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

Document Type

Journal Article

Publication Date

2-16-2001

Journal

Biochimica et Biophysica Acta - General Subjects

Volume

1525

Issue

1-2

DOI

10.1016/S0304-4165(00)00179-3

Keywords

7-Ethyl-10-hydroxycamptothecin; Bile acid; Intestinal absorption; Irinotecan; Micelle; Taurocholic acid

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, 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 μM 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-11 and SN-38 by 60% and 80%, respectively. © 2001 Elsevier Science B.V.

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