Marwali Muhammad R, Hu Chang-Ping, Mohandas Bhavna, Dandapat Abhijit, Deonikar Prabhakar, Chen Jiawei, Cawich Ian, Sawamura Tatsuya, Kavdia Mahendra, Mehta Jawahar L
Division of Cardiovascular Medicine, University of Arkansas for Medical Sciences and Central Arkansas Veterans Healthcare System, Little Rock, AR 72205-7199, USA.
J Pharmacol Exp Ther. 2007 Sep;322(3):1324-32. doi: 10.1124/jpet.107.122853. Epub 2007 May 30.
Lectin-like oxidized low-density lipoprotein (LDL) receptor-1 (LOX-1), a receptor for oxidized-LDL, is up-regulated in activated endothelial cells, and it plays a role in atherothrombosis. However, its role in platelet aggregation is unclear. Both aspirin and HMG CoA reductase inhibitors (statins) reduce LOX-1 expression in endothelial cells. In this study, we investigated the effect of aspirin and pravastatin on LOX-1 expression on plate-lets. After ADP stimulation, mean fluorescence intensity of LOX-1 expression on platelets increased 1.5- to 2.0-fold. Blocking LOX-1 inhibited ADP-induced platelet aggregation in a concentration- and time-dependent manner. We also established that LOX-1 is important for ADP-stimulated inside-out activation of platelet alpha(IIb)beta(3) and alpha(2)beta(1) integrins (fibrinogen receptors). The specificity of this interaction was determined by arginine-glycine-aspartate-peptide inhibition. Furthermore, we found that LOX-1 inhibition of integrin activation is mediated by inhibition of protein kinase C activity. In other experiments, treatment with aspirin (1-10 mM) and pravastatin (1-5 microM) reduced platelet LOX-1 expression, with a synergistic effect of the combination of aspirin and pravastatin. Aspirin and pravastatin both reduced reactive oxygen species (ROS) released by activated platelets measured as malonyldialdehyde (MDA) release and nitrate/nitrite ratio. Aspirin and pravastatin also enhanced nitric oxide (NO) release measured as nitrite/nitrite + nitrate (NOx) ratio in platelet supernates. Small concentrations of aspirin and pravastatin had a synergistic effect on the inhibition of MDA release and enhancement of nitrite/NOx. Thus, LOX-1 is important for ADP-mediated platelet integrin activation, possibly through protein kinase C activation. Furthermore, aspirin and pravastatin inhibit LOX-1 expression on platelets in part by favorably affecting ROS and NO release from activated platelets.
凝集素样氧化型低密度脂蛋白(LDL)受体-1(LOX-1)是氧化型LDL的一种受体,在活化的内皮细胞中上调,并且在动脉粥样硬化血栓形成中起作用。然而,其在血小板聚集中的作用尚不清楚。阿司匹林和HMG CoA还原酶抑制剂(他汀类药物)均可降低内皮细胞中LOX-1的表达。在本研究中,我们调查了阿司匹林和普伐他汀对血小板上LOX-1表达的影响。在ADP刺激后,血小板上LOX-1表达的平均荧光强度增加了1.5至2.0倍。阻断LOX-1以浓度和时间依赖性方式抑制ADP诱导的血小板聚集。我们还证实,LOX-1对于ADP刺激的血小板α(IIb)β(III)和α(2)β(I)整合素(纤维蛋白原受体)的外向内激活很重要。这种相互作用的特异性通过精氨酸-甘氨酸-天冬氨酸肽抑制来确定。此外,我们发现LOX-1对整合素激活的抑制作用是通过抑制蛋白激酶C活性介导的。在其他实验中,用阿司匹林(1-10 mM)和普伐他汀(1-5 μM)处理可降低血小板LOX-1表达,阿司匹林和普伐他汀联合使用具有协同作用。阿司匹林和普伐他汀均降低了以丙二醛(MDA)释放和硝酸盐/亚硝酸盐比率衡量的活化血小板释放的活性氧(ROS)。阿司匹林和普伐他汀还增强了以血小板上清液中亚硝酸盐/亚硝酸盐+硝酸盐(NOx)比率衡量的一氧化氮(NO)释放。低浓度的阿司匹林和普伐他汀对MDA释放的抑制和亚硝酸盐/NOx的增强具有协同作用。因此,LOX-1对于ADP介导的血小板整合素激活很重要,可能是通过蛋白激酶C激活。此外,阿司匹林和普伐他汀部分通过有利地影响活化血小板释放的ROS和NO来抑制血小板上的LOX-1表达。