Toxicita metabolitov benzo[c]fenantridinových alkaloidov
|Další prezentace na konferencích
|Fakulta / Pracoviště MU
|Benzophenanthridine alkaloids belong among the substances exhibiting a number of biological activities (antitumor, anti-inflammatory, antimicrobial, antimycotic, antiplaque) and are currently being given great attention to potential therapeutic uses. The most researched, the majority of commercially available alkaloids - sanguinarine and chelerythrine are accompanied by a group of minor alkaloids, which, despite their great structural similarity, exhibit a diverse spectrum of effects. Their metabolism is not fully elucidated, with identification of metabolites of these alkaloids and their further biotransformation being a prerequisite for better understanding of the relationships between their structure and properties. In our study, we studied the biotransformation of selected minor benzophenanthridine alkaloids by an in vitro rat liver microsome model. The resulting metabolites were identified by liquid chromatography coupled to mass spectrometry and the major metabolites were purified, concentrated, and their cytotoxicity was determined as compared to that of the original alkaloid. The observed biotransformation reactions included O-demethylation, demethylenation, reduction, and hydroxylation.