College of Plant Protection, Northwest A&F University, Yangling 712100, Shaanxi Province, PR China.
Key Laboratory of Vector Biology and Pathogen Control of Zhejiang Province, College of Life Science, Huzhou University, Huzhou 313000, Zhejiang Province, PR China.
Bioorg Med Chem Lett. 2021 Sep 15;48:128246. doi: 10.1016/j.bmcl.2021.128246. Epub 2021 Jul 4.
To discover non-food renewable forest bioactive products as new potential pesticidal alternatives for crop protection, a series of C15-imines alkaloids were obtained by structural modification of matrine and oxymatrine. Compounds Id, Ih, Ii and IIg (>2-3 folds of their precursors) showed the most potent antifeedant activity against armyworm. Against red spider mite, compounds Ie, Il, IIb, IIc and IIg displayed 1.8-3.1 folds acaricidal activity of their precursors. Notably, compound IIg exhibiting the most pronounced pesticidal activities, can be used as a promising bio-sourced agrochemical agent. The study of stress responses showed that the nAChR subunit α5 and VGSC might be the targets of action of matrine, oxymatrine and IIg against red spider mite.
为了发现非食用可再生森林生物活性产品作为作物保护的新的潜在农药替代品，通过苦参碱和氧化苦参碱的结构修饰得到了一系列 C15-亚胺生物碱。化合物 Id、Ih、Ii 和 IIg（比它们的前体高 2-3 倍）对粘虫表现出最强的拒食活性。对红蜘蛛，化合物 Ie、Il、IIb、Iic 和 IIg 对其前体的杀螨活性提高了 1.8-3.1 倍。值得注意的是，化合物 IIg 表现出最显著的杀虫活性，可作为有前途的生物源农用化学品。应激反应研究表明，nAChR 亚基 α5 和 VGSC 可能是苦参碱、氧化苦参碱和 IIg 对红蜘蛛作用的靶点。
