it is obvious that the cell wall of the normal cells functions as a penetration barrier to polyene antibiotics.
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  • JYOTIRMOY NANDI, S. K. BOSE
    1976 Volume 29 Issue 1 Pages 50-57
    Published: 1976
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Versicolin is mainly active against Trichophyton rubrum. It is inactivated by serum. However, attainable blood level can be fifteen to twenty times higher than the fungicidal concentration for as long as 4 hours after a single intravenous administration of the maximum tolerable dose of 25 mg/kg body weight of mouse. It has no haemolytic activity like other polypeptide antibiotics. Skin does not show the presence of any measurable amount of the antibiotic. It is excreted through urine to the extent of 65 % of the maximum tolerable dose of the antibiotic administered intravenously. Versicolin is effective against experimental infection by T. rubrum in guinea pigs at dose as low as 2.5 mg/kg body weight. The antibiotic shows no sign of subacute toxicity at these curative doses.
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  • JØRGEN HILDEN, FOLKE RØNNIKE, HENNING SCHOU
    1976 Volume 29 Issue 1 Pages 58-64
    Published: 1976
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    In two growth tests, one employing EHRLICH ascites tumor cells in suspension culture, the other employing intact roots of wheat (Triticum sativum LAM.), the growth inhibiting action of bleomycin (BLM) was shown to be intensified by human serum. Practical consequences of the finding are suggested. No such serum-drug interaction has been demonstrated with other anti-tumor compounds, including methotrexate (MTX) and threosulphan (TRSF). Isolation of the active factor(s) in serum has not yet been attempted.
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  • G.L. DUNN, J.R.E. HOOVER, D.A. BERGES, J.J. TAGGART, L.D. DAVIS, E.M. ...
    1976 Volume 29 Issue 1 Pages 65-80
    Published: 1976
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The synthesis of a series of related broad-spectrum 7-phenylglycyl cephalosporins with 3-heterocyclicthiomethyl substituents is described. The effects of benzene-ring hydroxylation and 3-substituent variation on the in vitro antibacterial activity, height and duration of mouse serum levels, and effectiveness in protecting against bacterial infection in the mouse are examined. Included for comparison are cephalexin, cephaloglycin and their ortho-, meta- and para-hydroxy derivatives. The biological properties examined were influenced by the position of the hydroxyl group and by the nature of the 3-substituent. The 7-(p-hydroxyphenylglycyl)-3-heterocyclicthiomethyl analogs were found to produce significantly higher serum levels on oral administration to mice than their unhydroxylated counterparts. This effect was not observed with the 7-(m-hydroxyphenylglycyl)-3-heterocyclicthiomethyl cephalosporins, nor with the p-hydroxyphenylglycyl analog of cephalexin. While m- and p-hydroxylation had little effect on in vitro activity the oNS-hydroxyphenylglycyl cephalosporins tested had very low antibacterial activities and were not examined further. One derivative, 7-[R-2-amino-2-(4-hydroxyphenyl)acetamido]-3-(1H-1, 2, 3-triazole-4(5)-ylthiomethyl)-3-cephem-4-carboxylic acid (SK&F 60771) was found to have outstanding in vitro and in vivo activities along with oral and subcutaneous serum levels in the mouse that were significantly higher than those obtained with cephalexin. This derivative which has been given the generic name cefatrizine was selected for extensive additional biological evaluation.
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  • YOICHI NAKAI, YOSHIO KANAI, TAKESHI FUGONO, SHIGEHARU TANAYAMA
    1976 Volume 29 Issue 1 Pages 81-90
    Published: 1976
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    1. The metabolic fate of 14C-cephacetrile was studied in rats and rabbits. The plasma level of intravenously injected cephacetrile decreased with half-lives of 17 and 22 minutes in rats and rabbits respectively, this decline being associated with a rapid appearance of the active metabolite, desacetylcephacetrile. Intramuscularly injected cephacetrile was rapidly absorbed by rats with a maximum plasma level at 20 minutes and a half-life of 16 minutes. Cephacetrile and desacetylcephacetrile did not enter erythrocytes. Cephacetrile was weakly bound to the plasma protein in the rat, rabbit and man.
    2. Both in rats and rabbits, almost all of the injected radioactivity was excreted in the urine within 72 hours as the intact antibiotic and desacetylcephacetrile, only small amounts appearing in feces via bile. Neither the γ-lactone of desacetyl-7-cyanacetamidocephalosporanic acid nor the violet-reddish pigment (CGP-695) produced from cephacetrile were detectable in the plasma or urine of the animals.
    3. In rats given the labeled antibiotic intravenously, the radioactivity was widely distributed with concentrations being high in the kidney, plasma and liver, and lowest in the brain. The radioactivity crossed the rat placenta and appeared in the fetus. Radioactivity in these tissues disappeared as the plasma level declined.
    4. During daily intramuscular injection of 14C-cephacetrile to rats, no significant changes were observed in the peak level of the plasma radioactivity or in the half-lives. In addition, dosing of the labeled antibiotic for 7 days caused no increase in tissue levels of radioactivity.
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  • KEN'ICHI YAMAZAKI, KIMIHIKO ABE, MITSUJI SANO
    1976 Volume 29 Issue 1 Pages 91-92
    Published: 1976
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • TOMIO TAKEUCHI, MASASHI MIYAMOTO, MASAAKI ISHIZUKA, HIROSHI NAGANAWA, ...
    1976 Volume 29 Issue 1 Pages 93-96
    Published: 1976
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • HAMAO UMEZAWA, TAKAAKI AOYAGI, HIROYUKI SUDA, MASA HAMADA, TOMIO TAKEU ...
    1976 Volume 29 Issue 1 Pages 97-99
    Published: 1976
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • HIROYUKI SUDA, TOMOHISA TAKITA, TAKAAKI AOYAGI, HAMAO UMEZAWA
    1976 Volume 29 Issue 1 Pages 100-101
    Published: 1976
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • HIKARU NAKAMURA, HIROYUKI SUDA, TOMOHISA TAKITA, TAKAAKI AOYAGI, HAMAO ...
    1976 Volume 29 Issue 1 Pages 102-103
    Published: 1976
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • RYOSUKE YAHASHI, ISAO MATSUBARA
    1976 Volume 29 Issue 1 Pages 104-106
    Published: 1976
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • HIDEO OTSUKA, JUN'ICHI SHOJI, KEIICHI KAWANO, YOSHIMASA KYOGOKU
    1976 Volume 29 Issue 1 Pages 107-110
    Published: 1976
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • HIROSHI MAEDA, JIRO TAKESHITA
    1976 Volume 29 Issue 1 Pages 111-112
    Published: 1976
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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