大鼠肠道菌群对羊耳菊提取物的代谢作用研究

公司研发的数据处理工具Metabolite Tools，Data Analysis等对代谢信息进行综合分析。通过比较空白样品图谱，肠菌样品图谱以及两者的差异图谱，各色谱峰的准分子离子，碎片离子，分析羊耳菊提取物在大鼠肠道菌群作用下可能产生的代谢产物。结果提示，羊耳菊提取物在肠道菌群作用下，检测到14个代谢产物，主要包括单咖啡酰基奎宁酸的异构，水解的小分子化合物和咖啡酸的还原，甲基化和乙酰化等代谢产物，同时仅检测到1个二咖啡酰基奎宁酸的甲基化代谢产物。以此推测，咖啡酰基奎宁酸类成分在肠道菌群的作用下可能多数水解为分子量小，疏水性更强的代谢产物，使得其更容易被肠道吸收。

[关键词]羊耳菊提取物； 肠道菌群； 代谢产物； UPLCQTOFMS/MS

Metabolism of Inula cappa extract by rat intestinal bacteria in vitro

GONG Zipeng1，2，3，4， HOU Jingyu1，2，3，4， LI Mei1，2，3，4， WU Linlin1，2，3，4， CHEN Tingting1，2，3，4，

LI Yongjun1，2，3，4， WANG Aimin1，2，3，4， LAN Yanyu1，2，3，4， WANG Yonglin1，2，3，4*

（1. Guizhou Provincial Key Laboratory of Pharmaceutics， Guizhou Medical University， Guiyang 550004， China；

2. Engineering Research Center for the Development and Application of Ethnic Medicine and Traditional Chinese Medicine

（Ministry of Education）， Guizhou Medical University， Guiyang 550004， China；

3. School of Pharmacy， Guizhou Medical University， Guiyang 550004， China；

4. National Engineering Research Center of Miao′s Medicines， Guiyang 550004， China）

[Abstract]To investigate the metabolism of major components in Inula cappa by rat intestinal bacteria in vitro I cappa extract was incubated for 24 h with rat intestinal bacteria under anaerobic environment After the samples were precipitated by nbutanol， UPLCQTOFMS/MS was applied for the qualitative analysis of the metabolites， combined with data software such as Metabolite Tools， Data Analysis and so on The potential metabolites in rat intestinal bacteria were analyzed by comparing the total ion current of the test samples and blank samples and analyzing the quasimolecular ion and fragment ion of all chromatograms The results injected that fourteen metabolites were detected in rat intestinal flora Various types of metabolic reactions happen to caffeoylquinic acid in intestinal flora， including isomerization， hydrolyzation， there were also methylation， hydrogenation and acetylation of caffeic acid At the same time， a methylate of dicaffeoylquinic acid was also detected Presumably， caffeoylquinic acids were gradually transformed into more hydrophobic metabolites with smaller molecular mass， which were better absorbed by the intestinal tract.

[Key words]Inula cappa extracts； intestinal bacteria； metabolites； UPLCQTOFMS/MS

中藥及其制剂的给药方式多数以口服为主，在胃肠道被吸收后分布到靶器官从而发挥疗效，再经代谢作用最后排出体外。胃肠道不仅是药物吸收的主要部位，同时对药物也有一定的代谢作用，部分难以吸收的药物可能在肠道菌群的作用下转变为易吸收的成分，因此肠道菌群对药物疗效的发挥起到了重要的作用。并且中药及其制剂成分复杂，在体内的代谢过程和作用机制尚不明确，直接口服给药后，研究其体内过程和直接药效物质比较困难，因此选择肠道菌群体外代谢实验，研究民族药羊耳菊中主要药效物质的体外代谢规律，能够为药材的体内过程研究奠定一定基础[14]。