ABSTRACT
This chapter discusses the nature and significance of resveratrol’s effects on estrogen receptors (ERs). Resveratrol was originally recognized as a phytoestrogen based on its ability to bind and activate ERα, but has since been found to bind ERß as well. Artificial estrogen-responsive reporter genes have been widely used in studying ER regulation of gene expression. Experiments using different cell lines and reporter constructs suggest that the estrogenicity of resveratrol, both in terms of potency and of whether it behaves as a superagonist, full agonist, partial agonist, or antagonist, can depend on the cell type, the specific sequence and promoter context of the estrogen response elements, and the ER isoform and subtype. In estrogen-dependent cells, the latter effect appears to predominate at lower concentrations, which may have important implications for the potential use of resveratrol in vivo against breast cancer and other estrogen-responsive malignancies.
