Water-soluble extracts of delipidated fruits or seeds of African Xylopia aethiopica from the Annonaceae family and its cosmetic uses.

A water-soluble extract from delipidated Xylopia Aethiopica seeds, used in a cosmetic composition, addresses skin aging and barrier function issues by enhancing key gene expressions related to skin health and reducing those associated with skin degradation.

FR3153250A1Active Publication Date: 2025-03-28SOUDANT ETIENNE
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Patent Information

Application Number
FR2023010111
Authority / Receiving Office
FR · FR
Patent Type
Applications
Current Assignee / Owner
Filing Date
2023-09-25
Publication Date
2025-03-28
Estimated Expiration
2043-09-25

AI Technical Summary

Technical Problem

Current cosmetic products often rely on complex formulations with multiple active ingredients, which can be greasy and may not effectively address skin aging, barrier function, and homeostasis.

Method used

A water-soluble extract of delipidated fruits or seeds from Xylopia Aethiopica, obtained through cold pressing and subsequent extraction in water or hydroethanolic solutions, is used in a cosmetic composition to provide multifunctional benefits.

Benefits of technology

The extract enhances skin firmness by improving the expression of genes related to skin health, such as IGFBP3, TGM1, and DSG1, while reducing the expression of genes associated with skin degradation, thereby addressing skin aging and barrier function.

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Abstract

Cosmetic use of water-soluble extracts of delipidated fruits or seeds of African Xylopia aethiopica of the Annonaceae family with multifunctional effects and intended to be placed in contact with the various superficial parts of the human body.
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Description

Title of the invention: Water-soluble extracts of defatted fruits or seeds of African Xylopia aethiopica of the An-nonaceae family and its cosmetic uses.

[0001] The present invention relates to a cosmetic composition intended to be brought into contact with the various superficial parts of the human body (epidermis, hair and capillary systems, nails, lips and external genital organs) or with the teeth and oral mucous membranes, with a view, exclusively or mainly, to cleaning them, perfuming them, modifying their appearance, protecting them, keeping them in good condition or correcting body odors and characterized in that it comprises at least one aqueous, glycerin or hydroalcoholic extract of delipidated fruits or seeds of African Xylopia aethiopica of the Annonaceae family with the aim of advantageously using a multifunctional active ingredient making it possible to both reduce aging, strengthen the barrier effect of the skin, its cohesion and its homeostasis,to slow down epidermal proliferation in order to give it more time to build up properly while promoting its proper maturation and differentiation, including that of the horny envelopes, in order to also protect the extracellular matrices and good formation of their collagens, contributing to improving the firmness of the skin.

[0002] We know that more and more cosmetics are trying to claim a more organic, more ecological, more natural mode of action with the new ISO 16128 standard, vegan and even slow cosmetics (ecological, healthy, intelligent and reasonable) taking into account the real needs of the skin, advocating the use of fewer ingredients to do better, even frugality, positive contributions for the skin and realistic promises. A response to this concern could then be plant extracts with multiple, multifunctional and complementary properties that are sufficient in themselves and therefore often do not require the addition of other active substances in cosmetic compositions.

[0003] Many people think that the surface of the skin on which cosmetics are applied is a dead and inert structure. In fact, this is not the case and the epidermis, including its surface horny layer, is the site of intense biochemical reactions where activators, inhibitors and inhibitor inhibitors ensure a balance and homeostasis that vary with the time of day, the seasons and age. Each of the epidermal cells and particularly the keratinocytes which are the predominant cells of the epidermis, presents a complex and fine metabolism leading to maturation and cellular differentiation under the control of the expression of the 36000 genes and variants that compose them.

[0004] It is then easy to imagine the interest of being able to select and test plant substances on the expression of all of these genes in order to be able to select the most interesting extracts and develop the most effective extraction and production methods. Among all the plants studied, the African Xylopia aethiopica of the An-nonaceae family has numerous and known properties and is a species commonly used in tropical Africa as a spice and for the medicinal properties of its fruits and seeds. Analysis of the fatty acids of the seeds confirms the absence of toxic compounds, thus justifying the common use of the fruits in the food sector. The curative properties of the fruit of Xylopia aethiopica are justified by the antimicrobial and antifungal power. Its dried fruit is used as a spice and for its medicinal properties, particularly against flu, bronchitis and dysentery. It is also recommended for relieving eye-related pathologies. In Senegal, it is used to flavor Touba coffee, a drink that has become traditional.

[0005] One of the aims of the invention is to provide a non-greasy composition because there is an obvious advantage of use for the skin and the user.

[0006] Another aim of the invention is to propose the use of such a composition in the context of a cosmetic application.

[0007] It is from the observation that very often plants, and particularly their seeds, contain a significant portion of lipids which hinder the release of substances of interest and require the use of complex solvents other than simple water, hydroethanolic solvents or vegetable glycerin that the idea came to separate, beforehand, these lipids from the rest of the plant to be extracted.

