Objective To investigate the effects and mechanisms of magnesium canthardin on growth, apoptosis and invasion of human astroglioma cell U251MG. Methods Human astroglioma cells U251MG were cultured in vitro. They were divided into blank group (Control), lowdose magnesium cantharidin group (Canthardin 5 μM), mediumdose magnesium cantharidin group (Canthardin 10 μM) and highdose magnesium cantharidin group (Canthardin 10μM). Cell proliferation was detected by colony formation assay. Apoptosis was detected by Hocest staining. Cell invasion was detected by Transwell method. The expression of related proteins were detected by Western blot. Results The results of plate cloning experiments showed that magnesium cantharidin could significantly inhibit proliferation of human astroglioma cell U251MG, showing dosedependence (P＜0.05). Hocest staining results showed magnesium cantharidin could significantly promote apoptosis of human astroglioma cells, showing dosedependence (P＜0.05). Transwell chamber experiments showed that magnesium cantharidin could significantly inhibit cell invasion, showing dosedependence (P＜0.05). The test results of Western blot showed expression of PCNA protein, VEGF protein, Bax protein and pAKT protein in human astroglioma cells were significantly decreased after processed by magnesium cantharidin (P＜0.05), while expression of Caspase3 protein and Bcl2 protein were significantly increased (P＜0.05). There was no significant difference in expression of total AKT protein (P＞0.05).〖WTHZ〗Conclusion Magnesium cantharidin can inhibit proliferation and invasion of human astroglioma cell U-251MG and promote its apoptosis by regulating Akt signaling pathway, showing dosedependence in certain concentration range.