Department of Biomedical Sciences, Pharmacology Division, College of Medicine, Al-Ahsa, King Faisal University, Saudi Arabia.
Eur J Pharmacol. 2010 Jul 10;637(1-3):162-70. doi: 10.1016/j.ejphar.2010.04.007. Epub 2010 Apr 23.
The protective effects of telmisartan, the angiotensin II-receptor antagonist, were investigated in rats with type 2 diabetes mellitus exposed to acute gastric ulceration. Following successful induction of diabetes, telmisartan treatment (1 mg/kg/day, orally) was started and continued for 8 weeks, after which acute gastric ulceration was induced by indomethacin. Telmisartan significantly attenuated the hyperglycemia and hypoinsulinemia in diabetic rats. Also, telmisartan significantly reduced the elevations of total gastric acid output, pepsin activity, gastric ulcer index and gastric mucosal tumor necrosis factor-alpha, nitric oxide, malondialdehyde and caspase-3 activity, and restored the depleted antioxidant defenses (reduced glutathione level, and superoxide dismutase and catalase activities) caused by indomethacin administration in diabetic rats. Histopathological gastric tissue damage induced by indomethacin in diabetic rats was ameliorated by telmisartan treatment. Immunohistochemical analysis revealed that telmisartan markedly attenuated the reduction in insulin content of pancreatic islet beta-cells, and prevented the indomethacin-induced overexpression of inducible nitric oxide synthase and nuclear factor-kappaB in gastric mucosa of diabetic rats. It was concluded that telmisartan represents a potential therapeutic option to reduce the risk of gastric ulceration induced by nonsteroidal anti-inflammatory drugs in type 2 diabetic patients.
替米沙坦,血管紧张素 II 受体拮抗剂,在 2 型糖尿病大鼠急性胃溃疡模型中的保护作用。成功诱导糖尿病后,开始给予替米沙坦(1mg/kg/天,口服)治疗,并持续 8 周,然后用吲哚美辛诱导急性胃溃疡。替米沙坦显著减轻了糖尿病大鼠的高血糖和胰岛素血症。此外,替米沙坦还显著降低了总胃酸分泌量、胃蛋白酶活性、胃溃疡指数和胃黏膜肿瘤坏死因子-α、一氧化氮、丙二醛和半胱氨酸天冬氨酸蛋白酶-3 的活性,并恢复了吲哚美辛给药引起的糖尿病大鼠抗氧化防御能力的降低(还原型谷胱甘肽水平和超氧化物歧化酶和过氧化氢酶活性)。替米沙坦治疗改善了糖尿病大鼠由吲哚美辛引起的胃组织损伤的组织病理学变化。免疫组化分析显示,替米沙坦显著减轻了胰岛β细胞胰岛素含量的降低,并阻止了吲哚美辛诱导的糖尿病大鼠胃黏膜中诱导型一氧化氮合酶和核因子-κB 的过度表达。结论是,替米沙坦可能是减少 2 型糖尿病患者非甾体类抗炎药引起的胃溃疡风险的一种潜在治疗选择。