【摘要】：目的:從瑤藥葫蘆鉆中篩選出具有α-葡萄糖苷酶抑制活性的有效部位。方法:將葫蘆鉆水提物依次用石油醚、乙酸乙酯、正丁醇萃取得到不同極性部位,分別測定各部位對α-葡萄糖苷酶的抑制活性,并對篩選出的活性強(qiáng)且得率相對較高的部位進(jìn)行酶抑制動力學(xué)研究;考察各部位對葡萄糖、蔗糖和淀粉負(fù)荷小鼠血糖值的影響(以阿卡波糖片為陽性對照)。結(jié)果:體外酶活性抑制試驗(yàn)顯示,葫蘆鉆乙酸乙酯部位[得率為0.40%、酶活性抑制率為(72.90±2.85)%]具有較強(qiáng)的α-葡萄糖苷酶抑制活性,且呈現(xiàn)出劑量依賴的快速非競爭性可逆抑制類型。體內(nèi)耐糖量實(shí)驗(yàn)結(jié)果表明,阿卡波糖片和葫蘆鉆各部位對葡萄糖負(fù)荷小鼠的血糖值均沒有影響(P0.05),而阿卡波糖片和葫蘆鉆乙酸乙酯部位能降低蔗糖負(fù)荷小鼠30、60 min的血糖值以及淀粉負(fù)荷小鼠30、60、120min的血糖值(P0.05或P0.01)。結(jié)論:乙酸乙酯部位是瑤藥葫蘆鉆中α-葡萄糖苷酶抑制活性的有效部位。
[Abstract]:Objective: to screen the effective fractions with 偽-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 偽-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 鹵2.85)%] had a strong 偽-glucosidase inhibitory activity, and the inhibition rate was (72.90 鹵2.85)%, and the inhibition rate was (72.90 鹵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 偽-glucosidase inhibitory activity in gourd drills.
【作者單位】： 桂林醫(yī)學(xué)院藥學(xué)院;
【基金】：桂林醫(yī)學(xué)院高層次人才科研啟動項(xiàng)目(No.KY2014016)
【分類號】：R29

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