宋果灵对乙酰胆碱酯酶活性的抑制作用  

Study on the Inhibitory Effect of Songorine on the Activity of Acetylcholinesterase

作　　者：杨小生[1] 万里翔[1] 贺新生[1] 侯大斌[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

出　　处：《安徽农业科学》2008年第9期3499-3499,3505,共2页Journal of Anhui Agricultural Sciences

基　　金：国家"十一五"科技支撑计划项目(2006BAE01A01-12)

摘　　要：[目的]认识宋果灵具体的杀虫机制,为开发此类植物源农药以及进行酶法筛选提供毒理学参考。[方法]配制浓度分别为0、0.005、0.01、0.020、.0350、.05 mg/ml的宋果灵,研究宋果灵对乙酰胆碱酯酶活性的抑制作用及可能的机制。[结果]随着宋果灵浓度的升高,乙酰胆碱酯酶活性逐渐下降,说明宋果灵对乙酰胆碱酯酶活性有抑制作用,线性回归方程为:y=-0.118 9x+99.387,R2=0.934 4,IC50=0.412 mg/ml。宋果灵含有N原子,与质子结合后,带正电,NH4+正离子与Trp84、Phe330的侧链芳环形成阳离子-π相互作用,从而抑制了酶活性。[结论]宋果灵可以作为农药先导化合物,用于合成高效、低毒、无公害的新农药。[Objective] The research aimed to get know of the concrete insecticidal mechanism of songorine and provide toxicological reference for developing this kind of plant pesticide and screening by enzyme method. [Method] Songorine with different concn. （0, 0.1305, 0.01, 0.02, 0.035, 0.05 mg/ml） were set up to study the inhibitory effect and possible mechanism of songorine on the activity of acetylcholinestemse. [ Result ] With the increasing of songrine concentration, the activity of acetylcholinestemse was gradually decreased, which indicated that songrine had an inhibitory effect on the activity of acetylcholinestemse. Its linear regression equitation was y = - 0. 118 9x ＋ 99.387 with R^2 of 0.934 4 and IC50 of 0.412 mg/ml. Songorine contained N atom and was with positive electricity when it was linked with proton, and the NH4^＋ positive ion formed the positive ion- πinteraction with Trp84 and Phe330 of side chain aromatic ring, which inhibited acetylcholinestemse activity. [ Conclusion] Songorine could be taken as pesticide leading compound and used to synthesize new pesticides with high-efficiency, low-toxicity and no harm.

关 键 词：宋果灵 乙酰胆碱酯酶活性 杀虫机制 

分 类 号：S482.3[农业科学—农药学]