Transport of quercetin di-sodium salt in the human intestinal epithelial Caco-2 cell monolayer 139
Quercetin di-sodium salt (QDS), a water-soluble derivative of quercetin (Q), is a potent free radical scavenger. The aim of this study was to examine the in vitro intestinal transport of QDS compared to that of Q using the Caco-2 human intestinal epithelial cell line. The apical (A) to basolateral (...
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| Veröffentlicht in: | European journal of drug metabolism and pharmacokinetics 2007-07, Vol.32 (3), p.139-147 |
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| container_title | European journal of drug metabolism and pharmacokinetics |
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| creator | MILANE, H. A AL AHMAD, A NAITCHABANE, M VANDAMME, T. F JUNG, L UBEAUD, G |
| description | Quercetin di-sodium salt (QDS), a water-soluble derivative of quercetin (Q), is a potent free radical scavenger. The aim of this study was to examine the in vitro intestinal transport of QDS compared to that of Q using the Caco-2 human intestinal epithelial cell line. The apical (A) to basolateral (B) transport of QDS was found to be higher than the B to A transport of this compound. This polarized transport involved the presence of a carrier protein system. The involvement of the sodium/glucose transporter-1 (SGLT-1) was shown by using phloridzin, a selective inhibitor of this conveyor system. However, the transport of Q was not affected by this inhibitor. Moreover, the influx of QDS was pH-sensitive and decreased at pH 5.5 compared with that observed at pH 7.4 and 6.5. The permeability of QDS was 10-fold higher than that of Q. This could be explained by the involvement of SLGT-1 and the absence of an active efflux pump in the absorption of QDS in comparison with Q. This finding was supported by comparing the solubility of Q with that of QDS. This study indicates that both the higher solubility of QDS and its dependence on the SGLT-1 transport system resulted in more efficient permeability compared to Q. |
| doi_str_mv | 10.1007/BF03190476 |
| format | Article |
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A ; AL AHMAD, A ; NAITCHABANE, M ; VANDAMME, T. F ; JUNG, L ; UBEAUD, G</creator><creatorcontrib>MILANE, H. A ; AL AHMAD, A ; NAITCHABANE, M ; VANDAMME, T. F ; JUNG, L ; UBEAUD, G</creatorcontrib><description>Quercetin di-sodium salt (QDS), a water-soluble derivative of quercetin (Q), is a potent free radical scavenger. The aim of this study was to examine the in vitro intestinal transport of QDS compared to that of Q using the Caco-2 human intestinal epithelial cell line. The apical (A) to basolateral (B) transport of QDS was found to be higher than the B to A transport of this compound. This polarized transport involved the presence of a carrier protein system. The involvement of the sodium/glucose transporter-1 (SGLT-1) was shown by using phloridzin, a selective inhibitor of this conveyor system. However, the transport of Q was not affected by this inhibitor. Moreover, the influx of QDS was pH-sensitive and decreased at pH 5.5 compared with that observed at pH 7.4 and 6.5. The permeability of QDS was 10-fold higher than that of Q. This could be explained by the involvement of SLGT-1 and the absence of an active efflux pump in the absorption of QDS in comparison with Q. This finding was supported by comparing the solubility of Q with that of QDS. This study indicates that both the higher solubility of QDS and its dependence on the SGLT-1 transport system resulted in more efficient permeability compared to Q.