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Cyperus esculentus (Tiger nut) has been grossly underutilized and unexploited despite its nutritional and medicinal potentials. This research aimed to evaluate the phytochemical, proximate, GC-MS and pharmacological properties such as antioxidant, anticancer, anti-elastase, anti-melanogenic and anti-tyrosinase activity in ethanol and n-hexane extracts of tiger nut. The pharmacological activities were measured using spectrophotometry, agar well diffusion, MCF-7 and HeLa cell methods. The tiger nut extracts (ethanol and n-hexane) in the phytochemical and proximate analysis showed the existence of bioactive compounds such as alkaloids, glycosides, flavonoids, crude fibres, tannins, proteins, carbohydrates, oxalates, phytates and fats content. The ethanol extract showed superior pharmacological (anticancer, antibacterial, anti-melanogenic and antioxidant) activities, especially against the MCF-7 cell line. The results for scavenging activity of ethanol extract (IC50= 535.57 μg/mL) showed significant differences (p< 0.05) when compared with n-hexane extract (IC50= 645.5 μg/mL). The GC-MS assessment of both extracts showed the existence of bioactive compounds. Different concentrations (100, 200 and 350 mg/mL) of tiger nut extracts against Shigella sp., Salmonella sp., Staphylococcus aureus and Escherichia coli demonstrated the highest level of inhibitions at 350 mg/mL. The findings of the current research showed that tiger nut has a high content of nutrients and bioactive phytochemicals.