WO2012017141A1 - Plant extract for the production of a slimming composition and method of control for slimming using such a composition - Google Patents
Plant extract for the production of a slimming composition and method of control for slimming using such a composition Download PDFInfo
- Publication number
- WO2012017141A1 WO2012017141A1 PCT/FR2011/000430 FR2011000430W WO2012017141A1 WO 2012017141 A1 WO2012017141 A1 WO 2012017141A1 FR 2011000430 W FR2011000430 W FR 2011000430W WO 2012017141 A1 WO2012017141 A1 WO 2012017141A1
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- composition
- extract
- family
- vitellaria
- slimming
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
- A23L33/105—Plant extracts, their artificial duplicates or their derivatives
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/30—Dietetic or nutritional methods, e.g. for losing weight
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
- A61K8/9783—Angiosperms [Magnoliophyta]
- A61K8/9789—Magnoliopsida [dicotyledons]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- 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
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
Definitions
- the present invention relates to the use of a plant extract selected from the group consisting of the Balanitaceae family and the Vitellaria genus for topical or oral cosmetic, pharmaceutical or nutraceutical compositions with lipidic slimming action.
- One of the main objects of the present invention is the discovery, surprisingly and unexpectedly, of plant extracts capable of simultaneously stimulating lipolysis and inhibiting adipocyte differentiation, so as to optimize the slimming action by using two different biological and biochemical pathways from a single plant extract.
- the plant extracts selected from the group consisting of the family Balanitaceae and the genus Vitellaria stimulate the production of Zinc-alpha2-glycoprotein (ZAG), an LMF or lipid mobilization factor (ST RUSSELL Biochim Biophys.
- G6PDH Glucose-6-Phosphate Dehydrogenase
- adipocytes Part of the fat of the human body is stored as triglycerides in the cells of the hypoderm called adipocytes. Thinning accompanies a decrease in fat stored in adipocytes.
- the adipocytes are very active cells, they play a preponderant role in the control of the energy balance of the body.
- the adipocytes ensure the metabolism of fats. Fat anabolism, lipogenesis, results in a process of storage of fatty substances in the form of triglycerides under the action of enzymatic reactions inside the adipocytes.
- Lipogenesis is upregulated by insulin and is either by the uptake into the blood of fatty acids derived from lipoproteins (chylomicrons or very low density lipoproteins VLDL) and their hydrolysis by lipoprotein lipase, or by neosynthesis in the cell. from glucose. Lipogenesis thus leads to the storage of fats in the form of triglycerides in adipocytes. The catabolism of fats, lipolysis, results in a mobilization of triglycerides and their degradation under the action of enzyme, triglycerides lipases. They are activated by cyclic AMP.
- the cyclic AMP is regulated by Adenylate Cyclase, the latter is, moreover, repressed by 5 hydr hydrolysis via phosphodiesterase. Lipolysis thus leads to the release of fatty acids and the destocking of adipocytes.
- Cyclase, or by inhibition of are hydrolyzed by blocking phosphodiesterase.
- NPY neuropeptide Y
- Adipocyte differentiation consists of transforming the pre-adipocytes, themselves derived from dermal fibroblasts, which are non-functional in terms of lipid metabolism control, into functional adipocytes, that is to say capable of storing lipids by lipogenesis. and able to destock them by lipolysis.
- the family Balanitaceae is represented by a single genus Balanites.
- the genus Balanites is mainly represented by the species Balanites aegyptiaca, Balanites maughamii and Balanites wilsoniana. These species are tropical trees and shrubs absent in America. They are characterized by their high content of sapogenins especially at the level of their fruits between 1 and 9%. Their seeds are oleaginous.
- the Balanitaceae family has already found cosmetic applications aimed at decreasing the melanin content and more generally aimed at lightening the skin as demonstrated and published by the applicant in patent FR 0902932. Therefore, it has not been revealed in the literature any use of at least one plant belonging to the family Balanitaceae in or for the preparation of a topical or oral composition intended for thinning.
- Vitellaria belongs to the family Sapotaceae, this genus consists of only one species Vitellaria paradoxa CF. Gaertn. This is a African tropical tree, also called Shea or Butyrospermum parkii. Its seeds are oleaginous, and provide shea butter. This plant is very widely known and used in various cosmetic applications. Traditionally women in West and Central Africa use shea butter topically to maintain and hydrate their skin and that of their baby. They also use this butter as a massage oil to relax muscles and soothe aching joints.
