Major active components in grapefruit, orange, and apple juices responsible for OATP2B1-mediated drug interactions.
Identifieur interne : 000D97 ( Main/Exploration ); précédent : 000D96; suivant : 000D98Major active components in grapefruit, orange, and apple juices responsible for OATP2B1-mediated drug interactions.
Auteurs : Yoshiyuki Shirasaka [Japon] ; Megumi Shichiri ; Takanori Mori ; Takeo Nakanishi ; Ikumi TamaiSource :
- Journal of pharmaceutical sciences [ 1520-6017 ] ; 2013.
English descriptors
- KwdEn :
- Animals, Beverages, Citrus paradisi, Citrus sinensis, Dose-Response Relationship, Drug, Estrone (analogs & derivatives), Estrone (metabolism), Flavanones (pharmacology), Flavonoids (pharmacology), Food-Drug Interactions, Fruit, Hesperidin (pharmacology), Humans, Kinetics, Least-Squares Analysis, Malus, Models, Biological, Nonlinear Dynamics, Oocytes, Organic Anion Transporters (antagonists & inhibitors), Organic Anion Transporters (genetics), Organic Anion Transporters (metabolism), Osmolar Concentration, Phlorhizin (pharmacology), Quercetin (pharmacology), Xenopus laevis.
- MESH :
- chemical , analogs & derivatives : Estrone.
- chemical , antagonists & inhibitors : Organic Anion Transporters.
- chemical , genetics : Organic Anion Transporters.
- chemical , metabolism : Estrone, Organic Anion Transporters.
- chemical , pharmacology : Flavanones, Flavonoids, Hesperidin, Phlorhizin, Quercetin.
- Animals, Beverages, Citrus paradisi, Citrus sinensis, Dose-Response Relationship, Drug, Food-Drug Interactions, Fruit, Humans, Kinetics, Least-Squares Analysis, Malus, Models, Biological, Nonlinear Dynamics, Oocytes, Osmolar Concentration, Xenopus laevis.
Abstract
We aimed to explore the major active components in grapefruit juice (GFJ), orange juice (OJ), and apple juice (AJ) that are responsible for OATP2B1-mediated drug interactions, by means of in vitro studies using Xenopus oocytes expressing OATP2B1 with a typical OATP2B1 substrate, estrone-3-sulfate. All three juices inhibited OATP2B1-mediated estrone-3-sulfate uptake with half-maximum inhibition (IC(50) ) values of 0.222% (GFJ), 0.807% (OJ), and 2.27% (AJ). Eight major flavonoids (naringin, naringenin, hesperidin, hesperetin, phloridzin, phloretin, quercetin, and kaempferol) contained in the juices inhibited OATP2B1-mediated estrone-3-sulfate uptake with IC(50) values of 4.63, 49.2, 1.92, 67.6, 23.2, 1.31, 9.47, and 21.3 µM, respectively. When the concentration-IC(50) ratios ([C]/IC(50) ) of these flavonoids in GFJ, OJ, and AJ were calculated, values of [C]/IC(50) ≥ 100 were obtained for naringin in GFJ and hesperidin in OJ. No flavonoid in AJ showed a ratio higher than unity. However, significant inhibition of OATP2B1 was observed with a mixture of phloridzin, phloretin, hesperidin, and quercetin at the concentrations present in AJ. In conclusion, our results indicate that naringin and hesperidin are the major OATP2B1 inhibitors in GFJ and OJ, respectively, whereas a combination of multiple components appears to be responsible for OATP2B1 inhibition by AJ.
DOI: 10.1002/jps.23357
PubMed: 23132664
Affiliations:
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uniqKey="Mori T" first="Takanori" last="Mori">Takanori Mori</name></author><author><name sortKey="Nakanishi, Takeo" sort="Nakanishi, Takeo" uniqKey="Nakanishi T" first="Takeo" last="Nakanishi">Takeo Nakanishi</name></author><author><name sortKey="Tamai, Ikumi" sort="Tamai, Ikumi" uniqKey="Tamai I" first="Ikumi" last="Tamai">Ikumi Tamai</name></author></titleStmt><publicationStmt><idno type="wicri:source">PubMed</idno><date when="2013">2013</date><idno type="RBID">pubmed:23132664</idno><idno type="pmid">23132664</idno><idno type="doi">10.1002/jps.23357</idno><idno type="wicri:Area/PubMed/Corpus">000515</idno><idno type="wicri:Area/PubMed/Curation">000515</idno><idno type="wicri:Area/PubMed/Checkpoint">000515</idno><idno type="wicri:Area/Ncbi/Merge">001137</idno><idno type="wicri:Area/Ncbi/Curation">001137</idno><idno type="wicri:Area/Ncbi/Checkpoint">001137</idno><idno type="wicri:Area/Main/Merge">000E01</idno><idno type="wicri:Area/Main/Curation">000D97</idno><idno 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Shichiri</name></author><author><name sortKey="Mori, Takanori" sort="Mori, Takanori" uniqKey="Mori T" first="Takanori" last="Mori">Takanori Mori</name></author><author><name sortKey="Nakanishi, Takeo" sort="Nakanishi, Takeo" uniqKey="Nakanishi T" first="Takeo" last="Nakanishi">Takeo Nakanishi</name></author><author><name sortKey="Tamai, Ikumi" sort="Tamai, Ikumi" uniqKey="Tamai I" first="Ikumi" last="Tamai">Ikumi Tamai</name></author></analytic><series><title