The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
Volume 35 , Issue 4
Showing 1-27 articles out of 27 articles from the selected issue
  • HIROSHI KASE, SHIGETO KITAMURA, KIYOSHI NAKAYAMA
    1982 Volume 35 Issue 4 Pages 385-390
    Published: 1982
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    A 2-deoxystreptamine idiotrophic mutant of Micromonospora sagamiensis, KY 11509, was found to produce unknown antibacterial substances, which were named SU-2 complex. Each component, SU-1, SU-2 and SU-3 were isolated from a culture broth of KY 11509. Chromatographic data suggested that these components were new antibiotics. The antibiotics exhibited potent and broad spectrum of antibacterial activity. The amount of SU-1, SU-2 and SU-3 production reached their maximum level (197, 82 and 58 μg/liter, respectively) in 3 to 4 days. Addition of cobalt chloride markedly stimulated SU-1 production but suppressed SU-2 and SU-3 production. Isolation of a mutant possessing a higher productivity of SU-2 complex is also described.
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  • HIDEO OISHI, TAKAO NOTO, HIROSHI SASAKI, KOJI SUZUKI, TOSHIAKI HAYASHI ...
    1982 Volume 35 Issue 4 Pages 391-395
    Published: 1982
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    A strain of actinomycetes, isolated from a soil sample, has produced a novel antibiotic (C11H14O2S) containing a unique thiolactone moiety in its molecule. On the basis of taxonomic studies the producing organism was identified as belonging to the genus Nocardia. The antibiotic, named thiolactomycin, exhibits a broad antibacterial spectrum and particularly potent activity against Salmonella, Serratia and Bacteroides. Furthermore, the acute toxicity is weak in experimental animals. These results indicate that thiolactomycin is distinct from other known antibiotics and represents a new type of antibiotic.
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  • HIROSHI SASAKI, HIDEO OISHI, TOSHIAKI HAYASHI, IKUTOSHI MATSUURA, KUNI ...
    1982 Volume 35 Issue 4 Pages 396-400
    Published: 1982
    Released: April 12, 2006
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    Thiolactomycin, a new antibiotic produced by a soil isolate, Nocardia sp. No. 2-200, is shown to have the structure (4S)-(2E, 5E)-2, 4, 6-trimethyl-3-hydroxy-2, 5, 7-octatriene-4-thiolide on the basis of spectroscopic and X-ray crystallographic analyses. This compound containing an unusual thiolactone moiety is reported here as a representative of a new type of antibiotic.
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  • TAKAO NOTO, SATOHIDE MIYAKAWA, HIDEO OISHI, HISAO ENDO, HIROSHI OKAZAK ...
    1982 Volume 35 Issue 4 Pages 401-410
    Published: 1982
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Thiolactomycin is a new broad-spectrum antibiotic, active in vitro against many species of Gram-positive cocci, Enterobacteriaceae, Haemophilus, acid-fast bacteria and anaerobic bacteria. However, the activity is generally moderate and bacteriostatic in action. This antibiotic eludes cross resistance with any of the known antibacterial drugs such as ampicill in, carbenicillin or cycloserine. The effect on Gram-negative bacilli in vitro is little affected by the inoculum size, the presence of horse serum, the pH of the medium or the type of medium. When thiolactomycin was added to the assay medium, the minimum inhibitory concentration of ampicillin against inducible β-lactamase producing strains of Staphylococcus aureus and Pseudonzonasa eruginosa was reduced. Thiolactomycin inhibited the production of inducible β-lactamase in several organisms.
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  • SATOHIDE MIYAKAWA, KOJI SUZUKI, TAKAO NOTO, YUSUKE HARADA, HIROSHI OKA ...
    1982 Volume 35 Issue 4 Pages 411-419
    Published: 1982
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The new thiolactone antibiotic, thiolactomycin, is rapidly absorbed in rats when administered either orally or by intramuscular injection. A peak in concentration of the drug is reached in the blood and in various visceral organs within 15 minutes after administration. The concentration decreases rather rapidly and about 51- 69% of the drug is excreted in urine during the first 24 hours. Though the in vitro effect of thiolactomycin is moderate, it effectively protected mice challenged intraperitoneally with several strains of S. marcescens and K. pneumoniae and was more effective than carbenicillin in treating experimental acute urinary tracts infected with S. marcescens. Also, in mice whose immunodefense was decreased by treatment with cyclophosphamide, thiolactomycin was more effective than carbenicillin against S. marcescens challenge.
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  • NOEL D. JONES, MICHAEL O. CHANEY, HERBERT A. KIRST, GENE M. WILD, RICH ...
