Resveratrol has been reported to have hypolipidemic properties. We investigated whether resveratrol and its analogs: pterostilbene, piceatannol and resveratrol trimethyl ether, would activate the peroxisome proliferator-activated receptor alpha (PPARα) isoform. This nuclear receptor is proposed to mediate the activity of lipid-lowering drugs such as the fibrates. The four stilbenes and ciprofibrate (positive control) were evaluated for the activation of endogenous PPARα in H4IIEC3 cells transfected with a luciferase gene reporter construct. Pterostilbene demonstrated the highest induction of PPARα; the maximal response to pterostilbene was similar to that obtained with the hypolipidemic drug, ciprofibrate.