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The methanol extracts of 21 grains were evaluated for inhibitory activities against α-glucosidase and aldose reductase isolated from Sprague Dawley male rats. Among these samples, the methanol extracts of Elymus sibiricus (94%), Fagopyrum esculentum (90%), and Perilla frutescens var. japonica (85%) exhibited highly effective inhibition against α-glucosidase at the concentration of 1 ㎎/mL. At 0.1 ㎎/mL, the extract of E. sibiricus exhibited the most effective inhibition. In tests with aldose reductase, the methanol extracts of F. esculentum (98%), Panicum bisulcatum (96%), Setaria italica (90%), and Sorghum bicolor (98%) exhibited highly effective inhibition at 0.1 ㎎/mL. At the concentration of 0.01 ㎎/mL, the extract of F. esculentum and S. bicolor exhibited an effective inhibition (>80% inhibition). Based on their potent inhibitory activities, the activity of each solvent fraction from three samples was determined, and potent activities were produced from ethyl acetate fraction of E. sibiricus against α-glucosidase and hexane fractions of F. esculentum and S. bicolor against aldose reductase. IC_(50) values of E. sibiricus, F. esculentum, and S. bicolor were 0.10, 0.013, and 0.010 ㎎/mL, respectively. As naturally occurring therapeutic agents, the grains described could be useful for developing new agents or lead compounds as α-glucosidase and aldose reductase inhibitors.
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