摘要
目的研究没食子酸对α-葡萄糖苷酶的抑制作用及其抑制类型,探索酚酸类化合物在治疗糖尿病方面的价值及Caco-2细胞模型在筛选降糖药方面的作用。方法以麦芽糖为底物,采用酶-抑制剂模型和Caco-2细胞模型研究没食子酸对α-葡萄糖苷酶活力的影响,采用Caco-2细胞模型研究没食子酸对葡萄糖吸收的影响。结果没食子酸对两种模型的α-葡萄糖苷酶均有抑制作用,半数抑制量(IC50)为577.5μg/mL和182.6μg/mL;250μg/mL的没食子酸对α-葡萄糖苷酶抑制作用低于同浓度的阿卡波糖(P<0.05)。没食子酸是α-葡萄糖苷酶的竞争型抑制剂。没食子酸对葡萄糖吸收有抑制作用。结论没食子酸对α-葡萄糖苷酶和葡萄糖吸收有一定抑制作用。Caco-2细胞模型在筛选降糖药方面具有重要意义。
Objective To investigate the α-glycosidase inhibition and inhibition type of gallic acid by using enzyme-inhibition model and Caco-2 cell model.To study the potential value of phenolic acid on treating diabetes and the meaning of Caco-2 cell model on screening antidiabetic drug.Methods Enzyme-inhibition model and Caco-2 cell model were used to study the influence of gallic acid on α-glycosidase activity.Otherwise,using Caco-2 cell model to study the effect of gallic acid on glucose absorption.Results When we made maltose as substrate,gallic acid displayed α-glycosidase inhibition on enzyme-inhibition model,the IC50 was 577.5 μg/mL;Gallic acid also had α-glycosidase inhibition on Caco-2 cell model,its IC50 was 182.6 μg/mL.The α-glycosidase inhibition of 250 μg/mL gallic acid was lower than the same concentration of acarbose（P 0.05）.Gallic acid is a competitive inhibitor for α-glycosidase.At the same time,gallic acid inhibited glucose absorption.Conclusion Gallic acid is a α-glycosidase inhibitor,and the traditional Chinese medicines which contain it can be developed to medicine or health product treating non-insulin dependent diabetes.Caco-2 cell model can be used to screen the antidiabetic drug.
出处
《中国药业》
CAS
2011年第21期8-10,共3页
China Pharmaceuticals
基金
陕西省自然科学基金资助项目
项目编号:2005K18-Z9
