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內科學誌 Scopus

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篇名 Peroxisome Proliferator-Activated Receptors (PPARs)和活化劑(Agonists):文獻回顧
卷期 19:1
並列篇名 Peroxisome Proliferator-Activated Receptors (PPARs) and Agonists: Review of Literatures
作者 謝純岑楊宜瑱翁國昌黃建寧
頁次 14-26
關鍵字 過氧酶體增生活化接受器血管緊縮素接受器拮抗劑多重特異效果Peroxisome proliferator-activated receptorPPARFibratesThiazolidinedionesAngiotensin receptor antagonistsARBsPleiotropic effectsScopusTSCI
出刊日期 200802

中文摘要

肥胖症(obesity)和代謝症候群(metabolicsyndrome)已成爲一種流行病。由肥胖症和代謝 症候群所延伸出來的醫療問題,如跋島素阻抗(insulin resistance, IR )、糖尿病(Type 2 DM )、高血廛、高血脂症、心血管疾病等已造成龐大的醫療負擔,更是國人十大死亡原因的重要 危險因子。Peroxisome proliferator-activated receptors ( PPARs)是細胞核内接受器,主要參輿 脂質和葡萄糖的代謝。Fibrates和thiazolidinediones (TZDs)分別是市面上的PPAR a和PPAR r活化劑,是治療代謝症候群的利器。Fibrates可有效降低三酸甘油脂(TG)、升高高密度脂 蛋白膽固醇(HDL-C) : TZDs被証實可控制血糖、改善胰島素阻抗;兩者皆具備多重特異效 果(pleiotropic effects ),學理上和誠驗中發現可以改善發炎反應和血管功能,因而降低心血 管風險。最近也有一些雙重(dual) PPAR a I j 化劑(glitazars)進入了 phase III臨床減驗階 段。Glitazars截取PPAR a和PPAR T活化劑的療效,但也逃脱不離PPARs接受器的共同效 應(class effects of PPARs )。部分血管緊縮素接受器括抗劑(angiotensin receptor antagonists ARBs)近來被發現具備選擇性PPAR r調節活性(selective PPAR j modulation),可以治療代 謝症候群中多項成因。PPAR0/J是最近被熱烈研究的話題;它擁有除了 PPARa和PPAR T活性以外的特性。本文藉由整理一系列PPARs的相關文獻,提供讀者更進一步的了解。

英文摘要

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, hy-perlipidemia 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 PPAR a and PPAR r 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 PPAR a lj agonists, the glitazars have entered phase III clinical trials. Glitazars obtain the beneficial effects of PPAR ^ and PPAR j agonists, as well as the side effects of each PPAR due to class effects. Pan-P-PAR and selective PPAR j modulator (SPPAR j 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 j modulation activity, and can be used to treat multiple components of metabolic syndrome. PPAR (S16 has gained most interests recently because it has unique features other than the PPAR a and PPAR j activity. We here reviewed some of literatures and summarized them to the readers.

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