20味中成药对5个人肝微粒体酶活性的影响

徐斌; 赵刚; 位华; 钱小峰; 李静娴; 徐文

留言板

尊敬的读者、作者、审稿人, 关于本刊的投稿、审稿、编辑和出版的任何问题, 您可以本页添加留言。我们将尽快给您答复。谢谢您的支持!

姓名
邮箱
手机号码
标题
留言内容
验证码

x 关闭永久关闭

应中央军委要求，2022年9月起，《药学实践杂志》将更名为《药学实践与服务》，双月刊，正文96页；2023年1月起，拟出版月刊，正文64页，数据库收录情况与原《药学实践杂志》相同。欢迎作者踊跃投稿！

20味中成药对5个人肝微粒体酶活性的影响

徐斌, 赵刚, 位华, 钱小峰, 李静娴, 徐文

文章导航 > 药学实践与服务 > 2009 > 27(5): 353-356

徐斌, 赵刚, 位华, 钱小峰, 李静娴, 徐文. 20味中成药对5个人肝微粒体酶活性的影响[J]. 药学实践与服务, 2009, 27(5): 353-356.

引用本文:

徐斌, 赵刚, 位华, 钱小峰, 李静娴, 徐文. 20味中成药对5个人肝微粒体酶活性的影响[J]. 药学实践与服务, 2009, 27(5): 353-356.

XU Bin, ZHAO Gang, WEI Hua, QIAN Xiao-feng, LI Jing-xian, XU Wen. Effects of 20 Chinese patent medicines on the catalytic activities of five main cytochrome P450s of human liver microsome[J]. Journal of Pharmaceutical Practice and Service, 2009, 27(5): 353-356.

Citation:

XU Bin, ZHAO Gang, WEI Hua, QIAN Xiao-feng, LI Jing-xian, XU Wen. Effects of 20 Chinese patent medicines on the catalytic activities of five main cytochrome P450s of human liver microsome[J]. Journal of Pharmaceutical Practice and Service, 2009, 27(5): 353-356.

20味中成药对5个人肝微粒体酶活性的影响

徐斌^1,,
赵刚²,
位华²,
钱小峰²,
李静娴²,
徐文²

1.
上海交通大学医学院附属瑞金医院,上海200025
2.
中国人民解放军第二军医大学长征医院,上海200003

基金项目: “重大新药创制”科技重大专项课题资助。基金名称:中药5类新药甘西鼠尾总酚酸片临床前研究(2009ZX09102-134);中药药效物质基础及物质资源库研究关键技术(2009ZX09502-013)

Effects of 20 Chinese patent medicines on the catalytic activities of five main cytochrome P450s of human liver microsome

1.
Ruijin Hospital, School of Medicine, Shanghai Jiao Tong University, Shanghai 200025, China
2.
Changzheng Hospital, Second Military Medical University, Shanghai 200003, China

