CHARACTERIZATION AND APPLICATION OF A VINBLASTINE-SELECTED CACO-2 CELL LINE FOR EVALUATION OF P-GLYCOPROTEIN

Autor: Jack O. Houchins, Susan E. Pratt, D. A. Laska, Xialong Xia, Brenda R. Hanssen, Jeffery Horn, Terry D. Lindstrom, Anne H. Dantzig, Daniel C. Williams
Rok vydání: 2002
Předmět:
Zdroj: In Vitro Cellular & Developmental Biology - Animal. 38:401
ISSN: 1543-706X
DOI: 10.1290/1071-2690(2002)038<0401:caaoav>2.0.co;2
Popis: The role of the adenosine triphosphate–binding cassette (ABC) superfamily of membrane transporters is well documented in tumor cell multidrug resistance. More recently, growing evidence of their influence on oral bioavailability, drug excretion rates, and drug–drug interaction potential at the intestinal level has stimulated much investigation. Our laboratory is interested in evaluating the apical (AP) ABC transporter P-glycoprotein (Pgp [mdr-1]) for its role in xenobiotic efflux at the intestinal level. We propagated Caco-2 cells in the presence of vinblastine (a cytotoxic, Pgp substrate) to promote transporter expression though selection. That is, the cell population expressing Pgp, or with the capacity to up-regulate Pgp expression, survived and expanded in the presence of vinblastine. We have used this selected cell line (Caco-2 VinB) to develop a fluorescent-based assay to study the chemical modulators of Pgp activity. Using the Caco-2 VinB cells, we have successfully demonstrated the differ...
Databáze: OpenAIRE