Leptadenia pyrotechnica Forssk is a traditional medicinal herb used for treatment of inflammatory diseases and cancer. In this research, the aqueous ethanolic crude extract of Leptadenia pyrotechnica aerial parts, along with its ethyl acetate, n-butanol and water partitioning fractions were evaluated for their antioxidant capacity, polyphenolic content, anti-inflammatory and anti-cancer properties. The total antioxidant capacity was estimated by the FRAP, DPPH, ABTS and β-carotene bleaching assays.The ethyl acetate fraction exhibited the highest polyphenolic content (252.27 mg gallic acid/g) and the best antioxidant activity (1.2, 0.57, 0.45 mmol ascorbic acid equivalent/g in the FRAP, ABTS and DPPH assays, respectively). Furthermore, the same extract showed appreciable anti-inflammatory via lipoxygenase (LOX) inhibitory activity (IC₅₀ = 1.41 µg/mL). Moreover, the ethyl acetate fraction also showed the strongest cytotoxic effect (IC₅₀ = 43.16 µg/mL) against MCF-7 human breast cancer cell line. These results suggest that this plant may be considered an interesting source of compounds with antioxidant, anti-inflammatory and anti-cancer properties for therapeutic, nutraceutical and functional food applications.