Department of Biology, College of Science, University of Hail, Hail, PO Box 2440, Saudi Arabia.
University of Manouba, ISBST, BVBGR-LR11ES31, Biotechpole Sidi Thabet, 2020 Ariana, Tunisia.
Cell Mol Biol (Noisy-le-grand). 2022 Jan 2;67(4):143-162. doi: 10.14715/cmb/2021.67.4.17.
Developing new prophylactic and therapeutic agents with broad-spectrum antiviral activities is urgently needed to combat emerging human severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). Since no available clinically antiviral drugs have been approved to eradicate COVID-19 as of the writing of this report, this study aimed to investigate bioactive short peptides from Allium subhirsutum L. (Hairy garlic) extracts identified through HR-LC/MS analysis that could potentially hinder the multiplication cycle of SARS-CoV-2 via molecular docking study. The obtained promising results showed that the peptides (Asn-Asn-Asn) possess the highest binding affinities of -8.4 kcal/mol against S protein, (His-Phe-Gln) of -9.8 kcal/mol and (Gln-His-Phe) of -9.7 kcal/mol towards hACE2, (Thr-Leu-Trp) of -10.3 kcal/mol and (Gln-Phe-Tyr) of -9.8 kcal/mol against furin. Additionally, the identified peptides show strong interactions with the targeted and pro-inflammatory ranging from -8.1 to -10.5 kcal/mol for NF-κB-inducing kinase (NIK), from -8.2 to -10 kcal/mol for phospholipase A2 (PLA2), from -8.0 to -10.7 kcal/mol for interleukin-1 receptor-associated kinase 4 (IRAK-4), and from -8.6 to -11.6 kcal/mol for the cyclooxygenase 2 (COX2) with Gln-Phe-Tyr model seems to be the most prominent. Results from pharmacophore, drug-likeness and ADMET prediction analyses clearly evidenced the usability of the peptides to be developed as an effective drug, beneficial for COVID-19 treatment.
开发具有广谱抗病毒活性的新型预防和治疗药物,对于对抗新兴的人类严重急性呼吸综合征冠状病毒 2 (SARS-CoV-2) 至关重要。由于截至本报告撰写时,尚无可用的临床抗病毒药物被批准用于消除 COVID-19,因此本研究旨在通过分子对接研究,从 Allium subhirsutum L.(毛蒜)提取物中鉴定具有生物活性的短肽,这些短肽可能会阻碍 SARS-CoV-2 的繁殖周期。研究获得了有前景的结果,表明这些肽(Asn-Asn-Asn)对 S 蛋白具有最高的结合亲和力(-8.4 kcal/mol),(His-Phe-Gln)对 hACE2 的结合亲和力为-9.8 kcal/mol,(Gln-His-Phe)为-9.7 kcal/mol,(Thr-Leu-Trp)对 furin 的结合亲和力为-10.3 kcal/mol,(Gln-Phe-Tyr)为-9.8 kcal/mol。此外,鉴定的肽与靶向和促炎蛋白之间存在强烈的相互作用,其范围从 NF-κB 诱导激酶 (NIK) 的-8.1 到-10.5 kcal/mol,磷脂酶 A2 (PLA2) 的-8.2 到-10 kcal/mol,白细胞介素 1 受体相关激酶 4 (IRAK-4) 的-8.0 到-10.7 kcal/mol,环加氧酶 2 (COX2) 的-8.6 到-11.6 kcal/mol,其中 Gln-Phe-Tyr 模型最为突出。基于药效团、类药性和 ADMET 预测分析的结果,清楚地证明了这些肽具有开发成有效药物的用途,有利于 COVID-19 的治疗。