Su Xuesong, Yu Rui, Yang Xu, Zhou Guangyu, Wang Yanqiu, Li Li, Li Detian
Department of Nephrology, Shengjing Hospital of China Medical University, Shenyang, China.
Clin Exp Pharmacol Physiol. 2015 Jun;42(6):671-9. doi: 10.1111/1440-1681.12403.
Peritoneal dialysis (PD) is an effective treatment for patients with end-stage renal diseases, but long-term continuous PD causes peritoneal fibrosis (PF). This study aims to evaluate the anti-fibrotic effect of telmisartan on a rat model of PF and to investigate the underlying mechanisms. Five-sixths kidney nephrectomy and PD were used to establish the PF rat model. Glucose (2.5%) was used to establish an in vitro model in rat peritoneal mesothelial cells (PMC). Haematoxylin-eosin staining was used to examine the structural alterations. Masson's trichrome staining was used to observe the tissue fibrosis in peritoneal membrane of rats. Real-time polymerase chain reaction was used to measure messenger RNA expressions of profibrotic factors. Western blotting was used to determine protein expressions of profibrotic factors, peroxisome proliferator-activated receptor-γ, and mitogen-activated protein kinases (MAPK). Results demonstrated that administration of telmisartan dose-dependently attenuated the thickening of the peritoneal membrane and the fibrosis induced by long-term PD fluid exposure in rats. In addition, telmisartan treatment inhibited the upregulation of profibrotic factors induced by PD in the peritoneum of rats and by high-concentration glucose in PMC. Telmisartan was also effective in inhibiting PD and high-concentration, glucose-induced phosphorylation of MAPK in the peritoneum and PMC. Furthermore, peroxisome proliferator-activated receptor-γ (PPARγ) inhibitor GW9662 blocked these protective effects of telmisartan in PMC. The results suggest that telmisartan is effective in attenuating PD-induced PF, and this effect may be associated with the inhibition of profibrotic factor expression and MAPK phosphorylation via PPARγ activation.
腹膜透析(PD)是终末期肾病患者的一种有效治疗方法,但长期持续腹膜透析会导致腹膜纤维化(PF)。本研究旨在评估替米沙坦对PF大鼠模型的抗纤维化作用,并探讨其潜在机制。采用六分之五肾切除和腹膜透析建立PF大鼠模型。用2.5%葡萄糖建立大鼠腹膜间皮细胞(PMC)的体外模型。苏木精-伊红染色用于检查结构改变。Masson三色染色用于观察大鼠腹膜的组织纤维化。实时聚合酶链反应用于测量促纤维化因子的信使核糖核酸表达。蛋白质印迹法用于测定促纤维化因子、过氧化物酶体增殖物激活受体-γ和丝裂原活化蛋白激酶(MAPK)的蛋白表达。结果表明,替米沙坦给药可剂量依赖性减轻大鼠长期腹膜透析液暴露所致的腹膜增厚和纤维化。此外,替米沙坦治疗可抑制腹膜透析在大鼠腹膜和高浓度葡萄糖在PMC中诱导的促纤维化因子上调。替米沙坦还可有效抑制腹膜透析和高浓度葡萄糖诱导的腹膜和PMC中MAPK的磷酸化。此外,过氧化物酶体增殖物激活受体-γ(PPARγ)抑制剂GW9662可阻断替米沙坦在PMC中的这些保护作用。结果表明,替米沙坦可有效减轻腹膜透析诱导的PF,且这种作用可能与通过激活PPARγ抑制促纤维化因子表达和MAPK磷酸化有关。