摘要: 目的:考察六神丸等20个常用中成药对CYP1A2、CYP2C9、CYP2C19、CYP2D6和CYP3A4这5个人肝微粒体中主要的药物代谢酶的活性是否有影响。方法:采用人肝微粒体孵育法,分别采用非那西丁、甲苯磺丁脲、美芬妥因、氢溴酸右美沙芬和咪达唑仑作为5个酶的探针药物,采用液相色谱-质谱联用法测定了探针药物代谢产物的浓度,比较分别加入待测药物和空白缓冲液时代谢产物的初始生成速度。结果:六神丸对CYP1A2有明显抑制作用,IC₅₀为28.75μg/mL;肝苏颗粒对CYP2C19有明显抑制作用,IC₅₀为29.80μg/mL;丹参片对CYP1A2有明显抑制作用,IC₅₀为48.55μg/mL;贝羚胶囊对CYP1A2有明显抑制作用,IC₅₀为17.45μg/mL;复方夏天无片对CYP2D6有明显抑制作用,IC₅₀为40.26μg/mL;丹参酮胶囊对CYP1A2、CYP2C9、CYP2C19、CYP2D6和CYP3A4均有明显抑制作用,IC₅₀分别为7.04、13.97、55.77、33.90μg/mL和34.57μg/mL;通风定胶囊对CYP2D6有明显抑制作用,IC₅₀为37.56μg/mL结论:所测定的多数中成药对药物代谢酶有明显的抑制作用,这些药物与药物代谢酶的底物药物联用发生药物相互作用的可能性较大,临床联合用药须谨慎。
- 中成药 /
- 人肝微粒体 /
- 药物代谢酶 /
- 抑制
Abstract: Objective :The effects of the 20 Chinese Patent Medicines on the catalytic activities of five main drug metabolism enzymes of human liver microsome,CYP1A2,CYP2C9,CYP2C19,CYP2D6 and CYP 3A4,were assessed. Methods : Human liver microsome incubation experiment was carried out to assay the injection on the catalytic activities of the enzymes.Phenacetin,tolbutamide,S-mephenytoin,dextromethorphane and midazolam were used as the substrates of the enzymes.After the incubation,the five metabolites of the substrates were quantified by HPLC-MS/MS method.The inhibition was calculated by comparing the formation velocities of metabolites with or without test drug. Results : Liu Shen Pill showed obvious inhibitory effect on CYP1A2 with an IC₅₀ of 28.75 μg/mL;Gan Su Granule showed obvious inhibitory effect on CYP2C19 with an IC₅₀ of 29.80 μg/mL;Dan Shen Tablet showed obvious inhibitory effect on CYP1A2 with an IC₅₀ of 48.55 μg/mL;Bei Ling Capsule showed obvious inhibitory effect on CYP1A2 with an IC₅₀ of 17.45 μg/mL;Xia Tian Wu Compound Tablet showed obvious inhibitory effect on CYP2D6 with an IC₅₀ of 40.26 μg/mL;Tanshinone Capsule showed obvious inhibitory effects on CYP1A2,CYP2C9,CYP2C19,CYP2D6 and CYP3A4 with IC₅₀s of 7.04,13.97,55.77,33.90 and 34.57 μg/mL.Tong Feng Ding Capsule showed obvious inhibitory effect on CYP2D6 with an IC₅₀ of 37.56 μg/mL. Conclusion :Most test drugs showed obvious inhibitory effect on the catalytic activities of drug metabolism enzymes.The result indicated that Chinese Patent Medicine had the potential to induce drug-drug interactions and special attention should be paid when they are used in combined with other drugs.
- Chinese patent medicine /
- human liver microsome /
- drug metabolism enzyme /
- inhibition

