KINASE INHIBITORS FROM POLYGONUM-CUSPIDATUM
KINASE INHIBITORS FROM POLYGONUM-CUSPIDATUM
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DOI：
10.1021/np50100a021
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发表时间：
1993-10-01
影响因子：
5.1
通讯作者：
CHANG, CJ
中科院分区：
文献类型：
--
作者：
JAYATILAKE, GS;JAYASURIYA, H;CHANG, CJ
利用生物测定技术对虎杖进行分离，发现了一种羟基二苯乙烯类化合物白藜芦醇[1]，它是从牛胸腺中部分纯化的蛋白酪氨酸激酶(P56lck)的抑制物。白藜芦醇的反式和顺式异构体都具有类似的蛋白酪氨酸激酶抑制活性。比较白藜芦醇与白藜芦醇(白藜芦醇-O_3-β-葡萄糖苷)[2]和白藜芦醇-O_4‘-β-葡萄糖苷[3]抑制蛋白酪氨酸激酶活性的IC50值，表明两个苯环上的游离羟基是抑制蛋白酪氨酸酶活性所必需的。蛋白激酶C抑制分析表明，只需要在一个苯环上有两个自由羟基。
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.