Objective To investigate the reversal mechanism of Tetredrine(TTD) on multidrug resistance in leukemia cell line K562/ADM.Methods Using flow cytometry(FCM) assay,the intracellular ADM concentration and the expression of P-glycoprotein(P-gp) were examined.The mRNA expressions of multidrug resistance(MDR) was measured by fluorescent quantitative reverse transcriptase polymerase chain reaction(RT-PCR).Apoptotic changes were observed by Anexin-V.Results 10 μmol/L TTD significantly increased the intracellular concentration of ADM and reduced the expression of MDR1 mRNA/P-gp in K562/ADM cells.TTD can effectively enhanced the effect of ADM on apoptosis of K562/ADM cells.Conclusion The reversal mechanism of multidrug resistance in K562/ADM takes place through different ways,such as down-regulating mRNA and protein expression levels of MDR1,increasing intracellular drug concentration,and raising the number of apoptosis cells.