Pladienolides, New Substances from Culture of Streptomyces platensis Mer-11107 III. In Vitro and In Vivo Antitumor Activities

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Other Title
  • Pladienolides, new substances from culture of streptomyces platensis mer-11107
  • III. <i>In Vitro</i> and <i>In Vivo</i> Antitumor Activities

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We have discovered seven novel 12-membered macrolides, pladienolides A to G, from Streptomyces platensis Mer-11107, with pladienolide B the most potently inhibiting hypoxia induced-VEGF expression and proliferation of the U251 cancer cell line. A growth inhibitory study using a 39-cell line drug-screening panel demonstrated that pladienolide B has strong antitumor activities in vitro. A COMPARE analysis reveals that it has a unique antitumor spectrum that sets it apart from anticancer drugs currently in clinical use. This result suggests that pladienolide B has a novel mechanism of action. A series of xenograft studies were conducted to evaluate the in vivo potency of pladienolides. Pladienolide B extensively inhibited tumor growth in xenograft models. In the most sensitive model, using BSY-1 xenografts, tumors were completely regressed by administration of pladienolide B. For the reason of their novel mechanism of action and excellent in vivo efficacy, pladienolides appear to have major potential for use in cancer treatment.

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Details 詳細情報について

  • CRID
    1390282679128172672
  • NII Article ID
    130003504157
  • DOI
    10.7164/antibiotics.57.188
  • COI
    1:CAS:528:DC%2BD2cXivVChsLo%3D
  • ISSN
    18811469
    00218820
    http://id.crossref.org/issn/00218820
  • PubMed
    15152804
  • Text Lang
    en
  • Article Type
    journal article
  • Data Source
    • JaLC
    • Crossref
    • PubMed
    • CiNii Articles
    • OpenAIRE
  • Abstract License Flag
    Disallowed

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