Resveratrol, a polyphenolic compound found in grapes and wine, is an agonist for the estrogen receptor
TLDR
It is concluded that resveratrol is a phytoestrogen and that it exhibits variable degrees of estrogen receptor agonism in different test systems, which broaden the spectrum of its biological actions and may be relevant to the reported cardiovascular benefits of drinking wine.Abstract:
The phytochemical resveratrol, which is found in grapes and wine, has been reported to have a variety of anti-inflammatory, anti-platelet, and anti-carcinogenic effects. Based on its structural similarity to diethylstilbestrol, a synthetic estrogen, we examined whether resveratrol might be a phytoestrogen. At concentrations (≈3–10 μM) comparable to those required for its other biological effects, resveratrol inhibited the binding of labeled estradiol to the estrogen receptor and it activated transcription of estrogen-responsive reporter genes transfected into human breast cancer cells. This transcriptional activation was estrogen receptor-dependent, required an estrogen response element in the reporter gene, and was inhibited by specific estrogen antagonists. In some cell types (e.g., MCF-7 cells), resveratrol functioned as a superagonist (i.e., produced a greater maximal transcriptional response than estradiol) whereas in others it produced activation equal to or less than that of estradiol. Resveratrol also increased the expression of native estrogen-regulated genes, and it stimulated the proliferation of estrogen-dependent T47D breast cancer cells. We conclude that resveratrol is a phytoestrogen and that it exhibits variable degrees of estrogen receptor agonism in different test systems. The estrogenic actions of resveratrol broaden the spectrum of its biological actions and may be relevant to the reported cardiovascular benefits of drinking wine.read more
Citations
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Therapeutic potential of resveratrol: the in vivo evidence.
Joseph A. Baur,David A. Sinclair +1 more
TL;DR: A comprehensive and critical review of the in vivo data on resveratrol is provided, and its potential as a therapeutic for humans is considered.
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Role of Resveratrol in Prevention and Therapy of Cancer: Preclinical and Clinical Studies
Bharat B. Aggarwal,Anjana Bhardwaj,Rishi S. Aggarwal,Navindra P. Seeram,Shishir Shishodia,Yasunari Takada +5 more
TL;DR: In vivo, resveratrol blocks the multistep process of carcinogenesis at various stages: it blocks carcinogen activation by inhibiting aryl hydrocarbon-induced CYP1A1 expression and activity, and suppresses tumor initiation, promotion and progression.
Journal ArticleDOI
Phytochemicals: nutraceuticals and human health.
Cora J. Dillard,J. Bruce German +1 more
TL;DR: The rapid growth in the use of phytochemicals in nutraceutical and functional foods requires that the food and pharmaceutical industries face new challenges.
Journal ArticleDOI
Resveratrol Suppresses TNF-Induced Activation of Nuclear Transcription Factors NF-κB, Activator Protein-1, and Apoptosis: Potential Role of Reactive Oxygen Intermediates and Lipid Peroxidation
TL;DR: Resveratrol’s anticarcinogenic, anti-inflammatory, and growth-modulatory effects may be partially ascribed to the inhibition of activation of NF-κB and AP-1 and the associated kinases.
Journal ArticleDOI
Resveratrol Inhibits Cyclooxygenase-2 Transcription and Activity in Phorbol Ester-treated Human Mammary Epithelial Cells
Kotha Subbaramaiah,Wen Jing Chung,Pedro Michaluart,Nitin T. Telang,Tadashi Tanabe,Hiroyasu Inoue,Mei-Shiang Jang,John M. Pezzuto,Andrew J. Dannenberg +8 more
TL;DR: It is found that resveratrol also directly inhibited the activity of COX-2, a phenolic antioxidant found in grapes and other food products, which is likely to be important for understanding the anti-cancer and anti-inflammatory properties of resver atrol.
References
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Firefly luciferase gene: structure and expression in mammalian cells.
TL;DR: Assaying the expression of luciferase provides a rapid and inexpensive method for monitoring promoter activity and is estimated to be from 30- to 1,000-fold more sensitive than assaying chloramphenicol acetyltransferase expression.
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Use of an aqueous soluble tetrazolium/formazan assay for cell growth assays in culture.
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