• 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Mass Spectrometry Letters >In Vitro Inhibitory Effect of Licoricidin on Human Cytochrome P450s
【24h】

In Vitro Inhibitory Effect of Licoricidin on Human Cytochrome P450s

机译：Licoricidin对人细胞色素P450的体外抑制作用

获取原文
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

Licoricidin isolated from Glycyrrhiza uralensis is known to have anticancer, anti-nephritic, anti-Helicobacter pylori, and antibacterial effects. In this study, a cocktail probe assay and liquid chromatography-tandem mass spectrometry (LC-MS/MS) were used to investigate the modulating effect of licoricidin on cytochrome P450 (CYP) enzymes in human liver microsomes. When licoricidin was incubated at with CYP probes for 60 min at , it showed potent inhibitory effects on CYP2B6-catalyzed bupropion hydroxylation and CYP2C9-catalyzed diclofenac 4`-hydroxylation with half maximal inhibitory concentration ( ) values of 3.4 and , respectively. The inhibition mode of licoricidin was revealed as competitive, dose-dependent, and non-time-dependent, and following the pattern of Lineweaver-Burk plots. The inhibitory effect of licoricidin has been confirmed in human recombinant cDNA-expressed CYP2B6 and 2C9 with values of 4.5 and , respectively. In conclusion, this study has shown the potent inhibitory effect of licoricidin on CYP2B6 and CYP2C9 activity could be important for predicting potential herb-drug interactions with substrates that mainly undergo CYP2B- and CYP2C9-mediated metabolism.
机译：已知从甘草中分离出的Licoricidin具有抗癌，抗肾病，抗幽门螺杆菌和抗菌作用。在这项研究中，使用了鸡尾酒探针测定法和液相色谱-串联质谱法（LC-MS / MS）来研究licoricidin对人肝微粒体中细胞色素P450（CYP）酶的调节作用。当将licoricidin与CYP探针在一起于70℃温育60分钟时，它显示出对CYP2B6催化的安非他酮羟基化和CYP2C9催化的双氯芬酸4'-羟基化的有效抑制作用，其最大抑制浓度（）值分别为3.4和。 licoricidin的抑制模式显示为竞争性，剂量依赖性和非时间依赖性，并且遵循Lineweaver-Burk图的模式。已经在人重组cDNA表达的CYP2B6和2C9中确认了licoricidin的抑制作用，其值分别为4.5和4.5。总之，这项研究表明，licoricidin对CYP2B6和CYP2C9活性的有效抑制作用对于预测与主要经历CYP2B和CYP2C9介导的代谢的底物之间的潜在药效相互作用可能是重要的。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号