Jung Keun-Hwa, Chu Kon, Lee Soon-Tae, Kim Se-Jeong, Song Eun-Cheol, Kim Eun-Hee, Park Dong-Kyu, Sinn Dong-In, Kim Jeong-Min, Kim Manho, Roh Jae-Kyu
Stroke and Neural Stem Cell Laboratory, Department of Neurology, Clinical Research Institute, Seoul National University Hospital, 28, Yongon-Dong, Chongro-Gu, Seoul, 110-744, Republic of Korea.
J Pharmacol Exp Ther. 2007 Sep;322(3):1051-8. doi: 10.1124/jpet.107.120097. Epub 2007 May 30.
Angiotensin II exerts its central nervous system effects primarily via its receptors AT1 and AT2, and it participates in the pathogenesis of ischemia via AT1. The selective AT1 receptor blocker (ARB) is used in the hypertension treatment, and it exerts a variety of pleiotropic effects, including antioxidative, antiapoptotic, and anti-inflammatory effects. In this study, we investigated the therapeutic effect of the ARB telmisartan in experimental intracerebral hemorrhage (ICH) in normotensive rats. ICH was induced via the collagenase infusion or autologous blood injection. Either telmisartan at 30 mg/kg/dose or phosphate-buffered saline was orally administered 2 h after ICH induction. We evaluated hemorrhage volume, brain water content, and functional recovery, and we performed the histological analysis for terminal deoxynucleotidyl transferase dUTP nick-end labeling, leukocyte infiltration, and microglia activation. A variety of intracellular signals, in terms of oxidative stress, apoptotic molecules, and inflammatory mediators, were also measured. Telmisartan reduced hemorrhage volume, brain edema, and inflammatory or apoptotic cells in the perihematomal area. Telmisartan was noted to induce the expression of endothelial nitric-oxide synthase and peroxisome proliferator-activated receptor gamma and decrease oxidative stress, apoptotic signal, tumor necrosis factor-alpha, and cyclooxygenase-2 expression. The telmisartan-treated rats exhibited less pronounced neurological deficits and recovered better. Thus, telmisartan seems to offer neural protection, including antiapoptosis, anti-inflammatory, and antioxidant benefits in the intracerebral hemorrhage rat model.
血管紧张素II主要通过其受体AT1和AT2发挥中枢神经系统作用,并通过AT1参与缺血的发病机制。选择性AT1受体阻滞剂(ARB)用于治疗高血压,具有多种多效性作用,包括抗氧化、抗凋亡和抗炎作用。在本研究中,我们调查了ARB替米沙坦对正常血压大鼠实验性脑出血(ICH)的治疗效果。通过注入胶原酶或自体血注射诱导ICH。在诱导ICH后2小时口服给予30mg/kg剂量的替米沙坦或磷酸盐缓冲盐水。我们评估了出血量、脑含水量和功能恢复情况,并对末端脱氧核苷酸转移酶dUTP缺口末端标记、白细胞浸润和小胶质细胞活化进行了组织学分析。还测量了多种细胞内信号,包括氧化应激、凋亡分子和炎症介质。替米沙坦减少了血肿周围区域的出血量、脑水肿以及炎症或凋亡细胞。注意到替米沙坦可诱导内皮型一氧化氮合酶和过氧化物酶体增殖物激活受体γ的表达,并降低氧化应激、凋亡信号、肿瘤坏死因子-α和环氧化酶-2的表达。接受替米沙坦治疗的大鼠神经功能缺损较轻,恢复较好。因此,在脑出血大鼠模型中,替米沙坦似乎具有神经保护作用,包括抗凋亡、抗炎和抗氧化益处。