FR2898503A1 - Cosmetic or dermatological composition with a slimming effect comprises a substance that stimulates expression of SIRT1 protein deacetylase - Google Patents
Cosmetic or dermatological composition with a slimming effect comprises a substance that stimulates expression of SIRT1 protein deacetylase Download PDFInfo
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- FR2898503A1 FR2898503A1 FR0650849A FR0650849A FR2898503A1 FR 2898503 A1 FR2898503 A1 FR 2898503A1 FR 0650849 A FR0650849 A FR 0650849A FR 0650849 A FR0650849 A FR 0650849A FR 2898503 A1 FR2898503 A1 FR 2898503A1
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
- A61Q19/06—Preparations for care of the skin for countering cellulitis
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- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
- A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
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Abstract
Description
UTILISATION DE SUBSTANCES AGISSANT SUR LES SIRT- 1 POUR LEUR ACTIVITEUSE OF SUBSTANCES ACTING ON SIRT-1 FOR THEIR ACTIVITY
AMINCISSANTESLIMMING
La présente invention concerne l'utilisation cosmétique de substances agissant sur les protéines déacétylases SIRT-1 pour leur activité amincissante. L'invention se rapporte également aux compositions amincissantes comprenant au moins une substance agissant sur les protéines déacétylases SIRT-1. The present invention relates to the cosmetic use of substances acting on the SIRT-1 deacetylase proteins for their slimming activity. The invention also relates to slimming compositions comprising at least one substance acting on the SIRT-1 deacetylase proteins.
De nos jours, le culte de la minceur modèle un certain idéal de silhouette et on se soucie de plus en plus de son image et de son aspect extérieur. En particulier, beaucoup de femmes cherchent à lutter contre la cellulite qui donne à la peau un aspect granuleux et capitonné dit en peau d'orange et une consistance molle et flasque. Nowadays, the cult of slimming models a certain ideal of silhouette and we care more and more about its image and its external appearance. In particular, many women seek to combat cellulite which gives the skin a grainy and padded appearance said in orange peel and a soft and flabby consistency.
C'est pourquoi l'objectif de la présente invention est de proposer des produits présentant une action amincissante capables de lutter efficacement contre la cellulite et de limiter les désagréments qui en découlent. La cellulite correspond à un développement excessif de la masse grasse dans la couche profonde de la peau, le tissu adipeux, généralement au niveau des hanches et des cuisses. Le tissu adipeux est composé de cellules spécialisées : les adipocytes. Ces cellules proviennent de cellules précurseurs, les préadipocytes, et sont présentes à différents stades de différenciation au niveau du tissu adipeux. Le processus de différenciation adipocytaire, l'adipogenèse, est sous la dépendance de la communication cellulaire qui se fait par l'intermédiaire d'hormones et de facteurs de croissance. Plusieurs facteurs de transcription participent également au déroulement du programme de différenciation, notamment les PPAR (Peroxysome Proliferator-Activated Receptors) qui sont induits de façon précoce. Une fois arrivés à maturation, les adipocytes sont des cellules arrondies contenant des lipides sous forme de gouttelettes constituées presque exclusivement de triglycérides. Le tissu adipeux remplit plusieurs fonctions essentielles : protection mécanique et thermique, production de différentes substances endocrines et paracrines et surtout stockage ou mise à disposition de l'énergie. C'est cette dernière fonction qui est impliquée dans la cellulite, faisant de l'adipocyte une cellule extensible, qui augmente ou diminue de volume sous l'effet du remplissage des graisses, appelé lipogenèse, ou de la vidange, la lipolyse. Plusieurs phénomènes sont impliqués dans le dépôt de graisses au niveau du tissu adipeux : - un déséquilibre entre la lipogenèse et la lipolyse, conduisant à une hypertrophie des adipocytes, et - une augmentation de l'adipogenèse, conduisant à une hyperplasie des adipocytes et donc à une