The toxicity of materials derived from root of Asiasarum heterotropoides against early third instar larvae from susceptible Culex pipiens pallens, Aedes aegypti, and Ochlerotatus togoi was examined using direct contact mortality bioassays. Results were compared with those following the treatment with two currently used mosquito larvicides, temephos and fenthion. The bioactive principles of A. heterotropoides root were identified as asarinin, asarone, methyleugenol, pellitorine, and pentadecane by spectroscopic analysis. As judged by 24 h LC50 values, pellitorine (2.08-2.38 ppm) was the most toxic compound, followed by asarinin (10.49-16.49 ppm) and asarone (22.38-26.99 ppm). These compounds were less toxic than either temephos (0.16-0.20) or fenthion (LC50, 0.23-0.29). Weak activity was produced by methyleugenol (53.30-58.52 ppm) and pentadecane (96.71-99.19 ppm). A. heterotropoides root-derived materials, particularly pellitorine, merit further study as potential mosquito larvicides for protection from humans and domestic animals from vector-borne diseases and nuisance caused by mosquitoes.