Comparative Evaluation of Quercetin, Isoquercetin and Rutin as Inhibitors of alpha-Glucosidase

文献类型： 外文期刊

第一作者： Li, Yan Qin

作者： Li, Yan Qin;Zhou, Feng Chao;Gao, Fei;Bian, Jun Sheng;Shan, Fang

作者机构：

关键词： Flavonoid compound;alpha-glucosidase;inhibitor;diabetes;tartary buckwheat

期刊名称：JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY （ 影响因子：5.279； 五年影响因子：5.269 ）

ISSN： 0021-8561

年卷期： 2009 年 57 卷 24 期

页码：

收录情况： SCI

摘要： Three flavonoids from tartary buckwheat bran, namely, quercetin (Que), isoquercetin (Iso) and rutin (Rut), have been evaluated as alpha-glucosidase inhibitors by fluorescence spectroscopy and enzymatic kinetics and have also been compared with the market diabetes healer, acarbose. The results indicated that Que, Iso and Rut could bind alpha-glucosidase to form a new complex, which exhibited a strong static fluorescence quenching via nonradiation energy transfer, and an obvious blue shift of maximum fluorescence. The sequence of binding constants (K(A)) was Que > Iso > Rut, and the number of binding sites was one for all of the three cases. The thermodynamic parameters were obtained by calculations based on data of binding constants. They revealed that the main driving force of the above-mentioned interaction was hydrophobic. Enzymatic kinetics measurements showed that all of the three compounds were effective inhibitors against alpha-glucosidase. Inhibitory modes all belonged to a mixed type of noncompetitive and anticompetitive. The sequence of affinity (1/K(i)) was in accordance with the results of binding constants (K(A)). The concentrations which gave 50% inhibition (IC(50)) were 0.017 mmol.L(-1), 0.185 mmol.L(-1) and 0.196 mmol.L(-1), compared with acarbose's IC(50) (0.091 mmol.L(-1)); the dose of acarbose was almost five times of that of Que and half of that of Iso and Rut. Our results explained why the inhibition on alpha-glucosidase of tartary buckwheat bran extractive substance (mainly Rut) was much weaker than that of its hydrolysis product (a mixture of Que, Iso and Rut). This work would be significant for the development of more powerful antidiabetes drugs and efficacious utilization of tartary buckwheat, which has been proved as an acknowledged food in the diet of diabetic patients.

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