The primary ethanol extracts of Litsea cubeba were separated and purified by liquid - liquid extraction method. The biological activity of the extraction compositions against Tribolium castaneum was studied and the effective insecticidal compositions were determined. The results showed that the repellent rate of chloroform extracts at 1.57mg/cm2 against Tribolium castaneum was 81.26% and the contact-killing corrected mortality at 50mg/mL was 75.98%. The chloroform extracts contented 20 kinds of organic compounds by GC-MS and 7-hydroxy-3, 7-dimethyl-Octanal was 21.15%, 2, 6-Diisopro-pylaniline was 16.41%, Chlorobutanol was 10.54%. The bioactivators possessed repelling and contact-killing may be 7-hydroxy -3, 7- dimethyl-Octanal , 2, 6-Diisopropylaniline.