Insecticide compounds selection based on activation of ecdysteroid receptors in Diptera (S2) and Lepidoptera (Sf9) cell lines

Abstract

Nuclear receptors are important targets in the research for the discovery of brand-new insecticides, and the ecdysteroid receptor is one of the most important targets nowadays. In this study, nine organocalcogenic compounds analogs of dibenzoylhydrazine were tested in a screening system, that presented at least 80% of compatibility in at least one of the three micromolar concentrations tested. We optimized in embryonic cell lines of the order Lepidoptera (SF9) and Diptera (S2), and these cell lines were transfected with a specific reporter plasmid. The nine compounds tested did not present agonist activity in both cell lines tested. In S2 cells the DAF-2 molecule inhibited the ECR-USP luminescence in 29.91%, and the DAF-4 molecule significantly inhibited the nuclear receptor luminescence in 51 to 55% compared to 20-Hydroxyecdysone (control). In SF9 cells, DAF-2 inhibited ECR-USP luminescence in 19.62%, and DAF-4 inhibited the receptor luminescence by 35.14% compared to 20-Hydroxyecdysone (control). In silico analysis of the Drosophila melanogaster receptor with the compound, DAF-2 showed inhibition of amino acids THR467 and MET-508 and with compound DAF-4 inhibition of ARG-511. For the of Heliothis virescens receptor for dendritic compounds, DAF-2 promoted inhibition of amino acids THR-343 and ARG-387 and DAF-4 inhibited ASN-504 and ARG-387