The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
Volume 36 , Issue 1
Showing 1-17 articles out of 17 articles from the selected issue
  • SHUZO SATOI, MASASHI AWATA, NAOKI MUTO, MITSUO HAYASHI, HITOSHI SAGAI, ...
    1983 Volume 36 Issue 1 Pages 1-5
    Published: 1983
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    A new aminoglycoside antibiotic, G-367 S1 (2'-N-formylsisomicin, C20H37N5O8) produced by a rare actinomycetes, Dactylosporangium thailandense G-367 (FERM-P 4840) has been isolated by column chromatography on a cation-exchange resin. G-367 S1 is active against Gram-positive and Gram-negative bacteria.
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  • I. CULTIVATION, ISOLATION, AND SOME CHEMICAL AND BIOLOGICAL PROPERTIES
    H. IRSCHIK, K. GERTH, T. KEMMER, H. STEINMETZ, H. REICHENBACH
    1983 Volume 36 Issue 1 Pages 6-12
    Published: 1983
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Antibiotic activity was isolated from the culture supernatant of the myxobacterium Myxococcus fulvus strain Mx f65. It was active against Gram-positive bacteria (MIC 0.3-5 μg/ml), at higher concentrations also against Gram-negative ones (MIC 6-100 μg/ml), and not at all against yeasts and molds. The activity could be resolved into 4 closely related peptides, the myxovalargins. One of them, myxovalargin A, was by far the most plentiful. The compounds appear to be new antibiotics and seem to interfere with protein synthesis.
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  • L. A. DOLAK, F. REUSSER, L. BACZYNSKYJ, S. A. MIZSAK, B. R. HANNON, T. ...
    1983 Volume 36 Issue 1 Pages 13-19
    Published: 1983
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • A. CUER, G. DAUPHIN, J. C. BELOEIL
    1983 Volume 36 Issue 1 Pages 20-24
    Published: 1983
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The isolation and identification of a bioconversion product of grisorixin from a strain of Streptomyces rimosus is reported. The structure of this product was elucidated from physicochemical data, in particular 13C NMR spectra. Its ionophorous and antibiotic properties are markedly different from those of grisorixin.
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  • MASAYUKI SUNAGAWA, TOMIHISA OHTA, SHIGEO NOZOE
    1983 Volume 36 Issue 1 Pages 25-29
    Published: 1983
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The biosynthetic introduction of oxygen in position 7 of brefeldin A, a structurally unique macrolide with an alicyclic ring, was studied. [4-2H]Brefeldin C was prepared efficiently from brefeldin A. A high incorporation ratio of the labeled brefeldin C into brefeldin A by Eupenicillium brefeldianum clearly indicates that the oxygen in position 7 of brefeldin A does not contribute to the cyclopentane ring formation but is introduced during the last step of brefeldin A biosynthesis.
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  • HIROJI YOSHIKAWA, YO TAKIGUCHI, MICHIYA TERAO
    1983 Volume 36 Issue 1 Pages 30-35
    Published: 1983
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The biosynthetic relationship of the herbicidins produced by Streptomyces saganonensis was studied with blocked mutants by means of a bioconversion method using growing and resting cells. It is proposed that the biosynthetic sequence for herbicidins is; herbicidin G→herbicidin F→herbicidin A. Both herbicidins A and F were converted to herbicidin B by nonenzymatic reactions. Herbicidin G was also converted to herbicidin C non-enzymatically.
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  • EFFECT ON ANTIBACTERIAL ACTIVITY OF α-SUBSTITUENTS IN THE 2-(2-AMINO-4-THIAZOLYL) ACETYL SIDE CHAIN OF A CEPHALOSPORIN NUCLEUS
    HISASHI TAKASUGI, ZENZABURO TOZUKA, TAKAO TAKAYA
    1983 Volume 36 Issue 1 Pages 36-41
    Published: 1983
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Synthesis and in vitro antibacterial activity of semisynthetic cephalosporins (I) having an α-substituted 2-(2-amino-4-thiazolyl)acetyl side chain at the 7-position were described.
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  • S. M. HUSSAIN QADRI, M. R. KARIM, D. J. FLOURNOY
    1983 Volume 36 Issue 1 Pages 42-46
    Published: 1983
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The in vitro activity of U-57930E, a pipecolic acid amide of clindamycin, was compared with those of clindamycin, ampicillin, carbenicillin and tetracycline against 321 anaerobic clinical isolates. The MIC (μg/ml) of U-57930E that inhibited 95% Bacteroides fragilis, Peptococcus prevotii, B. melaninogenicus and P. asaccharolyticus was 0.0625; 0.03125 for Pepto-streptococcus anaerobius, B. vulgatus, Propionibacterium and Peptococcus species. Clindamycin, on the other hand, gave MIC values of 0.5μg/ml for B. fragilis, P. prevotii and P. asaccharolyticus, 0.25 for Propionibacterium sp. All strains of Clostridium perfringens were inhibited by 0.5μg/ml of U-57930E. Both clindamycin and U-57930E showed similar MIC values for all strains of Fusobacterium nucleatum and Propionibacterium acnes tested. The MIC values for ampicillin, carbenicillin and tetracycline were within the expected range. U-57930E had a 4-8 fold lower MIC than clindamycin and is significantly active against anaerobic bacteria.
