title: Anthocyanins and their metabolites are weak inhibitors of cytochrome P450 3A4.
abstract: The cytochrome P450 enzyme cytochrome P450 3A4 (CYP3A4) controls the metabolism of about 60% of all drugs, and its inhibition may dramatically affect drug safety. Modulation of cytochrome P450 activity has been observed by constituents of fruit extracts including several flavonoids. The present investigation addresses CYP3A4 inhibition by anthocyanins, their aglycons, proanthocyanidins, and phenolic metabolites using a chemiluminescent assay. Test compounds inhibited CYP3A4 activity in a concentration-dependent manner featuring IC(50) values from 12.2 up to 7,842 microM. In the order of decreasing effect size, anthocyanidins were followed by anthocyanins, proanthocyanidins, and phenolic acids. When compared to earlier data on furanocoumarins from grapefruit extract, the inhibitory activity of tested anthocyanins, and anthocyanidins was shown to be about 10,000-fold weaker, and was negligible for phenolic acids (>100 000-fold weaker). Future studies are invited to address effects of the above flavonoids on other CYP isoforms for more detailed toxicity profiles.
authors: Department of Psychiatry, University of Regensburg, Regensburg, Germany. andrea.dreiseitel@klinik.uni-regensburg.de
authors: Andrea
authors: A
authors: Dreiseitel
authors: Peter
authors: P
authors: Schreier
authors: Anett
authors: A
authors: Oehme
authors: Sanja
authors: S
authors: Locher
authors: Goeran
authors: G
authors: Hajak
authors: Philipp G
authors: PG
authors: Sand
mesh_terms: D000872:Anthocyanins / Q000378:metabolism / Q000494:pharmacology*; D051544:Cytochrome P-450 CYP3A; D065692:Cytochrome P-450 CYP3A Inhibitors; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D018565:Food-Drug Interactions
chemical_list: D000872:Anthocyanins; D065692:Cytochrome P-450 CYP3A Inhibitors; D004791:Enzyme Inhibitors; D051544:Cytochrome P-450 CYP3A; C510163:CYP3A4 protein, human