To investigate the influence of scutellarin on the activities of CYP1A2, CYP2C11, CYP2D1, and CYP3A1/2 in rats in vivo. Scutellarin and saline were intravenously administered to male Wistar rats via the caudal vein for 7 days consecutively. On the 8th day, the rats were treated with probe drugs of caffeine (10 mg/kg), tolbutamide (10 mg/kg), metoprolol (20 mg/kg), dapsone (10 mg/kg) by intraperitoneal injection, and the blood samples were collected at different times. The probe drugs in the blood samples were measured by ultra performance liquid chromatography mass spectrometer (UPLC-MS/MS) and the changes of the pharmacokinetics parameters of the drugs were observed to evaluate the effects of scutellarin on the four CYP450 isoforms in rats. The activity of CYP1A2 in rats was inhibited significantly after treatment with scutellarin by increased caffeine t1/2 (21.76%, P < 0.05), T(max) (43.05%, P < 0.05), C(max) (43.92%, P < 0.01) and AUC(0-infinity) (50.88%, P < 0.01) in the scutellarin-treated group compared with those of the blank control. The activity of CYP2C11 in rats was inhibited significantly after treatment with scutellarin by increased tolbutamide t1/2 (16.74%, P < 0.01), T(max) (116.87%, P < 0.05), C(max) (63.78%, P < 0.01) and AUC(0-infinity) (70.61%, P < 0.01) in the scutellarin-treated group compared with those of the blank control. The activity of CYP3A1/2 in rats was inhibited significantly after treatment with scutellarin by increased dapsone t1/2 (45.28%, P < 0.05), T(max) (81.55%, P < 0.05), C(max) (155.58%, P < 0.01)and AUC(0-infinity) (176.35%, P < 0.01) in the scutellarin-treated group compared with those of the blank control. The pharmacokinetic parameters of metoprolol were not significantly changed in the scutellarin-treated group compared with those of the blank control. Scutellarin could significantly inhibit CYP1A2, CYP2C11 and CYP3A1/2 activities in rats in vivo, but had no effects on the activity of CYP2D1.

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