Raen Reana, Islam Muhammad Muinul, Islam Redwanul, Islam Md Rabiul, Jarin Tanima
Department of Biomedical Engineering, Khulna University of Engineering & Technology, Khulna, Bangladesh.
Department of Biomedical Engineering, Chittagong University of Engineering & Technology, Chittagong, Bangladesh.
Mol Divers. 2025 Apr;29(2):1589-1617. doi: 10.1007/s11030-024-10935-4. Epub 2024 Jul 24.
The excessive activation of the monkeypox virus (MPXV-Congo_8-156) is linked to various skin and respiratory disorders such as rashes, fluid-filled blisters, swollen lymph nodes and encephalitis (inflammation of the brain), highlighting MPXV-Congo_8-156 as a promising target for drug intervention. Despite the effectiveness of Cidofovir, in inhibiting MPXV activity, its limited ability to penetrate the skin and its strong side effects restrict its application. To address this challenge, we screened 500 compounds capable of penetrating the skin and gastrointestinal tract to identify potent MPXV inhibitors. Various characterization schemes and structural models of MPXV-Congo_8-156 were explored with bioinformatics tools like PROTPARAM, SOPMA, SWISS-MODEL and PROCHECK. Using molecular docking in PyRx, we evaluated the binding affinities of these compounds with MPXV-Congo_8-156 and identified the top five candidates ranging from - 9.2 to - 8.8 kcal/mol. ADMET analysis indicated that all five compounds were safer alternatives, showing no AMES toxicity or carcinogenicity in toxicological assessments. Molecular dynamics (MD) simulations, conducted for 100 ns each, confirmed the docking interactions of the top five compounds alongside the control (Cidofovir), validating their potential as MPXV inhibitors. The compounds with PubChem CID numbers 4061636, 4422538, 3583576, 4856107 and 4800629 demonstrated strong support in terms of root-mean-square deviation (RMSD), root-mean-square fluctuation (RMSF), radius of gyration (Rg), solvent-accessible surface area (SASA) value, hydrogen bond analysis, and Molecular Mechanics Poisson-Boltzmann Surface Area (MM-PBSA) analysis. Thus, our investigation identified these five compounds as promising inhibitors of MPXV, offering potential therapeutic avenues. However, further in vivo studies are necessary to validate our findings.
猴痘病毒(MPXV - Congo_8 - 156)的过度激活与各种皮肤和呼吸系统疾病有关,如皮疹、充满液体的水泡、淋巴结肿大和脑炎(脑部炎症),这突出表明MPXV - Congo_8 - 156是药物干预的一个有前景的靶点。尽管西多福韦在抑制MPXV活性方面有效,但其穿透皮肤的能力有限且副作用强烈,限制了其应用。为应对这一挑战,我们筛选了500种能够穿透皮肤和胃肠道的化合物,以鉴定有效的MPXV抑制剂。使用诸如PROTPARAM、SOPMA、SWISS - MODEL和PROCHECK等生物信息学工具探索了MPXV - Congo_8 - 156的各种表征方案和结构模型。通过PyRx中的分子对接,我们评估了这些化合物与MPXV - Congo_8 - 156的结合亲和力,并确定了排名前五的候选物,其范围为 - 9.2至 - 8.8千卡/摩尔。ADMET分析表明,所有这五种化合物都是更安全的替代品,在毒理学评估中未显示AMES毒性或致癌性。分别进行了100纳秒的分子动力学(MD)模拟,证实了排名前五的化合物与对照(西多福韦)的对接相互作用,验证了它们作为MPXV抑制剂的潜力。具有PubChem CID编号4061636、4422538、3583576、4856107和4800629的化合物在均方根偏差(RMSD)、均方根波动(RMSF)、回转半径(Rg)、溶剂可及表面积(SASA)值、氢键分析和分子力学泊松 - 玻尔兹曼表面积(MM - PBSA)分析方面表现出有力支持。因此,我们的研究确定这五种化合物是有前景的MPXV抑制剂,提供了潜在的治疗途径。然而,需要进一步的体内研究来验证我们的发现。