[0008] It was by studying the properties of different water-soluble extracts of fruits or seeds of Xylopia aethiopica after defatting obtained after one or more successive cold pressings, on the expression of the genes of normal human keratinocytes that the applicant discovered, quite unexpectedly, that these extracts of Xylopia aethiopica had numerous properties of interest to healthy skin and therefore to cosmetics, particularly those concerned with minimalist formulas using multifunctional active ingredients since a given extract could have numerous properties which complement each other and reduce the use of numerous different active substances.

[0009] Consequently, a cosmetic or pharmaceutical composition intended to be placed in contact with the various superficial parts of the human body (epidermis, hair and capillary systems, nails, lips and external genital organs) or with the teeth and oral mucous membranes, with a view, exclusively or mainly, to cleaning them, perfume, modify their appearance, protect them, keep them in good condition or correct body odors and characterized in that it comprises at least one water-soluble extract of defatted fruits or seeds of African Xylopia aethiopica of the Annonaceae family with the aim of advantageously using a multifunctional active ingredient allowing both to reduce aging, strengthen the barrier effect of the skin, its cohesion and its homeostasis, to slow down epidermal proliferation in order to give it more time to build up well while promoting its good maturation and its good differentiation including that of the horny envelopes. In order to also allow the protection of the extracellular matrices and a good formation of their collagens contributing to the improvement of the firmness of the skin.

[0010] The applicant has in fact tested several aqueous or hydroethanolic extracts of Xylopia aethiopica on the complete genome of normal human keratinocytes and particularly by analysis of gene expression at the scale of the entire genome (36,000 transcribed genes and variants) of normal human epidermal keratinocytes following the extraction of the total transcribed RiboNucleic Acids (RNA) followed by hybridization on DeoxyRibonucleic Acid (DNA) microchips. The principle of the DNA chip is based on the property that denatured DNA (single strand) has of spontaneously reforming its double helix when it is in the presence of a complementary strand (hybridization reaction). Since it is possible to attach up to a million probes to a biochip, DNA chips constitute a massive approach that the inventor used since they allow in a single experiment to have an estimate on the expression of several tens of thousands of genes.

[0011] The invention therefore relates to a cosmetic composition comprising a water-soluble extract of defatted fruits or seeds of African Xylopia aethiopica of the Annonaceae family and a cosmetically acceptable vehicle.

[0012] Advantageously, said cosmetically acceptable vehicle is also that used as solvent during the extraction and is chosen from water with or without enzyme, a hydroethanolic solution or a water / glycerol mixture.

[0013] Also advantageously, said water-soluble extract of fruits or seeds of Xylopia aethiopica is produced from fruits or seeds previously defatted by cold pressing, one to three times successively, in order to obtain a content of 10% or less by mass of lipids relative to the total mass of the fruits or seeds.

[0014] Even more advantageously, said water-soluble extract of delipidated fruits or seeds of Xylopia aethiopica comprises less than 1% by mass of lipids relative to the total mass of the extract, in particular from 0% to 1% by mass of lipids relative to the total mass of the extract.

[0015] In the context of the invention, the term “from 0% to 1% by mass of lipids” means: fact that the extract may comprise 0, 0.25, 0.5, 0.75, 1% by mass of lipid relative to the mass of the extract.

[0016] Also within the scope of the invention, said extract of delipidated fruits or seeds of Xylopia aethiopica has been made water-soluble by solubilization in a solvent chosen from water with or without enzyme, a hydroethanolic solution or a water / glycerol mixture before being able to be used as is in the composition or stored after complete drying before being resolubilized in these same cosmetically acceptable solvents before use.

[0017] In the context of the invention, the term "water-soluble extract of a plant or part of a plant such as seeds" means the result of any extraction in a water-soluble solvent such as, for example, water itself, a hydroethanolic solution or glycerin and which can both serve as a cosmetically acceptable vehicle and therefore be formulated directly in order to produce a final cosmetic composition. These extracts can be formulated directly at around 0.1% to 5% or stored in the dry state after evaporation of the water or water plus ethanol or even as is in the case of a glycerin solvent.

[0018] Advantageously, the composition is characterized in that said water-soluble extract of delipidated fruits or seeds of Xylopia aethiopica represents from 0.1% to 5% by mass relative to the total mass of the composition.

[0019] In the context of the invention, the term "from 0.1% to 5% by mass" means that the composition may comprise 0.1, 0.2, 0.3, 0.4, 0.5, 0.6, 0.7, 0.8, 0.9, 1, 1.1, 1.2, 1.3, 1.4, 1.5, 1.6, 1.7, 1.8, 1.9, 2, 2.1, 2.2, 2.3, 2.4, 2.5, 2.6, 2.7, 2.8, 2.9, 3, 3.1, 3.2, 3.3, 3.4, 3.5, 3.6, 3.7, 3.8, 3.9, 4, 4.1, 4.2, 4.3, 4.4, 4.5, 4.6, 4.7, 4.8, 4.9 or 5% by mass of defatted extract relative to the total mass of the composition.

