Deoxyschizandrin has been found to act as an agonist of the adiponectin receptor 2 (AdipoR2).Deoxyschizandrin (DS), one of the major pharmacological effective lingans isolated from Schisandra fruits, has been shown to provide hepatoprotection, anti oxidation and antitumor activities. The present study aims to investigate the metabolism of DS by cytochrome P450s (CYPs) in human liver microsomes (HLMs). After DS was incubated with HLMs and NADPH-generating system, only one mono-hydroxylated metabolite was detected and was identified as schizandrin by comparing the tandem mass spectra and the chromatographic retention time with that of the standard compound. A combination of correlation analysis, chemical inhibition studies, assays with recombinant CYPs and enzyme kinetics indicated that CYP3A4 was the specific hepatic isoform that cleared DS.
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