The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
Volume 43 , Issue 2
Showing 1-15 articles out of 15 articles from the selected issue
  • HIDEO SUZUKI, MAKOTO TAHARA, MASAKO TAKAHASHI, FUMIKO MATSUMURA, TAKAY ...
    1990 Volume 43 Issue 2 Pages 129-134
    Published: February 25, 1990
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Resorthiomycin, a novel antitumor antibiotic, was isolated from the fermentation broth of a strain of Streptomyces collinus by ethyl acetate extraction, silica gel chromatography and HPLC. Resorthiomycin exhibited an in vitro cytotoxic activity against mouse leukemia L5178Y cells (IC50, 15.5 μg/ml) and also inhibited the clonogenic activity of a multidrug-resistant mutant of human hepatoma PLC/PRF/5 cells to a greater extent than that of the parental cells. On the other hand, this antibiotic does not possess any antibacterial or antifungal activity.
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  • MAKOTO TAHARA, TAKAYOSHI OKABE, KAZUO FURIHATA, NOBUO TANAKA, HIDEYO Y ...
    1990 Volume 43 Issue 2 Pages 135-137
    Published: February 25, 1990
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Resorthiomycin was revealed to be a new antibiotic with a molecular weight of 284 and a chemical formula of C14H20O4S as determined by MS and elemental analysis. The structure of resorthiomycin was determined to be 6-acetyl-4-(3-hydroxybutyl)-2-methyl-5-methylthioresorcinol by IR spectrum and 1H and 13C NMR.
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  • MAKOTO TAHARA, AKIHIRO TOMIDA, TOSHIO NISHIMURA, HIDEYO YAMAGUCHI, HID ...
    1990 Volume 43 Issue 2 Pages 138-142
    Published: February 25, 1990
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Resorthiomycin suppressed the clonogenic activity of a multidrug-resistant mutant cell line of Chinese hamster V79 cells more potently than its parental cells. Moreover, resorthiomycin at 40μg/ml potentiated the cytotoxic activity of vincristine and actinomycin D on V79 cells over 3-fold. Uptake of [3H]actinomycin D into V79 cells was stimulated 2-fold by 40μg/ml of resorthiomycin during 2 hours incubation. On the other hand, incorporation of [3H]thymidine and [3H]uridine into mouse leukemia L5178Y cells was inhibited in a dose-dependent manner at resorthiomycin concentrations ranging from 5 to 40μg/ml. In ATP-depleted L5178Y cells, membrane transport of [3H]thymidine and 2-[3H]deoxyglucose was strongly suppressed by resorthiomycin. These results suggest that resorthiomycin acts on the plasma membrane and perturbes some membrane function.
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  • TAKAAKI AOYAGI, SHIGEMI YOSHIDA, YASUSHI NAKAMURA, YASUHIRO SHIGIHARA, ...
    1990 Volume 43 Issue 2 Pages 143-148
    Published: February 25, 1990
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Probestin has been isolated as part of a program designed to find microorganism-produced inhibitors of aminopeptidase M from Streptomyces azureus MH663-2F6. It was purified by use of column chromatography of Amberlite XAD-4, silica gel, YMC-gel, Toyopearl HW-40, YMC D-ODS-5 (HPLC) and then isolated as colorless powders. Probestin is competitive with the substrate, and the inhibition constant (Ki) of it was 1.9×10-8 M.
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  • SHIGEMI YOSHIDA, YASUSHI NAKAMURA, HIROSHI NAGANAWA, TAKAAKI AOYAGI, T ...
    1990 Volume 43 Issue 2 Pages 149-153
    Published: February 25, 1990
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Probestin, a new inhibitor of aminopeptidase M, has been isolated from the culture broth of Streptomyces azureus MH663-2F6. The 1H and 13C NMR studies and amino acid analysis confirmed the presence of one 3-amino-2-hydroxy-phenylbutanoic acid, leucine and two proline residues in the molecule. Stereochemistries of these amino acids were determined by HPLC analysis. The fragmentation pattern shown in the mass spectrum and the chemical analysis on probestin clarified the amino acid sequence. Thus the structure of probestin was defined as (2S, 3R)-3-amino-2-hydroxy4-phenylbutanoyl-L-leucyl-L-prolyl-L-proline.
