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Piceatannol and its parent compound, trans-resveratrol, decreased the in vitro catalytic activity of rat CYP1A1 and CYP1A2 by mixed inhibition. trans-Resveratrol was not a mechanism-based inactivator of rat CYP1A in vitro and the administration of this compound (50 mg/kg) to rats did not affect hepatic microsomal CYP1A-mediated enzyme activity.