Review
Version 1
Preserved in Portico This version is not peer-reviewed
Flavonoids As CYP3A4 Inhibitors In Vitro
Version 1
: Received: 9 January 2024 / Approved: 10 January 2024 / Online: 10 January 2024 (10:24:39 CET)
A peer-reviewed article of this Preprint also exists.
Kondža, M.; Brizić, I.; Jokić, S. Flavonoids as CYP3A4 Inhibitors In Vitro. Biomedicines 2024, 12, 644, doi:10.3390/biomedicines12030644. Kondža, M.; Brizić, I.; Jokić, S. Flavonoids as CYP3A4 Inhibitors In Vitro. Biomedicines 2024, 12, 644, doi:10.3390/biomedicines12030644.
Abstract
Flavonoids, a diverse group of polyphenolic compounds found abundantly in fruits, vegetables, and beverages like tea and wine, offer a plethora of health benefits. However, their potential interaction with drug metabolism, particularly through inhibition of the cytochrome P450 3A4 enzyme, the most versatile and abundant enzyme in the liver. CYP3A4 is responsible for metabolizing approximately 50% of clinically prescribed drugs across diverse therapeutic classes, so these interactions have raised concerns about potential adverse effects. This review delves into the scientific evidence surrounding flavonoid-mediated CYP3A4 inhibition, exploring the inhibitory potential of investigated flavonoids and future implications. Kusehnol I, chrysin, leachianone A and sophoraflavone G showed the largest inhibitory potentials and lowest IC50 values. While the clinical significance of flavonoid-mediated CYP3A4 inhibition in dietary contexts is generally considered low due to moderate intake and complex interactions, it poses a potential concern for individuals consuming high doses of flavonoid supplements or concurrently taking medications metabolized by CYP3A4. This can lead to increased drug exposure, potentially triggering adverse reactions or reduced efficacy.
Keywords
CYP enzymes; CYP3A4; flavonoid; inhibition; natural products
Subject
Medicine and Pharmacology, Pharmacy
Copyright: This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
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