- shea butter has been widely used in the oily phases of oil-in-water emulsions, water-in-oil emulsions, balms or cosmetic oils.
- patent FR 2859103 filed by SILAB describes an especially cosmetic active derived from shea cake having anti-radical and detoxifying properties
- the patent FR 2912055 filed by IDENOV LAB describes a shea extract rich in gallic acid participating in calming skin irritation
- patent FR 2698785 filed by THREL Jean-No ⁇ l shows that a shea extract can potentiate an activator of Adenylate Cyclase on a melanocyte model so as to contribute indirectly to the synthesis of melanin
- patent FR 2676645 SILAB demonstrates that unsaponifiables of shea butter can improve the effectiveness of sunscreens
- SEDERMA discloses the use of cosmetically textile shea butter in encapsulated form
- in FR2779645 patent SEDERMA demonstrates the use of shea combined with a coffee extract to promote healing and generate a soothing effect on the skin. Therefore, it has not been revealed in the literature any use of at least one plant belonging to the genus Vitellaria in or for the
- the composition is a topical or oral cosmetic, pharmaceutical or nutraceutical composition which contains at least one lipophilic vegetable fraction chosen from the group formed by the genus Vitellaria as an active agent against adiposity.
- the composition is a topical or pharmaceutical cosmetic composition which contains at least one lipohile vegetable fraction selected from the group consisting of the Balanitaceae family as an active agent against adiposity.
- the composition is a topical or oral cosmetic or pharmaceutical composition which contains as slimming and lipolytic active agent at least one lipophilic vegetable fraction chosen from the group formed by the genus Vitellaria.
- said or at least one of the active agent (s) active slimming is a lipophilic extract of plant seeds of the genus Vitellaria species paradoxa present in the composition at a concentration expressed as a percentage of weight relative to the total weight of the composition of between 0.0001 and 10%, preferably close to 0.05% according to the tested extract
- the composition is a topical or pharmaceutical cosmetic composition which contains as agent slimming and lipolytic active agent at least one lipophilic plant fraction selected from the group consisting of the family Balanitaceae.
- said or at least one of the slimming active agent (s) is a lipophilic extract of plant seeds of the Balanitaceae family, preferably genus Balanites species aegyptiaca present in the plant. composition at a concentration, expressed as a percentage by weight relative to the total weight of the composition, preferably between 0.0001 and 10%, preferably around 0.5%, depending on the extract tested.
- the oral nutraceutical, pharmaceutical or cosmetic composition contains in each case at least one active agent formed of a lipophilic plant extract of seeds of the genus Vitellaria species paradox, incorporated in a nutraceutically or pharmaceutically acceptable vehicle compatible with oral ingestion, present in the composition at a concentration expressed as a percentage by weight relative to the total weight of the composition, preferably between 0.0001 and 100%, preferably around 1% depending on the extract tested.
- the composition may furthermore comprise any additive usually used in the oral, nutraceutical or pharmaceutical cosmetic field, such as sequestering agents, antioxidants, preservatives, fillers, electrolytes, humectants, dyes, bases or acids.
- any additive usually used in the oral, nutraceutical or pharmaceutical cosmetic field such as sequestering agents, antioxidants, preservatives, fillers, electrolytes, humectants, dyes, bases or acids.
- these additives may be present in the composition in a proportion of from 0% to 99.9999% by weight relative to the total weight of the composition.
- the topical composition contains in each case at least one active agent formed of a plant extract, as mentioned above incorporated in a pharmaceutically or cosmetically acceptable vehicle compatible with a topical application.
- the composition may furthermore comprise any additive usually used in the field of topical or pharmaceutical cosmetics, such as sequestering agents, antioxidants, sunscreens, preservatives, fillers, electrolytes, humectants, dyes, bases or common acids, minerals, perfumes, essential oils, cosmetic active ingredients, moisturizers, vitamins, essential fatty acids, vegetable or mineral oils, silicones or their derivatives, sphingolipids, self-tanning compounds, soothing and protective agents for the skin.
- any additive usually used in the field of topical or pharmaceutical cosmetics such as sequestering agents, antioxidants, sunscreens, preservatives, fillers, electrolytes, humectants, dyes, bases or common acids, minerals, perfumes, essential oils, cosmetic active ingredients, moisturizers, vitamins, essential fatty acids, vegetable or mineral oils, silicones or their derivative
- additives may be present in the composition in a proportion of from 0% to 99.9999% by weight relative to the total weight of the composition.
