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从苦荞蛋白模拟胃肠道消化物中鉴定和表征两种新型二肽基肽酶-IV抑制肽。

Identification and characterization of two novel dipeptidyl peptidase-IV inhibitory peptides from the simulated gastrointestinal digestion of Tartary buckwheat proteins.

作者信息

Wu Weijing, Qiu Ju, Wang Libo, Tan Qianglai, Zhuang Ziyuan, Wang Yanling, Wu Lanlan

机构信息

Xiamen Medical College, Xiamen, Fujian 361023, China; Engineering Research Center of Natural Cosmeceuticals College of Fujian Province, Xiamen Medical College, Xiamen 361023, China.

Key Laboratory of Precision Nutrition and Food Quality, Department of Nutrition and Health, China Agricultural University, No.17 Tsinghua East Road, Haidian District, Beijing 100083, China..

出版信息

Food Chem. 2025 May 1;473:143067. doi: 10.1016/j.foodchem.2025.143067. Epub 2025 Jan 23.

DOI:10.1016/j.foodchem.2025.143067
PMID:39884244
Abstract

This study analyzed dipeptidyl peptidase-IV (DPP-IV) inhibitory peptides from Tartary buckwheat (Fagopyrum tataricum) protein hydrolysates, known for managing chronic diseases. Simulated gastrointestinal digestion enhanced the inhibitory activity of DPP-IV. Using anion-exchange resin DEAE-52, reverse high-performance liquid chromatography, and LC-MS/MS, eight novel peptides were identified. Among them, the peptides LAGQS (LA5) and LREIDDADK (LR9) exhibited the strongest inhibition in both competitive and noncompetitive modes. Molecular docking revealed electrostatic, hydrogen bond, and hydrophobic interactions for both peptides, with LR9 also engaging in π-cation interactions. Based on the Caco-2 model, the in situ DPP-IV inhibitory effect of LR9 was superior to that of LA5, likely because of LR9's greater stability during hydrolysis. Moreover, LA5 could not be transported through the Caco-2 monolayer, and LR9 demonstrated moderate transportability. These findings highlight Tartary buckwheat protein's potential for application in high-value plant-based products, including functional foods and pharmaceuticals targeting blood glucose regulation using DPP-IV inhibitory peptides.

摘要

本研究分析了苦荞(鞑靼荞麦)蛋白水解物中的二肽基肽酶-IV(DPP-IV)抑制肽,苦荞以对慢性病有调理作用而闻名。模拟胃肠道消化增强了DPP-IV的抑制活性。通过阴离子交换树脂DEAE-52、反相高效液相色谱和液相色谱-串联质谱,鉴定出了8种新型肽。其中,肽LAGQS(LA5)和LREIDDADK(LR9)在竞争性和非竞争性模式下均表现出最强的抑制作用。分子对接揭示了这两种肽的静电、氢键和疏水相互作用,LR9还参与了π-阳离子相互作用。基于Caco-2模型,LR9的原位DPP-IV抑制作用优于LA5,这可能是因为LR9在水解过程中具有更高的稳定性。此外,LA5不能通过Caco-2单层转运,而LR9表现出适度的转运能力。这些发现突出了苦荞蛋白在高价值植物基产品中的应用潜力,包括使用DPP-IV抑制肽的功能性食品和针对血糖调节的药物。

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