Islam Md Tarikul, Aktaruzzaman Md, Saif Ahmed, Akter Ayesha, Bhat Mashooq Ahmad, Hossain Mirza Mahfuj, Alam S M Nur, Rayhan Rifat, Rehman Saira, Yaseen Muhammad, Raihan Md Obayed
Department of Genetic Engineering and Biotechnology, Jashore University of Science and Technology, Jashore, 7408, Bangladesh.
Department of Pharmacy, Faculty of Biological Science and Technology, Jashore University of Science and Technology, Jashore, 7408, Bangladesh.
Mol Biotechnol. 2025 Jun;67(6):2382-2398. doi: 10.1007/s12033-024-01204-8. Epub 2024 Jun 4.
Dengue fever (DF) is an endemic disease that has become a public health concern around the globe. The NS3 protease-helicase enzyme is an important target for the development of antiviral drugs against DENV (dengue virus) due to its impact on viral replication. Inhibition of the activity of the NS3 protease-helicase enzyme complex significantly inhibits the infection associated with DENV. Unfortunately, there are no scientifically approved antiviral drugs for its prevention. However, this study has been developed to find natural bioactive molecules that can block the activity of the NS3 protease-helicase enzyme complex associated with DENV infection through molecular docking, MM-GBSA (molecular mechanics-generalized born surface area), and molecular dynamics (MD) simulations. Three hundred forty-two (342) compounds selected from twenty traditional medicinal plants were retrieved and screened against the NS3 protease-helicase protein by molecular docking and MM-GBSA studies, where the top six phytochemicals have been identified based on binding affinities. The six compounds were then subjected to pharmacokinetics and toxicity analysis, and we conducted molecular dynamics simulations on three protein-ligand complexes to validate their stability. Through computational analysis, this study revealed the potential of the two selected natural bioactive inhibitors (CID-440015 and CID-7424) as novel anti-dengue agents.
登革热(DF)是一种地方病,已成为全球公共卫生关注的问题。NS3蛋白酶解旋酶是开发抗登革病毒(DENV)抗病毒药物的重要靶点,因为它对病毒复制有影响。抑制NS3蛋白酶解旋酶复合物的活性可显著抑制与登革病毒相关的感染。不幸的是,目前尚无经科学批准的预防该疾病的抗病毒药物。然而,本研究旨在通过分子对接、分子力学-广义玻恩表面面积法(MM-GBSA)和分子动力学(MD)模拟,寻找能够阻断与登革病毒感染相关的NS3蛋白酶解旋酶复合物活性的天然生物活性分子。从20种传统药用植物中筛选出342种化合物,通过分子对接和MM-GBSA研究对NS3蛋白酶解旋酶蛋白进行筛选,根据结合亲和力确定了前六种植物化学物质。然后对这六种化合物进行药代动力学和毒性分析,并对三种蛋白质-配体复合物进行分子动力学模拟,以验证其稳定性。通过计算分析,本研究揭示了两种选定的天然生物活性抑制剂(CID-440015和CID-7424)作为新型抗登革热药物的潜力。