ArticleBritish journal of pharmacology2000
Effect of furanocoumarin derivatives in grapefruit juice on the uptake of vinblastine by Caco-2 cells and on the activity of cytochrome P450 3A4.
Article in British journal of pharmacology, 2000. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 35 papers.
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Who cites it
35 citing papers in PubMed, 156 citations in OpenAlex.
- Effect of Low-Furanocoumarin Hybrid Grapefruit Juice Consumption on Midazolam Pharmacokinetics.Journal of clinical pharmacology · 2017Trial
- Impact of citrus soft drinks relative to grapefruit juice on ciclosporin disposition.British journal of clinical pharmacology · 2006Trial
- Pharmacokinetic analysis of felodipine-grapefruit juice interaction based on an irreversible enzyme inhibition model.British journal of clinical pharmacology · 2000Trial
- Bergaptol, a Major Furocoumarin in Citrus: Pharmacological Properties and Toxicity.Molecules (Basel, Switzerland) · 2024Review
- Effect ofFrontiers in pharmacology · 2024Article
- Recommendations on the use of azole antifungals in hematology-oncology patients.Revista espanola de quimioterapia : publicacion oficial de la Sociedad Espanola de Quimioterapia · 2023Review
- Effects of bergapten on the pharmacokinetics of macitentan in rats bothFrontiers in pharmacology · 2023Article
- Pharmaceutical Excipients and Drug Metabolism: A Mini-Review.International journal of molecular sciences · 2020Review
- Differences in xanthotoxin metabolites in seven mammalian liver microsomes.Experimental and therapeutic medicine · 2020Article
- Anticancer Potential of Furanocoumarins: Mechanistic and Therapeutic Aspects.International journal of molecular sciences · 2020Review
- Synthesis of Spin-Labelled Bergamottin: A Potent CYP3A4 Inhibitor with Antiproliferative Activity.International journal of molecular sciences · 2020Article
- The Multifarious Link between Cytochrome P450s and Cancer.Oxidative medicine and cellular longevity · 2020Review
- Potential Influence of Centrally Acting Herbal Drugs on Transporters at the Blood-Cerebrospinal Fluid Barrier and Blood-Brain Barrier.European journal of drug metabolism and pharmacokinetics · 2018Review
- Increased tacrolimus blood concentration by Beni-Madonna - a new hybrid citrus cultivar categorized as 'Tangor', in a liver transplant patient: likely furanocoumarin-mediated inhibition of CYP3A4 or P-glycoprotein.British journal of clinical pharmacology · 2018Article
- Natural Products as Alternative Choices for P-Glycoprotein (P-gp) Inhibition.Molecules (Basel, Switzerland) · 2017Review
- Extracts of Immature OrangeFrontiers in pharmacology · 2017Article
- P-glycoprotein inhibitors of natural origin as potential tumor chemo-sensitizers: A review.Journal of advanced research · 2015Review
- Improved oral bioavailability of BCS class 2 compounds by self nano-emulsifying drug delivery systems (SNEDDS): the underlying mechanisms for amiodarone and talinolol.Pharmaceutical research · 2013Article
- Identification of the residue in human CYP3A4 that is covalently modified by bergamottin and the reactive intermediate that contributes to the grapefruit juice effect.Drug metabolism and disposition: the biological fate of chemicals · 2012Article
- The effect of grapefruit juice on drug disposition.Expert opinion on drug metabolism & toxicology · 2011Review
Corrections and comments
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Authors and funding
8 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
1. The presence of inhibitors of drug efflux transporters, such as P-glycoprotein (P-gp), in grapefruit juice (GFJ) was confirmed based on the uptake of [(3)H]-vinblastine (VBL) by Caco-2 cells. 2. The uptake of [(3)H]-VBL by Caco-2 cells was significantly increased by the ethyl acetate extract of GFJ as well as by cyclosporin A. The extract was separated on a Cosmosil column and the eluate with 60% methanol increased [(3)H]-VBL uptake, while the activity to inhibit CYP3A4 was greatest in the 70 and 80% eluates. 3. These results show that the major inhibitor of efflux transport of VBL is different from that of CYP3A4. 4. Further separation of the 60% methanol eluate afforded dihydroxybergamottin (DHBG). Both ethyl acetate extract of GFJ and DHBG increased steady-state [(3)H]-VBL uptake by LLC-GA5-COL300 cells. Besides DHBG, other furanocoumarins contained in GFJ, such as bergamottin, FC726, bergaptol and bergapten, increased the steady-state uptake of [(3)H]-VBL by Caco-2 cells. 5. The order of inhibitory potency of these compounds was FC726>DHBG>bergamottin>bergapten>bergaptol . While, the IC(50) values for inhibition of CYP3A4 were 0.075, 0.45, 1.0, 1.0 and >20 microM, respectively. Bergaptol specifically inhibited VBL efflux. 6. DHBG was thus identified as a candidate for inhibitors of VBL transport, together with other furanocoumarins. Moreover, partly involvement of the P-gp inhibition was suggested. 7. Therefore, the inhibition of efflux transport of drugs as well as of drug metabolism by CYP3A4 could be an important cause of drug-GFJ interaction.
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