Fluorescein-methotrexate transport in brush border membrane vesicles from rat small intestine

被引：6

作者：

Li, TS ^{[1
]}

Tomimatsu, T ^{[1
]}

Ito, K ^{[1
]}

Horie, T ^{[1
]}

机构：

[1] Chiba Univ, Grad Sch Pharmaceut Sci, Dept Biopharmaceut, Inage Ku, Chiba 2638522, Japan

来源：

LIFE SCIENCES | 2003年 / 73卷 / 20期

关键词：

fluorescein-methotrexate; small intestine; membrane transport; methotrexate; brush border membrane vesicles;

D O I：

10.1016/S0024-3205(03)00616-7

中图分类号：

R-3 [医学研究方法]; R3 [基础医学];

学科分类号：

1001 ;

摘要：

The transport characteristics of fluorescein-methotrexate (F-MTX) in isolated brush border membrane vesicles (BBMVs) from rat small intestine were studied. F-MTX uptake in BBMVs was measured by a rapid filtration technique. Our results demonstrated that F-MTX uptake into vesicles was 1) significantly increased under the experimental conditions of an outwardly directed OH- gradient or an inwardly directed H+ gradient, 2) sensitive to temperature, 3) increased with decreasing pH of the incubation buffer, 4) significantly inhibited by 4,4'-diisothiocyanostilbene-2,2'-disulfonic acid (DIDS) at the early stage of the uptake, and 5) significantly inhibited by methotrexate (MTX). Thus, the transport of F-MTX in BBMVs was shown to be mediated in part by the reduced folate transporter (RFC) which was known to transport MTX through the epithelium of small intestine. (C) 2003 Elsevier Inc. All rights reserved

引用

页码：2631 / 2639

页数：9

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