Siddiquee Noimul Hasan, Hossain Md Ifteker, Priya Farhana Mansoor, Azam Sakia Binte, Talukder Md Enamul Kabir, Barua Durjoy, Malek Salina, Saha Niloy, Muntaha Sidratul, Paul Ridoy, Ritu Israt Jahan, Tuly Farjana Islam, Hossain Abir
Department of Microbiology, Noakhali Science and Technology University, Noakhali, Bangladesh.
Bioinformatics Laboratory (BioLab), Noakhali, Bangladesh.
PLoS One. 2024 Dec 30;19(12):e0310802. doi: 10.1371/journal.pone.0310802. eCollection 2024.
The rare zoonotic Borna disease virus (BDV) causes fatal neurological disease in various animals, with a high mortality rate exceeding 90% in central Europe. However, unlike most viruses, it establishes persistent infections within the host cell nucleus, hindering treatment. As successful BDV treatments remain elusive, the researchers turned to a computational approach, utilizing molecular docking, ADME/T, post-docking MMGBSA, MD simulation, DCCM, and PCA to identify promising phytochemical drug candidates targeting the BDV Nucleoprotein (PDB ID: 1N93). From IMPPAT 1940 unique phytochemical compounds of a total of 8617 compounds from 36 Indian medicinal plants were retrieved. Three compounds were chosen as leads with higher binding affinity of -6.244, -6.116, and -6.07 kcal/mol with CID 163114683 (IMPHY000668) Nimbochalcin, CID 20871246 (IMPHY007896) 3,4-Dihydroxy-5-oxocyclohex-3-ene-1-carboxylic acid, and CID 243 (IMPHY002962) Benzoic acid. The three top compounds coordinated with the protein's common amino acid residues at GLN 161, ARG 165, ILE 145, ILE 162, ILE 149, and VAL 229 during molecular docking, which implies that both lead compounds and the control ligand interact within the protein's shared active site. Afterwards, negative binding free energies of Nimbochalcin, 3,4-Dihydroxy-5-oxocyclohex-3-ene-1-carboxylic acid, and Benzoic acid were -51.21, -13.94, and -22.95 kcal/mol, accordingly. Favorable Pk and toxicological characteristics are shared by all of the chosen drugs, indicating their efficacy and safety. Using MD simulation, these three compounds were further assessed, and their stability in binding to the target protein was confirmed and subsequently, DCCM and PCA analyses were carried out from MD trajectory. MD simulations found that the protein binding site is highly stable when complexed with CID 20871246 and has a higher negative binding free energy value, indicating a strong interaction between the compound and the protein. Principal component analysis (PCA) identified three main components (PC1, PC2, and PC3) that accounted for 53.43%, 12.31%, and 5.97% of the variance, respectively. These findings provide intriguing evidence that the CID 20871246-1N93 complex is more stable than the other complexes. The BDV nucleoprotein was the target of this study's investigation where CID 20871246 (3,4-dihydroxy-5-oxocyclohex-3-ene-1-carboxylic acid) exhibited tremendous antiviral activity which is found in the flower of the plant Mangifera indica revealing as a possible therapeutic candidate.
罕见的人畜共患博尔纳病病毒(BDV)可在多种动物中引发致命的神经系统疾病,在中欧其死亡率超过90%。然而,与大多数病毒不同的是,它能在宿主细胞核内建立持续性感染,这给治疗带来了阻碍。由于尚未找到成功治疗BDV的方法,研究人员转向了一种计算方法,利用分子对接、ADME/T、对接后MMGBSA、分子动力学(MD)模拟、离散变分连续介质模型(DCCM)和主成分分析(PCA)来确定针对BDV核蛋白(PDB ID:1N93)的有前景的植物化学药物候选物。从IMPPAT中检索到了来自36种印度药用植物的总共8617种化合物中的1940种独特植物化学化合物。选择了三种化合物作为先导物,它们与CID 163114683(IMPHY000668)宁檬查尔辛、CID 20871246(IMPHY007896)3,4 - 二羟基 - 5 - 氧代环己 - 3 - 烯 - 1 - 羧酸和CID 243(IMPHY002962)苯甲酸的结合亲和力较高,分别为 - 6.244、 - 6.116和 - 6.07千卡/摩尔。在分子对接过程中,这三种顶级化合物与蛋白质的常见氨基酸残基GLN 161、ARG 165、ILE 145、ILE 162、ILE 149和VAL 229配位,这意味着先导化合物和对照配体都在蛋白质的共享活性位点内相互作用。之后,宁檬查尔辛、3,4 - 二羟基 - 5 - 氧代环己 - 3 - 烯 - 1 - 羧酸和苯甲酸的负结合自由能分别为 - 51.21、 - 13.94和 - 22.95千卡/摩尔。所有选定的药物都具有良好的药代动力学(Pk)和毒理学特性,表明它们的有效性和安全性。使用MD模拟对这三种化合物进行了进一步评估,证实了它们与靶蛋白结合的稳定性,随后,从MD轨迹进行了DCCM和PCA分析。MD模拟发现,当与CID 20871246复合时,蛋白质结合位点高度稳定,并且具有更高的负结合自由能值,表明该化合物与蛋白质之间有强烈的相互作用。主成分分析(PCA)确定了三个主要成分(PC1、PC2和PC3),分别占方差的53.43%、12.31%和5.97%。这些发现提供了有趣的证据,表明CID 20871246 - 1N93复合物比其他复合物更稳定。本研究的调查目标是BDV核蛋白,其中CID 20871246(3,4 - 二羟基 - 5 - 氧代环己 - 3 - 烯 - 1 - 羧酸)表现出巨大的抗病毒活性,该化合物存在于芒果植物的花中,显示为一种可能的治疗候选物。