| 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 | |
| 通讯作者 | Li, L (reprint author), Kunming Med Univ, Yunnan Key Lab Pharmacol Nat Prod, Ren Min W Rd 191, Kunming 650031, Peoples R China |
| 2011-02-01 | |
| 发表期刊 | CHEMICO-BIOLOGICAL INTERACTIONS
 |
| ISSN | 0009-2797 |
| 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 |
| 学科领域 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Toxicology |
| DOI | 10.1016/j.cbi.2010.12.004 |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000290291200004 |
| 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 |
| 推荐引用方式 GB/T 7714 | 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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