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Oleuropein and hydroxytyrosol, two major polyphenolic compounds extracted from the olive tree (Olea europaea), have involved significant consideration scientific interest due to their strong pharmacological properties, including anticancer, antioxidant, an-ti-inflammatory, and antidiabetic effects. These compounds play a crucial role in modu-lating oxidative stress, neutralizing free radicals, and protecting against cellular damage, thereby contributing to neuroprotection, cardiovascular health, and metabolic regula-tion. Their anticancer potential has been widely demonstrated through their ability to inhibit tumor progression, induce apoptosis, and in various tumor models they boost the efficiency of chemotherapy, including breast and hepatocellular carcinoma. Addi-tionally, their anti-inflammatory activity is attributed to the regulation of cytokines, suppression of NF-κB signaling, and modulation of immune responses, which could be beneficial in managing chronic inflammatory and autoimmune diseases. Moreover, their role in diabetes management has been extensively studied, showing their ability to im-prove insulin sensitivity, regulate glucose metabolism, and reduce lipid accumulation in hepatic and adipose tissues, thus preventing metabolic complications. Despite extensive preclinical evidence supporting the therapeutic benefits of these compounds, their clin-ical translation remains challenging due to issues related to bioavailability, stability, and optimal dosage. Future research should focus on improving their pharmacokinetic properties, developing advanced drug delivery systems, and carrying out extensive clinical trials to confirm their safety and effectiveness in humans. The integration of these compounds into functional foods, nutraceuticals, and pharmaceutical formula-tions holds immense promise for preventive and therapeutic applications, potentially offering natural alternatives to conventional therapeutic agents for managing metabolic, inflammatory, and degenerative diseases.