Cytochrome P450 1A1 expression and activity in Caco-2 cells: modulation by apple juice extract and certain apple polyphenols.

摘要: Cytochrome P450 (CYP) 1A1 plays a role in drug metabolism of intestinal cells (e.g., by activating certain chemical carcinogens such as polycyclic aromatic hydrocarbons into carcinogenic metabolites). In the human colon carcinoma cell line Caco-2, we investigated effects defined polyphenolic apple juice extract (AJE), major principle flavonoid/dihydrochalkone constituents quercetin and phloretin, corresponding prototype glycosides rutin phlorizin on CYP1A1 expression activity. Incubations were carried out with or without potent aryl hydrocarbon receptor agonist/CYP1A1 inducer 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD). AJE acted weak inducers mRNA protein, AJE, quercetin, led to slight induction CYP1A1-catalyzed 7-ethoxyresorufin O-deethylase (EROD) However, phloretin highly effective suppressing co-incubations 1 nM TCDD. The antagonistic effect...