[0020] The effects of different plant extracts were thus investigated on gene expression in Normal Human Epidermal Keratinocytes (NHEK). More precisely, a complete transcriptome analysis (full transcriptome), i.e. all the genes expressed at a given time, was carried out using the Affymetrix GeneAtlas platform and the U219 “full human transcriptome” chip containing 36,000 so-called transcribed genes and variants.

[0021] This method, described in more detail in the examples below, makes it possible to choose, depending on the genes stimulated, i.e. whose expression is significantly increased, or inhibited, i.e. whose expression is significantly reduced, the most interesting plants for cosmetic use and which has made it possible to show the interest of Xylopia aethiopica of the Annonaceae family among other plants thus tested.

[0022] Then by taking the most interesting gene or genes, this method allows the optimum protocol(s) to be selected in order to obtain the best possible results. Here for Xylopia aethiopica of the Annonaceae family the Insulin-like Growth Factor Binding Protein 3 (IGFBP3) gene was used to determine that it was the delipidated fruits or seeds then extracted in a simple solvent which allowed to obtain an increase in expression of more than 2000% in contact with normal human keratinocytes (NHEK). The relative expression of this IFGBP3 gene in the control keratinocytes had a signal intensity of 32.66 while in the keratinocytes put in contact with the water-soluble extract of Xylopia aethiopica thus selected had a signal intensity of 710.74, i.e. a stimulation of the expression of this gene called fold change or rate of modification, under the experimental conditions, of 21.75 times.

[0023] This made it possible to determine an optimum when the extraction was carried out in simple solvents such as water, hydroethanolic mixtures in which the ethanol is then recycled after complete evaporation or mixtures of water and glycerin, whose moisturizing properties for the skin are no longer in doubt.

[0024] These tests make it possible to demonstrate the interest of a cosmetic composition characterized in that it is made up of a water-soluble extract of defatted fruits or seeds of African Xylopia aethiopica of the Annonaceae family produced by mechanical separation of the fruits or seeds from the fruits followed by drying for at least 1 day and then by one or more cold pressings of these fruits or seeds, after or without prior roasting, followed again by drying in an oven for 1 to 5 hours and at a temperature between 50°C and 60°C in order to avoid the proliferation of microorganisms, then by extraction or maceration in water with or without the addition of enzymes, a hydroethanolic solution or a water / glycerol mixture or even by maceration in glycerol alone and which can then be filtered or centrifuged and be stored and used directly in their respective solvent or dried again or freeze-dried or even zeodrated,having the effect of reducing aging, strengthening the barrier effect of the skin, its cohesion and homeostasis, slowing down epidermal proliferation in order to give it more time to build up properly while promoting its proper maturation and differentiation, including that of the horny envelopes. In order to also protect the extracellular matrices and good formation of their collagens, contributing to improving the firmness of the skin.

[0025] The invention also relates to a water-soluble extract of defatted fruits or seeds of African Xylopia aethiopica of the Annonaceae family, characterized in that it comprises water with or without enzyme, a hydroethanolic solution or a water / glycerol mixture and that it is prepared from 10% by weight of defatted then dried fruits or seeds.

[0026] Which makes it possible to obtain a water-soluble extract of defatted fruits or seeds of African Xylopia aethiopica of the Annonaceae family characterized in that it is intended to be applied to healthy skin to strengthen and promote skin protection to reduce aging, strengthen the skin's barrier effect, its cohesion and homeostasis, slow down epidermal proliferation in order to give it more time to build well while promoting its good maturation and good differentiation including that of the horny envelopes. In order to also protect the extracellular matrices and a good formation of their collagens contributing to the improvement of skin firmness.

[0027] Or more precisely a water-soluble extract of delipidated fruits or seeds of African Xylopia aethiopica of the Annonaceae family for the treatment or prevention of negative effects caused by aging, an alteration of the barrier effect of the skin, its cohesion and its homeostasis, an increase in epidermal proliferation not allowing it to build up completely and correctly, without sufficient maturation and differentiation with fragile horny envelopes;when the negative effects also concern the extracellular matrices too degraded by peptidases and with poor formation of their collagens leading to a loss of firmness, all linked to an under-expression of Insulin-like Growth Factor Binding Protein 3 (IGFBP3), TransGlutaMinase 1 (TGM1), Capsasel4 (Capsl4), Desmoglein 1 (DSG1), DeCoriN (DCN) or even, on the contrary, in the context of the over-expression of genes promoting skin problems, the destruction of extracellular matrices and the loss of homeostasis, such as Matrix MetalloPeptidases 1, 3 and 10 (MMPI,3,10), XIAP Associated Factor 1 (XAF1) and TransGlutaMinase 2 (TGM2). ;

