Pladienolides, new substances from culture of Streptomyces platensis Mer-11107. I. Taxonomy, fermentation, isolation and screening

  • J Antibiot (Tokyo). 2004 Mar;57(3):173-9. doi: 10.7164/antibiotics.57.173.
Takashi Sakai  1 ,  Tomohiro Sameshima ,  Motoko Matsufuji ,  Naoto Kawamura ,  Kazuyuki Dobashi ,  Yoshiharu Mizui
Affiliations
  • 1. Tsukuba Research Laboratories, Eisai Co., Ltd., 5-1-3, Tokodai, Tsukuba, Ibaraki 300-2635, Japan. [email protected]
PMID: 15152802 DOI: 10.7164/antibiotics.57.173
Abstract

Seven new macrolides having a 12-membered ring, which we termed pladienolides, were isolated from the fermentation broth of Streptomyces platensis Mer-11107. Six of the seven pladienolides inhibited hypoxia-induced reporter gene expression controlled by human VEGF promoter with IC50 values of 0.0018-2.89 microM. They also demonstrated growth-inhibitory activity against U251 human glioma cells in vitro. Pladienolides are highly potent inhibitors of both hypoxia signals and Cancer cell proliferation, and thus may be useful as antitumor agents.

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