The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
Volume 30 , Issue 12
Showing 1-25 articles out of 25 articles from the selected issue
  • JUN'ICHI SHOJI, HIROSHI HINOO, YOSHIHARU WAKISAKA, KENZO KOIZUMI, MIKA ...
    1977 Volume 30 Issue 12 Pages 1029-1034
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Two new members of polymyxin group antibiotics, polymyxins S1 and T1, were isolated from the culture broths of strains identified as Bacillus polymyxa Rs-6 and Bacillus polymyxa E-12, respectively. These antibiotics are strongly basic substances, their hydrochloric acid salts are soluble in water and methanol. They are primarily active against Gram-negative bacteria in vitro and in vivo though polymyxin T1 exhibits higher activities against Gram-positive bacteria than other polymyxin group antibiotics.
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  • JUN'ICHI SHOJI, TOSHIYUKI KATO, IIIROSHI HINOO
    1977 Volume 30 Issue 12 Pages 1035-1041
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Amino acid analysis on the acid hydrolyzate of polymyxin S1 revealed its amino acid composition. Isolation of the constituent amino acids and measurement of their optical activities clarified their chiralities: Dab(5L), Thr(3L), Ser(1D) and Phe(1D). The constituent fatty acid was identified with anteisononanoic acid by gas chromatography and mass spectrometry. By the action of polymyxin acylase, deacyl polymyxin S was obtained. Successive EDMAN degradation reaction on deacyl polymyxin S revealed the amino acid sequence. Further evidence for the structure of polymyxin S1 was obtained by partial acid hydrolysis on tetra-(DNP)-polymyxin S1.
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  • JUN'ICHI SHOJI, TOSHIYUKI KATO, HIROSHI HINOO
    1977 Volume 30 Issue 12 Pages 1042-1048
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Amino acid analysis of the acid hydrolyzate of polymyxin T1, revealed the amino acid composition. Isolation of the constituent amino acids and measurement of their optical activities clarified their chiralities. These were 2, 4-diaminobutyric acid (6L), Thr(1L), Leu(2L) and Phe(1D). The constituent fatty acid was identified as anteisononanoic acid by gas chromatography and mass spectrometry. Deacylation with polymyxin acylase afforded deacyl polymyxin T. Successive EDMAN degradation on deacyl polymyxin T revealed most of its amino acid sequence. The chemical cleavage reaction for fragmentation of threonyl peptide on penta(DNP)-polymyxin T1 cleaved it at the C-terminal side of the Thr residue to afford a DNP-octapeptide, whose sequence was clarified by EDMAN degradation. Thus, the structure of polymyxin T1 was determined.
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  • MAMORU ARAI, AKIO TORIKATA, RYUZO ENOKITA, HISAYOSHI FUKATSU, RUMI NAK ...
    1977 Volume 30 Issue 12 Pages 1049-1054
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Pholipomycin is a new member of the phosphoglycolipid family of antibiotics. Taxonomic studies of the producing organism revealed that it has morphologically characteristic aerial mycelia in which two to three spores are borne usually on short and clavate side branches. The species name, Streptomyces lividoclavatus, has been proposed. Pholipomycin is produced mainly in the solid residue of the fermentation culture broth and is isolated by methanol extraction of the mycelial cake followed by purification on ion-exchange resin and silica gel chromatography.
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  • MAMORU ARAI, RUMI NAKAYAMA, KAYOKO YOSHIDA, MICHIKO TAKEUCHI, SUSUMU T ...
    1977 Volume 30 Issue 12 Pages 1055-1059
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Physico-chemical characterization of pholipomycin revealed that this antibiotic is a new member of phosphoglycolipid antibiotics. Pholipomycin was differentiated from other members by the products formed on acid hydrolysis as follows: the presence of glucosamine, a 257nm chromophore and moenocinol-type C25 lipids, but the absence of glucose, 6-deoxyglucosamine and glycine.
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  • AKIO TORIKATA, HIROJI YOSHIKAWA, TOSHIAKI KATAYAMA, MAMORU ARAI, MASAK ...
    1977 Volume 30 Issue 12 Pages 1060-1063
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Pholipomycin, a new member of the phosphoglycolipid antibiotics, was primarily active against gram-positive bacteria including clinically isolated resistant bacteria. It differed from other members of the antibiotic family as it also demonstrated activity against gram-negative bacteria. Pholipomycin protected mice from infection with Staphylococcus aureus and was nontoxic to mice having an LD50 (i.v.) of 600mg/kg. Besides possessing antimicrobiol activity, pholipomycin, when administered orally, appeared to promote growth in chickens and pigs.
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  • MITSUYOSHI YAMAMOTO, RYO OKACHI, ISAO KAWAMOTO, TAKASHI NARA
    1977 Volume 30 Issue 12 Pages 1064-1072
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    A chemically defined medium was devised in order to study the requirements for fortimicin A production by Micromonospora olivoasterospora KY 11515. Soluble starch was the best carbon source; NH4Cl and NH4NO3 were suitable nitrogen sources both for the growth and fortimicin production. Amino acids such as L-arginine, L-asparagine, L-aspartic acid and L-glutamic acid showed some stimulatory effects on both growth and antibiotic production of M. olivoasterospora while L-serine stimulated only antibiotic production and L-citrulline only the growth. K2HPO4, MgSO4•7H2O and CaCO3 were essential especially for the antibiotic production. The most important finding was that vitamin B12, cobalt and nickel showed marked stimulatory effects on fortimicin A production.
