Goji berry is a famous edible and medicinal substance around the world. In this research, 15 phenylpropionyl phenylethylamine derivatives (1−15), including one new compound (1), were separated and identified from goji berry. All isolates were elucidated via extensive nuclear magnetic resonance spectral analyses and chemical techniques. Six known isolates were first obtained from Lycium genus. Six isolates were effectively split into double chromatographic peaks accompanied by the basically identical areas, indicating they belong to racemates. The oxygen radical absorbance capacity (ORAC) experiment indicated that all isolates displayed a capacity of scavenging free radicals, and most of them exhibited higher ORAC than epigallocatechingallate. In ethanol/palmitic acid-established in vitro hepatocyte injury model, four phenylpropionyl phenylethylamine derivatives (1, 2, 9, and 15) significantly alleviated hepatocyte injury, among which compound 1 exerted the strongest protective activity. Notably, the hepatoprotective effect of compound 1 was further confirmed in ethanol-established liver damage mouse model, reflected by the reduction of lipid accumulation and the attenuation of pathological alteration. Combined with the in vitro results, the in vivo observations suggested that compound 1 suppressed cell apoptosis and the outburst of inflammation. Our findings provided first-hand evidence proving that goji berry-derived phenylpropionyl phenylethylamine derivatives hold a potential in treating alcoholic liver disease.