Effects of ETP-508, a novel endothelin receptor antagonist, on bleomycin-induced pulmonary fibrosis in rats
AIM: To investigate the effects of ETP-508, a novel endothelin receptor antagonist, on bleomycin (BLM) -induced pulmonary fibrosis in rats. METHODS: Rats were divided into 4 groups: BLM group, ETP-508 group, dexamethasone group and control group. Pulmonary fibrosis was induced by endotracheal injection of bleomycin (5 mg/kg). ETP508 group was treated with intraperitoneal injection of ETP-508 (100 μg/kg, every other day), dexamelhasone group was treated with intraperitoneal injection of dexamethasone (1 mg/kg, every other day) and BLM model group and control group were treated with saline. At the 28th day, the rats were executed and the concentrations of ET-1 and hydroxyproline (HYP) in lung tissues were determined. Histopathological examination was conducted. RESULTS: HYP concentrations in BLM group were significantly higher than those of the other groups and histopathological examination showed fibrosis. ET-1 concentrations of BLM group were significantly higher than those of control group and dexamethasone group (P ＜ 0.01). ET-1 concentrations in ETP508 group were higher than those of other groups, with significant differences from those in control group and dexamethasone group(P ＜ 0.01, respectively) and BLM group (P ＜ 0.05). There were no significant differences between control group and dexamethasone group (P ＞ 0.05). CONCLUSION: ETP-508, a novel endothelin receptor antagonist, has restraining effects on the pulmonary fibrosis formation, which may result from the prevention of the banding of ET-1 and endothelin receptor.
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万方数据
维普
