Objective:To study the inhibitory effect of Zishen Qinggan Formula and its effective ingredients (2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucopyranoside,1-deoxynojirimycin,cassiaside,rubrofusarin gentiobioside,aurantio-obtusin,chryso-obtusin,resveratrol)on DPP-4,and study the possible mechanism of its hypoglycemic effect.Method:Establish vitro screening method of DPP-4 inhibitor,and the amount of enzyme,substrate concentration,the optimum pH and reaction time were optimized.And select the Sitagliptin Phosphate tablets as positive control drug.Through the screening model has been established,calculate the inhibition rate,calculate IC50.Result:The inhibition rate of DPP-4 of cassiaside,rubrofusarin gentiobioside,aurantio-obtusin,chryso-obtusin are less than 10%.IC50 value for the DPP-4 of resveratrol,2,3,5,4'-tetrahydroxystilbene-2-O-3-D-glucopyranoside,1-deoxynojirimycin,extract of Zishen Qinggan formula and Sitagliptin Phosphate are (48.805 ± 12.874)mmol/L,(2.845 ± 0.428) mmol/L,(0.305 ± 0.002) mmol/L,(1.628 ± 0.324) mmol/L,(0.003 ± 0.0005) mmol/L.Conclusions:Zishen Qinggan Formula and its effective ingredients have certain inhibitory effect on DPP-4,and Jasminoidin has the obvious inhibitory action to the DPP-4,and DPP-4 inhibitory effect may be the mechanism for regulating blood sugar.