CENTAUREIDIN, A CYTOTOXIC FLAVONE FROM POLYMNIA-FRUTICOSA, INHIBITS TUBULIN POLYMERIZATION

被引:73
作者
BEUTLER, JA
CARDELLINA, JH
LIN, CM
HAMEL, E
CRAGG, GM
BOYD, MR
机构
[1] NCI,MOLEC PHARMACOL LAB,DEV THERAPEUT PROGRAM,BETHESDA,MD 20892
[2] NCI,DIV CANC TREATMENT,DEV THERAPEUT PROGRAM,NAT PROD BRANCH,FREDERICK,MD 21702
关键词
D O I
10.1016/S0960-894X(01)81233-6
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The characteristic pattern of differential cytotoxicity of a crude extract of the tropical plant Polymnia fruticosa was found to be similar to those of known tubulin-interactive compounds. Fractionation of the extract led to centaureidin as the major cytotoxic principle. Centaureidin inhibited tubulin polymerization, inhibited the binding of [H-3]-colchicine to tubulin, and induced mitotic figure formation in whole cells at cytotoxic concentrations. This is the first known example of a flavone with antimitotic activity.
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页码:581 / 584
页数:4
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