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从阿育吠陀药用植物中通过计算机辅助发现用于治疗阿尔茨海默病的双靶点化合物。

Computer-aided discovery of dual-target compounds for Alzheimer's from ayurvedic medicinal plants.

作者信息

Shah Mohibullah, Pervaiz Sadia, Ahmad Iqra, Ansari Shahid Habib, Junior Valdir Ferreira De Paula, Ahmed Sibtain, Khan Muhammed Umer, Fawy Khaled Fahmi, Nishan Umar, Dib Hanna, Abdelfattah Mohamed A O

机构信息

Department of Biochemistry, Bahauddin Zakariya University, Multan, Pakistan.

Department of Animal Science, Federal University of Ceara, Fortaleza, Brazil.

出版信息

PLoS One. 2025 Jun 25;20(6):e0325441. doi: 10.1371/journal.pone.0325441. eCollection 2025.

Abstract

Alzheimer's disease (AD) is a neurodegenerative disorder characterized by cognitive decline, driven by the accumulation of amyloid-beta plaques and neurofibrillary tangles. It involves the dysfunction of key enzymes such as Acetylcholinesterase (AChE) and β-secretase (BACE1), making them critical targets for therapeutic intervention. In this study we investigated an in-house library of 820 secondary metabolites obtained from Ayurvedic plants against AChE and BACE1 with the aim to discover novel leads for AD. Virtual screening resulted in 15 ligands, mostly belonging to the ursane-type or dammarene-type triterpene saponins of Centella asiatica, reestablishing the potency of this plant in drug discovery against AD. The binding affinities were further verified by molecular dynamics (MD) simulation trajectories, including root mean square fluctuations (RMSF), root mean square deviation (RMSD), hydrogen bonding analysis, Coulomb interaction calculation, Lennard-Jones interactions, and the total interaction energy. Moreover, extensive Principal Component Analysis (PCA) and Gibbs free energy landscape were performed. Our results demonstrated three compounds, namely (S)-eriodictyol 7-O-(6-β-O-trans-p-coumaroyl)-β-d-glucopyranoside, sitoindoside-X and 1,5-di-o-caffeoyl quinic acid as more effective in treating AD due to their comparable drug-like properties. Drug-likeness, structural chemistry, pharmacophore, and ADMET (Absorption, Distribution, Metabolism, Excretion, and Toxicity) analysis support their potential for future drug development. To establish the effectiveness of these lead compounds against AD, additional experimental testing should be performed.

摘要

阿尔茨海默病(AD)是一种神经退行性疾病,其特征为认知能力下降,由β-淀粉样蛋白斑块和神经原纤维缠结的积累所驱动。它涉及乙酰胆碱酯酶(AChE)和β-分泌酶(BACE1)等关键酶的功能障碍,使其成为治疗干预的关键靶点。在本研究中,我们研究了一个从阿育吠陀植物中获得的包含820种次生代谢产物的内部文库对AChE和BACE1的作用,旨在发现针对AD的新型先导化合物。虚拟筛选产生了15种配体,大多属于积雪草的乌苏烷型或达玛烷型三萜皂苷,重新确立了这种植物在AD药物发现中的潜力。通过分子动力学(MD)模拟轨迹进一步验证了结合亲和力,包括均方根波动(RMSF)、均方根偏差(RMSD)、氢键分析、库仑相互作用计算、 Lennard-Jones相互作用以及总相互作用能。此外,还进行了广泛的主成分分析(PCA)和吉布斯自由能景观分析。我们的结果表明,三种化合物,即(S)-圣草酚7-O-(6-β-O-反式-对香豆酰基)-β-D-吡喃葡萄糖苷、积雪草苷-X和1,5-二-O-咖啡酰奎宁酸,因其具有类似药物的性质,在治疗AD方面更有效。药物相似性、结构化学、药效团和ADMET(吸收、分布、代谢、排泄和毒性)分析支持它们在未来药物开发中的潜力。为了确定这些先导化合物对AD的有效性,应进行额外的实验测试。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e26b/12193798/6c34ae62219c/pone.0325441.g001.jpg

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