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基于结构的筛选和天然次生代谢物的分子对接与动态模拟,针对五种不同逆转录病毒的 RNA 依赖性 RNA 聚合酶。

Structure based screening and molecular docking with dynamic simulation of natural secondary metabolites to target RNA-dependent RNA polymerase of five different retroviruses.

机构信息

College of Life Sciences, Anhui Normal University, Wuhu, China.

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

出版信息

PLoS One. 2024 Aug 5;19(8):e0307615. doi: 10.1371/journal.pone.0307615. eCollection 2024.

Abstract

Viral diseases pose a serious global health threat due to their rapid transmission and widespread impact. The RNA-dependent RNA polymerase (RdRp) participates in the synthesis, transcription, and replication of viral RNA in host. The current study investigates the antiviral potential of secondary metabolites particularly those derived from bacteria, fungi, and plants to develop novel medicines. Using a virtual screening approach that combines molecular docking and molecular dynamics (MD) simulations, we aimed to discover compounds with strong interactions with RdRp of five different retroviruses. The top five compounds were selected for each viral RdRp based on their docking scores, binding patterns, molecular interactions, and drug-likeness properties. The molecular docking study uncovered several metabolites with antiviral activity against RdRp. For instance, cytochalasin Z8 had the lowest docking score of -8.9 (kcal/mol) against RdRp of SARS-CoV-2, aspulvinone D (-9.2 kcal/mol) against HIV-1, talaromyolide D (-9.9 kcal/mol) for hepatitis C, aspulvinone D (-9.9 kcal/mol) against Ebola and talaromyolide D also maintained the lowest docking score of -9.2 kcal/mol against RdRp enzyme of dengue virus. These compounds showed remarkable antiviral potential comparable to standard drug (remdesivir -7.4 kcal/mol) approved to target RdRp and possess no significant toxicity. The molecular dynamics simulation confirmed that the best selected ligands were firmly bound to their respective target proteins for a simulation time of 200 ns. The identified lead compounds possess distinctive pharmacological characteristics, making them potential candidates for repurposing as antiviral drugs against SARS-CoV-2. Further experimental evaluation and investigation are recommended to ascertain their efficacy and potential.

摘要

病毒疾病由于其快速传播和广泛影响,对全球健康构成严重威胁。RNA 依赖的 RNA 聚合酶(RdRp)参与宿主中病毒 RNA 的合成、转录和复制。本研究调查了特别是来自细菌、真菌和植物的次生代谢产物的抗病毒潜力,以开发新型药物。我们使用一种虚拟筛选方法,结合分子对接和分子动力学(MD)模拟,旨在发现与五种不同逆转录病毒的 RdRp 具有强相互作用的化合物。根据对接分数、结合模式、分子相互作用和类药性特性,为每个病毒 RdRp 选择了前五个化合物。分子对接研究揭示了几种对 RdRp 具有抗病毒活性的代谢物。例如,细胞松弛素 Z8 对 SARS-CoV-2 的 RdRp 的对接分数最低为-8.9(千卡/摩尔),aspulvinone D(-9.2 kcal/mol)对 HIV-1,talaromyolide D(-9.9 kcal/mol)对丙型肝炎,aspulvinone D(-9.9 kcal/mol)对埃博拉病毒,而 talaromyolide D 也保持了对登革热病毒 RdRp 酶的最低对接分数-9.2 kcal/mol。这些化合物表现出与标准药物(瑞德西韦-7.4 kcal/mol)相当的显著抗病毒潜力,该药物被批准用于靶向 RdRp,并且没有显著毒性。分子动力学模拟证实,最佳选择的配体牢固地结合到各自的靶蛋白上,模拟时间为 200 ns。鉴定的先导化合物具有独特的药理特性,使它们成为重新用作针对 SARS-CoV-2 的抗病毒药物的潜在候选药物。建议进行进一步的实验评估和研究,以确定它们的疗效和潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/947c/11299834/12d315f42226/pone.0307615.g001.jpg

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