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Titolo:
Increase in doxorubicin cytotoxicity by inhibition of P-glycoprotein activity with lomerizine
Autore:
Shiraki, N; Hamada, A; Ohmura, T; Tokunaga, J; Oyama, N; Nakano, M;
Indirizzi:
Kumamoto Univ Hosp, Dept Pharm, Kumamoto 8608556, Japan Kumamoto Univ Hosp Kumamoto Japan 8608556 Pharm, Kumamoto 8608556, Japan
Titolo Testata:
BIOLOGICAL & PHARMACEUTICAL BULLETIN
fascicolo: 5, volume: 24, anno: 2001,
pagine: 555 - 557
SICI:
0918-6158(200105)24:5<555:IIDCBI>2.0.ZU;2-L
Fonte:
ISI
Lingua:
ENG
Soggetto:
MULTIDRUG-RESISTANCE; CALCIUM ANTAGONISM; CELLS; EXPRESSION; REVERSAL; DRUGS; VERAPAMIL; CANCER; AGENTS; LEVEL;
Keywords:
lomcrizine; doxorubicin; P-glycoprotein; multidrug resistance;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
26
Recensione:
Indirizzi per estratti:
Indirizzo: Nakano, M Kumamoto Univ Hosp, Dept Pharm, 1-1-1 Honjo, Kumamoto 8608556, Japan Kumamoto Univ Hosp 1-1-1 Honjo Kumamoto Japan 8608556 56, Japan
Citazione:
N. Shiraki et al., "Increase in doxorubicin cytotoxicity by inhibition of P-glycoprotein activity with lomerizine", BIOL PHAR B, 24(5), 2001, pp. 555-557

Abstract

Acquired resistance to chemotherapy is a major problem during cancer treatment. One mechanism for drug resistance is overexpression of the MDR (multidrug resistance)l gene encoding the transmembrane efflux pump, P-glycoprotein (P-gp), Calcium channel blockers such as verapamil, nifedipine and nicardipine have been shown to reverse cellular drug resistance by inhibiting P-gp drug efflux. This study evaluated whether a new calcium channel blocker,lomerizine, influenced doxorubicin (Dox) cytotoxicity and P-gp activity ina P-Kp-expressing cell line compared to a non-expressing subline. Verapamil, and even more markedly; lomerizine, increased cellular uptake of calceintransported by P-gp in a P-gp-expressing erythroleukemia cell line, K562-Dos. Ten muM of lomerizine reduced the IC50 of doxorubicin in the K562-Dox from 60000 ng/ml to 800 ng/ml, whereas the IC50 of doxorubicin in the K562 subline was only marginally affected by these drugs. Lomerizine showed greater reduction in P-gp efflux than verapamil at an equimolar concentration, These results suggest that lomerizine has the clinical potential to reverse tumor MDR involving the efflux protein P-gp.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 15/07/20 alle ore 14:54:32