首页>>文献首页>>文献正文

Screening for selective inhibitors of xanthine oxidase from Flos Chrysanthemum using ultrafiltration LC–MS combined with enzyme channel blocking

luohanguo 添加于 2017/5/14 12:12:25  32次阅读 | 0次推荐 | 0个评论

In this study, a new method based on ultrafiltration liquid chromatography-mass spectrometry (UF-LC–MS) combined with enzyme channel blocking (ECB) was developed to discover bioactive components from herbal medicines. Xanthine oxidase (XOD), a critical enzyme for treating gout, was employed as the target protein for screening. By comparing chromatographic profiles of the compounds binding to XOD before and after the ECB experiment, the selective ligands could be distinguished from the non-selective binders. In this experiment, febuxostat bound to the channel entering into the active site of the enzyme and prevented potential ligands from binding. Finally, four compounds, namely, luteolin-7-O-glucoside, apigenin-7-O-glucoside, luteolin and apigenin were screened and identified as the candidate XOD inhibitors based on the ultrafiltration chromatogram of Flos Chrysanthemum, a famous traditional Chinese medicine used in many prescriptions for gout treatment. To verify the compounds screened further, a microplate method was applied to evaluate their enzyme inhibitory activities. The IC50 values of the above 4 compounds were 23.61, 38.80, 1.54 and 1.96 μM, respectively. The structure-function relationship was also estimated according to the in vitro assay. The results were in favor of the hypothesis that the Flos Chrysanthemum extract might be used for gout treatment by inhibiting XOD.

作 者:Hui-Peng Song, Hui Zhang, Yu Fu, Hua-yan Mo, Mu Zhang, Jun Chen, , Ping Li
期刊名称:
期卷页: 第卷 第期 页
学科领域:医学科学 » 中药学 » 民族药学
添加人是否为作者:
原文链接:http://www.sciencedirect.com/science/article/pii/S1570023214003018
DOI:
ISBN:
关键词:
备 注:
来自论坛的回复:
文献笔记

   
导出选项:

评论 (0 个评论)

Page 1 of 1
<<<[1]>>>
发表评论:
验证码  
 

举报 | Archiver | 科学网( 京ICP备07017567 )

GMT+8, 2011-2-15 11:31

Powered by ScienceNet.cn

Copyright © 2007-2011 科学时报社