Department of Pharmacology, College of Medicine, University of Tennessee Health Science Center, Memphis, Tennessee 38163, USA.
Am J Physiol Heart Circ Physiol. 2010 Dec;299(6):H1891-901. doi: 10.1152/ajpheart.00655.2010. Epub 2010 Sep 17.
Reactive oxygen species (ROS) contribute to various models of hypertension, including deoxycorticosterone acetate (DOCA)-salt-induced hypertension. Recently, we have shown that ROS, generated by cytochrome P-450 1B1 (CYP1B1) from arachidonic acid, mediate vascular smooth muscle cell growth caused by angiotensin II. This study was conducted to determine the contribution of CYP1B1 to hypertension and associated pathophysiological changes produced by DOCA (30 mg/kg) given subcutaneously per week with 1% NaCl + 0.1% KCl in drinking water to uninephrectomized rats for 6 wk. DOCA-salt treatment increased systolic blood pressure (SBP). Injections of the selective inhibitor of CYP1B1, 2,3',4,5'-tetramethoxystilbene (TMS; 300 μg/kg ip every 3rd day) initiated at the 4th week of DOCA-salt treatment normalized SBP and decreased CYP1B1 activity but not its expression in the aorta, heart, and kidney. TMS also inhibited cardiovascular and kidney hypertrophy, prevented the increase in vascular reactivity and endothelial dysfunction, and minimized the increase in urinary protein and K(+) output and the decrease in urine osmolality, Na(+) output, and creatinine clearance associated with DOCA-salt treatment. These pathophysiological changes caused by DOCA-salt treatment and associated increase in vascular superoxide production, NADPH oxidase activity, and expression of NOX-1, and ERK1/2 and p38 MAPK activities in the aorta, heart, and kidney were inhibited by TMS. These data suggest that CYP1B1 contributes to DOCA-salt-induced hypertension and associated pathophysiological changes, most likely as a result of increased ROS production and ERK1/2 and p38 MAPK activity, and could serve as a novel target for the development of agents like TMS to treat hypertension.
活性氧(ROS)参与了包括脱氧皮质酮醋酸盐(DOCA)-盐诱导的高血压在内的各种高血压模型。最近,我们已经表明,来自花生四烯酸的细胞色素 P-450 1B1(CYP1B1)产生的 ROS 介导了血管平滑肌细胞生长,这种生长是由血管紧张素 II 引起的。本研究旨在确定 CYP1B1 在 DOCA(30mg/kg)皮下注射和含 1%NaCl+0.1%KCl 的饮用水联合应用于单侧肾切除大鼠 6 周后引起的高血压和相关病理生理改变中的作用。DOCA-盐处理增加了收缩压(SBP)。在 DOCA-盐处理的第 4 周开始,用 CYP1B1 的选择性抑制剂 2,3',4,5'-四甲氧基二苯乙烯(TMS;300μg/kg 每 3 天腹腔注射)进行注射,使 SBP 正常化,并降低了 CYP1B1 活性,但不降低主动脉、心脏和肾脏中的 CYP1B1 表达。TMS 还抑制了心血管和肾脏肥大,防止了血管反应性和内皮功能障碍的增加,并最大限度地减少了与 DOCA-盐处理相关的尿蛋白和 K+排泄增加以及尿渗透压、Na+排泄和肌酐清除率降低。这些由 DOCA-盐处理引起的病理生理变化,以及由此导致的血管超氧化物产生、NADPH 氧化酶活性以及主动脉、心脏和肾脏中 NOX-1、ERK1/2 和 p38 MAPK 活性的增加,都被 TMS 抑制。这些数据表明,CYP1B1 参与了 DOCA-盐诱导的高血压和相关的病理生理变化,很可能是由于 ROS 产生增加以及 ERK1/2 和 p38 MAPK 活性增加所致,并且可能成为像 TMS 这样的药物治疗高血压的新型靶点。