[关键词]
[摘要]
为了解槲皮素、芦丁、没食子酸及其与维生素C联用对黄嘌呤氧化酶(XOD)的抑制特性,本文通过建立黄嘌呤氧化酶体外抑制模型,以别嘌呤醇为阳性对照,测定这三种天然化合物在不同浓度下对XOD的抑制效果及抑制动力学。结果表明:三种物质对黄嘌呤氧化酶均有抑制作用,且具有浓度依赖性,其抑制效果与结构和本身性质有明显相关性,抑制作用强弱次序为槲皮素>芦丁>没食子酸,半抑制浓度IC50值分别为(5.51±0.41) μmol/L、(48.66±0.49) μmol/L、>200 μmol/L;单一没食子酸抑制效果较弱,而没食子酸在维生素C的协同下,对XOD的抑制率从20.17%提高至40.96%,起到提高抑制效果和体系稳定性的双重作用;以上三种物质对XOD的抑制类型属于不同模式的非经典型混合抑制剂。本文对研究此类物质的抑制机理和应用有重要意义。
[Key word]
[Abstract]
In order to understand the inhibitory properties of quercetin, rutin, gallic acid and its combination with vitamin C on Xanthine oxidase (XOD), a vitro inhibition model of XOD was established to evaluate the inhibitory effect of these three natural compounds on XOD at different concentrations. Allopurinol was used as the positive control. The inhibitory effects and kinetics of these three natural compounds on XOD at different concentrations were detected. The results showed that all the three substances had the inhibitory effect on XOD with concentration dependence, and the inhibitory effect was greatly related to the structure and their nature. The order of inhibition of XOD was as follow: quercetin > rutin > gallic acid. The IC50 values were (5.51±0.41) μmol/L, (48.66±0.49) μmol/L and >200 μmol/L for the three substances respectively. In this work, the inhibition effect of gallic acid was weak and it was demonstrated that vitamin C could assist gallic acid to participate in the reaction. The inhibition rate increased from 20.17% to 40.96%. It could achieve the dual effect of enhanced inhibition of XOD activity and stability. The types of XOD inhibition by quercetin, rutin, and gallic acid belong to different modes of atypical mixed inhibitors. This work will be of great significance to study the inhibition mechanism and application of these substances.
[中图分类号]
[基金项目]
国家级大学生创新创业训练计划项目资助(201910340021);浙江省大学生科技创新活动计划(新苗人才计划)项目(2019R411018)