虎杖中的激酶抑制剂。

Kinase inhibitors from Polygonum cuspidatum.

作者信息

Jayatilake G S, Jayasuriya H, Lee E S, Koonchanok N M, Geahlen R L, Ashendel C L, McLaughlin J L, Chang C J

机构信息

Department of Medicinal Chemistry and Pharmacognosy, School of Pharmacy and Pharmacal Sciences, Purdue University, West Lafayette, Indiana 47907.

出版信息

J Nat Prod. 1993 Oct;56(10):1805-10. doi: 10.1021/np50100a021.

DOI:10.1021/np50100a021

PMID:8277318

Abstract

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.

摘要

对药用植物虎杖（蓼科）进行生物测定导向的分级分离，发现了一种羟基茋——白藜芦醇[1]，它是从牛胸腺中部分纯化得到的一种蛋白酪氨酸激酶（p56lck）的抑制剂。白藜芦醇的反式和顺式异构体都具有相当的蛋白酪氨酸激酶抑制活性。将白藜芦醇对蛋白酪氨酸激酶抑制活性的IC50值与云杉新苷（白藜芦醇-O3-β-葡萄糖苷）[2]和白藜芦醇-O4'-β-葡萄糖苷[3]的IC50值进行比较，结果表明两个苯环上都需要有游离羟基才能抑制蛋白酪氨酸激酶。蛋白激酶C抑制分析表明仅一个苯环上需要有两个游离羟基。