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

Citation
K. Kobayashi et al., Effect of bile acids on the uptake of irinotecan and its active metabolite, SN-38, by intestinal cells, BBA-GEN SUB, 1525(1-2), 2001, pp. 125-129
Citations number
20
Categorie Soggetti
Biochemistry & Biophysics
Journal title
BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS
ISSN journal
03044165 → ACNP
Volume
1525
Issue
1-2
Year of publication
2001
Pages
125 - 129
Database
ISI
SICI code
0304-4165(20010216)1525:1-2<125:EOBAOT>2.0.ZU;2-5
Abstract
The intestinal transport of irinotecan (CPT-11) and its active metabolite, SN-38, has been previously reported (K. Kobayashi et al., Int. J. Cancer, 8 3 (1999) 491-496). In the present study, the effect of the two major primar y 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 ac idic intestinal pH conditions, micelle formation induced by 20 mM TCA signi ficantly reduced the cellular uptake of CPT-II and SN-38 by 60% and 80%, re spectively. (C) 2001 Elsevier Science B.V. All rights reserved.