Tiliroside, a glycosidic flavonoid, possesses anti-diabetic activities. Tiliroside is a noncompetitive inhibitor of α-amylase with a Ki value of 84.2? μM. Tiliroside inhibits carbohydrate digestion and glucose absorption in the gastrointestinal tract.In Vitro: Tiliroside inhibits pancreatic α-amylase (IC50=0.28?mM) in vitro.In Vivo: In male ICR mice, the increase in postprandial plasma glucose levels was significantly suppressed in the Tiliroside-administered group.