用于治疗 2 型糖尿病的黄酮类化合物的α-淀粉酶和α-葡萄糖苷酶抑制活性的硅学筛选

Bui Thanh Tung, Le Thi Huong, Trinh Thi Duong, Nguyen Thi Huyen, Nguyễn Thi Thuy
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引用次数: 0

摘要

α-葡萄糖苷酶和α-淀粉酶是一种酶,在淀粉和碳水化合物的水解过程中发挥着重要作用。它们与血糖水平的升高和降低有关。类黄酮是一类常见的天然化合物,已被证明具有许多有益健康的作用。本研究采用分子对接方法和类药物标准,预测药代动力学-毒性(ADMET)来筛选和评估治疗 2 型糖尿病的潜在类黄酮化合物。经过筛选,我们得到了 46 个结合能低于阳性对照阿卡波糖的化合物。利用利宾斯基的五人法则,我们评估了化合物的药物相似性,并确定了 12 个符合标准的化合物。然后,继续根据药代动力学和毒理学参数(ADMET)进行分析,我们得到了包括高良姜素、马偕素和堇菜素在内的 3 个化合物,这些化合物具有同时抑制α-葡萄糖苷酶和α-淀粉酶两种酶的能力,并具有以下积极特性:结合能低于对照组,在活性位点与靶蛋白产生许多相互作用,具有药物样特性,药代动力学特性相对较好,毒性较低,具有开发成药物的潜力。因此,要将这些潜在化合物开发成治疗 2 型糖尿病的药物,还需要进一步的体外和体内研究。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Screening In Silico Alpha-amylase and Alpha-glucosidase Inhibitory Activity of Flavonoid Compounds for the Treatment of Type 2 Diabetes
Diabetes mellitus (diabetes) is a chronic disease associated with metabolic disorders and hyperglycemia. α-glucosidase and α-amylase, which play an important role in the hydrolysis of starch and carbohydrates, are enzymes. They are related to the increase and decrease in blood glucose levels. Flavonoids are a common group of natural compounds that have been shown to have many beneficial health effects. This study used molecular docking methods and drug-like criteria, predicting pharmacokinetics-toxicity (ADMET) to screen and evaluate potential flavonoid compounds in the treatment of type 2 diabetes. After screening the compounds, we obtained 46 compounds with lower binding energies than the positive controls, which are acarbose. Using Lipinski's rule of five, we evaluated the drug-likeness of the compounds and identified 12 compounds that met the criteria. Then, continuing to analyze according to pharmacokinetic and toxicological parameters (ADMET), we obtained 3 compounds including Galangin, Maackiain, and Corylin, that have the potential to be developed into drugs when showing the ability to simultaneously inhibit both enzymes α-glucosidase and α-amylase have positive properties: binding energy is lower than the control, creates many interactions with target proteins in the active site, has drug-like properties, relatively good pharmacokinetic properties and low toxicity. Therefore, further in vitro and in vivo studies are needed to develop these potential compounds into drugs for the treatment of type 2 diabetes.        
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