Chen Bao-Ying, Qu Ping, Tie Ru, Zhu Miao-Zhang, Zhu Xiao-Xing, Yu Jun
Department of Radiology, Tangdu Hospital, Fourth Military Medical University, Xi'an, Shaanxi, China.
Regul Pept. 2010 Sep 24;164(2-3):139-43. doi: 10.1016/j.regpep.2010.06.007. Epub 2010 Jul 7.
In order to investigate the effects of vasonatrin peptide (VNP), a novel man-made natriuretic peptide, on liver fibrosis, mice received carbon tetrachloride (CCl(4)) injection for 12weeks and with or without VNP treatment during the last 6weeks. Hematoxylin-eosin (HE) staining and Sirius red staining were performed to evaluate the status of liver fibrosis. After treatment of VNP, DNA and collagen synthesis of cultured HSC-T6 hepatic stellate cells were assessed by [(3)H]-thymidine and [(3)H]-proline incorporation, respectively. Additionally, involved signaling pathway was identified by radioimmunoassay to detect the levels of intracellular cGMP and by mimicking experiments using 8-br-cGMP (a membrane-permeable cGMP analog). Also, blocking experiments were performed using HS-142-1, an antagonist of guanylyl cyclase-coupled natriuretic peptide receptor (NPR), or KT-5823, the cGMP-dependent protein kinase (PKG) inhibitor. As a result, VNP markedly alleviated CCl(4)-induced liver fibrosis in mice. In vitro, HSC-T6 cells demonstrated a dose-dependent reduction of DNA and collagen synthesis in the presence VNP. In addition, VNP significantly increased the intracellular levels of cGMP. These effects of VNP were mimicked by 8-br-cGMP, although inhibited by HS-142-1 or KT-5823. Taken together, VNP ameliorates liver fibrosis by inhibiting collagen production from hepatic stellate cells via guanylyl cyclase-coupled NPR/cGMP/PKG pathway, indicating that VNP might be a new effective reagent in the treatment of liver fibrosis.
为了研究新型人造利钠肽血管钠肽(VNP)对肝纤维化的影响,小鼠接受四氯化碳(CCl₄)注射12周,并在最后6周接受或不接受VNP治疗。进行苏木精-伊红(HE)染色和天狼星红染色以评估肝纤维化状态。VNP治疗后,分别通过[³H] - 胸腺嘧啶核苷和[³H] - 脯氨酸掺入评估培养的HSC - T6肝星状细胞的DNA和胶原合成。此外,通过放射免疫测定法检测细胞内cGMP水平,并使用8 - br - cGMP(一种可透过细胞膜的cGMP类似物)进行模拟实验来鉴定相关信号通路。同时,使用鸟苷酸环化酶偶联利钠肽受体(NPR)拮抗剂HS - 142 - 1或cGMP依赖性蛋白激酶(PKG)抑制剂KT - 5823进行阻断实验。结果显示,VNP显著减轻了CCl₄诱导的小鼠肝纤维化。在体外,VNP存在时HSC - T6细胞的DNA和胶原合成呈剂量依赖性降低。此外,VNP显著提高了细胞内cGMP水平。VNP的这些作用可被8 - br - cGMP模拟,但被HS - 142 - 1或KT - 5823抑制。综上所述,VNP通过鸟苷酸环化酶偶联的NPR/cGMP/PKG途径抑制肝星状细胞的胶原生成,从而改善肝纤维化,表明VNP可能是治疗肝纤维化的一种新型有效药物。