In the search for effective and environmentally friendly mosquito control agents, we have examined natural sources, such as microbes and plants, and the synthetic analogs of natural products.These plants and microbes have evolved in their ecological niches to produce defensive compounds against other competing organisms in their surroundings such as microbes, plants, and insects as a means to enhance their survival. Thus, some of these plants and microbes have bioactive compounds with insecticidal, fungicidal, and phytotoxic activities. In our previous research, we successfully isolated bioactive constituents from natural sources. We have carried out synthetic modifications and total synthesis of marginally active isolated compounds to achieve significantly higher active compounds. We have focused on plants in the Rutaceae family as the members of this family are known to possess bioactive compounds with algicidal, antifungal, insecticidal, and fungicidal activities. In this article, we report the isolation and structure elucidation of mosquito larvicidal constituents from Poncirus trifoliata (Rutaceae) root extract.