Plasma Pharmacokinetics and Tissue Distribution of Arctiin and Its Main Metabolite in Rats by HPLC-UV and LC-MS

被引：41

作者：

He Fan ^{[1
,2
]}

Dou De-Qiang ^{[2
]}

Sun Yu ^{[2
]}

Zhu Lin ^{[3
]}

Xiao Hong-Bin ^{[3
]}

Kang Ting-Guo ^{[1
]}

机构：

[1] Liaoning Univ Tradit Chinese Med, Dept Pharmacognosy, Dalian 116600, Peoples R China

[2] Liaoning Univ Tradit Chinese Med, Dept Chinese Med Chem, Dalian 116600, Peoples R China

[3] Chinese Acad Sci, Dalian Inst Chem Phys, Dalian, Peoples R China

来源：

PLANTA MEDICA | 2012年 / 78卷 / 08期

关键词：

arctiin; arctigenin; HPLC-MS; pharmacokinetics; tissue distribution; Arctium lappa; Compositae; SPRAGUE-DAWLEY RATS; TRANSFORMATION; ARCTIGENIN; LIGNANS; MAMMARY; L;

D O I：

10.1055/s-0031-1298433

中图分类号：

Q94 [植物学];

学科分类号：

071001 [植物学];

摘要：

The pharmacokinetic profile of arctiin, the major active lignan in fruits of Arctium lappa L., was investigated. Its main metabolite arctigenin was identified by an LC-MS method, and an HPLC-UV technique was developed for the simultaneous quantification of the metabolite and arctiin in plasma and organs. Chromatographic separation was performed on an Agilent (TM) C-18 HPLC column with acetonitrile and water by linear gradient elution. Arctiin and arctigenin were identified online by LC-MS. The pharmacokinetics and tissue distribution of arctiin and arctigenin were determined for the first time by using a simple, selective, and accurate HPLC method. The AUC(0-t) values of arctigenin were larger compared with arctiin after oral administration of arctiin. The concentration of the metabolite was significantly higher than the concentration of arctiin in the stomach and small intestine in rats after oral administration of arctiin, indicating that the stomach and small intestine were the major organs of arctiin metabolism. These findings could provide support for the clinical studies conducted with Fructus Arctii.

引用

页码：800 / 806

页数：7

共 15 条

[1]

Mass fragmentation study of the trimethylsilyl derivatives of arctiin, matairesinoside, arctigenin, phylligenin, matairesinol, pinoresinol and methylarctigenin: Their gas and liquid chromatographic analysis in plant extracts [J].