National Engineering Research Center for Functional Food, Collaborative Innovation Center of Food Safety and Quality Control in Jiangsu Province, School of Food Science and Technology, Jiangnan University, Wuxi, China.
Binzhou Zhongyu Food Company Limited, Key Laboratory of Wheat Processing, Ministry of Agriculture and Rural Affairs, National Industry Technical Innovation Center for Wheat Processing, Bohai Advanced Technology Institute, Binzhou, China.
Crit Rev Food Sci Nutr. 2024;64(8):2053-2075. doi: 10.1080/10408398.2022.2120454. Epub 2022 Sep 12.
Dipeptidyl Peptidase IV (DPP-IV) inhibitory peptides are attracting increasing attention, owing to their potential role in glycemic regulation by preventing the inactivation of incretins. However, few reviews have summarized the current understanding of DPP-IV inhibitory peptides and their knowledge gaps. This paper reviews the production, identification and structure-activity relationships (SAR) of DPP-IV inhibitory peptides. Importantly, their bioavailability and hypoglycemic effects are critically discussed. Unlike the traditional method to identifying peptides after separation step by step, the bioinformatics approach identifies peptides via virtual screening that is more convenient and efficient. In addition, the bioinformatics approach was also used to investigate the SAR of peptides. Peptides with proline (Pro) or alanine (Ala) residue at the second position of N-terminal are exhibit strong DPP-IV inhibitory activity. Besides, the bioavailability of DPP-IV inhibitory peptides is related to their gastrointestinal stability and cellular permeability, and studies showed that the glucose homeostasis has been improved by these peptides. Especially, the intestinal transport of DPP-IV inhibitory peptides and cell biological assays used to evaluate their potential role in glycemic regulation are innovatively summarized. For further successful development of DPP-IV inhibitory peptides in glycemic regulation, future study should elucidate their SAR and hypoglycemic effects .
二肽基肽酶 IV（DPP-IV）抑制肽由于其在通过防止肠降血糖素失活来调节血糖方面的潜在作用而受到越来越多的关注。然而，很少有综述总结了 DPP-IV 抑制肽的当前认识及其知识空白。本文综述了 DPP-IV 抑制肽的生产、鉴定和构效关系（SAR）。重要的是，还批判性地讨论了它们的生物利用度和降血糖作用。与传统的通过逐步分离来鉴定肽的方法不同，生物信息学方法通过虚拟筛选来鉴定肽，这种方法更方便、更高效。此外，生物信息学方法还用于研究肽的 SAR。N 端第二位为脯氨酸（Pro）或丙氨酸（Ala）残基的肽具有很强的 DPP-IV 抑制活性。此外，DPP-IV 抑制肽的生物利用度与其胃肠道稳定性和细胞通透性有关，研究表明这些肽改善了葡萄糖稳态。特别是，总结了 DPP-IV 抑制肽的肠道转运和细胞生物学测定，用于评估它们在血糖调节中的潜在作用，这是创新性的。为了在血糖调节中进一步成功开发 DPP-IV 抑制肽，未来的研究应阐明其 SAR 和降血糖作用。
