Docket Number: 16204
Serial Number: 11207038

Summary: Resveratrol, a stilbenoid antioxidant found in grapes, wine, peanuts and other berries, has been reported to have hypolipidemic properties. We 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. Patent Status: Patent Application Filed on August 18, 2005 . Link at USPTO filed under patent title “Pterostilbene as a new agonist for the peroxisome proliferator-activated receptor alpha isoform.” Inventors: Agnes M Rimando Natural Products Utilization Research UNIVERSITY AVENUE UNIVERSITY, MS, 38677 Phone: (662) 915-1037 Fax: (662) 915-1035 agnes.rimando@ars.usda.gov Dennis Feller University of Mississippi Wallace Yokoyama Processed Foods Research USDA, ARS, PWA, WRRC-PFR 800 BUCHANAN STREET ALBANY, CA, 94710 Phone: (510) 559-5695 Fax: (510) 559-5777 wally.yokoyama@ars.usda.gov