Intestinal uptake of nateglinide by an intestinal fluorescein transporter

被引：17

作者：

Itagaki, S ^{[1
]}

Otsuka, Y ^{[1
]}

Kubo, S ^{[1
]}

Okumura, H ^{[1
]}

Saito, Y ^{[1
]}

Kobayashi, M ^{[1
]}

Hirano, T ^{[1
]}

Seki, K ^{[1
]}

机构：

[1] Hokkaido Univ, Grad Sch Pharmaceut Sci, Dept Clin Pharmaceut & Therapeut, Kita Ku, Sapporo, Hokkaido 0600812, Japan

来源：

BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES | 2005年 / 1668卷 / 02期

关键词：

nateglinide; intestine; monocarboxylate transporter; fluorescein; absorption; Caco-2;

D O I：

10.1016/j.bbamem.2004.12.005

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Nateglinide, a novel oral hypoglycemic agent, rapidly reaches its maximum serum concentration after oral administration, suggesting that it is rapidly absorbed in the intestine. However, nateglinide itself is not transported by MCT1 or PEPT1. The aim of this study was to characterize the transporters on the apical side of the small intestine that are responsible for the rapid absorption of nateglinide. It has been reported that the uptake of fluorescein by Caco-2 cells occurs via an H+-driven transporter and that the intestinal fluorescein transporter is probably not MCTI. We examined the contribution of the fluorescein transporter to the uptake of nateglinide by Caco-2 cells. Fluorescein competitively inhibited H+-dependent nateglinide uptake. All of fluorescein transporter inhibitors examined reduced the uptake of nateglinide. Furthermore, nateglinide inhibited fluorescein uptake. We conclude that the intestinal nateglinide/H+ cotransport system is identical to the intestinal fluorescein/H+ cotransport system. (C) 2004 Elsevier B.V All rights reserved.

引用

页码：190 / 194

页数：5

共 25 条

[11]

ITOH T, IN PRESS CANC CHEM P

[12] Transepithelial transport of fluorescein in caco-2 cell monolayers and use of such transport in in vitro evaluation of phenolic acid availability [J].