Department of Botany, Islamia College University, Peshawar 25000, Pakistan.
Department of Chemistry, University of Malakand, Upper Dir 23050, Pakistan.
Molecules. 2019 Jan 24;24(3):427. doi: 10.3390/molecules24030427.
α-glucosidase is responsible for the hydrolysis of complex carbohydrates into simple absorbable glucose and causes postprandial hyperglycemia. α-glucosidase inhibition is thus the ideal target to prevent postprandial hyperglycemia. The present study was therefore designed to analyze the effects of various compounds isolated from against α-glucosidase including β-Sitosterol , β-Sitosterol3--β-d-glucopyranoside , 3, 5, 7-trihydroxy-2-(-tolyl) chorman-4-one , Quercetin-3-0-β-d-glucopyranoside (3→0-3)- β-d- Quercetin -3-0- β ⁻d-galactopyranoside and 5, 7, 4-Trihydroxyflavon-3-glucopyranoid 5. The in vitro spectrophotometric method was used for the analysis of test compounds against possible inhibition. Similarly, molecular docking studies were performed using the MOE software. These compounds showed concentration-dependent inhibition on α-glucosidase, and compounds (IC: 143 ± 0.47 µM), (IC:133 ± 6.90 µM) and (IC: 146 ± 1.93 µM) were more potent than the standard drug, acarbose (IC: 290 ± 0.54 µM). Computational studies of these compounds strongly supported the in vitro studies and showed strong binding receptor sensitivity. In short, the secondary metabolites isolated from demonstrated potent α-glucosidase inhibition that were supported by molecular docking with a high docking score.
α-葡萄糖苷酶负责将复杂碳水化合物水解成可吸收的简单葡萄糖,导致餐后高血糖。因此,抑制α-葡萄糖苷酶是预防餐后高血糖的理想靶点。本研究旨在分析从 中分离得到的各种化合物对α-葡萄糖苷酶的抑制作用,包括 β-谷甾醇、β-谷甾醇 3-O-β-D-吡喃葡萄糖苷、3,5,7-三羟基-2-(对甲苯基)查耳酮-4-酮、槲皮素-3-O-β-D-吡喃葡萄糖苷(3→0-3)-β-D-槲皮素-3-O-β-D-半乳糖吡喃糖苷和 5,7,4-三羟基黄酮-3-葡萄糖苷。采用分光光度法体外分析测试化合物对可能的抑制作用。同样,使用 MOE 软件进行了分子对接研究。这些化合物对α-葡萄糖苷酶表现出浓度依赖性抑制作用,化合物 (IC:143 ± 0.47 µM)、 (IC:133 ± 6.90 µM)和 (IC:146 ± 1.93 µM)比标准药物阿卡波糖(IC:290 ± 0.54 µM)更有效。这些化合物的计算研究强烈支持了体外研究,并显示出与受体结合的高灵敏度。总之,从 中分离得到的次生代谢产物表现出强烈的α-葡萄糖苷酶抑制作用,这得到了高对接分数的分子对接的支持。