Insect neuropeptides play a very important role in an insect's life. The insect kinins (InKs) are a family of neuropeptides isolated from a number of insects. Owing to their multifunctions such as the regulation of hindgut contraction, diuresis, and the release of digestive enzymes, InKs are considered as a potential tool for pest management. But their susceptibility to both exo- and endopeptidases precludes their application in practice. However, some InKs analogs, designed to protect peptidase-susceptible sites, have exhibited good antifeedant and insecticidal activities. And the InKs receptors have been regarded as potential targets for develotment of bioinsecticides. To find a biostable and bioactive insecticide candidate with simplified structure, a series of N-terminal modified insect kinin mimetics 1a-1j   were designed and synthesized based on the lead compound [Aib]-Phe-Phe-[Aib]-Trp-Gly-NH2. Aphicidal activity against Aphis glycines was evaluated using the leaf-dipping method. The results showed that all the analogs maintained good aphicidal activity. In particular, the pentapeptide analog 1 j (LC50=0.045 mmol/L) exhibited similar aphicidal activity to the lead (LC50=0.048 mmol/L). Based on these results, we surmised that insect kinin analogs could be structurally simplified to pentapeptide while retaining good aphicidal activity. The analog 1 j can be used as the lead for further discovery of potential bioinsecticides.

Insect kinins mimetics: Design, synthesis, and aphicidal activity as potential bioinsecticides

248th National Meeting (2014)

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