Anti-tumor activity of a 3-oxo derivative of oleanolic acid

Cancer Lett. 2006 Feb 28;233(2):289-96. doi: 10.1016/j.canlet.2005.03.019. Epub 2005 Sep 9.

Abstract

Oleanolic acid (3beta-hydroxy-olea-12-en-28-oic acid, OA) exists widely in plant kingdom and possesses various pharmacological activities. In recent years, it was found that it had marked anti-tumor effects and exhibited cytotoxic activity towards many cancer cell lines in culture. In this article, the anti-tumor and differentiation-inducing effects of a derivative of OA modified at C-3, 3-oxo oleanolic acid (3-oxo-olea-12-en-28-oic acid, 3-oxo-OA, 3-7-1) was reported. In vitro, 3-7-1 were found to inhibit significantly the growth of cancer cells derived from different tissues. And 3-7-1 had inhibitory effect on melanoma in vivo. This selection may relate to the differentiation induced by 3-7-1. The inhibition of 3-7-1 on B16-BL6 suggests that 3-7-1 may be a useful anti-cancer agent for melanoma.

MeSH terms

  • Antineoplastic Agents / pharmacology*
  • Cell Differentiation / drug effects
  • Cell Survival / drug effects
  • DNA Topoisomerases, Type I / metabolism
  • Humans
  • Monophenol Monooxygenase / metabolism
  • Neoplasms, Experimental / drug therapy*
  • Neoplasms, Experimental / metabolism
  • Oleanolic Acid / analogs & derivatives
  • Oleanolic Acid / pharmacology*
  • Thymidine / metabolism
  • Tumor Cells, Cultured / drug effects

Substances

  • Antineoplastic Agents
  • Oleanolic Acid
  • Monophenol Monooxygenase
  • DNA Topoisomerases, Type I
  • Thymidine