Abstract
Flavonoids are known to play a role in hypoglycemia by inhibiting α-glucosidase. However, their interaction mechanism with α-glucosidase still needs to be elaborated. In this study, the α-glucosidase inhibitory activities of 15 flavonoids were investigated. Their molecular volume had a negative effect on inhibitory activity, while the number of phenolic hydroxyl groups on the B ring was positively correlated with inhibitory activity. To explain the significant differences in activity, the interaction behaviors of myricetin and dihydromyricetin, which have similar structures, were compared by spectrofluorimetry, molecular docking, and the independent gradient model (IGM). In the fluorescence analysis, myricetin exhibited a higher binding capacity. Based on molecular docking and IGM analysis, their non-covalent interactions with α-glucosidase could be visualized and quantified. It was found that they had different binding modes with the enzymes and that myricetin possessed stronger hydrogen bonding and van der Waals force interactions, which explained the thermodynamic results.
Highlights
Diabetes mellitus is one of the most serious and chronic diseases characterized by hyperglycemia, which can lead to many complications including nephropathy, neuropathy, and cardiovascular diseases [1,2]
Ring had a positive effect on their inhibitory activity. The former might be due to the large molecular size of flavonoid glycosides, which hindered their access to the enzyme
The molecular docking results suggested that they had different orientations in the active center of α-glucosidase
Summary
Diabetes mellitus is one of the most serious and chronic diseases characterized by hyperglycemia, which can lead to many complications including nephropathy, neuropathy, and cardiovascular diseases [1,2]. Its incidence is rising rapidly with the ageing population and increase in obesity. Its incidence is predicted to increase from 2.8% (171 million) in the year 2000 to 4.4% (366 million) by the year 2030 [3]. Of diabetes cases, and postprandial blood glucose plays a key role in the development of type II diabetes and its complications [4]. One effective strategy for controlling postprandial hyperglycemia is to delay glucose absorption by using α-glucosidase inhibitors [5]. Synthetic α-glucosidase inhibitors (acarbose, miglitol, and voglibose) all have drawbacks such as hepatotoxicity and adverse gastrointestinal symptoms, which necessitate the search for safer and more effective alternatives [3]
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