中国中药杂志

2018, v.43(21) 4330-4338

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基于UHPLC-QTOF-MS/MS技术的铁筷子中3个香豆素在大鼠体内代谢研究
In vivo metabolism of three coumarins from Chimonanthi Radix based on UHPLC-QTOF-MS/MS

张晶;温泉;徐旭;陈林;冯育林;杨世林;罗云;谭婷;
ZHANG Jing;WEN Quan;XU Xu;CHEN Lin;FENG Yu-lin;YANG Shi-lin;LUO Yun;TAN Ting;The National Pharmaceutical Engineering Center (NPEC) for Solid Preparation in Chinese Herbal Medicine, Jiangxi University of Traditional Chinese Medicine;Key Laboratory of Modern Preparation of Traditional Chinese Medicine, Ministry of Education,Jiangxi University of Traditional Chinese Medicine;

摘要(Abstract):

东莨菪苷(SC-1)、东莨菪内酯(SC-2)和异嗪皮啶(IS-1)是苗药铁筷子中主要活性成分,这3个香豆素类化合物的体内代谢还未报道,该研究对铁筷子中3个香豆素化合物SC-1,SC-2,IS-1在大鼠体内的代谢进行分析。采用超高效液相色谱-电喷雾飞行时间质谱(UHPLC-QTOF-MS/MS)技术,大鼠分别尾静脉注射3个香豆素化合物后,鉴定粪便、尿液、血浆中的代谢产物。总共鉴定了3个香豆素原型及其在大鼠体内的11个代谢产物。通过对代谢产物的鉴定分析了其主要代谢途径,发现在大鼠体内这3个香豆素成分发生了葡萄糖醛酸化、磺酸化、还原等代谢反应。对3个香豆素化合物代谢产物的分析,基本阐明了其在体内的代谢过程,为进一步的药理活性及其机制研究提供了依据。
Scopolin(SC-1), scopoletin(SC-2) and isofraxidin(IS-1) are the main active constituents in Chimonanthi Radix. However, the in vivo metabolism of SC-1, SC-2 and IS-1 have not been comprehensively clarified. In this study, the in vivo metabolic profiles of these three coumarins in the rat plasma, urine and feces were analyzed. Ultra-high performance liquid chromatography-quadrupole time of flight mass spectrometry(UHPLC-QTOF-MS/MS) method was applied to characterize the prototypes and metabolites of SC-1, SC-2 and IS-1 in rat feces, urine, and plasma after intravenous administration. A total of 11 metabolites of the three parent compounds were tentatively identified. The main metabolic pathways were analyzed by identification of metabolites, and it was found that these three coumarins underwent multiple in vivo metabolic reactions including glucuronidation, sulfonation, isomerism and reduction. In this study, the analysis of metabolites of three coumarins basically demonstrated their in vivo metabolic process, providing basis for the further pharmacokinetics and pharmacological evaluations of SC-1, SC-2 and IS-1.

关键词(KeyWords): 铁筷子;UHPLC-QTOF-MS/MS;香豆素;代谢产物;东莨菪苷;东莨菪内酯;异嗪皮啶
Chimonanthi Radix;UHPLC-QTOF-MS/MS;coumarin;metabolite;scopolin;scopoletin;isofraxidin

Abstract:

Keywords:

基金项目(Foundation): 国家自然科学基金项目(81460600,81603274,81760711);; 江西省自然科学基金项目(20171BAB205100);; 江西省卫生计生委中医药科研项目(2016A042);; 江西中医药大学院士工作站专项(2016ZR001)

作者(Author): 张晶;温泉;徐旭;陈林;冯育林;杨世林;罗云;谭婷;
ZHANG Jing;WEN Quan;XU Xu;CHEN Lin;FENG Yu-lin;YANG Shi-lin;LUO Yun;TAN Ting;The National Pharmaceutical Engineering Center (NPEC) for Solid Preparation in Chinese Herbal Medicine, Jiangxi University of Traditional Chinese Medicine;Key Laboratory of Modern Preparation of Traditional Chinese Medicine, Ministry of Education,Jiangxi University of Traditional Chinese Medicine;

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