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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• 作者：Nobuhiko Katunuma ; Atsushi Ohashi ; Etsuko Sano ; Naozumi Ishimaru ; Yoshio Hayashi and Etsuko Murata
• 关键词：Catechin ; Caspase-3 ; Apoptosis ; d-Galactosamine ; Serum aminotransferase
• 刊名：FEBS Letters
• 出版年：2006
• 期刊代码：70_00145793
• 类别：bio
• 出版时间：6 February 2006
• 卷：580
• 期：3
• 页码：741-746
• 文件大小：1228 K

摘要

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 × 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.