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计算机模拟研究表明,结构多样的植物次生代谢物在降低 SARS-CoV-2 发病机制方面发挥了作用。

In silico studies evidenced the role of structurally diverse plant secondary metabolites in reducing SARS-CoV-2 pathogenesis.

机构信息

Centre for Rural Development and Technology, Indian Institute of Technology Delhi, New Delhi, Delhi, 110016, India.

出版信息

Sci Rep. 2020 Nov 25;10(1):20584. doi: 10.1038/s41598-020-77602-0.

Abstract

Plants are endowed with a large pool of structurally diverse small molecules known as secondary metabolites. The present study aims to virtually screen these plant secondary metabolites (PSM) for their possible anti-SARS-CoV-2 properties targeting four proteins/ enzymes which govern viral pathogenesis. Results of molecular docking with 4,704 ligands against four target proteins, and data analysis revealed a unique pattern of structurally similar PSM interacting with the target proteins. Among the top-ranked PSM which recorded lower binding energy (BE), > 50% were triterpenoids which interacted strongly with viral spike protein-receptor binding domain, > 32% molecules which showed better interaction with the active site of human transmembrane serine protease were belongs to flavonoids and their glycosides, > 16% of flavonol glycosides and > 16% anthocyanidins recorded lower BE against active site of viral main protease and > 13% flavonol glycoside strongly interacted with active site of viral RNA-dependent RNA polymerase. The primary concern about these PSM is their bioavailability. However, several PSM recorded higher bioavailability score and found fulfilling most of the drug-likeness characters as per Lipinski's rule (Coagulin K, Kamalachalcone C, Ginkgetin, Isoginkgetin, 3,3'-Biplumbagin, Chrysophanein, Aromoline, etc.). Natural occurrence, bio-transformation, bioavailability of selected PSM and their interaction with the target site of selected proteins were discussed in detail. Present study provides a platform for researchers to explore the possible use of selected PSM to prevent/ cure the COVID-19 by subjecting them for thorough in vitro and in vivo evaluation for the capabilities to interfering with the process of viral host cell recognition, entry and replication.

摘要

植物拥有大量结构多样的小分子,这些小分子被称为次生代谢产物。本研究旨在通过虚拟筛选这些植物次生代谢产物(PSM),寻找针对四种控制病毒发病机制的蛋白/酶的可能抗 SARS-CoV-2 特性。对 4704 种配体与四种靶蛋白进行分子对接的结果和数据分析显示,具有相似结构的 PSM 与靶蛋白相互作用的独特模式。在记录较低结合能(BE)的排名靠前的 PSM 中,超过 50%是与病毒刺突蛋白受体结合域强烈相互作用的三萜类化合物,超过 32%的与人类跨膜丝氨酸蛋白酶活性位点相互作用更好的分子属于类黄酮及其糖苷,超过 16%的黄酮醇糖苷和超过 16%的花色苷记录了对病毒主要蛋白酶活性位点的较低 BE,超过 13%的黄酮醇糖苷与病毒 RNA 依赖性 RNA 聚合酶的活性位点强烈相互作用。这些 PSM 的主要关注点是它们的生物利用度。然而,有几种 PSM 记录了更高的生物利用度评分,并发现它们符合大多数 Lipinski 规则的药物相似性特征(Coagulin K、Kamalachalcone C、Ginkgetin、Isoginkgetin、3,3'-Biplumbagin、Chrysophanein、Aromoline 等)。本文详细讨论了选定 PSM 的天然发生、生物转化、生物利用度以及它们与选定蛋白靶位点的相互作用。本研究为研究人员提供了一个平台,通过对选定的 PSM 进行全面的体外和体内评估,以探索它们在预防/治疗 COVID-19 方面的可能用途,这些评估旨在评估它们干扰病毒宿主细胞识别、进入和复制过程的能力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/738b/7689506/c0b05bb335a5/41598_2020_77602_Fig1a_HTML.jpg

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