Isemura M, Saeki K, Kimura T, Hayakawa S, Minami T, Sazuka M
Laboratory of Cellular Biochemistry, Graduate School of Nutritional and Environmental Sciences, The University of Shizuoka, Japan.
Biofactors. 2000;13(1-4):81-5. doi: 10.1002/biof.5520130114.
Epigallocatechin gallate (EGCg) and theaflavins, a major constituent of green tea infusion and the constituents of black tea, respectively, were found to inhibit matrix metalloproteinases (MMPs) which are intimately associated with tumor invasion and metastasis. EGCg and related polyphenols exhibited apoptosis-inducing activity for several cancer cell lines including human stomach and colon cancer cells. Comparison of the activity of these compounds revealed the importance of the number and the steric disposition of hydroxyl groups. A pyrogallol-type structure in a molecule is a minimum requirement for apoptosis induction of catechin compounds and that in the B ring has an important role in the activity. These data would provide useful information for designing anti-cancer agents on the basis of anti-inhibitory activity for MMPs and/or apoptosis-inducing activity.
表没食子儿茶素没食子酸酯(EGCg)和茶黄素分别是绿茶浸出物和红茶的主要成分,它们被发现可抑制与肿瘤侵袭和转移密切相关的基质金属蛋白酶(MMPs)。EGCg和相关多酚对包括人胃癌和结肠癌细胞在内的几种癌细胞系表现出诱导凋亡的活性。这些化合物活性的比较揭示了羟基数量和空间排列的重要性。分子中的邻苯三酚型结构是儿茶素化合物诱导凋亡的最低要求,且B环中的该结构在活性中起重要作用。这些数据将为基于对MMPs的抗抑制活性和/或诱导凋亡活性来设计抗癌药物提供有用信息。