    1982 Volume 35 Issue 4 Pages 420-425
    Published: 1982
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    5-O-Mycarosyltylactone has been isolated as a predominant factor from fermentation broths of a Streptomyces fradiae mutant. The relative configurations of mycarose and tylactone (protylonolide) have been determined by X-ray crystal structure analysis. Hydrolysis of 5-O-mycarosyltylactone yielded (-)-tylactone and L-(-)-mycarose. Taken together, these two experiments establish the absolute configuration of (-)-tylactone. Bioconversion of (-)-tylactone to tylosin by tyl G mutants of S. fradiae proves the absolute configuration of tylosin. Physicochemical data for tylactone and a unique component piece of tylactone are also reported.
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  • JERRY R. MARTIN, R. LARRY DEVAULT, ARTHUR C. SINCLAIR, RUTH S. STANASZ ...
    1982 Volume 35 Issue 4 Pages 426-430
    Published: 1982
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    A new erythromycin, designated erythromycin F, was isolated from the mother liquors of an early commercial strain of Streptomyces erythreus. Although not established experimentally, erythromycin F may be a biosynthetic precursor of erythromycin E.
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  • G. RAK, H. ANKE, H. LAATSCH
    1982 Volume 35 Issue 4 Pages 431-435
    Published: 1982
    Released: April 12, 2006
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    A strain of Amblyosporium spongiosum (PERS.) Hughes sensu Pirozynski, HA 8006 isolated from an infected Lactarius deliciosus was found to produce two antibiotics, 8006-I and 8006-II. The same compounds could be isolated from cultures of several strains of the genus Amblyosporium obtained from the Centraalbureau voor Schimmelcultures. The highest yields of 8006-I (80 mg/liter culture) were obtained from the mycelium of strain HA 8006. Antibiotic 8006-I is unstable in the presence of light or oxygen and has a carotenoid structure.
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  • G. RAK, H. ANKE
    1982 Volume 35 Issue 4 Pages 436-440
    Published: 1982
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    8006-I is an antibacterial antibiotic with a rather broad spectrum of activity. The minimum inhibitory concentrations for the most sensitive bacteria are in the range of one to ten μg/ml. Yeasts are not affected by concentrations up to 100 μg/ml. Some filamentous fungi like Fusarium oxysporum and Mucor miebei are inhibited at 100 μ g/ml. In Ehrlich carcinoma ascitic cells the incorporation of uridine and leucine and to a lesser extent that of thymidine is reduced. In isolated nuclei of these cells the incorporation of UTP into RNA is inhibited. At low concentrations, the incorporation of uracil into trichloroacetic acid-precipitable material is almost completely inhibited in cells of Bacillus subtilis; at higher concentrations all macromolecular syntheses are affected. No reduction of respiration of the cells is observed. The antibiotic exhibits weak hemolytic activity and lytic activity towards bacteria. In vitro an inhibition of both DNA- and RNA polymerase from Escherichia coli is observed. Poly(U)-directed poly(Phe) synthesis is not affected.
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  • YOSHIHARU WAKISAKA, KENZO KOIZUMI, YOJI NISHIMOTO
    1982 Volume 35 Issue 4 Pages 441-449
    Published: 1982
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    A preferential isolation procedure was devised for asporogenous (Asp), Gram-positive (Gp), aerobic o r facultative anaerobic bacteria which included the genera Arthrobacter, Corynebacterium, Brevibacterium, Microbacterium, Mycobacterium, and Micrococcus (Asp-Gp bacteria). An antibiotics-mixture agar which contained 5 to 10 μg per ml of colistin, 10 to 20 μg per ml of nalidixic acid and 30 μg per ml of cycloheximide was used in the isolation. Using this technique 47 Asp-Gp bacteria representing 26 subgroups of coryneform bacteria and Micrococcus were isolated from 3 soil samples. The method was far more efficient than the standard dilution-plate technique. This preferential method is available to isolate Asp-Gp bacteria from a sample containing about 500-fold more of other Gram-positive and negative bacteria.
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  • YOSHIHARU WAKISAKA, KENZO KOIZUMI
    1982 Volume 35 Issue 4 Pages 450-457
    Published: 1982
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    In general, spores of B. cereus, B. megaterlun, B. sphaericus and B. subtilis strains germinated uniformly within a short time of incubation in a germination medium. In contrast, spores of B. circulans, B. brevis, B. laterosporus, B. pulvifaciens, B. polymyxa, B. pumilus, B. licneniformis and B. coagulans strains were usually slow and/or uneven germinators under the same conditions of incubation. The former group of Bacillus strains occur frequently in soils as the predominant population and the latter group of Bacillus species are found in many cases as minor populations. The minor populations of Bacillus were isolated with difficulty by the standard ilution-plate technique, but could easily be enriched by treating the soil sample in a germination medium for 2 to 3 hours at 30 to 35°C, followed by heating it at 65°C for 10 minutes ("minor-shifted isolation"). Using this technique, the minor Bacillus strains could be isolated from samples containing 100- to 1, 000-fold more of the rapid germinators of Bacillus.
