Quercetin-3-Oleate Contributes to Skin Wound Healing Targeting FFA1/GPR40

被引：27
|
作者：
Carullo, Gabriele [1 ]
Governa, Paolo [2 ]
Leo, Antonio [3 ,4 ]
Gallelli, Luca [3 ,4 ]
Citraro, Rita [3 ,4 ]
Cione, Erika [1 ]
Caroleo, Maria Cristina [1 ]
Biagi, Marco [5 ]
Aiello, Francesca [1 ]
Manetti, Fabrizio [2 ]
机构：
[1] Univ Calabria, Dept Excellence 2018 2022, Dept Pharm Hlth & Nutr Sci, Edificio Polifunz, I-87036 Arcavacata Di Rende, CS, Italy
[2] Univ Siena, Dept Excellence 2018 2022, Dept Biotechnol Chem & Pharm, Via Aldo Moro 2, I-53100 Siena, Italy
[3] Univ Catanzaro, Dept Hlth Sci, Viale Europa, I-88100 Catanzaro, Italy
[4] MaterDomini Hosp, Clin Pharmacol & Pharmacovigilance Unit, Viale Europa, I-88100 Catanzaro, Italy
[5] Univ Siena, Dept Phys Sci Hearth & Environm, Via Laterina 8, I-53100 Siena, Italy
来源：
CHEMISTRYSELECT | 2019年 / 4卷 / 29期
关键词：
Quercetin-3-oleate; wound healing; FFA1; GPR40; Docking simulations; immunomodulation; MIGRATION; INHIBITORS; GROWTH; REPAIR;
D O I：
10.1002/slct.201902572
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
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 mu M with slight TGF-beta 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.
引用
收藏
页码：8429 / 8433
页数：5
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