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基于计算机的丙型肝炎病毒 RNA 解旋酶及其被白藜芦醇、罗卡酰胺和其他紫檀芪类化合物抑制的研究。

In silico study on the Hepatitis E virus RNA Helicase and its inhibition by silvestrol, rocaglamide and other flavagline compounds.

机构信息

Department of Food and Drug, University of Parma, 43124, Parma, Italy.

出版信息

Sci Rep. 2022 Sep 15;12(1):15512. doi: 10.1038/s41598-022-19818-w.

Abstract

Hepatitis E Virus (HEV) follows waterborne or zoonotic/foodborne transmission. Genotype 3 HEV infections are worldwide spread, especially in swine populations, representing an emerging threat for human health, both for farm workers and pork meat consumers. Unfortunately, HEV in vitro culture and analysis are still difficult, resulting in a poor understanding of its biology and hampering the implementation of counteracting strategies. Indeed, HEV encodes for only one non-structural multifunctional and multidomain protein (ORF1), which might be a good candidate for anti-HEV drugging strategies. In this context, an in silico molecular modelling approach that consisted in homology modelling to derive the 3D model target, docking study to simulate the binding event, and molecular dynamics to check complex stability over time was used. This workflow succeeded to describe ORF1 RNA Helicase domain from a molecular standpoint allowing the identification of potential inhibitory compounds among natural plant-based flavagline-related molecules such as silvestrol, rocaglamide and derivatives thereof. In the context of scouting potential anti-viral compounds and relying on the outcomes presented, further dedicated investigations on silvestrol, rocaglamide and a promising oxidized derivative have been suggested. For the sake of data reproducibility, the 3D model of HEV RNA Helicase has been made publicly available.

摘要

戊型肝炎病毒(HEV)通过水传播或动物源性/食源性传播。基因型 3 HEV 感染在全球范围内传播,特别是在猪群中,这对人类健康构成了新的威胁,无论是对于农场工人还是猪肉消费者。不幸的是,HEV 的体外培养和分析仍然困难,导致对其生物学的了解不足,从而阻碍了对抗策略的实施。事实上,HEV 仅编码一个非结构多功能和多结构域蛋白(ORF1),这可能是抗 HEV 药物研发的一个很好的候选靶点。在这种情况下,采用了一种基于同源建模的计算分子建模方法来推导 3D 模型靶标,对接研究来模拟结合事件,以及分子动力学来检查复合物随时间的稳定性。该工作流程成功地从分子角度描述了 ORF1 RNA 解旋酶结构域,从而能够识别天然植物来源的 flavagline 类分子(如 silvestrol、rocaglamide 及其衍生物)中潜在的抑制化合物。为了寻找潜在的抗病毒化合物,并基于所呈现的结果,建议进一步对 silvestrol、rocaglamide 和一种有前途的氧化衍生物进行专门研究。为了保证数据的可重复性,HEV RNA 解旋酶的 3D 模型已经公开。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c510/9477874/a5be40072a4d/41598_2022_19818_Fig1_HTML.jpg

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