Abstract: Type II diabetes mellitus (T2DM) is one of the most prevalent metabolic diseases worldwide and α-glucosidase inhibitors are oral medications that are effective in the prevention and management of T2DM. Food-derived bioactive peptides are potential sources of α-glucosidase inhibitors, which have shown to have hypoglycemic activity and can effectively control postprandial blood glucose by inhibiting α-glucosidase activity, thus intervening and regulating T2DM, and have great prospects in the development of hypoglycemic peptide products. At present, there is no systematic strategy for exploring the structure-activity relationship, safety and bioavailability of food-derived α-glucosidase inhibitory peptides, hampering their research and development. In this paper, we systematically review the structural characteristics, toxicity, allergenicity, and bioavailability (gastrointestinal digestive enzyme resistance, mucus permeability, transit efficiency in small intestinal epithelial cells and liver metabolism) of food-derived α-glucosidase inhibitory peptides that have been successfully identified in recent years. This review is expected to provide a theoretical reference for the rational development of food-derived α-glucosidase inhibitory peptides and the further processing of related functional foods.

Key words: food-derived α-glucosidase inhibitory peptides; structural features; toxicity; allergenicity; bioavailability