Uptake of irinotecan metabolite SN-38 by the human intestinal cell line Caco-2

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). Human intestinal epithelial Caco-2 cells were used to investigate the mechanistic basis of transepithelial uptake of SN-38. We investi...

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Published inCancer chemotherapy and pharmacology Vol. 55; no. 5; pp. 420 - 424
Main Authors ITOH, Tatsuya, ITAGAKI, Shirou, SUMI, Yoshinobu, HIRANO, Takeshi, TAKEMOTO, Isao, ISEKI, Ken
Format Journal Article
LanguageEnglish
Published Berlin Springer 01.05.2005
Springer Nature B.V
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Summary: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). 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. 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. 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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ISSN:0344-5704
1432-0843
DOI:10.1007/s00280-004-0937-4