A Review of the In Vitro Inhibition of α-Amylase and α-Glucosidase by Chalcone Derivatives

Abstract

Diabetes mellitus is a chronic metabolic disease relating to steady hyperglycemia resulting from the impairment of the endocrine and non-endocrine systems. Many new drugs having varied targets were discovered to treat this disease, especially type 2 diabetes. Among those, α-glucosidase inhibitors showed their effects by preventing the digestion of carbohydrates through their inhibition against α-amylase and αglucosidase. Recently, chalcones have attracted considerable attention as they have a simple structure, are easily synthesized as well as have a variety of derivatives. Some reports suggested that chalcone and its derivates could inhibit α-amylase and α-glucosidase. This narrative review provides a comprehensive evaluation of the inhibition of chalcone and its derivatives against α-amylase and α-glucosidase that were reviewed and reported in published scientific articles. Twenty-eight articles were reviewed after screening 207 articles found in four databases, including PubMed, Google Scholar, VHL (Virtual Health Library), and GHL (Global Health Library). This review presented the inhibitory effects of varied chalcones, including chalcones with a basic structural framework, azachalcones, bis-chalcones, chalcone oximes, coumarinchalcones, cyclohexane chalcones, dihydrochalcones, and flavanone-coupled chalcones. Many of these chalcones had significant inhibition against α-amylase as well as α-glucosidase that were comparable to or even stronger than standard inhibitors. This suggested that such compounds could be potential candidates for the discovery of new anti-diabetic remedies in the years to come.

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“…α-amylase breaks down α-linked polysaccharides into smaller oligosaccharides, while α-glucosidases are membrane-bound enzymes in the small intestine that hydrolyze carbohydrate species into absorbable monosaccharides, such as glucose [ 41 ]. α-amylase and α-glucosidase inhibitors can help manage hyperglycemia as a promising approach to the management of type 2 diabetes by delaying the breakdown of carbohydrates, which lowers postprandial plasma glucose levels [ 42 , 43 , 44 ]. The ellagic acid derivatives 3,3′-di-O-methyl ellagic acid, 3,3′,4′-tri-O-methyl ellagic acid-4-O-β-D-xylopyranoside, 3,3′,4′-tri-O-methyl ellagic acid-4-O-β-D-glucopyranoside, and 3,3′-di-O-methyl ellagic acid-4-O-β-D-glucopyranoside, as well as the flavonoid myricetin-3-O-rhamnoside, exhibited moderate to good antidiabetic activity compared to the standard acarbose.…”

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“…Furthermore, UHPLC-HRMSMS analysis revealed a precursor ion [(M + HCOOH)-H]at m/z 557.2609. Fragment ions at m/z 511, attributed to the loss of formic acid, and at m/z 349, originating from the further loss of a dehydrated hexose moiety, were associated with amygdalin (23). 1.…”

“…Additionally, the inhibition of carbohydrate hydrolysing enzymes (α-amylase and α-glucosidase), and pancreatic lipase was one of the most applied preventing approaches to counteract MetS and obesity. In fact, the inhibition of carbohydrate hydrolysing enzymes delays the carbohydrate digestion with a consequent hypoglycaemic effect, whereas the inhibition of pancreatic lipase reduces the absorption of ingested fats with a consequent hypolipidemic effect [23,24].…”