Intestinal glucose absorption/inhibition activity by natural bioactive compounds is considered a new strategy for prevention/treatment of uncontrolled hyperglycemia and diabetes as well as chronic human metabolic disorders. This mini review provides scientific evidence of the contribution of natural bioactive nutrients to inhibit glucose absorption in the small bowel. Many studies were realized on intestinal glucose transport in vitro and on postprandial glucose levels in vivo. In this context, the main designated constituents are ()-catechin, ()-epicatechin, ()-epigallocatechin, epicatechingallate, tannic acid, resveratrol, and chlorogenic acid. The therapeutic approaches are to retard the absorption of glucose by inhibition of carbohydrate-hydrolyzing enzymes such as intestinal glycosidases (α-amylase and α-glycosidase) and the inhibition of intestinal Na+-dependent glucose absorption mediated by reduced expression of glucose transporter (SGLT1). These studies revealed that natural bioactive compounds, as potential candidates, can be designed as natural products for the development of novel functional foods or nutraceuticals to relieve hyperglycemia/diabetes.
