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

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...

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Bibliographic Details
Published in:Cancer letters 2010-06, Vol.292 (1), p.48-53
Main Authors: Yang, Huanjie, Sun, Dong Kui, Chen, Di, Cui, Qiuzhi Cindy, Gu, Yan Yan, Jiang, Tao, Chen, Wei, Wan, Sheng Biao, Dou, Q. Ping
Format: Article
Language:English
Subjects:
Animals
Antineoplastic Agents - therapeutic use
Apoptosis
Apoptosis - drug effects
Breast cancer
Cancer prevention
Catechin - analogs & derivatives
Catechin - chemistry
Catechin - pharmacology
Catechin - therapeutic use
Cell Line, Tumor
Drug discovery
Female
Fluorine
Hematology, Oncology and Palliative Medicine
Humans
Hydrocarbons, Fluorinated - therapeutic use
Kinases
Laboratory animals
Mammary Neoplasms, Experimental - drug therapy
Mammary Neoplasms, Experimental - metabolism
Mice
Mice, Nude
Polyphenols
Proteasome inhibitor
Proteasome Inhibitors
Rodents
Statistical analysis
Studies
Tea
Tea polyphenol
Tumors
Xenograft Model Antitumor Assays
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Summary: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.
ISSN:0304-3835
1872-7980
DOI:10.1016/j.canlet.2009.11.006