The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
Volume 55, Issue 10
Displaying 1-11 of 11 articles from this issue
  • TOSHIYUKI SAITO, HIDEO HIRAI, YOON-JEONG KIM, YASUHIRO KOJIMA, YASUE M ...
    2002 Volume 55 Issue 10 Pages 847-854
    Published: October 25, 2002
    Released on J-STAGE: January 27, 2009
    JOURNAL FREE ACCESS
    A novel κ opioid receptor binding inhibitor CJ-15, 208 (I) was isolated from the fermentation broth of a fungus, Ctenomyces serratus ATCC15502. The structure of I was determined to be a cyclic tetrapeptide consisting of one tryptophan, one D-prohne, and two L-phenylalanine. Compound I was a selective binding inhibitor for the κ opioid receptor: 47nM (IC50) for κ, 260nM for μ, and 2, 600nM for δ. In the electrically-stimulated twitch response assay of rabbit vas deferens I recovered the suppression by a κ agonist asimadoline with an ED50 of 1.3μM, indicating that it is a κ antagonist.
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  • I. Taxonomy, Production, Isolation, Physicochemical Properties and Biological Activities
    YASUSHI SAKAI, TETSUO YOSHIDA, KEIKO OCHIAI, YOUICHI UOSAKI, YUTAKA SA ...
    2002 Volume 55 Issue 10 Pages 855-862
    Published: October 25, 2002
    Released on J-STAGE: January 27, 2009
    JOURNAL FREE ACCESS
    Six structurally related antitumor antibiotics named GEX1 compounds were isolated from a culture broth of Streptomyces sp. GEX1A was identified as a known herbicide, herboxidiene, structurally interested by the tetrahydropyran moiety and the side chain including a conjugated diene. GEX1Q1-Q5 were determined as novel compounds related to herboxidiene. All GEX1 compounds showed cytotoxicity with IC50 values of 0.0037-0.99μM against human tumor cell lines in vitro, but were not active against both Gram-positive and -negative bacteria. Though GEX1A/herboxidiene exhibited antitumor activity in murine tumor-planted mouse models, both GEX1Q3 and GEX1Q5 did not.
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  • II. The Effects on Cell Cycle Progression and Gene Expression
    YASUSHI SAKAI, TETSUYA TSUJITA, TADAKAZU AKIYAMA, TATSUHIKO YOSHIDA, T ...
    2002 Volume 55 Issue 10 Pages 863-872
    Published: October 25, 2002
    Released on J-STAGE: January 27, 2009
    JOURNAL FREE ACCESS
    Six GEX1 compounds, GEX1A/herboxidiene and its related 5 novel compounds, were isolated from a culture broth of Streptomyces sp. GEX1 compounds induced both G1 and G2/M arrest in a human normal fibroblast cell line, WI-38. All six compounds up-regulated luciferase reporter gene expression directed by enhancer/promoter of various genes, such as cdc2, IL-2 and SV40 early genes. All GEX1 compounds showed cytotoxic activities in the same order of the up-regulating activities on gene expression, suggesting that these two activities are related. Despite the up-regulating activities on the reporter gene expression, GEX1A/herboxidiene did not enhance the expression of any endogenous genes involved in the cell cycle, proliferation and apoptosis. Although the unique effects of GEX1 compounds on cell cycle and the reporter gene expression were similar to those of trichostatin A (TSA), an inhibitor of histone deacetylase (HDAC), GEX1A/herboxidiene did not affect histone acetylation in cells. In addition, GEX1A/herboxidiene treatment gave rise to the shorter sized transcripts of the cdc25A and cdc2 genes as well as the normal sized ones. These results suggest that GEX1 compounds modulate gene expression by an unknown mechanism.
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  • TAMOTSU FURUMAI, KEITARO ETO, TOMOMITSU SASAKI, HIROKO HIGUCHI, HIROYA ...
    2002 Volume 55 Issue 10 Pages 873-880
    Published: October 25, 2002
    Released on J-STAGE: January 27, 2009
    JOURNAL FREE ACCESS
    In screening for anti-MRSA antibiotics, novel lydicamycin congeners, TPU-0037-A, B, C and D, were isolated from a culture broth of an actinomycete strain. The producing strain, TP-A0598, was isolated from a seawater sample collected in Toyama Bay, Japan, and identified as Streptomyces platensis based on taxonomic characteristics. TPU-0037-A, B, C and D were purified by HP-20 resin, ODS column chromatographies and preparative HPLC, consecutively, and their structures were determined to be 30-demethyllydicamycin, 14, 15-dehydro-8-deoxylydicamycin, 30-demethyl-8-deoxylydicamycin and 8-deoxylydicamycin, respectively, by NMR and MS analyses. The new congeners showed antibiotic activity against Gram-positive bacteria including MRSA with the MIC of 1.56-12.5μg/ml.
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  • Taxonomy, Fermentation, Isolation, Structure Elucidation and Biological Activities
    VERONIKA HELLWIG, TORSTEN GROTHE, ANKE MAYER-BARTSCHMID, RAINER ENDERM ...
