Biotransformation of 5‐demethyltangeretin in mice: generation of anti‐cancer metabolites

• DOI: 10.1096/fasebj.30.1_supplement.145.1
• Publication Date: 2021-06-07T05:00:24Z
• Authors: Xian Wu; Yue Sun; Minqi Wang; Zili Gao; Mingyue Song; Hang Xiao
• Keywords: Biotransformation; Demethylation; Hydroxylation; Glucuronide; Primary metabolite; Metabolic pathway

5-demethyltangeretin (5DT) is a unique polymethoxyflavone isolated from citrus peels, and showed potent inhibitory effects on various human cancer cells. Biotransformation of dietary bioactive components plays critical roles in their biological activities because they can be transformed to metabolites with significant bioactivities. In this study, we determined the metabolic fate 5DT mice bioactivities its major metabolite. Our results that underwent extensive biotransformation fed 5DT, produced demethylated hydroxylated via phase I metabolism, glucuronide sulfate conjugates II metabolism. particular, 4′ position B-ring was primary site for demethylation (formation xanthomicrol, XAN), 3′ hydroxylation 5, 3′, 4′-tridemethyltangeretin, TDT). Interestingly, colonic levels XAN much higher than 5DT. Therefore, further investigated colon It found significantly inhibited cell growth by inducing G2 cycle arrest cellular apoptosis. Overall, study identified demonstrated anti-cancer potential metabolites. Support or Funding Information This supported funding USDA. pathways