@article{fdi:010071356,
  title = {{R}esveratrol formulated with a natural deep eutectic solvent inhibits active matrix metalloprotease-9 in hormetic conditions},
  author = {{S}hamseddin, {A}. and {C}rauste, {C}. and {D}urand, {E}. and {V}illeneuve, {P}. and {D}ubois, {G}. and {D}urand, {T}. and {V}ercauteren, {J}. and {V}eas, {F}rancisco},
  editor = {},
  language = {{ENG}},
  abstract = {{D}espite 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. {E}ven though a hormetic mode of action was clearly established for {RES}, the high doses commonly used to mitigate these issues, lead to adverse effects. {C}ommon hallmarks of multiple pathologies results from pathological-enhanced endothelial permeability due to both enhanced inflammation and matrix metalloprotease-9 (a{MMP}-9) activities. {T}he main aim of this work was to optimize the {RES} capacity to inhibit a{MMP}-9 by using a new class of solvents, natural deep eutectic solvents ({NADES}) for a new {RES} formulation as compared with dimethyl-sulfoxide ({DMSO}). {T}o obtain the appropriate {NADES}, 18 compounds combinations were prepared to select those exhibiting the optimized capacity to dissolve {RES}. {T}he {RES}-{NADES} 1,2-propanediol:choline-chloride:water ({PCW}, 1:1:1 molar ratio) and compared with {RES}-{DMSO} for their a{MMP}-9-inhibitory capacities. {L}ow concentrations of {RES}-{NADES}/{PCW} formulation exhibited both a biocompatible solubility and a strong increased a{MMP}-9-inhibitory activity, at least 10-fold, higher than {RES}-{DMSO}, reaching its hormetic mode of action. {F}ollowing in vivo validations, some particular {NADES} could potentially be considered as the new generation of formulation for druggable compounds. {P}ractical applications: {F}ormulation of resveratrol in {N}atural {D}eep {E}utectic solvents ({NADES}) optimizes its capacity to inhibit active matrix metalloprotease-9. {T}he {R}esveratrol-{NADES} 1,2-propanediol:choline-was the most efficient and low concentrations exhibited both a biocompatible solubility and an increased a{MMP}-9-inhibitory activity, at least 10-fold, higher than {RES}-{DMSO}. {C}onsequently, the {NADES}/{PCW} formulation allowed resveratrol to reach its hormetic mode of action. {F}ollowing in vivo validations, some particular {NADES} could potentially be considered as the new generation of formulation for druggable compounds.},
  keywords = {{H}ormesis ; {MMP}-9 ; {M}etalloproteases ; n{ADES} (natural deep eutectic solvents) ; {R}esveratrol},
  booktitle = {},
  journal = {{E}uropean {J}ournal of {L}ipid {S}cience and {T}echnology},
  volume = {119},
  numero = {11},
  pages = {art. 1700171 [9 p.]},
  ISSN = {1438-7697},
  year = {2017},
  DOI = {10.1002/ejlt.201700171},
  URL = {https://www.documentation.ird.fr/hor/fdi:010071356},
}