Olive oil is widely recognized for its cancer-prevention properties, and its by-products, such as pomace and leaves, offer an opportunity for compound extraction. This study comprehensively reviews the antitumor activities of olive extracts and compounds in both in vitro and in vivo studies. Key compounds, including hydroxytyrosol (HT), oleuropein (OL), oleocanthal (OC), and maslinic acid (MA), demonstrated significant antiproliferative, apoptotic, antimigratory, and anti-invasive effects, along with selective cytotoxicity, particularly against breast and colorectal cancer. HT, OC, and MA showed anti-angiogenic effects, while HT and OC showed antimetastatic effects. Moreover, HT, OL, and OC also presented synergistic effects when combined with anticancer drugs, improving their efficacy. Additionally, HT, OL, and MA exhibited protective effects against several side effects of chemotherapy. These compounds are able to modulate important signaling pathways such as the mammalian target of rapamycin, regulate oxidative stress through reactive oxygen species production, modulate angiogenic factors, and induce autophagy. Interestingly, the synergistic effects of the compounds within olive extracts appear to be stronger than their individual action. There is a need for dose optimization, further mechanistic studies to clarify the precise mechanisms of action, and future studies using olive pomace extracts with animal models.
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