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Type 2 diabetes (T2D) is one of the most prevalent metabolic diseases worldwide and is characterized by increased postprandial hyperglycemia (PPHG). α-Amylase and α-glucosidase inhibitors have been shown to slow the release of glucose from starch and oligosaccharides, resulting in a delay of glucose absorption and a reduction in postprandial blood glucose levels. Since current α-glucosidase inhibitors used in the management of T2D, such as acarbose, have been associated to strong gastrointestinal side effects, the search for novel and safer drugs is considered a hot topic of research. Flavonoids are phenolic compounds widely distributed in the Plant Kingdom and important components of the human diet. These compounds have shown promising antidiabetic activities, including the inhibition of α-amylase and α-glucosidase. The aim of this review is to provide an overview on the scientific literature concerning the structure-activity relationship of flavonoids in inhibiting α-amylase and α-glucosidase, including their type of inhibition and experimental procedures applied. For this purpose, a total of 500 compounds is covered in this review. Available data may be considered of high value for the design and development of novel flavonoid derivatives with effective and potent inhibitory activity against those carbohydrate-hydrolyzing enzymes, to be possibly used as safer alternatives for the regulation of PPHG in T2D.

Flavonoids as potential agents in the management of type 2 diabetes through the modulation of α-amylase and α-glucosidase activity: a review