- the topical or pharmaceutical cosmetic composition for controlling lipolysis and adipocyte differentiation is applicable topically and is in the form of an oil or lotion or an oil-in-water gel or emulsion or a water-in-oil emulsion. or cream.
- the oral, nutraceutical or pharmaceutical cosmetic composition for controlling lipolysis and adipocyte differentiation is ingestable in the form of syrup, capsule, powder, ampoule, oral solution, oil, oil-in-water emulsion or water in oil, dough, chocolate or biscuit.
- the pharmaceutical composition for controlling lipolysis and adipocyte differentiation according to the invention may be in injectable form.
- the injectable form of control is in the form of lotion or gel or emulsion oil in water or water in oil or oil.
- the invention also relates to a method for controlling lipolysis and adipocyte differentiation for cosmetic purposes for thinning in a mammal comprising at least one step of parenteral administration of an effective amount of a selected lipophilic plant extract in the group formed by the family Balanitaceae and the genus Vitellaria.
- formulation below allow to illustrate the compositions according to the invention without however limiting the scope.
- Examples illustrating the activity of stimulating the production of Zinc-alpha2-glycoprotein (ZAG) and of inhibiting the activity of Glucose-6-Phosphate Dehydrogenase (G6PDH) of the various compositions according to the invention are also described, as well as examples illustrating the activity of stimulation of lipolysis.
- the proportions of the various constituents are expressed as a percentage by weight relative to the total weight of the composition.
- a cosmetic topical slimming composition in the form of a cream containing a lipohile extract of Balanites, in particular Balanites aegyptiaca, will be described.
- the vegetable lipohil extract used is derived from the oilseed seeds of Balanites. These seeds are processed, in particular decocated to separate the shell from the kernel.
- the almond is then delipidated preferably by cold pressing or hot almonds, or by extraction with an apolar solvent such as, inter alia, hexane, or by supercritical CO2 extraction to separate the lipid fraction of almonds.
- This lipid fraction undergoes, either according to a first extraction method, an extraction with a polar alcoholic solvent such as, among others, ethanol or methanol containing between 0.01% and 10% of water, and preferably between 3 and 6% of water. water, or, according to a second mode of extraction, extraction with water in supercritical state.
- the supernatant of this extraction contains the active fraction of the lipohile extract according to the invention and can integrate the composition at a concentration preferably in the range 0.001% to 10%
- the directly obtained extract contains the active fraction of the lipohile extract according to the invention and can integrate the composition at a concentration preferably in the range 0.001% to 1%.
- the extract obtained can thus be directly integrated into the topical cosmetic composition or, according to the first extraction mode can be dried by sublimation of the polar alcoholic solvent, in particular under vacuum to obtain a concentrated extract free of solvent.
- the concentrated extract devoid of solvent, is a more or less thick or viscous liquid which can set at room temperature, it is lipophilic and is incorporated in the oily or oily phase of the composition.
- This concentrated extract is incorporated into the composition at a concentration preferably in the range 0.001% to 1%.
- composition may have a formulation as follows:
- Lipophilic extract Balanites aegyptiaca 0.5
- an "anti-pocket" cosmetic composition in the contour of the eyes that is in the form of serum and containing a lipohile extract of Vitellaria, in particular Vitellaria paradoxa will be described.
- the vegetable lipohile extract used is derived from the oil seeds of Vitellaria. These seeds are processed, in particular decocated to separate the shell from the kernel.
- the almond is then delipidated, preferably after mechanical grinding, for example by cold or hot pressing of the almonds, or by extraction with an apolar solvent such as, inter alia, hexane, or by extraction with supercritical CO 2 in order to isolate the lipid fraction of almonds in whole or in part.
- This lipid fraction is then subjected to either an extraction with a polar alcoholic solvent, according to a first extraction method, such as, among others, ethanol or methanol containing between 0.01% and 10% of water, and preferably between 3 and 6%. of water, ie extraction with water in supercritical state, according to a second mode of extraction.
- a first extraction method such as, among others, ethanol or methanol containing between 0.01% and 10% of water, and preferably between 3 and 6%. of water
- a second mode of extraction ie extraction with water in supercritical state
- the extract obtained can thus be directly integrated, with or without a solvent, into the cosmetic composition or, according to the first extraction method, can be dried by sublimation of the polar alcoholic solvent, in particular under vacuum, to obtain a concentrated extract devoid of solvent.
