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- Title
DPP-IV Inhibitory Potentials of Flavonol Glycosides Isolated from the Seeds of Lens culinaris: In Vitro and Molecular Docking Analyses.
- Authors
Kim, Bo-Ram; Kim, Hyo Young; Kim, Jin-Baek; Jin, Chang Hyun; Han, Ah-Reum; Choi, Inhee
- Abstract
Dipeptidyl peptidase IV (DPP-IV), a new target for the treatment of type 2 diabetes mellitus, degrades incretins such as glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic polypeptide. DPP-IV inhibitors shorten the inactivation of GLP-1, permitting the incretin to stimulate insulin release, thereby combating hyperglycemia. In our ongoing search for new DPP-IV inhibitors from medicinal plants and foods, three flavonol glycosides (<bold>1</bold>–<bold>3</bold>) were isolated from the seeds of <italic>Lens culinaris</italic> Medikus (Fabaceae) and tested for their DPP-IV–inhibitory activity. We demonstrated for the first time, that compounds <bold>1</bold>–<bold>3</bold> inhibited DPP-IV activity in a concentration-dependent manner in our in vitro bioassay system. In addition, molecular docking experiments of compounds <bold>1</bold>–<bold>3</bold> within the binding pocket of DPP-IV were conducted. All investigated compounds readily fit within the active sites of DPP-IV, in low-energy conformations characterized by the flavone core structure having optimal electrostatic attractive interactions with the catalytic triad residues of DPP-IV.
- Subjects
FLAVONOL glycosides; LENTILS; TREATMENT of diabetes; CD26 antigen; GLUCAGON-like peptide 1; MOLECULAR docking
- Publication
Molecules, 2018, Vol 23, Issue 8, p1998
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules23081998