Modulation of drug transport by selected flavonoids: Involvement of P-gp and OCT?
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences. Bd. 25. H. 2-3. 2005 S. 263 - 271
Erscheinungsjahr: 2005
ISBN/ISSN: 0928-0987
Publikationstyp: Zeitschriftenaufsatz
Sprache: Englisch
Doi/URN: 10.1016/j.ejps.2005.03.001
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Inhaltszusammenfassung
Flavonoids, as a common component of daily nutrition, are a possible source of interference with absorption processes, due to modulation of transporting proteins. In this study, the influence of selected flavonoids (quercetin, isoquercitrin, spiraeoside, rutin, kaempferol, naringenin, naringin, and kaempferol) on the transport of the P-gp substrate [3H]talinolol across Caco-2 cell monolayers was investigated. To elucidate the mechanism behind the interaction observed in this system the potenc...Flavonoids, as a common component of daily nutrition, are a possible source of interference with absorption processes, due to modulation of transporting proteins. In this study, the influence of selected flavonoids (quercetin, isoquercitrin, spiraeoside, rutin, kaempferol, naringenin, naringin, and kaempferol) on the transport of the P-gp substrate [3H]talinolol across Caco-2 cell monolayers was investigated. To elucidate the mechanism behind the interaction observed in this system the potency of the flavonoids to replace [3H]talinolol from its P-gp binding site as well as their activity to inhibit OCT2-mediated [14C]TEA uptake into LLC-PK(1) cells were measured, as P-gp and OCT have been shown to be present in Caco-2 cells. Six of the investigated flavonoids reduced the secretory flux of talinolol across Caco-2 cells (IC50-values: hesperetin» weiterlesen» einklappen
Autoren
Klassifikation
DFG Fachgebiet:
2.11 - Grundlagen der Biologie und Medizin
DDC Sachgruppe:
Medizin