Flowers of Erigeron annuus L. were extracted with 80% aqueous MeOH, and the concentrated extract was partitioned with EtOAc, n-BuOH, and H2O. Repeated silica gel and ODS column chromatography of the EtOAc fraction led to the isolation of a sterol, through activity-guided fractionation, using ACAT inhibitory activity measurements. From the physico-chemical data, including NMR, MS, and IR, the chemical structure of the compound was determined to be an ergosterol peroxide (1), which has been isolated for the first time from this plant. This compound exhibited hACAT-1 and Lp-PLA2 inhibitory effects, with inhibitory values of 51.6 +/- 0.9 and 51.7 +/- 1.2%, at a treatment concentration of 0.23 mM.