Hypouricaemic action of mangiferin results from metabolite norathyriol via inhibiting xanthine oxidase activity

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

	Hypouricaemic action of mangiferin results from metabolite norathyriol via inhibiting xanthine oxidase activity
	Niu, Yanfen 1; Liu, Jia 1; Liu, Hai-Yang2 ; Gao, Li-Hui 1; Feng, Guo-Hua 1; Liu, Xu 1; Li, Ling 1
刊名	PHARMACEUTICAL BIOLOGY
	2016-09-01
卷号	54 期号:9 页码:1680-1686
关键词	Active metabolite hyperuricaemia structure-activity relationship uric acid production
英文摘要	Context Mangiferin has been reported to possess a potential hypouricaemic effect. However, the pharmacokinetic studies in rats showed that its oral bioavailability was only 1.2%, suggesting that mangiferin metabolites might exert the action.Objective The hypouricaemic effect and the xanthine oxidase inhibition of mangiferin and norathyriol, a mangiferin metabolite, were investigated. Inhibition of norathyriol analogues (compounds 3-9) toward xanthine oxidase was also evaluated.Materials and methods For a dose-dependent study, mangiferin (1.5-6.0mg/kg) and norathyriol (0.92-3.7mg/kg) were administered intragastrically to mice twice daily for five times. For a time-course study, mice received mangiferin and norathyriol both at a single dose of 7.1mol/kg. In vitro, inhibition of test compounds (2.4-2.4mM) against xanthine oxidase activity was evaluated by the spectrophotometrical method. The inhibition type was identified from Lineweaver-Burk plots.Results Norathyriol (0.92, 1.85 and 3.7mg/kg) dose dependently decreased the serum urate levels by 27.0, 33.6 and 37.4%, respectively. The action was more potent than that of mangiferin at the low dose, but was equivalent at the higher doses. Additionally, the hypouricaemic action of them exhibited a time dependence. In vitro, norathyriol markedly inhibited the xanthine oxidase activities, with the IC50 value of 44.6M, but mangiferin did not. The kinetic studies showed that norathyriol was an uncompetitive inhibitor by Lineweaver-Burk plots. The structure-activity relationships exhibited that three hydroxyl groups in norathyriol at the C-1, C-3 and C-6 positions were essential for maintaining xanthine oxidase inhibition.Discussion and conclusion Norathyriol was responsible for the hypouricaemic effect of mangiferin via inhibiting xanthine oxidase activity.
类目[WOS]	Plant Sciences ; Medical Laboratory Technology ; Pharmacology & Pharmacy
研究领域[WOS]	Plant Sciences ; Medical Laboratory Technology ; Pharmacology & Pharmacy
关键词[WOS]	POLYGALA-CROTALARIOIDES ; URIC-ACID ; HYPERURICEMIA ; XANTHONES ; ENZYME ; SERUM ; GOUT
收录类别	SCI
语种	英语
WOS记录号	WOS:000382572400021
内容类型	期刊论文
源URL	[http://ir.kib.ac.cn/handle/151853/33584]
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, Biomed Engn Res Ctr, Kunming, Peoples R China 2.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming, Peoples R China
推荐引用方式 GB/T 7714	Niu, Yanfen,Liu, Jia,Liu, Hai-Yang,et al. Hypouricaemic action of mangiferin results from metabolite norathyriol via inhibiting xanthine oxidase activity[J]. PHARMACEUTICAL BIOLOGY,2016,54(9):1680-1686.
APA	Niu, Yanfen.,Liu, Jia.,Liu, Hai-Yang.,Gao, Li-Hui.,Feng, Guo-Hua.,...&Li, Ling.(2016).Hypouricaemic action of mangiferin results from metabolite norathyriol via inhibiting xanthine oxidase activity.PHARMACEUTICAL BIOLOGY,54(9),1680-1686.
MLA	Niu, Yanfen,et al."Hypouricaemic action of mangiferin results from metabolite norathyriol via inhibiting xanthine oxidase activity".PHARMACEUTICAL BIOLOGY 54.9(2016):1680-1686.