The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
Volume 39 , Issue 2
Showing 1-21 articles out of 21 articles from the selected issue
  • ATSUSHI TAKAHASHI, KUNIMOTO HOTTAN, ORIKO SAITO, MOTO MORIOKA, YOSHIRO ...
    1986 Volume 39 Issue 2 Pages 175-183
    Published: 1986
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    An actinomycete isolate designated as TS-1980 with multiple resistance to aminoglycoside antibiotics was found to produce novel antibiotics. The strain showed taxonomic features identical to the type strain of Nocardiopsis mutabilis except for the temperature range for growth and the utilization of mannitol and raffinose. Based on the capability of growing at lower temperature range, the strain was named N. mutabilis subsp. cryophilis subsp. nov. Physico-chemical and biological characterization of a purified antibiotic revealed its novel polyamine-type nature with a broad antimicrobial activity. The antibiotic was named dopsisamine.
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  • MASAYUKYI AMATO, HIRONOBU IINUMA, HIROSHI NAGANAWA, YUHJI YAMAGISHI, M ...
    1986 Volume 39 Issue 2 Pages 184-191
    Published: 1986
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Valanimycin, a new azoxy antibiotic, was isolated from culture broths of a streptomycete. Valanimycin is an unstable oil at room temperature and active against some Gram-positive and Gram-negative bacteria, mouse leukemia L1210 cells in cultures, and prolongs the life span of mice inoculated with Ehrlich carcinoma or L1210.
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  • DISCOVERY, FERMENTATION, CULTURE CHARACTERIZATION AND BIOLOGICAL ACTIVITY
    J. B. TUNAC, S. W. MAMBER, B. D. GRAHAM, W. E. DOBSON
    1986 Volume 39 Issue 2 Pages 192-197
    Published: 1986
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    A novel phenazine antitumor antibiotic is described, produced by Streptomyces lomondensis subsp. galanosa NRRL 15738. The antibiotic is selectively active versus the bacterium Streptococcus pneumoniae (MIC <0.46 μg/ml); the antitumor activity versus murine P388 leukemia is T/C 149.
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  • I. TAXONOMY, FERMENTATION, ISOLATION, AND PHYSICO-CHEMICAL AND BIOLOGICAL CHARACTERISTICS
    MASANORI OKAMOTO, KEIZO YOSHIDA, MOTOAKI NISHIKAWA, TAKESHI ANDO, MORI ...
    1986 Volume 39 Issue 2 Pages 198-204
    Published: 1986
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    A PAF antagonist, designated as FR-900452, was isolated from fermentation products of Streptomyces phaeofaciens and the molecular formula was determined as C22H25N3O3S. The compound inhibited PAF-induced rabbit platelet aggregation with an IC50 of 3.7×10-7 M, but was much less active against collagen-, arachidonic acid- or ADP-induced aggregation (IC50; 6.4×10-5, >10-4 or >10-4 M, respectively).
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  • ITSUO KUROBANE, NORIHIRO ZAITA, AKIO FUKUDA
    1986 Volume 39 Issue 2 Pages 205-214
    Published: 1986
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Six strains of Fusarium martii produced fusarubin and dihydrofusarubins A and B. Further examination of strains, T-77 and T-127, showed that four additional metabolites were produced. By 1H and 13C NMR spectral analyses, these additional metabolites have been identified as 3-O-methyl and 3-O-ethyl ethers of fusarubin and dihydrofusarubin A. The methyl ethers are new compounds and showed moderate cytostatic activity against mouse leukemia L1210 culture cells as well as moderate antibiotic activity against Gram-positive bacteria and fungi. 3-O-Methyl and 3-O-ethyl ethers of dihydrofusarubin A were converted non-enzymically to the respective ethers of fusarubin under alkaline conditions. Since in addition, only dihydrofusarubin derivatives were formed when an acidic pH was maintained in the culture, it can be concluded that only these are true metabolites of Fusarium martii.
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  • V. SYNTHESIS AND ANTIBACTERIAL ACTIVITY OF 3-[2-(2- AMINOTHIAZOL-4-YL)-( Z)-2-(O-SUBSTITUTED OXYIMINO)- ACETAMIDO]-1-(1H-TETRAZOL-5-YL)-2-AZETIDINONES HAVING VARIOUS FUNCTIONAL GROUPS AT C-4 POSITION OF β-LACTAM
    CHOSAKU YOSHIDA, KIYOSHI TANAKA, RIKIZO HATTORI, YOSHIKAZU FUKUOKA, MI ...
    1986 Volume 39 Issue 2 Pages 215-229
    Published: 1986
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    The synthesis and antibacterial activity of the 3-[2-(2-aminothiazol-4-yl)-( Z)-2-(O-substituted oxyimino)acetamido]-1-(1H-tetrazol-5-yl)-2-azetidinones having various functional groups at C-4 position of β-lactam are described. These compounds exhibited a strong activity against a variety of Gram-negative bacteria including β-lactamase-producing strains. Among various C-4 substituents explored, the fluoromethyl and carbamoyloxymethyl moiety were found to increase the activity.
