Hara-Terawaki Aya, Takagaki Akiko, Kobayashi Hirotsugu, Nanjo Fumio
Food Research Laboratories, Mitsui Norin Co., Ltd.
Biol Pharm Bull. 2017;40(8):1331-1335. doi: 10.1248/bpb.b17-00127.
Eleven kinds of catechin metabolites produced from (-)-epigallocatechin (EGC) and (-)-epigallocatechin gallate (EGCg) by intestinal microbiota were evaluated for inhibitory activity on the proliferation of HeLa cells, which are human cervical cancer cells. Among the catechin metabolites, 1-(3,4,5-trihydroxyphenyl)-3-(2,4,6-trihydroxyphenyl)propan-2-ol (EGC-M2), 4-hydroxy-5-(3,4,5-trihydroxyphenyl)valeric acid (EGC-M7), and 5-(3,4,5-trihydroxyphenyl)valeric acid (EGC-M9) were found to show inhibitory activity on HeLa cell proliferation as compared with control. The results suggested that three adjacent hydroxyl groups in the phenyl moiety may play an important role in the inhibitory activity. In addition, the inhibitory activity was also examined with four (-)-epicatechin (EC) metabolites possessing two adjacent hydroxyl groups in the phenyl moiety. Only 5-(3,4-dihydroxyphenyl)valeric acid (EC-M9) showed inhibitory activity and therefore valeric acid moiety likely contributes to the inhibitory activity. EGC-M9 showed the strongest inhibitory activity with IC of 5.58 µM. Thus, in this study it was found for the first time that several catechin metabolites derived from EGC, EGCg, and EC inhibit the proliferation of cervical cancer cells.
评估了肠道微生物群由（-）-表没食子儿茶素（EGC）和（-）-表没食子儿茶素没食子酸酯（EGCg）产生的11种儿茶素代谢产物对人宫颈癌细胞HeLa细胞增殖的抑制活性。在这些儿茶素代谢产物中，与对照组相比，发现1-（3,4,5-三羟基苯基）-3-（2,4,6-三羟基苯基）丙-2-醇（EGC-M2）、4-羟基-5-（3,4,5-三羟基苯基）戊酸（EGC-M7）和5-（3,4,5-三羟基苯基）戊酸（EGC-M9）对HeLa细胞增殖具有抑制活性。结果表明，苯基部分的三个相邻羟基可能在抑制活性中起重要作用。此外，还对苯基部分具有两个相邻羟基的四种（-）-表儿茶素（EC）代谢产物的抑制活性进行了检测。只有5-（3,4-二羟基苯基）戊酸（EC-M9）显示出抑制活性，因此戊酸部分可能对抑制活性有贡献。EGC-M9表现出最强的抑制活性，IC50为5.58 μM。因此，在本研究中首次发现，几种源自EGC、EGCg和EC的儿茶素代谢产物可抑制宫颈癌细胞的增殖。
