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双重PPARα/γ激动剂替格列扎改善非糖尿病患者的餐后脂质代谢和糖耐量。

Improvement of postprandial lipid handling and glucose tolerance in a non-diabetic population by the dual PPARalpha/gamma agonist, tesaglitazar.

作者信息

Fagerberg Bjorn, Schuster Herbert, Birketvedt Grethe Støa, Tonstad Serena, Ohman Karl Peter, Gause-Nilsson Ingrid

机构信息

Wallenberg Laboratory for Cardiovascular Research, Sahlgrenska University Hospital, 41345 Göteborg, Sweden.

出版信息

Diab Vasc Dis Res. 2007 Sep;4(3):174-80. doi: 10.3132/dvdr.2007.038.

DOI:10.3132/dvdr.2007.038
PMID:17907107
Abstract

This study examined the effect of tesaglitazar (GALIDA), a dual peroxisome proliferator-activated receptor (PPAR)alpha/gamma agonist, on postprandial metabolism. This investigation was part of the Study in Insulin Resistance (SIR) (SH-SBT-0001), a randomised, double-blind, placebo-controlled study that reported improvements in fasting lipid and glucose values with tesaglitazar (0.1, 0.25, 0.5 or 1 mg once daily for 12 weeks) in hypertriglyceridaemic, abdominally obese, non-diabetic patients. A subgroup of 222 patients underwent postprandial lipid and glucose testing at baseline and treatment end. Tesaglitazar 0.25, 0.5 and 1 mg reduced postprandial area under the curve (AUC) for triglycerides by 20% (p=0.003), 30% (p<0.0001) and 41% (p<0.0001), respectively. Free fatty acid (FFA) levels were reduced by 17% with tesaglitazar 0.5 mg (p=0.002) and by 29% with tesaglitazar 1 mg (p<0.0001). Tesaglitazar significantly improved glucose tolerance and increased the proportion of patients with normal glucose tolerance as measured by the oral glucose tolerance test (OGTT). To conclude, postprandial dyslipidaemia and hyperglycaemia, indicators of increased vascular risk, were significantly improved by tesaglitazar treatment in these non-diabetic, hypertriglyceridaemic, abdominally obese subjects.

摘要

本研究考察了双过氧化物酶体增殖物激活受体(PPAR)α/γ激动剂替格列扎(GALIDA)对餐后代谢的影响。该调查是胰岛素抵抗研究(SIR)(SH-SBT-0001)的一部分,这是一项随机、双盲、安慰剂对照研究,报告称替格列扎(0.1、0.25、0.5或1毫克,每日一次,共12周)可改善高甘油三酯血症、腹型肥胖、非糖尿病患者的空腹血脂和血糖值。222名患者的亚组在基线和治疗结束时接受了餐后血脂和血糖检测。0.25毫克、0.5毫克和1毫克的替格列扎分别使甘油三酯的餐后曲线下面积(AUC)降低了20%(p=0.003)、30%(p<0.0001)和41%(p<0.0001)。0.5毫克的替格列扎使游离脂肪酸(FFA)水平降低了17%(p=0.002),1毫克的替格列扎使游离脂肪酸水平降低了29%(p<0.0001)。替格列扎显著改善了糖耐量,并增加了通过口服葡萄糖耐量试验(OGTT)测量的糖耐量正常患者的比例。总之,在这些非糖尿病、高甘油三酯血症、腹型肥胖受试者中,替格列扎治疗显著改善了餐后血脂异常和高血糖,而餐后血脂异常和高血糖是血管风险增加的指标。

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Improvement of postprandial lipid handling and glucose tolerance in a non-diabetic population by the dual PPARalpha/gamma agonist, tesaglitazar.双重PPARα/γ激动剂替格列扎改善非糖尿病患者的餐后脂质代谢和糖耐量。
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[Peroxisome proliferator-activated receptor α/γ agonist tesaglitazar stabilizes atherosclerotic plaque in diabetic low density lipoprotein receptor knockout mice].[过氧化物酶体增殖物激活受体α/γ激动剂替格列扎能稳定糖尿病低密度脂蛋白受体敲除小鼠的动脉粥样硬化斑块]
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引用本文的文献

1
The PPAR α / γ Agonist, Tesaglitazar, Improves Insulin Mediated Switching of Tissue Glucose and Free Fatty Acid Utilization In Vivo in the Obese Zucker Rat.过氧化物酶体增殖物激活受体α/γ激动剂替格列扎改善肥胖 Zucker 大鼠体内胰岛素介导的组织葡萄糖和游离脂肪酸利用的转换。
PPAR Res. 2013;2013:305347. doi: 10.1155/2013/305347. Epub 2013 Oct 27.
2
Dual PPAR α / γ Agonism Normalizes Lipoprotein Profile of Renal Dyslipidemia.双重过氧化物酶体增殖物激活受体α/γ激动剂可使肾脏脂代谢紊乱的脂蛋白谱正常化。
PPAR Res. 2013;2013:391628. doi: 10.1155/2013/391628. Epub 2013 Mar 28.