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  • II. THE IN VITRO ANTIBACTERIAL PROPERTIES OF L-640, 876, A NEW TYPE OF β-LACTAM ANTIBIOTIC
    LAWRENCE R. KOUPAL, BARBARA WEISSBERGER, DANIEL L. SHUNGU, ELLEN WEINB ...
    1983 Volume 36 Issue 1 Pages 47-53
    Published: 1983
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    A new semisynthetic cephalosporin antibiotic designated 7-β-(1-benzylpyridinium-4-yl)-amino-3-{[(1-methyl-1H-tetrazol-5-yl)thio]methyl)ceph-3-em-4-carboxylate (L-640, 876) was compared for antibacterial activity in vitro with mecillinam, cefoxitin and cefotaxime. The antibacterial spectrum of L-640, 876 and the effect of culture medium composition and inoculum size on activity are most similar to those of mecillinam. In some cases the inoculum effect on MICs correlated with instability of the compound to certain β-lactamases and in others to the presence of ionized compounds such as sodium chloride in the medium. On balance, L-640, 876 was superior to mecillinam in potency and breadth of spectrum.
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  • III. THE MODE OF ACTION OF L-640, 876 AND THE EFFECT OF NaCl ON MEMBRANE PERMEABILITY AND BINDING
    LAWRENCE R. KOUPAL, BARBARA A. PELAK, PATRICK J. CASSIDY, HANS H. GADE ...
    1983 Volume 36 Issue 1 Pages 54-63
    Published: 1983
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    L-640, 876, 7-β(1-benzylpyridinium-4-yl)amino-3-{[(1-methyl-1H-tetrazol-5-yl)thio]methyl}-ceph-3-em-4-carboxylate, is a potent representative of a new family of β-lactam antibiotics which are similar in some respects to mecillinam. When L-640, 876 and mecillinam were compared for effects on growth and morphology of Escherichia coli, it was observed that both drugs caused the formation of lemon-shaped cells during the first 30 minutes of exposure and during this period the culture turbidity increased without an appreciable change in culture viability. Unlike mecillinam, after 60 minutes of exposure to L-640, 876 the majority of the lemon-shaped cells transformed into spindle-shaped cells and in the continuing presence of the drug formed osmotically fragile spheroplasts. Membrane binding studies indicated that, like mecillinam, L-640, 876 was bound to the PBP-2 of E. coli and Proteus morganii; however, some binding of L-640, 876 to the PBP-3 of E. coli was detected. In Staphylococcus aureus binding differences were more evident as L-640, 876 was more rapidly bound to PBP-1 and 2 whereas mecillinam was rapidly bound to PBP-3. The reversal of inhibition of certain strains of Gramnegative bacteria by high ionic strength media could not be directly attributed to a reversal of antibiotic binding to the PBPs. Permeability studies indicated that the superior potency of L-640, 876 in E. coli was partly due to its higher concentration in the periplasm which was unaffected by the simultaneous addition of drug and NaCl, however, in cells cultured in high ionic strength medium there was a marked reduction in penetration rate of all β-lactams tested.
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  • IV. COMPARISON OF THE IN VIVO ANTIBACTERIAL ACTIVITIES OF L-640, 876, MECILLINAM, CEFOXITIN AND CEFOTAXIME
    EVEMARIE CELOZZI, BARBARA ANN PELAK, EDWARD O. STAPLEY, HANS H. GADEBU ...
    1983 Volume 36 Issue 1 Pages 64-69
    Published: 1983
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The novel β-lactam, L-640, 876, exhibited excellent therapeutic activity when administered parenterally but not orally to mice infected with a variety of pathogenic bacteria. In this respect, the compound was as potent as cefotaxime against representative Gram-positive and Gram-negative organisms, in most cases, equal to or more potent than cefoxitin, and more effective than mecillinam. When administered subcutaneously to normal mice at dose levels ranging from 10 to 50 mg/kg, L-640, 876 provided an adequate dose response, recovery of ca. 45% of biological activity in the urine, and excellent distribution at the highest dose level into liver, lung, kidney, heart muscle, but not brain.
