College of Life Sciences and Biotechnology, Korea University, 145 Anamro, Seungbukgu, Seoul 02841, Republic of Korea.
College of Pharmacy, Dongguk University, 32 Donggukro, Ilsandonggu, Goyangsi 10326, Republic of Korea.
Biomolecules. 2023 Aug 21;13(8):1272. doi: 10.3390/biom13081272.
The diamondback moth is a detrimental insect pest of brassicaceous crops which was among the first crop insects to be reported as DDT resistant. It has since proven to be significantly resistant to nearly every synthetic insecticide used in the field in many crucifer-producing regions. Due to insecticide control failures in some parts of the world, economically viable crucifer production is now all but impossible. As a result, there has been an increasing effort to identify new compounds with strong pesticidal activity. Cantharidin is one such compound that has been shown to be highly effective against a variety of insect pests. However, its chemical synthesis and potential toxicity to non-target organisms have been a major source of concern. Herein, using rational design approaches, a new series of cantharidin-based verbenone derivatives were synthesized and evaluated for their insecticidal activities against the diamondback moth. Among different compounds screened, compounds , , , and emerged as the most potent compounds exhibiting 100% mortality at a concentration of 100 mg/L after four days. These compounds demonstrated a good anti-feeding effect against the diamondback moth on cabbage leaves. Subsequently, a 3D QSAR study was carried out to identify the key structural features of the synthesized compounds and their correlation with insecticidal activity.
小菜蛾是十字花科作物的有害昆虫，是最早报道对滴滴涕具有抗性的作物昆虫之一。此后，它已被证明对许多十字花科作物生产地区田间使用的几乎每一种合成杀虫剂都具有显著的抗性。由于世界上某些地区的杀虫剂控制失败，经济可行的十字花科作物生产现在几乎不可能。因此，人们越来越努力地寻找具有强烈杀虫活性的新化合物。斑蝥素就是这样一种化合物，它对多种害虫都有很高的防治效果。然而，其化学合成及其对非靶标生物的潜在毒性一直是人们关注的主要问题。在此，我们采用合理的设计方法，合成了一系列新型斑蝥素基马鞭草酮衍生物，并对其对小菜蛾的杀虫活性进行了评价。在所筛选的不同化合物中，化合物 、 、 、 和 表现出最强的杀虫活性，在 4 天后浓度为 100mg/L 时，死亡率达到 100%。这些化合物在甘蓝叶片上对小菜蛾表现出良好的拒食作用。随后，进行了 3D-QSAR 研究，以确定合成化合物的关键结构特征及其与杀虫活性的相关性。
