PT - JOURNAL ARTICLE AU - Robert F. Casper AU - Monique Quesne AU - Ian M. Rogers AU - Takuhiko Shirota AU - André Jolivet AU - Edwin Milgrom AU - Jean-François Savouret TI - Resveratrol Has Antagonist Activity on the Aryl Hydrocarbon Receptor: Implications for Prevention of Dioxin Toxicity DP - 1999 Oct 01 TA - Molecular Pharmacology PG - 784--790 VI - 56 IP - 4 4099 - http://molpharm.aspetjournals.org/content/56/4/784.short 4100 - http://molpharm.aspetjournals.org/content/56/4/784.full SO - Mol Pharmacol1999 Oct 01; 56 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