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Bletilla striata is a dried tuber of B striata (Thunb.) Reichb.f. of Orchidaceae plant, which is mainly used for hemoptysis, vomiting blood, trauma bleeding, sore swollen poison, and cracked skin. There have been few research reports on the effect of this herb on cytochrome P450 (CYP), therefore, the study was aimed to investigate the effects of the B striata extracts on the activity of 6 subtypes (CYP2D6, 1A2, 2C19, 2E1, 3A4, and 2C9) using a cocktail method. The B striata extracts were administrated to rats in 0.21 or 0.63 g/kg once a day for 7 or 14 days. The 3 control groups were used to ensure the accuracy of the results. Subsequently, a cocktail of tolbutamide, chlorzoxazone, midazolam, metoprolol, omeprazole, and caffeine was injected. A ultra performance liquid chromatography–tandem mass spectrometer was developed and validated to investigate the concentration of the probes and the pharmacokinetic parameters were calculated to investigate the effects of the extracts on the activity of 6 enzymes under different doses and different dosing periods. The results suggested that the B striata extracts could induce the activities of CYP2D6, 1A2, and 2C19 and could inhibit the activities of CYP2E1, 3A4, and 2C9. When used in combination with drugs that are metabolized by CYP2D6, 1A2, 2C19, 2E1, 3A4, and 2C9, appropriate dose adjustments were needed to avoid toxic side effects caused by drug interactions.

Cocktail Method: Effect of the Bletilla striata Extracts on CytochromeP450 Activity in Rat