ArticleMolecules (Basel, Switzerland)2021
Characterization of the CYP3A4 Enzyme Inhibition Potential of Selected Flavonoids.
Article in Molecules (Basel, Switzerland), 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 34 citations in OpenAlex.
- Phytomedicine-mediated time-dependent inactivation of CYP3A4 by chemical modification.Journal of pharmaceutical analysis · 2026Review
- Chrysin as a Multifunctional Therapeutic Flavonoid: Emerging Insights in Pathogenesis Management: A Narrative Review.International journal of molecular sciences · 2025Review
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- Potential Interaction of Pinocembrin with Drug Transporters and Hepatic Drug-Metabolizing Enzymes.Pharmaceuticals (Basel, Switzerland) · 2025Article
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- Isolation, Characterization, In Vitro and In Silico Assessment of Undescribed Bioactive Constituents fromACS omega · 2024Article
- Physcion inhibition of CYP2C9, 2D6 and 3A4 in human liver microsomes.Pharmaceutical biology · 2024Article
- Cardiovascular Effects of Herbal Products and Their Interaction with Antihypertensive Drugs-Comprehensive Review.International journal of molecular sciences · 2024Review
- Flavonoids as CYP3A4 Inhibitors In Vitro.Biomedicines · 2024Review
- Pharmacological Mechanism of Herbal Interventions for Bipolar Disorder.Current pharmaceutical design · 2024Review
- Effects of Dietary Flavonoids on the Metabolism of Vortioxetine and its Potential Mechanism.Current medicinal chemistry · 2024Article
- Inhibition Effect of Okanin Toward Human Cytochrome P450 3A4 and 2D6 with Multi-spectroscopic Studies and Molecular Docking.Journal of fluorescence · 2024Article
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- Evidence-based capacity of natural cytochrome enzyme inhibitors to increase the effectivity of antineoplastic drugs.Discover oncology · 2022Review
- Network Analysis of the Herb-Drug Interactions of Citrus Herbs Inspired by the "Grapefruit Juice Effect".ACS omega · 2022Article
- Prevention of Anthracycline-Induced Cardiotoxicity: The Good and Bad of Current and Alternative Therapies.Frontiers in cardiovascular medicine · 2022Review
- In Vitro and In Vivo Studies of Anti-Lung Cancer Activity ofAntioxidants (Basel, Switzerland) · 2021Article
- Effects of Acacetin on the Pharmacokinetics of Diazepam in vivo and in vitro.Iranian journal of pharmaceutical research : IJPRArticle
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Authors and funding
6 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Acacetin, apigenin, chrysin, and pinocembrin are flavonoid aglycones found in foods such as parsley, honey, celery, and chamomile tea. Flavonoids can act as substrates and inhibitors of the CYP3A4 enzyme, a heme containing enzyme responsible for the metabolism of one third of drugs on the market. The aim of this study was to investigate the inhibitory effect of selected flavonoids on the CYP3A4 enzyme, the kinetics of inhibition, the possible covalent binding of the inhibitor to the enzyme, and whether flavonoids can act as pseudo-irreversible inhibitors. For the determination of inhibition kinetics, nifedipine oxidation was used as a marker reaction. A hemochromopyridine test was used to assess the possible covalent binding to the heme, and incubation with dialysis was used in order to assess the reversibility of the inhibition. All the tested flavonoids inhibited the CYP3A4 enzyme activity. Chrysin was the most potent inhibitor:
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