level="j">Journal of pharmaceutical sciences</title><idno type="eISSN">1520-6017</idno><imprint><date when="2013" type="published">2013</date></imprint></series></biblStruct></sourceDesc></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Animals</term><term>Beverages</term><term>Citrus paradisi</term><term>Citrus sinensis</term><term>Dose-Response Relationship, Drug</term><term>Estrone (analogs & derivatives)</term><term>Estrone (metabolism)</term><term>Flavanones (pharmacology)</term><term>Flavonoids (pharmacology)</term><term>Food-Drug Interactions</term><term>Fruit</term><term>Hesperidin (pharmacology)</term><term>Humans</term><term>Kinetics</term><term>Least-Squares Analysis</term><term>Malus</term><term>Models, Biological</term><term>Nonlinear Dynamics</term><term>Oocytes</term><term>Organic Anion Transporters (antagonists & inhibitors)</term><term>Organic Anion Transporters (genetics)</term><term>Organic Anion Transporters (metabolism)</term><term>Osmolar Concentration</term><term>Phlorhizin (pharmacology)</term><term>Quercetin (pharmacology)</term><term>Xenopus laevis</term></keywords><keywords scheme="MESH" type="chemical" qualifier="analogs & derivatives" xml:lang="en"><term>Estrone</term></keywords><keywords scheme="MESH" type="chemical" qualifier="antagonists & inhibitors" xml:lang="en"><term>Organic Anion Transporters</term></keywords><keywords scheme="MESH" type="chemical" qualifier="genetics" xml:lang="en"><term>Organic Anion Transporters</term></keywords><keywords scheme="MESH" type="chemical" qualifier="metabolism" xml:lang="en"><term>Estrone</term><term>Organic Anion Transporters</term></keywords><keywords scheme="MESH" type="chemical" qualifier="pharmacology" xml:lang="en"><term>Flavanones</term><term>Flavonoids</term><term>Hesperidin</term><term>Phlorhizin</term><term>Quercetin</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Animals</term><term>Beverages</term><term>Citrus paradisi</term><term>Citrus sinensis</term><term>Dose-Response Relationship, Drug</term><term>Food-Drug Interactions</term><term>Fruit</term><term>Humans</term><term>Kinetics</term><term>Least-Squares Analysis</term><term>Malus</term><term>Models, Biological</term><term>Nonlinear Dynamics</term><term>Oocytes</term><term>Osmolar Concentration</term><term>Xenopus laevis</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">We aimed to explore the major active components in grapefruit juice (GFJ), orange juice (OJ), and apple juice (AJ) that are responsible for OATP2B1-mediated drug interactions, by means of in vitro studies using Xenopus oocytes expressing OATP2B1 with a typical OATP2B1 substrate, estrone-3-sulfate. All three juices inhibited OATP2B1-mediated estrone-3-sulfate uptake with half-maximum inhibition (IC(50) ) values of 0.222% (GFJ), 0.807% (OJ), and 2.27% (AJ). Eight major flavonoids (naringin, naringenin, hesperidin, hesperetin, phloridzin, phloretin, quercetin, and kaempferol) contained in the juices inhibited OATP2B1-mediated estrone-3-sulfate uptake with IC(50) values of 4.63, 49.2, 1.92, 67.6, 23.2, 1.31, 9.47, and 21.3 µM, respectively. When the concentration-IC(50) ratios ([C]/IC(50) ) of these flavonoids in GFJ, OJ, and AJ were calculated, values of [C]/IC(50) ≥ 100 were obtained for naringin in GFJ and hesperidin in OJ. No flavonoid in AJ showed a ratio higher than unity. However, significant inhibition of OATP2B1 was observed with a mixture of phloridzin, phloretin, hesperidin, and quercetin at the concentrations present in AJ. In conclusion, our results indicate that naringin and hesperidin are the major OATP2B1 inhibitors in GFJ and OJ, respectively, whereas a combination of multiple components appears to be responsible for OATP2B1 inhibition by AJ.</div></front></TEI><affiliations><list><country><li>Japon</li></country></list><tree><noCountry><name sortKey="Mori, Takanori" sort="Mori, Takanori" uniqKey="Mori T" first="Takanori" last="Mori">Takanori Mori</name><name sortKey="Nakanishi, Takeo" sort="Nakanishi, Takeo" uniqKey="Nakanishi T" first="Takeo" last="Nakanishi">Takeo Nakanishi</name><name sortKey="Shichiri, Megumi" sort="Shichiri, Megumi" uniqKey="Shichiri M" first="Megumi" last="Shichiri">Megumi Shichiri</name><name sortKey="Tamai, Ikumi" sort="Tamai, Ikumi" uniqKey="Tamai I" first="Ikumi" last="Tamai">Ikumi Tamai</name></noCountry><country name="Japon"><noRegion><name sortKey="Shirasaka, Yoshiyuki" sort="Shirasaka, Yoshiyuki" uniqKey="Shirasaka Y" first="Yoshiyuki" last="Shirasaka">Yoshiyuki Shirasaka</name></noRegion></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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