Events8th International Electronic Conference on Medicinal Chemistry
Published
with-doi10.3390/ECMC2022-13205 (registering DOI)
This submission belongs to the session S3. General of the event 8th International Electronic Conference on Medicinal Chemistry
Published date
01 Nov, 2022
Academic Editor
author-avatarMaria Emília Sousa
Citation
Sonia Floris, Francesca Pintus, Antonella Fais, Benedetta Era, Eugenio Uriarte, Maria J. Matos, A selected series of hydroxy-3-arylcoumarins as multitarget compounds for skin aging diseases , in Proceedings of 8th International Electronic Conference on Medicinal Chemistry, 1 November–30 November 2022, MDPI: Basel, Switzerland, doi: 10.3390/ECMC2022-13205
Share
Email
Facebook
Twitter
LinkedIn

A selected series of hydroxy-3-arylcoumarins as multitarget compounds for skin aging diseases

image
1. Department of Life and Environmental Sciences, University of Cagliari, 09042 Monserrato, Cagliari, Italy
2. Departamento de Química Orgánica, Facultade de Farmacia, Universidade de Santiago de Compostela, 15782 Santiago de Compostela, Spain
3. Departamento de Química Orgánica, Facultade de Farmacia, Universidade de Santiago de Compostela, 15782 Santiago de Compostela, Spain CIQUP/Departamento de Química e Bioquímica, Faculdade de Ciências, Universidade do Porto, 4169–007 Porto, Portugal
Abstract

Skin aging is a progressive biological process of the human body that depends, among several phenomena, on degradation of proteins of extracellular matrix as well as the appearance of hyperpigmented spots. In previous studies, we demonstrated that differently substituted 3-arylcoumarins efficiently inhibit skin aging-related enzymes, such as tyrosinase, elastase and collagenase. According to these considerations, we have modulated this scaffold to improve the inhibitory potency against tyrosinase, elastase and collagenase, extending the study to the inhibition another enzyme, hyaluronidase. Moreover, photo-protective effect of the compounds has been also evaluated by determining the Sun Protection Factor. Starting from 3-(3’-hydroxyphenyl)-6,7-dihydroxycoumarin and 3-(2’-hydroxyphenyl)-6,7-dihydroxycoumarin, that overall revealed to possess the best inhibitory effects against skin aging-related enzymes, we selected for this study new molecules including bromine atoms together with the previously studied hydroxyl groups. Some compounds present multitarget properties towards the selected enzymes, along with a good photo-protective effect. These data support our previous findings on 3-arylcoumarin as promising scaffolds for the design of skin anti-aging agents.

Keywords
Hydroxy-3-arylcoumarins
Tyrosinase
Elastase
Collagenase
Hyaluronidase
Sun protection factor
Skin aging
Poster
sciforum-065788.pdf
Interactionts between heterometallic bridged cis-or trans-Pt(II)-Zn(II)complexes and calf thymus DNA
Evaluation of cytotoxic activity of small aminated quinolinequinones in vitro as anti-cancer molecules