ANTHOCYANINS AND ANTHOCYANIDINS ARE POOR INHIBITORS OF CYP2D6

作者：Dreiseitel Andrea^*; Schreier Peter; Oehme Anett; Locher Sanja; Rogler Gerhard; Piberger Heidi; Hajak Goeran; Sand Philipp G

来源：Methods and Findings in Experimental and Clinical Pharmacology, 2009, 31(1): 3-9.

DOI：10.1358/mf.2009.31.1.1323011

• Cytochrome P450
• Flavonoid
• Anthocyanin
• Anthocyanidin

The cytochrome P450 CYP2D6 isoform is involved in the metabolism of about 50% of oil 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 mu M to > 800 mu M for 77 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 anthocyonidins were shown to be about 1,000-fold less potent, they ore 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.

• 出版日期2009-2