Catalogo Articoli (Spogli Riviste)

OPAC HELP

Titolo:
CELLULAR UPTAKE, CYTOTOXICITY, AND TRANSPORT KINETICS OF ANTHRACYCLINES IN HUMAN SENSITIVE AND MULTIDRUG-RESISTANT K562 CELLS
Autore:
PRAET M; STRYCKMANS P; RUYSSCHAERT JM;
Indirizzi:
FREE UNIV BRUSSELS,LAB CHIM PHYS MACROMOL INTERFACES,CP 206-2,BLVD TRIOMPHE B-1050 BRUSSELS BELGIUM INST JULES BORDET,DEPT HEMATOL B-1000 BRUSSELS BELGIUM
Titolo Testata:
Biochemical pharmacology
fascicolo: 10, volume: 51, anno: 1996,
pagine: 1341 - 1348
SICI:
0006-2952(1996)51:10<1341:CUCATK>2.0.ZU;2-M
Fonte:
ISI
Lingua:
ENG
Soggetto:
P-GLYCOPROTEIN; DRUG-RESISTANCE; CYCLOSPORINE-A; FLOW-CYTOMETRY; LEUKEMIA-CELLS; VERAPAMIL; ADRIAMYCIN; LINES; MODULATION; EFFLUX;
Keywords:
ANTHRACYCLINES; MULTIDRUG RESISTANCE; P-GLYCOPROTEIN; TRANSPORT KINETICS; K562 CELLS; FLOW CYTOMETRY;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
28
Recensione:
Indirizzi per estratti:
Citazione:
M. Praet et al., "CELLULAR UPTAKE, CYTOTOXICITY, AND TRANSPORT KINETICS OF ANTHRACYCLINES IN HUMAN SENSITIVE AND MULTIDRUG-RESISTANT K562 CELLS", Biochemical pharmacology, 51(10), 1996, pp. 1341-1348

Abstract

Multidrug resistance in tumor cells is often associated with the presence of an similar to 170 kDa plasma membrane glycoprotein (Pgp) that acts as a drug-efflux pump and decreases intracellular antitumor drug concentration. We measured the uptake of seven anthracyclines (daunorubicin, doxorubicin, 4'-epi-doxorubicin, 4'-deoxy-doxorubicin, iododoxorubicin, 3'-(3-methoxymorpholino)-doxorubicin (FCE23762) and 4-demethoxy-daunorubicin) into K562 cells sensitive and resistant (K562/DNR) todaunorubicin. The K562/DNR subline expresses Pgp at the membrane surface, whereas its sensitive counterpart does not. Laser flow cytometry was used to quantitate intracellular anthracycline content. Uptake of daunorubicin, doxorubicin, 4'-epi-doxorubicin, and 4'-deoxy-doxorubicin was minimal in the K562/DNR subline as compared to their uptake in sensitive cells. On the contrary, iododoxorubicin, FCE23762, and 4-demethoxy-daunorubicin accumulate to nearly the same extent into sensitiveand resistant K562 cells. Growth inhibition data indicated chat the resistance factor for iododoxorubicin, FCE23762, and 4-demethoxy-daunorubicin is markedly decreased as compared to the other drugs. Fluorescence measurements were carried out to determine the kinetic parameters associated with the influx and efflux of the drugs into and out of K562 cells. Kinetic data indicated that iododoxorubicin, FCE23762, and 4-demethoxy-daunorubicin are not actively rejected from resistant cells,suggesting that they are poor substrates for Pgp-mediated transport. This observation is related to their ability to overcome the multidrug-resistant phenotype of K562/DNR cells in vitro.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 17/01/21 alle ore 18:14:37