Background Colon cancer, a prevalent form of gastrointestinal malignancy, poses a significant public health issue globally. The onset of colon cancer is a complex mechanism implicating genetic and environmental factors, including dietary habits and lifestyle choices.Purpose The current study was undertaken to investigate the anti-tumor effects of artemetin against colon cancer cells.Materials and Methods The influence of artemetin on the proliferation of HCT-116 cells was evaluated with an MTT (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl tetrazolium bromide) test. Also, the extent of apoptosis in both untreated and artemetin-exposed HCT-116 cells was studied using a dual staining technique. The activities of the caspase enzymes (caspase-3, -8, and -9) in both untreated and artemetin-exposed HCT-116 cells were evaluated using a commercial diagnostic kit.Results The administration of several dosages of artemetin significantly suppressed the HCT-116 cells dose-dependently. Furthermore, artemetin treatment significantly induced apoptosis in HCT-116 cells, which is evidenced by dual staining assay. Artemetin treatment also elevated the caspase-3, -8, and -9 activities in the colon cancer cells.Conclusion The present study revealed that artemetin possesses anti-cancer activities against colon cancer, reducing cell viability and inducing caspase-mediated apoptosis in HCT-116 cells. Consequently, the present findings indicate artemetin as a favorable anti-tumor candidate for future colon cancer therapy.