中乌头碱衍生物的合成及其杀虫活性测定  

Synthesis and Bioactivity of Derivatives from Mesaconitine

作　　者：许源[1] 侯大斌[2] 杨海君[3] 袁小红[1] 王惠[1] 赵祥升[1] 

机构地区：[1]西南科技大学生命科学与工程学院,四川绵阳621010 [2]西南科技大学生物药物研究所,四川绵阳621010 [3]西南科技大学材料科学与工程学院,四川绵阳621010

出　　处：《安徽农业科学》2009年第9期3890-3892,共3页Journal of Anhui Agricultural Sciences

基　　金：国家"十一五"科技支撑重大专项课题(2006BAE01A01-12)

摘　　要：[目的]为了探讨中乌头碱(Mesaconitine)结构与杀虫活性间的关系。[方法]以中乌头碱为原料合成了7种衍生物,并经质谱与核磁共振结合鉴定了其结构;以稻飞虱(Nilaparvata legen)、粘虫(Mythima separate)、红蜘蛛(Tetranychus cinnabarnus)、蚜虫(Aphis medicagini)为试虫,测定了衍生物的杀虫活性。[结果]化合物A、B、C、F、G具有一定杀虫活性,其中化合物F和G对稻飞虱活性显著,死亡率分别达到70%和85%。[结论]中乌头碱分子中,保留3-OH1、3-OH1、5-OH有利于保持化合物的杀虫活性,中乌头碱的无机酸盐对稻飞虱有较高杀虫活性。[Objective] The research aimed to study the relationship between structure and insecticidal activity of mesaconitine.[Method] Seven derivatives were synthesized from mesaconitine,their structure were characterized by EI-MS and NMR;The insecticidal activity of mesaconitine and its seven derivatives were tested against Nilaparvata legen,Mythima separate,Tetranychus cinnabarnus and Aphis medicagini.[Result] The results indicated that compound A,B, C,F,G exhibited insecticidal activity,of which F and G were significant to Nilaparvata legen. [Conclusion] The structure-insecticidal activity relationship studies mentioned above showed that 3-OH,13-OH and 15-OH of mesaconitine were beneficial to the insecticidal activity. The inorganic salts of mesaconitine were exhibited high insecticidal activity against Nilaparvata legen.

关 键 词：二萜生物碱 结构修饰 生物活性 中乌头碱 

分 类 号：O629[理学—有机化学] Q949.9[理学—化学]