目的 研究红花注射液对大鼠细胞色素P450 2D6亚型(CYP2D6)的影响。方法 利用探针药物右美沙芬(DM),高效液相色谱法测定各实验组(对照组,红花注射液0.9、1.8、3.6 mL/kg组)大鼠体内尿液中与体外肝微粒体温孵系统中DM的代谢率,考察红花注射液对大鼠CYP2 D6活性的影响。结果 体内实验和体外实验中,红花注射液1.8和3.6 mL/kg组DM的代谢率均明显低于对照组(P<0.05、0.01);抑制实验中,体外肝微粒体温孵系统中红花注射液组和西咪替丁组DM的代谢率明显低于空白组(P<0.05);含红花生药量为30 mg/mL时红花注射液组DM的代谢率与西咪替丁(0.6 mg/mL)时DM的代谢率相近,抑制能力相当;红花注射液的IC50为10.64 mg/mL。结论 红花注射液对大鼠CYP2D6有显著的抑制作用。

Objective ?To?investigate?the?effect?ofHonghua Injection?on?the?activity?of?rat liver?CYP2D6.Methods ?The metabolic?rates of probe dextromethorphan(DM)in the blank and Honghua?Injection groups(O.9,1.8,and 3.6mL/kg)invivo urine and?in vitro liver microsome incubated system?were determinedby high performance liquid chromatography(HPLC).Thevariation of the metabolic rate?of DM represented the effect ofHonghua Injectionon the activityof rat liver CYP2D6 in口而o and in vitro.?Results ?In vivo and in vitro,the DM metabolic?rates of treatedgroups(1.8and 3.6mL/kg)arelower?than that in the blankgroup(P<0.05,0.01);TheDM metabolic rates in Honghua Injection group and?Cimetidine?groupwere?significantlylower than?that in?the blankgroupin?inhibitory study(P<0.05,?respectively);The DM metabolic rate inHonghua Injectiongroup(30 mg/mL)wasabout the same as that?in Cimetidinegroup(O.6 mg/mL),the inhibiting ability was similar in above-mentioned twogroups;The?50 o.4inhibitory concentration(IC50)of Honghua Injection?is 10.64 mg/mL.Conclusion ?TheHonghua?Injection could significantly inhibit CYP2D6 in rat.?

黑龙江省教育厅科学技术研究项目(11531114)