摘要
白藜芦醇因具有广泛的生物活性而备受重视,有报道称白藜芦醇有降血糖的功效。α-葡萄糖苷酶抑制剂能够降低血糖含量,有效防治Ⅱ型糖尿病。因此,为了确定白藜芦醇的降血糖机制,研究白藜芦醇与α-葡萄糖苷酶活性的关系,本研究采用分光光度法测定α-葡萄糖苷酶活力,采用双倒数作图法研究白藜芦醇的酶抑制动力学,并采用对接模拟方法对白藜芦醇与α-葡萄糖苷酶的结合模式进行探讨。结果表明:白藜芦醇非竞争性地抑制α-葡萄糖苷酶活性,且有较强的抑制作用,半抑制浓度(half maximal inhibitory concentration,IC50)为5.047μmol/L,抑制常数为5.743μmol/L,明显强于阳性对照阿卡波糖(IC50=632.6μmol/L);对接模拟结果表明其与α-葡萄糖苷酶有多种可能的结合模式,且都不影响阿卡波糖与α-葡萄糖苷酶的结合。因此,白藜芦醇有被开发为降糖药物的潜力,也可作为膳食补充剂发挥一定的降血糖功效。
Due to its extensive biological activities such as hypoglycemic effects, resveratrol has gained much attention.Besides,α-glucosidase inhibitors can decrease hyperglycemia, which is closely related to the treatment of type-2 diabetes.In the present study, enzyme-inhibitory kinetics and computer simulation were applied to investigate the effect of resveratrol on the activity of α-glucosidase. The activity of α-glucosidase was measured by spectrophotometry, the inhibition kinetics was investigated using Lineweaver-Burk method, and the binding mechanisms between resveratrol and α-glucosidase were explored using molecular docking simulation. The results indicated that resveratrol was a stronger inhibitor(half maximal inhibitory concentration(IC50)= 5.047 μmol/L) than acarbose(IC50 = 632.6 μmol/L). The inhibition type was noncompetitive, and the value of Ki was 5.743 μmol/L. Molecular docking results demonstrated that the existence of multiple binding modes between resveratrol and α-glucosidase did not affect the binding interaction between acarbose andα-glucosidase. Therefore, resveratrol had potent inhibitory activity against α-glucosidase, and thus had the potential to be developed as an antidiabetic drug or as a dietary supplement in a synergetic manner with acarbose for the treatment of diabetes.
作者
姜丽丽
张中民
陈道玉
王珍
薛宏宇
刘勇
JIANG Lili;ZHANG Zhongmin;CHEN Daoyu;WANG Zhen;XUE Hongyu;LIU Yong(School of Life Science and Medicine, Dalian University of Technology, Panjin 124221, China)
出处
《食品科学》
EI
CAS
CSCD
北大核心
2019年第11期70-74,共5页
Food Science
基金
辽宁省自然科学基金(博士启动基金)项目(201601033)
