当前位置: X-MOL 学术Pestic. Biochem. Phys. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Insecticidal, antifeedant and acetylcholinesterase inhibitory activity of sesquiterpenoids derived from eudesmane, their molecular docking and QSAR
Pesticide Biochemistry and Physiology ( IF 4.7 ) Pub Date : 2024-02-28 , DOI: 10.1016/j.pestbp.2024.105841
Muñoz-Núñez Evelyn , Pastene-Navarrete Edgar , Quiroz-Carreño Soledad , Céspedes-Acuña Carlos , Madrid-Villegas Alejandro , Alarcón-Enos Julio

This work evaluated the insecticidal, antifeedant and AChE inhibitory activity of compounds with eudesmane skeleton. The insecticidal activity was tested against larvae of and , the compounds and were the most active (LC 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 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 larvae showed an antifeedant index (AI) of 99% at 72 h for compounds , and . The QSAR studies show that the properties associated with the polarity of the compounds would be responsible for the biological activities found.

中文翻译:

桉树倍半萜类化合物的杀虫、拒食和乙酰胆碱酯酶抑制活性及其分子对接和 QSAR

本工作评价了具有桉烷骨架的化合物的杀虫、拒食和乙酰胆碱酯酶抑制活性。测试了 和 的幼虫杀虫活性,化合物 和 的活性最强(LC 分别为 104.2 和 106.7 μM;82.0 和 84.4 μM)。同样,上述化合物表现出最高的乙酰胆碱酯酶抑制活性,IC 值分别为 0.26 ± 0.016 和 0.77 ± 0.016 μM。酶动力学研究以及分子对接表明,这些化合物将是酶的非竞争性抑制剂。对幼虫的拒食活性显示,化合物 、 和 72 小时时的拒食指数 (AI) 为 99%。 QSAR 研究表明,与化合物极性相关的特性可能与所发现的生物活性有关。
更新日期:2024-02-28
down
wechat
bug