Tu Jie, Chen Jun, Zhu Shuyun, Zhang Chunxiao, Chen Hua, Liu Youbing
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.
Pharmacogn Mag. 2013 Oct;9(36):309-14. doi: 10.4103/0973-1296.117826.
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.
To determine potent α-glucosidase inhibitory compounds from wheat bran and to identify the inhibition on α-glucosidase.
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.
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.
The therapeutic potentiality of ARs in the management of the postprandial hyperglycemia will proliferate the utilization of wheat bran in controlling type 2 diabetes.
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。
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。
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。
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。
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。