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In vitro interactions with repeated grapefruit juice administration--to peel or not to peel?

Brill, Shlomo and Zimmermann, Christian and Berger, Karin and Drewe, Juergen and Gutmann, Heike. (2009) In vitro interactions with repeated grapefruit juice administration--to peel or not to peel? Planta medica : Zeitschrift für Arzneipflanzenforschung : official organ of the Society for Medicinal Plant Research, Vol. 75. pp. 332-335.

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Official URL: http://edoc.unibas.ch/dok/A6003892

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Abstract

Interactions of acutely administered grapefruit juice (GFJ) with cytochrome P450 isoform 3A4 (CYP3A4) and P-glycoprotein (Pgp) function are well established. In this study, we investigated in vitro the effect of repeated administration of GFJ and its major constituents (the flavonoid naringin, its aglycone naringenin and the furanocoumarin bergamottin) on mRNA expression of MDR1 and CYP3A4 in LS180 cells. Since the bergamottin content is higher in the peel than in the fruit, we compared GFJ containing peel (GFJP+) with juice without any peel extract (GFJP-). GFJP- (1%) showed no significant effect on MDR1 and CYP3A4 mRNA expression, whereas 1% GFJP+ increased expression of MDR1 3.7-fold (P>0.01) and CYP3A4 2.3-fold (P>0.05). Of the tested constituents, only 10 microM bergamottin and 200 microM naringenin induced MDR1 mRNA levels 2.9- and 4.0-fold, respectively (P>0.01 for both), and CYP3A4 mRNA levels 3.2- and 15.6-fold (P>0.01 for both), respectively. Western blot analysis and rhodamine 123 uptake experiments partly confirmed these findings on the protein and the functional level. In summary, GFJ containing no peel extract may have a lower potential for interactions with CYP3A4 or P-glycoprotein.
Faculties and Departments:03 Faculty of Medicine > Departement Biomedizin > Former Units at DBM > Gastroenterology (Beglinger)
03 Faculty of Medicine > Bereich Medizinische Fächer (Klinik) > Klinische Pharmakologie > Klinische Pharmakologie (Krähenbühl)
03 Faculty of Medicine > Departement Klinische Forschung > Bereich Medizinische Fächer (Klinik) > Klinische Pharmakologie > Klinische Pharmakologie (Krähenbühl)
UniBasel Contributors:Drewe, Jürgen and Gutmann, Heike
Item Type:Article, refereed
Article Subtype:Research Article
Bibsysno:Link to catalogue
Publisher:Hippokrates-Verl.
ISSN:0032-0943
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:01 Feb 2013 08:46
Deposited On:01 Feb 2013 08:42

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