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Ripened berries of Rivina humilis L. (pigeon berry) were investigated for pigment and nutritional composition, in vitro bioactivities, and cancer cell cytotoxicity of its extracts. Ten betalain pigments (total content–0.35 g/100 g fresh weight, and 1.7 g/100 g dry weight) with high level of betaxanthins were characterised. Carbohydrates (6.2 g), proteins (1.1 g), lipids (0.7 g), phenols (105.7 mg gallic acid equivalent), niacin (5.3 mg), and total tocopherols (0.77 mg) in 100 g fresh weight were observed. Antioxidant bioactivity of MeOH extract (maximum at 100 μg/mL) against OH and β-carotene oxidation was studied. The extract (1000 μg/mL) effectively protected kidney lipid peroxidation compared to butylated hydroxy anisole. Betalains rich extract, and purified betacyanins and betaxanthins revealed EC₅₀ against DPPH (51.0, 0.29, 0.11 μg/mL), and reducing power (39.3, 2.79, and 1.34 μg/mL) which was higher than that of …