Abstract
The metabolism of cinobufagin (CB) in rat liver microsomes was studied. By comparison of retention times and fragmentation patterns obtained by thermospray LC/MS with those of authentic standards, four metabolites of CB were also identified, in addition to deacetylCB (M1) and 3-epideacetylCB (M2), which have been reported previously. The additional four metabolites were identified to be 3-epiCB (M4), 3-ketoCB (M5), 3-keto-16 beta-OH-deacetylCB (M3), and 3-keto-16 alpha-OH-deacetylCB (M6). The primary metabolic products of CB were M1 and M2, with a small amount of M4 and trace amounts of M3, M5, and M6. These results indicate that major metabolic routes of CB were deacetylation at the 16-position and epimerization at the 3-position via the 3-keto intermediate.
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