Modulation of the activity of ABC transporters (P-glycoprotein, MRP2, BCRP) by flavonoids and drug response

The present article aims to review the up-to-date information on the most recent studies of the interaction of flavonoids with ABC transporters, in particular the drug pharmacokinetic consequences of such a relationship. In addition, the modulation of the expression of the ABC transporters by flavon...

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Veröffentlicht in:Journal of pharmaceutical sciences 2010-02, Vol.99 (2), p.598-617
Hauptverfasser: Alvarez, Ana I., Real, Rebeca, Pérez, Miriam, Mendoza, Gracia, Prieto, Julio G., Merino, Gracia
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container_end_page 617
container_issue 2
container_start_page 598
container_title Journal of pharmaceutical sciences
container_volume 99
creator Alvarez, Ana I.
Real, Rebeca
Pérez, Miriam
Mendoza, Gracia
Prieto, Julio G.
Merino, Gracia
description The present article aims to review the up-to-date information on the most recent studies of the interaction of flavonoids with ABC transporters, in particular the drug pharmacokinetic consequences of such a relationship. In addition, the modulation of the expression of the ABC transporters by flavonoids is also illustrated. Flavonoids are a large group of plant polyphenols present extensively in our daily diets and herbal products. High intake of isoflavones has been associated with a variety of beneficial effects on several common diseases. These polyphenols interact with ABC drug transporters involved in drug resistance and drug absorption, distribution and excretion. A number of studies have demonstrated inhibition of drug transporters by flavonoids. This flavonoid-ABC-transporter interaction could be beneficial for poorly absorbed drugs but could also result in severe drug intoxication, especially drugs with a narrow therapeutic window. On the other hand, flavonoids are themselves substrates of ABC transporters. These proteins can affect the oral availability and tissue distribution of these compounds, modifying their beneficial effects. The challenge is to find a suitable way to predict harmful drug–flavonoid interactions mediated by these transporters. © 2009 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 99:598–617, 2010
doi_str_mv 10.1002/jps.21851
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In addition, the modulation of the expression of the ABC transporters by flavonoids is also illustrated. Flavonoids are a large group of plant polyphenols present extensively in our daily diets and herbal products. High intake of isoflavones has been associated with a variety of beneficial effects on several common diseases. These polyphenols interact with ABC drug transporters involved in drug resistance and drug absorption, distribution and excretion. A number of studies have demonstrated inhibition of drug transporters by flavonoids. This flavonoid-ABC-transporter interaction could be beneficial for poorly absorbed drugs but could also result in severe drug intoxication, especially drugs with a narrow therapeutic window. On the other hand, flavonoids are themselves substrates of ABC transporters. These proteins can affect the oral availability and tissue distribution of these compounds, modifying their beneficial effects. 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Pharm. Sci</addtitle><description>The present article aims to review the up-to-date information on the most recent studies of the interaction of flavonoids with ABC transporters, in particular the drug pharmacokinetic consequences of such a relationship. In addition, the modulation of the expression of the ABC transporters by flavonoids is also illustrated. Flavonoids are a large group of plant polyphenols present extensively in our daily diets and herbal products. High intake of isoflavones has been associated with a variety of beneficial effects on several common diseases. These polyphenols interact with ABC drug transporters involved in drug resistance and drug absorption, distribution and excretion. A number of studies have demonstrated inhibition of drug transporters by flavonoids. This flavonoid-ABC-transporter interaction could be beneficial for poorly absorbed drugs but could also result in severe drug intoxication, especially drugs with a narrow therapeutic window. On the other hand, flavonoids are themselves substrates of ABC transporters. These proteins can affect the oral availability and tissue distribution of these compounds, modifying their beneficial effects. 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subjects ABC transporters
Animals
ATP Binding Cassette Transporter, Sub-Family G, Member 2
ATP-Binding Cassette Transporters - biosynthesis
ATP-Binding Cassette Transporters - drug effects
ATP-Binding Cassette Transporters - metabolism
ATP-Binding Cassette, Sub-Family B, Member 1 - biosynthesis
ATP-Binding Cassette, Sub-Family B, Member 1 - drug effects
ATP-Binding Cassette, Sub-Family B, Member 1 - metabolism
BCRP/ABCG2
Biological and medical sciences
Cytochrome P-450 Enzyme Inhibitors
Cytochrome P-450 Enzyme System - metabolism
drug interaction
Enzyme Inhibitors - pharmacology
flavonoids
Flavonoids - metabolism
Flavonoids - pharmacology
Flavonoids - toxicity
General pharmacology
Humans
Medical sciences
MRP2/ABCC2
Multidrug Resistance-Associated Proteins - biosynthesis
Multidrug Resistance-Associated Proteins - drug effects
Multidrug Resistance-Associated Proteins - metabolism
Neoplasm Proteins - biosynthesis
Neoplasm Proteins - drug effects
Neoplasm Proteins - metabolism
P-glycoprotein/ABCB1
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
title Modulation of the activity of ABC transporters (P-glycoprotein, MRP2, BCRP) by flavonoids and drug response
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