augmentation du tissu adipeux. Aussi, pour répondre à son objectif, la présente invention vise à utiliser des substances capables d'agir sur ces mécanismes impliqués dans les désordres du tissu adipeux et dans la formation de la cellulite. En particulier, la présente invention se propose d'utiliser des substances capables de stimuler et/ou d'augmenter l'expression des protéines déacétylases SIRT-1 pour la préparation d'une composition destinée à une activité amincissante. This is why the objective of the present invention is to provide products having a slimming action capable of effectively fighting against cellulite and to limit the inconvenience resulting therefrom. Cellulite is an excessive development of fat mass in the deep layer of the skin, adipose tissue, usually at the hips and thighs. Adipose tissue is composed of specialized cells: adipocytes. These cells come from precursor cells, the preadipocytes, and are present at different stages of differentiation in adipose tissue. The process of adipocyte differentiation, adipogenesis, is dependent on cellular communication through hormones and growth factors. Several transcription factors also participate in the development of the differentiation program, including PPARs (Peroxysome Proliferator-Activated Receptors) that are induced early. Once mature, the adipocytes are rounded cells containing lipids in the form of droplets consisting almost exclusively of triglycerides. The adipose tissue fulfills several essential functions: mechanical and thermal protection, production of various endocrine and paracrine substances and especially storage or provision of energy. It is this latter function that is involved in cellulite, making the adipocyte an expandable cell, which increases or decreases in volume under the effect of fat filling, called lipogenesis, or emptying, lipolysis. Several phenomena are involved in the deposition of fat in the adipose tissue: - an imbalance between lipogenesis and lipolysis, leading to hypertrophy of the adipocytes, and - an increase in adipogenesis, leading to a hyperplasia of the adipocytes and therefore to an increase in adipose tissue. Also, to meet its purpose, the present invention aims to use substances capable of acting on these mechanisms involved in adipose tissue disorders and in the formation of cellulite. In particular, the present invention proposes to use substances capable of stimulating and / or increasing the expression of the SIRT-1 deacetylase proteins for the preparation of a composition intended for a slimming activity.
Les SIRT-1 sont des enzymes NAb(+)-dépendantes (Nicotinamide Adénine binucélotide - dépendantes) qui jouent un rôle à la fois : - au niveau de la mobilisation des graisses dans les adipocytes, et au niveau de l'adipogenèse. SIRT - 1 are NAb (+) - dependent (Nicotinamide adenine binucelotide - dependent) enzymes that play a role at the same time: - at the level of fat mobilization in adipocytes, and at the level of adipogenesis.
En effet, les SIRT-1 sont capables d'intervenir au niveau de la lipolyse et de moduler l'accumulation des triglycérides dans les adipocytes matures. Ainsi, l'utilisation de substances capables de stimuler et/ou d'augmenter l'expression des SIRT-1 selon la présente invention permet de réduire la quantité de triglycérides accumulés dans les adipocytes matures et de diminuer le volume des cellules graisseuses. En parallèle, les SIRT-1 sont capables de relier et de réprimer les gènes contrôlant le régulateur de graisse PPAR-y (Peroxysome Proliferator-Activated Receptors gamma), facteur de transcription participant à l'adipogenèse. Indeed, SIRT-1 are able to intervene at the level of lipolysis and modulate the accumulation of triglycerides in mature adipocytes. Thus, the use of substances capable of stimulating and / or increasing the expression of SIRT-1 according to the present invention makes it possible to reduce the amount of triglycerides accumulated in mature adipocytes and to reduce the volume of fat cells. In parallel, SIRT-1 are able to bind and repress the genes controlling the PPAR-y (Peroxysome Proliferator-Activated Receptors gamma) fat regulator, a transcription factor involved in adipogenesis.
