The leaves of Calotropis procera were air dried, grounded and soaked with ethanol. The extracts obtained (29.79g, CP1) was fractionated sequentially using aqueous methanol with petroleum ether, chloroform and ethyl acetate respectively. The residue of ethanol extract (marc) was extracted with 5M HCl, basified and extracted with chloroform. These were labeled as CP1-01 to CP1-05 for the plant. Each of these fractions was phytochemically screened to detect the class of secondary metabolite present. The fractions obtained from the plant were found to be selectively active against brine shrimp larvae. These fractions were also subjected to antimalaria parasites bioassay. Fractions CP1, CP1-04 and CP1-05 were found to be active against tested organisms, withCP1-04 being the most active. CP1-04 was further subjected to activity guided column chromatography that led to the isolation of two pure compounds CP1-04-1 and CP1-04-61. Compound CP1-04-61 was found to be active against the malaria parasite. This was further purified and subjected to qualitative and quantitative analysis.