Inhibition of α-glucosidasesinvolved in the digestion and absorption of carbohydrates can decrease the postprandial increase of blood glucose level after a mixed carbohydrate diet. Therefore, we investigated the changes in α-glucosidase inhibitory activity of wheat during germination process. We also investigated total phenolics and oxygen radical absorbance capacity (ORAC) during germination process of wheat. Wheat was germinated for 0, 12, 24 and 48 hrs and results showed that both phenolic contents and α-glucosidase inhibitory activities increased with germination time. More specifically, total phenolic content increased from (293mg/100g-F.W.) at 0 hrs germination to a high (4,082mg/100g-F.W.) achieved after 48 hrs germination. Additionally, alpha-glucosidase inhibitory activity was dramatically increased from a low 10% inhibition at 0 hrs germination to a high 60% inhibitory activity observed at 48 hrs. These results suggest that wheat, depending on the germination time, has the potential to contribute as a dietary supplement for controlling hyperglycemia and oxidative stress-linked diabetes complications. It may due to the natural response of plant seed to overcome the biotic/abiotic stress from environment during germination period.