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Effect of proinflammatory cytokine IL-6 on efflux transport of rebamipide in Caco-2 cells
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy. Otsuka Pharmaceut Co Ltd, Formulat Res Inst, Bioavailabil Res Project, Tokushima, Japan..
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy.
2017 (English)In: Xenobiotica, ISSN 0049-8254, E-ISSN 1366-5928, Vol. 47, no 9, 821-824 p.Article in journal (Refereed) Published
Abstract [en]

1. Effect of IL-6, a pro-inflammatory cytokine, on efflux transport of rebamipide, an antiulcer drug, was investigated in Caco-2 cells. 2. Rebamipide had a greater basal-to-apical than apical-to-basal transport rate. Efflux transport of rebamipide was inhibited by cyclosporine A, a P-gp inhibitor, and probenecid, which is a general MRP inhibitor, but not by Ko143, a BCRP inhibitor. 3. By the addition of IL-6, mannitol transport was slightly increased in a concentration-dependent manner in both directions of absorption and efflux. The addition of IL-6 did not change efflux transport of rebamipide even though efflux transport of digoxin, a typical substrate of P-gp, was significantly decreased by the addition of IL-6, indicating decrease of the function of P-gp. 4. Therefore, it was suggested that increase of MRP(s)-mediated transport compensates for the decrease of P-gp mediated transport of rebamipide. These findings suggested that rebamipide absorption is unlikely to be changed in IBD patients.

Place, publisher, year, edition, pages
Taylor & Francis, 2017. Vol. 47, no 9, 821-824 p.
Keyword [en]
Caco-2 cells, efflux transporters, intestinal drug absorption, IL-6, permeability, rebamipide
National Category
Pharmacology and Toxicology
Identifiers
URN: urn:nbn:se:uu:diva-330086DOI: 10.1080/00498254.2016.1229085ISI: 000404681300010PubMedID: 27557477OAI: oai:DiVA.org:uu-330086DiVA: diva2:1148042
Available from: 2017-10-09 Created: 2017-10-09 Last updated: 2017-10-09Bibliographically approved

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