Catalytic inhibition of topoisomerase IIα by demethylzeylasterone, a 6-oxophenolic triterpenoid from Kokoona zeylanica

T. R. Furbacher, A. A.L. Gunatilaka

Research output: Contribution to journalArticle

15 Scopus citations

Abstract

In a study to evaluate celastroloids as potential anticancer agents, demethylzeylasterone (5), a 6-oxophenolic triterpenoid from Kokoona zeylanica, was found to be an inhibitor of the enzyme topoisomerase IIa (IC50. = 17.ΜM). Studies of the relationship of this inhibitor to both DNA and the enzyme resulted in 5 being classified as a "catalytic inhibitor" of topoisomerase II. Demethylzeylasterone selectively inhibits the growth of the breast cancer cell line MCF-7 (IC50 = 12.5ΜM) without inhibiting the growth of non-small cell lung cancer (NCI-H460) and CNS glioma (SF-268) cell lines. This is the first report of topoisomerase II inhibitory activity in a celastroloid.

Original languageEnglish (US)
Pages (from-to)1294-1296
Number of pages3
JournalJournal Of Natural Products
Volume64
Issue number10
DOIs
StatePublished - Nov 14 2001

ASJC Scopus subject areas

  • Analytical Chemistry
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Drug Discovery
  • Complementary and alternative medicine
  • Organic Chemistry

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