Effect of bile acids on the uptake of irinotecan and its active metabolite, SN-38, by intestinal cells

被引：4

作者：

Kobayashi, K

Ceryak, S

Matsuzaki, Y

Kudoh, S

Bouscarel, B

机构：

[1] George Washington Univ, Med Ctr, Dept Med, Gastroenterol Res Lab, Washington, DC 20037 USA

[2] Nippon Med Sch, Dept Internal Med 4, Tokyo 113, Japan

[3] Saitama Canc Ctr, Dept Pulm Med, Ina, Saitama, Japan

[4] Univ Tsukuba, Div Gastroenterol, Ibaraki, Osaka, Japan

[5] George Washington Univ, Dept Biochem & Mol Biol, Washington, DC USA

来源：

BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS | 2001年 / 1525卷 / 1-2期

关键词：

irinotecan; 7-ethyl-10-hydroxycamptothecin; intestinal absorption; bile acid; taurocholic acid; micelle;

D O I：

10.1016/S0304-4165(00)00179-3

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：

The intestinal transport of irinotecan (CPT-11) and its active metabolite, SN-38, has been previously reported (K. Kobayashi et al., Int. J. Cancer, 83 (1999) 491-496). In the present study, the effect of the two major primary bile acids, cholic acid (CA) and taurocholic acid (TCA), on the uptake of CPT-11 and SN-38 by hamster intestinal epithelial cells was investigated. These two bile acids at concentrations up to 200 muM did not directly alter the cellular uptake of CPT-11 and SN-38. However, under physiologically acidic intestinal pH conditions, micelle formation induced by 20 mM TCA significantly reduced the cellular uptake of CPT-II and SN-38 by 60% and 80%, respectively. (C) 2001 Elsevier Science B.V. All rights reserved.

引用

页码：125 / 129

页数：5

共 20 条

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