[0028] Indeed, Insulin-like Growth Factor Binding Protein 3 (IGFBP3) is a true marker of aging which decreases when senescence is induced in skin cell culture by hydrogen peroxide (H2O2) compared to cells that have remained young. There is therefore a cosmetic interest in increasing its expression physiologically. The increase in the expression of 1TGFBP3 induces a partial inhibition of the processes of proliferation, division and progression of the epidermal cell cycle allowing the epidermis and its horny layer to have more time to build up properly, which is further promoted by Capsase 14 when it is also better expressed. Capsacel4 is a protease encoded by the CAPS 14 gene and is a protease playing a central role in apoptosis phenomena, a true regulator of cellular homeostasis, as well as in the terminal differentiation of keratinocytes. It thus allows a barrier effect for the skin and the regulation of insensible water loss of the skin which has all the time to express itself when 1TGFBP3 is active. Apoptosis which is slowed down by two genes, XIAP Associated Factor 1 (XAF1) and Transglutaminase 2 (TGM2) which are precisely inhibited by the water-soluble extract of defatted fruits or seeds of Xylopia aethiopica. There is therefore an interest for skin homeostasis in reducing its expression. Desmoglein is a desmosomal protein naturally encoded by the DSG1 gene, mainly expressed in the last layers of the epidermis and responsible for the adhesion properties of the famous desmosomes, a real snap button, ensuring cell-cell junction essential to the barrier effect of the skin and its cohesion. Transglutaminase 1 (TGM1) is a protein that allows the polymerization of proteins that will form the horny envelope during the terminal differentiation of keratinocytes into corneocytes. Decorin is a protein encoded by the DCN gene that binds around collagen fibers to control their diameter, which is thus homogeneous in the extracellular matrix, guaranteeing firmness and homogeneity, which deteriorates like firmness during aging. Matrix metallopeptidase 1 (MMPI) is a protein encoded by the MMPlet gene and is part of a group of MMP genes that degrade the extracellular matrix by attacking its fibers such as collagens but also growth factors that often prevent healing. MMP3 and MMP10 are stomelysins that degrade several types of collagen but also fibronectin, laminin and elastin, the latter all playing a role in skin firmness. These 3 MMPs, significantly inhibited by the said extract, all participate in the dismantling of the extracellular matrix and reducing their expression is therefore favorable to maintaining skin firmness.

[0029] The invention also relates to the cosmetic use of water-soluble extract of delipidated fruits or seeds of African Xylopia aethiopica of the An-nonaceae family intended to be used for the treatment or prevention of negative effects caused by aging, an alteration of the barrier effect of the skin, its cohesion and its homeostasis, an increase in epidermal proliferation not allowing it to build up completely and correctly, without sufficient maturation and differentiation with fragile horny envelopes;when also the negative effects concern the extracellular matrices too degraded by peptidases and with a poor formation of their collagens leading to a loss of firmness, all linked to an under-expression of Insulin-like Growth Factor Binding Protein 3 (IGFBP3), TransGlutaMinase 1 (TGM1), Capsasel4 (Capsl4), Desmoglein 1 (DSG1), DeCoriN (DCN) or even, on the contrary, in the context of the over-expression of genes promoting skin problems, the destruction of extracellular matrices and the loss of homeostasis, such as Matrix Metallo-Peptidases 1, 3 and 10 (MMPI,3,10), XIAP Associated Factor 1 (XAF1) and Trans- ; Glutaminase 2 (TGM2)

[0030] All characterized in that the aqueous, hydroethanolic or hydro-glycerin extracts are capable of improving the expression of Binding Protein 3 (IGFBP3), TransGlutaMinase 1 (TGM1), Capsasel4 (Caps 14), Desmoglein 1 (DSG1), DeCoriN (DCN) and of reducing those of Matrix MetalloPeptidases 1, 3 and 10 (MMPI,3,10), XIAP Associated Factor 1 (XAF1) and TransGlutaMinase 2 (TGM2) optimized by the analysis of gene expression at the whole genome scale (36,000 transcribed genes and variants) of normal human epidermal keratinocytes and by hybridization on DNA microarrays.

