Metabolic profiling of isomeric aglycones central‐icaritin (c‐IT) and icaritin (IT) in osteoporotic rats by UPLC‐QTOF‐MS

摘要: The isomers, although of similarly chemical structures, have different pharmacological activities due to their metabolic processes in vivo. Central-icaritin (c-IT) and icaritin (IT) are isomers major bioactive aglycones the Herba Epimedii. In this study, we found that anti-osteoporotic effect c-IT was stronger than IT on bone structural changes osteoporotic rats evaluated by Micro-μCT with parameters mineral density (BMD), content (BMC), tissue (TMC), (TMD). treatment significantly increased microarchitecture, compared (p < 0.05). order explain differences anti-osteoporosis, profiling pathways plasma, bile, urine, faeces ovariectomized (OVX) were investigated ultra-performance liquid chromatography quadrupole time flight mass spectrometry (UPLC-QTOF-MS) after oral administration or (80 mg/kg). Finally, 59 metabolites 43 identified elucidating corresponding quasimolecular ions fragment ions. could be quickly absorbed into blood reached a maximum plasma concentration, then rapidly conversed its glucuronidation metabolites, most which excreted out urine. Interestingly, conjugated speeds slower IT. existed enterohepatic circulation, decreased metabolism excretion rate c-IT, prolonged anti-osteoporosis effect. Our findings provided evidence difference profiles rats, might shed new lights improving effects c-IT. Copyright © 2014 John Wiley & Sons, Ltd.