Novel Locally Active Estrogens Accelerate Cutaneous Wound Healing-Part 2

Abstract Estrogen deprivation is associated with delayed healing, while estrogen replacement therapy (ERT) accelerates acute wound healing and protects against development of chronic wounds. However, current estrogenic molecules have undesired systemic effects, thus the aim of our studies is to gene...

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Autores principales:	Mario Brufani, Nicoletta Rizzi, Clara Meda, Luigi Filocamo, Francesca Ceccacci, Virginia D’Aiuto, Gabriele Bartoli, Angela La Bella, Luisa M. Migneco, Rinaldo Marini Bettolo, Francesca Leonelli, Paolo Ciana, Adriana Maggi
Formato:	article
Lenguaje:	EN
Publicado:	Nature Portfolio 2017
Materias:	Medicine R Science Q
Acceso en línea:	https://doaj.org/article/0f04ac462ec840b896f7ee6f46151370
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spelling	oai:doaj.org-article:0f04ac462ec840b896f7ee6f461513702021-12-02T11:40:52ZNovel Locally Active Estrogens Accelerate Cutaneous Wound Healing-Part 210.1038/s41598-017-02820-y2045-2322https://doaj.org/article/0f04ac462ec840b896f7ee6f461513702017-05-01T00:00:00Zhttps://doi.org/10.1038/s41598-017-02820-yhttps://doaj.org/toc/2045-2322Abstract Estrogen deprivation is associated with delayed healing, while estrogen replacement therapy (ERT) accelerates acute wound healing and protects against development of chronic wounds. However, current estrogenic molecules have undesired systemic effects, thus the aim of our studies is to generate new molecules for topic administration that are devoid of systemic effects. Following a preliminary study, the new 17β-estradiol derivatives 1 were synthesized. The estrogenic activity of these novel compounds was evaluated in vitro using the cell line ERE-Luc B17 stably transfected with an ERE-Luc reporter. Among the 17β-estradiol derivatives synthesized, compounds 1e and 1f showed the highest transactivation potency and were therefore selected for the study of their systemic estrogenic activity. The study of these compounds in the ERE-Luc mouse model demonstrated that both compounds lack systemic effects when administered in the wound area. Furthermore, wound-healing experiments showed that 1e displays a significant regenerative and anti-inflammatory activity. It is therefore confirmed that this class of compounds are suitable for topical administration and have a clear beneficial effect on wound healing.Mario BrufaniNicoletta RizziClara MedaLuigi FilocamoFrancesca CeccacciVirginia D’AiutoGabriele BartoliAngela La BellaLuisa M. MignecoRinaldo Marini BettoloFrancesca LeonelliPaolo CianaAdriana MaggiNature PortfolioarticleMedicineRScienceQENScientific Reports, Vol 7, Iss 1, Pp 1-14 (2017)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine R Science Q
spellingShingle	Medicine R Science Q Mario Brufani Nicoletta Rizzi Clara Meda Luigi Filocamo Francesca Ceccacci Virginia D’Aiuto Gabriele Bartoli Angela La Bella Luisa M. Migneco Rinaldo Marini Bettolo Francesca Leonelli Paolo Ciana Adriana Maggi Novel Locally Active Estrogens Accelerate Cutaneous Wound Healing-Part 2
description	Abstract Estrogen deprivation is associated with delayed healing, while estrogen replacement therapy (ERT) accelerates acute wound healing and protects against development of chronic wounds. However, current estrogenic molecules have undesired systemic effects, thus the aim of our studies is to generate new molecules for topic administration that are devoid of systemic effects. Following a preliminary study, the new 17β-estradiol derivatives 1 were synthesized. The estrogenic activity of these novel compounds was evaluated in vitro using the cell line ERE-Luc B17 stably transfected with an ERE-Luc reporter. Among the 17β-estradiol derivatives synthesized, compounds 1e and 1f showed the highest transactivation potency and were therefore selected for the study of their systemic estrogenic activity. The study of these compounds in the ERE-Luc mouse model demonstrated that both compounds lack systemic effects when administered in the wound area. Furthermore, wound-healing experiments showed that 1e displays a significant regenerative and anti-inflammatory activity. It is therefore confirmed that this class of compounds are suitable for topical administration and have a clear beneficial effect on wound healing.
format	article
author	Mario Brufani Nicoletta Rizzi Clara Meda Luigi Filocamo Francesca Ceccacci Virginia D’Aiuto Gabriele Bartoli Angela La Bella Luisa M. Migneco Rinaldo Marini Bettolo Francesca Leonelli Paolo Ciana Adriana Maggi
author_facet	Mario Brufani Nicoletta Rizzi Clara Meda Luigi Filocamo Francesca Ceccacci Virginia D’Aiuto Gabriele Bartoli Angela La Bella Luisa M. Migneco Rinaldo Marini Bettolo Francesca Leonelli Paolo Ciana Adriana Maggi
author_sort	Mario Brufani
title	Novel Locally Active Estrogens Accelerate Cutaneous Wound Healing-Part 2
title_short	Novel Locally Active Estrogens Accelerate Cutaneous Wound Healing-Part 2
title_full	Novel Locally Active Estrogens Accelerate Cutaneous Wound Healing-Part 2
title_fullStr	Novel Locally Active Estrogens Accelerate Cutaneous Wound Healing-Part 2
title_full_unstemmed	Novel Locally Active Estrogens Accelerate Cutaneous Wound Healing-Part 2
title_sort	novel locally active estrogens accelerate cutaneous wound healing-part 2
publisher	Nature Portfolio
publishDate	2017
url	https://doaj.org/article/0f04ac462ec840b896f7ee6f46151370
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Novel Locally Active Estrogens Accelerate Cutaneous Wound Healing-Part 2

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