Fragaria nubicola, known as Tibetan strawberry, is an edible plant possessing various health-promoting effects. However, its functional compositions were rarely studied. In this work, monoamine oxidase B (MAO-B) inhibitors in this plant were rapidly screened using the enzyme-functionalized magnetic nanoparticles coupled with UPLC-QTOF-MS. Two inhibitors, quercetin-3-O-β-D-glucuronide-6″-methyl ester (1) and kaempferol-3-O-β-D-glucuronide-6″-methyl ester (2), were identified from this plant with the IC 50 values of 19.44 ± 1.17 and 22.63 ± 1.78 μM, respectively. Enzyme kinetic analysis and molecular docking were carried out to investigate the mechanism of inhibition. Contents of both compounds as well as those of total phenolics and flavonoids were quantified to be 24.76