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<p>The growing need for sustainable mosquito control solutions led us to develop an optimized larvicidal formulation against <i>Culex pipiens Linnaeus, 1758 (Diptera: Culicidae)</i>, a key disease vector. Based on preliminary LC<sub>50</sub> evaluations, we developed a synergistic essential oil (EO) blend composed of <i>Artemisia absinthium</i> Linnaeus (58%), <i>A. arborescens</i> L. (26%), and <i>A. campestris</i> L. (16%), subsequently encapsulated in β-cyclodextrin (βCD) to enhance its stability and efficacy. This study pursued three main objectives: (1) characterizing the optimized EO formulation, (2) developing and validating its βCD encapsulation, and (3) elucidating its mechanism of action through molecular docking. The GC–MS analysis of this specific three-species blend identified camphor (40.21%), thujone (27.71%), and chamazulene (14.19%) as the dominant bioactive compounds. Successful formation of EO-βCD inclusion complexes was confirmed through comprehensive characterization: SEM–EDX revealed uniform encapsulation morphology, FTIR spectroscopy verified molecular interactions, and TGA demonstrated significantly improved thermal stability. Larvicidal efficacy was systematically evaluated through two-way ANOVA comparing three treatments (free EO, encapsulated EO, and temephos control) across three exposure periods (24, 48, and 72 h). Bioassays revealed the encapsulated formulation’s superior larvicidal activity against <i>C. pipiens</i>, with LC<sub>50</sub> values decreasing from 23.87 µg/mL at 48 h to 11.61 µg/mL at 72 h—representing a 48% improvement over non-encapsulated EO. Molecular docking simulations (AutoDock Vina) uncovered the mechanistic basis for this enhanced activity, showing chamazulene's strong binding affinity (− 6.8 kcal/mol) to acetylcholinesterase through hydrophobic interactions with Val A29, His A132, and Pro A63 residues, plus a critical pi-anion bond with Asp A131. These results demonstrate that βCD encapsulation transforms our optimized <i>Artemisia</i> EO blend into a potent, eco-friendly larvicide with triple advantages: enhanced stability, controlled release properties, and targeted neurotoxic action. Further research should focus on optimizing formulations, evaluating environmental impacts, and scaling up use in vector control programs.</p>

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Synergistic formulation of Artemisia essential oils in beta-cyclodextrin: in vitro and in silico analysis of insecticidal activity against Culex pipiens

  • 期刊论文

  • 发表日期：

    2025年7月1日

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  • Abdellatif Alami,
  • Amine Ez-zoubi,
  • Mouhcine Fadil,
  • Yassine Ez zoubi,
  • Sara Lebrazi,
  • Naima Boutahiri,
  • Abdellah Farah

摘要

The growing need for sustainable mosquito control solutions led us to develop an optimized larvicidal formulation against Culex pipiens Linnaeus, 1758 (Diptera: Culicidae), a key disease vector. Based on preliminary LC50 evaluations, we developed a synergistic essential oil (EO) blend composed of Artemisia absinthium Linnaeus (58%), A. arborescens L. (26%), and A. campestris L. (16%), subsequently encapsulated in β-cyclodextrin (βCD) to enhance its stability and efficacy. This study pursued three main objectives: (1) characterizing the optimized EO formulation, (2) developing and validating its βCD encapsulation, and (3) elucidating its mechanism of action through molecular docking. The GC–MS analysis of this specific three-species blend identified camphor (40.21%), thujone (27.71%), and chamazulene (14.19%) as the dominant bioactive compounds. Successful formation of EO-βCD inclusion complexes was confirmed through comprehensive characterization: SEM–EDX revealed uniform encapsulation morphology, FTIR spectroscopy verified molecular interactions, and TGA demonstrated significantly improved thermal stability. Larvicidal efficacy was systematically evaluated through two-way ANOVA comparing three treatments (free EO, encapsulated EO, and temephos control) across three exposure periods (24, 48, and 72 h). Bioassays revealed the encapsulated formulation’s superior larvicidal activity against C. pipiens, with LC50 values decreasing from 23.87 µg/mL at 48 h to 11.61 µg/mL at 72 h—representing a 48% improvement over non-encapsulated EO. Molecular docking simulations (AutoDock Vina) uncovered the mechanistic basis for this enhanced activity, showing chamazulene's strong binding affinity (− 6.8 kcal/mol) to acetylcholinesterase through hydrophobic interactions with Val A29, His A132, and Pro A63 residues, plus a critical pi-anion bond with Asp A131. These results demonstrate that βCD encapsulation transforms our optimized Artemisia EO blend into a potent, eco-friendly larvicide with triple advantages: enhanced stability, controlled release properties, and targeted neurotoxic action. Further research should focus on optimizing formulations, evaluating environmental impacts, and scaling up use in vector control programs.