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Objective: To discuss whether the self-developed magnesium cantharidate possesses better anti-proliferation activity in Hep-2 cells linethan Sodium Cantharidate. Methods: The sulforhodamie B(SRB) assay and cell colony forming tests were employed to detect the influence of Magnesium Cantharidate and Sodium Cantharidateon Hep-2 cells. Results: Compared with Sodium Cantharidate,Magnesium Cantharidate has higher inhibitory effects on the proliferation of Hep-2 cells. The IC50 of Magnesium Cantharidate and the Sodium Cantharidate was 2.19, 15.75 μmol·L-1, respectively. Cell clone forming experiments suggested that the cell colony was difficult to form when the concentration of Magnesium Cantharidate and the Sodium Cantharidate were 1.75 and 3.50 μmol·L-1. Conclusion:Magnesium Cantharidate may have higher inhibitory effects on proliferation of Hep-2 cell than Sodium Cantharidate and has the development potential in suppressing cancer. [ABSTRACT FROM AUTHOR]