- the concentrated extract, devoid of solvent, according to the first extraction method or the direct extract according to the second extraction method is a more or less thick or viscous liquid which can set at room temperature, it is fat soluble and incorporates in the oily or oily phase of the composition.
- This concentrated extract according to the first extraction method or the direct extract according to the second extraction mode is incorporated in the composition at a concentration, preferably in the range 0.0001% to 3%.
- the composition may have a formulation as follows:
- EXAMPLE 3 An example of a slimming nutraceutical composition in the form of a powder containing a lipohile extract of Vitellaria, in particular Vitellaria paradoxa, will be described.
- a lipohile extract of Vitellaria paradoxa can be the subject of a nutraceutical composition.
- the vegetable lipohile extract used is derived from the oil seeds of Vitellaria. These seeds are processed, in particular decocated to separate the shell from the kernel.
- the almond is then delipidated preferably after grinding mechanical, for example, by cold pressing or hot almonds, or by extraction with an apolar solvent such as, inter alia, hexane, or supercritical CO2 extraction to isolate the lipid fraction of almonds in all or part.
- This lipid fraction is then subjected to either an extraction with a polar alcoholic solvent, according to a first extraction method, such as, among others, ethanol or methanol containing between 0.01% and 10% of water, and preferably between 3 and 6%. of water, ie extraction with water in supercritical state, according to a second mode of extraction.
- a first extraction method such as, among others, ethanol or methanol containing between 0.01% and 10% of water, and preferably between 3 and 6%. of water, ie extraction with water in supercritical state, according to a second mode of extraction.
- the supernatant according to the first extraction method, or the product directly extracted according to the second extraction mode contains the active fraction of the lipohile extract according to the invention.
- the extract obtained can thus be directly integrated, with or without a solvent, into the cosmetic composition or, according to the first extraction method, can be dried by sublimation of the polar alcoholic solvent, in particular under vacuum, to obtain a concentrated extract devoid of solvent.
- the concentrated extract, devoid of solvent, according to the first extraction method or the direct extract according to the second extraction method is a more or less thick or viscous liquid which can set at room temperature, it is fat soluble and incorporates in the oily or oily phase of the composition.
- This concentrated extract according to the first extraction method or the direct extract according to the second extraction mode is incorporated in the composition at a concentration, preferably in the range 0.0001% to 3%.
- the composition may have a formulation as follows: Dehydrated acerola pulp 99% Lipohile extract Vitellaria paradoxa tested 1%
- the vegetable lipohile extract used is derived from the oil seeds of Vitellaria. These seeds are processed, in particular decocated to separate the shell from the kernel.
- the almond is then delipidated, preferably after mechanical grinding, for example by cold or hot pressing of the almonds, or by extraction with an apolar organic solvent such as, inter alia, hexane, or by extraction with supercritical CO 2 so to isolate the lipid fraction of almonds in whole or in part.
- This lipid fraction is then subjected to either an extraction with a polar alcoholic solvent, according to a first extraction method, such as, among others, ethanol or methanol containing between 0.01% and 10% of water, and preferably between 3 and 6%.
- the supernatant according to the first extraction method, or the product directly extracted according to the second extraction mode contains the active fraction of the lipohile extract according to the invention.
- the extract obtained can thus be directly integrated, with or without a solvent, into the cosmetic composition or, according to the first extraction method, can be dried by sublimation of the polar alcoholic solvent, in particular under vacuum, to obtain a concentrated extract devoid of solvent.
- the concentrated extract, devoid of solvent, according to the first extraction method or the direct extract according to the second extraction method is a more or less thick or viscous liquid which can set at room temperature, it is fat soluble and incorporates in the oily or oily phase of the composition.
- This concentrated extract according to the first extraction mode or the direct extract according to the second extraction mode is incorporated in the composition at a concentration, preferably in the range 0.0001% to 100%.
- the composition may have a formulation as follows: Cocoa powder
- Leaf extract Stevia rebaudiana
- compositions containing extracts of Balanites aegyptiaca (Balanitaceae) and Vitellaria paradoxa (Sapotaceae) are compositions that induce destocking of fats in mammals. This destocking is explained by stimulation of lipolysis due to the increased production of Zinc-alpha 2-glycoprotein (ZAG), an LF or lipid mobilization factor which binds to the adrenergic ⁇ 3 adrenergic receptors.
- ZAG Zinc-alpha 2-glycoprotein
- a G protein so as to activate Adenylate Cyclase.
- Adenylate Cyclase then transforms ⁇ into cAMP that activates a protein kinase.