[1]	李锐, 张倩倩, 王瑞冬, 高小峰. 国家集中带量采购政策下样本医院良性前列腺增生治疗药物使用情况分析 . 药学实践与服务, 2025, 43(2): 1-6. doi: 10.12206/j.issn.2097-2024.202408031
[2]	杨嘉宁, 赵一颖, 肖伟. 七味脂肝方对非酒精性脂肪性肝炎动物模型的药效学评价 . 药学实践与服务, 2024, 42(9): 389-398. doi: 10.12206/j.issn.2097-2024.202404096
[3]	杨念, 张博乐, 张俊霞, 张振强. 一种中药组合物对ANIT诱导的小鼠胆汁淤积肝损伤的保护作用研究 . 药学实践与服务, 2024, 42(12): 508-511, 519. doi: 10.12206/j.issn.2097-2024.202305008
[4]	修建平, 杨朝爱, 刘禧澳, 潘乾禹, 韦广旭, 王卫星. 全反式维甲酸对肝星状细胞活化及氧化应激的作用和机制探索 . 药学实践与服务, 2024, 42(7): 291-296. doi: 10.12206/j.issn.2097-2024.202312054
[5]	宋雨桐, 夏德润, 顾珩, 唐少文, 易洪刚, 沃红梅. 帕博利珠单抗与铂类化疗方案在晚期非小细胞肺癌一线治疗中的药物经济学评价 . 药学实践与服务, 2024, 42(8): 334-340. doi: 10.12206/j.issn.2097-2024.202303023
[6]	张艺昕, 关欣怡, 王博宁, 闻俊, 洪战英. 二氢吡啶类钙离子拮抗药物手性分析及其立体选择性药动学研究进展 . 药学实践与服务, 2024, 42(8): 319-324. doi: 10.12206/j.issn.2097-2024.202308062
[7]	张晶晶, 索丽娜, 郑兆红. 89例细菌性肝脓肿的临床特征及抗感染治疗分析 . 药学实践与服务, 2024, 42(6): 267-272. doi: 10.12206/j.issn.2097-2024.202302039
[8]	何亚伦, 祁智, 常杰. 消胀通便膏在晚期肝癌患者阿片类药物相关性便秘中的应用研究 . 药学实践与服务, 2024, 42(12): 520-523. doi: 10.12206/j.issn.2097-2024.202309009
[9]	夏哲炜, 曾垣烨, 朱海菲, 李育, 陈啸飞. 核磁共振磷谱法测定磷酸氢钙咀嚼片中药物含量 . 药学实践与服务, 2024, 42(9): 399-401, 406. doi: 10.12206/j.issn.2097-2024.202404063
[10]	陈怡君, 王卓, 何苗, 张宇, 田泾. 泌尿系统碎石术抗菌药物预防使用合理管控实践 . 药学实践与服务, 2024, 42(): 1-5. doi: 10.12206/j.issn.2097-2024.202402034
[11]	晁亮, 王辉, 沈淑琦, 游飘雪, 冀凯宏, 洪战英. 基于UHPLC-Q/TOF-MS代谢组学策略的葛根-知母药对防治阿尔茨海默病的药效与作用机制研究 . 药学实践与服务, 2024, 42(): 1-11. doi: 10.12206/j.issn.2097-2024.202409035
[12]	张元林, 宋凯, 孙蕊, 舒飞, 舒丽芯, 杨樟卫. 基于真实世界数据的药物利用研究综述 . 药学实践与服务, 2024, 42(6): 238-243. doi: 10.12206/j.issn.2097-2024.202312010
[13]	毛智毅, 王筱燕, 陈晓颖, 汤逸斐. 度拉糖肽联合二甲双胍对肥胖型2型糖尿病患者机体代谢、体脂成分及血清脂肪因子的影响 . 药学实践与服务, 2024, 42(7): 305-309. doi: 10.12206/j.issn.2097-2024.202305032
[14]	白学鑫, 陈玉平, 盛春泉, 武善超. 具核梭杆菌小分子抑制剂的筛选及其抗结直肠癌活性研究 . 药学实践与服务, 2024, 42(12): 503-507. doi: 10.12206/j.issn.2097-2024.202405009
[15]	杨媛媛, 安晓强, 许佳捷, 江键, 梁媛媛. 正极性驻极体联合5-氟尿嘧啶对瘢痕成纤维细胞生长抑制的协同作用 . 药学实践与服务, 2024, 42(6): 244-247. doi: 10.12206/j.issn.2097-2024.202310027
[16]	张岩, 李炎君, 刘家荟, 邓娇, 原苑, 张敬一. 药物性肝损伤不良反应分析 . 药学实践与服务, 2024, 42(): 1-5. doi: 10.12206/j.issn.2097-2024.202404034
[17]	刘汝雄, 杨万镇, 涂杰, 盛春泉. 铁死亡调控蛋白GPX4的小分子抑制剂研究进展 . 药学实践与服务, 2024, 42(9): 375-378. doi: 10.12206/j.issn.2097-2024.202312075
[18]	孙丹倪, 黄勇, 张嘉宝, 王培. 代谢相关脂肪性肝病的无创诊断与药物治疗 . 药学实践与服务, 2024, 42(10): 411-418. doi: 10.12206/j.issn.2097-2024.202403049

点击查看大图

计量

文章访问数: 2121
HTML全文浏览量: 243
PDF下载量: 905
被引次数: 0

20味中成药对5个人肝微粒体酶活性的影响

1. 上海交通大学医学院附属瑞金医院,上海200025

2. 中国人民解放军第二军医大学长征医院,上海200003

收稿日期: 2009-08-17

关键词:

中成药 /

人肝微粒体 /

药物代谢酶 /

抑制

摘要: 目的:考察六神丸等20个常用中成药对CYP1A2、CYP2C9、CYP2C19、CYP2D6和CYP3A4这5个人肝微粒体中主要的药物代谢酶的活性是否有影响。方法:采用人肝微粒体孵育法,分别采用非那西丁、甲苯磺丁脲、美芬妥因、氢溴酸右美沙芬和咪达唑仑作为5个酶的探针药物,采用液相色谱-质谱联用法测定了探针药物代谢产物的浓度,比较分别加入待测药物和空白缓冲液时代谢产物的初始生成速度。结果:六神丸对CYP1A2有明显抑制作用,IC₅₀为28.75μg/mL;肝苏颗粒对CYP2C19有明显抑制作用,IC₅₀为29.80μg/mL;丹参片对CYP1A2有明显抑制作用,IC₅₀为48.55μg/mL;贝羚胶囊对CYP1A2有明显抑制作用,IC₅₀为17.45μg/mL;复方夏天无片对CYP2D6有明显抑制作用,IC₅₀为40.26μg/mL;丹参酮胶囊对CYP1A2、CYP2C9、CYP2C19、CYP2D6和CYP3A4均有明显抑制作用,IC₅₀分别为7.04、13.97、55.77、33.90μg/mL和34.57μg/mL;通风定胶囊对CYP2D6有明显抑制作用,IC₅₀为37.56μg/mL结论:所测定的多数中成药对药物代谢酶有明显的抑制作用,这些药物与药物代谢酶的底物药物联用发生药物相互作用的可能性较大,临床联合用药须谨慎。