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  • SHINICHI KOIZUMI, TOSHIHARU NAGATSU, HIRONOBU IINUMA, MASAJI OHNO, TOM ...
    1982 Volume 35 Issue 4 Pages 458-462
    Published: 1982
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Phenylalanine hydroxylase was shown to be inhibited by oudenone and its derivatives in vitro. At a concentration of 2.3×10-3 M, oudenone inhibited phenylalanine hydroxylase by 50%, and some of the oudenone derivatives showed more potent inhibition. The kinetic data have shown that the inhibition by oudenone is competitive with a tetrahydropterin cofactor (6-7-dimethyltetrahydropterin, DMPH4) and noncompetitive with phenylalanine and oxygen. Among 12 oudenone derivatives, there was no parallel structure-activity relationship between the inhibitory effect for phenylalanine hydroxylase and that for tyrosine hydroxylase. A derivative of oudenone, [compound No. 142; 2-(3-(3, 4-dihydroxyphenyl)-1-oxopropyl)cyclohexan-1, 3-dione] showed the most potent inhibition among the oudenone derivatives. It inhibited phenylalanine hydroxylase by 50% at a concentration of 1.8×10-5M. This inhibition was a mixed type with either a tetrahydropterin cofactor, DMPH4, or with the substrate phenylalanine, which was different from the inhibition by oudenone. However, the same noncompetitive inhibition was shown toward oxygen.
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  • MASAYUKI NARISADA, TADASHI YOSHIDA, HIROSHI ONOUE, MITSUAKI OHTANI, TE ...
    1982 Volume 35 Issue 4 Pages 463-482
    Published: 1982
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    A number of new optically active 1-oxacephem compounds were synthesized and tested for antibacterial activity. Various 7α-unsubstituted 1-oxacephem nuclei 2a-e and a 7α-methoxy-1-oxacephem nucleus 3, reported previously, were converted into the corresponding phenylacetylamino-, 2-thienylacetylamino-, D-mandelylamino-, D-phenylglycylamino-, and arylmalonylamino-1-oxacephem carboxylic acids. All the compounds except for the phenylglycylamino derivatives exhibited four- to sixteen-fold enhanced antibacterial activity compared with that of the corresponding cephalosporins. A combination of the 7α-methoxy-3-(1-methyl-1Htetrazol-5-yl)thiomethyl-1-oxacephem nucleus and a 7β-arylmalonylamino side chain, as represented by compound 1 (disodium salt of 33), produced the highest efficacy among them: high antibacterial activity with a widely expanded spectrum against Gram-negative bacteria including resistant strains and Pseudonronas aeruginosa was observed.
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  • SUSAN E. JENSEN, DONALD W. S. WESTLAKE, SAUL WOLFE
    1982 Volume 35 Issue 4 Pages 483-490
    Published: 1982
    Released: April 12, 2006
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    Cell-free extracts prepared by sonication of Streptomyces clavuligerus cyclized δ-(L-α-aminoadipyl)-L-cysteinyl-D-valine (ACV) into a penicillin-type antibiotic. The antibacterial spectrum of this antibiotic suggested it was a mixture of isopenicillin N and penicillin N indicating that both cyclization and racemase activities were present. Cyclization activity was optimal in extracts prepared from 48 hours cultures. Extracts incubated at 20°C produced antibiotic for 2 hours before activity ceased. Cyclization activity showed an absolute requirement for dithiothreitol( DTT) and O2 and was stimulated by ascorbic acid and FeSO4. No requirement for ATP was observed.
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  • SATOSHI OMURA, HARUO TANAKA, JUNJI INOKOSHI, HIDEO SAKAKIBAR, TATSURO ...
    1982 Volume 35 Issue 4 Pages 491-496
    Published: 1982
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The analysis of [3H]tetrahydroleucomycin A3 binding to Escherichia coli ribosomes are described. The dissociation constant for tetrahydroleucomycin A3 binding to ribosomes was 1.15×10-8M. One molecule of tetrahydroleucomycin A3 was bound to each 70 S ribosome (50 S subunit) as reported with erythromycin. The effect of leucomycins and their 3''-O-acyl derivatives on [3H]tetrahydroleucomycin A3 binding to ribosomes was examined. In general, 3''-O-acyl derivatives of leucomycins exhibited stronger antimicrobial activity against Gram-positive bacteria and weaker (or equivalent) activity against E. coli than their mother compounds. However, the affinities to ribosomes were approximately equivalent to those of the mother compounds, suggesting that Gram-positive bacterial cells are more permeable to 3''-O-acyl derivatives than to the mother compounds.
