3,5,2 ',4 '-Tetrahydroxychalcone, a new non-purine xanthine oxidase inhibitor
Niu, Yanfen1; Zhu, Huajie2; Liu, Jia1; Fan, Huafang2,3; Sun, Ling1; Lu, Wei1; Liu, Xu1; Li, Ling1
2011-02-01
发表期刊CHEMICO-BIOLOGICAL INTERACTIONS
ISSN0009-2797
卷号189期号:3页码:161-166
摘要Xanthine oxidase is a key enzyme that catalyses hypoxanthine and xanthine to uric acid and the overproduction of uric acid will lead to hyperuricemia which is an important cause of gout. In the present study, three chalcone derivatives were synthesized and evaluated for inhibitory activity against xanthine oxidase in vitro. Of the compounds, only Compound 1, 3,5,2',4'-tetrahydroxychalcone, exhibited a significant inhibitory activity on xanthine oxidase with an IC(50) value of 22.5 mu M. Lineweaver-Burk transformation of the inhibition kinetics data demonstrated that it was a competitive inhibitor of xanthine oxidase and Ki value was 17.4 mu M. In vivo, intragastric administration of Compound 1 was able to significantly reduce serum uric acid levels and inhibited hepatic xanthine oxidase activities of hyperuricemic mice in a dose-dependent manner. Acute toxicity study in mice showed that Compound 1 was very safe at a dose of up to 5 g/kg. These results suggest that Compound 1 is a novel competitive xanthine oxidase inhibitor and is worthy of further development. (C) 2010 Elsevier Ireland Ltd. All rights reserved.
关键词Xanthine Oxidase 3 Hyperuricemia 5 Uric Acid 2 ' 4 '-tetrahydroxychalcone
资助信息NSFC[30960453, 30873141]; Yunnan Provincial Foundation[20080C021, 2009M018]; 973 Program[2009CB522300]
收录类别SCI
语种英语
引用统计
文献类型期刊论文
条目标识符http://ir.kib.ac.cn/handle/151853/5317
专题植物化学与西部植物资源持续利用国家重点实验室
作者单位1.Kunming Med Univ, Yunnan Key Lab Pharmacol Nat Prod, Kunming 650031, Peoples R China
2.Chinese Acad Sci, Kunming Inst Botany, Organ Synth & Nat Product Lab, State Key Lab Phytochem & Plant Resources W China, Kunming 650204, Peoples R China
3.Hunan Univ, Coll Chem & Chem Engn, Changsha 410082, Hunan, Peoples R China
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Niu, Yanfen,Zhu, Huajie,Liu, Jia,et al. 3,5,2 ',4 '-Tetrahydroxychalcone, a new non-purine xanthine oxidase inhibitor[J]. CHEMICO-BIOLOGICAL INTERACTIONS,2011,189(3):161-166.
APA Niu, Yanfen.,Zhu, Huajie.,Liu, Jia.,Fan, Huafang.,Sun, Ling.,...&Li, Ling.(2011).3,5,2 ',4 '-Tetrahydroxychalcone, a new non-purine xanthine oxidase inhibitor.CHEMICO-BIOLOGICAL INTERACTIONS,189(3),161-166.
MLA Niu, Yanfen,et al."3,5,2 ',4 '-Tetrahydroxychalcone, a new non-purine xanthine oxidase inhibitor".CHEMICO-BIOLOGICAL INTERACTIONS 189.3(2011):161-166.
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