title: Transepithelial transport of rosuvastatin and effect of ursolic acid on its transport in Caco-2 monolayers.
abstract: The aim of this study was to determine transepithelial transport characteristics of rosuvastatin and effect of ursolic acid (P-gp potential inhibitor) and ko143 (ABC transporters selective inhibitor) on its transport in Caco-2 monolayers. A reliable Caco-2 cell monolayers model was established. The TEER value was used to inspect integrity of cell model. Apparent permeability coefficients (Papp(BL-AP) and Papp(AP-BL)) were used to analyze transepithelial transport of rosuvastatin. Uptake of rosuvastatin was time- and concentration-dependent in Caco-2 cell. The ko143 but not ursolic acid had effect on the uptake of rosuvastatin in Caco-2 cell monolayer model and affected apparent permeability coefficient and apparent permeability of rosuvastatin. Active transport and passive diffusion absorption existed in transepithelial transport of rosuvastatin in Caco-2 cell model. Ursolic acid had no effect on transport of rosuvastatin in Caco-2 cell monolayer. The result indicated that ursolic acid may not cause effect on intestinal absorption of rosuvastatin.
authors.affiliation: Department of Pharmacy, The First Affiliated Hospital of Nanchang University, China.
authors.forename: Wen Jin
authors.initials: WJ
authors.lastname: Hua
authors.forename: Hu Jin
authors.initials: HJ
authors.lastname: Fang
authors.forename: Wei Xiao
authors.initials: WX
authors.lastname: Hua
mesh_terms: D000070997:ATP Binding Cassette Transporter, Subfamily G, Member 2; D018528:ATP-Binding Cassette Transporters / Q000502:physiology; D001692:Biological Transport / Q000187:drug effects; D018938:Caco-2 Cells; D005464:Fluorobenzenes / Q000493:pharmacokinetics*; D006801:Humans; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors / Q000493:pharmacokinetics*; D009363:Neoplasm Proteins / Q000502:physiology; D011743:Pyrimidines / Q000493:pharmacokinetics*; D000068718:Rosuvastatin Calcium; D013449:Sulfonamides / Q000493:pharmacokinetics*; D014315:Triterpenes / Q000494:pharmacology*; D000097245:Ursolic Acid
chemical_list: D000070997:ATP Binding Cassette Transporter, Subfamily G, Member 2; D018528:ATP-Binding Cassette Transporters; D005464:Fluorobenzenes; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D009363:Neoplasm Proteins; D011743:Pyrimidines; D000068718:Rosuvastatin Calcium; D013449:Sulfonamides; D014315:Triterpenes; D000097245:Ursolic Acid; C116614:ABCG2 protein, human