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学科主题临床医学
Determination of the inhibitory potential of 6 fluoroquinolones on CYP1A2 and CYP2C9 in human liver microsomes
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
2008-12-01
DOI10.1111/j.1745-7254.2008.00908.x
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
引用统计
被引频次:20[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/67108
专题北京大学第一临床医学院_临床药理研究所
作者单位Peking Univ, Hosp 1, Inst Clin Pharmacol, Beijing 100191, Peoples R China
推荐引用方式
GB/T 7714
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.
APA Zhang, Li,Wei, Min-ji,Zhao, Cai-yun,&Qi, Hui-min.(2008).Determination of the inhibitory potential of 6 fluoroquinolones on CYP1A2 and CYP2C9 in human liver microsomes.ACTA PHARMACOLOGICA SINICA,29(12),1507-1514.
MLA Zhang, Li,et al."Determination of the inhibitory potential of 6 fluoroquinolones on CYP1A2 and CYP2C9 in human liver microsomes".ACTA PHARMACOLOGICA SINICA 29.12(2008):1507-1514.
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