The purpose of this study was to isolate citral from sweet orange oil by combined usage of molecular distillation and column chromatography. Additionally, the antioxidant activity (by DPPH radical scavenging activity and reducing power) of citral was evaluated. A significant and linear correlation coefficient between the antioxidant activity and the concentration of citral was found (R2=0.9925). On the other hand, the cytotoxic effects of the citral against tumoral human cell line Hela was examined by MTT assay and the IC50 values was 32.56 μg/mL. Overall, results presented here suggest that the citral possesses antioxidant activity and cytotoxic properties, and is a potential source of active ingredients for food and pharmaceutical industry.