Affiliations 

  • 1 Department of Pharmacy, Faculty of Medicine, University of Malaya, 50603, Kuala Lumpur, Malaysia
  • 2 Research Center for Crystalline Materials, Faculty of Science and Technology, Sunway University, 47500, Bandar Sunway, Selangor Darul Ehsan, Malaysia
  • 3 Institute of Biological Sciences, Faculty of Science, University of Malaya, 50603, Kuala Lumpur, Malaysia
  • 4 Center for Natural Product and Drug Discovery (CENAR), Department of Chemistry, Faculty of Science, University of Malaya, 50603, Kuala Lumpur, Malaysia
Chem Biodivers, 2019 Jun;16(6):e1900032.
PMID: 30957403 DOI: 10.1002/cbdv.201900032

Abstract

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.

* Title and MeSH Headings from MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.