Itoh Tatsuya, Itagaki Shirou, Sumi Yoshinobu, Hirano Takeshi, Takemoto Isao, Iseki Ken
Department of Pharmacy, Sapporo Social Insurance General Hospital, Chuo 2-jo, 6-chome, Atsubetsu-ku, Sapporo 004-8618, Japan.
Cancer Chemother Pharmacol. 2005 May;55(5):420-4. doi: 10.1007/s00280-004-0937-4. Epub 2004 Nov 23.
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.
