Background & objectives: Aedes aegypti mosquito is the principal vector of the viruses responsible for urban yellow fever, dengue, dengue haemorrhagic fever, as well as Zika and chikungunya in Brazil. The present study was aimed to investigate the insecticidal potential of the extract and fractions of Ottonia anisum, along with special metabolites isolated from it, as natural alternatives against larvae (L3) of Ae. aegypti, vector of potentially deadly tropical infections in Brazil. Methods: The plant species O. anisum was collected in March 2015, at Xerém area, in Rio de Janeiro City, Brazil. Crude extracts and the isolated pure compounds were screened for toxicity against Ae. aegypti larvae (L3). Bioassays were performed on 20 larvae (L3) of Ae. aegypti in triplicate. The samples were dissolved in a mixture of acetone and DMSO at final concentrations of 1-200 μg/ml. The toxicity of the solutions was evaluated towards the growth and development of Ae. aegypti larvae till emergence of adults. Results: The crude hexane extract showed 100% larval mortality 24 h after treatment at a concentration of 200 μg/ ml. The bioassays using 1-butyl-3,4-methylenedioxybenzene revealed 100% mortality among L3 larvae, 24 h after the treatment at a concentration of 30 μg/ml, the LC50 recorded was 1.6 μg/ml. At concentration of 10 μg/ml, the L3 larval mortality recorded was 92%. Interpretation & conclusion: The metabolite 1-butyl-3,4-methylenedioxybenzene showed potent toxicity against Ae. aegypti larvae. This arylbutanoid agent could be used as a natural alternative adjuvant pesticide, in new compositions that would be environmentally safer.