茶儿茶素代谢物M4和M6及其甲氧基衍生物的合成与生物活性
Synthesis and biological activity of the tea catechin metabolites, M4 and M6 and their methoxy-derivatives.
作者信息
Lambert Joshua D, Rice Joseph E, Hong Jungil, Hou Zhe, Yang Chung S
机构信息
Department of Chemical Biology, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, Piscataway, NJ 08854-8020, USA.
出版信息
Bioorg Med Chem Lett. 2005 Feb 15;15(4):873-6. doi: 10.1016/j.bmcl.2004.12.070.
Syntheses are reported for metabolites M4 (1) and M6 (2) of the green tea polyphenols epicatechin (EC) and epigallocatechin (EGC) and their gallate derivatives. Several methoxy-derivatives of 1 and 2 were also prepared. Compounds 1 and 2 were evaluated for growth inhibitory activity against a panel of immortalized and malignant human cell lines with 1 being the more active compound. The possible antiinflammatory activity of 1 and its trimethoxy derivative was also evaluated. Neither compound inhibited the release of arachidonic acid, although 1 inhibited NO production by 50% at 20 microM.
报告了绿茶多酚表儿茶素（EC）和表没食子儿茶素（EGC）及其没食子酸酯衍生物的代谢产物M4（1）和M6（2）的合成。还制备了1和2的几种甲氧基衍生物。对化合物1和2针对一组永生化和恶性人类细胞系的生长抑制活性进行了评估，其中1是活性更强的化合物。还评估了1及其三甲氧基衍生物可能的抗炎活性。两种化合物均未抑制花生四烯酸的释放，尽管1在20微摩尔浓度时可抑制50%的一氧化氮生成。
Zotero 插件