Olukman Murat, Sezer Ebru Demirel, Ulker Sibel, Sözmen Eser Y, Cınar Gülcihan Mehtap
Department of Medical Pharmacology, Faculty of Medicine, Ege University, Bornova, 35100 İzmir, Turkey.
Exp Diabetes Res. 2010;2010:828531. doi: 10.1155/2010/828531. Epub 2010 Dec 27.
Diabetic endothelial dysfunction is accompanied by increased oxidative stress and upregulated proinflammatory and inflammatory mediators in the vasculature. Activation of peroxisome proliferator-activated receptor-alpha (PPAR-α) results in antioxidant and anti-inflammatory effects. This study was designed to investigate the effect of fenofibrate, a PPAR-α activator, on the endothelial dysfunction, oxidative stress, and inflammation in streptozotocin diabetic rats. Diabetic rats received fenofibrate (150 mg kg(-1) day(-1)) for 4 weeks. Fenofibrate treatment restored the impaired endothelium-dependent relaxation and increased basal nitric oxide availability in diabetic aorta, enhanced erythrocyte/liver superoxide dismutase and catalase levels, ameliorated the abnormal serum/aortic thiobarbituric acid reactive substances, and prevented the increased aortic myeloperoxidase without a significant change in serum total cholesterol and triglyceride levels. It did not affect the decreased total homocysteine level and the increased tumor necrosis factor-α level in the serum of diabetic rats. Fenofibrate-induced prevention of the endothelial function seems to be related to its potential antioxidant and antiinflammatory activity.
糖尿病性内皮功能障碍伴随着血管中氧化应激增加以及促炎和炎症介质上调。过氧化物酶体增殖物激活受体-α(PPAR-α)的激活会产生抗氧化和抗炎作用。本研究旨在探讨PPAR-α激活剂非诺贝特对链脲佐菌素诱导的糖尿病大鼠内皮功能障碍、氧化应激和炎症的影响。糖尿病大鼠接受非诺贝特(150 mg kg⁻¹ 天⁻¹)治疗4周。非诺贝特治疗恢复了糖尿病主动脉中受损的内皮依赖性舒张功能,并增加了基础一氧化氮的可用性,提高了红细胞/肝脏超氧化物歧化酶和过氧化氢酶水平,改善了血清/主动脉中异常的硫代巴比妥酸反应性物质,并防止了主动脉髓过氧化物酶增加,而血清总胆固醇和甘油三酯水平无显著变化。它对糖尿病大鼠血清中降低的总同型半胱氨酸水平和升高的肿瘤坏死因子-α水平没有影响。非诺贝特诱导的内皮功能保护作用似乎与其潜在的抗氧化和抗炎活性有关。