摘要
目的探讨刺五加提取物对α-葡萄糖苷酶的抑制作用及其机制。方法通过体外酶活性抑制实验测定半数最大抑制浓度(IC_(50)),结合酶动力学和荧光光谱法分析抑制类型与相互作用方式,并进行热力学分析。结果刺五加提取物对α-葡萄糖苷酶表现出明显的剂量依赖性抑制作用(IC_(50)为0.86 mg·m L^(-1)),属于非竞争性为主的混合型抑制;荧光光谱显示其通过动态淬灭引起酶构象变化;热力学结果显示主要作用力为疏水作用。结论刺五加提取物通过构象改变和疏水作用抑制α-葡萄糖苷酶,具潜在降糖应用价值。
Objective To investigate the inhibitory effect and underlying mechanism of Eleutherococcus senticosus extract onα-glucosidase.Methods The half-maximal inhibitory concentration(IC_(50))was determined using in vitro enzyme inhibition assays.Enzyme kinetics and fluorescence spectroscopy were employed to analyze the inhibition type,interaction mechanism,and thermodynamic parameters.Results E.senticosus extract exhibited a dose-dependent inhibitory effect onα-glucosidase,with an IC_(50)value of 0.86 mg·mL^(-1).The inhibition was characterized as predominantly mixed-type with a non-competitive component.Fluorescence spectroscopy revealed that the extract induced conformational changes in the enzyme through dynamic quenching.Thermodynamic analysis indicated that hydrophobic interactions were the main driving force.Conclusion E.senticosus extract inhibitsα-glucosidase through conformational modulation and hydrophobic interactions,suggesting its potential application in blood glucose regulation.
作者
闫琳
倪天凤
陈小强
张莹
YAN Lin;NI Tianfeng;CHEN Xiaoqiang;ZHANG Ying(College of Chemistry,Chemical Engineering and Resource Utilization,Northeast Forestry University,Harbin 150040,China;Key Laboratory of Forest Plant Ecology,Ministry of Education,Northeast Forestry University,Harbin 150040,China;College of Resources and Environment,Xizang Agricultural&Animal Husbandry University,Nyingchi 860000,China;Engineering Research Centre of Forest Bio-preparation,Ministry of Education,Northeast Forestry University,Harbin 150040,China;Heilongjiang Provincial Key Laboratory of Ecological Utilization of Forestry-based Active Substances,Harbin 150040,China;National Engineering Laboratory of Bioresource Eco Utilization,Harbin 150040,China)
出处
《药学研究》
2026年第2期134-140,共7页
Journal of Pharmaceutical Research
基金
东北林业大学大学生创新训练计划项目(No.202310225478)。
关键词
刺五加
Α-葡萄糖苷酶
动力学分析
荧光光谱
降糖活性
Eleutherococcus senticosus
α-glucosidase
Kinetic analysis
Fluorescence spectroscopy
Hypoglycemic activity
