論文 - 詳細
| RRC ID | 51732 |
|---|---|
| 著者 | Kimura O, Fujii Y, Haraguchi K, Ohta C, Koga N, Kato Y, Endo T. |
| タイトル | Effect of quercetin on the uptake and efflux of aristolochic acid I from Caco-2 cell monolayers. |
| ジャーナル | J Pharm Pharmacol |
| Abstract |
OBJECTIVE:The purpose of this study was to determine whether quercetin decreases the uptake of aristolochic acid I (AAI) from the apical membranes of Caco-2 cells via H(+) -linked MCTs at neutral pH as well as to confirm the secretion of AAI through the Caco-2 cell monolayers via ABC transporters. METHODS:Caco-2 cells cultured on the dishes or permeable membranes were incubated with AAI in the absence or presence of quercetin or transporter inhibitors. KEY FINDINGS:Coincubation with quercetin decreased the uptake of AAI by Caco-2 cells cultured on the dishes at pH 7.4, and a similar decrease in AAI uptake was found when the cells were coincubated with acetic acid or benzoic acid. In contrast, the basolateral-to-apical transport of AAI was higher than the apical-to-basolateral transport of AAI at pH 7.4, and the former transport was decreased by quercetin and the BCRP inhibitors of Ko-143 and mitoxantrone, but not by P-gp or MRP2 inhibitors. CONCLUSIONS:AAI appears to be secreted from the apical membranes of Caco-2 cells via BCRP at neutral pH, although a small amount of AAI is taken up from the apical membranes via H(+) -linked MCTs, and quercetin may decrease both the BCRP-mediated efflux and the MCT-mediated influx of AAI. |
| 巻・号 | 68(7) |
| ページ | 883-9 |
| 公開日 | 2016-7-1 |
| DOI | 10.1111/jphp.12557 |
| PMID | 27166429 |
| MeSH | ATP-Binding Cassette Transporters / antagonists & inhibitors Acetic Acid / pharmacology Aristolochic Acids / pharmacokinetics* Benzoic Acid / pharmacology Biological Transport / drug effects* Caco-2 Cells Cells, Cultured Cyclosporine / pharmacology Diketopiperazines / pharmacology Heterocyclic Compounds, 4 or More Rings / pharmacology Humans Hydrogen-Ion Concentration Indomethacin / pharmacology Intestinal Absorption / drug effects* Mitoxantrone / pharmacology Pravastatin / pharmacology Propionates / pharmacology Quercetin / pharmacology* Quinidine / pharmacology Quinolines / pharmacology |
| IF | 2.309 |
| 引用数 | 4 |
| リソース情報 | |
| ヒト・動物細胞 | CACO-2(RCB0988) |