Dengue is a tropical disease caused by an arbovirus transmitted by Aedes aegypti. Since no effective vaccine is available for treating dengue, the present study focused on population vector control through investigating the use of the lignan grandisin, isolated from Piper solmsianum C. DC., Piperaceae, against the larvae of A. aegypti. Grandisin caused larval (L3) mortality at LC50 150 μg/mL. Histological analysis on A. aegypti larvae treated with grandisin (LC50 50 μg/mL) showed changes in the anterior-middle midgut, with intense tissue destruction and cell disorganization.