Abstract Title:

Inhibition of aryl hydrocarbon receptor-dependent transcription by resveratrol or kaempferol is independent of estrogen receptorα expression in human breast cancer cells.

Abstract Source:

Cancer Lett. 2010 Dec 28;299(2):119-29. Epub 2010 Sep 16. PMID: 20846786

Abstract Author(s):

Laura Macpherson, Jason Matthews

Article Affiliation:

Department of Pharmacology&Toxicology, University of Toronto, Toronto, Ontario, Canada M5S 1A8.

Abstract:

Resveratrol and kaempferol are natural chemopreventative agents that are also aryl hydrocarbon receptor (AHR) antagonists and estrogen receptor (ER) agonists. In this study we evaluated the role of ERα in resveratrol- and kaempferol-mediated inhibition of AHR-dependent transcription. Kaempferol or resveratrol inhibited dioxin-induced cytochrome P450 1A1 (CYP1A1) and CYP1B1 expression levels and recruitment of AHR, ERα and co-activators to CYP1A1 and CYP1B1. Both phytochemicals induced the expression and recruitment of ERα to gene amplified in breast cancer 1 (GREB1). RNAi-mediated knockdown of ERα in T-47D cells did not affect the inhibitory action of either phytochemical on AHR activity. Both compounds also inhibited AHR-dependent transcription in ERα-negative MDA-MB-231 and BT-549 breast cancer cells. These data show that ERα does not contribute to the AHR-inhibitory activities of resveratrol and kaempferol.

Study Type : In Vitro Study

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