TY - JOUR T1 - Resveratrol Has Antagonist Activity on the Aryl Hydrocarbon Receptor: Implications for Prevention of Dioxin Toxicity JF - Molecular Pharmacology JO - Mol Pharmacol SP - 784 LP - 790 VL - 56 IS - 4 AU - Robert F. Casper AU - Monique Quesne AU - Ian M. Rogers AU - Takuhiko Shirota AU - André Jolivet AU - Edwin Milgrom AU - Jean-François Savouret Y1 - 1999/10/01 UR - http://molpharm.aspetjournals.org/content/56/4/784.abstract N2 - 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 ER -