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  • KENICHI SUZUKI, HIROSHI YAMAGUCHI, SIGERU MIYAZAKI, KOUJI NAGAI, SHUN- ...
    1990 Volume 43 Issue 2 Pages 154-157
    Published: February 25, 1990
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    We found a new inhibitor of mammalian DNA topoisomerase I, named topostin, from a bacterial culture. The bacteria was identified as Flexibacter topostinus sp. nov., B-572. Morphological and physiological characteristics, and utilization of sugars were examined. Comparison of the strain with known species of the genus Flexibacter was made and indicates that the strain is a new species of the genus Flexibacter. The bacteria produced the inhibitor in parallel with their growth up to 72 hours.
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  • YOJI IKEGAMI, NORIAKI TAKEUCHI, MINORU HANADA, YOKO HASEGAWA, KAZUYUKI ...
    1990 Volume 43 Issue 2 Pages 158-162
    Published: February 25, 1990
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    We describe the isolation of inhibitors of mammalian DNA topoisomerase I, named topostins, from a culture broth of Flexibacter topostinus sp. nov. and some properties of the inhibitors. Topostins Al, A2 and B were isolated by differential solubility in solvents, adsorption chromatography on silica gel and gel nitration on a Sephadex LH-20 column. Topostins Al, A2 and B had specific activities of 4, 700, 16, 000 and 22, 000 U/mg, respectively. The most active metabolite topostin B comprised two components with MW of 567 and 553 in an equimolar ratio.
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  • HIROYUKI OSADA, HIDETOSHI TAKAHASHI, KYOKO TSUNODA, HIROO KUSAKABE, KI ...
    1990 Volume 43 Issue 2 Pages 163-167
    Published: February 25, 1990
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    In the course of our screening program using a bleb-forming assay, a new inhibitor of protein kinase C (PKC) was found in the fermentation of a streptomycete. The inhibitor, RK-286C (4'-demethylamino-4'-hydroxystaurosporine), inhibited the morphological change of K562 cells, a human chronic erythroleukemia cell, induced by phorbol 12, 13-dibutylate at the concentration of 3 μM. The same concentration of the compound inhibited the activity of PKC in vitro and the aggregation of rabbit platelets induced by collagen and arachidonic acid.
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  • HIDETOSHI TAKAHASHI, HIROYUKI OSADA, MASAKAZU URAMOTO, KIYOSHI ISONO
    1990 Volume 43 Issue 2 Pages 168-173
    Published: February 25, 1990
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    RK-286C, a new inhibitor of protein kinase C, has been found by the bleb-forming assay using K562 cells. It was produced by Streptomyces sp. RK-286 and purified by solvent extraction, silica gel chromatography and preparative HPLC. Spectrometric analysis revealed that the structure is 4'-demethylamino-4'-hydroxystaurosporine.
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  • HIROKO OGINO, KATSUYOSHI IWAMATSU, KIYOAKI KATANO, SATORU NAKABAYASHI, ...
    1990 Volume 43 Issue 2 Pages 174-188
    Published: February 25, 1990
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    A series of new aminothiazolylglycylcephalosporins with a mono- or dihydroxypyridonecarbonyl group at the α-amino group of the C-7 substituent have been prepared and antibacterial activity of these compounds was investigated. Among them, the compounds having a l, 5-dihydroxy-4-pyridone-2-carbonyl group showed excellent anti-pseudomonal activity. In particular, (6R, 7R)-7-[(RS)-2-(2-aminothiazol-4-yl)-2-(1, 5-dihydroxy-4-pyridone-2-carboxamido)-acetamido]-3-[[l-(2-hydroxyethyl)pyridinium-4-yl]thiomethyl]ceph-3-em-4-carboxylate(MT0703, 7g) was found to be a well balanced compound with respect to antibacterial activity.
