Mulberry leaves are rich in 1-deoxynojirimycin (DNJ) and 2-O-α-D-galactopyranosyl-deoxynojirimycin (GAL-DNJ). Compared to DNJ, the bioactive potency of GAL-DNJ is low. We proposed that the conversion of GAL-DNJ into DNJ may improve its bioavailability. We evaluated this hypothesis and constructed a novel enzymatic-based method to induce the hydrolysis of GAL-DNJ to DNJ in order to improve the therapeutic potency of mulberry leaves.