Antitumor activity of novel fluoro-substituted (-)-epigallocatechin-3-gallate analogs

作者：Yang, Huanjie; Sun, Dong Kui; Chen, Di; Cui, Qiuzhi Cindy; Gu, Yan Yan; Jiang, Tao; Chen, Wei; Wan, Sheng Biao^*; Dou, Q. Ping

来源：Cancer Letters, 2010, 292(1): 48-53.

DOI：10.1016/j.canlet.2009.11.006

• Breast cancer
• Proteasome inhibitor
• Drug discovery
• Cancer prevention
• Tea polyphenol

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.

• 出版日期2010-6-1
• 单位中国海洋大学