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

被引：30
|
作者：
Yang, Huanjie [2 ,3 ]
Sun, Dong Kui [1 ]
Chen, Di [2 ,3 ]
Cui, Qiuzhi Cindy [2 ,3 ]
Gu, Yan Yan [1 ]
Jiang, Tao [1 ]
Chen, Wei [4 ,5 ]
Wan, Sheng Biao [1 ]
Dou, Q. Ping [2 ,3 ]
机构：
[1] Ocean Univ China, Key Lab Marine Drug, Minist Educ, Sch Med & Pharm, Qingdao, Peoples R China
[2] Wayne State Univ, Prevent Program, Barbara Ann Karmanos Canc Inst, Sch Med, Detroit, MI USA
[3] Wayne State Univ, Sch Med, Dept Pathol, Detroit, MI 48201 USA
[4] Wayne State Univ, Karmanos Canc Inst, Detroit, MI USA
[5] Wayne State Univ, Dept Internal Med, Detroit, MI 48202 USA
来源：
CANCER LETTERS | 2010年 / 292卷 / 01期
关键词：
Breast cancer; Proteasome inhibitor; Drug discovery; Cancer prevention; Tea polyphenol; GREEN TEA CATECHINS; HUMAN PROSTATE-CANCER; PROTEASOME INHIBITORS; APOPTOSIS INDUCERS; POLYPHENOLS; METHYLATION; SUPPRESSES; THERAPY; TARGET; TRIAL;
D O I：
10.1016/j.canlet.2009.11.006
中图分类号：
R73 [肿瘤学];
学科分类号：
100214 ;
摘要：
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. (C) 2009 Elsevier Ireland Ltd. All rights reserved.
引用
收藏
页码：48 / 53
页数：6
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