The growth responses of Ruta chalepensis leaf-derived materials toward human intestinal bacteria were examined. The biologically active constituent of the R. chalepensis extract was characterized as quinoline-4-carboxaldehyde($C_{10}H_{7}NO$). The growth responses varied depending on the bacterial strain, chemicals, and dose tested. At 0.25 and 0.1 mg/disk, quinoline-4-carboxaldehyde strongly inhibited the growth of Clostridium perfringens and weakly inhibited the growth of Escherichia coli without any adverse effects on the growth of three lactic acid bacteria. Furthermore, at 0.05 and 0.025 mg/disk, this isolate showed moderate activity against C. perfringens. In comparison, chloramphenicol at as low as 0.01 mg/disk significantly inhibited the growth of all bacteria tested, and cinnamaldehyde at 0.25 mg/disk did not inhibit Bifidobacterium bifidum, B. longum, E. coli, and Lactobacillus acidophilus, with the exception of C. perfringens. The structure-activity relationship revealed that quinoline-3-carboxaldehyde had strong growth inhibition against C. perfringens, but quinoline, quinoline-3-carboxylic acid, and quinoline-4-carboxylic acid did not inhibit the growth of B. bifidum, B. longum, C. perfringens, E. coli, and L. acidophilus. These results indicate that the carboxyl aldehyde functional group of quinolines seems to be required for growth-inhibiting activity against C. perfringens, thus indicating at least one of the pharmacological actions of R. chalepensis leaf.