北京大学医学部机构知识库
Advanced  
IR@PKUHSC  > 北京大学第一临床医学院  > 临床药理研究所  > 期刊论文
学科主题: 临床医学
题名:
Determination of the inhibitory potential of 6 fluoroquinolones on CYP1A2 and CYP2C9 in human liver microsomes
作者: Zhang, Li; Wei, Min-ji; Zhao, Cai-yun; Qi, Hui-min
关键词: cytochrome P450 enzyme ; liquid chromatography/mass spectrometry ; liver microsome ; fluoroquinolone
刊名: ACTA PHARMACOLOGICA SINICA
发表日期: 2008-12-01
DOI: 10.1111/j.1745-7254.2008.00908.x
卷: 29, 期:12, 页:1507-1514
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Chemistry, Multidisciplinary ; Pharmacology & Pharmacy
研究领域[WOS]: Chemistry ; Pharmacology & Pharmacy
关键词[WOS]: TANDEM MASS-SPECTROMETRY ; INTENSIVE-CARE-UNIT ; IN-VITRO COCKTAIL ; WARFARIN INTERACTION/ ; HEALTHY-VOLUNTEERS ; DRUG-INTERACTIONS ; ORGANIC-SOLVENTS ; RAT PLASMA ; 500 MG ; LEVOFLOXACIN
英文摘要:

Aim: To determine the inhibitory potential of 2 new fluoroquinolones, caderofloxacin and antofloxacin, together with 4 marketed fluoroquinolones, moxifloxacin, gatifloxacin, levofloxacin, and ciprofloxacin, on the activity of cytochrome P450 isoforms 1A2 (CYP1A2) and 2C9 (CYP2C9). Methods: Probe substrates, phenacetin (CYP1A2), and tolbutamide (CYP2C9) were incubated with human liver microsomes and the metabolites were analyzed by liquid chromatography/mass spectrometry using electrospray ionization in positive or negative mode. Glipizide was used as the internal standard in both modes. The inhibitory potential of fluoroquinolones on CYP1A2 and CYP2C9 was investigated. Results: The IC(50) values (mu mol/L) determined with the cocktail were in agreement with individual probe substrates ((X-naphthoflavone: 0.27 vs 0.26; sulfaphenazole: 0.49 vs 0.37). Ciprofloxacin showed weak inhibition on both the activity of CYP1A2 (IC(50) 135 mu mol/L) and CYP2C9 (IC(50) 180 mu mol/L), whereas levofloxacin inhibited only CYP2C9 (IC(50) 210 mu mol/L). Caderofloxacin, antofloxacin, moxifloxacin, and gatifloxacin showed little or no inhibition on the activity of CYP1A2 or CYP2C9 when tested at comparable concentrations (0-200 mg/L). Conclusion: Caderofloxacin, antofloxacin, moxifloxacin, and gatifloxacin are negligible inhibitors to CYP1A2 and CYP2C9. The in vitro system can be used as a high-throughput model to screen similar compounds for the early identification of drug-drug interaction potential.

语种: 英语
WOS记录号: WOS:000261710300014
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/67108
Appears in Collections:北京大学第一临床医学院_临床药理研究所_期刊论文

Files in This Item:

There are no files associated with this item.


作者单位: Peking Univ, Hosp 1, Inst Clin Pharmacol, Beijing 100191, Peoples R China

Recommended Citation:
Zhang, Li,Wei, Min-ji,Zhao, Cai-yun,et al. Determination of the inhibitory potential of 6 fluoroquinolones on CYP1A2 and CYP2C9 in human liver microsomes[J]. ACTA PHARMACOLOGICA SINICA,2008,29(12):1507-1514.
Service
Recommend this item
Sava as my favorate item
Show this item's statistics
Export Endnote File
Google Scholar
Similar articles in Google Scholar
[Zhang, Li]'s Articles
[Wei, Min-ji]'s Articles
[Zhao, Cai-yun]'s Articles
CSDL cross search
Similar articles in CSDL Cross Search
[Zhang, Li]‘s Articles
[Wei, Min-ji]‘s Articles
[Zhao, Cai-yun]‘s Articles
Related Copyright Policies
Null
Social Bookmarking
Add to CiteULike Add to Connotea Add to Del.icio.us Add to Digg Add to Reddit
所有评论 (0)
暂无评论
 
评注功能仅针对注册用户开放,请您登录
您对该条目有什么异议,请填写以下表单,管理员会尽快联系您。
内 容:
Email:  *
单位:
验证码:   刷新
您在IR的使用过程中有什么好的想法或者建议可以反馈给我们。
标 题:
 *
内 容:
Email:  *
验证码:   刷新

Items in IR are protected by copyright, with all rights reserved, unless otherwise indicated.

 

 

Valid XHTML 1.0!
Copyright © 2007-2017  北京大学医学部 - Feedback
Powered by CSpace