二萜生物碱白乌头宁衍生物的合成及拒食活性  

Synthesis and Antifeedant Activity of Diterpene Alkaloid Bikhaconine Derivatives

作　　者：李静[1] 陈琳[1,2] 秦大斌[1] LI Jing;CHEN Lin;QIN Da-bin(School of Chemistry and Chemical Engineering,China West Normal University,Nanchong 637002,Sichuan,China;School of Life Science and Engineering,Southwest Jiaotong University,Chengdu 610031,China)

机构地区：[1]西华师范大学化学化工学院,四川南充637002 [2]西南交通大学生命科学与工程学院,成都610031

出　　处：《农药》2021年第8期558-562,共5页Agrochemicals

基　　金：国家自然科学基金青年基金(21807089);四川省科技厅应用基础研究(2021YJ0222);中央高校基本科研业务费(2682021CX085)。

摘　　要：[目的]寻找具有较高拒食活性的二萜生物碱类化合物,为开发高效低毒的农药奠定基础。[方法]以C19-二萜生物碱白乌头宁为母体结构,对其进行结构修饰,合成二萜生物碱衍生物,并采用非选择性叶碟法考察目标化合物对甜菜夜蛾[Spodoptera exigua(Hübner)]的拒食活性。[结果]目标化合物的结构采用1H NMR、13C NMR和HR-ESIMS波谱技术进行确证,经过生物活性测试表明,在1000 mg/L剂量下,化合物2a、2e、2g对甜菜夜蛾具有良好的拒食活性,拒食率(%FR)分别为92.20%、93.03%和96.90%。[结论]所合成的C19-二萜生物碱衍生物对甜菜夜蛾具有较好的拒食效果,初步构效关系表明,引入氟原子取代的苯甲酰基对该类化合物的活性起促进作用,此类化合物可作为新型杀虫剂研究的先导化合物,具有一定的开发潜力。[Aims] This study aims to search for diterpenoid alkaloids derivatives with high antifeedant activity, and to lay the foundation for the development of high-efficiency and low-toxic pesticides. [Methods] Taking the diterpenoid alkaloids of Bikhaconine as the parent structure, a series of derivatives was synthesized and the antifeedant activity of the target compounds was investigated against Spodoptera exigua(Hübner) by using the non-choice leaf disc method.[Results] The structure of the target compounds was confirmed by1 H NMR,13 C NMR and HR-ESI-MS spectroscopy techniques. The biological activity test showed that compounds 2 a, 2 e, and 2 g have good effects against S. exigua(Hübner) at a dose of 1000 mg/L, and the percentage of food reduction(% FR) were 92.20, 93.03 and 96.90%respectively. [Conclusions] The synthesized diterpenoid alkaloids derivatives have a good antifeedant effect against S.exigua(Hübner). The preliminary structure-activity relationship shows that the introduction of benzoyl substituted with fluorine atoms can promote the activity of these compounds, which can be used as the leading compounds in the study of new insecticides, and have a certain potential for development.

关 键 词：二萜生物碱 植物源杀虫剂 拒食活性 

分 类 号：TQ460.3[化学工程—制药化工]