- This protein kinase activates a lipase that degrades the triacylglycerol stored in fatty acids.
- ZAG thus activates the enzymatic cascade which leads to lipolysis.
- ZAG therefore stimulates lipolysis directly by overexpressing cAMP.
- This destocking of fats is also explained by inhibition of differentiation of pre-adipocytes by inhibition of Glucose 6 phosphodihydrogenase (G6PDH).
- the extracts according to the invention can be used in slimming, lipolytic, anti-cellulite, firming, toning, anti-puffiness products under the eyes, and more generally in products intended for to improve and refine the silhouette, the face and the bust.
- compositions may be in the form of capsules glued to textile fibers of slimming garments or of textile impregnated with capsules in contact with the skin or of polymers impregnated with capsules in contact with the skin, of capsules incorporated in massage products, of massage oils, oil-in-water emulsion, water-in-oil emulsion, serum, lotion, gel, soap, in dermocosmetic products, in makeup products, as co-active in firming, tensor and anti-aging products.
- non-rinsed cosmetic products comprising these active ingredients are to be used preferably at least twice a week in a three-month course.
- the rinsed cosmetic compositions comprising these active ingredients are to be used preferably at least twice a day, in course of three months.
- Cosmetics including these assets can be used every day.
- the lipophilic extract of Vitellaria paradoxa in the nutraceutical field, only the lipophilic extract of Vitellaria paradoxa can be used in a "food" manner in view of current European regulations, and therefore incorporate slimming compositions according to the invention.
- the lipohile extract of Vitellaria paradoxa according to the invention may incorporate slimming compositions, or against adiposity, nutraceuticals and pharmaceuticals. These compositions may be in the form of powders, gels, lotions, pastes, gums, chocolates, capsules, capsules, oil-in-water emulsions, water-in-oil emulsions, oils or bulbs.
- the extracts according to the invention can incorporate injectable compositions.
- injectable compositions may be in the form of extemporaneously dilutable powders, gel, lotion, serum, oil-in-water or water-in-oil emulsion.
- the extracts selected for the demonstration are extracts from a hydroalcoholic extraction of the lipid fraction of the seeds of the plants, then concentrated by vacuum evaporation of ethanol and water using a "rotavapor" system.
- the lipohile extract of the lipid fraction of Balanites aeqyptiaca seeds has a composition as follows: Lipid fraction of the seed 50% Ethanoi 96 ° 50%
- composition being expressed as a percentage by weight relative to the total weight of said composition.
- This extract is kept stirring in the dark for 4 hours at room temperature. This extract is allowed to settle in the dark at room temperature for 24 hours. The supernatant is recovered.
- the supernatant is then concentrated by evaporation of the 96 ° ethanol in a "rotavapor” system at 40 ° C. under vacuum.
- the resulting concentrated extract is referred to in the following as "LIPOHILE EXTRACT BALANITES AEGYPTIACA TEST".
- the lipohile extract of the lipid fraction of the seeds of Vitellaria paradoxa has a composition as follows:
- composition being expressed as a percentage by weight relative to the total weight of said composition.
- This extract is kept stirring in the dark for 4 hours at room temperature. This extract is allowed to settle in the dark at room temperature for 24 hours. The supernatant is recovered.
- the supernatant is then concentrated by evaporation of the 96 ° ethanol in a "rotavapor” system at 40 ° C. under vacuum.
- the resulting concentrated extract is referred to in the following as "EXTRACT LIPOHILE VITELLARIA PARADOXA TEST".
- the "LIPOIL EXTRACT BALANITES AEGYPTIACA TEST” SNHBCO2 is first diluted to 50% in DMSO (VA /), to be diluted in the culture medium.
- the "LIPOHIL EXTRACT VITELLARIA PARADOXA TEST” SNBKSTBF is first diluted to 10% DMSO (P / V), to be diluted in the culture medium.
- the ZAG is quantified in the culture media using a sensitive and specific ELISA kit, and the proteins contained in the cell lysates are quantified by a spectrocolorimetric method using blue Coomassie (Bradford M., 1976 Anal Biochem., 72, 248-254).
- the results are given in the form of a ratio "ng of ZAG / mg of total proteins of the cell layer" (averages +/- standard deviation, SD).
- the statistical significance of the differences observed between the conditions "control” and "reference product” or "DMSO” is evaluated by a Student's test (Student t-test, p ⁇ 0.05).