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  • V. L-640, 876 TREATMENT OF INDUCED ENTEROTOXIGENIC COLIBACILLOSIS (SCOURS) IN CALVES AND PIGLETS
    THOMAS M. JACKS, KLAUS D. SCHLEIM, BRINTON M. MILLER, DANIEL L. SHUNGU ...
    1983 Volume 36 Issue 1 Pages 70-75
    Published: 1983
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    A new semisynthetic cephalosporin antibiotic designated L-640, 876, 7-β-(1-benzylpyridinium-4-yl)amino-3-{[(1-methyl-1H-tetrazol-5-yl)thio]methyl}ceph-3-em-4-carboxylate, was highly active in vitro against 110 enteropathogenic strains of Escherichia coli and Salmonella species of animal origin. The MIC90 was 0.125μg/ml for the E. coli strains, 2 μg/ml for the S. choleraesuis strains and 4μg/ml for the S. typhimurium strains. In colostrum-fed calves infected with E. coli strain B44, L-640, 876 administered by gavage at 30 mg/calf (0.67 mg/kg) twice a day for 3 days, starting at 20-hour post-inoculation, eliminated the diarrhea and reduced the mortality from 82% in the infected, nonmedicated calves to 11% in the infected, medicated calves (P<0.05). In colostrum-fed piglets infected with E. coli strain P155, L-640, 876 administered by gavage at 12.5 or 20mg/piglet (10 or 16mg/kg) twice a day for 3 days, starting at 6-hour post-inoculation, eliminated the diarrhea and reduced the mortality from 79% in the infected, nonmedicated to 25% in the infected, medicated piglets (P<0.05). Thus, L-640, 876 was highly effective in restoring the calves and piglets to good health by eliminating diarrhea and reducing mortality.
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  • KENICHI SATO, YOSHIHARU MATSUURA, KIYOSHI MIYATA, MATSUHISA INOUE, SUS ...
    1983 Volume 36 Issue 1 Pages 76-85
    Published: 1983
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The susceptibility of 80 Bacteroides fragilis group strains isolated from clinical specimens to β-lactam antibiotics was investigated by agar dilution method. Twenty strains showed high resistance to the antibiotics. The resistance level of the isolates to cephaloridine was related to the amount of β-lactamase activity (cephalosporinase; CSase) produced. B. fragilis GN11477, B. thetaiotaomicron GN11478 and B. vulgatus GN11479 were selected from among the CSase producing strains, and the enzymes were purified about 300-fold by affinity chromatography employed ampicillin as ligand bound to activated CH Sepharose 4B. The enzyme preparations gave a single protein band on polyacrylamide gel electrophoresis. The molecular weights of the three enzymes were estimated to be approximately 32, 000 and their isoelectric points were 5.2, 4.9 and 4.5, respectively. The optimal pH and the optimal temperature of the enzymes were 7.2 and 37°C, respectively. The enzyme activities were inhibited by iodine, some divalent ions, p-chloromercuribenzoate, clavulanic acid, cephamycin derivatives and cloxacillin. The enzymes showed hydrolytic activity against cephaloridine, cephalothin, cefazolin, cefuroxime and also newly introduced cephalosporins such as cefotaxime, cefoperazone and cefinenoxime. Each mouse antisera obtained against the purified enzymes showed cross-reactions with its each enzyme and others in neutralization test.
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  • MASA HAMADA, TAKAKO IKEDA, MAYUMI MANABE, SHUICHI GOMI, SHINICHI KONDO ...
    1983 Volume 36 Issue 1 Pages 86
    Published: 1983
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • CHEMICAL CONVERSION OF NEOMYCIN B TO PAROMOMYCIN I, 6'''-DEAMINO-6'''-HYDROXYNEOMYCIN B AND 6'''-DEAMINO-6'''-HYDROXY-PAROMOMYCIN I
    SOICHIRO TODA, SUSUMU NAKAGAWA, TAKAYUKI NAITO, HIROSHI KAWAGUCHI
    1983 Volume 36 Issue 1 Pages 87-91
    Published: 1983
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • SEI-ICHI SAITO, YUJI UMEZAWA, TAKEO YOSHIOKA, TOMOHISA TAKITA, HAMAO U ...
    1983 Volume 36 Issue 1 Pages 92-95
    Published: 1983
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • 2. ISOLATION OF THE FIRST NATURAL PRODUCTS WITH A C-P-H BOND AND THEIR INVOLVEMENT IN THE C-P-C BOND FORMATION
    HARUO SETO, TORU SASAKI, SATOSHI IMAI, TAKASI TSURUOKA, HIROSHI OGAWA, ...
    1983 Volume 36 Issue 1 Pages 96-98
    Published: 1983
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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