Catechin derivatives: Specific inhibitor for caspases-3, 7 and 2, and the prevention of apoptosis at the cell and animal levels
Catechin derivatives: Specific inhibitor for caspases-3, 7 and 2, and the prevention of apoptosis at the cell and animal levels
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DOI：
10.1016/j.febslet.2005.12.087
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发表时间：
2006-02-06
期刊：
影响因子：
3.5
通讯作者：
Murata, E
中科院分区：
文献类型：
--
作者：
Katunuma, N;Ohashi, A;Murata, E
茶儿茶素衍生物在体外抑制caspase -3、2和7的活性，并在细胞和动物水平上阻止实验性凋亡。表没食子儿茶素没食子酸酯在1 × 10(-7) M时对这些caspases的抑制作用最强，而半胱氨酸组织蛋白酶和caspase-8则不受抑制。Caspase-3的抑制表现为二级变构型，而caspase -2和7的抑制表现为非竞争型。这些儿茶素对体外培养的HeLa细胞凋亡有抑制作用。d -半乳糖胺在体内诱导大鼠肝细胞凋亡。在这种情况下，细胞质中caspase-3活性、血清转氨酶和dUTP缺口形成受到影响，这些升高被儿茶素抑制。(c) 2006年欧洲生化学会联合会。Elsevier B.V.版权所有。
Tea-catechin derivatives are shown to inhibit activities of caspases-3, 2 and 7 in vitro, and prevented experimental apoptosis at the cell and animal levels. Epigallo-catechin-gallate showed the strongest inhibition at 1 X 10(-7) M to these caspases, but cysteine cathepsins and caspase-8 were not inhibited. Caspase-3 inhibition showed a 2nd-order allosteric-type, but the inhibition of caspases-2 and 7 showed a non-competitive-type. The apoptosis-test using cultured HeLa cells was inhibited by these catechins. In rat hepatocytes, apoptosis was induced by D-galactosamine in vivo. In this case, caspase-3 activity in the cytoplasm, the serum aminotransferases and dUTP nick formation detected by TUNNEL-staining were effects, and these elevations were suppressed by administration of catechin. (c) 2006 Federation of European Biochemical Societies. Published by Elsevier B.V. All rights reserved.