</description><identifier>ISSN: 0378-7966</identifier><identifier>EISSN: 2107-0180</identifier><identifier>DOI: 10.1007/BF03190476</identifier><identifier>PMID: 18062406</identifier><language>eng</language><publisher>Genève: Médecine et hygiène</publisher><subject>Antioxidants - metabolism ; Biological and medical sciences ; Biological Transport ; Caco-2 Cells ; Cations, Monovalent ; Cell Membrane Permeability ; Epithelial Cells - metabolism ; Free Radical Scavengers - metabolism ; Humans ; Hydrogen-Ion Concentration ; In Vitro Techniques ; Intestinal Absorption ; Intestinal Mucosa - metabolism ; Medical sciences ; Pharmacology. Drug treatments ; Quercetin - metabolism ; Salts - metabolism ; Sodium - metabolism ; Sodium-Glucose Transporter 1 - metabolism ; Solubility</subject><ispartof>European journal of drug metabolism and pharmacokinetics, 2007-07, Vol.32 (3), p.139-147</ispartof><rights>2007 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c315t-7641b09309200865c9c46d0bef46dd184841597d0bb7e61367e87a5945b25ac93</citedby><cites>FETCH-LOGICAL-c315t-7641b09309200865c9c46d0bef46dd184841597d0bb7e61367e87a5945b25ac93</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27924,27925</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=19218880$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/18062406$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>MILANE, H. A</creatorcontrib><creatorcontrib>AL AHMAD, A</creatorcontrib><creatorcontrib>NAITCHABANE, M</creatorcontrib><creatorcontrib>VANDAMME, T. F</creatorcontrib><creatorcontrib>JUNG, L</creatorcontrib><creatorcontrib>UBEAUD, G</creatorcontrib><title>Transport of quercetin di-sodium salt in the human intestinal epithelial Caco-2 cell monolayer 139</title><title>European journal of drug metabolism and pharmacokinetics</title><addtitle>Eur J Drug Metab Pharmacokinet</addtitle><description>Quercetin di-sodium salt (QDS), a water-soluble derivative of quercetin (Q), is a potent free radical scavenger. The aim of this study was to examine the in vitro intestinal transport of QDS compared to that of Q using the Caco-2 human intestinal epithelial cell line. The apical (A) to basolateral (B) transport of QDS was found to be higher than the B to A transport of this compound. This polarized transport involved the presence of a carrier protein system. The involvement of the sodium/glucose transporter-1 (SGLT-1) was shown by using phloridzin, a selective inhibitor of this conveyor system. However, the transport of Q was not affected by this inhibitor. Moreover, the influx of QDS was pH-sensitive and decreased at pH 5.5 compared with that observed at pH 7.4 and 6.5. The permeability of QDS was 10-fold higher than that of Q. This could be explained by the involvement of SLGT-1 and the absence of an active efflux pump in the absorption of QDS in comparison with Q. This finding was supported by comparing the solubility of Q with that of QDS. This study indicates that both the higher solubility of QDS and its dependence on the SGLT-1 transport system resulted in more efficient permeability compared to Q.</description><subject>Antioxidants - metabolism</subject><subject>Biological and medical sciences</subject><subject>Biological Transport</subject><subject>Caco-2 Cells</subject><subject>Cations, Monovalent</subject><subject>Cell Membrane Permeability</subject><subject>Epithelial Cells - metabolism</subject><subject>Free Radical Scavengers - metabolism</subject><subject>Humans</subject><subject>Hydrogen-Ion Concentration</subject><subject>In Vitro Techniques</subject><subject>Intestinal Absorption</subject><subject>Intestinal Mucosa - metabolism</subject><subject>Medical sciences</subject><subject>Pharmacology. Drug treatments</subject><subject>Quercetin - metabolism</subject><subject>Salts - metabolism</subject><subject>Sodium - metabolism</subject><subject>Sodium-Glucose Transporter 1 - metabolism</subject><subject>Solubility</subject><issn>0378-7966</issn><issn>2107-0180</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2007</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpFkD1PwzAQhi0EolXpwg9AXliQDOc4_hqhooBUiaXMkeM4apATBzsZ-u8xolJvee9ePbrhQeiWwiMFkE8vW2BUQynFBVoWFCQBquASLYFJRaQWYoHWKX1DHqY05-IaLTIhihLEEtX7aIY0hjjh0OKf2UXrpm7ATUdSaLq5x8n4CedmOjh8mHsz5GNyKUPGYzd2ufddXjfGBlJg67zHfRiCN0cXMWX6Bl21xie3PuUKfW1f95t3svt8-9g874hllE9EipLWoBnoAkAJbrUtRQO1a3M0VJWqpFzL3NTSCcqEdEoarkteF9xYzVbo4f-vjSGl6NpqjF1v4rGiUP25qs6uMnz3D49z3bvmjJ7MZOD-BJhkjW-zJtulM6cLqpQC9gsDKG8R</recordid><startdate>20070701</startdate><enddate>20070701</enddate><creator>MILANE, H. A</creator><creator>AL AHMAD, A</creator><creator>NAITCHABANE, M</creator><creator>VANDAMME, T. F</creator><creator>JUNG, L</creator><creator>UBEAUD, G</creator><general>Médecine et hygiène</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope></search><sort><creationdate>20070701</creationdate><title>Transport