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Non-alcoholic fatty liver disease (NAFLD) is a type of steatosis caused by excess lipids accumulating in the liver. The prevalence of NAFLD has increased annually due to modern lifestyles and a lack of adequate medical treatment. Thus, we were motivated to investigate the bioactive components of Formosan plants that could attenuate lipid droplet (LD) accumulation. In a series of screenings of 3000 methanolic extracts from the Formosan plant extract bank for anti-LD accumulation activity, the methanolic extract of aerial parts of <i>Elaeagnus glabra</i> Thunb. showed excellent anti-LD accumulation activity. <i>E. glabra</i> is an evergreen shrub on which only a few phytochemical and biological studies have been conducted. Here, one new flavonoid (<b>1</b>), two new triterpenoids (<b>2</b> and <b>3</b>), and 35 known compounds (<b>4</b>–<b>38</b>) were isolated from the ethyl acetate layer of aerial parts of <i>E. glabra</i> via a bioassay-guided fractionation process. Their structures were characterized by 1D and 2D NMR, UV, IR, and MS data. Among the isolated compounds, methyl pheophorbide a (<b>37</b>) efficiently reduced the normalized LD content to 0.3% with a concentration of 20 μM in AML12 cell lines without significant cytotoxic effects. 3-<i>O</i>-(<i>E</i>)-Caffeoyloleanolic acid (<b>13</b>) and methyl pheophorbide a (<b>37</b>) showed inhibitory effects on superoxide anion generation or elastase release in fMLP/CB-treated human neutrophils (IC₅₀ < 3.0 μM); they displayed effects similar to those of the positive control, namely, LY294002. These findings indicate that <i>E. glabra</i> can be used for developing a new botanical drug for managing LD accumulation and against inflammation-related diseases.