In our present study, we investigated the effects of continentalic acid on Streptococcus mutans (S. mutans) biofilm. Methanol extract of Aralia continentalis (A. continentalis) was suspended in water and sequentially partitioned with CHCl3, ethyl acetate (EtOAc), and n-butanol (n-BuOH). The CHCl3 fraction showed the highest activity and an antibacterial compound against S. mutans was isolated from this preparation through various chromatography methods by bioassay guided fractionation. MS, ¹H - NMR and ¹³C-NMR analysis showed that the active principle was continentalic acid which was confirmed to show significant inhibitory effects against S. mutans biofilm. These results may provide some scientific rationale for the traditional use these extracts for the treatment of dental diseases.