Alami Abdellatif, Ez-Zoubi Amine, Fadil Mouhcine, Zoubi Yassine Ez, Lebrazi Sara, Boutahiri Naima, Farah Abdellah
Laboratory of Applied Organic Chemistry, Faculty of Sciences and Techniques of Fez, Sidi Mohamed Ben Abdellah University, Fez, Morocco.
Biotechnology, Environmental Technology and Valorization of Bio-Resources Team, Laboratory of Research and Development in Engineering Sciences, Faculty of Sciences and, Techniques Al-Hoceima, Abdelmalek Essaadi University, Tetouan, Morocco.
Environ Sci Pollut Res Int. 2025 Jul;32(33):20070-20085. doi: 10.1007/s11356-025-36849-8. Epub 2025 Aug 14.
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 LC 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 LC 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.
对可持续蚊虫控制解决方案的需求不断增长，促使我们开发一种针对致倦库蚊（Culex pipiens Linnaeus，1758，双翅目：蚊科）的优化杀幼虫制剂，致倦库蚊是一种关键的疾病传播媒介。基于初步的半数致死浓度（LC）评估，我们开发了一种由苦艾（Artemisia absinthium Linnaeus，占58%）、树艾（A. arborescens L.，占26%）和田野艾（A. campestris L.，占16%）组成的协同精油（EO）混合物，随后将其包裹在β-环糊精（βCD）中以提高其稳定性和功效。本研究有三个主要目标：（1）表征优化后的精油制剂，（2）开发并验证其βCD包封，（3）通过分子对接阐明其作用机制。对这种特定的三种植物混合物进行气相色谱-质谱（GC-MS）分析，确定樟脑（40.21%）、侧柏酮（27.71%）和天蓝烃（14.19%）为主要生物活性化合物。通过全面表征证实了成功形成了精油-βCD包合物：扫描电子显微镜-能谱仪（SEM-EDX）显示出均匀的包封形态，傅里叶变换红外光谱（FTIR）验证了分子相互作用，热重分析（TGA）表明热稳定性显著提高。通过双向方差分析系统地评估了杀幼虫功效，比较了三种处理（游离精油、包封精油和双硫磷对照）在三个暴露时间段（24、48和72小时）的效果。生物测定表明，包封制剂对致倦库蚊具有优异的杀幼虫活性，其LC值从48小时的23.87微克/毫升降至72小时的11.61微克/毫升，比未包封的精油提高了48%。分子对接模拟（AutoDock Vina）揭示了这种增强活性的作用机制，显示天蓝烃通过与缬氨酸A29、组氨酸A132和脯氨酸A63残基的疏水相互作用以及与天冬氨酸A131的关键π-阴离子键，对乙酰胆碱酯酶具有很强的结合亲和力（-6.8千卡/摩尔）。这些结果表明，βCD包封将我们优化的艾蒿精油混合物转化为一种高效、环保的杀幼虫剂，具有三重优势：增强的稳定性、控释特性和靶向神经毒性作用。进一步的研究应集中在优化制剂、评估环境影响以及扩大在病媒控制项目中的应用规模。
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