[0031] The invention further relates to the cosmetic use of water-soluble extract of delipidated fruits or seeds of African Xylopia aethiopica of the An-nonaceae family intended to be used to induce a pro-differentiating effect by increasing the expression of genes coding for keratinocyte differentiation (SPRR2A, DCN, DSG1, TGM1, KRT1) knowing that: SPRR2A and 2D correspond to small proteins released during the maturation or differentiation of keratinocytes and which are then taken up by transglutaminases at the level of the stratum corneum to form the horny envelope surrounding the corneocytes giving them sufficient rigidity to allow good cohesion and therefore an essential barrier effect as well as a beautiful appearance on the surface of the skin. KRT1 for Keratin 1 is a keratin and an intermediate filament of the cytoskeleton playing an important role in maintaining the skin barrier. TGMlest, as already seen above, the gene that produces Transglutaminase 1, a protein that allows the polymerization of the different molecules that form the envelopes of corneocytes (involucrin, keratin 1, small SPRR-type proteins). DSG1 for Desmoglein 1, as also already seen above, it is a desmosomal protein naturally encoded by the DSG1 gene, mainly expressed in the last layers of the epidermis and responsible for the adhesion properties of the famous desmosomes, a real snap button, ensuring the cell-cell junction essential to the barrier effect of the skin and its cohesion. The epidermis therefore sees its keratinocytes differentiate better, its horny envelopes form better, as a result of which the skin will be more beautiful on the surface, more resistant to the harmful effects of aging and presenting a better quality barrier effect.

[0032] Advantageously, the invention relates to the non-therapeutic cosmetic use of a composition, for topical application to healthy skin with the aim of advantageously using a multifunctional active ingredient making it possible to both reduce aging, strengthen the barrier effect of the skin, its cohesion and its homeostasis, and slow down epidermal proliferation in order to give it more time to build itself up properly. while promoting its proper maturation and differentiation including that of the horny envelopes, while protecting the extracellular matrices and the proper formation of their collagens contributing to improving the firmness of the skin.

[0033] For cosmetic use, we then see the interest of a composition comprising a water-soluble extract of delipidated fruits or seeds of African Xylopia aethiopica of the Annonaceae family, characterized in that it is in the form of an oil-in-water (O / W) or water-in-oil (W / O) emulsion, multiple emulsion (O / W / O, W / O / W), microemulsion, twin-phase emulsion, PIT emulsion, nanoemulsion, pseudoemulsion, aqueous gel, fatty gel, hydroalcoholic gel, suspension, freeze-dried gel or emulsion and / or one of the preceding forms containing microcapsules, nanocapsules, liposomes, ethosomes and which can be presented in the form of creams, serums, liquids, pastes, lotions, emulsions, gels, solids, powders, masks, sticks, sprays, aerosols.

[0034] As well as a composition comprising a water-soluble extract of defatted fruits or seeds of African Xylopia aethiopica of the Annonaceae family obtained by the process according to characterized in that it is in the form of a two-phase micellar makeup remover, a foaming gel, a gel lotion, an exfoliant, a moisturizing cream, a moisturizing serum, a serum improving the appearance of wrinkles, a moisturizing body milk, a regenerating mask, a regenerating cream, a slimming body cream, an anti-aging cream, a regenerating serum, a balm, a mist, an eye treatment, a concentrate, or a detoxifying mask.

[0035] All this therefore allows the non-therapeutic cosmetic use of a water-soluble extract of delipidated fruits or seeds of African Xylopia aethiopica of the Annonaceae family, characterized in that the composition is applied to healthy skin, with the aim of advantageously using a multifunctional active ingredient allowing both to reduce aging, to strengthen the barrier effect of the skin, its cohesion and its homeostasis, to slow down epidermal proliferation in order to give it more time to build up well while promoting its good maturation and its good differentiation including that of the horny envelopes. In order to also allow the protection of the extracellular matrices and a good formation of their collagens contributing to the improvement of the firmness of the skin.

[0036] Cosmetic care method for healthy skin to advantageously use a multifunctional active ingredient allowing at the same time to reduce aging, reinforce the barrier effect of the skin, its cohesion and its homeostasis, to slow down epidermal proliferation in order to give it more time to build up well while promoting its good maturation and its good differentiation including that of the horny envelopes and also to allow to protect the extracellular matrices and a good formation of their collagens contributing to the improvement of the firmness of the skin, comprising the topical administration of a cosmetic composition of a water-soluble extract of delipidated fruits or seeds of Xylopia aethiopica and optimized by the use of analysis of the expression of the whole genome (full genome) of cultured human keratinocytes (NHEK) in order to determine all of their properties as well as the optimization of their preparations, the association of enzymes or not during the extraction or maceration stages, the interest or not of prior roasting, the % of delipidated and dried fruits or seeds or the nature of the final drying and characterized both by an increase in the expression of certain genes of interest and by a decrease in the expression of other genes of interest.

