Pinocembrin and its linolenoyl ester derivative induce wound healing activity in HaCaT cell line potentially involving a GPR120/FFA4 mediated pathway
Articolo
Data di Pubblicazione:
2021
Citazione:
Pinocembrin and its linolenoyl ester derivative induce wound healing activity in HaCaT cell line potentially involving a GPR120/FFA4 mediated pathway / S. Mazzotta, P. Governa, V. Borgonetti, P. Marcolongo, C. Nanni, A. Gamberucci, F. Manetti, F. Pessina, G. Carullo, A. Brizzi, F. Aiello. - In: BIOORGANIC CHEMISTRY. - ISSN 0045-2068. - 108:(2021 Mar), pp. 104657.1-104657.9. [10.1016/j.bioorg.2021.104657]
Abstract:
Wound healing represents an urgent need from the clinical point of view. Several diseases result in wound conditions which are difficult to treat, such as in the case of diabetic foot ulcer. Starting from there, the medicinal research has focused on various targets over the years, including GPCRs as new wound healing drug targets. In line with this, GPR120, known to be an attractive target in type 2 diabetes drug discovery, was studied to finalize the development of new wound healing agents. Pinocembrin (HW0) was evaluated as a suitable compound for interacting with GPR120, and was hybridized with fatty acids, which are known endogenous GPR120 ligands, to enhance the wound healing potential and GPR120 interactions. HW0 and its 7-linolenoyl derivative (HW3) were found to be innovative wound healing agents. Immunofluorescence and functional assays suggested that their activity was mediated by GPR120, and docking simulations showed that the compounds could share the same pocket occupied by the known GPR120 agonist, TUG-891.
Tipologia IRIS:
01 - Articolo su periodico
Keywords:
FFA4; GPR120; HaCaT cell line; Molecular docking; Pancreatic porcine lipase; Pinocembrin; PUFAs; TUG-891; Wound healing; β-arrestin; Cell Survival; Cells, Cultured; Dose-Response Relationship, Drug; Esters; Flavanones; Humans; Linolenic Acids; Molecular Docking Simulation; Molecular Structure; Receptors, G-Protein-Coupled; Structure-Activity Relationship; Wound Healing;
Elenco autori:
S. Mazzotta, P. Governa, V. Borgonetti, P. Marcolongo, C. Nanni, A. Gamberucci, F. Manetti, F. Pessina, G. Carullo, A. Brizzi, F. Aiello
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