| Hypouricaemic action of mangiferin results from metabolite norathyriol via inhibiting xanthine oxidase activity | |
Niu, Yanfen1; Liu, Jia1; Liu, Hai-Yang2 ; Gao, Li-Hui1; Feng, Guo-Hua1; Liu, Xu1; Li, Ling1
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| 2016-09-01 | |
| 发表期刊 | PHARMACEUTICAL BIOLOGY
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| 卷号 | 54期号:9页码:1680-1686 |
| 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. |
| 关键词 | Active Metabolite Hyperuricaemia Structure-activity Relationship Uric Acid Production |
| DOI | 10.3109/13880209.2015.1120322 |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000382572400021 |
| 引用统计 | |
| 文献类型 | 期刊论文 |
| 条目标识符 | http://ir.kib.ac.cn/handle/151853/33584 |
| 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, 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. |
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