Dipeptidyl peptidase IV(DPP IV) is a new target for treating type II diabetes. Glucose-dependent insulin-releasing peptide, and the insulin glucagon-like peptide-1 could promote insulin secretion, biosynthesis, inhibit β-cell apoptosis, lower the blood sugar and other functions. DPP IV could degradate the level of glucose-dependent insulin-releasing peptide and glucagon-like peptide-1 to the loss of biological activity. Our experiment is to optimize the screening system for DPP IV inhibitors, based on DPP IV from Caco-2, results showed that the concentration of Gly-Pro-pNA is 0.064 mg/mL,reaction time is 30 minutes, temperature 37 ?C and the concentration of IIe-Pro-IIe 0.68 mmol/L. Therely astablishing a rapid screening system of dipeptidyl peptidase. Application of the model 18 Uyghur herbal extracts were screened and some had the inhibitory activity of DPP IV. The study will provide support for further exploration and utilization of Uyghur herbs.