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Partial and weak oestrogenicity of the red wine constituent resveratrol: consideration of its superagonist activity in MCF‐7 cells and its suggested cardiovascular protective effects
Author(s) -
Ashby J.,
Tinwell H.,
Pennie W.,
Brooks A. N.,
Lefevre P. A.,
Beresford N.,
Sumpter J. P.
Publication year - 1999
Publication title -
journal of applied toxicology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.784
H-Index - 87
eISSN - 1099-1263
pISSN - 0260-437X
DOI - 10.1002/(sici)1099-1263(199901/02)19:1<39::aid-jat534>3.0.co;2-m
Subject(s) - wine , resveratrol , mcf 7 , agonist , chemistry , in vitro , receptor , endocrinology , estrogen receptor , pharmacology , estrogen , medicine , partial agonist , biology , biochemistry , food science , human breast , cancer , cancer cell , breast cancer
It was recently reported that the red wine phytoestrogen resveratrol (RES) acts as a superagonist to oestrogen‐responsive MCF‐7 cells. This activity of RES was speculated to be relevant to the ‘French paradox’ in which moderate red wine consumption is reported to yield cardiovascular health benefits to humans. We report here that RES binds to oestrogen receptors (ER) isolated from rat uterus with an affinity 5 orders of magnitude lower than does either the reference synthetic oestrogen diethylstilboestrol (DES) or oestradiol (E 2 ). In comparison with E 2 or DES, RES is only a weak and partial agonist in a yeast hER‐α transcription assay and in cos‐1 cell assays employing transient transfections of ER‐α or ER‐β associated with two different ER‐response elements. Resveratrol was also concluded to be inactive in immature rat uterotrophic assays conducted using three daily administrations of 0.03–120 mg kg −1 /day −1 RES (administered by either oral gavage or subcutaneous injection). These data weaken the suggestion that the oestrogenicity of RES may account for the reported cardiovascular protective effects of red wine consumption, and they raise questions regarding the extent to which oestrogenicity data derived for a chemical using MCF‐7 cells (or any other single in vitro assay) can be used to predict the hormonal effects likely to occur in animals or humans. Copyright © 1998 John Wiley & Sons, Ltd.