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Antioxidant as an Effective Lipid-Lowering Drug

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Resveratrol, a stilbenoid antioxidant found in grapes, wine, peanuts and other berries, has been reported to have hypolipidemic properties. Researchers at the Agricultural Research Services Mid-South Region investigated whether resveratrol and its three analogs (pterostilbene, piceatannol and resveratrol trimethyl ether) would activate the peroxisome proliferator-activated receptor alpha (PPAR.alpha.) isoform.

This nuclear receptor is proposed to mediate the activity of lipid-lowering drugs such as the fibrates. The four stilbenes were

evaluated along with ciprofibrate (positive control) at 1, 10, 100, 300 .mu.M concentrations for the activation of endogenous PPAR.alpha. in H4IIEC3 cells. Cells were transfected with a peroxisome proliferator response element-AB (rat fatty acyl CoA .beta.-oxidase response element)--luciferase gene reporter construct. Of the four analogs, pterostilbene demonstrated the highest induction of PPAR.alpha., showing 7- and 9-14 fold increases in luciferase activity at 100 and 300 .mu.M, respectively, relative to control. The maximal luciferase activity

responses to pterostilbene at 100 .mu.M are similar to those obtained with the hypolipidemic drug ciprofibrate. These results suggest that pterostilbene acts as a PPAR.alpha. agonist, like that of the fibrate class, and may be a more effective hypolipidemic agent than resveratrol.

For more information, visit http://www.ars.usda.gov/research/patents/patents.htm?serialnum=11207038.

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