Catalogo Articoli (Spogli Riviste)

OPAC HELP

Titolo:
Reversal of vinblastine resistance in human leukemic cells by haloperidol and dihydrohaloperidol
Autore:
Kataoka, Y; Ishikawa, M; Miura, M; Takeshita, M; Fujita, R; Furusawa, S; Takayanagi, M; Takayanagi, Y; Sasaki, K;
Indirizzi:
Tohoku Pharmaceut Univ, Dept Pharmacol & Pharm, Sendai, Miyagi 9818558, Japan Tohoku Pharmaceut Univ Sendai Miyagi Japan 9818558 Miyagi 9818558, Japan Tohoku Pharmaceut Univ, Dept Pharmacol & Toxicol, Inst Canc Res, Sendai, Miyagi 9818558, Japan Tohoku Pharmaceut Univ Sendai Miyagi Japan 9818558 Miyagi 9818558, Japan
Titolo Testata:
BIOLOGICAL & PHARMACEUTICAL BULLETIN
fascicolo: 6, volume: 24, anno: 2001,
pagine: 612 - 617
SICI:
0918-6158(200106)24:6<612:ROVRIH>2.0.ZU;2-B
Fonte:
ISI
Lingua:
ENG
Soggetto:
CALCIUM-CHANNEL BLOCKERS; HUMAN CANCER-CELLS; MULTIDRUG-RESISTANCE; P-GLYCOPROTEIN; TUMOR-CELLS; ADRIAMYCIN-RESISTANT; MEMBRANE-VESICLES; SELECTIVE BINDING; PLASMA-MEMBRANE; P388 LEUKEMIA;
Keywords:
K562 cell; haloperidol; dihydrohaloperidol; vinblastine; multidrug resistance;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
35
Recensione:
Indirizzi per estratti:
Indirizzo: Ishikawa, M Tohoku Pharmaceut Univ, Dept Pharmacol & Pharm, 4-4-1 Komatsushima, Sendai, Miyagi 9818558, Japan Tohoku Pharmaceut Univ 4-4-1 Komatsushima Sendai Miyagi Japan 9818558
Citazione:
Y. Kataoka et al., "Reversal of vinblastine resistance in human leukemic cells by haloperidol and dihydrohaloperidol", BIOL PHAR B, 24(6), 2001, pp. 612-617

Abstract

Haloperidol, an antipsychotic, was investigated in cells overexpressing P-glycoprotein to determine whether it was a clinically effective drug to reverse for reversing multidrug resistance (MDR) mediated by P-glycoprotein. Anontoxic concentration of haloperidol (1-30 mum) enhanced the cytotoxic effects of vinblastine (VBL) concentration-dependently in VBL-resistant humanleukemia (K562/VBL) cells, but had no effect in the parent cells. Haloperidol also enhanced the cytotoxicities of epirubicin, doxorubicin and actinomycin D in the K562/VBL cells, but not those of idarubicin or cisplatin; this enhancement was less than that of the VBL, toxicity in the VBL-resistant tumor line. Haloperidol increased the intracellular accumulation of VBI. inthe K562/VBL, cells, and the binding of [H-3]-azidopine to the cell-surface protein, P-glycoprotein, was inhibited by haloperidol in a concentration-dependent manner. Haloperidol was less potent than verapamil. Thus, haloperidol appeared to potentiate anticancer agents through the reversal of MDR by competitively inhibiting drug-binding to P-glycoprotein. In contrast, themain metabolite of haloperidol, dihydrohaloperidol, without antipsychotic activity had less of an effect, Therefore, haloperidol might be useful in reversing drug-resistance.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 25/01/20 alle ore 07:26:49