灯盏花素及灯盏乙素对肝细胞色素P450酶体内代谢的影响  

In vivo effects of breviscapine and scutellarin on the activities of hepatic cytochrome P450 enzymes

作　　者：李天英[1] 石迪[1] 郑岩 郑春宇 李秋红[1] LI Tian-ying;SHI Di;ZHENG Yan;ZHENG Chun-yu;LI Qiu-hong(Heilongjiang University of Chinese Medicine,Herbin 150040,China)

机构地区：[1]黑龙江中医药大学,黑龙江哈尔滨150040

出　　处：《化学工程师》2020年第10期73-76,共4页Chemical Engineer

基　　金：黑龙江省自然科学基金项目(H2016069);国家自然科学基金委青年基金项目(81704177);中国博士后科学基金资助项目(2017M610215);黑龙江中医药大学科研基金面上项目(2019MS36)。

摘　　要：目的探讨灯盏花素及灯盏乙素对CYP2E1、CYP2C9和CYP3A4的影响。方法灯盏花素组、灯盏乙素组及对照组给予灯盏花素、灯盏乙素及生理盐水后,各组分别给予氯唑沙宗、甲苯磺丁脲和咪达唑仑的混合探针溶液,采集血浆样品,经处理后进行HPLC分析。结果三组两两比较,各组中氯唑沙宗的药动学参数均无显著差异。灯盏乙素组的甲苯磺丁脲分别和灯盏花素组、对照组比较,甲苯磺丁脲的药动学参数均呈现显著差异,灯盏花素组的甲苯磺丁脲与对照组相比,药动学参数无明显差异。灯盏花素组及灯盏乙素组的咪达唑仑分别与对照组比较,咪达唑仑的药动学参数均有显著变化。结论灯盏花素对CYP3A4有抑制作用,对CYP2E1和CYP2C9无影响;灯盏乙素对CYP2C9和CYP3A4有抑制作用,对CYP2E1无影响。OBJECTIVE The present study investigated how Breviscapine injection(BI)and scutellarin influenced CYP4502E1,2C9 and 3A4.METHODS After pretreatment with BI or scutellarin,the rats were administrated intravenously a cocktail containing chlorzoxazone,tolbutamide and midazolam,and blood samples were collected at different time points after drug administration,and HPLC analysis was performed.RESULTS There was no significant influence in pharmacokinetic parameters of chlorzoxazone and tolbutamide in BI pretreated rats,and no substantial change of chlorzoxazone after pretreatment with scutellarin.But a few pharmacokinetic parameters of midazolam in BI pretreated rats were affected significantly,while some pharmacokinetic parameters of tolbutamide and midazolam were altered obviously after pretreatment with scutellarin.CONCLUSION The results indicated that BI inhibited CYP3A4,did not have significant effects on CYP2E1 and CYP2C9,while scutellarin inhibited CYP2C9 and CYP3A4,could not significantly affect CYP2E1 in rats.

关 键 词：灯盏花素 灯盏乙素 细胞色素P450酶 

分 类 号：R285[医药卫生—中药学]