NDLI: Effect of quercetin on the transport of N-acetyl 5-aminosalicylic acid.

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Effect of quercetin on the transport of N-acetyl 5-aminosalicylic acid.

Content Provider	World Health Organization (WHO)-Global Index Medicus
Author	Kamishikiryo, Jun Matsumura, Ryusuke Takamori, Tomohiro Sugihara, Narumi
Description	Country affiliation: Japan Author Affiliation: Kamishikiryo J ( Faculty of Pharmacy and Pharmaceutical Sciences, Fukuyama University, Fukuyama, Hiroshima, Japan.)
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.
File Format	HTM / HTML
ISSN	00223573
Issue Number	7
Volume Number	65
e-ISSN	20427158
Journal	Journal of Pharmacy and Pharmacology
Language	English
Publisher	Wiley
Publisher Date	2013-07-01
Publisher Place	Great Britain (UK)
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Discipline Pharmacology Aminosalicylic Acids Pharmacokinetics Multidrug Resistance-associated Proteins Metabolism Quercetin Pharmacology Biological Transport Caco-2 Cells Drug Interactions Humans Mitoxantrone Propionates Quinidine Quinolines Journal Article
Content Type	Text
Resource Type	Article
Subject	Pharmacology Pharmaceutical Science

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