摘要
目的:运用"鸡尾酒"探针药物法,探讨射干总苷和射干总苷元对肝药酶亚型的作用。方法:以地西泮为内标物,采用"鸡尾酒"探针技术,检测咖啡因、美托洛尔、氯唑沙宗、甲苯磺丁脲四种探针药物在大鼠血清代谢中的含量变化,通过HPLC方法得出血药浓度数据,绘制平均药-时曲线,计算药代动力学参数。结果:实验组咖啡因(CYP1A2)的AUC明显增大(P <0. 05),经t检验,结果具有统计学意义;实验组美托洛尔(CYP2D6)的半衰期明显减小(P <0. 05),经过t检验,结果具有统计学意义。结论:射干总苷和射干总苷元对CYP1A2酶具有抑制作用,对CYP2D6酶具有诱导作用。
Objective: To study the effects of total tectoridin and total tectorigenin on hepatic enzyme subtype by cooktail probe approach. Methods: The contents of caffeine,metoprolol,chlorzoxazone and tolbutamide in serum were measured by using cocktail probe technique with diazepam as internal standard. The plasma concentrations of the different probe drugs were determined by HPLC. The mean drug-time curve is plotted and we calculated the pharmacokinetic parameters. Results: In experimental group,the AUC of caffeine significantly increased than those in control group. The results were statistically significant by t test.. The half life of metoprolol significantly decreased than those in control group. The results were statistically significant by t test. Conclusion:Total tectoridin and total tectorigenin can inhibit the metabolic activities of CYP1 A2 and include the metabolic activities of CYP2 D6.
作者
张倩玉
王光函
康愿涛
尤献民
邹桂欣
夏林波
李国信
ZHANG Qianyu;WANG Guanghan;KANG Yuantao;YOU Xianmin;ZOU Guixin;XIA Linbo;LI Guoxin(Liaoning University of Traditional Chinese Medicine, Shenyang 110847 , Liaoning, China;Liaoning Province Institute of Traditional Chinese Medicine, Shenyang 110034,Liaoning, China)
出处
《辽宁中医杂志》
CAS
2019年第4期796-799,共4页
Liaoning Journal of Traditional Chinese Medicine
基金
"十三五"国家重大新药创制科技重大专项(2017ZX09301019)
辽宁省科学事业公益研究基金(20170019)
辽宁省创新中药关键技术研究平台
关键词
“鸡尾酒”探针
射干异黄酮
肝药酶代谢
cooktail
isoflavones from Belamcandae Rhizoma
liver drug enzyme metabolism
作者简介
张倩玉(1993-),女,辽宁大连人,硕士研究生,研究方向:中药分析研究;通讯作者:李国信(1963-),男,辽宁沈阳人,教授,博士研究生导师,博士,研究方向:中药临床药理,E-man:syyljdlgx024@126.
