多酚的血小板聚集抑制活性可由 67kda 层粘连蛋白受体介导:治疗静脉血栓栓塞症的新疗法。

Satya Prakash, Amit Ghosh, Arnab Nayek, Sheetal Kiran
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引用次数: 0

摘要

背景:血栓性疾病仍然是一大杀手。阿司匹林、替卡格雷、氯吡格雷等是最广泛使用的常规抗血小板药物。大量患者对这种药物产生耐药性,导致治疗效果不佳:目的:针对对抗血小板药物耐药的患者,需要开发一种抗血小板效果稳定、出血风险最小的新型抗血小板药物:方法:使用 Autodock Vina 1.1.2 进行蛋白质配体对接,研究 67LR 与不同多酚的相互作用:结果:在 18 种多酚中,大蒜素与 67LR 的结合亲和力最高,没食子酸与 67LR 的结合亲和力最低。在 18 个分子中,结合亲和力从高到低的前 10 个分子介于-10.6(大蒜素)和-6.5(表没食子儿茶素)之间:结论:多酚类物质可通过 67 LR 抑制血小板聚集,是治疗血栓性疾病的一种替代疗法。此外,了解多酚类物质是否与阿司匹林和氯吡格雷具有相同的干预途径也很有意义。有效的多酚类物质有助于新型抗血小板药物的化合物开发。
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The Platelet Aggregation Inhibition Activity of Polyphenols can be Mediated by 67kda Laminin Receptor: A New Therapeutic Strategy For the Treatment of Venous Thromboembolism.

Background: Thrombotic disease is still a major killer. Aspirin, Ticagrelor, Clopidogrel, etc. are the most widely used conventional antiplatelet drugs. The significant number of patients who are resistant to this drug shows a poor outcome.

Objective: Developing a new antiplatelet agent with a stable antiplatelet effect and minimal bleeding risk is required for a patient who is resistant to antiplatelet drugs.

Methods: Protein-ligand docking was performed using Autodock Vina 1.1.2 to study the interaction of 67LR with different Polyphenols.

Results: Among the 18 polyphenols, thearubigin has the highest binding affinity towards 67LR and gallic acid shows the lowest binding affinity. Among the 18 molecules, the top 4 molecules from the highest to lowest binding affinity range from-10.6 (thearubigin) to -6.5 (Epigallocatechin).

Conclusion: Polyphenols may inhibit platelet aggregation through 67 LR and can be an alternative treatment for Thrombotic Disease. Moreover, it will be interesting to know whether polyphenols interfere with the same pathways as aspirin and clopidogrel. Effective polyphenols could help prototype the compound development of novel antiplatelet agents.

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来源期刊
Cardiovascular and Hematological Agents in Medicinal Chemistry
Cardiovascular and Hematological Agents in Medicinal Chemistry Medicine-Cardiology and Cardiovascular Medicine
CiteScore
2.70
自引率
0.00%
发文量
34
期刊介绍: Cardiovascular & Hematological Agents in Medicinal Chemistry aims to cover all the latest and outstanding developments in medicinal chemistry and rational drug design for the discovery of new Cardiovascular & Hematological Agents. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of current topics in Cardiovascular & Hematological medicinal chemistry. Cardiovascular & Hematological Agents in Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments in cardiovascular & hematological drug discovery.
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