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

页码：48 / 53

页数：6

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