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  • HARUO IKEDA, HARUO TANAKA, SATOSHI OMURA
    1982 Volume 35 Issue 4 Pages 497-503
    Published: 1982
    Released: April 12, 2006
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    Covalently closed circular (ccc) DNAs were isolated by a technique involving alkaline denaturation from the spiramycin producer Streptomyces ambofaciens KA-1028 and also from spiramycin non-producing strains AF-11 and QN-25; plasmids could not be detected in these strains by a cleared lysate method. It was found that most of the ccc DNA in these strains was present in the chromosomal and membrane fractions. These ccc DNAs had identical mobilities in agarose gel electrophoresis. The size was calculated to be 53.1×106 daltons from the contour length measurements. The ccc DNA gave one fragment on digestion with Hind III, three fragments with Eco R1, and twenty-eight fragments with Bain H1.
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  • HARUO IKEDA, HARUO TANAKA, SATOSHI OMURA
    1982 Volume 35 Issue 4 Pages 507-516
    Published: 1982
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Spiramycin-producing Streptomyces ambofaciens KA-1028 harboring the pSA1 plasmid gave rise to spiramycin non-producing variants at high frequencies by various curing treatments. However, a number of the spiramycin non-producing progeny obtained by treatment with acridine dyes, still harbored plasmid DNAs which could not be differentiated from plasmid pSA1 by contour length, cleavage patterns and heteroduplex analysis. By treatment with mitomycin C, plasmid pSA1 was cured at high efficiency and spiramycin non-producing strains were obtained. Strain U-1717R obtained by regeneration of protoplasts of plasmid-cured strain U-1717 regained spiramycin production on growth on solid medium only. Furthermore, transconjugants obtained by mating between strain KA-1028 and U-1717R-24 (streptomycin-resistant) regained spiramycin production in both liquid and solid media. We conclude that the genes for the biosynthesis of spiramycin are encoded in a replicon other than plasmid pSA1 but that this plasmid plays a role in the regulation of spiramycin production.
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  • AKIO IWASAKI, TAKEO DEUSHI, ISAMU WATANABE, MASAO OKUCHI, HISAKATSU IT ...
    1982 Volume 35 Issue 4 Pages 517-519
    Published: 1982
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • KUNIKATSU SHIRAHATA, HIROSHI KASE, SHIGETO KITAMURA, TAKAO IIDA
    1982 Volume 35 Issue 4 Pages 520-523
    Published: 1982
    Released: April 12, 2006
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  • MILTON J. Jr. ZMIJEWSKI, MARCIA GOEBEL
    1982 Volume 35 Issue 4 Pages 524-526
    Published: 1982
    Released: April 12, 2006
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  • J. LEBOUL, J. DAVIES
    1982 Volume 35 Issue 4 Pages 527-528
    Published: 1982
    Released: April 12, 2006
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  • TENA T. WEI, JAMES A. CHAN, PETER P. ROLLER, ULRICH WEISS, RONALD M. S ...
    1982 Volume 35 Issue 4 Pages 529-532
    Published: 1982
    Released: April 12, 2006
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  • TATSUO ITO, NORIO EZAKI, KAZUNORI OHBA, SHOICHI AMANO, YASUMITSU KONDO ...
    1982 Volume 35 Issue 4 Pages 533-535
    Published: 1982
    Released: April 12, 2006
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  • NAOKI TSUJI, KAZUO NAGASHIMA, MASAAKI KOBAYASHI, YOSHIHIRO TERUI, KOIC ...
    1982 Volume 35 Issue 4 Pages 536-540
    Published: 1982
    Released: April 12, 2006
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  • YASUHIRO ITOH, SHUJI TAKAHASHI, MAMORU ARAI
    1982 Volume 35 Issue 4 Pages 541-542
    Published: 1982
    Released: April 12, 2006
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  • YUJI MORI, MAKOTO TSUBOI, MAKOTO SUZUKI, KAZUTAKA FUKUSHIMA, TADASHI A ...
    1982 Volume 35 Issue 4 Pages 543-544
    Published: 1982
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • TENA T. WEI, KEVIN M. BYRNE, DANA WARNICK-PICKLE, MICHAEL GREENSTEIN
    1982 Volume 35 Issue 4 Pages 545-548
    Published: 1982
    Released: April 12, 2006
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