Objective: 7,8-Dihydroxyflavone, a tyrosine kinase receptor agonist, is a flavonoid that has recently gained the attention of researchers due to its anticancer properties. Nevertheless, molecular pathways of 7,8-dihy-droxyflavone for hepatocarcinoma are uncertain. Our aim was to identify the impact of 7,8-dihydroxyflavone on human hepatocarcinoma. Material and Methods: Human hepatocarcinoma cell line-7 cells were used as human hepatocarcinoma cells, and 7,8-dihydroxyflavone was applied to the cells at various doses. The cytotoxic and apoptotic effects of 7,8-dihydroxyflavone were determined with Alamar Blue and flow cytometry. The properties of 7,8-dihy-droxyflavone on the mRNA expressions related with Bcl-2, Bax, cleaved-caspase-3 genes, and protein expressions were determined via quantitative real-time polymerase chain reaction and western blot analysis, respectively. Results: 7,8-Dihydroxyflavone-enhanced cell death in human hepatocarcinoma cell line-7 via the overexpres-sion of cleaved-caspase-3 (P =.003) and decreased Bcl-2 (P =.038) protein levels. Furthermore, cleaved-caspase-3 mRNA overexpression (P =.001) markedly led to 7,8-dihydroxyflavone-induced apoptosis. Conclusion: 7,8-Dihydroxyflavone could promote apoptotic cell death by modulating caspase pathways and suppressing antiapoptotic protein. These characteristics may mediate to clinical practice of 7,8-dihydroxyfla-vone for prevention and therapy of hepatocarcinoma.