論文 - 詳細
| RRC ID | 44468 |
|---|---|
| 著者 | Kamishikiryo J, Matsumura R, Takamori T, Sugihara N. |
| タイトル | Effect of quercetin on the transport of N-acetyl 5-aminosalicylic acid. |
| ジャーナル | J Pharm Pharmacol |
| Abstract |
OBJECTIVES:The aim of this study was to investigate the transporter-mediated transport of N-acetyl 5-aminosalicylic acid (Ac-5-ASA) and the effect of quercetin on Ac-5-ASA transport. METHODS:Caco-2 cell monolayers grown in Transwells were used to study the transport of Ac-5-ASA in the absence or presence of quercetin, and apical-to-basolateral and basolateral-to-apical apparent permeability (PappAB and PappBA values, respectively) was determined. The effect of transporter inhibitors, such as MK571, quinidine and mitoxantrone, on the transport of Ac-5-ASA was investigated. KEY FINDINGS:In the absence of transporter mediators, the transport of Ac-5-ASA was much higher in the basolateral-to-apical direction than in the opposite direction. The PappBA/PappAB ratio of Ac-5-ASA was 4.89. Quercetin inhibited the apical efflux of Ac-5-ASA and decreased the PappBA/PappAB ratio to 1.05. Of the transporter inhibitors, MK571 decreased the PappBA/PappAB ratio to 1.07; however, neither quinidine nor mitoxantrone had an effect on Ac-5-ASA transport. CONCLUSIONS:Ac-5-ASA was excreted by multidrug resistance-associated protein 2 from Caco-2 cells, and its transport was inhibited by quercetin. Our findings suggest that dose levels of sulfasalazine or 5-aminosalicylic acid can be decreased by coadministration of quercetin, leading to improved pharmaceutical care for inflammatory bowel diseases. |
| 巻・号 | 65(7) |
| ページ | 1037-43 |
| 公開日 | 2013-7-1 |
| DOI | 10.1111/jphp.12062 |
| PMID | 23738731 |
| MeSH | Aminosalicylic Acids / pharmacokinetics* Biological Transport Caco-2 Cells Drug Interactions Humans Mitoxantrone / pharmacology Multidrug Resistance-Associated Protein 2 Multidrug Resistance-Associated Proteins / metabolism* Propionates / pharmacology Quercetin / pharmacology* Quinidine / pharmacology Quinolines / pharmacology |
| IF | 2.571 |
| 引用数 | 4 |
| WOS 分野 | PHARMACOLOGY & PHARMACY |
| リソース情報 | |
| ヒト・動物細胞 | CACO-2(RCB0988) |