SULFATION PATHWAYS Potential benefits of a sulfated resveratrol derivative for topical application

• Type: Article in International Scientific Journal
• Date: 2018

Authors

Marta Correia da Silva (Author) FFUP; Verónica Rocha (Author) Other; Cláudia Marques (Author) Other; Cláudia M Deus (Author) Other; Adriana Marques-Carvalho (Author) Other; Paulo J Oliveira (Author) Other; Andreia Palmeira (Author) FFUP; Madalena Pinto (Author) FFUP; Emilia Sousa (Author) FFUP; Sousa Lobo JM (Author) FFUP; Isabel F Almeida (Author) FFUP

Journal

Title: Journal of Molecular Endocrinology

Vol. 61

Pages: M27-M39

ISSN: 0952-5041

Publisher: BioScientifica Ltd.

Indexing

ISI Web of Knowledge - 6 Citations

Scopus - 8 Citations

Other information

Authenticus ID: P-00P-GKC

DOI: 10.1530/jme-18-0031

Abstract (EN): Resveratrol (RSV) is a polyphenolic compound with antioxidant, anti-inflammatory and anti-aging properties partly associated with sirtuin 1 (SIRT1)-activation in the skin. However, poor water solubility may limit RSV efficacy. This work aimed to clarify the interest of a new synthetic water-soluble RSV derivative (resveratrol glucoside sulfate, RSV-GS) for topical application. Resveratrol glucoside sulfate was synthesized using microwave-assisted sulfation. Cytotoxicity assays were performed with the keratinocyte HaCaT cell line, using MTT reduction, neutral red uptake, Alamar Blue/resazurin reduction, trypan blue exclusion and measurement of ATP concentration. Western blotting was used to evaluate SIRT1 protein content. Regarding SIRT1 binding, an in silico docking study was performed, using AutoDock Vina. Our results showed that the synthetic derivative RSV-GS was 1000 times more soluble in water than RSV and its non-sulfated glucoside. No relevant decrease in HaCaT cell viability was observed for concentrations up to 5mM for RSV-GS, and up to 500 mu M for resveratrol glucoside, while a significant decrease in HaCaT viability occurred from 100 mu M for RSV. RSV-GS and RSV showed a similar behavior regarding protective effect against oxidative stress-induced cytotoxicity. SIRT1 protein content increased after treatment with 500 mu M of RSV-GS and 100 mu M of RSV. Moreover, in silico studies predicted that RSV-GS binds more stably to SIRT1 with a lower binding free energy than RSV. Although these results support the possible use of RSV-GS in topical formulations, in vivo safety and efficacy studies are needed before considering the use of RSV-GS in commercial products.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 13