RT Journal Article SR Electronic T1 Resveratrol Has Antagonist Activity on the Aryl Hydrocarbon Receptor: Implications for Prevention of Dioxin Toxicity JF Molecular Pharmacology JO Mol Pharmacol FD American Society for Pharmacology and Experimental Therapeutics SP 784 OP 790 VO 56 IS 4 A1 Robert F. Casper A1 Monique Quesne A1 Ian M. Rogers A1 Takuhiko Shirota A1 André Jolivet A1 Edwin Milgrom A1 Jean-François Savouret YR 1999 UL http://molpharm.aspetjournals.org/content/56/4/784.abstract AB Aryl hydrocarbon receptor (AhR) ligands such as dioxin and benzo[a]pyrene are environmental contaminants with many adverse health effects, including immunosuppression, carcinogenesis, and endothelial cell damage. We show here that a wine component, resveratrol (3,5,4′-trihydroxystilbene), is a competitive antagonist of dioxin and other AhR ligands. Resveratrol promotes AhR translocation to the nucleus and binding to DNA at dioxin-responsive elements but subsequent transactivation does not take place. Resveratrol inhibits the transactivation of several dioxin-inducible genes including cytochrome P-450 1A1 and interleukin-1β, both ex vivo and in vivo. Resveratrol has adequate potency and nontoxicity to warrant clinical testing as a prophylactic agent against aryl hydrocarbon-induced pathology. The American Society for Pharmacology and Experimental Therapeutics