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对一些新引入的天然产物进行密度泛函理论(DFT)、分子对接和分子动力学模拟研究,以探究其抗新型冠状病毒(SARS-CoV-2)的潜在用途。

DFT, molecular docking and molecular dynamics simulation studies on some newly introduced natural products for their potential use against SARS-CoV-2.

作者信息

Erdogan Taner

机构信息

Dept. of Chemistry and Chemical Processing Tech, Kocaeli Vocat. Sch. Kocaeli University, Kocaeli, Turkey.

出版信息

J Mol Struct. 2021 Oct 15;1242:130733. doi: 10.1016/j.molstruc.2021.130733. Epub 2021 May 22.

Abstract

Throughout the history, natural products always give new paths to develop new drugs. As with many other diseases, natural compounds can be helpful in the treatment of COVID-19. SARS-CoV-2 main protease enzyme has an important role in viral replication and transcription. Therefore, inhibiting this enzyme may be helpful in the treatment of COVID-19. In this study, it is aimed to investigate eight natural compounds which have recently entered the literature, computationally for their potential use against SARS-CoV-2. For this purpose, first, density functional theory (DFT) calculations were performed on the investigated compounds, and energy minimizations, geometry optimizations, vibrational analyses, molecular electrostatic potential map calculations were carried out. After DFT calculations, geometry optimized structures were subjected to molecular docking calculations with the use of SARS-CoV-2 main protease (pdb id: 5r80) and top-scoring ligand-receptor complexes were obtained. In the next part of the study, molecular dynamics (MD) simulations were performed on the top-scoring ligand-receptor complexes to investigate the stability of the ligand-receptor complexes and the interactions between ligands and receptor in more detail. Additionally, in this part of the study, binding free energies are calculated with the use of molecular mechanics with Poisson-Boltzmann surface area (MM-PBSA) method. Results showed that, all ligand-receptor complexes remain stable during the MD simulations and most of the investigated compounds but especially two of them showed considerably high binding affinity to SARS-CoV-2 main protease. Finally, in the study, ADME (adsorption, desorption, metabolism, excretion) predictions and drug-likeness analyses were performed on the investigated compounds.

摘要

纵观历史,天然产物始终为新药研发提供新途径。与许多其他疾病一样,天然化合物可能有助于治疗新冠肺炎。新型冠状病毒2型主要蛋白酶在病毒复制和转录中起重要作用。因此,抑制这种酶可能有助于治疗新冠肺炎。本研究旨在通过计算研究最近进入文献的八种天然化合物对新型冠状病毒2型的潜在用途。为此,首先对所研究的化合物进行密度泛函理论(DFT)计算,并进行能量最小化、几何结构优化、振动分析和分子静电势图计算。DFT计算后,将几何结构优化的结构与新型冠状病毒2型主要蛋白酶(pdb编号:5r80)进行分子对接计算,得到得分最高的配体-受体复合物。在研究的下一部分,对得分最高的配体-受体复合物进行分子动力学(MD)模拟,以更详细地研究配体-受体复合物的稳定性以及配体与受体之间的相互作用。此外,在研究的这一部分中,使用分子力学与泊松-玻尔兹曼表面积(MM-PBSA)方法计算结合自由能。结果表明,所有配体-受体复合物在MD模拟过程中均保持稳定,大多数所研究的化合物,尤其是其中两种,对新型冠状病毒2型主要蛋白酶表现出相当高的结合亲和力。最后,在本研究中,对所研究的化合物进行了ADME(吸收、解吸、代谢、排泄)预测和类药性质分析。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/047c/8140653/1a21b8d9f217/fx1_lrg.jpg

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