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In this work, the metabolite profiles of icariin in rat feces, bile and urine were qualitatively investigated, and the possible metabolic pathways of icariin were subsequently proposed. After oral administration of icariin at a single dose of 100 mg/kg, rat biological samples were collected and pretreated. Then, these pretreated samples were detected by ultraperformance liquid chromatography/quadrupole-time-of-flight mass spectrometry (UPLC–Q-TOF-MS). In all, 17 metabolites were identified in the biosamples. Of these, 5, including F8−F9 (icariside I), D3−D4 (isopentenyl alcohol-icaritin-3-O-rha-7-O-gluA) and N3 (1,3-isoprene icariside II), were to our knowledge reported for the first time. The results indicated that icariin was metabolized via desugarization, dehydrogenation, hydroxylation, demethylation and glucuronidation pathways  in vivo . This study revealed the possible metabolite profiles of icariin in rats.

Metabolite Profiles of Icariin in Rat Feces, Bile and Urine by Ultraperformance Liquid-Chromatography/Quadrupole-Time-of-Flight Mass Spectrometry