Abstract: Diabetes mellitus has become one of the most serious chronic diseases all over the world, which need to be to prevented, intervened, regulated by innovative means. Food derived small peptides can regulate blood glucose by acting with receptors, enzymes, biological molecules and glucose transporters. They show high tissue affinities, significant specificities, with low side effects, which are promising strategies for diabetes mellitus. This survey summarizes the mechanisms, food protein sources, preparation and activity evaluation procedures, structure-activity relationships and challenges during commercial development of food derived blood glucose regulating peptides. Specifically, it includes the sequence characteristics of DPP-IV inhibitory peptide, α-glucosidase inhibitory peptides and α-amylase inhibitory peptides. Besides, the active sites are also discussed from different perspectives of sequence alignment: bioinformatics technologies such as in silico analysis, molecular structure alignment/docking, and quantitative structure activity relationship analysis. It may provide ideas for future research: a. Exploring the mechanism from the aspect of cell pathways and metabonomic to improve in vivo efficacy. b. Combining cell/animal experiments with clinical trials to evaluate digestive stability, bioavailability and safety. c. Innovative carriers to improve the solubility, stability and permeability of peptides. Supports for promoting the industrial application of diabetes functional foods are expected.