Comparative Studies on the Photoreactivity, Efficacy, and Safety of Depigmenting Agents

Author:

Mota Sandra12ORCID,Rosa Gonçalo P.34ORCID,Barreto Maria Carmo4ORCID,Garrido Jorge5ORCID,Sousa Emília67ORCID,Cruz Maria T.8910ORCID,Almeida Isabel F.12ORCID,Quintas Clara211

Affiliation:

1. UCIBIO—Applied Molecular Biosciences Unit, MedTech, Faculty of Pharmacy, Department of Drug Sciences, Laboratory of Pharmaceutical Technology, University of Porto, 4050-313 Porto, Portugal

2. Associate Laboratory i4HB—Institute for Health and Bioeconomy, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal

3. LAQV-REQUIMTE, Department of Chemistry, University of Aveiro, 3810-192 Aveiro, Portugal

4. cE3c—Centre for Ecology, Evolution and Environmental Changes/Azorean Biodiversity Group, CHANGE and Faculty of Sciences and Technology, University of Azores, 9500-321 Ponta Delgada, Portugal

5. CIQUP-IMS, ISEP, Polytechnic of Porto, 4249-015 Porto, Portugal

6. Laboratory of Organic and Pharmaceutical Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal

7. CIIMAR—Interdisciplinary Center of Marine and Environmental Research, University of Porto, Avenida General Norton de Matos, S/N, 4450-208 Matosinhos, Portugal

8. Faculty of Pharmacy, University of Coimbra, 3000-548 Coimbra, Portugal

9. CNC-UC—Center for Neuroscience and Cell Biology, University of Coimbra, 3000-548 Coimbra, Portugal

10. CIBB—Centre for Innovative Biomedicine and Biotechnology, University of Coimbra, 3000-548 Coimbra, Portugal

11. UCIBIO—Applied Molecular Biosciences Unit, Faculty of Pharmacy, Department of Drug Sciences, Laboratory of Pharmacology, University of Porto, 4050-313 Porto, Portugal

Abstract

Depigmenting products are increasingly used to counteract skin hyperpigmentation and related psychosocial issues. This study aimed to compare different depigmenting agents—4-butylresorcinol; bakuchiol; tranexamic acid; ascorbyl glucoside; α-arbutin; and ascorbic acid—for photoreactivity; tyrosinase inhibition; and safety. Photoreactivity was assessed using the Reactive Oxygen Species assay. In vitro tyrosinase inhibition was compared, and cell viability was assessed in B-16V melanocytes to evaluate safety. Results showed 4-butylresorcinol, ascorbyl glucoside, and α-arbutin are non-photoreactive, while for ascorbic acid and bakuchiol it was not possible to reach conclusive results due to the lack of specificity of the ROS assay. 4-Butylresorcinol, acting as a competitive inhibitor, displayed potent tyrosinase inhibition, followed by ascorbic acid and bakuchiol. Both 4-butylresorcinol and bakuchiol reduced cell viability in a concentration-dependent manner. The insights obtained in this work support the development of depigmenting products by providing useful scientific guidance on the photostability, tyrosinase inhibitory efficacy, and skin safety of depigmenting agents.

Publisher

MDPI AG

Subject

Drug Discovery,Pharmaceutical Science,Molecular Medicine

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