Abstract: OBJECTIVE To observe the effect of Picrorhiza rhizome and Hypericum perforatum on in vitro protein non-enzyme glycosylation, evaluate the relationship between the anti-oxidation effect and non-enzyme glycosylation, and analyze the possibility of their use in the treatment of diabetes. METHOD BSA and glucose were used to produce an in vitro system for non-enzyme glycosylation, and the reaction fluid was divided into a control group and groups with different concentration, which were incubated for 60 days. The fluorescent value of each groups were then determined. RESULT The two drugs with different concentrations could markedly and dose-dependently inhibit the formation of AGEs. CONCLUSION The two drugs can inhibit the protein non-enzyme glycosylation, which is probably related to their anti-oxidation function.