Dehydro-digitoxosides of digitoxigenin: Formation and importance for the digitoxin metabolism in the rat

  title={Dehydro-digitoxosides of digitoxigenin: Formation and importance for the digitoxin metabolism in the rat},
  author={Achim Schmoldt and Christoph Rohloff},
  journal={Naunyn-Schmiedeberg's Archives of Pharmacology},
  • A. SchmoldtC. Rohloff
  • Published 1 November 1978
  • Biology, Chemistry
  • Naunyn-Schmiedeberg's Archives of Pharmacology
SummaryOnly in the presence of NADPH and oxygen digitoxosides of digitoxigenin can be metabolized by rat liver microsomes. The metabolism includes 12β-hydroxylation, formation of digitoxosides less the terminal digitoxose and of lipophilic metabolites. The lipophilic metabolites of digitoxin (dt-3), digitoxigeninbis-digitoxoside (dt-2), and of — mono-digitoxoside (dt-1) are formed by oxidation of the axial OH-group of the terminal digitoxosyl yielding the corresponding dehydro-digitoxosides… 

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No metabolism could be measured in vitro in the absence of NADPH or O2 suggesting that unchanged digitoxosides cannot be hydrolyzed by microsomal enzymes.

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  • E. CoxS. E. Wright
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    The Journal of pharmacology and experimental therapeutics
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    Drug metabolism and disposition: the biological fate of chemicals
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The isolated perfused rat liver can be used as a model for in vivo studies of cardiac glycoside metabolism and biliary excretion and metabolic pattern, obtained from these studies in an isolated perfuse rat liver, mimic those seen in the intact rat.

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