Journal
MOLECULES
Volume 23, Issue 8, Pages -Publisher
MDPI
DOI: 10.3390/molecules23081998
Keywords
Lens culinaris; flavonol glycoside; dipeptidyl peptidase IV; diabetes; molecular docking analysis
Funding
- Radiation Technology R&D program through the National Research Foundation of Korea (NRF) - Ministry of Science, ICT & Future Planning [2017M2A2A6A05018541]
- National Research Foundation of Korea [2017M2A2A6A05018541] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
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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 (1-3) were isolated from the seeds of Lens culinaris Medikus (Fabaceae) and tested for their DPP-IV-inhibitory activity. We demonstrated for the first time, that compounds 1-3 inhibited DPP-IV activity in a concentration-dependent manner in our in vitro bioassay system. In addition, molecular docking experiments of compounds 1-3 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.
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