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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
10
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pubmed:dateCreated |
2001-10-26
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pubmed:abstractText |
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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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Antigens, Neoplasm,
http://linkedlifedata.com/resource/pubmed/chemical/Antineoplastic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/DNA,
http://linkedlifedata.com/resource/pubmed/chemical/DNA Topoisomerases, Type II,
http://linkedlifedata.com/resource/pubmed/chemical/DNA topoisomerase II alpha,
http://linkedlifedata.com/resource/pubmed/chemical/DNA-Binding Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Enzyme Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Methyl Green,
http://linkedlifedata.com/resource/pubmed/chemical/Topoisomerase II Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Triterpenes
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pubmed:status |
MEDLINE
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pubmed:month |
Oct
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pubmed:issn |
0163-3864
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
64
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1294-6
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pubmed:dateRevised |
2011-11-17
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pubmed:meshHeading |
pubmed-meshheading:11678653-Antigens, Neoplasm,
pubmed-meshheading:11678653-Antineoplastic Agents,
pubmed-meshheading:11678653-Breast Neoplasms,
pubmed-meshheading:11678653-Carcinoma, Non-Small-Cell Lung,
pubmed-meshheading:11678653-Catalysis,
pubmed-meshheading:11678653-DNA,
pubmed-meshheading:11678653-DNA Topoisomerases, Type II,
pubmed-meshheading:11678653-DNA-Binding Proteins,
pubmed-meshheading:11678653-Electrophoresis, Agar Gel,
pubmed-meshheading:11678653-Electrophoretic Mobility Shift Assay,
pubmed-meshheading:11678653-Enzyme Inhibitors,
pubmed-meshheading:11678653-Female,
pubmed-meshheading:11678653-Glioma,
pubmed-meshheading:11678653-Humans,
pubmed-meshheading:11678653-Inhibitory Concentration 50,
pubmed-meshheading:11678653-Lung Neoplasms,
pubmed-meshheading:11678653-Methyl Green,
pubmed-meshheading:11678653-Molecular Structure,
pubmed-meshheading:11678653-Plants, Medicinal,
pubmed-meshheading:11678653-Saccharomyces cerevisiae,
pubmed-meshheading:11678653-Structure-Activity Relationship,
pubmed-meshheading:11678653-Topoisomerase II Inhibitors,
pubmed-meshheading:11678653-Triterpenes,
pubmed-meshheading:11678653-Tumor Cells, Cultured
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pubmed:year |
2001
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pubmed:articleTitle |
Catalytic inhibition of topoisomerase IIalpha by demethylzeylasterone, a 6-oxophenolic triterpenoid from Kokoona zeylanica.
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pubmed:affiliation |
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.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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