异东莨菪素通过调节PI3K/Akt和MAPK对胶原诱导的人血小板的抗血小板作用

Q4 Pharmacology, Toxicology and Pharmaceutics Korean Journal of Pharmacognosy Pub Date : 2020-01-01 DOI:10.22889/KJP.2020.51.3.151
Dong-Ha Lee
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引用次数: 0

摘要

当血管受损时,会发生快速的止血反应,以尽量减少失血,维持正常循环。在这个过程中,血小板的活化和聚集是必不可少的。然而,血小板聚集过度或血小板聚集异常可能是心血管疾病的原因,如血栓形成、中风和动脉粥样硬化。因此,寻找能够调节血小板活化和抑制聚集反应的物质,对预防和治疗心血管疾病具有重要意义。异东莨菪素主要存在于植物蒿或东莨菪的根部,有报道称其具有抗癌和阿尔茨海默病的潜在药理作用,但其在血小板聚集和血栓形成中的作用和机制尚不清楚。本研究证实了异东莨菪素对胶原诱导的人血小板聚集、txa2生成和细胞内颗粒分泌(ATP和血清素释放)的主要调控作用。此外,我们还研究了异东莨菪素对血小板聚集中参与信号转导的磷酸化蛋白PI3K/Akt和MAPK磷酸化的影响。因此,异东莨菪素显著抑制PI3K/Akt和MAPK的磷酸化,通过产生txa2和细胞内颗粒分泌(ATP和5 -羟色胺释放)显著抑制血小板聚集。因此,我们认为异东莨菪碱是一种抗血小板物质,可调节磷蛋白如PI3K/Akt和MAPK的磷酸化,是血小板源性心血管疾病的预防和治疗药物。
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Anti-platelet Effects of Isoscopoletin through Regulation of PI3K/Akt and MAPK on Collagen-induced Human Platelets
 When blood vessels are damaged, a rapid hemostatic reaction occurs to minimize blood loss and maintain normal circulation. Platelet activation and aggregation is essential in this process. However, excessive platelet aggregation or abnormal platelet aggregation may be the cause of cardiovascular disease, such as thrombosis, stroke and atherosclerosis. Therefore, it is important to prevent and treat cardiovascular disease by finding substances that can regulate platelet activation and suppress aggregation reactions. Isoscopoletin, which is mainly found in the roots of plants Artemisia or Scopolia, has been reported to have potential pharmacological effects on anticancer and Alzheimer’s disease, but its role and mechanisms for platelet aggregation and thrombus formation are unknown. This study confirmed the effect of isoscopoletin on major regulation of collageninduced human platelet aggregation, TXA 2 production and intracellular granular secretion (ATP and serotonin release). In addition, the effects of isoscopoletin on phosphorylation of phosphorylated proteins PI3K/Akt and MAPK involved in signal transduction in platelet aggregation was studied. As a result, isoscopoletin significantly inhibited the phosphorylation of PI3K/Akt and MAPK, significantly inhibiting platelet aggregation through TXA 2 production and intracellular granular secretion (ATP and serotonin release). Therefore, we suggest that isoscopoletin is an anti-platelet substance that regulates phosphorylation of phosphorus proteins such as PI3K/Akt and MAPK and is valuable as a preventive and therapeutic agent for platelet-derived cardiovascular disease.
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来源期刊
Korean Journal of Pharmacognosy
Korean Journal of Pharmacognosy Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
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