瑶药葫芦钻中α-葡萄糖苷酶抑制活性部位的筛选
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篇名: 瑶药葫芦钻中α-葡萄糖苷酶抑制活性部位的筛选
TITLE:
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(P>0.05),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、120 min的血糖值(P<0.05或P<0.01)。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 α-glucosidase inhibitory active part from Pothos chinensis. METHODS: The aqueous extractions of P. chinensis were extracted by petroleum, ethyl acetate, n-butyl alcohol in turn to obtain different polarparts. Effect of each part on α-glucosidase inhibitory activity was determined, and enzyme inhibition kinetics was conducted for the screened parts with strong activity and relatively high yield rate; effects of each part on blood glucose level of mice loaded with glucose, sucrose and starch were respectively determined (using Acacoside tablet as positive control). RESULTS: Enzyme inhibition kinetics in vitro showed the ethyl acetate part [yield rate was 0.40%, enzyme activity inhibition rate was (72.90±2.85)%] had strong α-glucosidase inhibitory activity and showed a dose-dependent, fast, non-competitive and reversible model. Results of in vivo glucose tolerance indicated that Acacoside tablet and each part of P. chinensis had no effects on blood glucose level of glucose-loaded mice (P>0.05); while Acacoside tablet and ethyl acetate part in P. chinensis could reduce 30, 60 min blood glucose level of sucrose-loaded mice and 30, 60, 120 min blood glucose level of starch-loaded mice (P<0.05 or P<0.01). CONCLUSIONS: Ethyl acetate part is the α-glucosidase inhibitory active part from Yao medicine P. chinensis.
期刊: 2017年第28卷第16期
作者: 许有瑞,伊辉,张可锋,廖迎#,林家逊,段小群
AUTHORS: XU Yourui,YI Hui,ZHANG Kefeng,LIAO Ying,LIN Jiaxun,DUAN Xiaoqun
关键字: 瑶药;葫芦钻;α-葡萄糖苷酶抑制剂;不同极性部位;小鼠;耐糖量实验
KEYWORDS: Yao medicine; Pothos chinensis; α-glucosidase inhibitor; Different polar parts; Mice; Glucose tolerance test
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