Resveratrol, a natural product derived from grape, exhibits antiestrogenic activity and inhibits the growth of human breast cancer cells
Article first published online: 20 APR 1999
Copyright © 1999 Wiley-Liss, Inc.
Journal of Cellular Physiology
Volume 179, Issue 3, pages 297–304, June 1999
How to Cite
Lu, R. and Serrero, G. (1999), Resveratrol, a natural product derived from grape, exhibits antiestrogenic activity and inhibits the growth of human breast cancer cells. J. Cell. Physiol., 179: 297–304. doi: 10.1002/(SICI)1097-4652(199906)179:3<297::AID-JCP7>3.0.CO;2-P
- Issue published online: 20 APR 1999
- Article first published online: 20 APR 1999
- Manuscript Accepted: 29 DEC 1998
- Manuscript Received: 9 SEP 1998
- National Institutes of Health. Grant Number: RO1CA 58449
- U.S. Army Medical Research and Material Command. Grant Number: DAMD 17-96-1-6072
Resveratrol is a natural phytoalexin compound found in grapes and other food products. In this study, the effect of resveratrol on the growth of human breast cancer cells was examined. Results show that resveratrol inhibits the growth of estrogen receptor(ER)-positive MCF-7 cells in a dose-dependent fashion. Detailed studies with MCF-7 cells demonstrate that resveratrol antagonized the growth-promoting effect of 17-β-estradiol (E2) in a dose-dependent fashion at both the cellular (cell growth) and the molecular (gene activation) levels. At 5 × 10−6 M, resveratrol abolished the growth-stimulatory effect mediated by concentrations of E2 up to 10−9 M. The antiestrogenic effect of resveratrol could be observed at a concentration of 10−6 M and above. The antiestrogenic effect of resveratrol was also demonstrated at the molecular level. Resveratrol in a dose-dependent fashion antagonized the stimulation by E2 of progesterone receptor gene expression in MCF-7 cells. Moreover, expression of transforming growth factor-α and insulin-like growth factor I receptor mRNA was inhibited while the expression of transforming growth factor β2 mRNA was significantly elevated in MCF-7 cells cultivated in the presence of resveratrol (10−5 M). In summary, our results show that resveratrol, a partial ER agonist itself, acts as an ER antagonist in the presence of estrogen leading to inhibition of human breast cancer cells. J. Cell. Physiol. 179:297–304, 1999. © 1999 Wiley-Liss, Inc.