The present study evaluated the total phenolic and flavonoid contents and the antioxidant and cytotoxic properties of Eremanthus erythropappus. Dried and powdered of E. erythropappus leaves were extracted with ethanol by static maceration followed by partition to obtain the hexane, dichloromethane, ethyl acetate, and butanol fractions. Phytochemical screening and the total phenolic and flavonoid contents were determined. The antioxidant activity was evaluated by DPPH, reducing power of Fe+3 and β-carotene/linoleic acid assays. The cytotoxic test was performed by brine shrimp lethality bioassay. Tannins, flavonoids, coumarins, terpenoids and steroids and saponins were detected in the ethanol extract and fractions. In these samples, the total phenolic and flavonoid contents ranged from 0.98 ± 0.15 to 16.27 ± 0.23 g/100 g and 0.84 ± 0.06 to 5.09 ± 0.22 g/100 g, respectively. The ethanol extract and fractions showed antioxidant effect as free radical scavengers and inhibitors of lipid peroxidation. In addition, the tested samples were cytotoxic against brine shrimp. These results suggest that E. erythropappus is an important and promising source of bioactive compounds with antioxidant and cytotoxic properties.