Clinical Biochemistry Research Center, Basic Health Sciences Institute, Shahrekord University of Medical Sciences, Shahrekord, Iran.
Mol Divers. 2024 Aug;28(4):2513-2546. doi: 10.1007/s11030-023-10692-w. Epub 2023 Jul 18.
The monkeypox spread has been announced a public health emergency of international concern (PHEIC) by the World Health Organization (WHO). Both monkeypox and smallpox viruses are placed in the genus Orthopoxvirus. Despite recommendations for the administration of smallpox drugs versus monkeypox, no specific drug for monkeypox has yet been introduced. A reliable and effective method against this outbreak can be the use of natural products. This study aimed for identification of natural flavonoid derivatives as potential thymidine kinase inhibitors, the main drug target of monkeypox virus. Thymidine kinase protein structure was predicted by homology modeling and the quality of generated model was evaluated. Then, the interaction between natural flavonoids and the modeled thymidine kinase was explored by molecular docking. Based on docking results, more than half of the flavonoids with higher docking scores compared to reference drug (ganciclovir) were exhibited better binding affinities toward the protein. In addition, stability of the top flavonoids including eupatorin, fisetin, rhamnetin and scutellarein, was confirmed by MD simulations and binding free energy calculations using MM/PBSA analysis. These selected compounds were also shown acceptable results for drug likeness and ADMET analysis. Therefore, the results of the study showed that these flavonoids could be considered as potential thymidine kinase inhibitors for use against monkeypox virus.
世界卫生组织(WHO)宣布猴痘疫情为国际关注的突发公共卫生事件(PHEIC)。猴痘病毒和天花病毒都属于正痘病毒属。尽管有针对天花药物与猴痘药物的使用建议,但目前尚未推出针对猴痘的特定药物。针对此次疫情,可靠有效的方法可以是使用天然产物。本研究旨在鉴定天然类黄酮衍生物作为潜在的胸苷激酶抑制剂,这是猴痘病毒的主要药物靶点。通过同源建模预测胸苷激酶蛋白结构,并评估生成模型的质量。然后,通过分子对接探索天然类黄酮与建模胸苷激酶之间的相互作用。基于对接结果,与参比药物(更昔洛韦)相比,具有更高对接评分的一半以上类黄酮显示出与蛋白质更好的结合亲和力。此外,通过 MD 模拟和使用 MM/PBSA 分析的结合自由能计算,对包括 eupatorin、fisetin、rhamnetin 和 scutellarein 在内的 top 类黄酮的稳定性进行了确认。这些选定的化合物在药物相似性和 ADMET 分析方面也表现出可接受的结果。因此,该研究结果表明,这些类黄酮可被视为针对猴痘病毒的潜在胸苷激酶抑制剂。