[0037] Examples are given below without being limiting in order to illustrate the invention:

[0038] Example 1. Obtaining delipidated water-soluble extracts of fruits or seeds of Xylopia aethiopica: The water-soluble extracts of defatted fruits or seeds of African Xylopia aethiopica of the Annonaceae family are made by mechanical separation of the fruits or seeds from the fruits followed by drying for a minimum of 1 day and then by one or more cold pressings of these seeds or fruits, after or without prior roasting, followed by drying in an oven for 1 to 5 hours and at a temperature between 50°C and 60°C in order to avoid the proliferation of microorganisms, then extraction or maceration in water with or without the addition of enzymes, a hydroethanolic solution or a water / glycerol mixture or even maceration in glycerol alone and which can then be filtered or centrifuged and be stored and used directly in their respective solvent or dried again or freeze-dried or even zeodrated. They can therefore include water with or without enzyme, a hydroethanolic solution or a water / glycerol mixture and be prepared from 10% by weight of defatted fruits or seeds then dried from the solvent used for extraction or maceration. These extracts can be tested directly or can be dried, dehydrated, lyophilized or zeodrated before testing. In the latter case, they are rehydrated or diluted with purified water as a solvent. We will call EXA (for Xylopia Aethiopica Extract) the extracts obtained and used in the following examples.

[0039] Example 2. Tests and example results. The biological model: Normal human epidermal keratinocytes (NHEK) at passage 3, cultured at 37°C and 5% CO2. Culture medium supplemented with EGF at 0.25ng / ml and EP at 25ug plus gentamicin 25ug. The test medium consists of keratinocytes SFM with only gentamicin 25 ug / ml. Experimental conditions: Keratinocytes were seeded in 24-well plates and cultured in culture medium for 24 hours and then in test medium for another 24 hours. The medium was then replaced with test medium containing or not (control) the test compounds and the cells were incubated for 24 hours. All experimental conditions were carried out in triplicate (n=3). At the end of the incubation, the culture supernatants were removed and the cell lawns were rinsed with PBS solution. The plate was immediately frozen dry at -80°C. Prior to extraction, culture replicates were pooled. Total RNA from each sample was extracted using TriPure Isolation Reagent® according to the supplier's recommended protocol. RNA quantity and quality were assessed by capillary electrophoresis (Bioanalyzer 2100, Agilent). The synthesis of biotinylated antisense RNA (aRNA) was carried out using the “GeneChip 3TVT Express” kit (Affymetrix®). For each biotinylated RNA sample, an electrophoretic profile was performed (Bioanalyzer 2100, Agilent) before and after fragmentation. Hybridization of labeled and fragmented aRNAs to the Affymetrix® U219 chip (36,000 transcripts and variants) was performed on the GeneAtlas™ fluidics Affymetrix® hybridization station for 20 hours at 45°C. The U219 chips were then scanned using the GeneAtlas™ Imaging station (Affymetrix® - resolution 2 pm) to generate signal intensity data as shown in the example results below. Signal intensity data were normalized using Expression Console software (Affymetrix®), based on the RMA algorithm. Quality control of the labeling and hybridization was then performed. Quality controls of the hybridization and labeling steps allowed validation of the experimental process Once normalized with Expression Console software, the data was transferred and formatted into a Microsoft Excel file. Calculations and filters have been added to these files to sort the data and make it easier to use. The fold change thresholds (value corresponding to the ratio: signal intensity value of a probe corresponding to the treated sample / signal intensity value of a probe corresponding to the control) were defined and applied to the normalized data. The following abbreviations are used in the analysis files: - UR: Upregulated - over-expression or stimulation of the probe or gene when the fold change is greater than 2, - DR: Downregulated - underexpression or inhibition of the probe or gene when the fold change is less than 0.5. Each analysis file consists of: - The signal intensity value (RE: Relative Expression) corresponding to each of the samples, - Calculations of “fold change” or modification rate for each comparison, Information relating to each gene. Filters inserted into these files allow the selection of significantly modulated genes. Examples of gene probes corresponding to the variation in expression of Insulin-like Growth Factor Binding Protein 3 (IGFBP3), TransGlutaMinase 1 (TGM1), Capsasel4 (Capsl4), Desmoglein 1 (DSG1), DeCoriN (DCN) or Matrix MetalloPeptidases 1, 3 and 10 (MMPI,3,10), XIAP Associated Factor 1 (XAF1) and TransGlutaMinase 2 (TGM2) obtained with this methodology and with EXA for the Extract of delipidated fruits or seeds of Xylopia aethiopica, the numbers indicated correspond to the intensity of the signal obtained for the control and for the EXA test: Signal intensity for Insulin-like Growth Factor Binding Prot.3 (IGFBP3): - Control: 32.66 - EXA: 710.37 - Change rate: 21.75 - Regulation: UR Signal intensity for Transglutaminase 1 (TGM1): - Control: 57.55 - EXA: 239.96 - Modification rate: 4.17 - Regulation: UR Signal intensity for Capsasel4 (Caps 14): - Witness: 24.33 - EXA: 82.48 - Change rate: 3.39 - Regulation: UR Signal intensity for Desmoglein 1 (DSG1): - Control: 37.34 - EXA: 169.10 - Modification rate: 4.53 - Regulation: UR Signal intensity for Decorin (DCN): - Witness: 20.00 - EXA: 69.86 - Change rate: 3.49 - Regulation: UR Signal intensity for Matrix Metallopeptidase 1 (MMPI): - Witness: 420.32 - EXA: 59.20 - Change rate: 0.14 - Regulation: DR Signal intensity for Matrix Metallopeptidase 3 (MMP3): - Witness: 290.23 - EXA: 46.48 - Change rate: 0.16 - Regulation: DR Signal intensity for Matrix Metallopeptidase 10 (MMP 10): - Witness: 543.10 - EXA: 57.78 - Change rate: 0.11 - Regulation: DR Signal intensity for XIAP Associated Factor 1 (XAF1): - Witness: 270.36 - EXA: 87.14 - Change rate: 0.32 - Regulation: DR Signal intensity for Transglutaminase 2 (TGM2): - Witness: 246.45 - EXA: 26.61 - Change rate: 0.11 - Regulation: DR

