Inhibitory effects of Citrus flavonoids on starch digestion and antihyperglycemic effects in HepG2 cells.

Flavonoids are a class of important bioactive natural products and are being extensively used in functional foods. In the present study, the effects of four Citrus flavonoids (i.e., hesperidin, naringin, neohesperidin, and nobiletin) on amylase-catalyzed starch digestion, major digestive enzyme activities (e.g., pancreatic α-amylase and α-glucosidase), and glucose use in HepG2 cells were investigated. The results showed that all of the tested Citrus flavonoids significantly inhibited amylase-catalyzed starch digestion. Moreover, naringin and neohesperidin mainly inhibited amylose digestion, whereas hesperidin and nobiletin inhibited both amylose and amylopectin digestion. However, these flavonoids showed weak inhibitory activities against digestive enzymes. Furthermore, glucose consumption, glycogen concentration, and glucokinase activity were significantly elevated, and glucose-6-phosphatase activity was markedly decreased by Citrus flavonoids. These results demonstrate that Citrus flavonoids play important roles in preventing the progression of hyperglycemia, partly by binding to starch, increasing hepatic glycolysis and the glycogen concentration, and lowering hepatic gluconeogenesis. This work suggests that Citrus flavonoids might be potentially used for the prevention of postprandial hyperglycemia.