Rho kinase inhibition activity of pinocembrin in rat aortic rings contracted by angiotensin II
Rho kinase inhibition activity of pinocembrin in rat aortic rings contracted by angiotensin II
复制标题
松香素对血管紧张素II收缩大鼠主动脉环的Rho激酶抑制活性
DOI：
10.3724/sp.j.1009.2013.00258
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发表时间：
2013-05-01
影响因子：
4.6
通讯作者：
Du Guan-Hua
中科院分区：
文献类型：
--
作者：
Li Li;Yang Hai-Guang;Du Guan-Hua
目的：研究松属素对血管紧张素II（Ang II）诱导的血管收缩的影响，并探讨其作用的分子机制。方法：在内皮剥脱的大鼠胸主动脉环上测定等长血管张力。用Western blot分析测定肌球蛋白磷酸酶靶单位1（MYPT 1）的磷酸化水平、Rho激酶1（ROCK 1、ROK β或p160 ROCK）和血管紧张素II 1型受体（AT（1）R）的蛋白水平。结果：Pinocembrin对Ang Ⅱ（100 nmol.l（-1））收缩的去内皮主动脉环有舒张作用，且呈剂量依赖性。在血管紧张素II刺激的内皮剥脱的主动脉环中，用松属素（25和100 μ mol.l（-1））预处理20分钟显著减弱MYPT 1磷酸化和ROCK 1蛋白水平。同时，松属素对血管紧张素Ⅱ诱导的大鼠主动脉环AT（1）R蛋白水平无影响。结论：这些结果表明，松属素抑制血管紧张素II诱导的大鼠内皮剥脱的主动脉环的血管收缩，其机制至少部分是由于RhoA/ROCK通路的阻断。
AIM: To investigate the effects of pinocembrin on angiotensin II (Ang II)-induced vascular contraction, and to explore its molecular mechanism of actions. METHODS: The isometric vascular tone was measured in rat thoracic aortic rings with denuded endothelium. Phosphorylation level of myosin phosphatase target unit 1 (MYPT1), and protein levels of Rho kinase 1 (ROCK1, ROK beta or p160ROCK) and angiotensin II type-1 receptor (AT(1)R) were determined by Western blot analysis. RESULTS: Pinocembrin produced a relaxant effect on endothelium-denuded aortic rings contracted by Ang II (100 nmol.l(-1)) in a dose-dependent manner. In endothelium-denuded aortic rings stimulated by Ang II, pretreatment with pinocembrin (25 and 100 mu mol.l(-1)) for 20 min significantly attenuated MYPT1 phosphorylation and ROCK1 protein levels. Meanwhile, the protein level of AT(1)R in response to Ang II was not affected by pinocembrin in rat aortic rings. CONCLUSION: These findings indicate that pinocembrin inhibits vasoconstriction induced by Ang II in rat endothelium-denuded aortic rings, and the mechanism at least in part, is due to the blockade of the RhoA/ROCK pathway.