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Home » Archive » 2017

TDK conference 2017

Effect of quercetin derivatives on CYP450 enzymes in porcine intestinal epithelial cells
Bakumenko Lubov Nyikolajevna - year 5
University of Veterinary Medicine, Department of Pharmacology and Toxicology
Supervisors: Dr. Orsolya Farkas, Dr. Zita Karancsi

Abstract:

Flavonoid supplements have become really popular in the recent past years bacause of their beneficial effects. These compounds are found in many fruits, vegeables and in some beverages, thus they can be consumed in large quantities during a regular diet.

In the recent years it has been reviewed, that there can be interactions between some flavonoids and cytochrome P450 enzymes, which play a critical role in the metabolism of xenobiotics. As a consequence, simultaneous consumption of flavonoids and drugs can alter the farmakocinetics of the latter. In case of oral administration CYP450 enzymes of small intestine play an important role in the metabolism, therefore our studies focus on this organ.

The goal of our study was to examine the effect of quercetin and its derivates, 3-methyl-quercetin and 3’7-dimethyl-quercetin on the CYP enzyme activity. We also wanted to study, how they behave in the presence of known CYP-inductor, and by adding antipirin we wanted to reveal any potential food-drug interactions. The studied flavonoid compounds were applied at a concentration of 25 and 50 μM in order to examinethe concentration dependence of their effect.

In our study we used IPEC-J2 porcine intestinal epithelial cells. These cells were treated with flavonoids of concentration 25 and 50 μM, and the changes they caused in the enzyme activity was compered with the enzyme activity of control cells and the ones, which were treated with inductor (phenobarbital 1mM) and with inhibitor (50 μM naphtoflavone+25 μM ketoconazole). We also studied the enzyme activity of the cells, which were treated simultaneosly with flavonoids of concentration 25 and 50 μM and inductor, and the effect of the combination of the same concentration of flavonoids and antipyrine. CYP activity was measured by luminescent method.

Both the quercetin and the 3-o-methyl-quercetin significantly inhibited the CYP3A4 enzyme, but the 3’7-dimethylquercetin did not alter the enzyme activity. In the case, when the cells were treated with combination of a flavonoid and the inductor, the CYP3A4 enzyme was also inhibitid by quercetin and 3-o-methyl-quercetin. By the simultaneous application of antipyrine and quercetin we could observe significant inhibiting effect compared to the antipirin application.

The results verify our assumption, that some flavonoids can modify CYP enzyme activity, so further studies would be needed to study the potential drug-interactions.



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