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Quercetin‐3‐Oleate Contributes to Skin Wound Healing Targeting FFA1/GPR40
Author(s) -
Carullo Gabriele,
Governa Paolo,
Leo Antonio,
Gallelli Luca,
Citraro Rita,
Cione Erika,
Caroleo Maria Cristina,
Biagi Marco,
Aiello Francesca,
Manetti Fabrizio
Publication year - 2019
Publication title -
chemistryselect
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.437
H-Index - 34
ISSN - 2365-6549
DOI - 10.1002/slct.201902572
Subject(s) - hacat , wound healing , free fatty acid receptor 1 , in vitro , chemistry , pharmacology , quercetin , receptor , microbiology and biotechnology , biochemistry , medicine , biology , agonist , immunology , antioxidant
The hybrid molecule Quercetin‐3‐oleate (AV2), accommodates within the binding pocket for allosteric full GPR40 agonists. AV2 endorses skin wound healing acting as a promoter of keratinocytes proliferation and overcomes immunosuppressive conditions in vitro . AV2 stimulated HaCaT wound healing by 51% compared to the untreated control, at the concentration of 1 μM with slight TGF‐β production and MMP‐9 release. Pretreatment with the known GPR40 antagonist DC260126 abolished its wound healing power. Docking simulations suggested that both molecules share the same binding site.