崔 涛1, 2,曾 勇2 *,梅林雨2,高 晶2,伊秀林2,司端运2.吡咯里嗪类非甾体抗炎药ML-3000衍生物对人P450同工酶的体外抑制作用[J].药物评价研究,2013,36():1-4
吡咯里嗪类非甾体抗炎药ML-3000衍生物对人P450同工酶的体外抑制作用
Inhibition of ML-3000 derivatives in Non-steroidal anti-inflammatory drugs of the pyrrolizine on human cytochrome P450 isozymes in vitro system
投稿时间:2013-04-27  
DOI:
中文关键词:  肝细胞色素P450;NO供体化合物;IC50
英文关键词:cytochrome P450; NO donor compound; IC50
基金项目:
作者单位
崔 涛1, 2,曾 勇2 *,梅林雨2,高 晶2,伊秀林2,司端运2 1. 天津中医药大学,天津 300193;2. 天津药物研究院 天津市新药安全评价研究中心,天津 300193 
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中文摘要:
      目的 研究吡咯里嗪类ML-3000及其两种NO供体衍生物ML-4000和ML-5000对人P450同工酶CYP2D6、CYP1A2、CYP2C9、CYP2C19和CYP3A4的体外抑制作用。方法 采用Gentest公司的高通量P450酶抑制剂筛选试剂盒(High throughput Inhibitor Screening Kit),测定ML-3000、ML-4000和ML-5000对五种P450同工酶CYP2D6、CYP1A2、CYP2C9、CYP2C19和CYP3A4的体外抑制作用。结果 ML-3000、ML-4000和ML-5000抑制CYP3A4的IC50分别为7.07、0.40和2.82 μmol/L,对其他4个酶(CYP1A2、CYP2D6、CYP2C9和CYP2C19)的IC50均大于10 μmol/L。结论 三种化合物对CYP3A4活力均有抑制作用,其中ML-4000的抑制能力最强。3种化合物对其他4个酶基本没有抑制作用。
英文摘要:
      Objective Investigate the inhibition effect of ML-3000 and two NO donor derivatives in pyrrolizine on five human cytochrome P450 isozymes CYP2D6, CYP1A2, CYP2C9, CYP2C19 and CYP3A4. Methods Determine inhibition effect of ML-3000, ML-4000 and ML-5000 on five human cytochrome P450 isozymes CYP2D6, CYP1A2, CYP2C9, CYP2C19 and CYP3A4 with High Throughput Inhibitor Sceening Kit. Results IC50 values of ML-3000, ML-4000 and ML-5000 to CYP3A4 were 7.07, 0.40 and 2.82 μM, respectively. IC50 values of ML-3000, ML-4000 and ML-5000 to others were more than 10μM. Conclusion Three compounds have inhibition effects on CYP3A4. Among them ML-4000 has the strongest inhibition effect. The inhibition effect of three compounds on other four enzymes doesn’t exist basically.
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