Grain bound polyphenols: Molecular interactions, release characteristics, and regulation mechanisms of postprandial hyperglycemia

Frequent postprandial hyperglycemia causes many chronic diseases. Grain polyphenols are widely recognized as natural active ingredients with high potential to treat chronic diseases due to their excellent postprandial hyperglycemic regulating effects. However, previous studies on polyphenols in grains mainly focused on the functional properties of free polyphenols and the extraction and physicochemical properties of bound polyphenols, ignoring the functional properties of bound polyphenols. Comprehensively understanding the binding properties of grain bound polyphenols (GBPs) and their mechanisms in regulating blood glucose levels is essential for developing and applying grain resources. This review summarizes the molecular interactions between GBPs and grain components and their effects on release characteristics and bioavailability at various stages. Meanwhile, the review focuses on elucidating the regulatory mechanism of post-release GBPs on postprandial hyperglycemia levels, incorporating insights from molecular docking, the gastrointestinal-brain axis, and gut flora. GBPs slow food digestion by occupying the active site of digestive enzymes and altering the secondary structure of enzymes and the hydrophobic environment of amino acid residues to inhibit enzyme activity. They modulate intestinal epithelial transport proteins (SGLT1, GLUT2, and GLUT4) to limit glucose absorption and increase glucose consumption. They also stimulate the release of short-term satiety hormones (CKK, GLP-1, and PYY) through the gastrointestinal-brain axis to decrease post-meal food intake. Furthermore, they optimize gut microbiota composition, promoting short-chain fatty acid production and bile acid metabolism. Therefore, developing functional foods with glucose-modulating properties based on GBPs is crucial for obesity prevention, diabetes management, and low-GI food development.