De fait, l'utilisation de substances capables de stimuler et/ou d'augmenter l'expression des SIRT-1 selon la présente invention permet également de moduler l'activité du facteur de transcription PPAR-y et de limiter l'adipogenèse. Ainsi, le nombre d'adipocytes matures dans le tissu adipeux diminue. L'utilisation d'au moins une substance capable de stimuler et/ou d'augmenter l'expression des SIRT-1 selon l'invention, permet donc de réduire à la fois le nombre et le volume des cellules graisseuses du tissu adipeux et de limiter la cellulite. De manière préférentielle les substances capables de stimuler et/ou d'augmenter l'expression des SIRT-1 selon la présente invention sont des actifs 20 obtenus à partir de végétaux. En particulier, ces végétaux peuvent être choisis par exemple parmi les familles des Amaranthacées, des Cyperacées, des Nymphaeacées et des Nelumbonacées. Les substances capables de stimuler et/ou d'augmenter l'expression des SIRT-1 selon l'invention sont destinées à être incorporées au sein de compositions 25 cosmétiques et/ou dermopharmaceutiques. La composition selon l'invention peut contenir de 0,01 à 20 % d'au moins une substance capable de stimuler et/ou d'augmenter l'expression des SIRT-1. In fact, the use of substances capable of stimulating and / or increasing the expression of SIRT-1 according to the present invention also makes it possible to modulate the activity of the PPAR-γ transcription factor and to limit adipogenesis. Thus, the number of mature adipocytes in adipose tissue decreases. The use of at least one substance capable of stimulating and / or increasing the expression of the SIRT-1s according to the invention thus makes it possible to reduce both the number and the volume of fat cells of the adipose tissue and of limit cellulite. Preferably, the substances capable of stimulating and / or increasing the expression of SIRT-1 according to the present invention are active agents obtained from plants. In particular, these plants may be chosen for example from the families Amaranthaceae, Cyperaceae, Nymphaeaceae and Nelumbonaceae. Substances capable of stimulating and / or increasing the expression of SIRT-1 according to the invention are intended to be incorporated into cosmetic and / or dermopharmaceutical compositions. The composition according to the invention may contain from 0.01 to 20% of at least one substance capable of stimulating and / or increasing the expression of SIRT-1.
L'administration d'une composition contenant au moins une substance capable de stimuler et/ou d'augmenter l'expression des SIRT-1 selon l'invention est de préférence effectuée par voie topique. La composition selon l'invention peut se présenter sous forme de crèmes, émulsions huile-dans-eau, eau-dans-huile ou émulsions multiples, solutions, suspensions ou encore poudres. La présente invention est maintenant décrite en s'appuyant sur des résultats de tests effectués à partir d'exemples non limitatifs de substances capables de stimuler et/ou d'augmenter l'expression des SIRT-1. 1 EVALUATION DE L'EFFET DE SUBSTANCES SELON L'INVENTION 1.1 Test 1 : Evaluation in vitro de l'expression des ARNm codant pour les SIRT-1 L'objectif de cette étude est d'évaluer la capacité de principes actifs à augmenter l'expression des ARNm codant pour les SIRT-1. Administration of a composition containing at least one substance capable of stimulating and / or increasing the expression of SIRT-1 according to the invention is preferably carried out topically. The composition according to the invention may be in the form of creams, oil-in-water emulsions, water-in-oil or multiple emulsions, solutions, suspensions or powders. The present invention is now described based on test results made from non-limiting examples of substances capable of stimulating and / or increasing the expression of SIRT-1. 1 EVALUATION OF THE EFFECT OF SUBSTANCES ACCORDING TO THE INVENTION 1.1 Test 1: In vitro Evaluation of the Expression of the mRNA Encoding the SIRT-1 The objective of this study is to evaluate the capacity of active ingredients to increase the expression of mRNAs encoding SIRT-1.
