Fraxinellone significantly reduced the relative growth rate, food consumption rate as well as the efficiency of conversion of ingested food into biomass of Heliothis virescens when incorporated into artificial diets at concentrations of 4.31 × 10-5 mol/L and above. After being fed with fraxinellone-treated diets for 24 h, the larval midguts of H. virescens possess significantly lower activities of a-amylase and non-specific proteases and higher activities ofcytochrome P450s. In vitro, the compound did not inhibit the activities of α-amylase and non-specific proteases extracted from the larval midguts. Clear evidence of post-ingestive toxicity of fraxinellone to midgut cells was observed under an electron microscope. The modes of action of the compound against insects were discussed.