To evaluate therapeutic efficacy of aldose reductase (AR) inhibition, the seeds of Perilla frutescens var. japonica (PF) were tested for inhibition of AR. The stepwise polarity fractions of PF were tested. The CH2Cl2 and EtOAc fractions showed highest activities (IC50 5.47 and 3.63 μg/mL, respectively). Compounds 1-5 were isolated from the CH2Cl2 and EtOAc fractions by silica-gel and LH-20 Sephadex. Their structures were elucidated as β-sitosterol (1), diosmetin (2), kaempferol (3), luteolin (4), and apigenin (5). Compounds 1-5 were exhibited AR inhibitory. Among them, luteolin (4) and apigenin (5) exhibited AR inhibitory activities (IC50 0.40 and 1.10 μg/mL, respectively). Our results demonstrated that PF could be a worthy natural source for curing against diabetic complications.