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喜马拉雅生物活性分子作为人类免疫缺陷病毒的潜在进入抑制剂。

Himalayan bioactive molecules as potential entry inhibitors for the human immunodeficiency virus.

机构信息

Structural Bioinformatics Lab, CSIR-Institute of Himalayan Bioresource Technology (CSIR-IHBT), Palampur, HP, 176061, India; Biotechnology Division, CSIR-IHBT, Palampur, HP, 176061, India; Academy of Scientific & Innovative Research (AcSIR), CSIR-IHBT Campus, Palampur, HP, 176061, India.

Structural Bioinformatics Lab, CSIR-Institute of Himalayan Bioresource Technology (CSIR-IHBT), Palampur, HP, 176061, India; Biotechnology Division, CSIR-IHBT, Palampur, HP, 176061, India; Academy of Scientific & Innovative Research (AcSIR), CSIR-IHBT Campus, Palampur, HP, 176061, India.

出版信息

Food Chem. 2021 Jun 15;347:128932. doi: 10.1016/j.foodchem.2020.128932. Epub 2020 Dec 27.

Abstract

The human immunodeficiency virus interacts with the cluster of differentiation 4 receptors and one of the two chemokine receptors (CCR5 and CXCR4) to gain entry in human cells. Both the co-receptors are essential for viral entry, replication, and are considered critical targets for antiviral drugs. In this study, bioactive molecules from different Himalayan plants were screened considering their potential to bind with the CCR5 and CXCR4 co-receptors. We utilized computational and thermodynamic parameters to validate the binding of the selected biomolecules to the active site of the co-receptors. The molecules Butyl 2-ethylhexyl phthalate and Dactylorhin-A showed a higher binding affinity with CCR5 co-receptor than the standard antagonist Maraviroc. Moreover, Pseudohypericin, Amarogentin, and Dactylorhin-E exhibited stronger interactions with CXCR4 than the co-crystallized inhibitor Isothiourea-1 t. Hence, we suggest that these molecules could be developed as potential inhibitors of the CCR5 and CXCR4 co-receptors. However, this require further in-vitro and in-vivo validation.

摘要

人类免疫缺陷病毒(HIV)通过与分化群 4 受体(CD4)和两个趋化因子受体(CCR5 和 CXCR4)中的一个相互作用,进入人体细胞。这两种辅助受体对于病毒进入、复制都是必不可少的,被认为是抗逆转录病毒药物的关键靶点。在这项研究中,考虑到它们与 CCR5 和 CXCR4 辅助受体结合的潜力,对来自不同喜马拉雅植物的生物活性分子进行了筛选。我们利用计算和热力学参数来验证所选生物分子与辅助受体活性位点的结合。分子邻苯二甲酸丁基 2-乙基己酯和地胆草素-A 与 CCR5 辅助受体的结合亲和力高于标准拮抗剂马拉维若。此外,伪金丝桃素、当药苦苷和地胆草素-E 与 CXCR4 的相互作用比共结晶抑制剂异硫脲-1-t 更强。因此,我们认为这些分子可以开发为 CCR5 和 CXCR4 辅助受体的潜在抑制剂。然而,这需要进一步的体外和体内验证。

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