基于结构从 Azadirachta indica 中发现可作为曼氏血吸虫硫氧还蛋白谷胱甘肽还原酶潜在抑制剂的植物化合物

IF 1.8 4区 生物学 Q4 BIOCHEMISTRY & MOLECULAR BIOLOGY Cell Biochemistry and Biophysics Pub Date : 2024-10-07 DOI:10.1007/s12013-024-01577-2
Olugbenga Samson Onile, Omotara Raji, Victor Omoboyede, Adeyinka Ignatius Fadahunsi, Tolulope Adelonpe Onile, Abdul Onoruoiza Momoh, Samuel Olukunle, Hassan Nour, Samir Chtita
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引用次数: 0

摘要

血吸虫病是一种由血吸虫、曼氏血吸虫和日本血吸虫等血吸虫引起的寄生虫病,给全球健康造成了巨大负担。硫氧还蛋白谷胱甘肽还原酶(TGR)对维持寄生虫的氧化还原平衡和防止氧化应激至关重要,已被确定为有希望开发抗血吸虫药物的靶点。本研究旨在利用分子建模方法从 Azadirachta indica 植物化学物质中找出潜在的 TGR 抑制剂。我们通过分子对接筛选了 60 种从苘麻树皮和叶子中提取的化合物,以评估它们的结合亲和力,然后评估了最有希望的候选化合物的无结合能。评估了药物相似性和药代动力学特性,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,与标准药物吡喹酮相比(-4.349 kcal/mol),几种 A. indica 化合物的对接得分明显较低(高达 -9.669 kcal/mol)。值得注意的是,异鼠李素、异鼠李酮、宁巴黄酮、槲皮素和宁巴酚与 TGR 的相互作用很强,但异鼠李素显示出潜在的诱变性。进一步的结合自由能计算和分子动力学模拟证实了异鼠李酮、宁波黄酮和槲皮素作为潜在的 TGR 抑制剂的稳定性。总之,这些研究结果表明,异麦角酮、宁波诺尔和槲皮素作为抗血吸虫病治疗的候选药物,值得进一步进行实验验证。
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Structure-Based Discovery of Phytocompounds from Azadirachta indica as Potential Inhibitors of Thioredoxin Glutathione Reductase in Schistosoma mansoni.

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.

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来源期刊
Cell Biochemistry and Biophysics
Cell Biochemistry and Biophysics 生物-生化与分子生物学
CiteScore
4.40
自引率
0.00%
发文量
72
审稿时长
7.5 months
期刊介绍: Cell Biochemistry and Biophysics (CBB) aims to publish papers on the nature of the biochemical and biophysical mechanisms underlying the structure, control and function of cellular systems The reports should be within the framework of modern biochemistry and chemistry, biophysics and cell physiology, physics and engineering, molecular and structural biology. The relationship between molecular structure and function under investigation is emphasized. Examples of subject areas that CBB publishes are: · biochemical and biophysical aspects of cell structure and function; · interactions of cells and their molecular/macromolecular constituents; · innovative developments in genetic and biomolecular engineering; · computer-based analysis of tissues, cells, cell networks, organelles, and molecular/macromolecular assemblies; · photometric, spectroscopic, microscopic, mechanical, and electrical methodologies/techniques in analytical cytology, cytometry and innovative instrument design For articles that focus on computational aspects, authors should be clear about which docking and molecular dynamics algorithms or software packages are being used as well as details on the system parameterization, simulations conditions etc. In addition, docking calculations (virtual screening, QSAR, etc.) should be validated either by experimental studies or one or more reliable theoretical cross-validation methods.
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