Reversal of resistance to doxorubicin by CJZ3,a lomerizine amlodipine derivative,in doxorubicin-resistant human myelogenous leukemia(K562/DOX) cells
- VernacularTitle:洛美利嗪衍生物CJZ3对K562/DOX细胞阿霉素耐药的逆转作用
- Author:
Biansheng JI
;
Shumei YUE
;
Ling HE
- Publication Type:Journal Article
- Keywords:
CJZ3;
P-glycoprotein;
multidrug resistance;
doxorubicin;
reversal
- From:
Chinese Pharmacological Bulletin
2003;0(11):-
- CountryChina
- Language:Chinese
-
Abstract:
Aim To investigate the reversal of resistance to doxorubicin by CJZ3,a lomerizine derivative,in doxorubicin-resistant human myelogenous leukemia(K562/DOX)cells.Methods The effect of CJZ3 on P-glycoprotein(P-gp)function and resistance to doxorubicin in K562/DOX cells were observed by using flow cytometry and MTT assay.Results CJZ3 increased intracellular uptake and accumulation of rhodamine123(Rh123)in K562/DOX cells in a concentration-related manner,significantly inhibited the efflux of Rh123 from the cells,and increased the doxorubicin-induced cytotoxicity,apoptosis rate,Caspase-3 activity in doxorubicin-treated cells and the intracellular accumulation of doxorubicin.Conclusions The reversed effect of CJZ3 on resistance to doxorubicin in K562/DOX cells was associated with its inhibitory effect on P-gp function in vitro.
