Inhibition of Human Salivary and Pancreatic α-Amylase by Resveratrol Oligomers
Year: 2024
Type: article
Abstract: High Resolution Image Download MS PowerPoint Slide A key strategy to mitigate postprandial hyperglycemia involves inhibiting α-amylases, which commence the starch digestion process in the gut. This study examined the inhibitory effects of resveratrol and stilbenoid tetramers, vaticanol B, (−)-hopeaphenol, and vatalbinoside A on human salivary and pancreatic α-amylases experimentally and through molecular docking studies. Vaticanol B demonstrated the most potent inhibition with IC 50 values of 5.3 ± 0.3 μM for salivary and 6.1 ± 0.5 μM for pancreatic α-amylase (compared to acarbose with IC 50 values of 1.2 ± 0.1 μM and 0.5 ± 0.0 μM, respectively). Kinetic analysis suggested a competitive inhibition mode for vaticanol B. Resveratrol and vatalbinoside A were poor inhibitors of human α-amylases, while (−)-hopeaphenol exhibited moderate inhibition. Molecular docking supported the inhibition data, and several aspects of the structural configurations explained the stronger inhibition exerted by vaticanol B. Overall, vaticanol B shows promise as a natural alternative to acarbose for inhibiting α-amylase.
Source: Journal of Medicinal Chemistry
Language: English
Subfield: Endocrinology, Diabetes and Metabolism
Field: Medicine
Domain: Health Sciences
Open Access status: hybrid
Estimated APC paid: $4,500
Awards: Regional nuclear magnetic resonance infrastructure network for South East Queensland and Northern New South Wales, Upgrade of existing university low field and high field nuclear magnetic resonance facilities, Identification of new antibacterial agents that inhibit type III secretion, Mass Spectrometry Instrumentation for Therapeutic Lead Discovery, High-value functional ingredients from bean processing waste
OpenAlex ID: W4404115682