The EtOAc extract of Youngia koidzumiana significantly inhibited the diacylglycerol acyltransferase (DGAT) from rat liver microsomes. Bioactivity-guided fractionation led to the isolation of nine compounds, the structures of which were established using physicochemical and spectral data. Of the isolated compounds, oleanolic acid (2), methyl ursolate (7) and corosolic aicd (8) inhibited DGAT, with $IC_{50}$ values of 31.7, 26.4, and $44.3{mu}M$, respectively. However, sesquit-erpenoids showed only weak inhibitory effects toward DGAT.