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Abstract
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.