| Catalytic inhibition of topoisomerase IIalpha by demethylzeylasterone, a 6-oxophenolic triterpenoid from Kokoona zeylanica. | |
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MedLine Citation:
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PMID: 11678653 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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T R Furbacher; A A Gunatilaka |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Journal of natural products Volume: 64 ISSN: 0163-3864 ISO Abbreviation: J. Nat. Prod. Publication Date: 2001 Oct |
Date Detail:
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Created Date: 2001-10-26 Completed Date: 2001-12-21 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 7906882 Medline TA: J Nat Prod Country: United States |
Other Details:
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Languages: eng Pagination: 1294-6 Citation Subset: IM |
Affiliation:
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Southwest Center for Natural Products Research and Commercialization, Office of Arid Lands Studies, University of Arizona, 250 E. Valencia Road, Tucson, AZ 85706-6800, USA. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Antigens, Neoplasm Antineoplastic Agents / chemistry, isolation & purification*, pharmacology Breast Neoplasms Carcinoma, Non-Small-Cell Lung Catalysis DNA / antagonists & inhibitors DNA Topoisomerases, Type II, Eukaryotic / antagonists & inhibitors* 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 / diagnostic use Molecular Structure Plants, Medicinal / chemistry* Saccharomyces cerevisiae / drug effects, metabolism Structure-Activity Relationship Triterpenes / chemistry, isolation & purification*, pharmacology Tumor Cells, Cultured / drug effects |
| Chemical | |
Reg. No./Substance:
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0/Antigens, Neoplasm; 0/Antineoplastic Agents; 0/DNA-Binding Proteins; 0/Enzyme Inhibitors; 0/Triterpenes; 0/demethylzeylasterone; 82-94-0/Methyl Green; 9007-49-2/DNA; EC 5.99.1.-/DNA Topoisomerases, Type II, Eukaryotic; EC 5.99.1.3/DNA topoisomerase II alpha |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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