The conformational analysis of glycosidases affords a route to their specific inhibition through transition-state mimicry. Inspired by the rapid reaction rates of cyclophellitol and cyclophellitol aziridine-both covalent retaining β-glucosidase inhibitors-we postulated that the corresponding carba "cyclopropyl" analogue would be a potent retaining β-glucosidase inhibitor for those enzymes react...

The identification of naturally occurring α-glucosidase inhibitors has been actively pursued with the aim of developing therapeutics for the treatment of type 2 diabetes mellitus. To identify α-glucosidase inhibitors, we screened 40 natural compounds, including flavonoids and phenolics, using the structure-based molecular docking approach. The rank of each compound was determined on the basis o...

The aim of this work was to evaluate the inhibitory activities of methanolic extracts of Artocarpus altilis, Cinnamomum zeylanicum, Piper betel and Artocarpus heterophyllus on Wheat alpha amylase and Baker’s yeast alpha glucosidase at varying concentrations. Diabetes mellitus is a clinical condition characterized by hyperglycaemia in which an elevated amount of glucose circulates in the blood p...

A new approach for the discovery and subsequent structural elucidation of oligosaccharide-based inhibitors of -amylases based upon autoglucosylation of known -glucosidase inhibitors is presented. This concept, highly analogous to what is hypothesized to occur with acarbose, is demonstrated with the known -glucosidase inhibitor, D-gluconohydroximino-1,5-lactam. This was transformed from an inhib...

Diabetes mellitus (DM) is recognized as a serious global health problem that is characterized by high blood sugar levels. Type 2 DM is more common in diabetic populations. In this type of DM, inhibition of α-glucosidase is a useful treatment to delay the absorption of glucose after meals. As a megabiodiversity country, Indonesia still has a lot of potential unexploited forests to be developed a...

Polyphenolic compounds are known to be useful in formulating of nutritional or medicinal supplements for the treatment of several diseases. An important activity of polyphenols is the inhibition of digestive enzymes, especially carbohydrate-hydrolyzing enzymes such as α-amylase and α-glucosidase. Inhibitors of these enzymes are able to retard carbohydrate digestion, thus causing a reduction in ...

In this study, in vitro inhibitory activity of methanolic and chloroform extracts of some medicinal plants including C. wightii, T. ammi, N. sativa, C. arabica, L. usitatissimum, C. cyminum, and R. Graveolens was evaluated toward α-glucosidase, α-amylase, and lipase comparing with acarbose and orlistat as the standard inhibitors. Our results revealed that both methanolic and chloroform extracts...