Peroxisome Proliferator-Activated Receptors (PPARs)和活化劑(agonists)：文獻回顧

Abstract

Obesity and metabolic syndrome are becoming an epidemic worldwide. The medical problems associated with obesity and metabolic syndrome, including insulin resistance, type 2 diabetes mellitus, hypertension, hyperlipidemia and cardiovascular disease have costed a huge medical financial burden. These are also the noxious members of the Taiwan top-ten leading causes of death. PPARs are intra-nuclear receptors. They act as regulators of lipid and glucose metabolism. Fibrates and thiazolidinediones (TZDs) are marketed PPARα and PPARγ agonist respectively, and are used in the treatment of metabolic syndrome. Fibrates lower serum triglycerides and increase HDL-cholesterol, while TZDs improve glycemic control and insulin resistance. Both ameliorate inflammation and improve vascular function, and have been proved to decrease cardiovascular risks. Recently, many dual PPARα/γ agonists, the glitazars have entered phase Ⅲ clinical trials. Glitazars obtain the beneficial effects of PPARα and PPARγ agonists, as well as the side effects of each PPAR due to class effects. Pan-PPAR and selective PPAR γ modulator (SPPARγ M) have also gained much attention in the literature; however their clinical applications still need further investigation. Angiotensin receptor antagonists (ARBs) have recently been found to posses selective PPAR γ modulation activity, and can be used to treat multiple components of metabolic syndrome. PPARβ/δ has gained most interests recently because it has unique features other than the PPARα and PPARγ activity. We here reviewed some of literatures and summarized them to the readers.