（-）-表没食子儿茶素-3-O-没食子酸酯对拓扑异构酶I和II的抑制活性。
Inhibitory activities of (-)-epigallocatechin-3-O-gallate against topoisomerases I and II.
作者信息
Suzuki K, Yahara S, Hashimoto F, Uyeda M
机构信息
Faculty of Pharmaceutical Sciences, Kumamoto University, Japan.
出版信息
Biol Pharm Bull. 2001 Sep;24(9):1088-90. doi: 10.1248/bpb.24.1088.
The substitution of gallic acid at the 3 position of (-)-epigallocatechin-3-O-gallate (EGCG) increased the inhibition against topoisomerase I from calf thymus gland and topoisomerase II from human placenta, and the substitution of a hydroxyl group at the 3' position increased the inhibition against the topoisomerase I. These results suggested that the 3 and 3' positions of the EGCG molecule play important roles in the process of inhibition of topoisomerases I and II. EGCG showed strong inhibition against topoisomerases I from wheat germ, calf thymus gland and Vero cells, and showed weak or no inhibition against topoisomerases I from carcinoma cells such as A549, HeLa and COLO 201 cells. EGCG differentially inhibited the topoisomerases I from different sources.
在（-）-表没食子儿茶素-3-O-没食子酸酯（EGCG）的3位用没食子酸取代，增强了对小牛胸腺拓扑异构酶I和人胎盘拓扑异构酶II的抑制作用，而在3'位用羟基取代则增强了对拓扑异构酶I的抑制作用。这些结果表明，EGCG分子的3位和3'位在抑制拓扑异构酶I和II的过程中起重要作用。EGCG对来自小麦胚芽、小牛胸腺和Vero细胞的拓扑异构酶I表现出强烈抑制作用，而对A549、HeLa和COLO 201细胞等癌细胞的拓扑异构酶I表现出较弱抑制作用或无抑制作用。EGCG对不同来源的拓扑异构酶I有不同程度的抑制作用。
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