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PPAR Research
Volume 2012, Article ID 858352, 7 pages
Review Article

Nutraceuticals as Ligands of PPAR

1Division of Nutrition, BFLSON and Health Professions, Urban Life Building, 140 Decatur Street, Suite 862, Atlanta, GA 30303, USA
2Department of Pharmacology, Physiology and Toxicology, Joan C Edwards School of Medicine, Marshall University, One John Marshall Drive, Huntington, WV 25755, USA

Received 27 February 2012; Revised 10 April 2012; Accepted 13 April 2012

Academic Editor: Christopher J. Nicol

Copyright © 2012 Meera Penumetcha and Nalini Santanam. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.


Peroxisome proliferator-activated receptors (PPARs) are ligand-activated nuclear receptors that respond to several exogenous and endogenous ligands by modulating genes related to lipid, glucose, and insulin homeostasis. PPARγ, expressed in adipose tissue and liver, regulates lipid storage and glucose metabolism and is the target of type 2 diabetes drugs, thiazolidinediones (TZDs). Due to high levels of toxicity associated with the first generation TZDs, troglitazone (Rezulin), rosiglitazone (Avandia), and pioglitazone (Actos), there is a renewed search for newer PPAR drugs that exhibit better efficacy but lesser toxicity. In recent years, there has been a definite increase in the consumption of dietary supplements among diabetics, due to the possible health benefits associated with these nutraceutical components. With this impetus, investigations into alternative natural ligands of PPARs has also risen. This review highlights some of the dietary compounds (dietary lipids, isoflavones, and other flavanoids) that bind and transactivate PPARγ. A better understanding of the physiological effects of this PPAR activation by nutraceuticals and the availability of high-throughput technologies should lead to the discovery of less toxic alternatives to the PPAR drugs currently on the market.