[0040] In the examples below, which give examples of how these compositions are produced, without this list being exhaustive, the following abbreviations will be used: EXA for the extract of defatted fruits or seeds of Xylopia ae-thiopica.

[0041] Example 3. According to a first embodiment of the invention, the composition comprises for a liposome cream: - Cetyl alcohol..................................................................................4 g - B-sitosterol..................................................................................4 - Dicetyl phosphate................................................................................0.5 g - Preservative............................................................................0.3 g - Carbopol 981 ...................................................................0.2 g - Triethanolamine.........................................................................0.2 g - Phospholipid.............................................................................0.05 g - EXA..................................................................................1.5 g - Demineralized water qsp.................................................................100 g After use on a panel of 40 volunteers aged 18 to 70, the skin emerged significantly hydrated during the 3 hours of the first application, softer and looking younger and firmer for 65% of users after 4 weeks of daily use. The cohesion of the skin and its barrier effect are visibly improved, demonstrating an improvement in its homeostasis.

[0042] Example 4 According to a second embodiment of the invention, the composition comprises: Carboxypolymethylene or carboxylic polymer..................0.40 g Diethanolamine cetyl phosphate............................................1.50 g Octyl dodecanol............................................................5.50 g Cetyl alcohol..................................................................1.00 g Mineral oil.................................................................2.00 g Stearic acid.................................................................1.00 g Ethoxylated steryl alcohol (20 E)...........................................0.30 g Cetostearyl alcohol.................................................................1.80 g Preservative.................................................................0.15 g Baobab oil........................................................................0.50 g Triethanolamine..........................................................0.60 g Cyclomethicone............................................................12.00 g Dimethicone copolyol........................................................3.00 g Phenyl trimeticone................................................................2.00 g EXA................................................................................3.00 g Dextran.........................................................................1.00 g Glycerin............................................................................2.00 g Demineralized water qsp........................................................100 g After 4 weeks of use on 35 volunteers, the skin appeared smoothed 2 hours after each application. At the end of treatment, the number of wrinkles, their length and width were significantly reduced and the skin was more hydrated for 92% of users. readers. Overall, the appearance of the skin is visibly improved and it appears less aged and less stressed.

[0043] Example 5 According to a second embodiment of the invention, the composition comprises: - Acrylate C10-30........................................................0.50 g - Arginine............................................................0.001g - Glycerin..................................................................................1.00 g - EXA..........................................................................................0.20 g - Alcohol.................................................................2.00 g - Carbomer................................................................................0.126 g - EDTA..............................................................................................0.005 g - Preservative.......................................................................0.867 g - Jojoba oil.............................................................................0.5 g - Hydrogenated lecithin..................................................0.09 g - Hyaluronic acid....................................................................0.20 g - TEA 99%...................................................................................0.62 g - Colorings........................................................................0.0002 g - Demineralized water qsp.................................................................100 g After 4 weeks of use for 30 volunteers aged 20 to 70, the skin appeared significantly more hydrated and more beautiful.

[0044] Example 6. H / W emulsion: - Liquid paraffin.................................................6 g - Liquid lanolin................................................................3 g - Arlacel 165................................................................6 g - Tween 60...................................................................2 g - Cetyl alcohol................................................................1.2 g - Stearic acid.................................................2.5 g - Arginine........................................................................0.5 g - Volatile silicone oil................................................................10 g - Triethanolamine................................................................0.1g - Preservative.................................................................0.3 g - EXA..........................................................................5 g - Hyaluronic acid.......................................................0.5 g - Demineralized water qsp..................................................100 g. After 4 weeks of twice-daily use by 30 volunteers aged 33 to 70, the skin appeared significantly more toned and firmer for 100% of users.

