Food-derived dipeptidyl peptidase IV inhibitory peptides: Production, identification, structure-activity relationship, and their potential role in glycemic regulation

Abstract

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 in vivo 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 in vivo hypoglycemic effects .

Keywords:

• Dipeptidyl peptidase IV inhibitory peptides
• glycemic regulation
• structure-activity relationship
• bioinformatics approach
• bioavailability

Authors’ contributions

Mingkai Zhang was responsible for the study design, data collection and preparing the initial draft. Ling Zhu and Gangcheng Wu provided assistance in the concept of the work and also revised the manuscript. Tongtong Liu and Xiguang Qi checked and perfected the pictures and tables. Hui Zhang aided in revising the manuscript critically and provided comprehensive reviews. All authors reviewed the final manuscript before submission.

Disclosure statement

The authors have declared no conflict of interest.

Funding

The author(s) reported there is no funding associated with the work featured in this article.