Fungal Metabolite Asperaculane B Inhibits Malaria Infection and Transmission

Mosquito-transmittedPlasmodiumparasites cause millions of people worldwide to suffer malaria every year. Drug-resistantPlasmodiumparasites and insecticide-resistant mosquitoes make malaria hard to control. Thus, the next generation of antimalarial drugs that inhibit malaria infection and transmission are needed. We screened our Global Fungal Extract Library (GFEL) and obtained a candidate that completely inhibitedPlasmodium falciparumtransmission toAnopheles gambiae. The candidate fungal strain was determined asAspergillus aculeatus. The bioactive compound was purified and identified as asperaculane B. The concentration of 50% inhibition onP. falciparumtransmission (IC50) is 7.89 mu M. Notably, asperaculane B also inhibited the development of asexualP. falciparumwith IC(50)of 3 mu M, and it is nontoxic to human cells. Therefore, asperaculane B is a new dual-functional antimalarial lead that has the potential to treat malaria and block malaria transmission.