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...

Full description

Saved in:
Bibliographic Details
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
Subjects
Antineoplastic agents
Antineoplastic Agents, Phytogenic - pharmacokinetics
Biological and medical sciences
Biological Transport - drug effects
Caco-2 Cells
Camptothecin - analogs & derivatives
Camptothecin - pharmacokinetics
Coloring Agents - pharmacology
Enzyme Inhibitors - pharmacology
Flavonoids - pharmacology
Humans
Intestines - drug effects
Intestines - metabolism
Medical sciences
Pharmacology. Drug treatments
Sulfobromophthalein - pharmacology
Tumor Cells, Cultured - drug effects
Tumor Cells, Cultured - metabolism
Antineoplastic agent
Human
Caco-2 cells
Digestive system
Enzyme
Metabolite
DNA topoisomerase
Enzyme inhibitor
Diarrhea
Irinotecan
Isomerases
Digestive diseases
Intestinal disease
Baicalin
Online AccessGet full text

Cover

More Information
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.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
ISSN:0344-5704
1432-0843
DOI:10.1007/s00280-004-0937-4