    2002 Volume 55 Issue 10 Pages 881-892
    Published: October 25, 2002
    Released on J-STAGE: January 27, 2009
    JOURNAL FREE ACCESS
    A novel antibacterial antibiotic, for which the name altersetin is proposed, was isolated from the culture broth of two endophytic Alternaria species. The relative and absolute configuration were assigned by NOESY or CD data, respectively. Altersetin is chemically related to equisetin and showed potent MIC against several pathogenic Gram-positive bacteria, whereas Gram-negative bacteria and pathogenic yeast were not or much less susceptible. Moderate in vivo efficiacy was observed for altersetin in a murine sepsis model.
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  • RATNAKAR N. ASOLKAR, RAJENDRA P. MASKEY, ELISABETH HELMKE, HARTMUT LAA ...
    2002 Volume 55 Issue 10 Pages 893-898
    Published: October 25, 2002
    Released on J-STAGE: January 27, 2009
    JOURNAL FREE ACCESS
    In our screening of marine streptomycete isolates for bioactive components, a new macrolide antibiotic designated as chalcomycin B (1b) was isolated from the culture broth of a marine Streptomycete isolate B7064 together with chalcomycin (1a) as the active principles. The structure of the new antibiotic was determined by EI and ESI MS, 1H, 13C and 2D NMR spectroscopy and by comparison of the NMR data with those of chalcomycin.
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  • DENNIS DITULLIO, NANCY ROCHELEAU, M. KELLY TALBOT, WILLIAM MILLETT, JA ...
    2002 Volume 55 Issue 10 Pages 899-903
    Published: October 25, 2002
    Released on J-STAGE: January 27, 2009
    JOURNAL FREE ACCESS
    Random subsets of a modest-sized microbial collection have been examined for culture redundancy, initially by morphology, both to the naked eye and microscopically, of cultures grown on a variety of agar-based solid media. Subsequent analysis, by simple TLC, of the extractable metabolites produced by morphologically similar cultures grown in submerged shaken fermentation was carried out. Apparent duplicate cultures were further examined on Biolog SF-P MicroPlatesTM for differentiation. The results were subjected to a statistical analysis and the contribution of each stage in the process to resolving culture uniqueness was noted. A statistical extrapolation of the results, from the subsets of each culture type, to the total for that type within the entire collection, with 95% confidence limits, is presented. Morphological comparison, on four different agar media, gives a significant underestimation of the metabolic diversity of the collection. The weighted mean from the three types of cultures indicate that the expected content of the collection is approximately 93% unique strains.
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  • YURIKO TANAKA, FUMIO ISHIKAWA, HIROYUKI OSADA, SHINOBU IMAJOH-OHMI, TE ...
    2002 Volume 55 Issue 10 Pages 904-913
    Published: October 25, 2002
    Released on J-STAGE: January 27, 2009
    JOURNAL FREE ACCESS
    Reveromycin A (Rev.A) is an inhibitor of epidermal growth factor-dependent cell growth that is produced from the culture broth of an actinomycete strain. Rev.A was assessed for its ability to regulate antigen (Ag) presentation by A20-HL B lymphoma cells bearing trinitrophenyl (TNP)-specific surface IgM (sIgM) to cloned T cells specific for OVA323-339/I-Ad. Rev.A-treatment inhibited the presentation of Ag internalized via sIgM, but not of Ag via fluid-phase pinocytosis. Rev.A-treatment decreased protein synthesis, but a similar decrease in protein synthesis by cycloheximide induced much less inhibition of sIgM-mediated Ag presentation. Rev.A-treatment decreased the rate of re-expression of sIgM in A20-HL cells, the amount of Ag internalized via sIgM during 3 hours of incubation, and the generation of antigenic peptides from TNP-OVA internalized via sIgM. Rev.A-treatment was suggested to affect intracellular trafficking from early endosomes into late endocytic compartments of Ag internalized via sIgM. Rev.A might provide a useful tool for studying intracellular transport of Ag, especially Ag internalized via sIgM.
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  • VENETA BOJANOVA IVANOVA, YASUTAKA HOSHINO, KATSUKIYO YAZAWA, AKIKAZU A ...
    2002 Volume 55 Issue 10 Pages 914-918
    Published: October 25, 2002
    Released on J-STAGE: January 27, 2009
    JOURNAL FREE ACCESS
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  • TOMOHISA KUZUYAMA, SHUNJI TAKAHASHI, TOHRU DAIRI, HARUO SETO
    2002 Volume 55 Issue 10 Pages 919-923
    Published: October 25, 2002
    Released on J-STAGE: January 27, 2009
    JOURNAL FREE ACCESS
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  • II. Structure Elucidation of Bottromycins B2 and C2
    MIYUKI KANEDA
    2002 Volume 55 Issue 10 Pages 924-928
    Published: October 25, 2002
    Released on J-STAGE: January 27, 2009
    JOURNAL FREE ACCESS
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