Aldose reductase (AR), the key enzyme of the polyol pathway, is known to play important roles in the diabetic complication. The inhibitors of AR, therefore, would be potential agents for the prevention of diabetic complication. The AR inhibition activity of several isoflavonoids was evaluated in vitro against rat lens. Tectoridin-4′-O-β-d-glucoside exhibited strong AR inhibition activity on rat lens with an IC 50 of 0.54μM. Similar activities were recorded for the natural tectorigenin and tectoridin. In contrast, tectoridin-4′-O-β-d-glucoside showed a stronger inhibitory activity than tectorigenin and tectoridin. Our results indicate that glucose conjugation position in this type of isoflavonoids may be required for the activity.