Senecio vulgaris L. is a well known toxic plant, phytochemical investigation of the whole plant afforded the isolation of a new coumarin; 3,7-dihydroxy-5,6 dimethoxycoumarin-7-O-β-D-glucoside (1), in addition to the isolation of isorhamnetin-3-O-β-D-glucoside (2) and two known alkaloids of common occurrence in genus Senecio; senecionine (3) and seneciphylline (4). The isolated compounds were identified by physical and chemical analyses and by intensive investigation of their spectral data. EtOH extract, light petrol and CHCl3 fractions of S.vulgaris were found to have cytotoxic activity on colorectal cell line HCT-116 cell line, with IC50 values of 19.9, 27.3 and 17.8 μg mL-1, respectively. That indicates the most active cytotoxic fraction is the alkaloid-bearing chloroform fraction. These findings promote the future perspective of S. vulgaris as an anticancer agent. The antioxidant activity of EtOH extract, light petrol fraction and CHCl3 fraction was evaluated by DPPH assay, %inhibition was 23.31, 4.677 and 17.598, respectively. Also the ratio between senecionine and seneciophylline in their mixture was determined using 1H-NMR spectrum.