Antiplatelet activity of loureirin A by attenuating Akt phosphorylation: In vitro studies
Antiplatelet activity of loureirin A by attenuating Akt phosphorylation: In vitro studies
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龙血素 A 通过减弱 Akt 磷酸化的抗血小板活性：体外研究
DOI：
10.1016/j.ejphar.2014.10.059
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发表时间：
2015-01-05
影响因子：
5
通讯作者：
Ming, Zhang-Yin
中科院分区：
文献类型：
--
作者：
Hao, Hong-Zhen;He, Ao-Di;Ming, Zhang-Yin
龙血素A是从血竭中提取的一种黄酮类化合物，在中医中用于促进血液循环和祛瘀。然而，这些影响的机制尚未完全了解。本研究探讨龙血素A的体外抗血小板活性及其机制。我们的研究结果表明，龙血素A负面影响激动剂诱导的血小板聚集，如胶原，胶原相关肽（CRP），ADP和凝血酶。龙血素A以剂量依赖性方式抑制胶原诱导的血小板ATP分泌和凝血酶刺激的P-选择素表达。在存在龙血素A的情况下，血小板在固定的纤维蛋白原上的铺展显著受损。免疫印迹分析表明，100 μ M龙血素A几乎完全消除胶原诱导的Aid：有趣的是，次极大龙血素A（50 μ M）与磷脂酰肌醇3-激酶（PI 3 K）抑制剂Ly 294002对胶原蛋白的抑制作用是相加的。诱导血小板Akt磷酸化。综上所述，龙血素A对血小板活化具有抑制作用，可能是通过PI 3 K/Akt信号传导的损伤，（C）2014 Elsevier B. V.保留所有权利，
Loureirin A is a flavonoid extracted from Dragon's Blood that has been used to promote blood circulation and remove stasis in Chinese traditional medicine. However, the mechanisms of these effects are not fully understood. We explored the anti-platelet activity and underlying mechanism of loureirin A in vitro. Our results indicated that loureirin A negatively affected agonist-induced platelet aggregation such as collagen, collagen-related peptide (CRP), ADP and thrombin. Loureirin A inhibited collagen-induced platelet ATP secretion and thrombin-stimulated P-selectin expression in a dose-dependent manner. Platelet spreading on immobilized fibrinogen was significantly impaired in the presence of loureirin A Immunoblotting analysis indicated that 100 mu M of loureirin A almost completely eliminated collagen-induced Aid: phosphorylation at Ser473 interestingly, a submaximal (lose (50 mu M) of loureirin A had an additive inhibitory effect with the phosphoinositide 3-kinase (PI3K) inhibitor Ly294002 on collage-induced Akt phosphorylation in platelets. Taken together, loureirin A had an inhibitory effect on platelet activation, perhaps through an impairment of PI3K/Akt signaling, (C) 2014 Elsevier B.V. All rights reserved,