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

页码：8429 / 8433

页数：5

共 34 条

[1] Identification of Breast Cancer Inhibitors Specific for G Protein-Coupled Estrogen Receptor (GPER)-Expressing Cells [J].