Abstract: OBJECTIVE To characterize the metabolism of pinocembrin in human liver microsome by UPLC-MS/MS. METHODS Pinocembrin was incubated with human liver microsomal incubation system. UPLC-MS/MS was used to characterize the metabolites. RESULTS Naringenin, dihydrobaicalein, dihydronorwogonin and pinocembrin-7-O-glucuronide were identified within 6 min via UPLC-MS/MS. These 4 metabolites were first reported as the metabolites of pinocembrin in human liver microsomal incubation system. CONCLUSION The results indicated that pinocembrin can only be metabolited as the forms of hydroxylation and glucuronidation in human liver microsome. Dihydronorwogonin was the main hydroxylated metabolite. Pinocembrin-7-O-glucuronide was the predominant deactivated metabolic pathway.