Abstract: Plant peptide trypsin inhibitors(TI), as serine protease inhibitors, have a wide range of biological activities involved in many biological processes, such as hypoglycemic, anti-cancer, anti-inflammatory, disease-resistant, insect-resistant and so on, which possess important applications in food science and technology, medicine, agriculture and other fields. However, for its hypoglycemic activity, although there are some sporadic animal experiments, due to the lack of corresponding molecular targets and mechanism studies, the mechanisms of TI on hypoglycemic effect are still in the primary stage. This review summarizes the research progress of TI in the mechanism of hypoglycemic activity, focusing on the α-glucosidase as a molecular target, and prospects for the application and development of TI on hypoglycemic effect, which provides theoretical reference for future research on the hypoglycemic mechanism of trypsin inhibitor.