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

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 IIalpha (IC(50) = 17.6 microM). 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 (IC(50) = 12.5 microM) 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.
Authors	T R Furbacher, A A Gunatilaka
Journal	Journal of natural products (J Nat Prod) Vol. 64 Issue 10 Pg. 1294-6 (Oct 2001) ISSN: 0163-3864 [Print] United States
PMID	11678653 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References	Antigens, Neoplasm Antineoplastic Agents DNA-Binding Proteins Enzyme Inhibitors Topoisomerase II Inhibitors Triterpenes demethylzeylasterone Methyl Green DNA DNA Topoisomerases, Type II
Topics	Antigens, Neoplasm Antineoplastic Agents (chemistry, isolation & purification, pharmacology) Breast Neoplasms Carcinoma, Non-Small-Cell Lung Catalysis DNA (antagonists & inhibitors) DNA Topoisomerases, Type II DNA-Binding Proteins Electrophoresis, Agar Gel Electrophoretic Mobility Shift Assay Enzyme Inhibitors (chemistry, isolation & purification, pharmacology) Female Glioma Humans Inhibitory Concentration 50 Lung Neoplasms Methyl Green Molecular Structure Plants, Medicinal (chemistry) Saccharomyces cerevisiae (drug effects, metabolism) Structure-Activity Relationship Topoisomerase II Inhibitors Triterpenes (chemistry, isolation & purification, pharmacology) Tumor Cells, Cultured (drug effects)

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