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一种利用天然植物化学物质针对新冠病毒RNA依赖性RNA聚合酶的计算机模拟方法。

An in silico approach to target RNA-dependent RNA polymerase of COVID-19 with naturally occurring phytochemicals.

作者信息

Mahrosh Hafiza Salaha, Mustafa Ghulam

机构信息

Department of Biochemistry, Government College University, Faisalabad, 38000 Pakistan.

出版信息

Environ Dev Sustain. 2021;23(11):16674-16687. doi: 10.1007/s10668-021-01373-5. Epub 2021 Apr 3.

Abstract

The novel coronavirus disease 2019 (COVID-19) was firstly reported from Wuhan city of China and found as a highly contagious, transmittable and pathogenic viral infection. The World Health Organization declared COVID-19 as a pandemic since its emergence from China. The RNA-dependent RNA polymerase (nsp-12) is a complex with nsp-7 and nsp-8 cofactors and is a major constituent of viral replication and RNA synthesis machinery. In the current study, the RdRp of the virus was selected as a receptor protein for computational drug discovery. Computational homology modelling was done in order to find the hidden secondary structures and structural assessment of the viral protein to target them via antiviral drugs. The study was based on molecular docking of different phytochemicals to check their potentials against viral replicative proteins. Out of 200 ligands used in this study from different plants, the best ten were selected based on drug discovery parameters such as S-score, ligand interactions, hydrophobic interactions and druglikeness. The ten best selected ligands were found to be verbenalin, epigallocatechin, swertisin, nobiletin, pinoresinol, caftaric acid, hesperetin, islandicin, neochlorogenic acid and sesamin that exploit the potency as antagonists of viral protein. Among binding interactions of all ligands, Arg339 centred as the main interacting residue among almost all the ligands. Till now, many antiviral agents have shown potency in only mild cases of SARS-CoV-2, but no effective drug has been found for critical pulmonary cases. In clinical trials, many broad-spectrum antiviral agents have been still in trial periods of testing against SARS-CoV-2. Till date, no effective drug or vaccine has been validated with significant efficacy and potency against the SARS-CoV-2; therefore, there is an urgent need to design effective vaccine against nCoV-19 infection.

摘要

2019年新型冠状病毒病(COVID-19)最初在中国武汉市被报告,是一种具有高度传染性、可传播性和致病性的病毒感染。自COVID-19从中国出现以来,世界卫生组织宣布其为大流行病。RNA依赖性RNA聚合酶(nsp-12)是一种与nsp-7和nsp-8辅助因子形成的复合物,是病毒复制和RNA合成机制的主要组成部分。在当前研究中,该病毒的RdRp被选为用于计算机辅助药物发现的受体蛋白。进行了计算机同源建模,以找到病毒蛋白的隐藏二级结构并对其进行结构评估,以便通过抗病毒药物靶向它们。该研究基于不同植物化学物质的分子对接,以检查它们对病毒复制蛋白的潜在作用。在本研究中使用的来自不同植物的200种配体中,根据药物发现参数(如S评分、配体相互作用、疏水相互作用和类药性)选择了最佳的十种。发现最佳选择的十种配体是马鞭草苷、表没食子儿茶素、獐牙菜苷、川陈皮素、松脂醇、咖啡酸、橙皮素、岛青霉素、新绿原酸和芝麻素,它们具有作为病毒蛋白拮抗剂的潜力。在所有配体的结合相互作用中,Arg339几乎是所有配体的主要相互作用残基。到目前为止,许多抗病毒药物仅在轻度新型冠状病毒肺炎病例中显示出效力,但尚未找到针对重症肺炎病例的有效药物。在临床试验中,许多广谱抗病毒药物仍处于针对新型冠状病毒肺炎的试验测试阶段。迄今为止,尚未验证有针对新型冠状病毒肺炎具有显著疗效和效力的有效药物或疫苗;因此,迫切需要设计针对新型冠状病毒感染的有效疫苗。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6c76/8018901/7ec830eed5bb/10668_2021_1373_Fig1_HTML.jpg

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