1. Insecticidal, antifeedant and acetylcholinesterase inhibitory activity of sesquiterpenoids derived from eudesmane, their molecular docking and QSAR.
- Author
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Evelyn, Muñoz-Núñez, Edgar, Pastene-Navarrete, Soledad, Quiroz-Carreño, Carlos, Céspedes-Acuña, Alejandro, Madrid-Villegas, and Julio, Alarcón-Enos
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MOLECULAR docking , *CODLING moth , *SESQUITERPENES , *INDIANMEAL moth , *DROSOPHILA melanogaster , *ENZYME inhibitors - Abstract
This work evaluated the insecticidal, antifeedant and AChE inhibitory activity of compounds with eudesmane skeleton. The insecticidal activity was tested against larvae of Drosophila melanogaster and Cydia pomonella , the compounds 3 and 4 were the most active (LC 50 of 104.2 and 106.7 μM; 82.0 and 84.4 μM, respectively). Likewise, the mentioned compounds were those that showed the highest acetylcholinesterase inhibitory activity, with IC 50 of 0.26 ± 0.016 and 0.77 ± 0.016 μM, respectively. Enzyme kinetic studies, as well as molecular docking, show that the compounds would be non-competitive inhibitors of the enzyme. The antifeedant activity on Plodia interpunctella larvae showed an antifeedant index (AI) of 99% at 72 h for compounds 16 , 27 and 20. The QSAR studies show that the properties associated with the polarity of the compounds would be responsible for the biological activities found. [Display omitted] [ABSTRACT FROM AUTHOR]
- Published
- 2024
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