Anthocyanins and their metabolites are weak inhibitors of cytochrome P450 3A4

Molecular Nutrition & Food Research
Andrea DreiseitelPhilipp G Sand

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.

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Citations

Aug 4, 2009·Journal of Neural Transmission·Andrea DreiseitelPhilipp G Sand
Apr 5, 2016·Pharmacognosy Reviews·Seyede Nargess SadatiFarid Ramezany
May 12, 2009·Bioorganic & Medicinal Chemistry Letters·James McNultyJaume Bastida
Jul 9, 2009·Phytotherapy Research : PTR·Philipp G SandGoeran Hajak
Jan 17, 2013·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·Barbora SzotákováLenka Skálová
Jul 17, 2015·Oxidative Medicine and Cellular Longevity·Loai Basheer, Zohar Kerem
May 26, 2016·Phytotherapy Research : PTR·Antonella SmeriglioDomenico Trombetta
Apr 6, 2019·Journal of Basic and Clinical Physiology and Pharmacology·Johnson Segun ShowandeTitilayo Oyelola Fakeye
Mar 15, 2011·Journal of Agricultural and Food Chemistry·Hsien-Tsung YaoChong-Kuei Lii

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