Iyer Abishek, Kauter Kathleen, Alam Md Ashraful, Hwang Sung Hee, Morisseau Christophe, Hammock Bruce D, Brown Lindsay
School of Biomedical Sciences, The University of Queensland, Brisbane, QLD, Australia.
Exp Diabetes Res. 2012;2012:758614. doi: 10.1155/2012/758614. Epub 2011 Oct 10.
The signs of metabolic syndrome following chronic excessive macronutrient intake include body weight gain, excess visceral adipose deposition, hyperglycaemia, glucose and insulin intolerances, hypertension, dyslipidaemia, endothelial damage, cardiovascular hypertrophy, inflammation, ventricular contractile dysfunction, fibrosis, and fatty liver disease. Recent studies show increased activity of soluble epoxide hydrolase (sEH) during obesity and metabolic dysfunction. We have tested whether sEH inhibition has therapeutic potential in a rat model of diet-induced metabolic syndrome. In these high-carbohydrate, high-fat-fed rats, chronic oral treatment with trans-4-[4-(3-adamantan-1-ylureido)-cyclohexyloxy]-benzoic acid (t-AUCB), a potent sEH inhibitor, alleviated the signs of metabolic syndrome in vivo including glucose, insulin, and lipid abnormalities, changes in pancreatic structure, increased systolic blood pressure, cardiovascular structural and functional abnormalities, and structural and functional changes in the liver. The present study describes the pharmacological responses to this selective sEH inhibitor in rats with the signs of diet-induced metabolic syndrome.
长期过量摄入大量营养素后代谢综合征的体征包括体重增加、内脏脂肪过度沉积、高血糖、葡萄糖和胰岛素不耐受、高血压、血脂异常、内皮损伤、心血管肥大、炎症、心室收缩功能障碍、纤维化和脂肪肝病。最近的研究表明,肥胖和代谢功能障碍期间可溶性环氧化物水解酶(sEH)的活性增加。我们已经测试了sEH抑制在饮食诱导的代谢综合征大鼠模型中是否具有治疗潜力。在这些高碳水化合物、高脂肪喂养的大鼠中,用强效sEH抑制剂反式-4-[4-(3-金刚烷-1-基脲基)-环己氧基]-苯甲酸(t-AUCB)进行慢性口服治疗,可在体内减轻代谢综合征的体征,包括葡萄糖、胰岛素和脂质异常、胰腺结构变化、收缩压升高、心血管结构和功能异常以及肝脏的结构和功能变化。本研究描述了对具有饮食诱导的代谢综合征体征的大鼠使用这种选择性sEH抑制剂的药理反应。