期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 75, 期 -, 页码 289-296出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.01.058
关键词
Aloe-emodin; Xanthine oxidase; Inhibitor; Gout
资金
- Natural Science Foundation of P.R. China [21162006]
- Postdoctoral Science Foundation of China [2012M521659]
- Collegiate Natural Science Fund of Jiangsu Province [12KJB350001]
A series of aloe-emodin derivatives were synthesized and evaluated as xanthine oxidase inhibitors. Among them, four aloe-emodin derivatives showed significant inhibitory activities against xanthine oxidase. The compound 4,5-dihydroxy-9,10-dioxo-9,10-dihydroanthracene-2-carbaldehyde (A1) possessed the best xanthine oxidase inhibitory activity with IC50 of 2.79 mu M. Lineweaver-Burk plot analysis revealed that A1 acted as a mixed-type inhibitor for xanthine oxidase. The docking study revealed that the molecule A1 had strong interactions with the active site of xanthine oxidase and this result was in agreement with kinetic study. Consequently, compound A1 is a new-type candidate for further development for the treatment of gout. (C) 2014 Elsevier Masson SAS. All rights reserved.
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