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麦麸及其活性成分对α-葡萄糖苷酶的体外抑制作用

Inhibition of wheat bran and it's active compoments on α-glucosidase in vitro.

作者信息

Tu Jie, Chen Jun, Zhu Shuyun, Zhang Chunxiao, Chen Hua, Liu Youbing

机构信息

Department of Food Quality and Safety, School of Food and Biological Engineering, Jiangsu University, Zhenjiang, Jiangsu, 212013, P. R. China ; Department of Biotechnology and Engineering, College of Biology and Chemical Engineering, Jiangsu University of Science and Technology, Zhenjiang, Jiangsu, 212018, P. R. China.

出版信息

Pharmacogn Mag. 2013 Oct;9(36):309-14. doi: 10.4103/0973-1296.117826.

Abstract

BACKGROUND

Wheat bran is a traditional Chinese medicine; however, it is mostly used as feedstuff in China. Wheat bran is widely accepted as an important ingredient in many low-glycemic index foods in modern western societies; however, its glycemic control mechanism is unknown.

OBJECTIVE

To determine potent α-glucosidase inhibitory compounds from wheat bran and to identify the inhibition on α-glucosidase.

MATERIALS AND METHODS

Ethanolic extract of wheat bran was prepared to evaluate the inhibitory activity on α-glucosidase, then fractionation of the extract was guided by in vitro enzyme-inhibition assay, and the potent α-glucosidase inhibitory compounds were identified by high performance liquid chromatography and atmospheric pressure chemical ionization-mass spectrometry; finally the enzyme inhibition process was studied using the Michaelis-Menton and the Lineweaver-Burk equations.

RESULTS

Both baker's yeast and rat intestinal enzymes were mostly inhibited (87.9% and 66.8% inhibition, respectively) at concentration 0.6 mg/mL of the ethanolic extract of wheat bran. The petroleum ether fraction in the ethanolic extract of wheat bran showed significant activity against rat intestinal α-glucosidase, and revealed a dose-dependent effect. The inhibition was 76.57% at 0.3 mg/mL and 100% at 0.6 mg/mL. The active fraction 13 of petroleum ether fraction was identified as alkylresorcinols (ARs). ARs showed strong inhibition towards α-glucosidase and its IC50 value was found to be 37.58 μg/mL. The enzyme kinetic studies showed that, in the presence of ARs, the Michaelis-Menton constant (K m) remains constant whereas the maximal velocity (V max) decreases, revealing a non-competitive type of inhibition.

CONCLUSION

The therapeutic potentiality of ARs in the management of the postprandial hyperglycemia will proliferate the utilization of wheat bran in controlling type 2 diabetes.

摘要

背景

麦麸是一种传统中药;然而,在中国它大多被用作饲料。在现代西方社会,麦麸被广泛认为是许多低血糖指数食品中的一种重要成分;然而,其血糖控制机制尚不清楚。

目的

从小麦麸中确定有效的α-葡萄糖苷酶抑制化合物,并鉴定其对α-葡萄糖苷酶的抑制作用。

材料与方法

制备麦麸乙醇提取物以评估其对α-葡萄糖苷酶的抑制活性,然后通过体外酶抑制试验指导提取物的分级分离,并通过高效液相色谱和大气压化学电离质谱鉴定有效的α-葡萄糖苷酶抑制化合物;最后使用米氏方程和林-贝氏方程研究酶抑制过程。

结果

在麦麸乙醇提取物浓度为0.6mg/mL时,面包酵母和大鼠肠道酶大多受到抑制(分别为87.9%和66.8%的抑制率)。麦麸乙醇提取物中的石油醚馏分对大鼠肠道α-葡萄糖苷酶显示出显著活性,并呈现剂量依赖性效应。在0.3mg/mL时抑制率为76.57%,在0.6mg/mL时为100%。石油醚馏分的活性组分13被鉴定为烷基间苯二酚(ARs)。ARs对α-葡萄糖苷酶表现出强烈抑制作用,其半数抑制浓度(IC50)值为37.58μg/mL。酶动力学研究表明,在ARs存在的情况下,米氏常数(Km)保持不变,而最大速度(Vmax)降低,表明为非竞争性抑制类型。

结论

ARs在管理餐后高血糖方面具有治疗潜力,这将增加麦麸在控制2型糖尿病中的应用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9769/3793335/bfa7c0ea60b8/PM-9-309-g001.jpg

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