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Molecules 2018, 23(8), 1998; https://doi.org/10.3390/molecules23081998

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

1
Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute, Jeongeup-si, Jeollabuk-do 56212, Korea
2
Institut Pasteur Korea, Seongnam-si, Gyeonggi-do 13488, Korea
*
Author to whom correspondence should be addressed.
Received: 23 July 2018 / Revised: 8 August 2018 / Accepted: 8 August 2018 / Published: 10 August 2018
(This article belongs to the Special Issue Natural Product Isolation, Identification and Biological Activity)
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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 (13) 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 13 inhibited DPP-IV activity in a concentration-dependent manner in our in vitro bioassay system. In addition, molecular docking experiments of compounds 13 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. View Full-Text
Keywords: Lens culinaris; flavonol glycoside; dipeptidyl peptidase IV; diabetes; molecular docking analysis Lens culinaris; flavonol glycoside; dipeptidyl peptidase IV; diabetes; molecular docking analysis
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Kim, B.-R.; Kim, H.Y.; Choi, I.; Kim, J.-B.; Jin, C.H.; Han, A.-R. DPP-IV Inhibitory Potentials of Flavonol Glycosides Isolated from the Seeds of Lens culinaris: In Vitro and Molecular Docking Analyses. Molecules 2018, 23, 1998.

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