Reversal of P-glycoprotein-Mediated Multidrug Resistance in Human Leukemia Cell Line K562/A02 by Archangelicin

AimTo investigate the reversal effect of archangelicin (Arc) on multidrug resistance (MDR) in the doxorubicin (Dox)-resistant leukemic cell line K562/A02.MethodsCytotoxicity was assayed by 3-(4, 5-dimethylthiazol-2-yl)-2, 5-di-phenyltetrazolium bromide method; the DOX and Rh123 concentration in cells and the expression of P-glycoprotein were assayed by flow cytometry. The influence of Arc on P-gp expression at mRNA levels was determined by using real-time RT-PCR.ResultsArc was endowed with remarkable MDR-reversing effect in K562/A02, and the maximal reversal fold (RF) was 7.36. The action of Arc was confirmed by the increase of intracellular accumulation of Dox in K562/A02 cells. The function of P-gp was blocked, and the expression of MDR1 mRNA and P-gp were inhibited by Arc.ConclusionArc reversed effectively MDR via inhibiting P-gp expression and function, and may be used as MDR reversal drugs to increase the effectiveness of chemotherapy.