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  • HIROKO OGINO, KATSUYOSHI IWAMATSU, KIYOAKI KATANO, SATORU NAKABAYASHI, ...
    1990 Volume 43 Issue 2 Pages 189-198
    Published: February 25, 1990
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    A practical synthetic method for large scale production of MT0703, (6R, 1R)-l-[(RS)-2-(2-aminothiazol-4-yl)-2-(l, 5-dihydroxy-4-pyridone-2-carboxamido)acetamido]-3-[[l-(2-hydroxyethyl)pyridinium-4-yl]thiomethyl]ceph-3-em-4-carboxylate, was established. Its two diastereomers on configuration of the aminothiazolylglycyl moiety were synthesized using chemico-enzymatic method. The S-isomer of MT0703 was found to be more active against Gram-positive and Gram-negative bacteria including β-lactamase-producing strains than the R-isomer.
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  • GILLES ETIENNE, ELISE ARMAU, GÉRARD TIRABY
    1990 Volume 43 Issue 2 Pages 199-206
    Published: February 25, 1990
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Strains of Saccharomyces cerevisiae FL200 capable of growing on a solid medium containing a mixture of polyene macrolide antibiotics (nystatin, 40 μg/ml, amphotericin B, 40 μg/ml, pimaricin, 150 μg/ml and RP9971 antibiotic, 10 μg/ml) have been isolated after successive selection steps. The mutant strains, PR13 and PRC24, are 10 to 100 times more resistant than the wild-type strain to 8 polyene macrolide antibiotics. When 4% Tween 80 is added to the medium, resistance to these antifungal drugs is further increased. In addition, strain PRC24, derived from strain PR13, is resistant to a non-polyene macrolide antifungal antibiotic, cycloheximide. In contrast, PR13 and PRC24 are both highly susceptible to a large range of compounds, including non-polyenic antifungal, antitumor and antibacterial agents. These particular characteristics make these strains useful for the rapid detection of antifungal compounds of the polyene macrolide and cycloheximide types, as well as for the recognition of antimitotic substances.
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  • WOLFGANG WEBER, TIMM ANKE, BERT STEFFAN, WOLFGANG STEGLICH
    1990 Volume 43 Issue 2 Pages 207-212
    Published: February 25, 1990
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    Strobilurin E is a novel antibiotic of the (E)-β-methoxyacrylate (MOA) class produced by mycelial cultures of the agaric Crepidotus fulvotomentosus. In addition to an inhibition of fungal respiration, a feature of all MOA-antibiotics, the compound exhibits very high cytostatic activities which are accompanied by reversible morphological alterations of the cells.
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  • HIDEJI FUJII, TERUYO TAKADA, KYUICHI NEMOTO, TAKUMI YAMASHITA, FUMINOR ...
    1990 Volume 43 Issue 2 Pages 213-219
    Published: February 25, 1990
    Released: April 19, 2006
    JOURNALS FREE ACCESS
    The effect of deoxyspergualin (DSG, NKT-01) on humoral immunity was investigated both in vitro and in vivo. DSG inhibited the primary and secondary responses to T cell-dependent antigens and the response to T cell-independent antigens in thymic and athymic mice. However, natural antibodies in non-sensitized mice were affected less by the administration of DSG. The agent produced a dose-dependent inhibition of B cell proliferation and antibody production to lipopolysaccharide in vitro. Suppression of secondary antibody response was also shown, whenever antigen stimulation was not given, antibody production was not affected. These results suggest that DSG affects the proliferative stage of B lymphocytes in such a way as to inhibit their growth and antibody production.
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  • A. B. MAUGER, O. A. STUART
    1990 Volume 43 Issue 2 Pages 220-221
    Published: February 25, 1990
    Released: April 19, 2006
    JOURNALS FREE ACCESS
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