KINASE INHIBITORS FROM POLYGONUM-CUSPIDATUM

被引：226

作者：

JAYATILAKE, GS ^{[1
]}

JAYASURIYA, H ^{[1
]}

LEE, ES ^{[1
]}

KOONCHANOK, NM ^{[1
]}

GEAHLEN, RL ^{[1
]}

ASHENDEL, CL ^{[1
]}

MCLAUGHLIN, JL ^{[1
]}

CHANG, CJ ^{[1
]}

机构：

[1] PURDUE UNIV, SCH PHARM & PHARM SCI, DEPT MED CHEM & PHARMACOGNOSY, W LAFAYETTE, IN 47907 USA

来源：

JOURNAL OF NATURAL PRODUCTS | 1993年 / 56卷 / 10期

关键词：

D O I：

10.1021/np50100a021

中图分类号：

Q94 [植物学];

学科分类号：

071001 ;

摘要：

Bioassay-directed fractionation of a medicinal plant, Polygonum cuspidatum (Polygonaceae), has led to the discovery of a hydroxystilbene, resveratrol [1], as an inhibitor of a protein-tyrosine kinase (p56lck) partially purified from bovine thymus. Both trans and cis isomers of resveratrol possess comparable protein-tyrosine kinase inhibitory activity. Comparison of the IC50 values of resveratrol for protein-tyrosine kinase inhibitory activity with those of piceid (resveratrol-O3-beta-glucoside) [2) and resveratrol-O4'-beta-glucoside [3] shows the requirement of free hydroxyl groups on both phenyl rings for the protein-tyrosine kinase inhibition. Protein kinase C inhibitory analysis suggests the requirements of two free hydroxyl groups on one phenyl ring only.

引用

页码：1805 / 1810

页数：6

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