文献类型：期刊文献

中文题名：芹菜素在大鼠体内代谢产物的鉴定与分析

英文题名：Identification and Analysis of Apigenin Metabolites in Rats

作者：张亚洲 王涛 邹树良 刘海林 晏晨

第一作者：张亚洲

机构：[1]贵州理工学院制药工程学院;[2]广西药用植物园;[3]安顺市医院

第一机构：贵州理工学院食品药品制造工程学院

年份：2016

卷号：27

期号：4

起止页码：479-482

中文期刊名：中国药房

外文期刊名：China Pharmacy

收录：CSTPCD;;北大核心:【北大核心2014】；

基金：广西自然科学基金项目(No.2013GXNSFBA019187);贵州理工学院高层次人才科研项目(No.XJGC20141106)

语种：中文

中文关键词：芹菜素;高效液相串联离子阱飞行时间多级质谱法;大鼠;尿液;粪便;代谢产物;鉴定;分析

外文关键词：Apigenin; HPLC-IT-TOF-MSn; Rats; Urine; Feces; Metabolites; Identification; Analysis;

摘要：目的:阐明芹菜素在大鼠体内的生物转化形式,推测其可能的代谢途径。方法:取大鼠分为空白组和给药组(灌胃给予芹菜素,200 mg/kg),每组6只。给药24 h内分别收集两组的尿液和粪便,进行相应处理后同时在正离子模式和负离子模式下采用高效液相串联离子阱飞行时间多级质谱法进行分析检测。结果:从给药组的大鼠尿液中鉴定出9个代谢产物,分别为芹菜素发生2,3位双键还原(U1、U7、U8、U9)、与葡萄糖醛酸结合(U2、U3、U4)、与硫酸酯结合(U5、U6、U7、U8、U9)、与葡萄糖结合的产物(U2);从给药组的大鼠粪便样品中鉴定出4个代谢产物,分别为芹菜素发生2,3位双键还原(代谢产物F3)、与葡萄糖醛酸结合(F2)、与葡萄糖结合的产物(F1)。结论:芹菜素在大鼠体内主要仍以原型药物存在,推测在肠道细菌的作用下可发生2,3位双键的还原,在肠道与体内排泄时均可形成葡萄糖醛酸或葡萄糖结合产物,而形成硫酸酯结合产物则仅在体内排泄时发生。
OBJECTIVE：To clarify the bio-transformation form of apigenin in rats,and to speculate its possible metabolic pathway. METHODS：Rats were divided into blank group and medication group（apigenin 200 mg/kg,i.g.）with 6 rats in each group.Urine and feces samples were collected from 2 groups within 24 h after medication. After corresponding treatment,urine and feces samples were analyzed and detected by HPLC-IT-TOF-MSnunder cation mode and anion mode. RESULTS：9 metabolites were identified in urine sample of rats from medication group,i.e. 2,3-double bond reduction of apigenin（U1,U7,U8,U9）,bonded to glucuronic acid（U2,U3,U4）,bonded to sulphate（U5,U6,U7,U8,U9）and bonded to glucose（U2）. 4 metabolites were identified in feces sample of rats from medication group,i.e. 2,3-double bond reduction of apigenin（F3）,bonded to glucuronic acid（F2）and bonded to glucose（F1）. CONCLUSIONS：Apigenin mainly exists in form of prototype drug in rats. The reduction happens on 2,3-double bond by the intestinal bacteria,and the product of apigenin boned to glucuronic acid or glucose can be formed when excreting in intestinal tract and rats in vivo,while the product of apigenin boned to sulphate can be formed only when excreting in rats in vivo.