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引用本文:刘澄铭,职文倩,任静,张培玉,郜娜.和厚朴酚、厚朴酚、栀子苷、绿原酸和黄芪甲苷对人和大鼠体外CYP1A2、CYP3A和CYP2D的抑制作用[J].中国现代应用药学,2016,33(7):871-875.
LIU Chengming,ZHI Wenqian,REN Jing,ZHANG Peiyu,GAO Na.In Vitro Inhibitory Effects of Honokiol, Magnolol, Geniposide, Chlorogenic Acid, and Astragaloside Ⅳ on CYP1A2, CYP3A and CYP2D Activity in Human and Rats[J].Chin J Mod Appl Pharm(中国现代应用药学),2016,33(7):871-875.
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和厚朴酚、厚朴酚、栀子苷、绿原酸和黄芪甲苷对人和大鼠体外CYP1A2、CYP3A和CYP2D的抑制作用
刘澄铭1,2, 职文倩1,2, 任静1,2, 张培玉1,2, 郜娜3
1.郑州大学,临床药理研究所;2.临床医学系,郑州 450052;3.郑州大学临床药理研究所,郑州 450052
摘要:
目的 观察和厚朴酚、厚朴酚、栀子苷、绿原酸和黄芪甲苷5种中药成分体外对人和大鼠肝CYP1A2、CYP3A和CYP2D的抑制作用。方法 在人和大鼠肝微粒体孵育体系中,分别以非那西丁、咪达唑仑和右美沙芬为探针,应用HPLC检测受试物对探针代谢产物生成量的影响,评估5种中药成分对CYP1A2、CYP3A和CYP2D在该体系中的活性影响,并计算得到抑制率和IC50。结果 和厚朴酚对人和大鼠CYP1A2、CYP2D的IC50值分别为5.5、3.9、35.3和46.7 μmol·L-1;厚朴酚对人CYP1A2、大鼠CYP1A2和CYP2D的IC50值分别为23.8,29.1和39.9 μmol·L-1;栀子苷、绿原酸和黄芪甲苷对3种CYP酶亚型的IC50均>100 μmol·L-1;和厚朴酚对人和大鼠CYP3A的IC50均>100 μmol·L-1;厚朴酚对人CYP3A、CYP2D和大鼠CYP3A的IC50均>100 μmol·L-1。结论 和厚朴酚体外对人和大鼠CYP1A2和CYP2D有抑制作用,厚朴酚体外对人CYP1A2、大鼠CYP1A2和CYP2D有抑制作用,均呈浓度依赖性。
关键词:  和厚朴酚  厚朴酚  栀子苷  绿原酸  黄芪甲苷  细胞色素P450  肝微粒体
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基金项目:河南省高等学校重点科研项目计划(15A310025);郑州大学全国大学生创新创业训练计划资助项目(2014xjxm340)
In Vitro Inhibitory Effects of Honokiol, Magnolol, Geniposide, Chlorogenic Acid, and Astragaloside Ⅳ on CYP1A2, CYP3A and CYP2D Activity in Human and Rats
LIU Chengming1,2, ZHI Wenqian1,2, REN Jing1,2, ZHANG Peiyu1,2, GAO Na3
1.Zhengzhou University, Clinical Pharmacology Research Institute;2.Department of Clinical Medicine, Zhengzhou 450052, China;3.Clinical Pharmacology Research Institute, Zhengzhou University, Zhengzhou 450052, China
Abstract:
OBJECTIVE To evaluate the in vitro inhibitory effects of five kinds of herbal constituents (honokiol, magnolol, geniposide, chlorogenic acid, astragaloside Ⅳ) on CYP1A2, CYP3A and CYP2D in human and rat liver microsomes. METHODS The activities of CYP1A2, CYP3A and CYP2D in human and rat liver microsomes were evaluated by detecting turnovers of its substrates after treatment with the five kinds of herbal constituents in vitro by HPLC. Phenacetin, midazolam and dextromethorphan were used as substrates of CYP1A2, CYP3A and CYP2D, then the inhibition ratio and IC50 were calculated. RESULTS The IC50 of honokiol on CYP1A2 in human and rat were 5.5, 3.9 μmol·L-1 and CYP2D in human and rat were 35.3 and 46.7 μmol·L-1, respectively. The IC50 of magnolol on CYP1A2 in human, CYP1A2 and CYP2D in rat were 23.8, 29.1 and 39.9 μmol·L-1, respectively. The IC50 of geniposide, chlorogenic acid and astragaloside Ⅳ on the three kinds of CYP enzyme subtypes were greater than 100 μmol·L-1. The IC50 of honokiol on human and rat CYP3A were >100 μmol·L-1. The IC50 of magnolol on human CYP3A, CYP2D and rat CYP3A were also >100 μmol·L-1. CONCLUSION The activities of CYP1A2 and CYP2D in human and rat liver microsomes are respectively inhibited by honokiol, the activities of CYP1A2 in human and rat liver microsomes and CYP2D in rat liver microsomes are respectively inhibited by magnolol, which are all in a dose-dependent manner in vitro.
Key words:  honokiol  magnolol  geniposide  chlorogenic acid  astragaloside Ⅳ  cytochrome P450  liver microsomes
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