Title: Synthesis and study of the pancreatic α-amylase inhibitory activity of methyl acarviosin and its derivatives
Abstract: Pancreatic α-amylase is a target for type 2 diabetes mellitus treatment. However, small molecule inhibitors of α-amylase are currently scarce. In the course of developing small molecule α-amylase inhibitors, we designed and synthesized conjugates of glucose and acarviosin. The synthetic compounds showed mild α-amylase inhibitory activity with higher activity compared with non-glucose conjugated compounds, but lower activity compared to acarviosin. Comparison of these activities revealed transglycosylation of acarviosin during the enzyme reaction. Additionally, the α-amylase inhibitory activity of acarviosin is expressed through these transglycosylation products.