从发酵米糠中分离出一种新型抗糖尿病α-葡萄糖苷酶寡肽抑制剂。

Isolation of a Novel Anti-Diabetic α-Glucosidase Oligo-Peptide Inhibitor from Fermented Rice Bran.

作者信息

Hu Jingfei, Lai Xiaohua, Wu Xudong, Wang Huanyu, Weng Nanhai, Lu Jing, Lyu Mingsheng, Wang Shujun

机构信息

Jiangsu Key Laboratory of Marine Bioresources and Environment/Jiangsu Key Laboratory of Marine Biotechnology, Jiangsu Ocean University, Lianyungang 222005, China.

Co-Innovation Center of Jiangsu Marine Bio-Industry Technology, Jiangsu Ocean University, Lianyungang 222005, China.

出版信息

Foods. 2023 Jan 1;12(1):183. doi: 10.3390/foods12010183.

At present, the incidence rate of diabetes is increasing gradually, and inhibiting α-glucosidase is one of the effective methods used to control blood sugar. This study identified new peptides from rice bran fermentation broth and evaluated their inhibitory activity and mechanism against α-glucosidase. Rice bran was fermented with Bacillus subtilis MK15 and the polypeptides of <3 kDa were isolated by ultrafiltration and chromatographic column, and were then subjected to LC-MS/MS mass spectrometry analysis. The results revealed that the oligopeptide GLLGY showed the greatest inhibitory activity in vitro. Docking studies with GLLGY on human α-glucosidase (PDB ID 5NN8) suggested a binding energy of −7.1 kcal/mol. GLLGY acts as a non-competitive inhibitor and forms five hydrogen bonds with Asp282, Ser523, Asp616, and His674 of α-glucosidase. Moreover, it retained its inhibitory activity even in a simulated digestion environment in vitro. The oligopeptide GLLGY could be developed into a potential anti-diabetic agent.

目前，糖尿病的发病率正在逐渐上升，抑制α-葡萄糖苷酶是控制血糖的有效方法之一。本研究从米糠发酵液中鉴定出新的肽段，并评估了它们对α-葡萄糖苷酶的抑制活性及其作用机制。用枯草芽孢杆菌MK15发酵米糠，通过超滤和色谱柱分离出分子量小于3 kDa的多肽，然后进行LC-MS/MS质谱分析。结果表明，寡肽GLLGY在体外表现出最大的抑制活性。GLLGY与人α-葡萄糖苷酶（PDB ID 5NN8）的对接研究表明其结合能为−7.1 kcal/mol。GLLGY作为非竞争性抑制剂，与α-葡萄糖苷酶的Asp282、Ser523、Asp616和His674形成五个氢键。此外，即使在体外模拟消化环境中，它仍保留其抑制活性。寡肽GLLGY有望开发成为一种潜在的抗糖尿病药物。