Format

Send to

Choose Destination
Sci Rep. 2017 May 31;7(1):2510. doi: 10.1038/s41598-017-02820-y.

Novel Locally Active Estrogens Accelerate Cutaneous Wound Healing-Part 2.

Author information

1
Dipartimento di Scienze Biochimiche "A. Rossi Fanelli", Universita' degli Studi di Roma "La Sapienza", Via degli Apuli 9, I-00185, Roma, Italy.
2
Centre of Excellence on Neurodegenerative Diseases, Universita' degli Studi di Milano, Via Balzaretti, 9, I-20133, Milano, Italy.
3
Dipartimento di Scienze Biochimiche "A. Rossi Fanelli", Universita' degli Studi di Roma "La Sapienza", Via degli Apuli 9, I-00185, Roma, Italy. luigi.filocamo@uniroma1.it.
4
Istituto di Metodologie Chimiche-CNR, Unità Organizzativa di Supporto, Sede di Roma, Università degli Studi di Roma "La Sapienza", P. le Aldo Moro, 5, I-00185, Roma, Italy. francesca.ceccacci@uniroma1.it.
5
Dipartimento di Chimica "S. Cannizzaro", Universita' degli Studi di Roma "La Sapienza", P.le Aldo Moro 5, I-00185, Roma, Italy.
6
Dipartimento di Biologia Ambientale, Universita' degli Studi di Roma "La Sapienza", P.le Aldo Moro 5, I-00185, Roma, Italy.
7
Istituto di Metodologie Chimiche-CNR, Unità Organizzativa di Supporto, Sede di Roma, Università degli Studi di Roma "La Sapienza", P. le Aldo Moro, 5, I-00185, Roma, Italy.
8
Centre of Excellence on Neurodegenerative Diseases, Universita' degli Studi di Milano, Via Balzaretti, 9, I-20133, Milano, Italy. adriana.maggi@unimi.it.

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.

Supplemental Content

Full text links

Icon for Nature Publishing Group Icon for PubMed Central
Loading ...
Support Center