摘要：Breviscapine, is the total flavonoid components (the content of scutellarin >85%) extracted from the dried whole plant of Erigeron breviscapus (V ANT .) H AND .-M AZZ , and its preparations are generally used in the clinic for the treatment of cerebral and cardio-vascular diseases in China. In this paper, the metabolites of breviscapine in the urine of rats after oral administration were investigated. The ten metabolites were isolated by open-column chromatography and preparative high-performance liquid chromatography, and their structures were elucidated by MS, NMR spectroscopy including 1H-NMR, 13C-NMR, and NOESY (nuclear Overhauser enhancement spectroscopy), enzymatic hydrolysis and chemical evidence. The ten metabolites were identified as scutellarein-6,7-di- O -β- D -glucuronide (M-1), scutellarein (M-2), 6- O -methyl-scutellarin (M-3), 6- O -methyl-scutellarein (M-4), scutellarein-6- O -β- D -glucuronide (M-5), scutellarein-5- O -β- D -glucuronide (M-6), scutellarin (M-7), scutellarein-7- O -sulfate (M-8), apigenin-5- O -β- D -glucuronide (M-9), and apigenin-4′- O -β- D -glucuronide (M-10) respectively. The results of this study indicated that the metabolites of brevisvapine were excreted in rats urine as glucuronidated, sulfated or methylated forms, as well as the aglycone of scutellarin-scutellarein after oral administration, and the metabolic pathways were also proposed.
