Background Despite the advances in the diagnosis and treatment of colon cancer, the disease remains a major threat worldwide. Ligustrazine (LSZ) is an alkaloid with anti-tumor activity. This study aimed to elucidate the anti-tumor qualities of LSZ on colon cancer cells in vitro and vivo , as well as its involved mechanism. Methods In this study, CCK-8, colony formation, transwell invasion assay and flow cytometry were employed to examined the cells behaviors. Moreover, the proteins related to the epithelial mesenchymal transformation (EMT) process were determined by RT-qPCR and western blotting. Then, the expression of PI3K, AKT, and mTOR were tested by western blotting. Furthermore, a xenograft mouse model was used to investigate the role of LSZ in vivo . Results LSZ treatment (0.1, 0.5 and 1.5 mM) significantly inhibited SW480 cells’ efforts to proliferate, migrate and invade and also induced SW480 cell apoptosis. In addition, LSZ inhibited EMT process. Meanwhile, Western blotting indicated that LSZ treatment administered on a dose-dependent basis inhibited the phosphorylation of PI3K, AKT, and mTOR. Furthermore, in our animal experiments, the weight of colon cancer was significantly lower in LSZ-treated mice than in untreated ones, and the expression of Ki67 and N-cadherin positive cells was significantly lower in the treated mice than in their control group counterparts. Conclusions Together, the results suggested that LSZ inhibited proliferation, motility, and EMT of colon cancer cells through the PI3K/AKT/mTOR pathway in vitro and in vivo .
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