Abstract
The pharmacokinetic profile of arctiin, the major active lignan in fruits of Arctium lappa L., was investigated. Its main meta“bolite 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™ C18 HPLC column with acetonitrile and water by linear gradient elution. Arctiin and arctigenin
were identified on-line 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 AUC0-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.
Key words
arctiin - arctigenin - HPLC-MS - pharmacokinetics - tissue distribution -
Arctium lappa
- Compositae
