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This study was purposed to investigate the multidrug resistance reversal effect of Gambogic Acid in K562/AO2 cells and its mechanism.The IC50 of ADM was evaluated by MTT.Cell apoptosis was detected by flow cytometry.Morphological changes of K562/A02 cells stained by DAPI under fluorescence microscope.The expressions of Survivin and P-gp were determined by Western blot.The results showed that the ICS0 of ADM in K562 and K562/AO2 cells were 1.42 ± 0.07μg/ml and 28.42±1.40μg/ml respectively.If the concentration of GA was less than 0.0625μmol/L, the inhibitory effect on proliferation of K562 and K562/A02 cells was not observed.0.06251μmol/L GA could enhance the sensitivity of K562/A02 cells to ADM (p < 0.05) and the reversal multiples was 1.53.The apoptotic rate was raised after treating with ADM combined with 0.0625μmol /L GA for 48 hours (p<0.05).