Linked Life Data

15911222

Source:http://linkedlifedata.com/resource/pubmed/id/15911222

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
2-3
pubmed:dateCreated
2005-5-24
pubmed:abstractText
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<quercetin<kaempferol<<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<<naringenin<isoquercitrin<spiraeoside<<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.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jun
pubmed:issn
0928-0987
pubmed:author
pubmed:issnType
Print
pubmed:volume
25
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
263-71
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
2005
pubmed:articleTitle
Modulation of drug transport by selected flavonoids: Involvement of P-gp and OCT?
pubmed:affiliation
School of Pharmacy, Johannes Gutenberg-University Mainz, D-55099 Mainz, Germany.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't