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网络药理学研究以阐明抗组胺药抗COVID-19的潜在关键靶点

Network Pharmacology Study to Elucidate the Key Targets of Underlying Antihistamines against COVID-19.

作者信息

Oh Ki-Kwang, Adnan Md, Cho Dong-Ha

机构信息

Department of Bio-Health Convergence, College of Biomedical Science, Kangwon National University, Chuncheon 24341, Korea.

出版信息

Curr Issues Mol Biol. 2022 Apr 8;44(4):1597-1609. doi: 10.3390/cimb44040109.

Abstract

Antihistamines have potent efficacy to alleviate COVID-19 (Coronavirus disease 2019) symptoms such as anti-inflammation and as a pain reliever. However, the pharmacological mechanism(s), key target(s), and drug(s) are not documented well against COVID-19. Thus, we investigated to decipher the most significant components and how its research methodology was utilized by network pharmacology. The list of 32 common antihistamines on the market were retrieved via drug browsing databases. The targets associated with the selected antihistamines and the targets that responded to COVID-19 infection were identified by the Similarity Ensemble Approach (SEA), SwissTargetPrediction (STP), and PubChem, respectively. We described bubble charts, the Pathways-Targets-Antihistamines (PTA) network, and the protein-protein interaction (PPI) network on the RPackage via STRING database. Furthermore, we utilized the AutoDock Tools software to perform molecular docking tests (MDT) on the key targets and drugs to evaluate the network pharmacological perspective. The final 15 targets were identified as core targets, indicating that Neuroactive ligand-receptor interaction might be the hub-signaling pathway of antihistamines on COVID-19 via bubble chart. The PTA network was constructed by the RPackage, which identified 7 pathways, 11 targets, and 30 drugs. In addition, GRIN2B, a key target, was identified via topological analysis of the PPI network. Finally, we observed that the GRIN2B-Loratidine complex was the most stable docking score with -7.3 kcal/mol through molecular docking test. Our results showed that Loratadine might exert as an antagonist on GRIN2B via the neuroactive ligand-receptor interaction pathway. To sum up, we elucidated the most potential antihistamine, a key target, and a key pharmacological pathway as alleviating components against COVID-19, supporting scientific evidence for further research.

摘要

抗组胺药在减轻新型冠状病毒肺炎(COVID-19)症状方面具有强大功效,如抗炎和止痛。然而,针对COVID-19的药理机制、关键靶点和药物尚未有充分记载。因此,我们进行研究以解读最重要的成分及其如何通过网络药理学利用其研究方法。通过药物浏览数据库检索了市场上32种常见抗组胺药的清单。分别通过相似性整合方法(SEA)、瑞士靶点预测(STP)和PubChem确定了与所选抗组胺药相关的靶点以及对COVID-19感染有反应的靶点。我们通过STRING数据库在R包上描述了气泡图、通路-靶点-抗组胺药(PTA)网络和蛋白质-蛋白质相互作用(PPI)网络。此外,我们利用AutoDock Tools软件对关键靶点和药物进行分子对接试验(MDT),以评估网络药理学观点。最终确定了15个靶点为核心靶点,通过气泡图表明神经活性配体-受体相互作用可能是抗组胺药针对COVID-19的枢纽信号通路。通过R包构建了PTA网络,该网络确定了7条通路、11个靶点和30种药物。此外,通过PPI网络的拓扑分析确定了关键靶点GRIN2B。最后,通过分子对接试验观察到GRIN2B-氯雷他定复合物的对接分数最稳定,为-7.3千卡/摩尔。我们的结果表明,氯雷他定可能通过神经活性配体-受体相互作用途径对GRIN2B发挥拮抗剂作用。综上所述,我们阐明了最具潜力的抗组胺药、关键靶点和关键药理途径作为减轻COVID-19的成分,为进一步研究提供了科学依据。

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