Anthocyanins and anthocyanidins are poor inhibitors of CYP2D6.
The cytochrome P450 CYP2D6 isoform is involved in the metabolism of about 50% of all psychoactive drugs, including neuroleptic agents, selective serotonin reuptake inhibitors, selective norepinephrine reuptake inhibitors and tricyclic antidepressants. Therefore, inhibition of cytochrome P450 activity by foodstuffs has implications for drug safety. The present study addresses inhibitory effects of polyphenolic anthocyanins and their aglycons that are found in many dietary fruits and vegetables. Using a chemiluminescent assay, we obtained IC(50) values ranging from 55 microM to > 800 microM for 17 individual compounds. According to earlier data on furanocoumarins from grapefruit extract, CYP2D6 inhibition is achieved in the range of 190-900 nM. As the tested anthocyanins and anthocyanidins were shown to be about 1,000-fold less potent, they are unlikely to interfere with drug metabolism by CYP2D6. Further studies are warranted to examine the effects of the above flavonoids on other CYP isoforms for more detailed toxicity profiles.
Dreiseitel
Andrea
A
Department of Psychiatry, University of Regensburg, Regensburg, Germany. andrea.dreiseitel@klinik.uni-regensburg.de
Schreier
Peter
P
Oehme
Anett
A
Locher
Sanja
S
Rogler
Gerhard
G
Piberger
Heidi
H
Hajak
Goeran
G
Sand
Philipp G
PG
D000872:Anthocyanins / Q000008:administration & dosage / Q000494:pharmacology*; D065690:Cytochrome P-450 CYP2D6 Inhibitors; D005419:Flavonoids / Q000008:administration & dosage / Q000494:pharmacology*; D018565:Food-Drug Interactions; D005638:Fruit / Q000737:chemistry; D006801:Humans; D020128:Inhibitory Concentration 50; D008163:Luminescent Measurements / Q000379:methods; D010636:Phenols / Q000008:administration & dosage / Q000494:pharmacology*; D059808:Polyphenols; D014675:Vegetables / Q000737:chemistry
D000872:Anthocyanins; D065690:Cytochrome P-450 CYP2D6 Inhibitors; D005419:Flavonoids; D010636:Phenols; D059808:Polyphenols