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针对血管紧张素转化酶 2(ACE2)受体的不同化合物可能含有 SARS-CoV-2 的感染力:一项计算机研究。

Different compounds against Angiotensin-Converting Enzyme 2 (ACE2) receptor potentially containing the infectivity of SARS-CoV-2: an in silico study.

机构信息

Molecular Medicine Department, Biotechnology Research Center, Pasteur Institute of Iran, 69th Pasteur Street, Kargar Avenue, Tehran, Iran.

出版信息

J Mol Model. 2022 Mar 5;28(4):82. doi: 10.1007/s00894-022-05059-1.

Abstract

Novel SARS coronavirus or SARS-CoV-2 is a novel coronavirus that was identified and spread from Wuhan in 2019. On January 30th, the World Health Organization declared the coronavirus outbreak as a Global Public Health Emergency. Although Remdesivir and Molnupiravir are FDA-approved drugs for COVID-19, finding new efficient and low-cost antiviral drugs against COVID-19 for applying in more countries can still be helpful. One of the potential sources for finding new and low-cost drugs is the herbal compounds in addition to repurposing FDA-approved drugs. So, in this study, we focused on finding effective drug candidates against COVID-19 based on the computational approaches. As ACE2 serves as a critical receptor for cell entry of this virus. Inhibiting the binding site of SARS-CoV-2 on human ACE2 provides a promising therapeutic approach for developing drugs against SARS-CoV-2. Herein, we applied a bioinformatics approach to identify possible potential inhibitors of SARS-CoV-2. A library of FDA-approved compounds and five natural compounds was screened using Smina docking. Top-docking compounds are then applied in Molecular Dynamics (MD) simulation to assess the stability of ACE2-inhibitor complexes. Results indicate that Luteolin and Chrysin represent high conformation stability with ACE2 during 120 ns of Molecular Dynamics simulation. The binding free energies of Luteolin and Chrysin were calculated by the Molecular Mechanics/Poisson-Boltzmann Surface Area method (MM/PBSA) which confirmed the relative binding free energy of these drugs to ACE2 in favor of the effective binding. So, Luteolin and Chrysin could sufficiently interact with ACE2 and block the Spike binding pocket of ACE2 and can be a potential inhibitor against the binding of SARS-CoV-2 to ACE2 receptor which is an early stage of infection. Luteolin and Chrysin could be suggestive as beneficial compounds for preventing or reducing SARS-CoV-2 transmission and infection which need experimental work to prove.

摘要

新型严重急性呼吸系统综合征冠状病毒或 SARS-CoV-2 是一种新型冠状病毒,于 2019 年在中国武汉被发现并传播。1 月 30 日,世界卫生组织宣布冠状病毒爆发为全球公共卫生紧急事件。尽管瑞德西韦和莫努匹韦已获得 FDA 批准用于治疗 COVID-19,但寻找新的有效且低成本的抗 COVID-19 病毒药物,以在更多国家应用,仍然是有帮助的。寻找新的低成本药物的潜在来源之一除了重新利用 FDA 批准的药物外,还包括草药化合物。因此,在这项研究中,我们专注于基于计算方法寻找针对 COVID-19 的有效药物候选物。由于 ACE2 是该病毒进入细胞的关键受体,因此抑制 SARS-CoV-2 与人 ACE2 的结合位点为开发针对 SARS-CoV-2 的药物提供了有希望的治疗方法。在此,我们应用生物信息学方法来鉴定可能的 SARS-CoV-2 潜在抑制剂。使用 Smina 对接筛选了 FDA 批准的化合物库和五种天然化合物。然后将顶级对接化合物应用于分子动力学 (MD) 模拟,以评估 ACE2-抑制剂复合物的稳定性。结果表明,在 120ns 的分子动力学模拟过程中,木樨草素和白杨黄素与 ACE2 具有高构象稳定性。通过分子力学/泊松-玻尔兹曼表面积法 (MM/PBSA) 计算了木樨草素和白杨黄素的结合自由能,该方法证实了这些药物与 ACE2 的相对结合自由能有利于有效结合。因此,木樨草素和白杨黄素可以与 ACE2 充分相互作用并阻断 ACE2 的 Spike 结合口袋,可作为潜在的抑制剂,可阻止 SARS-CoV-2 与 ACE2 受体结合,这是感染的早期阶段。木樨草素和白杨黄素可能有助于预防或减少 SARS-CoV-2 的传播和感染,这需要实验工作来证明。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f104/8898033/f68fd008d7e4/894_2022_5059_Fig1_HTML.jpg

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