Alpha (α)-tomatine (simply tomatine) is the major saponin and occurs naturally in tomatoes, possesses a variety of biological properties including antioxidant, and anti-inflammatory. In additıon, tomatine is also known that it breaks down the cell membrane induces growth inhibition and apoptosis in different cancer cells: myeloid leukemia cells; prostate cancer cells; lung adenocarcinoma cells. However, the mechanisms of α-tomatine actions were not well understood. Nevertheless, was shown, that tomatine inhibited the NF-κB and phosphatidyl-inositol-3-kinase/Akt signaling pathways activation. However, the primary cellular target(s) for α-tomatine and its mechanisms for modulating apoptosis-associated pathways remain to be elucidated. The interaction of α-tomatine with cholesterol and the disruptive effect on the cell membrane may be one of the mechanisms by which α-tomatine induces apoptosis. The formation of complexes of α-tomatine and cholesterol may modulate the responsiveness of cell membrane receptors to growth stimuli and thus decrease the growth of cancer cells. Moreover, the anti-inflammatory mechanisms of α-tomatine, which may be a valuable therapeutic agent in the treatment of inflammation-related diseases was due to the ability of tomatine accelerated the phosphorylation of Akt in macrophages.