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

T. R. Furbacher, Leslie Gunatilaka

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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
Publication statusPublished - 2001

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ASJC Scopus subject areas

  • Plant Science
  • Chemistry (miscellaneous)
  • Drug Discovery
  • Organic Chemistry
  • Pharmacology

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