Identification of metabolites of selected benzophenanthridine alkaloids and their toxicity evaluation

• LC MS was used to determine the metabolites of benzophenanthridine alkaloids sanguilutine, sanguirubine, chelilutine, chelirubine, and macarpine.
• Two metabolites were purified and isolated and their cytotoxicity was compared to the original alkaloids.

Selected benzo[c]phenathridine alkaloids were biotransformed using rat liver microsomes and identified by liquid chromatography and mass spectrometry. While the metabolites of commercially available sanguinarine and chelerythrine have been studied in detail, data about the metabolism of the minor alkaloids remained unknown. Reactions involved in transformation include single and/or double O-demethylation, demethylenation, reduction, and hydroxylation. Two metabolites, when isolated, purified and tested for toxicity, were found to be less toxic than the original compounds.

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