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Molecular Insight and Mode of Inhibition of α-Glucosidase and α-Amylase by Pahangensin A from Alpinia pahangensis Ridl.

Kong Yong LooKok Hoong LeongYasodha SivasothyHalijah IbrahimKhalijah Awang
Published in: Chemistry & biodiversity (2019)
The inhibition of carbohydrate-hydrolyzing enzymes in human digestive organs is crucial in controlling blood sugar levels, which is important in treating type 2 diabetes. In the current study, pahangensin A (1), a bis-labdanic diterpene characterized previously in the rhizomes of Alpinia pahangensis Ridl., was identified as an active dual inhibitor for α-amylase (IC50 =114.80 μm) and α-glucosidase (IC50 =153.87 μm). This is the first report on the dual α-amylase and α-glucosidase inhibitory activities of a bis-labdanic diterpene. The Lineweaver-Burk plots of compound 1 indicate that it is a mixed-type inhibitor with regard to both enzymes. Based on molecular docking studies, compound 1 docked in a non-active site of both enzymes. The dual inhibitory activity of compound 1 makes it a suitable natural alternative in the treatment of type 2 diabetes.
Keyphrases
  • molecular docking
  • type diabetes
  • molecular dynamics simulations
  • endothelial cells
  • ionic liquid
  • cardiovascular disease
  • glycemic control
  • insulin resistance
  • metabolic syndrome
  • adipose tissue
  • smoking cessation