壮骨关节丸对大鼠肝微粒体P450的影响

[目的]考察壮骨关节丸对大鼠肝微粒体细胞色素P450的影响。[方法]壮骨关节丸及其两个新工艺按含生药2.1 g/kg连续给大鼠灌胃7 d,末次药后24 h断头处死大鼠并取肝脏,用钙沉降法制备肝微粒体。在体外用含氨苯砜、非那西丁、奥美拉唑、氯唑沙宗的cocktail探针代谢来考察肝微粒体CYP3A、CYP1A2、CYP2C19、CYP2E1的活性。[结果]cocktail探针在体外肝微粒体系统中代谢1 h后,包括壮骨关节丸及其两个新工艺的给药组剩余氯唑沙宗浓度显著高于对照组,而奥美拉唑、非那西丁、氨苯砜浓度与对照组之间差异无统计学意义。[结论]壮骨关节丸可以抑制大鼠肝脏CYP2E1活性,但对CYP1A2、CYP3A及CYP2C19无显著影响。

Influence of Zhuanggu Guanjie pill on liver microsome cytochrome P450 in rats

[Objective] To investigate the influence of Zhuanggu Guanjie pill (ZGGJ) on liver microsome cytochrome P450 in rats. [Methods] Rats were administered intragastrically with ZGGJ and their two new technologic products(crude drug, 2.1 g/kg)once a day for 7 days. The 24 hours after the last administration, rats were sacrificed and liver microsomes were prepared by calcium sedimentation. CYP3A, CYP1A2, CYP2C19, CYP2E1 activity of liver microsomes, including dapsone, phenacetin, omeprazole and chlorzoxazone were detected by cocktail probe in vitro. [Results] Cocktail probes were metabolized in liver microsomes system for 1 h. Chlorzoxazone concentration of administrated groups, including ZGGJ and their two new technologic products groups was significantly higher than control group. There was no significant difference of omeprazole, phenacetin, dapsone concentrations between administrated groups and the control group. [Conclusion] ZGGJ can inhibit CYP2E1 activity, but has no significant effect on CYP1A2, CYP3A and CYP2C19 in rats.