English Abstract

Effects of 20 Chinese patent medicines on the catalytic activities of five main cytochrome P450s of human liver microsome

1. Ruijin Hospital, School of Medicine, Shanghai Jiao Tong University, Shanghai 200025, China

2. Changzheng Hospital, Second Military Medical University, Shanghai 200003, China

Received Date: 2009-08-17

Keywords:

Abstract: Objective :The effects of the 20 Chinese Patent Medicines on the catalytic activities of five main drug metabolism enzymes of human liver microsome,CYP1A2,CYP2C9,CYP2C19,CYP2D6 and CYP 3A4,were assessed. Methods : Human liver microsome incubation experiment was carried out to assay the injection on the catalytic activities of the enzymes.Phenacetin,tolbutamide,S-mephenytoin,dextromethorphane and midazolam were used as the substrates of the enzymes.After the incubation,the five metabolites of the substrates were quantified by HPLC-MS/MS method.The inhibition was calculated by comparing the formation velocities of metabolites with or without test drug. Results : Liu Shen Pill showed obvious inhibitory effect on CYP1A2 with an IC₅₀ of 28.75 μg/mL;Gan Su Granule showed obvious inhibitory effect on CYP2C19 with an IC₅₀ of 29.80 μg/mL;Dan Shen Tablet showed obvious inhibitory effect on CYP1A2 with an IC₅₀ of 48.55 μg/mL;Bei Ling Capsule showed obvious inhibitory effect on CYP1A2 with an IC₅₀ of 17.45 μg/mL;Xia Tian Wu Compound Tablet showed obvious inhibitory effect on CYP2D6 with an IC₅₀ of 40.26 μg/mL;Tanshinone Capsule showed obvious inhibitory effects on CYP1A2,CYP2C9,CYP2C19,CYP2D6 and CYP3A4 with IC₅₀s of 7.04,13.97,55.77,33.90 and 34.57 μg/mL.Tong Feng Ding Capsule showed obvious inhibitory effect on CYP2D6 with an IC₅₀ of 37.56 μg/mL. Conclusion :Most test drugs showed obvious inhibitory effect on the catalytic activities of drug metabolism enzymes.The result indicated that Chinese Patent Medicine had the potential to induce drug-drug interactions and special attention should be paid when they are used in combined with other drugs.

徐斌, 赵刚, 位华, 钱小峰, 李静娴, 徐文. 20味中成药对5个人肝微粒体酶活性的影响[J]. 药学实践与服务, 2009, 27(5): 353-356.

引用本文:

徐斌, 赵刚, 位华, 钱小峰, 李静娴, 徐文. 20味中成药对5个人肝微粒体酶活性的影响[J]. 药学实践与服务, 2009, 27(5): 353-356.

Citation:

XU Bin, ZHAO Gang, WEI Hua, QIAN Xiao-feng, LI Jing-xian, XU Wen. Effects of 20 Chinese patent medicines on the catalytic activities of five main cytochrome P450s of human liver microsome[J]. Journal of Pharmaceutical Practice and Service, 2009, 27(5): 353-356.

全文HTML

下载: 全尺寸图片幻灯片

返回文章

用微信扫码二维码

分享至好友和朋友圈

主管、主办: 中国人民解放军海军军医大学地址: 上海市杨浦区国和路325号邮政编码: 200433

电话: （021）81871324,81871397 E-mail: yxsjzzs@163.com

网站备案号沪ICP备05003363号-1

本系统由北京仁和汇智信息技术有限公司开发

留言板

20味中成药对5个人肝微粒体酶活性的影响

Effects of 20 Chinese patent medicines on the catalytic activities of five main cytochrome P450s of human liver microsome

计量

出版历程

20味中成药对5个人肝微粒体酶活性的影响

1. 上海交通大学医学院附属瑞金医院,上海200025 2. 中国人民解放军第二军医大学长征医院,上海200003

English Abstract

Effects of 20 Chinese patent medicines on the catalytic activities of five main cytochrome P450s of human liver microsome

1. Ruijin Hospital, School of Medicine, Shanghai Jiao Tong University, Shanghai 200025, China 2. Changzheng Hospital, Second Military Medical University, Shanghai 200003, China

全文HTML

目录

1. 上海交通大学医学院附属瑞金医院,上海200025

2. 中国人民解放军第二军医大学长征医院,上海200003

1. Ruijin Hospital, School of Medicine, Shanghai Jiao Tong University, Shanghai 200025, China

2. Changzheng Hospital, Second Military Medical University, Shanghai 200003, China