Effect of bile acids on the uptake of irinotecan and its active metabolite, SN-38, by intestinal cells
Biochimica et Biophysica Acta - General Subjects
7-Ethyl-10-hydroxycamptothecin; Bile acid; Intestinal absorption; Irinotecan; Micelle; Taurocholic acid
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.
Kobayashi, K., Ceryak, S., Matsuzaki, Y., Shoji, K., & Bouscarel, B. (2001). Effect of bile acids on the uptake of irinotecan and its active metabolite, SN-38, by intestinal cells. Biochimica et Biophysica Acta - General Subjects, 1525 (1-2). http://dx.doi.org/10.1016/S0304-4165(00)00179-3