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Cancer Lett ; 292(1): 48-53, 2010 Jun 01.
Article in English | MEDLINE | ID: mdl-19962231

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.


Subject(s)
Antineoplastic Agents/therapeutic use , Catechin/analogs & derivatives , Fluorine , Mammary Neoplasms, Experimental/drug therapy , Proteasome Inhibitors , Animals , Apoptosis/drug effects , Catechin/chemistry , Catechin/pharmacology , Catechin/therapeutic use , Cell Line, Tumor , Female , Humans , Hydrocarbons, Fluorinated/therapeutic use , Mammary Neoplasms, Experimental/metabolism , Mice , Mice, Nude , Xenograft Model Antitumor Assays
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