TMC-69, a new antitumor antibiotic with Cdc25A inhibitory activity, produced by Chrysosporium sp. TC1068. Taxonomy, fermentation and biological activities

J Antibiot (Tokyo). 2001 May;54(5):421-7. doi: 10.7164/antibiotics.54.421.

Abstract

A new antibiotic designated TMC-69 has been isolated from the fermentation broth of a fungal strain Chrysosporium sp. TC 1068. TMC-69 exhibited moderate in vitro cytotoxic activity. TMC-69-6H, a derivative of TMC-69 prepared by hydrogenation, possessed more potent in vitro cytotoxicity than TMC-69, and exhibited in vivo antitumor activity against murine P388 leukemia and B16 melanoma. TMC-69-6H was found to specifically inhibit Cdc25A and B phosphatases.

MeSH terms

  • Animals
  • Antibiotics, Antineoplastic / pharmacology*
  • Biological Assay
  • Cell Division / drug effects
  • Chrysosporium / growth & development
  • Chrysosporium / metabolism*
  • Enzyme Inhibitors / pharmacology*
  • Humans
  • Hydrogenation
  • Inhibitory Concentration 50
  • Leukemia P388 / drug therapy
  • Melanoma, Experimental / drug therapy
  • Mice
  • Pyrans / pharmacology*
  • Tumor Cells, Cultured
  • cdc25 Phosphatases / antagonists & inhibitors*
  • cdc25 Phosphatases / metabolism

Substances

  • Antibiotics, Antineoplastic
  • Enzyme Inhibitors
  • Pyrans
  • TMC-69
  • TMC-69-6H
  • CDC25A protein, human
  • Cdc25a protein, mouse
  • cdc25 Phosphatases