Identification of major parent compounds and metabolites in bile, plasma and urine of rats after oral administration of Radix Scutellariae extract by UFLC-IT-TOF/MS  

采用UFLC-IT-TOF/MS鉴定大鼠口服黄芩提取物后胆汁、血浆和尿液中的主要成分(英文)

作　　者：陈正为[1,2] 佟玲[2,3] 李淑明[2] 李东翔[2] 刘小琳[2] 丁黎[1] 朱永宏[2] 周水平[2] 孙鹤[2] 

机构地区：[1]中国药科大学药物分析研究室,江苏南京210009 [2]天士力集团研究院,天津300402 [3]中国药科大学药物代谢研究中心,江苏南京210009

出　　处：《Journal of Chinese Pharmaceutical Sciences》2013年第4期319-328,共10页中国药学（英文版）

基　　金：National Key Special Project of Science and Technology for Innovation Drugs of China (Grant No. 2013ZX09402202)

摘　　要：Flavonoids are the main bioactive components of Radix Scutellariae, a well-known traditional Chinese medicine. After oral administration of Radix Scutellariae extract （RSE）, the bile, plasma and urine of rats were analyzed to identify the absorbed parent components and metabolites by ultra-fast liquid chromatography coupled with ion trap time-of-flight mass spectrometry （UFLC-IT-TOF/MS）. A total of 36 different flavonoids, including 13 new metabolites, were identified or tentatively characterized in bile, plasma and urine of rats based on their fragmentation patterns. Among them, 16 flavonoids were identified in RSE in vitro, 25 flavonoids in rat bile, 15 flavonoids in rat plasma, and 14 flavonoids in rat urine. The results indicated that glucuronidation, sulfation and methylation were the major metabolic pathways of flavonoids. It is the first time that the metabolism of RSE was studied comprehensively.黄酮类化合物是中国传统中药黄芩的主要活性成分。大鼠口服黄芩提取物后, 采用超快速液相色谱-离子阱飞行时间质谱(UFLC-IT-TOF/MS)对胆汁、血浆和尿液进行分析, 鉴定入血成分和代谢产物。根据对这些成分质谱裂解规律的分析, 共鉴定了36种不同的黄酮类化合物, 其中包括13个新的代谢产物。本实验在体外对黄芩提取物进行分析,鉴定了其中16个黄酮类成分, 大鼠胆汁中鉴定了25个黄酮类化合物, 血浆中15个黄酮类化合物, 尿液中14个黄酮类化合物。结果表明, 黄芩提取物中的黄酮类化合物以葡萄糖醛酸化、硫酸化和甲基化的为主要代谢途径。本实验首次对黄芩提取物的代谢产物进行综合分析。

关 键 词：Radix Scutellariae FLAVONOIDS METABOLITES UFLC-IT-TOF/MS 

分 类 号：R284[医药卫生—中药学]