中国中药杂志

2017, v.42(02) 357-362

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UPLC-ESI-Q-TOF-MS/MS分析槲皮苷在大鼠肠道菌群中的代谢
Analysis of metabolites of quercitrin in rat intestinal flora by using UPLC-ESI-Q-TOF-MS/MS

覃小丽;孙慧园;杨武;李勇军;郑林;刘亭;黄勇;
QIN Xiao-li;SUN Hui-yuan;YANG Wu;LI Yong-jun;ZHENG Lin;LIU Ting;HUANG Yong;Guizhou Provincial Key Laboratory of Pharmaceutics;School of Pharmacy,Guizhou Medical University;National Engineering Research Center of Miao's Medicines;Engineering Research Center for the Development and Application of Ethnic Medicine and Traditional Chinese Medicine,Ministry of Education;

摘要(Abstract):

该试验主要研究槲皮苷在大鼠肠道菌群中的代谢情况及其可能的生物转化途径,为中药糖苷类成分的代谢机制奠定基础。建立超高效液相色谱串联电喷雾飞行时间质谱测定槲皮苷及其代谢产物的分析方法,流动相为0.1%甲酸水-0.1%甲酸乙腈,梯度洗脱,流速为0.3 m L·min~(-1),扫描方式为电喷雾负离子模式,将大鼠肠道菌群在体外与槲皮苷共同孵育使其发生代谢,采用此方法对其代谢产物进行检测分析,结合Metabolite ToolsT M,质量亏损过滤(MDF)等技术,对代谢产物进行筛查分析以及推测代谢产物化学式。结果显示,槲皮苷发生脱糖、脱氧、乙酰化等反应,脱糖生成的苷元槲皮素进一步发生羟基化、脱氧、还原、开环等反应,得到槲皮素脱氧代谢产物山柰酚、槲皮素C2-C3双键加氢还原产物花旗松素、槲皮苷脱糖基产物槲皮素等。研究结果表明槲皮苷能够在大鼠肠道菌群中发生代谢,增加了化合物的疏水性和化学多样性。
To investigate the metabolism of quercitrin in rat intestinal flora and possible biological pathways,laying the foundation for the metabolic mechanism of traditional Chinese medicine glycosides ingredients. UPLC-Q-TOF-MS / MS method was established to detect the quercitrin and its metabolites with 0. 1 % formic acid solution( A)-0. 1 % formic acid acetonitrile( B) as the mobile phase for gradient elution at a flow rate of 0. 3 m L· min- 1. Electrospray negative ion mode was applied to analyze the metabolites of quercitrin in rat intestinal flora. Metabolite ToolsTM,mass defect filter(MDF) and other technologies were used to screen,analyze the metabolites and infer the chemical formula of the metabolites. The results showed that quercitrin would have degalactoside,deoxygenation and acetylation reactions,and the aglycone quercetin resulted from degalactoside would have further reactions such as hydroxylation,deoxygenation,reduction,and ring opening to achieve deoxygenation metabolite kaempferol,C2-C3 double bonds hydrogenation and reduction product taxifolin,and degalactoside product quercetin. The research results showed that quercitrin can be metabolized by rat intestinal flora,which could increase their hydrophobicity and chemical diversity.

关键词(KeyWords): 槲皮苷;肠道菌群;UPLC-Q-TOF-MS/MS;代谢
quercitrin;intestinal flora;UPLC-Q-TOF-MS /MS;metabolism

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基金项目(Foundation): 国家自然科学基金项目(81260688);; 贵州省研究生卓越人才计划项目(黔教研合ZYRC字[2014]012);; 现代药物研究开发协同创新中心项目(黔教合协同创新字[2013]04);; 民族药与中药开发应用产学研基地建设项目(黔科合KY字[2013]122);; 贵州省优秀青年科技人才培养对象专项(黔科合人字(2015)11号)

作者(Author): 覃小丽;孙慧园;杨武;李勇军;郑林;刘亭;黄勇;
QIN Xiao-li;SUN Hui-yuan;YANG Wu;LI Yong-jun;ZHENG Lin;LIU Ting;HUANG Yong;Guizhou Provincial Key Laboratory of Pharmaceutics;School of Pharmacy,Guizhou Medical University;National Engineering Research Center of Miao's Medicines;Engineering Research Center for the Development and Application of Ethnic Medicine and Traditional Chinese Medicine,Ministry of Education;

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