Summary
The human biliary metabolism of the antitumor agent N 2-methyl-9-hydroxyellipticinium acetate is described. Three major compounds have been identified by high-performance liquid chromatography and comparison with synthetic reference derivatives: the unchanged drug, the O-glucuronide conjugate and the cysteinyl-ellipticinium adduct. The latter one is the expected detoxification compound of an intermediate electrophilic quinone-imine derivative generated in vivo. This result provides a further evidence that hydroxylated forms of ellipticine derivatives might be activated by a biooxidation route.
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Part of this work was done by J. B. as part of his preparation for the degree of Doctor of Medicine in the Centre Claudius Regaud
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Bernadou, J., Monsarrat, B., Roche, H. et al. Evidence for electrophilic properties of N 2-methyl-9-hydroxy ellipticinium acetate (Celiptium) from human biliary metabolites. Cancer Chemother. Pharmacol. 15, 63–65 (1985). https://doi.org/10.1007/BF00257297
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DOI: https://doi.org/10.1007/BF00257297