宋果灵对乙酰胆碱酯酶活性的抑制作用

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。

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

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.(0,0.005,0.01,0.02,0.035,0.05 mg/ml) were set up to study the inhibitory effect and possible mechanism of songorine on the activity of acetylcholinesterase.Result] With the increasing of songrine concentration,the activity of acetylcholinesterase was gradually decreased,which indicated that songrine had an inhibitory effect on the activity of acetylcholinesterase.Its linear regression equitation was y=-0.118 9x+99.387 with R2 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 acetylcholinesterase activity.Conclusion] Songorine could be taken as pesticide leading compound and used to synthesize new pesticides with high-efficiency,low-toxicity and no harm.