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Open AccessArticle

The Modulation of Phase II Drug-Metabolizing Enzymes in Proliferating and Differentiated CaCo-2 Cells by Hop-Derived Prenylflavonoids

1
Faculty of Medicine and Dentistry, Palacký University, Hněvotínská 3, 77515 Olomouc, Czech Republic
2
Faculty of Pharmacy in Hradec Králové, Charles University, Heyrovského 1203, 50005 Hradec Králové, Czech Republic
*
Author to whom correspondence should be addressed.
Nutrients 2020, 12(7), 2138; https://doi.org/10.3390/nu12072138
Received: 2 June 2020 / Revised: 10 July 2020 / Accepted: 16 July 2020 / Published: 18 July 2020
(This article belongs to the Special Issue Dietary (Poly)Phenols and Health)
Prenylflavonoids in the human organism exhibit various health-beneficial activities, although they may interfere with drugs via the modulation of the expression and/or activity of drug-metabolizing enzymes. As intestinal cells are exposed to the highest concentrations of prenylflavonoids, we decided to study the cytotoxicity and modulatory effects of the four main hop-derived prenylflavonoids on the activities and mRNA expression of the main drug-conjugating enzymes in human CaCo-2 cells. Proliferating CaCo-2 cells were used for these purposes as a model of colorectal cancer cells, and differentiated CaCo-2 cells were used as an enterocyte-like model. All the tested prenylflavonoids inhibited the CaCo-2 cells proliferation, with xanthohumol proving the most effective (IC50 8.5 µM). The prenylflavonoids modulated the activities and expressions of the studied enzymes to a greater extent in the differentiated, as opposed to the proliferating, CaCo-2 cells. In the differentiated cells, all the prenylflavonoids caused a marked increase in glutathione S-transferase and catechol-O-methyltransferase activities, while the activity of sulfotransferase was significantly inhibited. Moreover, the prenylflavonoids upregulated the mRNA expression of uridine diphosphate (UDP)-glucuronosyl transferase 1A6 and downregulated that of glutathione S-transferase 1A1/2. View Full-Text
Keywords: prenylflavonoid; xanthohumol; enzymatic activity; mRNA expression; glutathione S-transferase; catechol-O-methyltransferase; sulfotransferase; UDP-glucuronosyl transferase; CaCo-2 cells prenylflavonoid; xanthohumol; enzymatic activity; mRNA expression; glutathione S-transferase; catechol-O-methyltransferase; sulfotransferase; UDP-glucuronosyl transferase; CaCo-2 cells
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Lněničková, K.; Šadibolová, M.; Matoušková, P.; Szotáková, B.; Skálová, L.; Boušová, I. The Modulation of Phase II Drug-Metabolizing Enzymes in Proliferating and Differentiated CaCo-2 Cells by Hop-Derived Prenylflavonoids. Nutrients 2020, 12, 2138.

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