کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
9917673 | 1556307 | 2005 | 9 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Modulation of drug transport by selected flavonoids: Involvement of P-gp and OCT?
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کلمات کلیدی
PBSMDRDMEMFBSP-gpTEER2-(N-morpholino)-ethanesulfonic acid - 2- (N-مورفولینو) -اتان سولفونیک اسیدP-glycoprotein - P-گلیکوپروتئینOct - اکتبرorganic cation transporter - حمل و نقل کاتیونی آلیfetal bovine serum - سرم جنین گاوCaco-2 cells - سلول های Caco-2LLC-PK1 cells - سلول های LLC-PK1Phosphate buffered saline - فسفات بافر شورFlavonoids - فلاونوئیدهاMeS - مسtransepithelial electrical resistance - مقاومت الکتریکی transepithelialMultidrug resistance - مقاومت چند داروییefflux ratio - نسبت خروجیTEA - چای
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
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-PK1 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 < quercetin < kaempferol âªÂ spiraeoside < isoquercitrin < naringin). But none of the selected flavonoids was able to replace [3H]talinolol from its binding to P-gp. However, the investigated flavonoids did show potency to inhibit OCT-mediated transport (IC50-values: quercetin < kaempferol âªÂ naringenin < isoquercitrin < spiraeoside âªÂ rutin < hesperetin < naringin). The present in vitro results demonstrate that flavonoids bear the ability to interfere with secretory intestinal transport processes. This might be due to an interaction with P-gp, but apparently not via competition at the talinolol binding site of P-gp. Another mode of interaction may be the inhibition of members of the OCT-family, which is located at the basolateral membrane of intestinal epithelial cells.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Pharmaceutical Sciences - Volume 25, Issues 2â3, June 2005, Pages 263-271
Journal: European Journal of Pharmaceutical Sciences - Volume 25, Issues 2â3, June 2005, Pages 263-271
نویسندگان
Monika Ofer, Siegfried Wolffram, Annette Koggel, Hilde Spahn-Langguth, Peter Langguth,