CHENG Ying, HUANG Yin, TIAN Yuan, XU Lei, LIU Guo-Qiang, ZAHNG Zun-Jian. Assessment of the effects of Radix Bupleuri and vinegar-baked Radix Bupleuri on cytochrome 450 activity by a six-drug cocktail approach[J]. Chinese Journal of Natural Medicines, 2013, 11(3): 302-308.
Citation: CHENG Ying, HUANG Yin, TIAN Yuan, XU Lei, LIU Guo-Qiang, ZAHNG Zun-Jian. Assessment of the effects of Radix Bupleuri and vinegar-baked Radix Bupleuri on cytochrome 450 activity by a six-drug cocktail approach[J]. Chinese Journal of Natural Medicines, 2013, 11(3): 302-308.

Assessment of the effects of Radix Bupleuri and vinegar-baked Radix Bupleuri on cytochrome 450 activity by a six-drug cocktail approach

  • AIM:To assess the effects of Radix Bupleuri and vinegar-baked Radix Bupleuri on cytochrome 450 activity of rats.METHODS:Six probe drugs(caffeine,midazolam,dextromethorphan,tolbutamide,omeprazole,chlorzoxazone) were simultaneously given to rats after different dosing of Radix Bupleuri or vinegar-baked Radix Bupleuri for seven days.The plasma concentrations of the six probes were measured by high performance liquid chromatography-triple quadrupole mass spectrometry(HPLC-MS/MS) and their corresponding pharmacokinetic parameters were calculated.RESULTS:The AUC and T1/2 of midazolam,dextromethorphan and chlorzoxazone decreased significantly(PT1/2 and AUC of omeprazole,but treatment of vinegar-baked Radix Bupleuri with normal dose did not change the pharmacokinetics of omeprazole.The pharmacokinetics of tolbutamide in all vinegar-baked Radix Bupleuri-treated rats showed no statistically significant difference(P>0.05) from that of controlled rats,however,treatment of Radix Bupleuri decreased tolbutamide T1/2.The pharmacokinetics of caffeine in all Radix Bupleuri or vinegar-baked Radix Bupleuri-treated rats showed no statistically significant difference(P>0.05) from that of controlled rats.CONCLUSION:The Radix Bupleuri and vinegar-baked Radix Bupleuri have different effects on the CYP2C9 and CYP2C19.Radix Bupleuri and vinegar-baked Radix Bupleuri have strong induction effects on the CYP2E1,CYP2D6 and CYP3A4,however,have no impact on CYP1A2.The reason of different therapeutic effects of Radix Bupleuri and vinegar-baked Radix Bupleuri extract may be the different effects of Radix Bupleuri and vinegar-baked Radix Bupleuri on the CYP2C9 and CYP2C19.
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