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DPP-IV Inhibitory Potentials of Flavonol Glycosides Isolated from the Seeds of Lens culinaris: In Vitro and Molecular Docking Analyses.


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 (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.

SUBMITTER: Kim BR 

PROVIDER: S-EPMC6222902 | biostudies-literature | 2018 Aug

REPOSITORIES: biostudies-literature

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DPP-IV Inhibitory Potentials of Flavonol Glycosides Isolated from the Seeds of <i>Lens culinaris</i>: In Vitro and <i>Molecular Docking</i> Analyses.

Kim Bo-Ram BR   Kim Hyo Young HY   Choi Inhee I   Kim Jin-Baek JB   Jin Chang Hyun CH   Han Ah-Reum AR  

Molecules (Basel, Switzerland) 20180810 8


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 (<b>1</b>⁻<b>3</b>) were isolated from the seeds o  ...[more]

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