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Shamseddin A., Crauste C., Durand E., Villeneuve P., Dubois G., Durand T., Vercauteren J., Veas Francisco. (2017). Resveratrol formulated with a natural deep eutectic solvent inhibits active matrix metalloprotease-9 in hormetic conditions. European Journal of Lipid Science and Technology, 119 (11), art. 1700171 [9 p.]. ISSN 1438-7697

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Lien direct chez l'éditeur doi:10.1002/ejlt.201700171

Titre
Resveratrol formulated with a natural deep eutectic solvent inhibits active matrix metalloprotease-9 in hormetic conditions
Année de publication2017
Type de documentArticle référencé dans le Web of Science WOS:000414581100012
AuteursShamseddin A., Crauste C., Durand E., Villeneuve P., Dubois G., Durand T., Vercauteren J., Veas Francisco.
SourceEuropean Journal of Lipid Science and Technology, 2017, 119 (11), p. art. 1700171 [9 p.]. p. art. 1700171 [9 p.] ISSN 1438-7697
RésuméDespite the promising anti-oxidant and anti-inflammatory effects of resveratrol (RES) on human health, pre-clinical and clinical studies are frequently disappointing, probably due to its low water-solubility and poor bioavailability. Even though a hormetic mode of action was clearly established for RES, the high doses commonly used to mitigate these issues, lead to adverse effects. Common hallmarks of multiple pathologies results from pathological-enhanced endothelial permeability due to both enhanced inflammation and matrix metalloprotease-9 (aMMP-9) activities. The main aim of this work was to optimize the RES capacity to inhibit aMMP-9 by using a new class of solvents, natural deep eutectic solvents (NADES) for a new RES formulation as compared with dimethyl-sulfoxide (DMSO). To obtain the appropriate NADES, 18 compounds combinations were prepared to select those exhibiting the optimized capacity to dissolve RES. The RES-NADES 1,2-propanediol:choline-chloride:water (PCW, 1:1:1 molar ratio) and compared with RES-DMSO for their aMMP-9-inhibitory capacities. Low concentrations of RES-NADES/PCW formulation exhibited both a biocompatible solubility and a strong increased aMMP-9-inhibitory activity, at least 10-fold, higher than RES-DMSO, reaching its hormetic mode of action. Following in vivo validations, some particular NADES could potentially be considered as the new generation of formulation for druggable compounds. Practical applications: Formulation of resveratrol in Natural Deep Eutectic solvents (NADES) optimizes its capacity to inhibit active matrix metalloprotease-9. The Resveratrol-NADES 1,2-propanediol:choline-was the most efficient and low concentrations exhibited both a biocompatible solubility and an increased aMMP-9-inhibitory activity, at least 10-fold, higher than RES-DMSO. Consequently, the NADES/PCW formulation allowed resveratrol to reach its hormetic mode of action. Following in vivo validations, some particular NADES could potentially be considered as the new generation of formulation for druggable compounds.
Plan de classementSciences fondamentales / Techniques d'analyse et de recherche [020] ; Santé : généralités [050]
LocalisationFonds IRD [F B010071356]
Identifiant IRDfdi:010071356
Lien permanenthttp://www.documentation.ird.fr/hor/fdi:010071356

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