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Evaluation of Inhibitory Effects of Caffeic acid and Quercetin on Human Liver Cytochrome P450 Activities
Author(s) -
Rastogi Himanshu,
Jana Snehasis
Publication year - 2014
Publication title -
phytotherapy research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.019
H-Index - 129
eISSN - 1099-1573
pISSN - 0951-418X
DOI - 10.1002/ptr.5220
Subject(s) - caffeic acid , quercetin , cyp1a2 , cyp3a4 , pharmacology , chemistry , ic50 , cytochrome p450 , non competitive inhibition , drug interaction , microsome , polyphenol , biochemistry , drug , enzyme , biology , antioxidant , in vitro
When herbal drugs and conventional allopathic drugs are used together, they can interact in our body which can lead to the potential for herb–drug interactions. This work was conducted to evaluate the herb–drug interaction potential of caffeic acid and quercetin mediated by cytochrome P450 (CYP) inhibition. Human liver microsomes (HLMs) were added to each selective probe substrates of cytochrome P450 enzymes with or without of caffeic acid and quercetin. IC 50 , K i values, and the types of inhibition were determined. Both caffeic acid and quercetin were potent competitive inhibitors of CYP1A2 ( K i = 1.16 and 0.93 μM, respectively) and CYP2C9 ( K i = 0.95 and 1.67 μM, respectively). Caffeic acid was a potent competitive inhibitor of CYP2D6 ( K i = 1.10 μM) and a weak inhibitor of CYP2C19 and CYP3A4 (IC 50 > 100 μM). Quercetin was a potent competitive inhibitor of CYP 2C19 and CYP3A4 ( K i = 1.74 and 4.12 μM, respectively) and a moderate competitive inhibitor of CYP2D6 ( K i = 18.72 μM). These findings might be helpful for safe and effective use of polyphenols in clinical practice. Our data indicated that it is necessary to study the in vivo interactions between drugs and pharmaceuticals with dietary polyphenols. Copyright © 2014 John Wiley & Sons, Ltd.