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  • I. SYNTHESIS AND ANTIBACTERIAL ACTIVITY OF NEW UREIDOPENICILLIN DERIVATIVES HAVING CATECHOL MOIETIES
    NOBUHIRO OHI, BUNYA AOKI, TEIZO SHINOZAKI, KANZI MORO, TAKAO NOTO, TOS ...
    1986 Volume 39 Issue 2 Pages 230-241
    Published: 1986
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    The synthesis and antibacterial activity of new ureidopenicillin derivatives having catechol moieties in the 6-acyl side chain are described. These compounds showed remarkably strong activities against Pseudomonas aeruginosa. Especially, 6-[(R)-2-[3-(3, 4-dihydroxybenzoyl)-3-
    methyl-1-ureido]-2-phenylacetamido]penicillanic acid (7a) had the most potent activity in vitro against Gram-negative bacteria, its activity being 30-60-fold greater than that of piperacillin against most strains of P. aeruginosa.
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  • II. EFFECT ON ANTIBACTERIAL ACTIVITY OF UREIDO NSUBSTITUENTS IN THE 6-[(R)-2-[3-(3, 4- DIHYDROXYBENZOYL)-1-UREIDO]-2- PHENYLACETAMIDO]PENICILLANIC ACIDS
    NOBUHIRO OHI, BUNYA AOKI, KANZI MORO, TOSHIHIKO KUROKI, NAOYUKI SUGIMU ...
    1986 Volume 39 Issue 2 Pages 242-250
    Published: 1986
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    The synthesis and the relationship between in vitro and in vivo activities of 6-[(R)-2-[3-(3, 4-dihydroxybenzoyl)-3-R1-1-ureido]-2-phenylacetamido]penicillanic acids having C2-8 alkyl or substituted alkyl groups as the substituents (R1) are described. In this series, 6-[(R)-2-[3-(3, 4-dihydroxybenzoyl)-3-(3-hydroxypropyl)-1-ureido]-2-phenylacetamido]penicillanic acid (1b, AO-1100) showed the most potent protective effect on mice in experimental Pseudomonas aeruginosa infections, although it did not have the strongest in vitro activity among the penicillins we synthesized.
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  • 7. DIHYDROSTREPTOMYCIN ANALOGUES
    DANA L. DELAWARE, MAHENDRA S. SHARMA, BHASHYAM S. IYENGAR, WILLIAM A. ...
    1986 Volume 39 Issue 2 Pages 251-258
    Published: 1986
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Dihydrostreptomycin analogues with structural variations in their guanidino groups were prepared. The analogue with a methyl group on the guanidine at C-1 was nearly as active as dihydrostreptomycin against bacteria. However, the 2-imidazolin-2-ylamino substituent at C-1 eliminated activity. No analogue with a substituent on the C-3 guanidino group was active.
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  • ACID BY THE THIENAMYCIN PRODUCER, STREPTOMYCES CATTLEYA
    MINORU SANADA, TETSUJI MIYANO, SHUICHI IWADARE, JOANNE M. WILLIAMSON, ...
    1986 Volume 39 Issue 2 Pages 259-265
    Published: 1986
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    An antimetabolite, THX, was isolated from fermentation broths of the thienamycin producer, Streptomyces cattleya, when the organism was grown in the presence of a fluorine-containing substrate. THX was subsequently identified as one of the four possible stereoisomers of 4-fluorothreonine. Inorganic fluoride or any one of a number of organofluorine compounds can be used as precursors of 4-fluorothreonine. In addition, 19F NMR has provided evidence that the organism synthesizes fluoroacetate under the same fermentation conditions. The in vitro antibacterial spectrum of 4-fluorothreonine is also presented.
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  • KARL-HEINZ MAURER, DIETER MECKE
    1986 Volume 39 Issue 2 Pages 266-271
    Published: 1986
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    The production of the sesquiterpenoid antibiotic pentalenolactone in the producer strain Streptomyces arenae TÜ 469 is controlled by the activity of the enzyme farnesylpyrophosphate cyclase. In contrast to the activity of this enzyme, the specific activities of all other enzymes of the mevalonoid pathway tested so far, proved to be not rate-limiting. Several metabolites of the pentalenolactone pathway were tested for inhibitory effects on the activity of the HMG-CoA reductase and farnesylpyrophosphate cyclase. The activity of the cyclase was inhibited by low concentrations of pentalenolactone and its derivatives, thus suggesting an end product inhibition of the starting enzyme of the pentalenolactone pathway. The activity of HMG-CoA reductase was not inhibited by pentalenene or any pentalenolactone- derivatives. According to these results, an end-product inhibition of the first enzyme which is specific for pentalenolactone synthesis seems to be a mechanism involved in the regulation of pentalenolactone biosynthesis.
