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圆叶接骨木成分的计算机分析及其作为人中性粒细胞弹性蛋白酶(HNE)、基质金属蛋白酶(MMP2 和 MMP9)和酪氨酸酶抑制剂的抑制作用。

In Silico Analysis of Cissus rotundifolia Constituents as Human Neutrophil Elastase (HNE), Matrix Metalloproteinases (MMP 2 and MMP 9), and Tyrosinase Inhibitors.

机构信息

Department of Biochemistry, St. Peter's Institute of Higher Education and Research (SPIHER), Avadi, Chennai, 54, Tamil Nadu, India.

Department of Biotechnology, St. Peter's Institute of Higher Education and Research (SPIHER), Avadi, Chennai, 54, India.

出版信息

Appl Biochem Biotechnol. 2022 Jan;194(1):232-245. doi: 10.1007/s12010-021-03758-8. Epub 2021 Nov 20.

Abstract

Cissus rotundifolia has been reported to possess various biological activities such as anti-diabetic, anti-fertility, anti-hyperlipidemic, anti-malarial, anti-osteoporotic, and anti-parasitic activities. Therefore in the present study, eleven selected constituents of Cissus rotundifolia which includes aconitic acid, astragalin, acteoside, aliospiroside A, beta amyrin, bergenin, formononetin, gallic acid, isovitexin, isoorientin, and isoquercitrin were studied on the docking behavior of human neutrophil elastase (HNE), matrix metalloproteinases (MMP 2 and MMP 9), and tyrosinase by using PatchDock method. Furthermore, molecular physicochemical, bioactivity score/drug-likeness, ADME (absorption, distribution, metabolism, and excretion), and toxicity analyses were also carried out using Molinspiration, Swiss ADME, and ProTox-II methods, respectively. The molecular physicochemical investigation showed that three ligands such as acteoside, aliospiroside A, and isoorientin have three violations for Lipinski's rule of five. Similarly, ADME analysis one ligand (formononetin) predicated to have high blood-brain barrier (BBB) permeability effect. The docking studies showed that isovitexin exhibited the highest atomic contact energy (-341.61 kcal/mol) for human neutrophil elastase (HNE), more over alliospiroside A has shown maximum atomic contact energy for both matrix metalloproteinases (MMP 2 [-618.00 kcal/mol] and MMP 9 [-634.73 kcal/mol]). Furthermore, isoquercitrin has exhibited the highest atomic contact energy (-145.70 kcal/mol) for tyrosinase. Thus, the present investigation outcome provides new knowledge in understanding eleven Cissus rotundifolia constituents as possible novel inhibitors against HNE, MMP 2, MMP 9, and tyrosinase.

摘要

圆叶葡萄被报道具有多种生物活性,如抗糖尿病、抗生育、抗高血脂、抗疟疾、抗骨质疏松和抗寄生虫活性。因此,在本研究中,对 11 种圆叶葡萄的选定成分,包括乌头酸、杨梅素、毛蕊花糖苷、阿里螺旋苷 A、β-香树脂醇、没食子酸、芒柄花苷、isovitexin、isoorientin、异槲皮苷,采用 PatchDock 方法研究了它们对人中性粒细胞弹性蛋白酶(HNE)、基质金属蛋白酶(MMP 2 和 MMP 9)和酪氨酸酶的对接行为。此外,还使用 Molinspiration、Swiss ADME 和 ProTox-II 方法分别进行了分子物理化学、生物活性评分/药物相似性、ADME(吸收、分布、代谢和排泄)和毒性分析。分子物理化学研究表明,三种配体,如毛蕊花糖苷、阿里螺旋苷 A 和异槲皮苷,有三个违反了 Lipinski 的五规则。同样,ADME 分析表明,一种配体(芒柄花苷)预测具有较高的血脑屏障(BBB)通透性。对接研究表明,异槲皮苷对人中性粒细胞弹性蛋白酶(HNE)表现出最高的原子接触能量(-341.61kcal/mol),此外,阿里螺旋苷 A 对基质金属蛋白酶(MMP 2 [-618.00kcal/mol]和 MMP 9 [-634.73kcal/mol])都表现出最大的原子接触能量。此外,异槲皮苷对酪氨酸酶表现出最高的原子接触能量(-145.70kcal/mol)。因此,本研究结果为理解 11 种圆叶葡萄成分作为可能的新型 HNE、MMP 2、MMP 9 和酪氨酸酶抑制剂提供了新的认识。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/70c0/8605470/13e48c4b0c7d/12010_2021_3758_Fig1_HTML.jpg

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