scholarly journals Development and Characterization of Novel and Selective Inhibitors of Cytochrome P450 CYP26A1, the Human Liver Retinoic Acid Hydroxylase

2016 ◽  
Vol 59 (6) ◽  
pp. 2579-2595 ◽  
Author(s):  
Philippe Diaz ◽  
Weize Huang ◽  
Charles M. Keyari ◽  
Brian Buttrick ◽  
Lauren Price ◽  
...  
2019 ◽  
Vol 92 (1) ◽  
pp. 115-123 ◽  
Author(s):  
Goran Benković ◽  
Hrvoje Rimac ◽  
Željan Maleš ◽  
Siniša Tomić ◽  
Zoran Lončar ◽  
...  

One of the most important groups of metabolic enzymes is cytochrome P450 superfamily. These enzymes are important in terms of the catalytic diversity and the large number of xenobiotics that are detoxified or activated by converting to reactive metabolites. Flavonoids are xenobiotics to which humans are exposed through diet. Data on their oxidative metabolism mediated by cytochromes P450 are limited. The aim of this study was to determine the enzymatic kinetics of O-demethylation and aromatic hydroxylation of flavonoid aglycons on recombinant cytochrome P450 enzymes and human liver microsomes systems. The study was performed on ten flavonoids, namely 3,7-dihydroxyflavone, 7-hydroxyflavone, acacetin, apigenin, flavone, galangin, kaempferol, naringenin, sakuranetin, and tangeretin using liquid chromatography coupled with mass spectrometry and UV detector. Most relevant enzyme involved in metabolism of flavonoid aglycons is CYP1A2, and its catalytic effectiveness ranges from 0.5 to 2.9 × 106 M–1 min–1. Having in mind high expression and involvement of CYP1A2 in metabolism of xenobiotics including drugs, and its intraindividual differences in expression and activity, potential of drug-flavonoid competitive interactions/inhibitions should be considered when consuming dietary supplement and foods rich in flavonoids.


1996 ◽  
Vol 330 (1) ◽  
pp. 87-96 ◽  
Author(s):  
Darryl C. Zeldin ◽  
Cindy R. Moomaw ◽  
Nate Jesse ◽  
Kenneth B. Tomer ◽  
Jeffrey Beetham ◽  
...  

1991 ◽  
Vol 200 (2) ◽  
pp. 511-517 ◽  
Author(s):  
Manuelle MAURICE ◽  
Stephane EMILIANI ◽  
Isabelle DALET-BELUCHE ◽  
Jean DERANCOURT ◽  
Reinhard LANGE

1998 ◽  
Vol 353 (2) ◽  
pp. 257-264 ◽  
Author(s):  
Qing-Yu Zhang ◽  
Gregory Raner ◽  
Xinxin Ding ◽  
Deborah Dunbar ◽  
Minor J. Coon ◽  
...  

Xenobiotica ◽  
2011 ◽  
Vol 41 (5) ◽  
pp. 358-371 ◽  
Author(s):  
Dong Kyun Kim ◽  
Kwang-Hyeon Liu ◽  
Ji Hyun Jeong ◽  
Hye Young Ji ◽  
Sei-Ryang Oh ◽  
...  

2009 ◽  
Vol 77 (2) ◽  
pp. 258-268 ◽  
Author(s):  
Justin D. Lutz ◽  
Vaishali Dixit ◽  
Catherine K. Yeung ◽  
Leslie J. Dickmann ◽  
Alex Zelter ◽  
...  

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