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题名: 3,5,2 ',4 '-Tetrahydroxychalcone, a new non-purine xanthine oxidase inhibitor
作者: Niu, Yanfen1; Zhu, Huajie2; Liu, Jia1; Fan, Huafang2, 3; Sun, Ling1; Lu, Wei1; Liu, Xu1; Li, Ling1
刊名: CHEMICO-BIOLOGICAL INTERACTIONS
关键词: 3,5,2 ',4 '-Tetrahydroxychalcone ; Xanthine oxidase ; Hyperuricemia ; Uric acid
英文摘要: 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.
出版日期: 2011-02-01
卷号: 189, 期号:3, 页码:161-166
DOI标识: 10.1016/j.cbi.2010.12.004
语种: 英语
ISSN号: 0009-2797
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内容类型: 期刊论文
URI标识: http://ir.kib.ac.cn/handle/151853/5317
Appears in Collections:植物化学与西部植物资源持续利用国家重点实验室_期刊论文

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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

Recommended Citation:
Niu, YF; Zhu, HJ; Liu, J; Fan, HF; Sun, L; Lu, W; Liu, X; Li, L.3,5,2 ',4 '-Tetrahydroxychalcone, a new non-purine xanthine oxidase inhibitor,CHEMICO-BIOLOGICAL INTERACTIONS,2011,189(3):161-166
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