瑶药葫芦钻中α-葡萄糖苷酶抑制活性部位的筛选

发布时间：2019-03-07 08:29

【摘要】：目的:从瑶药葫芦钻中筛选出具有α-葡萄糖苷酶抑制活性的有效部位。方法:将葫芦钻水提物依次用石油醚、乙酸乙酯、正丁醇萃取得到不同极性部位,分别测定各部位对α-葡萄糖苷酶的抑制活性,并对筛选出的活性强且得率相对较高的部位进行酶抑制动力学研究;考察各部位对葡萄糖、蔗糖和淀粉负荷小鼠血糖值的影响(以阿卡波糖片为阳性对照)。结果:体外酶活性抑制试验显示,葫芦钻乙酸乙酯部位[得率为0.40%、酶活性抑制率为(72.90±2.85)%]具有较强的α-葡萄糖苷酶抑制活性,且呈现出剂量依赖的快速非竞争性可逆抑制类型。体内耐糖量实验结果表明,阿卡波糖片和葫芦钻各部位对葡萄糖负荷小鼠的血糖值均没有影响(P0.05),而阿卡波糖片和葫芦钻乙酸乙酯部位能降低蔗糖负荷小鼠30、60 min的血糖值以及淀粉负荷小鼠30、60、120min的血糖值(P0.05或P0.01)。结论:乙酸乙酯部位是瑶药葫芦钻中α-葡萄糖苷酶抑制活性的有效部位。
[Abstract]:Objective: to screen the effective fractions with 伪-glucosidase inhibitory activity from the gourd drills of Yao medicine. Methods: the extracts were extracted with petroleum ether, ethyl acetate and n-butanol in turn, and their inhibitory activities on 伪-glucosidase were determined. The enzyme inhibition kinetics of the selected sites with strong activity and relatively high yield was studied. The effects of different parts on glucose, sucrose and starch-loaded mice blood glucose levels were investigated (using acarbose tablets as positive control). Results: the inhibition test of enzyme activity in vitro showed that the ethyl acetate fraction [yield was 0.40%, enzyme activity inhibition rate was (72.90 卤2.85)%] had a strong 伪-glucosidase inhibitory activity, and the inhibition rate was (72.90 卤2.85)%, and the inhibition rate was (72.90 卤2.85)%. A dose-dependent fast non-competitive reversible inhibition was found. The results of glucose tolerance test in vivo showed that the different parts of acarbose tablet and gourd drill had no effect on the blood glucose value of glucose-loaded mice (P0.05). The acarbose tablets and ethyl acetate fraction of Hulu drill decreased the sugar value of 30, 60 min and 30, 60120 min of starch loading mice (P0.05 or P0.01). 3. The results showed that Acarbose tablet and ethyl acetate fraction of Hulu drill could decrease the sugar value of mice under sucrose loading and starch loading (P0.05 or P0.01). Conclusion: ethyl acetate fraction is an effective part of 伪-glucosidase inhibitory activity in gourd drills.
【作者单位】：桂林医学院药学院;
【基金】：桂林医学院高层次人才科研启动项目(No.KY2014016)
【分类号】：R29

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