The DOI matches its Crossref record; 39 of the 39 references it cites were found in a registry or an index.
Naringin is a Major and Selective Clinical Inhibitor of Organic Anion-Transporting Polypeptide 1A2 (OATP1A2) in Grapefruit Juice
Abstract
We showed previously that grapefruit and orange juices inhibited human enteric organic anion-transporting polypeptide (OATP)1A2 in vitro and lowered oral fexofenadine bioavailability clinically. Inhibition of OATP1A2 transport by flavonoids in grapefruit (naringin) and orange (hesperidin) was conducted in vitro. Two randomized, crossover, pharmacokinetic studies were performed clinically. In one study, 120 mg of fexofenadine was ingested with 300 ml grapefruit juice, an aqueous solution of naringin at the same juice concentration (1,200 microM), or water. In the other study, fexofenadine was administered with grapefruit juice, with or 2 h before aqueous suspension of the particulate fraction of juice containing known clinical inhibitors of enteric CYP3A4, but relatively low naringin concentration (34 microM), or with water. Naringin and hesperidin's half-maximal inhibitions were 3.6 and 2.7 microM, respectively. Fexofenadine area under the plasma drug concentration-time curves (AUCs) with grapefruit juice and naringin solution were 55% (P<0.001) and 75% (P<0.05) of that with water, respectively. Fexofenadine AUCs with grapefruit juice and particulate fractions were 57% (P<0.001), 96% (not significant (NS)), and 97% (NS) of that with water, respectively. Individuals tested in both studies (n=9 of 12) had highly reproducible fexofenadine AUC with water (r(2)=0.85, P<0.001) and extent of reduction of it with grapefruit juice (r(2)=0.72, P<0.01). Naringin most probably directly inhibited enteric OATP1A2 to decrease oral fexofenadine bioavailability. Inactivation of enteric CYP3A4 was probably not involved. Naringin appears to have sufficient safety, specificity, and sensitivity to be a clinical OATP1A2 inhibitor probe. Inherent OATP1A2 activity may be influenced by genetic factors. This appears to be the first report of a single dietary constituent clinically modulating drug transport.
Overview
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Integrity signals
Registry
Cites
Statistics
Verification
Claims the paper makes
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Self-check
Percentages, sums and reported differences re-computed from the paper’s own numbers.
The self-check needs the paper’s full text.
Citations
Cites
Kelder, J., Grootenhuis, P. D. J., Bayada, D. M., Delbressine, L. P. C., & Ploemen, J.-P. (1999) · Pharmaceutical Research · doi:10.1023/a:1015040217741 · Cited by 813
Lown, K. S., Bailey, D. G., Fontana, R. J., Janardan, S. K., Adair, C. H., Fortlage, L. A., Brown, M. B., Guo, W., & Watkins, P. B. (1997) · Journal of Clinical Investigation · doi:10.1172/jci119439 · Cited by 624
Self-citationHo, R. H., Tirona, R. G., Leake, B. F., Glaeser, H., Lee, W., Lemke, C. J., Wang, Y., & Kim, R. B. (2006) · Gastroenterology · doi:10.1053/j.gastro.2006.02.034 · Cited by 611
Self-citationDresser, G. K., Bailey, D. G., Leake, B. F., Schwarz, U. I., Dawson, P. A., Freeman, D. J., & Kim, R. B. (2002) · Clinical Pharmacology & Therapeutics · doi:10.1067/mcp.2002.121152 · Cited by 606
Self-citationOATP and P-Glycoprotein Transporters Mediate the Cellular Uptake and Excretion of Fexofenadine