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  • TADASHI TESHIMA, SHINYA NOMOTO, TATEAKI WAKAMIYA, TETSUO SHIBA
    1977 Volume 30 Issue 12 Pages 1073-1079
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Tuberactinomycin O, one of the four congeners of the antituberculous peptide tuberactinomycin, was totally synthesized. The β-ureidodehydroalanine moiety was constructed from β, β-diethoxyalanine with excess urea in acidic medium after a cyclization reaction of a pentapeptide was finished. Cyclization was carried out by means of the 1-succinimidyl ester method. To the cyclic pentapeptide, β-lysine was introduced as the branched moiety and then deprotected to afford tuberactinomycin O which was completely identified with the natural form of the antibiotic.
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  • VINCENT GROUPE, RICHARD DONOVICK
    1977 Volume 30 Issue 12 Pages 1080-1086
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Whole shaken cultures of 20 random, unidentified actinomycetes were extracted with n-butanol at pH 4.5, 7.0, and 8.5, respectively. Residues of butanol-extractable materials (BXM) were reconstituted (100×) in buffers and freeze-dried. BXM were surprisingly well tolerated in animals and were screened against influenza A viral pneumonia in mice. One culture yielded BXM-80 which suppressed both chemical (LPS) and viral (NDV) pneumonia in mice as well as inhibited rat foot pad edema induced by carrageenin. Aspirin, Butazolidin, hydrocortisone, indomethacin, and prednisolone, which are known to inhibit carrageenin-induced rat foot pad edema were tested against chemical (LPS) and viral (NDV) pneumonia in mice. Only hydrocortisone and prednisolone suppressed LPS pneumonia. All of these 5 compounds failed to inhibit NDV pneumonia. Microbial products are suggested as a source for new and unique anti-inflammatory agents.
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  • KENNETH S. ROSENTHAL, DANIEL R. STORM
    1977 Volume 30 Issue 12 Pages 1087-1092
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    One of the apparent roles of the outer membrane system in gram-negative bacteria is to function as a selective permeability barrier. A number of antibiotics active against gram-positive bacteria are relatively ineffective against gram-negative bacteria presumably because of the implied barrier function of the outer membrane. This interpretation has been strengthened by studies demonstrating synergism between outer membrane perturbing agents such as EDTA or polymyxin B and specific antibiotics. In the case of polymyxin B, it is not totally clear that synergism with other antimicrobials is due to disruption of the outer membrane permeability barrier or to interactions with the inner membrane. In order to resolve this question, polymyxin B was covalently attached to agarose in order to limit interactions with the outer surface of E. coli. These studies demonstrate that immobilized polymyxin B acts synergistically with bacitracin, rifampicin, or lysozyme. It is proposed that synergistic effects exhibited by polymyxin B are due to its interaction with the outer membrane system.
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  • GOHTA MASUDA, SUSUMU TOMIOKA
    1977 Volume 30 Issue 12 Pages 1093-1097
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Biological β-lactam antibiotic-inactivating activities were detected in bacteriuria and suppurating pleural fluids. Clinical specimens were sterilized with membrane filters and the amounts of ampicillin and/or cephalothin which were being inactivated by 1 ml of each filtrate were determined. In general, filtrates which originally yielded Klebsiella sp. tended to show activity against ampicillin; whereas those yielding Enterobacter sp. and Pseudomonas aeruginosa showed activity against cephalothin.
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  • P. C. FUCHS, C. THORNSBERRY, A. L. BARRY, T. L. GAVAN, E. H. GERLACH, ...
    1977 Volume 30 Issue 12 Pages 1098-1106
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Ticarcillin, carbenicillin and BL-P1908, a new anti-pseudomonal semisynthetic penicillin, were subjected to several in vitrocomparisons-including minimal inhibitory and lethal concentrations (MIC and MLC), effects of inoculum size, effects of buffering the media and regression analyses of MIC and disc diffusion data. Whereas ticarcillin and carbenicillin showed comparable spectra of activity, with ticarcillin being more active against Pseudomonas aeruginosa and many Enterobacteriaceae, BL-P1908 exhibited a quite different spectrum, being much more active than either or the other two drugs against P. aeruginosa and Streptococcus faecalis, but virtually inactive against most of the Enterobacteriaceae. However, the MIC/MLC disparity against P. aeruginosa was much greater for BL-P1908 than for the other two drugs. The increase in MIC's resulting from increasing the inoculum sizes was comparable for the three drugs. The regression analyses showed good correlations between the disc diffusion and MIC data for all three drugs. Based on the regression analyses we conclude that for the 100-mcg carbenicillin disc the NCCLS recommended zone size breakpoints for P. aeruginosa should be utilized for all organisms, and that if a single disc should be selected as a representative for these two currently available antipseudomonal penicillins, the 75-mcg ticarcillin disc gave slightly better correlations with the MIC data of both drugs than the 100 mcg carbenicillin disc.
