Objective To compare the anti-tumor activity of cantharadin and the bound cantharidin extacted from meloids Mylabris cichorii on various human tumor cell lines in vitro.Methods WST-1 colorimetry was used to evaluate the inhibitory effect of cantharadin and the bound cantharidin on HT-29 cells,PLC/PRF/5 cells and BEL-7404 cells.Results Cantharidin displayed unstable inhibitory effect on the growth of HT-29 cells,while their inhibitory effect on the growth of PLC/PRF/5 cells and BEL-7404 cells was in a dose-dependent manner,but with a little activity under the high concentration.The bound cantharidin was able to effectively inhibit the proliferation of three kinds of the tumor cells with the IC50 value of 28.51 μmol/L,86.77 μmol/L and 21.27 μmol/L,respectively,in a dose-dependent manner.Conclusion The bound cantharidin showed more effective inhibitory effect on HT-29 cells,PLC/PRF/5 cells and BEL-7404 cells compared with cantharidin.The results of assay suggested that roles of the bound cantharidin could be more significantly contributed to anti-tumor than the roles of cantharidin.