To obtain novel potentially botanical insecticides from non-food bioactive products for an Integrated Pest Management system, a series of monosaccharides-matrine conjugates were prepared by modifications of the natural alkaloid matrine from Sophora flavescens under ultrasonic irradiation (yields were increased from 18 to 62% (without ultrasound) to 48–67 %, whereas the amount of reactants was reduced, especially the reaction time was sharply decreased from 3−16 h (without ultrasound) to 1 h). Against Mythimna separata, 3f and If (2.6 folds of that of matrine) exhibited the most promising insecticidal activity; against Tetranychus cinnabarinus, 3d and 3e (about 7.0 folds of that of matrine) showed the most pronounced acaricidal activity. Especially 3d and 3e displayed good control effects in the greenhouse. © 2020 Elsevier B.V.