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  • HIROSHI TAKESHIMA, AKIRA ENDO, KENJI WADA, TADASHI TANABE
    1986 Volume 39 Issue 2 Pages 275-280
    Published: 1986
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    In a previous study (A. ENDO, et al., J. Antibiotics 38: 599-604, 1985), 2-alkyl glutarate and its derivatives isolated from cultures of Gongronella butleri were shown to inhibit animal acetyl-CoA carboxylase. In the present communication, the inhibition of liver acetyl-CoA carboxylase was investigated with several 2-alkyl glutarate and 2-alkyl succinate analogs. Their inhibitory potency increased with the chain length of the alkyl moiety, and 2-tetradecanylglutarate was most potent among the inhibitors tested. Kinetic analysis indicated that inhibition by 2-tetradecanylglutarate was non-competitive with respect to the substrates, ATP, HCO3-and acetyl-CoA, and competitive with respect to the allosteric regulator citrate, giving a Ki value of 40 μM. Sucrose density gradient centrifugation analysis showed that the citrate-induced polymerization of the enzyme was inhibited by 2-tetradecanylglutarate.
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  • DONALD B. BOYD, JOHN L. OTT
    1986 Volume 39 Issue 2 Pages 281-285
    Published: 1986
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Recent work has shown that the activity of cephalosporins in inhibiting exocellular DD-peptidases from Streptomyces R61 and Actinomadura R39 are, at best, only poorly related to minimum inhibitory concentrations against pathogenic isolates. Taking into account the rate at which cephalosporins diffuse through porin channels, such as exist in certain Gram-negative organisms, does not help in establishing a relationship between MIC data and the kinetic data on the model enzymes. Most published cell wall permeability studies, the porin ones being a principal exception, have not examined long enough series of structurally related compounds to establish property-activity relationships.
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  • HIROYUKI OSADA, KIYOSHI ISONO
    1986 Volume 39 Issue 2 Pages 286-293
    Published: 1986
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    An ascamycin dealanylating enzyme (Xc-aminopeptidase) has been isolated from Xanthomonas citri and characterized as a proline iminopeptidase of molecular weight of 38, 000 (H. OSADA & K. ISONO, Biochem. J. 233: 459-463, 1986). Immunological studies have shown that all the mammalian cells tested possess a closely-related enzyme(s) on their cell membranes. This enzyme is more active in transformed cells than in nontransformed cells. A decreased
    ratio of ID50 (ascamycin/dealanylascamycin based on [35S]methionine uptake) in transformed cells compared with the nontransformed cell can be explained on the basis of the conversion of ascamycin to dealanylascamycin by the enzyme. It is suggested that ascamycin cannot be transported through mammalian cell membranes but dealanylascamycin can permeate; a similar situation exists in prokaryotic cells.
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  • YUJI WATANABE, SHUICHI TAWARA, YASUHIRO MINE, HIROYUKI KIKUCHI, SACHIK ...
    1986 Volume 39 Issue 2 Pages 294-303
    Published: 1986
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    The interactions between subinhibitory concentrations of cephalosporins and polymorphonuclear leukocytes in the killing of a strain of Escherichia coli are described and an attempt is made to define the responsible mechanism. Ceftizoxime was the most potent agent tested. Pretreatment of the E. coli strain with subinhibitory concentrations of ceftizoxime increased the susceptibility to both; phagocytic killing activity of the polymorphonuclear leukocytes and bactericidal activities of the oxygen metabolites and the granule extracts. A most interesting result was the increased susceptibility of the ceftizoxime-treated E. coli to killing by β-glucuronidase which normally is not bactericidal. It is suggested that the augmented killing could be due to bacteriolysis by β-glucuronidase.
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  • MINORU SANADA, TETSUJI MIYANO, SHUICHI IWADARE
    1986 Volume 39 Issue 2 Pages 304-305
    Published: 1986
    Released: April 19, 2006
    JOURNALS FREE ACCESS
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  • II. INHIBITION OF REVERSE TRANSCRIPTASE ACTIVITY
    HIROMASA OKADA, HIROYUKI MUKAI, YOSHIO INOUYE, SHOSHIRO NAKAMURA
    1986 Volume 39 Issue 2 Pages 306-308
    Published: 1986
    Released: April 19, 2006
    JOURNALS FREE ACCESS
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  • SATOSHI OMURA, HARUO TANAKA, HIROSHI KUGA, NOBUTAKA IMAMURA
    1986 Volume 39 Issue 2 Pages 309-310
    Published: 1986
    Released: April 19, 2006
    JOURNALS FREE ACCESS
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  • MITSUYUKI HOTTA, YOICHI HAYAKAWA, KAZUO FURIHATA, AKIRA SHIMAZU, HARUO ...
    1986 Volume 39 Issue 2 Pages 311-313
    Published: 1986
    Released: April 19, 2006
    JOURNALS FREE ACCESS
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  • HIKARU NAKAMURA, YOICHI IITAKA, MASAYA IMOTO, KUNIO ISSHIKI, HIROSHI N ...
    1986 Volume 39 Issue 2 Pages 314-315
    Published: 1986
    Released: April 19, 2006
    JOURNALS FREE ACCESS
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  • TAKAYOSHI OKABE, KOKICHI SUZUKI, HIDEO SUZUKI, YOSHIO INOUYE, SHOSHIRO ...
    1986 Volume 39 Issue 2 Pages 316-317
    Published: 1986
    Released: April 19, 2006
    JOURNALS FREE ACCESS
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