Metabolism profile of scutellarin in urine following oral administration to rats by ultra performance liquid chromatography coupled to time-of-flight mass spectrometry.

Scutellarin, a flavone glucuronide of 5,6,4'-trihydroxyflavone-7-O-glucoronide, is the main active component of the traditional Chinese botanic drug Erigeron breviscapus (Vant.) Hand.-Mazz. In this study, a method based on ultra performance liquid chromatography coupled with a time-of-flight mass spectrometer (UPLC/TOF MS) was established and validated to profile the metabolites of scutellarin in Sprague-Dawley rat urine following oral administration of single dose of scutellarin at 80.8 mg/kg. The column utilized was an Acquity BEH C18 (150 mm x 2.1 mm, 1.7 microm). The mobile phase was 0.2% formic acid and acetonitrile with gradient condition. Two standard curves of scutellarin were obtained for the concentration range of 1.065-10.65 microg/mL and 10.65-63.92 microg/mL, respectively. By automating the data processing of the software Masslynx developed by Waters Ltd., 17 metabolites of scutellarin were found and determined in rat urine, with the corresponding reactions in vivo such as isomerism, reduction, methylation, glucuronide conjugation, hydroxylation, hydroxylation and methylation, etc., most of which were discovered for the first time. For most metabolites, the time (T(p)) of peak excretion was 8-12h. Calculated as scutellarin, the cumulative urine excretion rate of the metabolites was 1.93%.