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Titolo:
Reversal of acquired resistance to doxorubicin in K562 human leukemia cells by astemizole
Autore:
Ishikawa, M; Fujita, R; Takayanagi, M; Takayanagi, Y; Sasaki, K;
Indirizzi:
Tohoku Pharmaceut Univ, Canc Res Inst, Dept Pharmacol & Toxicol, Aoba Ku, Sendai, Miyagi 9818558, Japan Tohoku Pharmaceut Univ Sendai Miyagi Japan 9818558 Miyagi 9818558, Japan
Titolo Testata:
BIOLOGICAL & PHARMACEUTICAL BULLETIN
fascicolo: 1, volume: 23, anno: 2000,
pagine: 112 - 115
SICI:
0918-6158(200001)23:1<112:ROARTD>2.0.ZU;2-P
Fonte:
ISI
Lingua:
ENG
Soggetto:
MULTIDRUG RESISTANCE; P-GLYCOPROTEIN; DRUG-RESISTANCE; MEMBRANE-VESICLES; CANCER-CELLS; VINBLASTINE; CYTOCHROME-P450-3A; VERAPAMIL;
Keywords:
astemizole; doxorubicin; multidrug-resistance; human leukemia cell (K562);
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
25
Recensione:
Indirizzi per estratti:
Indirizzo: Ishikawa, M Tohoku Pharmaceut Univ, Canc Res Inst, Dept Pharmacol & Toxicol, Aoba Ku, 4-4-1 Komatsushima, Sendai, Miyagi 9818558, Japan Tohoku Pharmaceut Univ 4-4-1 Komatsushima Sendai Miyagi Japan 9818558
Citazione:
M. Ishikawa et al., "Reversal of acquired resistance to doxorubicin in K562 human leukemia cells by astemizole", BIOL PHAR B, 23(1), 2000, pp. 112-115

Abstract

This study demonstrates that astemizole, a non-sedating anti-histaminergicdrug with low toxicity in vivo, greatly potentiates the growth-inhibitory activity of doxorubicin in doxorubicin-resistant human leukemia cells (K562/DXR). Astemizole synergistically potentiated the cytotoxicity of doxorubicin for K562/DXR cells at a concentration of 0.1-3 mu M in a dose-dependent manner, whereas they showed hardly any synthergistic effect in the parentalcell line (K562) at the same concentration. Since doxorubicin resistance in these cells is associated with the expression of high levels of P-glycoprotein, we evaluated the effect of astemizole on P-glycoprotein activity in cytofluorographic efflux experiments with doxorubicin. Our results indicatethat astemizole inhibits the P-glycoprotein pump-efflux activity in a dose-related manner. Moreover, it also inhibits the photolabeling of P-glycoprotein by [H-3]azidopine in a dose-dependent manner. These findings provide abiological basis for the potential therapeutic application of astemizole as an anticancer drug either alone or in combination with doxorubicin to multidrug-resistant leukemic cells.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 21/09/18 alle ore 07:36:59