Ethnopharmacological relevance: Alocasia macrorrhiza has been used as a folk medicine for cancer treatment in the Southwest of China. Aim of the study: The purpose of this study is to confirm the anticancer activity of aqueous extract of alocasia macrorrhiza against hepatic cancer and to elucidate its mechanism of action. Materials and methods: Human normal liver cells and hepatocellular carcinoma cells were tested in vitro for cytotoxicity, colony formation inhibition, EdU incorporation, AO/EB staining apoptotic cells, apoptotic DNA fragmentation, and cell cycle distribution in response to alocasia macrorrhiza extract. The mRNA and protein expressions of PPAR gamma, Cyclin D1, Rb, P21, Bax, Bcl-2 and caspase-3 were detected through RT-PCR and Western blotting; the tumor growth inhibition in vivo was tested by oral administration of the extract. Results: Alocasia macrorrhiza aqueous extract exhibited proliferation inhibition and apoptosis effects on human hepatocellular carcinoma cells in vitro, inhibited hepatoma growth in vivo. Conclusion: Alocasia macrorrhiza extract has potential cytotoxic and apoptotic effect on human hepato-cellular carcinoma cells and inhibits hepatoma growth in vivo, its mechanism of action might be associated with the inhibition of DNA synthesis, cell cycle (G(0)/C-1) arrest, apoptosis induction through up-regulation the mRNA and protein expressions of PPAR gamma, Rb, Bax and capase-3genes and down-regulation of the expressions of Cyclin D1 and Bcl-2 genes. (C) 2012 Elsevier Ireland Ltd. All rights reserved.