地榆鞣质在大鼠尿液中代谢产物分析  

Metabolites of Tannins from Sanguisorba officinalis L. in Rat Urine

作　　者：周本宏[1,2] 汪静[1] 吴玥[1] 易慧兰 谭珺[2] 张红盼[1] 

机构地区：[1]武汉大学人民医院药学部,湖北武汉430060 [2]武汉大学药学院,湖北武汉430072

出　　处：《中国现代中药》2017年第6期784-793,共10页Modern Chinese Medicine

摘　　要：目的:采用HPLC-Q-TOF/MS研究地榆鞣质在尿液中的代谢产物。方法:收集给药后大鼠尿样,采用ZORBAX Eclipse XDB-C_(18)(150 mm×2.1 mm,5μm)色谱柱,以乙腈-水为流动相梯度洗脱,在飞行时间质谱负离子模式下扫描,利用TOF/MS得到的准确相对分子质量及一级、二级质谱信息,对照化学成分数据库,鉴定地榆鞣质在大鼠尿液中可能的代谢产物,结合相关文献,推测地榆鞣质在大鼠体内可能的代谢途径。结果:从大鼠尿液中共检测到9个代谢产物,分别为:M1(Pyrogallol)、M2(Urolithin B)、M3(Methyl-Urolithin C)、M4(Urolithin A)、M5(Methyl-Urolithin A)、M6(Urolithin C-Glucuronidation)、M7(Dimethy-EA)、M8(Urolithin M5)、M9(没食子酸),其中M9为原型药物。结论:地榆鞣质经灌胃给予大鼠后,先经过I相代谢反应生成尿石素等极性偏小的代谢产物吸收进入体内,再发生Ⅱ相结合反应,与葡萄糖醛酸等结合,变成极性较大的物质,从尿液排除体外,进一步阐明了地榆鞣质在体内发挥药理作用的机理。Objective：To investigate the metabolites in urine of rats administrated with tannins extracted from Sanguisorba officinalis L.（STE） by gavage,liquid chromatography time of flight mass spectrometry （HPLC-TOF-MS） was employed.Methods：Rat’s urine samples were collected and analyze by liquid chromatography time of flight mass spectrometry （HPLC-TOF-MS）.The analysis was performed on a ZORBAX Eclipse XDB-C18 column with an acetonitrile-water gradient elution.Time of flight mass spectrometer （TOF/MS） was applied for qualitative analysis under negative ion mode.Based on the accurate molecular weight,MS and MS2 information of TOF/MS detection and the compound list established previously,the possible metabolites of STE were identified.Results：Nine metabolites were detected in the rat urine：pyrogallol （M1）,urolithin B （M2）,methyl-urolithin C （M3）,urolithin A （M4）,methyl-urolithin A （M5）,urolithin C-clucuronidation （M6）,dimethy-EA （M7）,urolithin M5 （M8）,gallic acid （M9）.M9 was the prototype drug.Conclusion：Tannins from S.officinalis set off I phase metabolic reactions first to generate weak polarity metabolites such as urolithins after entering in vivo,then the II phase reaction were happened to combined with glucuronide to increase its polarity,so as to excrete out through urine,which further clarifies the function mechanism of tannins from S.officinalis.

关 键 词：地榆 鞣质 代谢产物 尿石素 液质联用 

分 类 号：R977[医药卫生—药品]