Resveratrol formulated with a natural deep eutectic solvent inhibits active matrix metalloprotease-9 in hormetic conditions
Despite 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. The effect of resveratrol (RES) dissolved in either NADES/PCW or DMSO was assessed on the TNFa-activated human monocytes (THP-1). NADES/PCW was able to confer a significant increase of the MMP-9 inhibitory activity of RES, at low doses (at least 10-fold higher) than DMSO, Thus, these data on RES-NADES/PCW formulation support the hormetic effect of resveratrol in preserving the endothelial monolayer integrity by decreasing the exacerbated vascular permeability induced by the overproduction of active MMP-9, during inflammation resulting from infections, cancer, or other pathologies.
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Subjects: | Q02 - Traitement et conservation des produits alimentaires, 000 - Autres thèmes, resvératrol, solvant, http://aims.fao.org/aos/agrovoc/c_36145, http://aims.fao.org/aos/agrovoc/c_7236, |
Online Access: | http://agritrop.cirad.fr/585614/ http://agritrop.cirad.fr/585614/7/Shamseddin_et_al-2017-European_Journal_of_Lipid_Science.pdf |
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Q02 - Traitement et conservation des produits alimentaires 000 - Autres thèmes resvératrol solvant http://aims.fao.org/aos/agrovoc/c_36145 http://aims.fao.org/aos/agrovoc/c_7236 Q02 - Traitement et conservation des produits alimentaires 000 - Autres thèmes resvératrol solvant http://aims.fao.org/aos/agrovoc/c_36145 http://aims.fao.org/aos/agrovoc/c_7236 |
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Q02 - Traitement et conservation des produits alimentaires 000 - Autres thèmes resvératrol solvant http://aims.fao.org/aos/agrovoc/c_36145 http://aims.fao.org/aos/agrovoc/c_7236 Q02 - Traitement et conservation des produits alimentaires 000 - Autres thèmes resvératrol solvant http://aims.fao.org/aos/agrovoc/c_36145 http://aims.fao.org/aos/agrovoc/c_7236 Shamseddin, Aly Crauste, Céline Durand, Erwann Villeneuve, Pierre Dubois, Gregor Durand, Thierry Vercauteren, Joseph Veas, Francisco Resveratrol formulated with a natural deep eutectic solvent inhibits active matrix metalloprotease-9 in hormetic conditions |
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Despite 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. The effect of resveratrol (RES) dissolved in either NADES/PCW or DMSO was assessed on the TNFa-activated human monocytes (THP-1). NADES/PCW was able to confer a significant increase of the MMP-9 inhibitory activity of RES, at low doses (at least 10-fold higher) than DMSO, Thus, these data on RES-NADES/PCW formulation support the hormetic effect of resveratrol in preserving the endothelial monolayer integrity by decreasing the exacerbated vascular permeability induced by the overproduction of active MMP-9, during inflammation resulting from infections, cancer, or other pathologies. |
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Q02 - Traitement et conservation des produits alimentaires 000 - Autres thèmes resvératrol solvant http://aims.fao.org/aos/agrovoc/c_36145 http://aims.fao.org/aos/agrovoc/c_7236 |
author |
Shamseddin, Aly Crauste, Céline Durand, Erwann Villeneuve, Pierre Dubois, Gregor Durand, Thierry Vercauteren, Joseph Veas, Francisco |
author_facet |
Shamseddin, Aly Crauste, Céline Durand, Erwann Villeneuve, Pierre Dubois, Gregor Durand, Thierry Vercauteren, Joseph Veas, Francisco |
author_sort |
Shamseddin, Aly |
title |
Resveratrol formulated with a natural deep eutectic solvent inhibits active matrix metalloprotease-9 in hormetic conditions |
title_short |
Resveratrol formulated with a natural deep eutectic solvent inhibits active matrix metalloprotease-9 in hormetic conditions |
title_full |
Resveratrol formulated with a natural deep eutectic solvent inhibits active matrix metalloprotease-9 in hormetic conditions |
title_fullStr |
Resveratrol formulated with a natural deep eutectic solvent inhibits active matrix metalloprotease-9 in hormetic conditions |
title_full_unstemmed |
Resveratrol formulated with a natural deep eutectic solvent inhibits active matrix metalloprotease-9 in hormetic conditions |
title_sort |
resveratrol formulated with a natural deep eutectic solvent inhibits active matrix metalloprotease-9 in hormetic conditions |
url |
http://agritrop.cirad.fr/585614/ http://agritrop.cirad.fr/585614/7/Shamseddin_et_al-2017-European_Journal_of_Lipid_Science.pdf |
work_keys_str_mv |
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dig-cirad-fr-5856142024-01-29T05:40:49Z http://agritrop.cirad.fr/585614/ http://agritrop.cirad.fr/585614/ Resveratrol formulated with a natural deep eutectic solvent inhibits active matrix metalloprotease-9 in hormetic conditions. Shamseddin Aly, Crauste Céline, Durand Erwann, Villeneuve Pierre, Dubois Gregor, Durand Thierry, Vercauteren Joseph, Veas Francisco. 2017. European Journal of Lipid Science and Technology, 119 (11):e1700171, 9 p.https://doi.org/10.1002/ejlt.201700171 <https://doi.org/10.1002/ejlt.201700171> Resveratrol formulated with a natural deep eutectic solvent inhibits active matrix metalloprotease-9 in hormetic conditions Shamseddin, Aly Crauste, Céline Durand, Erwann Villeneuve, Pierre Dubois, Gregor Durand, Thierry Vercauteren, Joseph Veas, Francisco eng 2017 European Journal of Lipid Science and Technology Q02 - Traitement et conservation des produits alimentaires 000 - Autres thèmes resvératrol solvant http://aims.fao.org/aos/agrovoc/c_36145 http://aims.fao.org/aos/agrovoc/c_7236 Despite 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. The effect of resveratrol (RES) dissolved in either NADES/PCW or DMSO was assessed on the TNFa-activated human monocytes (THP-1). NADES/PCW was able to confer a significant increase of the MMP-9 inhibitory activity of RES, at low doses (at least 10-fold higher) than DMSO, Thus, these data on RES-NADES/PCW formulation support the hormetic effect of resveratrol in preserving the endothelial monolayer integrity by decreasing the exacerbated vascular permeability induced by the overproduction of active MMP-9, during inflammation resulting from infections, cancer, or other pathologies. article info:eu-repo/semantics/article Journal Article info:eu-repo/semantics/publishedVersion http://agritrop.cirad.fr/585614/7/Shamseddin_et_al-2017-European_Journal_of_Lipid_Science.pdf text Cirad license info:eu-repo/semantics/restrictedAccess https://agritrop.cirad.fr/mention_legale.html https://doi.org/10.1002/ejlt.201700171 10.1002/ejlt.201700171 info:eu-repo/semantics/altIdentifier/doi/10.1002/ejlt.201700171 info:eu-repo/semantics/altIdentifier/purl/https://doi.org/10.1002/ejlt.201700171 |