[0045] Example 7 W / O emulsion: - Protégin......................................................................19g - Glycerin..................................................................................3 g - Vaseline oil.................................................................................8 g - Mg sulfate.............................................................................0.5 g -EXA........................................................................0.5 g - Hyaluronic acid.................................................................0.02 g - Preservative............................................................2 g - Demineralized water qsp.................................................................100 g

[0046] Example 8. O / W gel emulsion - Carbopol 981 ..................................................................0.6 g - Ethyl alcohol.................................................................................15 g - Volatile silicone oil..................................................................3 g - Jojoba oil.............................................................................7 g - Preservative............................................................0.3 g - Perfume...................................................................0.4 g -EXA........................................................................................0.1 g - Triethanolamine........................................................................0.2 g - Demineralized water qsp.................................................................100 g

[0047] Example 9. Glycerin concentrate - Glycerin......................................................................65 g -EXA..................................................................................................5 g - Arginine........................................................................................1 g - Hyaluronic acid.........................................................1 g - Perfume..............................................................0.4 g - Demineralized water qsp.................................................................100 g

Claims

Claims

1. Cosmetic composition comprising a water-soluble extract of delipidated fruits or seeds of African Xylopia aethiopica of the Annonaceae family and a cosmetically acceptable vehicle.

2. Cosmetic composition according to claim 1, wherein said cosmetically acceptable vehicle is also that used as solvent during the extraction and is chosen from water with or without enzyme, a hydroethanolic solution or a water / glycerol mixture.

3. Cosmetic composition according to any one of claims 1 to 2, characterized in that said water-soluble extract of defatted fruits or seeds of African Xylopia aethiopica of the Annonaceae family is produced from fruits or seeds previously defatted by cold pressing, one to three times successively, in order to obtain a content of 10% or less by mass of lipids relative to the total mass of the fruits or seeds.

4. Cosmetic composition according to any one of claims 1 to 3, characterized in that said water-soluble extract of delipidated fruits or seeds of African Xylopia aethiopica of the Annonaceae family comprises less than 1% by mass of lipids relative to the total mass of the extract, in particular from 0% to 1% by mass of lipids relative to the total mass of the extract.

5. Cosmetic composition according to any one of claims 1 to 4, characterized in that said water-soluble extract of delipidated fruits or seeds of African Xylopia aethiopica of the Annonaceae family has been made water-soluble by solubilization in a solvent chosen from water with or without enzyme, a hydroethanolic solution or a water / glycerol mixture before being able to be used as is in the composition or stored after complete drying before being resolubilized in these same cosmetically acceptable solvents before use.

6. Composition according to any one of claims 1 to 5, characterized in that said water-soluble extract of defatted fruits or seeds of African Xylopia aethiopica of the Annonaceae family represents from 0.1% to 5% by mass relative to the total mass of the composition.

7. A composition according to any one of claims 1 to 6, wherein the composition is in the form of an oil-in-water (O / W) or water-in-oil (W / O) emulsion, a multiple emulsion (O / W / O, W / O / W), a mid- croemulsion, twin phase emulsion, PIT emulsion, nanoemulsion, pseudoemulsion, aqueous gel, fatty gel, hydroalcoholic gel, suspension, freeze-dried gel or emulsion and / or one of the preceding forms containing microcapsules, nanocapsules, liposomes, ethosomes and which may be presented in the form of creams, serums, liquids, pastes, lotions, emulsions, gels, solids, powders, masks, sticks, sprays, aerosols.

8. A composition according to any one of claims 1 to 6, said composition being in the form of a two-phase micellar makeup remover, a foaming gel, a gel lotion, an exfoliant, a moisturizer, a moisturizer serum, a serum improving the appearance of wrinkles, a moisturizer body milk, a regenerating mask, a regenerating cream, a slimming body cream, an anti-aging cream, a regenerating serum, a balm, a mist, an eye treatment, a concentrate, or a detoxifying mask.

9. Non-therapeutic cosmetic use of a composition as defined in any one of claims 1 to 8, for topical application to healthy skin with the aim of advantageously using a multifunctional active ingredient which simultaneously reduces aging, strengthens the barrier effect of the skin, its cohesion and its homeostasis, and slows down epidermal proliferation in order to give it more time to build up properly while promoting its proper maturation and differentiation, including that of the horny envelopes, while protecting the extracellular matrices and the proper formation of their collagens, contributing to improving the firmness of the skin.

10. Composition according to any one of claims 1 to 8 for its use in the prevention of the negative effects caused by aging with an alteration of the barrier effect of the skin, its cohesion and its homeostasis, an increase in epidermal proliferation not allowing it to build completely and correctly, without sufficient maturation and differentiation with fragile horny envelopes and when also the negative effects concern the extracellular matrices too degraded by peptidases leading to a loss of firmness, this by improving the expression of Desmoglein 1 (DSG1), DeCoriN (DCN) and by reducing those of Matrix MetalloPeptidases 1, 3 and 10 (MMPI, 3, 10).

Citation Information

Patent Citations

  • Use of Xylopia aethiopica, as an antagonist of alpha 2-adrenergic receptors in adipose, alone or in combination with at least one other alpha-2-blocker for the preparation of a slimming composition and cosmetic composition

    FR2964321A1