3,5,2 ',4 '-Tetrahydroxychalcone, a new non-purine xanthine oxidase inhibitor

CORC > 昆明植物研究所 > 中国科学院昆明植物研究所 > 植物化学与西部植物资源持续利用国家重点实验室

	3,5,2 ',4 '-Tetrahydroxychalcone, a new non-purine xanthine oxidase inhibitor
	Niu, Yanfen 1; Zhu, Huajie 2; Liu, Jia 1; Fan, Huafang 2,3; Sun, Ling 1; Lu, Wei 1; Liu, Xu 1; Li, Ling 1
刊名	CHEMICO-BIOLOGICAL INTERACTIONS
	2011-02-01
卷号	189 期号:3 页码:161-166
关键词	3 Xanthine oxidase Hyperuricemia Uric acid 5 2 ' 4 '-Tetrahydroxychalcone
ISSN号	0009-2797
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
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.
学科主题	Biochemistry & Molecular Biology; Pharmacology & Pharmacy; Toxicology
类目[WOS]	Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Toxicology
研究领域[WOS]	Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Toxicology
关键词[WOS]	URIC-ACID ; CHALCONES ; RAT
收录类别	SCI
资助信息	NSFC[30960453, 30873141]; Yunnan Provincial Foundation[20080C021, 2009M018]; 973 Program[2009CB522300]
语种	英语
WOS记录号	WOS:000290291200004
公开日期	2012-04-10
内容类型	期刊论文
源URL	[http://ir.kib.ac.cn/handle/151853/5317]
专题	昆明植物研究所_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.