Variation of flavonoids and furanocoumarins in grapefruit juices: a potential source of variability in grapefruit juice-drug interaction studies
- PMID: 16390207
- DOI: 10.1021/jf0516944
Variation of flavonoids and furanocoumarins in grapefruit juices: a potential source of variability in grapefruit juice-drug interaction studies
Abstract
Grapefruit juice (GFJ) has been found to interact with several medications, increasing their oral bioavailability and the risk of toxicity. Inhibition of CYP3A4 in the small intestine by flavonoids (such as naringin and naringenin) and furanocoumarins (including bergamottin and 6',7'-dihydroxybergamottin) present in GFJ seems to be the predominant mechanism, although P-glycoprotein and influx transporters in the small intestine are also involved. The quantity of interactive compounds ingested may affect the magnitude and mechanism of the food-drug interaction. Therefore, these four compounds were quantified by HPLC analysis in commercially available and fresh-squeezed GFJ and in grapefruit tissues. Considerable variability in naringin (174-1492 micromol/L), bergamottin (1.0-36.6 micromol/L), and 6',7'-dihydroxybergamottin (0.22-52.5 micromol/L) was observed, whereas naringenin could not be detected. White grapefruit showed higher concentrations of naringin and furanocoumarins located in the albedo and flavedo compared with red varieties. Findings from this study suggest considering concentrations of components with a potential for drug interactions in GFJ-drug interaction studies. The concentration of potentially contributing compounds may crucially influence the magnitude of observed interaction and impair direct comparison of studies in which different juices have been used.
Similar articles
-
Rapid Quantitation of Furanocoumarins and Flavonoids in Grapefruit Juice using Ultra-Performance Liquid Chromatography.Phytochem Anal. 2013 Nov-Dec;24(6):654-60. doi: 10.1002/pca.2449. Epub 2013 Jun 18. Phytochem Anal. 2013. PMID: 23780830 Free PMC article.
-
[Flavonoids--bioactive compounds in fruits juice].Rev Med Chir Soc Med Nat Iasi. 2010 Oct-Dec;114(4):1209-14. Rev Med Chir Soc Med Nat Iasi. 2010. PMID: 21500482 Romanian.
-
Effect of grapefruit juice in relation to human pharmacokinetic study.Curr Clin Pharmacol. 2006 May;1(2):157-61. doi: 10.2174/157488406776872550. Curr Clin Pharmacol. 2006. PMID: 18666368 Review.
-
A furanocoumarin-free grapefruit juice establishes furanocoumarins as the mediators of the grapefruit juice-felodipine interaction.Am J Clin Nutr. 2006 May;83(5):1097-105. doi: 10.1093/ajcn/83.5.1097. Am J Clin Nutr. 2006. PMID: 16685052 Clinical Trial.
-
[Grapefruit juice and drugs: a hazardous combination?].Therapie. 2002 Sep-Oct;57(5):432-45. Therapie. 2002. PMID: 12611197 Review. French.
Cited by
-
DDID: a comprehensive resource for visualization and analysis of diet-drug interactions.Brief Bioinform. 2024 Mar 27;25(3):bbae212. doi: 10.1093/bib/bbae212. Brief Bioinform. 2024. PMID: 38711369 Free PMC article.
-
Differences in the Perception of Dietary Supplements between Dietary Supplement/Medicine Users and Non-Users.Nutrients. 2022 Oct 3;14(19):4114. doi: 10.3390/nu14194114. Nutrients. 2022. PMID: 36235766 Free PMC article.
-
Nanoparticulate Drug Delivery Strategies to Address Intestinal Cytochrome P450 CYP3A4 Metabolism towards Personalized Medicine.Pharmaceutics. 2021 Aug 16;13(8):1261. doi: 10.3390/pharmaceutics13081261. Pharmaceutics. 2021. PMID: 34452222 Free PMC article. Review.
-
Intake of Furocoumarins and Risk of Skin Cancer in 2 Prospective US Cohort Studies.J Nutr. 2020 Jun 1;150(6):1535-1544. doi: 10.1093/jn/nxaa062. J Nutr. 2020. PMID: 32221600 Free PMC article.
-
Botanical Sources, Chemistry, Analysis, and Biological Activity of Furanocoumarins of Pharmaceutical Interest.Molecules. 2019 Jun 8;24(11):2163. doi: 10.3390/molecules24112163. Molecules. 2019. PMID: 31181737 Free PMC article. Review.
Publication types
MeSH terms
Substances
LinkOut - more resources
Full Text Sources
Other Literature Sources