Flavonoids, triterpenoids, and steroids were isolated from the leaves of Leucoseptrum stellipillum (MIQ.) KITAMURA et MURATA and identified as apigenin, luteolin, chrysoeriol, ursolic acid, pomolic acid, tormentic acid, β-sitosterol, and β-sitosterol glucoside by comparison of their spectral data with those of authentic specimens. Among these compounds, the triterpenoids showed significant antibacterial activities against Streptococcus mutans.