Cette étude consiste à placer des préadipocytes dans un milieu permettant leur différenciation en adipocytes matures, auquel on ajoute dans quatre tests les principes actifs suivants : - un principe actif issu de Célosia, une plante de la famille des Amaranthacées, à 0,1% et à 0,25%, - un principe actif issu de Souchet, une plante de la famille des Cyperacées, à 0,5%, et - un principe actif issu de Nénuphar, une plante de la famille des Nymphaeacées, à 0,1%. On prépare également en parallèle un échantillon témoin positif en présence de 25 captopril à 1mM. L'expression des ARNm de SIRT-1 est réalisée par PCR (Polymerase Chain Reaction) quantitative. This study consists of placing preadipocytes in a medium allowing their differentiation into mature adipocytes, to which the following active ingredients are added in four tests: - an active ingredient derived from Celosia, a plant of the Amaranthaceae family, at 0.1% and at 0.25%, - an active principle derived from Souchet, a plant of the family Cyperaceae, at 0.5%, and - an active ingredient from Nénuphar, a plant of the family Nymphaeacées, at 0.1% . A positive control sample was also prepared in the presence of captopril at 1 mM. The expression of the SIRT-1 mRNAs is carried out by quantitative PCR (Polymerase Chain Reaction).
Les résultats sont exprimés dans le tableau suivant : Taux d'expression des ARNm de SIRT-1 (en /G) Témoin 100 Captopril 1mM 114 Principe actif issu de Célosia, plante de la 103 famille des Amaranthacées, 0,1% Principe actif issu de Célosia, plante de la 125 famille des Amaranthacées, 0,25% Principe actif issu de Souchet, plante de 114 la famille des Cyperacées, 0,5% Principe actif issu de Nénuphar, plante 164 de la famille des Nymphaeacées, 0,1% On constate que les principes actifs issus de plantes des familles Amaranthacées, Cyperacées et Nymphaeacées augmentent l'expression des ARNm codant pour les SIRT-1. The results are expressed in the following table: Expression level of SIRT-1 mRNA (in / G) Control 100 Captopril 1mM 114 Active ingredient from Celosia, plant of the family 103 Amaranthaceae, 0.1% Active ingredient from of Celosia, plant of the 125 family of Amaranthaceae, 0.25% active ingredient from Souchet, plant of 114 family Cyperaceae, 0.5% active ingredient from water lily, plant 164 of the family of Nymphaeaceae, 0.1 It is found that the active ingredients derived from plants of Amaranthaceae, Cyperaceae and Nymphaeaceae families increase the expression of the mRNAs coding for SIRT-1.
1.2 Test 2 : Evaluation in vitro de la synthèse des SIRT-1 Cette étude a pour but de déterminer l'effet de principes actifs sur la synthèse des SIRT-1. Le protocole opératoire consiste à traiter des adipocytes avec un principe actif issu de Lotus, une plante de la famille des Nelumbonacées, à 0,1% et à 0,5%. 1.2 Test 2: In vitro evaluation of SIRT-1 synthesis This study aims to determine the effect of active ingredients on the synthesis of SIRT-1. The operative protocol consists of treating adipocytes with an active principle derived from Lotus, a plant of the family Nelumbonaceae, at 0.1% and 0.5%.
On prépare également en parallèle un échantillon témoin positif en présence de captopril à 1mM. On dose les protéines totales et on détermine l'évolution du taux de SIRT-1 par Western Blot. A positive control sample in the presence of captopril at 1mM is also prepared in parallel. The total proteins are assayed and the evolution of the SIRT-1 level is determined by Western blotting.
Les résultats sont présentés ci-dessous : Taux de SIRT-1 (en /G) Témoin 100 Captopril 1mM 113 Principe actif issu de Lotus, plante de 119 la famille des Nelumbonacées 0,1% Principe actif issu de Lotus, plante de 126 la famille des Nelumbonacées 0,5% Ces résultats montrent qu'un principe actif issu de plantes de la famille des Nelumbonacées à 0,1% et à 0,5% favorise la synthèse des SIRT-1. The results are presented below: SIRT-1 (in / G) rate Control 100 Captopril 1mM 113 Active ingredient from Lotus, plant of the family Nelumbonaceae 0.1% Active ingredient from Lotus, plant of 126 family 0.5% of Nelumbonaceae These results show that an active ingredient from plants of the Nelumbonaceae family at 0.1% and 0.5% promotes the synthesis of SIRT-1.