Cvetkovic, M., Leake, B., Fromm, M. F., Wilkinson, G. R., & Kim, R. B. (1999) · Drug Metabolism and Disposition · doi:10.1016/s0090-9556(24)15235-x · Cited by 597
Self-citationTransporters and drug therapy: Implications for drug disposition and disease
HO, R., & KIM, R. (2005) · Clinical Pharmacology & Therapeutics · doi:10.1016/j.clpt.2005.05.011 · Cited by 502
Self-citationWiniwarter, S., Bonham, N. M., Ax, F., Hallberg, A., Lennernäs, H., & Karlén, A. (1998) · Journal of Medicinal Chemistry · doi:10.1021/jm9810102 · Cited by 453
Kobayashi, D., Nozawa, T., Imai, K., Nezu, J.-I., Tsuji, A., & Tamai, I. (2003) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.103.051300 · Cited by 416
Intestinal Drug Transporter Expression and the Impact of Grapefruit Juice in Humans
Glaeser, H., Bailey, D. G., Dresser, G. K., Gregor, J. C., Schwarz, U. I., McGrath, J. S., Jolicoeur, E., Lee, W., Leake, B. F., Tirona, R. G., et al. (2007) · Clinical Pharmacology & Therapeutics · doi:10.1038/sj.clpt.6100056 · Cited by 407
Self-citationPolymorphisms in Human Organic Anion-transporting Polypeptide 1A2 (OATP1A2)
Lee, W., Glaeser, H., Smith, L. H., Roberts, R. L., Moeckel, G. W., Gervasini, G., Leake, B. F., & Kim, R. B. (2005) · Journal of Biological Chemistry · doi:10.1074/jbc.m411092200 · Cited by 365
Self-citation
Cited by
Alam, M. A., Subhan, N., Rahman, M. M., Uddin, S. J., Reza, H. M., & Sarker, S. D. (2014) · Advances in Nutrition · doi:10.3945/an.113.005603 · Cited by 788
Roth, M., Obaidat, A., & Hagenbuch, B. (2012) · British Journal of Pharmacology · doi:10.1111/j.1476-5381.2011.01724.x · Cited by 767
Coexistence of passive and carrier-mediated processes in drug transport
Sugano, K., Kansy, M., Artursson, P., Avdeef, A., Bendels, S., Di, L., Ecker, G. F., Faller, B., Fischer, H., Gerebtzoff, G., et al. (2010) · Nature Reviews Drug Discovery · doi:10.1038/nrd3187 · Cited by 649
Fingerprinting food: current technologies for the detection of food adulteration and contamination
Ellis, D. I., Brewster, V. L., Dunn, W. B., Allwood, J. W., Golovanov, A. P., & Goodacre, R. (2012) · Chemical Society Reviews · doi:10.1039/c2cs35138b · Cited by 440
The Role of Transporters in the Pharmacokinetics of Orally Administered Drugs
Shugarts, S., & Benet, L. Z. (2009) · Pharmaceutical Research · doi:10.1007/s11095-009-9924-0 · Cited by 438
Metadata
- Authors
- Bailey, D. G., Dresser, G. K., Leake, B. F., & Kim, R. B.
- Venue
- Clinical Pharmacology & Therapeutics
- Publisher
- Wiley
- Published
- 2007-02-14
- Volume
- 81
- Issue
- 4
- Pages
- 495-502
- ISSN
- 0009-9236 (ISSN-L)
- 1532-6535
- OpenAlex
- W2134431157
- Cited by
- 287
- References
- 39
- FWCI
- 8.75
- Type
- journal article
- Language
- en
- Open access
- closed
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
Are you an author, or do you see a problem with this page? Request a review
How to cite
Cite CoChat for the checks on this page, and the paper for its own findings.
- This page
- CoChat. (2026). Citation check: Naringin is a Major and Selective Clinical Inhibitor of Organic Anion-Transporting Polypeptide 1A2 (OATP1A2) in Grapefruit Juice. https://app.cochat.ai/papers/10.1038/sj.clpt.6100104
- The paper
- Bailey, D. G., Dresser, G. K., Leake, B. F., & Kim, R. B. (2007). Naringin is a Major and Selective Clinical Inhibitor of Organic Anion-Transporting Polypeptide 1A2 (OATP1A2) in Grapefruit Juice. Clinical Pharmacology & Therapeutics. https://doi.org/10.1038/sj.clpt.6100104
Data sources
Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
