Application of Probe Drugs for Detecting Influences of Gambogic Acid on Cytochrome P450 Isoforms / 中药新药与临床药理

ABSTRACT

Objective To research the influences of gambogic acid on rats'cytochrome P450 isoforms by using the Cocktail probe drugs. Methods Rats were randomly divided into several groups. One group of rats received gambogic acid solution containing 0.5 %CMC-Na (2 mg?mL-1,once per day) orally for six days. At the same time,the rats in the other group received 0.5 %CMC-Na solution serving as blank control group. Blood samples were collect at different time point,and the plasma concentration of cocktail probe drugs was determined by HPLC. Results There was insignificant difference of caffeine and dapsone metabolism between the gambogic acid group and the blank group,but the chlorzoxazone was eliminated faster in the gambogic acid group,and the half life of chlozoxazone was shorter. Conclusion Gambogic acid has no significant influence on the cytochrome P450 isoforms of CYP1A2 and CYP3A4,but has an induction on the CYP2E1.