The polyphenol fraction of Actinidia arguta (AP) inhibited α-glucosidase activity in vitro. The oral administration of AP with maltose and starch suppressed postprandial hyperglycemia associated with the intake of the respective sugars by rats. The area under the curve (AUC) of blood glucose in the oral glucose tolerance test (OGTT) of type 2 diabetic KK-A y mice, fed AP for 6 weeks, significantly decreased when compared with that of the control group. The fraction containing isoquercitrin and hyperoside, which was prepared from AP, showed a stronger inhibitory activity for maltase. The blood glucose levels in OGTT of KK-A y mice fed isoquercitrin for 4 weeks tended to be lower at 60 min after the administration of glucose.These results suggested that AP has antidiabetic effects, and isoquercitrin, a component of AP, may be useful in preventing type 2 diabetes mellitus. A decrease in the G6Pase activity and increase in the ACO or CPT activities in the liver of KK-A y mice fed AP or isoquercitrin suggested that the suppression of gluconeogenesis and the enhancement of β-oxidation of lipids, as well as the inhibition of maltase by AP and isoquercitrin, might also be related to their anti-diabetic effects.