Insecticidal activity of active component isolated from Ruta chalepensis leaves was examined against maize weevil, Sitophilus zeamais and compared with two different bioassay system, such as direct contact and fumigant method. The methanol extract of R. chalepensis leaves had strongly (+++) insecticidal activity at 50 mg/disk against S. zeamais. Methanol extract of R. chalepensis was partitioned with hexane, chloroform, ethyl acetate, butanol and water fraction, successively. In this result, the highest activity was shown in chloroform fraction against S. zeamais. Biologically active compound derived from chloroform fraction of R. chalepensis extract was purified by using SiO2 column chromatography and prep-HPLC. The insecticidal constituent of R. chalepensis was identified as quinoline-4-carboxaldehyde by various chromatography and spectroscopic analysis methods. At 2.5 mg/disk, the most toxic activity against S. zeamais was exerted by the direct contact method (100%), followed by the fumigant method (23%). These results revealed that the contact toxicity showed 4.35 times greater than the respiration toxicity. Furthermore, these results indicate that quinoline- 4-carboxaldehyde could be useful as a new preventive agent against damage caused by stored-product insects.