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Updated: Aug 20, 2026

Using Caco-2 Cells to Study Lipid Transport by the Intestine
Published on: August 20, 2015
Uptake of irinotecan metabolite SN-38 by the human intestinal cell line Caco-2
Tatsuya Itoh1, Shirou Itagaki, Yoshinobu Sumi
1Department of Pharmacy, Sapporo Social Insurance General Hospital, Chuo 2-jo, 6-chome, Atsubetsu-ku, Sapporo 004-8618, Japan.
Purpose:
The aim of this study was to investigate the transport mechanisms of transporters that contribute to the intestinal uptake of 7-ethyl-10-hydroxycamptothecin (SN-38).
Methods:
Human intestinal epithelial Caco-2 cells were used to investigate the mechanistic basis of transepithelial uptake of SN-38. We investigated the characteristics of SN-38 uptake into Caco-2 cells. The effects of baicalin and sulfobromophthalein (BSP) on the uptake of SN-38 by Caco-2 cells were examined.
Results:
Uptake of SN-38 was significantly reduced at 4 degrees C. Baicalin inhibited the uptake of SN-38 in a concentration-dependent manner. BSP significantly reduced the uptake of SN-38. However, probenecid, pravastatin and grepafloxacin did not affect the uptake of SN-38.
Conclusions:
The results suggest that a specific transport system mediates the uptake of SN-38 across the apical membrane in Caco-2 cells.
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