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刺五加提取物对α-葡萄糖苷酶的抑制作用及酶动力学分析

Inhibitory effect of α-glucosidase by Eleutherococcus senticosus extract and enzyme kinetics analysis

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【作者】 闫琳倪天凤陈小强张莹

【Author】 YAN Lin;NI Tianfeng;CHEN Xiaoqiang;ZHANG Ying;College of Chemistry,Chemical Engineering and Resource Utilization,Northeast Forestry University;Key Laboratory of Forest Plant Ecology,Ministry of Education,Northeast Forestry University;College of Resources and Environment,Xizang Agricultural & Animal Husbandry University;Engineering Research Centre of Forest Bio-preparation,Ministry of Education,Northeast Forestry University;Heilongjiang Provincial Key Laboratory of Ecological Utilization of Forestry-based Active Substances;National Engineering Laboratory of Bioresource Eco Utilization;

【通讯作者】 陈小强;张莹;

【机构】 东北林业大学化学化工与资源利用学院东北林业大学森林植物生态学教育部重点实验室西藏农牧学院资源与环境学院东北林业大学生物资源生态利用国家地方联合工程实验室黑龙江省林业生物质功能材料重点实验室东北林业大学林业生物质资源高效利用教育部工程研究中心

【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(IC50),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(IC50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。

【Abstract】 Objective To investigate the inhibitory effect and underlying mechanism of Eleutherococcus senticosus extract on α-glucosidase.Methods The half-maximal inhibitory concentration( IC50) 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 on α-glucosidase,with an IC50value of 0.86 mg·m L-1.The inhibition was characterized as predominantly mixed-type with a noncompetitive 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 inhibits α-glucosidase through conformational modulation and hydrophobic interactions,suggesting its potential application in blood glucose regulation.

【基金】 东北林业大学大学生创新训练计划项目(No.202310225478)
  • 【文献出处】 药学研究 ,Journal of Pharmaceutical Research , 编辑部邮箱 ,2026年02期
  • 【分类号】R285
  • 【下载频次】99
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