Abstract
Insecticides directed against acetylcholinesterase (AChE) are facing increased resistance among target species as well as increasing concerns for human toxicity. The result has been a resurgence of disease vectors, insects destructive to agriculture, and residential pests. We previously reported a free cysteine (Cys) residue at the entrance to the AChE active site in some insects but not higher vertebrates. We also reported Cys-targeting methanethiosulfonate molecules (AMTSn), which, under conditions that spared human AChE, caused total irreversible inhibition of aphid AChE, 95% inhibition of AChE from the malaria vector mosquito ( Anopheles gambia), and >80% inhibition of activity from the yellow fever mosquito ( Aedes aegypti) and northern house mosquito ( Culex pipiens). We now find the same compounds inhibit AChE from cockroaches ( Blattella germanica and Periplaneta americana), the flour beetle ( Tribolium confusum), the multi-colored Asian ladybird beetle ( Harmonia axyridis), the bed bug ( Cimex lectularius), and a wasp ( Vespula maculifrons), with IC 50 values of ∼1–11 μM. Our results support further study of Cys-targeting inhibitors as conceptually novel insecticides that may be free of resistance in a range of insect pests and disease vectors and, compared with current compounds, should demonstrate much lower toxicity to mammals, birds, and fish.
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