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Cancer Lett. 2010 Jun 1;292(1):48-53. doi: 10.1016/j.canlet.2009.11.006. Epub 2009 Dec 3.

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

Author information

1
The Prevention Program, Barbara Ann Karmanos Cancer Institute, and Department of Pathology, School of Medicine, Wayne State University, Detroit, MI, USA.

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.

PMID:
19962231
PMCID:
PMC2854268
DOI:
10.1016/j.canlet.2009.11.006
[Indexed for MEDLINE]
Free PMC Article

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