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 17Î²-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 17Î²-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.
Novel Locally Active Estrogens Accelerate Cutaneous Wound Healing-Part / M. Brufani, N. Rizzi, C. Meda, L. Filocamo, F. Ceccacci, V. D'Aiuto, G. Bartoli, A.L. Bella, L.M. Migneco, R.M. Bettolo, F. Leonelli, P. Ciana, A. Maggi. - In: SCIENTIFIC REPORTS. - ISSN 2045-2322. - 7:1(2017 May 31).
|Titolo:||Novel Locally Active Estrogens Accelerate Cutaneous Wound Healing-Part|
MAGGI, ADRIANA CATERINA (Corresponding)
|Settore Scientifico Disciplinare:||Settore BIO/14 - Farmacologia|
|Progetto:||Role of the Liver Estrogen Receptor in female Energy Metabolism, Reproduction and Aging: What About Your Liver Sexual Functions?|
Imaging of Neuroinflammation in Neurodegenerative Diseases
|Data di pubblicazione:||31-mag-2017|
|Digital Object Identifier (DOI):||http://dx.doi.org/10.1038/s41598-017-02820-y|
|Appare nelle tipologie:||01 - Articolo su periodico|