Abstract
Diabetes mellitus (DM) is a disease that is caused by a malfunction of carbohydrate metabolism, which plays an important role in the development of long-term diabetic complications. The excess glucose can be transformed to methylglyoxal (MG), a potential precursor of glycation. Glycation is a spontaneous non-enzymatic reaction that initially yields advanced glycation end-products (AGEs), which ultimately triggers several severe complications. Therefore, the inhibition of AGEs formation is the imperative approach for alleviating diabetic complications. The aim of this research was to investigate the glycation and α-glucosidase inhibitory abilities of compounds isolated from fingerroot. The dichloromethane extract afforded three flavanones, two chalcones, two dihydrochalcones, and one kavalactone. Most of the isolated compounds showed higher inhibition effect against AGEs formation than aminoguanidine (AG). Subsequent evaluation in MG-trapping assay indicated that their trapping potency was relatively comparable to AG. Their structure-activity relationships (SAR) of MG-trapping activity were investigated using the comparison of the structures of flavonoids. In addition, pinocembrin displayed moderate α-glucosidase inhibition against both maltase and sucrose, with IC50 values of 0.35 ± 0.021 and 0.39 ± 0.020 mM, respectively.
Highlights
Diabetes mellitus is a metabolic disease caused by a malfunction of carbohydrate metabolism characterized by high blood glucose level
It can be inferred that the trapping activity of 1 was comparable to that of AG
We examined the pathway in which pinocembrin (1) was preferably preceded, by determining the dissociation constants of EI (Ki ) and ESI (Ki 0 ) complexes (Table 2)
Summary
Diabetes mellitus is a metabolic disease caused by a malfunction of carbohydrate metabolism characterized by high blood glucose level (hyperglycemia). Chronic hyperglycemia in diabetes results in the development of long-term diabetic complication, and associates it with the increased risk of mortality and morbidity [1]. The excess glucose can be transformed to many potential precursors of glycation, such as glyoxal (GO), methylglyoxal (MG), and 3-deoxyglucosone (3-DG). Glycation is a Molecules 2018, 23, 3365; doi:10.3390/molecules23123365 www.mdpi.com/journal/molecules. Molecules 2018, 23, 3365 spontaneous non-enzymatic reaction between reducing sugars or their reactive metabolites such as MG and protein, via rearrangement, oxidation, dehydration, and polymerization to generate advanced glycation-end products (AGEs). Methylglyoxal (MG) is one of the reactive carbonyl species that plays an important role in glycation as a glycation precursor
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