Department of Clinical Pharmacology, Division of Pathological Sciences, Kyoto Pharmaceutical University, Kyoto, Japan.
Eur J Pharmacol. 2011 Apr 10;656(1-3):81-7. doi: 10.1016/j.ejphar.2011.01.043. Epub 2011 Feb 4.
Recombinant human erythropoietin (rHuEPO), used clinically for renal anemia, reportedly exhibits pleiotropic properties in various tissues. To test whether it ameliorates vascular injury, rHuEPO (75U/kg) was administered subcutaneously every 3days for 10days to 5/6 nephrectomized hypertensive rats (5/6Nx) treated with 1% NaCl. rHuEPO had no effect on increased systolic blood pressure or decreased hematocrit values, but normalized levels of proteinuria and creatinine clearance. Vasodilation in response to acetylcholine in the aortic ring was impaired in the 5/6Nx, and improved by treatment with rHuEPO. Immunohistochemical analysis revealed that the infiltration of adventitial areas by macrophages and expression of osteopontin were enhanced in the 5/6Nx aorta and the overexpression was suppressed by rHuEPO. rHuEPO also attenuated medial hyperplasia. Akt signaling was activated by the increased expression of phosphorylated Akt and GSK-3β in aorta from rHuEPO-treated 5/6Nx. rHuEPO restored plasma NOx (NO(2)(-)+NO(3)(-)) levels and endothelial nitric oxide synthase (eNOS) content in the 5/6Nx aorta. Treatment with an eNOS substrate, l-arginine, which caused a similar increase in plasma NOx levels as the rHuEPO treatment, resulted in a normalization of endothelial dysfunction and vascular inflammation. These results suggest that a low dose of rHuEPO exerted vasoprotective effects in rats with hypertensive renal failure.
重组人促红细胞生成素(rHuEPO)临床上用于治疗肾性贫血,据报道在各种组织中具有多种作用。为了验证其是否能改善血管损伤,将 rHuEPO(75U/kg)皮下注射,每 3 天一次,共 10 天,用于治疗 5/6 肾切除高血压大鼠(5/6Nx),同时给予 1%NaCl。rHuEPO 对增加的收缩压或降低的红细胞压积值没有影响,但使蛋白尿和肌酐清除率正常化。5/6Nx 主动脉对乙酰胆碱的血管舒张反应受损,rHuEPO 治疗可改善这种反应。免疫组织化学分析显示,5/6Nx 主动脉中血管外膜区域的巨噬细胞浸润和骨桥蛋白的表达增强,rHuEPO 可抑制其过表达。rHuEPO 还可减轻中膜增生。rHuEPO 治疗的 5/6Nx 主动脉中磷酸化 Akt 和 GSK-3β 的表达增加,激活 Akt 信号。rHuEPO 恢复了 5/6Nx 血浆中一氧化氮合酶(eNOS)的表达和内皮型一氧化氮合酶(NOx)水平。eNOS 底物 l-精氨酸的治疗可使血浆 NOx 水平升高,与 rHuEPO 治疗相似,导致内皮功能障碍和血管炎症正常化。这些结果表明,低剂量 rHuEPO 对高血压肾衰竭大鼠具有血管保护作用。