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基于结构从印楝中发现植物化合物作为曼氏血吸虫硫氧还蛋白谷胱甘肽还原酶的潜在抑制剂

Structure-Based Discovery of Phytocompounds from Azadirachta indica as Potential Inhibitors of Thioredoxin Glutathione Reductase in Schistosoma mansoni.

作者信息

Onile Olugbenga Samson, Raji Omotara, Omoboyede Victor, Fadahunsi Adeyinka Ignatius, Onile Tolulope Adelonpe, Momoh Abdul Onoruoiza, Olukunle Samuel, Nour Hassan, Chtita Samir

机构信息

Biotechnology Programme, Department of Biological Sciences, Elizade University, P.M.B 002, Ilara-Mokin, Ondo State, Nigeria.

Department of Biochemistry, School of Life Sciences (SLS), Federal University of Technology Akure, P.M.B 704, Akure, Nigeria.

出版信息

Cell Biochem Biophys. 2025 Jun;83(2):1677-1688. doi: 10.1007/s12013-024-01577-2. Epub 2024 Oct 7.

Abstract

Schistosomiasis, a parasitic disease caused by Schistosoma species such as S. haematobium, S. mansoni, and S. japonicum, poses a significant global health burden. The thioredoxin glutathione reductase (TGR) enzyme, crucial for maintaining the parasite's redox balance and preventing oxidative stress, has been identified as a promising target for anti-schistosomal drug development. This study aims to identify potential TGR inhibitors from Azadirachta indica phytochemicals using molecular modeling approaches. We screened 60 compounds derived from A. indica bark and leaves through molecular docking to assess their binding affinity, followed by the evaluation of binding-free energies for the most promising candidates. Drug-likeness and pharmacokinetic properties were assessed, and molecular dynamics simulations were conducted to explore the conformational stability of the protein-ligand complexes. Our findings revealed that several A. indica compounds exhibited significantly lower docking scores (up to -9.669 kcal/mol) compared to the standard drug praziquantel (-4.349 kcal/mol). Notably, Isorhamnetin, Isomargolonone, Nimbaflavone, Quercetin, and Nimbionol demonstrated strong interactions with TGR, although Isorhamnetin showed potential mutagenicity. Further binding free energy calculations and molecular dynamics simulations confirmed the stability of Isomargolonone, Nimbionol, and Quercetin as potential TGR inhibitors. In conclusion, these findings suggest that Isomargolonone, Nimbionol, and Quercetin warrant further experimental validation as promising candidates for anti-schistosomal therapy.

摘要

血吸虫病是一种由埃及血吸虫、曼氏血吸虫和日本血吸虫等血吸虫属寄生虫引起的寄生虫病,给全球健康带来了重大负担。硫氧还蛋白谷胱甘肽还原酶(TGR)酶对于维持寄生虫的氧化还原平衡和预防氧化应激至关重要,已被确定为抗血吸虫药物开发的一个有前景的靶点。本研究旨在使用分子建模方法从印楝植物化学物质中鉴定潜在的TGR抑制剂。我们通过分子对接筛选了60种从印楝树皮和树叶中提取的化合物,以评估它们的结合亲和力,随后对最有前景的候选物进行结合自由能评估。评估了药物相似性和药代动力学性质,并进行了分子动力学模拟以探索蛋白质-配体复合物的构象稳定性。我们的研究结果表明,与标准药物吡喹酮(-4.349 kcal/mol)相比,几种印楝化合物的对接分数显著更低(高达-9.669 kcal/mol)。值得注意的是,异鼠李素、异马戈洛酮、尼姆黄酮、槲皮素和尼姆比诺尔与TGR表现出强烈的相互作用,尽管异鼠李素显示出潜在的致突变性。进一步的结合自由能计算和分子动力学模拟证实了异马戈洛酮、尼姆比诺尔和槲皮素作为潜在TGR抑制剂的稳定性。总之,这些发现表明,异马戈洛酮、尼姆比诺尔和槲皮素作为抗血吸虫治疗的有前景候选物值得进一步的实验验证。

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