OBJECTIVE: To investigate the mechanism of the effects of apigenin on reducing uric acid and renal protection in oteracil potassium-induced hyperuricemia mice. METHODS: 50 mice were randomly divided into normal group, model group, allopurinol group (5 mg/kg), apigenin low-dose and high-dose groups (40, 80 mg/kg), with 10 mice in each group. Except for normal group, other groups were given oteracil potassium 250 mg/kg intragastrically to induce hyperuricemia model; 1 h after modeling, treatment groups were given relevant medicine intragastrically, and normal group and model group were given constant volume of normal saline intragastrically, once a day, for consecutive 7 d. Blood uric acid, urine uric acid and 24 h creatinine levels, the expression of kidney transporter associated protein (mURAT1, mOCT1, mOCT2, mOCTN1 and mOCTN2) were all determined in each group. RESULTS: Compared with normal group, blood uric acid, urine uric acid and mURAT1 levels of model group were significantly increased, while the expressions of mOCT1, mOCT2, mOCTN1 and mOCTN2, 24 h creatinine were significantly decreased (P<0.01 or P<0.001). Compared with model group, blood uric acid, urine uric acid and mURAT1 levels of apigenin low-dose and high-dose groups, allopurinol group were significantly decreased, while 24 h creatinine, the expressions of mOCT1, mOCT2, mOCTN1 and mOCTN2 were increased significantly (P<0.05 or P<0.01 or P<0.001). CONCLUSIONS: Apigenin can reduce uric acid level of oteracil potassium-induced hyperuricemia mice and propect kidney, the mechanism of which may be associated with down-regulating the expression of mURAT1 and up-regulating the expressions of mOCTN1, mOCTN2, mOCT1 and mOCT2.