Author/Authors :
Yang، نويسنده , , Huanjie and Sun، نويسنده , , Dong Kui and Chen، نويسنده , , Di and Cui، نويسنده , , Qiuzhi Cindy and Gu، نويسنده , , Yan-yan and Jiang، نويسنده , , Tao and Chen، نويسنده , , Wei and Wan، نويسنده , , Sheng Biao and Dou، نويسنده , , Q. Ping Dou، نويسنده ,
Abstract :
Epidemiological studies support the cancer-preventive effects of green tea and its main constituent (–)-epigallocatechin gallate [(–)-EGCG], however, (–)-EGCG is unstable under physiological conditions. Here we report that two novel fluoro-substituted (–)-EGCG analogs inhibited tumor growth with similar potency to that of Pro-EGCG (1) which has improved potency over parental compound (–)-EGCG in human breast cancer MDA-MB-231 xenografts. MDA-MB-231 tumors treated with each fluoro-substituted (–)-EGCG analog showed proteasome inhibition and apoptotic cell death, suggesting that the proteasome might be one of the cellular targets of fluoro-(–)-EGCGs and that proteasome inhibition is partially responsible for the observed antitumor activity.
Keywords :
Drug discovery , breast cancer , Tea polyphenol , Proteasome inhibitor , Cancer prevention
