Dreiseitel, Andrea and Schreier, Peter and Oehme, Anett and Locher, Sanja and Hajak, Goeran and Sand, Philipp G. (2008) Anthocyanins and their metabolites are weak inhibitors of cytochrome P450 3A4. MOLECULAR NUTRITION & FOOD RESEARCH, 52 (12). pp. 1428-1433. ISSN 1613-4125, 1613-4133
Full text not available from this repository. (Request a copy)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 IC50 values from 12.2 up to 7,842 mu M. 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 10000-fold weaker, and was negligible for phenolic acids (>100000-fold weaker). Future studies are invited to address effects of the above flavonoids on other CYP isoforms for more detailed toxicity profiles.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | GRAPEFRUIT JUICE; IN-VITRO; DRUG-INTERACTIONS; SCAVENGING ACTIVITY; PHENOLIC-COMPOUNDS; CYP3A ACTIVITY; POTENTIAL ROLE; FRUIT; ANTIOXIDANT; CANCER; Anthocyanidin; Anthocyanin; CYP3A4; Cytochrome P450; Flavonoid |
| Subjects: | 600 Technology > 610 Medical sciences Medicine |
| Divisions: | Medicine > Lehrstuhl für Psychiatrie und Psychotherapie |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 16 Oct 2020 12:04 |
| Last Modified: | 16 Oct 2020 12:04 |
| URI: | https://pred.uni-regensburg.de/id/eprint/30002 |
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