2 EXEMPLES DE COMPOSITIONS La présente invention couvre aussi les compositions cosmétiques et/ou dermopharmaceutiques incluant au moins une substance capable d'agir sur les SIRT-1 selon la présente invention dans différentes formes galéniques, adaptées à l'administration par voie topique cutanée. Ces compositions peuvent se présenter notamment sous forme de crèmes, émulsions huile-dans-eau, émulsions eau-dans-huile, émulsions multiples, solutions, suspensions ou poudres. Elles peuvent être plus ou moins fluides et avoir l'aspect d'une crème, d'une lotion, d'un lait, d'un sérum, d'une pommade, d'un gel, d'une pâte ou d'une mousse, ou sous forme solide. Ces compositions contiennent entre 0,01 et 20% en poids de substance(s) capable(s) d'agir sur les SIRT-1 selon la présente invention. Les exemples de compositions qui suivent sont obtenus par mélange des différents composants. Les quantités indiquées sont données en pourcentage de poids. 2.1 Exemple de gel crème amincissant : La formulation est la suivante : - Cetearyl octonoate : 10,0% - Ethanol : 8,0% - Principe actif agissant sur SIRT-1 : 4,0% - Arachidyl alcool/Behenyl Alcool/ Arachidyl glucoside : 2,0% - Polyacrilamide/C13C14 paraffine/ Laureth7 : 2,0% - Myreth-3 Myristate : 1,0% - Glycerol : 3,0% -bimethicone : 1,0% - Phenonip : 0,7% - Eau : 68,3% 2.2 Exemple de gel amincissant : La formulation est la suivante : - Cetearyl octonoate : 2, 0% - Ethanol : 8,0% - Principe actif agissant sur SIRT-1 : 5,0% biméthicone : 5,0% - Isononyl isononanoate : 3,0% - C13-14 Isoparaffin/Isostearyl isostearate/sodium polyacrylate/ polyacrylamide/polysorbate 60 : 3,0% -Glycerol : 2,0% - Phenonip : 0,5% Eau : 71,5% EXAMPLES OF COMPOSITIONS The present invention also covers cosmetic and / or dermopharmaceutical compositions including at least one substance capable of acting on the SIRT-1s according to the present invention in different galenic forms, adapted for topical administration to the skin. These compositions may especially be in the form of creams, oil-in-water emulsions, water-in-oil emulsions, multiple emulsions, solutions, suspensions or powders. They can be more or less fluid and have the appearance of a cream, a lotion, a milk, a serum, an ointment, a gel, a paste or a foam, or in solid form. These compositions contain between 0.01% and 20% by weight of substance (s) capable of acting on the SIRT-1s according to the present invention. The following examples of compositions are obtained by mixing the various components. The quantities indicated are given as a percentage of weight. 2.1 Example of slimming cream gel: The formulation is the following: - Cetearyl octonoate: 10.0% - Ethanol: 8.0% - Active ingredient acting on SIRT-1: 4.0% - Arachidyl alcohol / Behenyl Alcohol / Arachidyl glucoside : 2.0% - Polyacrilamide / C13C14 paraffin / Laureth7: 2.0% - Myreth-3 Myristate: 1.0% - Glycerol: 3.0% -bimethicone: 1.0% - Phenonip: 0.7% - Water : 68.3% 2.2 Example of slimming gel: The formulation is as follows: Cetearyl octonoate: 2.0% Ethanol: 8.0% Active ingredient acting on SIRT-1: 5.0% bimethicone: 5.0 % - Isononyl isononanoate: 3.0% - C13-14 Isoparaffin / Isostearyl isostearate / sodium polyacrylate / polyacrylamide / polysorbate 60: 3.0% -Glycerol: 2.0% - Phenonip: 0.5% Water: 71.5%
Claims (9)
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