Ghate Sudeep D, Pinto Larina, Alva Shivakiran, Srinivasa Mahendra Gowdru, Vangala Rajani Kanth, Naik Prashantha, Revanasiddappa B C, Rao R Shyama Prasad
Center for Bioinformatics, NITTE Deemed to be University, Mangaluru, 575018, India.
Central Research Laboratory, KS Hegde Medical Academy, NITTE Deemed to be University, Mangaluru, 575018, India.
Mol Divers. 2024 Dec;28(6):4067-4086. doi: 10.1007/s11030-023-10797-2. Epub 2024 Mar 22.
The mpox virus (MPXV), a member of the Poxviridae family, which recently appeared outside of the African continent has emerged as a global threat to public health. Given the scarcity of antiviral treatments for mpox disease, there is a pressing need to identify and develop new therapeutics. We investigated 5715 phytochemicals from 266 species available in IMMPAT database as potential inhibitors for six MPXV targets namely thymidylate kinase (A48R), DNA ligase (A50R), rifampicin resistance protein (D13L), palmytilated EEV membrane protein (F13L), viral core cysteine proteinase (I7L), and DNA polymerase (E9L) using molecular docking. The best-performing phytochemicals were also subjected to molecular dynamics (MD) simulations and in silico ADMET analysis. The top phytochemicals were forsythiaside for A48R, ruberythric acid for A50R, theasinensin F for D13L, theasinensin A for F13L, isocinchophyllamine for I7L, and terchebin for E9L. Interestingly, the binding energies of these potential phytochemical inhibitors were far lower than brincidofovir and tecovirimat, the standard drugs used against MPXV, hinting at better binding properties of the former. These findings may pave the way for developing new MPXV inhibitors based on natural product scaffolds. However, they must be further studied to establish their inhibitory efficacy and toxicity in in vitro and in vivo models.
猴痘病毒(MPXV)是痘病毒科的成员,最近在非洲大陆以外出现,已成为对公共卫生的全球威胁。鉴于针对猴痘疾病的抗病毒治疗药物稀缺,迫切需要识别和开发新的治疗方法。我们使用分子对接技术,研究了IMMPAT数据库中266种植物的5715种植物化学物质,作为六种MPXV靶点的潜在抑制剂,这六个靶点分别是胸苷酸激酶(A48R)、DNA连接酶(A50R)、利福平抗性蛋白(D13L)、棕榈酰化胞外病毒包膜蛋白(F13L)、病毒核心半胱氨酸蛋白酶(I7L)和DNA聚合酶(E9L)。对表现最佳的植物化学物质还进行了分子动力学(MD)模拟和计算机辅助药物代谢动力学、药物毒性及药物活性预测分析(ADMET)。针对A48R的最佳植物化学物质是连翘酯苷,针对A50R的是红玉红酸,针对D13L的是茶黄素F,针对F13L的是茶黄素A,针对I7L的是异辛可芬胺,针对E9L的是特切宾。有趣的是,这些潜在植物化学抑制剂的结合能远低于用于治疗MPXV的标准药物布林西多福韦和替考韦玛,这表明前者具有更好的结合特性。这些发现可能为基于天然产物支架开发新的MPXV抑制剂铺平道路。然而,必须对它们进行进一步研究,以确定其在体外和体内模型中的抑制效果和毒性。