| 混合探针底物法测定五味子成分对大鼠肝脏细胞色素P450同工酶的影响 |
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| 引用本文： | Wang BL,Hu JP,Sheng L,Li Y. 混合探针底物法测定五味子成分对大鼠肝脏细胞色素P450同工酶的影响[J]. 药学学报, 2011, 46(8): 922-927 |
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| 作者姓名： | Wang BL Hu JP Sheng L Li Y |
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| 作者单位： | 中国医学科学院北京协和医学院药物研究所; |
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| 基金项目： | 国家自然科学基金资助项目(81072696) |
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| 摘 要： | 研究大鼠多次口服五味子成分和体外对肝脏细胞色素P450酶(CYP450)6种同工酶的影响。采用超速离心法制备正常及多次口服五味子醇/水提物的大鼠肝微粒体并与探针药进行体外温孵,应用液相色谱?串联质谱分析方法测定CYP450的6种同工酶特异性探针底物非那西丁(CYP1A2)、右美沙芬(CYP2D2)、双氯芬酸钠(CYP2C6)、美芬妥英(CYP2C11)、氯唑沙宗(CYP2E1)、咪达唑仑(CYP3A1/2)在大鼠肝微粒体的代谢产物生成(对乙酰氨基酚、右啡烷、4-羟基双氯芬酸钠、4-羟基美芬妥英、6-羟基氯唑沙宗、1-羟基咪达唑仑)以反映各CYP450同工酶活性。五味子醇提物(28～120μg.mL-1)体外对大鼠肝微粒体CYP450的6个同工酶均有不同程度的抑制作用。大鼠多次口服五味子醇提物(1.5 g.kg-1,qd×7d)对肝脏CYP3A1/2和CYP2E1有显著诱导作用,对CYP2D2和CYP2C11有明显抑制作用,而对CYP2C6和CYP1A2无明显影响。五味子水提物(100～500μg.mL-1)体外对大鼠肝脏CYP450同工酶亦有抑制作用;体内多次给药(1.5 g.kg-1,qd×7d)对肝脏CY...
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| 关 键 词： | 五味子 细胞色素P450同工酶 诱导 抑制 |
Effects of Schisandra chinensis (Wuweizi) constituents on the activity of hepatic microsomal CYP450 isozymes in rats detected by using a cocktail probe substrates method |
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| Wang Bao-Lian,Hu Jin-Ping,Sheng Li,Li Yan. Effects of Schisandra chinensis (Wuweizi) constituents on the activity of hepatic microsomal CYP450 isozymes in rats detected by using a cocktail probe substrates method[J]. Acta pharmaceutica Sinica, 2011, 46(8): 922-927 |
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| Authors: | Wang Bao-Lian Hu Jin-Ping Sheng Li Li Yan |
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| Affiliation: | WANG Bao-lian,HU Jin-ping,SHENG Li,LI Yan(Institute of Materia Medica,Chinese Academy of Medical Sciences & Peking Union Medical College,Beijing 100050,China) |
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| Abstract: | Effects of constituents from Schisandra chinensis(Wuweizi) on six liver microsomal CYP450 isozymes(CYP1A2,CYP2C6,CYP2C11,CYP2D2,CYP2E1 and CYP3A1/2) were studied in rats in vivo and in vitro.The in vitro incubation was conducted using liver microsomes of rats after multiple dosing of alcoholic/water extract from Schisandra chinensis.A HPLC-MS method was applied to determine the metabolites formation of six CYP450s probe substrates(phenacetin-CYP1A2,dextromethorphan-CYP2D2,diclofenac sodium-CYP2C6,mephenytoi... |
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| Keywords: | Schisandra chinensis(Wuweizi) cytochrome P450 isozyme induction inhibition |
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