刺果番荔枝果实乙醇提取物抑制α⁃葡萄糖苷酶治疗2型糖尿病的实验研究  

Ethanol extract of Annona muricata Linn fruit perform antidiabetic effect on type 2 diabetic mice throughα⁃glucosidase inhibition

作　　者：秦海龙 姚佳惠 王燕 许奇鹏 刘征 李友宾[1] 龚晶雯 QIN Hai-long;YAO Jia-hui;WANG Yan;XU Qi-peng;LIU Zheng;LI You-bin;GONG Jing-wen(Hainan Provincial Key Laboratory for Research and Development of Tropical Herbs,Key Laboratory of Tropical Translational Medicine of Ministry of Education,Haikou Key Laboratory of Li Nationality Medicine,School of Pharmacy,Hainan Medical University,Haikou 571100,China)

机构地区：[1]海南省热带药用植物研究开发重点实验室,热带转化医学教育部重点实验室,海口市黎族医药重点实验室,海南医学院药学院,海南海口571100

出　　处：《海南医学院学报》2023年第7期481-487,共7页Journal of Hainan Medical University

基　　金：国家自然科学基金面上项目资助(81460591);2020年大学生创新创业训练计划项目(X202011810069)。

摘　　要：目的:研究95%乙醇回流提取的刺果番荔枝果实提取物(AME)治疗2型糖尿病作用以及可能的机制。方法:利用链脲佐菌素诱发ICR小鼠建立2型糖尿病,随机分组,分别给予50 mg/kg阿卡波糖或者AME(200、100和50 mg/kg),连续给药4周。每周测定小鼠体重、餐后血糖水平。第3周测定糖化血红蛋白水平。给药结束后进行OGTT实验,检测血清生化指标。通过酶抑制实验测定AME对体内外α⁃葡萄糖苷酶抑制活性和选择性。结果:AME能控制2型糖尿病小鼠的体重增长,显著降低餐后血糖、糖化血红蛋白及低密度脂蛋白水平,增强小鼠机体糖耐受的能力;非竞争性抑制小鼠肠道内α⁃葡萄糖苷酶活性。结论:AME可能非竞争性抑制α⁃葡萄糖苷酶活性以控制机体对餐后葡萄糖摄入,发挥2型糖尿病治疗作用。Objective:To explore the anti⁃diabetic effects and its underlying mechanism of Annona muricata Linn fruit eth⁃anol extract(AME).Methods:Streptozotocin⁃induced type 2 diabetic(T2DM)mouse model was constructed.Those diabetic mice were randomly grouped and given 50 mg/kg acarbose or AME(200 mg/kg,100 mg/kg or 50 mg/kg)for four weeks.The body weight,postprandial blood glucose and glycosylated hemoglobin levels were measured during the administration.After the administration,a glucose tolerance test was performed,and the levels of triglycerides,cholesterol and low⁃density lipoproteins in mice were detected by biochemical test kits.The inhibitory activity of AME onα⁃glucosidase in vivo and in vitro was determined by enzyme inhibition tests.Results:AME significantly reduced weight gain,postprandial blood glucose,glycosylated hemoglobin low⁃density lipoprotein levels in T2DM mice;enhanced glucose tolerance and pancreaticβ⁃cell function of T2DM mice;inhib⁃itedα⁃glucosidase activity in mouse intestine in an noncompetitive manner.Conclusion:AME may noncompetitive inhibitα⁃gluco⁃sidase activity and reduce postprandial glucose intake to achieve a therapeutic and regulatory effect on type 2 diabetes.

关 键 词：刺果番荔枝 2型糖尿病 α⁃葡萄糖苷酶 餐后血糖 

分 类 号：R285.5[医药卫生—中药学]