Next Article in Journal
A Computational Framework for Predicting Direct Contacts and Substructures within Protein Complexes
Previous Article in Journal
Use of Cardiac Biomarkers for Monitoring Improvement of Left Ventricular Function by Immunoadsorption Treatment in Dilated Cardiomyopathy
Open AccessArticle

Interactions of 7,8-Dihydroxyflavone with Serum Albumin as well as with CYP2C9, CYP2C19, CYP3A4, and Xanthine Oxidase Biotransformation Enzymes

1
Department of Pharmacology, Faculty of Pharmacy, University of Pécs, Szigeti út 12, H-7624 Pécs, Hungary
2
János Szentágothai Research Centre, University of Pécs, Ifjúság útja 20, H-7624 Pécs, Hungary
3
Department of Pharmacognosy, Faculty of Pharmacy, University of Pécs, Rókus u. 2, H-7624 Pécs, Hungary
4
Institute of Organic and Medicinal Chemistry, Medical School, University of Pécs, Szigeti út 12, H-7624 Pécs, Hungary
*
Author to whom correspondence should be addressed.
Biomolecules 2019, 9(11), 655; https://doi.org/10.3390/biom9110655
Received: 12 September 2019 / Revised: 15 October 2019 / Accepted: 23 October 2019 / Published: 25 October 2019
(This article belongs to the Section Biochemistry)
7,8-dihydroxyflavone (DHF) is a flavone aglycone which has beneficial effects in several central nervous system diseases. Most of the pharmacokinetic properties of DHF have been characterized, while only limited information is available regarding its interactions with serum albumin and biotransformation enzymes. In this study, the interactions of DHF with albumin was examined employing fluorescence spectroscopy and ultrafiltration. Furthermore, the inhibitory effects of DHF on cytochrome P450 (CYP2C9, CYP2C19, and CYP3A4) and xanthine oxidase (XO) enzymes were also tested using in vitro models. Our results demonstrate that DHF forms a stable complex with albumin (K = 4.9 × 105 L/mol) and that it is able to displace both Site I and Site II ligands. Moreover, DHF proved to be a potent inhibitor of each enzyme tested, showing similar or slightly weaker effects than the positive controls used. Considering the above-listed observations, the coadministration of DHF with drugs may interfere with the drug therapy due to the development of pharmacokinetic interactions. View Full-Text
Keywords: 7,8-dihydroxyflavone; serum albumin; cytochrome P450 enzymes; xanthine oxidase; pharmacokinetic interactions 7,8-dihydroxyflavone; serum albumin; cytochrome P450 enzymes; xanthine oxidase; pharmacokinetic interactions
Show Figures

Figure 1

MDPI and ACS Style

Fliszár-Nyúl, E.; Mohos, V.; Bencsik, T.; Lemli, B.; Kunsági-Máté, S.; Poór, M. Interactions of 7,8-Dihydroxyflavone with Serum Albumin as well as with CYP2C9, CYP2C19, CYP3A4, and Xanthine Oxidase Biotransformation Enzymes. Biomolecules 2019, 9, 655.

Show more citation formats Show less citations formats
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

1
Back to TopTop