Objective: The aim of the article was to explore the compatibility connotation of Aconiti Radix and Pinelliae Rhizoma from cytochrome P450 enzyme system (CYP)3A1/2 mediating metabolic herb-herbs interaction in rats. Method: Incubation in vitro and probe method in vivo were used to detect the activity of CYP3A.The fluorescence quantitative polymerase chain reaction (PCR) technology and Western blot were applied to determine expression of mRNA and protein. Result: Compared with unprocessed Aconiti Radix (RAR)/Aconiti Radix Cocta (ARC)-unprocessed Pinelliae Rhizoma (UPR)

the production rate of 6β-hydroxy-testosterone (6β-OH-Tes) and the expression of CYP3A protein were all decreased in RAR-Pinelliae Rhizoma Praeparatum (PRP)/Pinelliae Rhizoma Praeparatum Cum Zingibere et Alumine (PRPZA)

but partial dose group of ARC-PRP/PRPZA was significantly decreased.The expression of CYP3A1 mRNA were increased in 0.6

1.2 g·kg-1 groups of RAR-PRP/PRPZA as well as decreased in 0.6 g·kg-1 group of ARC-PRP/PRPZA.Compared with the corresponding dose group of RAR-UPR/PRP/PRPZA

the production rates of 6β-OH-Tes were most significantly reduced and the expression of CYP3A protein of ARC-UPR/PRP were decreased

while the expression of CYP3A1 mRNA were increased in most groups of ARC-UPR/PRP/PRPZA.The rates of 6'-hydroxy-buspirone (6'-OH-BP)/buspirone (BP) (AUC0-t of 6'-OH-BP/AUC0-t of BP) and 1-(2-pyrimidinyl)-piperazine (1-PP)/BP (AUC0-t of 1-PP/AUC0-t of BP) were all increased in RAR-PRP as well as did not change in RAR-PRPZA by comparing with RAR-UPR.The rates of 6'-OH-BP/BP were all decreased and the rates of 1-PP/BP did not change in ARC-PRP/PRPZA by comparing with ARC-UPR. Conclusion: Inhibition of RAR/ARC on CYP3A activity can be reversed by compatibility with UPR/PRP/PRPZA

which may accelerate the metabolism of some components in RAR/ARC

then the toxicity or the pharmacological action of RAR/ARC is weakened.