Wang Yi-Xin, da Cunha Valdeci, Martin-McNulty Baby, Vincelette Jon, Li Weiwei, Choy David F, Halks-Miller Meredith, Mahmoudi Mithra, Schroeder Miriam, Johns Anthony, Light David R, Dole William P
Department of Pharmacology, Berlex Biosciences, 2600 Hilltop Drive, Richmond, CA 94804, USA.
Eur J Pharmacol. 2005 Apr 11;512(2-3):215-22. doi: 10.1016/j.ejphar.2005.02.024.
Recent evidence indicates that the GTPase activated Rho/Rho-kinase pathway contributes angiotensin II-induced cardiac hypertrophy and vascular remodeling. We tested this hypothesis in vivo by determining the effects of fasudil, a Rho-kinase inhibitor, on angiotensin II-induced cardiac hypertrophy, coronary vascular remodeling, and ventricular dysfunction. Six-month-old apolipoprotein E deficient (apoE-KO) mice were subcutaneously infused with angiotensin II (1.44 mg/kg/day) using an osmotic mini-pump. Mice were randomly assigned to either vehicle or fasudil (136 or 213 mg/kg/day in drinking water) group. Infusion of angiotensin II for 4 weeks resulted in cardiac enlargement, myocyte hypertrophy, and myocardial interstitial and coronary artery perivascular fibrosis. These changes were accompanied by reduced aortic flow velocity and acceleration rate. Cardiac gene expression levels of atrial natriuretic peptide (ANP) and collagen type III detected by real-time reverse transcriptase polymerase chain reaction were significantly increased in angiotensin II-infused mice. Treatment with fasudil dose-dependently attenuated angiotensin II-induced cardiac hypertrophy, prevented perivascular fibrosis, blunted the increase in ANP and collagen type III expression, and improved cardiac function, without changing blood pressure. These data are consistent with a role for Rho-kinase activation in angiotensin II-induced cardiac remodeling and vascular wall fibrosis.
最近的证据表明,GTP酶激活的Rho/Rho激酶信号通路参与了血管紧张素II诱导的心脏肥大和血管重塑。我们通过确定Rho激酶抑制剂法舒地尔对血管紧张素II诱导的心脏肥大、冠状动脉血管重塑和心室功能障碍的影响,在体内验证了这一假设。使用渗透微型泵给6月龄载脂蛋白E缺陷(apoE-KO)小鼠皮下输注血管紧张素II(1.44 mg/kg/天)。小鼠被随机分为溶剂对照组或法舒地尔组(饮用水中浓度为136或213 mg/kg/天)。血管紧张素II输注4周导致心脏增大、心肌细胞肥大、心肌间质和冠状动脉血管周围纤维化。这些变化伴随着主动脉血流速度和加速度的降低。通过实时逆转录聚合酶链反应检测,血管紧张素II输注小鼠的心房利钠肽(ANP)和III型胶原蛋白的心脏基因表达水平显著升高。法舒地尔治疗剂量依赖性地减轻了血管紧张素II诱导的心脏肥大,预防了血管周围纤维化,抑制了ANP和III型胶原蛋白表达的增加,并改善了心脏功能,而不改变血压。这些数据与Rho激酶激活在血管紧张素II诱导的心脏重塑和血管壁纤维化中的作用一致。