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过氧化物酶体增殖物激活受体γ(PPARγ)与摩洛哥药用植物中植物化学物质的分子对接分析

Molecular docking analysis of PPARγ with phytochemicals from Moroccan medicinal plants.

作者信息

Elkhattabi Lamiae, Zouhdi Salwa, Moussetad Fairouz, Kettani Anass, Barakat Abdelhamid, Saile Rachid

机构信息

Laboratory of Biology and Health, Faculty of Sciences Ben M'Sik, Hassan II University of Casablanca, Morocco.

Laboratory of Genomics and Human Genetics, Institut Pasteur du Maroc, Casablanca.

出版信息

Bioinformation. 2023 Jul 31;19(7):795-806. doi: 10.6026/97320630019795. eCollection 2023.

Abstract

PPARγ agonists play a crucial role in regulating metabolic homeostasis for treating type-2 diabetes (T2D). Due to the adverse side effects associated with thiazolidinediones, a class of PPARγ agonists, there is a growing interest in identifying natural compounds from medicinal plants that have the potential to bind PPARγ. In this study, we extensively investigated Moroccan phytochemicals using computational structure-based screening with the crystal structure of the PPARγ ligand-binding domain (PDB ID: 7awc) to discover novel phytochemicals targeting PPARγ. The docking results of 540 Moroccan phytochemicals were integrated into online databases for further exploitation through in-depth studies. Drug-likeness analysis was performed to assess the phytochemicals drug-like properties. Two promising phytochemicals, 3,4-dicaffeoylquinic acid and Chlorogenic acid, were identified, both exhibiting high docking affinity and unique binding site interactions compared to the established PPARγ full agonist, rosiglitazone. Molecular dynamics simulations of 100 ns were conducted to examine the stability of the complexes formed by both compounds within the PPARγ active site, and their dynamic behavior was compared to the reference structure of PPARγ alone and with rosiglitazone. Binding free energy calculations demonstrated that 3,4-dicaffeoylquinic acid and Chlorogenic acid exhibited higher binding free energy than the reference agonist, suggesting their potential as candidates for experimental validation in future drug discovery efforts targeting PPARγ for the treatment of T2D and metabolic syndrome.

摘要

过氧化物酶体增殖物激活受体γ(PPARγ)激动剂在调节代谢稳态以治疗2型糖尿病(T2D)中起着关键作用。由于噻唑烷二酮类(一类PPARγ激动剂)存在不良副作用,人们越来越有兴趣从药用植物中鉴定出具有结合PPARγ潜力的天然化合物。在本研究中,我们利用基于结构的计算筛选方法,结合PPARγ配体结合域的晶体结构(蛋白质数据银行编号:7awc),对摩洛哥植物化学物质进行了广泛研究,以发现靶向PPARγ的新型植物化学物质。540种摩洛哥植物化学物质的对接结果被整合到在线数据库中,以便通过深入研究进一步开发利用。进行了类药性质分析以评估植物化学物质的类药特性。鉴定出两种有前景的植物化学物质,3,4 - 二咖啡酰奎宁酸和绿原酸,与已确立的PPARγ完全激动剂罗格列酮相比,它们都表现出高对接亲和力和独特的结合位点相互作用。进行了100纳秒的分子动力学模拟,以检查这两种化合物在PPARγ活性位点形成的复合物的稳定性,并将它们的动态行为与单独的PPARγ以及与罗格列酮的参考结构进行比较。结合自由能计算表明,3,4 - 二咖啡酰奎宁酸和绿原酸表现出比参考激动剂更高的结合自由能,这表明它们有潜力作为未来针对PPARγ治疗T2D和代谢综合征的药物发现实验验证的候选物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b437/10605085/496edd61f4e1/97320630019795F1.jpg

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