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  • R. N. JONES, C. THORNSBERRY, A. L. BARRY, P. C. FUCHS, T. L. GAVAN, E. ...
    1977 Volume 30 Issue 12 Pages 1107-1114
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Piperacillin (T-1220) is a new semisynthetic penicillin with an unusually broad spectrum of antimicrobial activity. In vitro comparisons of this drug with 6 other beta-lactam antimicrobics (ticarcillin, carbenicillin, ampicillin, cephalothin, cefamandole and cefoxitin) were conducted. These included minimal inhibitory concentrations (MIC) against 394 bacterial isolates, the minimal lethal concentrations (MLC) against 79 of those, as well as the effect of inoculum size on the MIC and MLC of the drugs. Piperacillin had significantly greater activity than did the other penicillins against Pseudomonas species and Klebsiella pneumoniae. Against P. aeruginosa piperacillin was 8- and 16-fold more active than ticarcillin and carbenicillin, respectively. The MLC of piperacillin rarely differed from the MIC by more than one log2 dilutions except against P. aeruginosa in which the MLC was 4-fold greater or more than the MIC of 45% of isolates tested. Ticarcillin, carbenicillin and cefoxitin showed minimal inoculum size effects. Cefamandole results showed the greatest inoculum size variation with 55% and 37% of isolates showing an 8-fold increase in MIC and MLC respectively by increasing inoculum from 105 to 107 CFU/ml. Piperacillin was intermediately effected having 25% of strains >8-fold increase in MIC.
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  • EUGENE S. WAGNER, BARRY LINDLEY, MADONNA TALBERT
    1977 Volume 30 Issue 12 Pages 1115-1118
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Benzylpenicillin, 5.2% 14C-enriched, was incubated with human whole blood. The erythrocyte component was washed and exhaustively dialyzed and found to contain 6.3% of the original radioactivity. None of the penicillin was found to bind to the cell membrane. Dialysis of the cell contents indicated that none of the penicillin binds irreversibly to the proteins within the cell. Infrared examination of the contents of the cell leads to the
    conclusion that benzylpenicillin (a monovalent anion) enters the erythrocyte and is hydrolyzed to benzylpenicilloic acid (a divalent anion). This structural change prevents the antibiotic from migrating out of the cell.
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  • G. LABER, E. SCHÜTZE
    1977 Volume 30 Issue 12 Pages 1119-1122
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Tiamulin concentrations have been determined in the serum of chickens, turkeys and swine after a single oral administration of various doses. The compound peaked between 2 and 4 hours after drug supply. In the highest dose used (50 mg/kg body weight), mean concentrations of 3.5, 2.9, 4.5μg/ml for chickens, turkeys and swine, respectively, could be obtained. In poultry, the levels declined between 12 and 24 hours to values not useful for calculation. In swine at 24 hours after administration measurable values could still be detected.
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  • KENSUKE TOBE, TAKESHI NISHINO, YOSHIMI HIRAI, SHOZO NAKAZAWA
    1977 Volume 30 Issue 12 Pages 1123-1126
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • YOSHIO ABE, SUSUMU NAKAGAWA, TAKAYUKI NAITO, HIROSHI KAWAGUCHI
    1977 Volume 30 Issue 12 Pages 1127-1129
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • MASARU UYEDA, SHINYA MORI, MASAKO MORITA, TERUMI OGATA, MARIKO MORI, M ...
    1977 Volume 30 Issue 12 Pages 1130-1131
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • R. J. MEHTA, M. K. FOX, D. J. NEWMAN, C. H. NASH
    1977 Volume 30 Issue 12 Pages 1132-1133
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • TETSUO SAWAI, KIYOTAKA MATSUBA, SABURO YAMAGISHI
    1977 Volume 30 Issue 12 Pages 1134-1136
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • SHINICHI KONDO, KENZABURO YOSHIDA, TAKAKO IKEDA, KATSUHARU IINUMA, YOS ...
    1977 Volume 30 Issue 12 Pages 1137-1139
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • J. A. CHAN, T. T. WEI, C. C. KALITA, D. J. WARNICK, A. L. GARRETSON, A ...
    1977 Volume 30 Issue 12 Pages 1140-1142
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • SHINICHI KONDO, MASASHI MIYAMOTO, HIROSHI NAGANAWA, TOMIO TAKEUCHI, HA ...
    1977 Volume 30 Issue 12 Pages 1143-1145
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • KUNIMOTO HOTTA, YOSHIRO OKAMI, HAMAO UMEZAWA
    1977 Volume 30 Issue 12 Pages 1146-1149
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • SHINICHI KONDO, TSUYOSHI MIYASAKA, KENZABURO YOSHIDA, KATSUHARU IINUMA ...
    1977 Volume 30 Issue 12 Pages 1150-1152
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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