Diabetic foot ulcer is becoming a social problem that affects patients, even at a young age. Several treatments are available but these are invasive and new compounds from natural sources are emerging as new tools for skin repair. From these, the flavonoid quercetin showed good properties although its easy autoxidation limited its therapeutic use [1]. In this context, a lipase-catalyzed esterification with oleic acid was proposed to overcome this limitation [2]. The hybrid quercetin-3-oleate showed good proliferative effects in keratinocyte HaCat cell line and an in intracellular TGFβ expression in skin fibroblast RAT-1 cell line. Docking simulations suggested that the compound could interact with both GPR40 and GPR120 receptors. The hybrid was efficacious in an animal model of skin wounds. In patients affected by diabetic foot ulcer, it favored the wound closure in 3-7 days. In conclusion, the topical administration of quercetin-3- oleate hybrid may represent an effective new pharmacological tool for skin repair.

Proceedings of the Merck & Elsevier Young Chemists Symposium (MEYCS 2018)

Gabriele Carullo;Francesca Aiello
Conceptualization
;
Erika Cione;Mariarita Perri;Mariateresa Badolato;DE LEO, ANTONIO;Maria Cristina Caroleo;
2018

Abstract

Diabetic foot ulcer is becoming a social problem that affects patients, even at a young age. Several treatments are available but these are invasive and new compounds from natural sources are emerging as new tools for skin repair. From these, the flavonoid quercetin showed good properties although its easy autoxidation limited its therapeutic use [1]. In this context, a lipase-catalyzed esterification with oleic acid was proposed to overcome this limitation [2]. The hybrid quercetin-3-oleate showed good proliferative effects in keratinocyte HaCat cell line and an in intracellular TGFβ expression in skin fibroblast RAT-1 cell line. Docking simulations suggested that the compound could interact with both GPR40 and GPR120 receptors. The hybrid was efficacious in an animal model of skin wounds. In patients affected by diabetic foot ulcer, it favored the wound closure in 3-7 days. In conclusion, the topical administration of quercetin-3- oleate hybrid may represent an effective new pharmacological tool for skin repair.
978-88-94952-03-2
File in questo prodotto:
Non ci sono file associati a questo prodotto.

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/20.500.11770/292681
 Attenzione

Attenzione! I dati visualizzati non sono stati sottoposti a validazione da parte dell'ateneo

Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus ND
  • ???jsp.display-item.citation.isi??? ND
social impact