[Objective] The experiment aimed to explore the relations between structure of aconitine, aconitine derivatives and insecticide. [Method] The aconitine derivatives such as 3-acetyl mesaconitine, 3-propionyl mesaconitine, 3-acetyl-13-Benzoyl-mesaconitine and 3-propionyl-13-Benzoyl-mesaconitine were synthesized by mesaconitine with acetic anhydride or propionic anhydride and their insecticidal activities were also determined. [Result] When the concentration was 500 mg/L, the insecticidal activities of mesaconitine against Nilaparvata legen and Aphis were 50% and 30% respectively while the insecticidal activities of 3-acetyl mesaconitine, 3-propionyl mesaconitine, 3-acetyl-13-Benzoyl-mesaconitine and 3-propionyl-13-Benzoyl-mesaconitine against Aphis medicagini were 40%, 30%, 30% and 20% respectively at 500 mg/L. [Conclusion] After hydroxyl esterification, the insecticidal activity of mesaconitine was declined and the existence of hydroxyl at 3rd position in mesaconitine played very important influences on insecticidal activity.