of quercetin di-sodium salt in the human intestinal epithelial Caco-2 cell monolayer 139</title><author>MILANE, H. A ; AL AHMAD, A ; NAITCHABANE, M ; VANDAMME, T. F ; JUNG, L ; UBEAUD, G</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c315t-7641b09309200865c9c46d0bef46dd184841597d0bb7e61367e87a5945b25ac93</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2007</creationdate><topic>Antioxidants - metabolism</topic><topic>Biological and medical sciences</topic><topic>Biological Transport</topic><topic>Caco-2 Cells</topic><topic>Cations, Monovalent</topic><topic>Cell Membrane Permeability</topic><topic>Epithelial Cells - metabolism</topic><topic>Free Radical Scavengers - metabolism</topic><topic>Humans</topic><topic>Hydrogen-Ion Concentration</topic><topic>In Vitro Techniques</topic><topic>Intestinal Absorption</topic><topic>Intestinal Mucosa - metabolism</topic><topic>Medical sciences</topic><topic>Pharmacology. Drug treatments</topic><topic>Quercetin - metabolism</topic><topic>Salts - metabolism</topic><topic>Sodium - metabolism</topic><topic>Sodium-Glucose Transporter 1 - metabolism</topic><topic>Solubility</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>MILANE, H. A</creatorcontrib><creatorcontrib>AL AHMAD, A</creatorcontrib><creatorcontrib>NAITCHABANE, M</creatorcontrib><creatorcontrib>VANDAMME, T. 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F</au><au>JUNG, L</au><au>UBEAUD, G</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Transport of quercetin di-sodium salt in the human intestinal epithelial Caco-2 cell monolayer 139</atitle><jtitle>European journal of drug metabolism and pharmacokinetics</jtitle><addtitle>Eur J Drug Metab Pharmacokinet</addtitle><date>2007-07-01</date><risdate>2007</risdate><volume>32</volume><issue>3</issue><spage>139</spage><epage>147</epage><pages>139-147</pages><issn>0378-7966</issn><eissn>2107-0180</eissn><abstract>Quercetin di-sodium salt (QDS), a water-soluble derivative of quercetin (Q), is a potent free radical scavenger. The aim of this study was to examine the in vitro intestinal transport of QDS compared to that of Q using the Caco-2 human intestinal epithelial cell line. The apical (A) to basolateral (B) transport of QDS was found to be higher than the B to A transport of this compound. This polarized transport involved the presence of a carrier protein system. The involvement of the sodium/glucose transporter-1 (SGLT-1) was shown by using phloridzin, a selective inhibitor of this conveyor system. However, the transport of Q was not affected by this inhibitor. Moreover, the influx of QDS was pH-sensitive and decreased at pH 5.5 compared with that observed at pH 7.4 and 6.5. The permeability of QDS was 10-fold higher than that of Q. This could be explained by the involvement of SLGT-1 and the absence of an active efflux pump in the absorption of QDS in comparison with Q. This finding was supported by comparing the solubility of Q with that of QDS. This study indicates that both the higher solubility of QDS and its dependence on the SGLT-1 transport system resulted in more efficient permeability compared to Q.</abstract><cop>Genève</cop><pub>Médecine et hygiène</pub><pmid>18062406</pmid><doi>10.1007/BF03190476</doi><tpages>9</tpages></addata></record> |
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| ispartof | European journal of drug metabolism and pharmacokinetics, 2007-07, Vol.32 (3), p.139-147 |
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| source | MEDLINE; SpringerNature Journals |
| subjects | Antioxidants - metabolism Biological and medical sciences Biological Transport Caco-2 Cells Cations, Monovalent Cell Membrane Permeability Epithelial Cells - metabolism Free Radical Scavengers - metabolism Humans Hydrogen-Ion Concentration In Vitro Techniques Intestinal Absorption Intestinal Mucosa - metabolism Medical sciences Pharmacology. Drug treatments Quercetin - metabolism Salts - metabolism Sodium - metabolism Sodium-Glucose Transporter 1 - metabolism Solubility |
| title | Transport of quercetin di-sodium salt in the human intestinal epithelial Caco-2 cell monolayer 139 |
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