- the change in absorbance at 340 nm is directly proportional to the activity of G6PDH.
- the G6PDH solution is incubated for 5 minutes at ambient temperature in the presence of substrates, and in the absence (buffer alone) or in the presence of EDTA (reference product) or increasing concentrations of active ingredients.
- VA / concentrations
- PAZ concentrations
- a "white product” is produced in the absence of G6PDH, for each of the concentrations of the products tested to take into account a possible absorbance at 340 nm of the test assets.
- the "LIPOIL EXTRACT BALANITES AEGYPTIACA TEST” SNHBCO2 is first diluted to 50% in DMSO (VA /), to be diluted in the culture medium.
- the "LIPOHIL EXTRACT VITELLARIA PARADOXA TEST” SNBKSTBF is first diluted to 10% of DMSO (P V), to be diluted in the culture medium.
- the amplitude of the enzymatic reaction is evaluated after 5 minutes of incubation in the presence of substrate and of the products under test, by spectrocolorimetry by reading the absorbance of the reaction mediums at 340 nm.
- the effect of the test product on the activity of G6PDH is calculated using the following formula: Q, [OD; *; in the presence of. " inhibitor ⁇ 100
- the results are given as a percentage of G6PDH activity relative to the control (averages +/- standard deviation, SD).
- the statistical significance of the differences observed between the conditions "Control” and “reference product” or “DMSO 1%” is evaluated by a Student t-test (p ⁇ 0.001) and a one-way analysis of variance (One Way ANOVA), followed by a Holm-Sidak test (p: ⁇ 0.05).
- the statistical significance of the observed differences between the conditions "control” and "product under test” is evaluated product by product, by a one-way analysis of variance (One Way ANOVA), followed, where necessary, by a Holm-Sidak test (p ⁇ 0.05).
- results presented in FIG. 2 relate to the active ingredients "EXTRACT LIPOHILE BALANITES AEGYPTIACA TEST” and “EXTRACT LIPOHILE VITELLARIA PARADOXA TEST” and show that under the experimental conditions selected after 5 minutes of incubation, the active ingredients “EXTRACT LIPOHILE BALANITES AEGYPTIACA TESTE” and “LIPOHILE EXTRACT VITELLARIA PARADOXA TESTE” significantly inhibit the activity of G6PDH. These results are validated by the fact that the 5 mM EDTA, used as a reference product, significantly inhibited the enzyme reaction in an expected manner after 5 minutes of incubation.
- the keratinocytes were incubated for 48 hours at 37 ° C. C, in a humid atmosphere and at 5% CO2, in absence (control) or in the presence of dexamethasone at 10 ⁇ (reference product) or in the presence of increasing concentrations of the test substances.
- PA concentrations
- PA concentrations
- SNHBCO2 is prepared from a 50% stock solution in DMSO (VA /), then diluted directly in the culture medium, with a maximum concentration of DMSO of 0.01% (VA /).
- SNBKSTBF is prepared from a 10% stock solution in DMSO (PA /), and then diluted directly in the culture medium with a maximum concentration of DMSO of 1% (VA /).
- the reference activators used with respect to lipolytic activity on adipocytes are caffeine and theophylline at 10 -4 M.
- the non-esterified fatty acids are quantified in the incubation media using a sensitive and specific spectrophotometric technique.
- results are given in the form of concentrations (in ⁇ ) of AGNE present in the incubation medium of the adipocytes (average +/- standard derivation, SD).
- the statistical significance of the differences observed between the conditions "control” and “reference product” is evaluated by a Student's test (Student t-test, p ⁇ 0.001).
- Significance statistic of the differences observed between the conditions “Witness” and “Products under test” is evaluated product by product, by a one-way analysis of variance (One Way ANOVA), followed, when this requires a test from Holm-Sidak (p ⁇ 0.05).
- results presented in FIG. 3 relate to the active ingredients "EXTRACT LIPOHIL BALA ITES AEGYPTIACA TEST” and “EXTRACT LIPOHILE VITELLARIA PARADOXA TEST” and show that under the experimental conditions retained after 2 hours of incubation at 37 ° C., the active ingredients “EXTRACT LIPOHILE BALANITES AEGYPTIACA TEST "and” EXTRACT LIPOHIL VITELLARIA PARADOXA TEST "significantly increase lipolysis.
Abstract
The invention relates to an extract of a plant chosen from the group made up of the family Balanitaceae and the genus Vitellaria belonging to the family Sapotaceae for use thereof both as a control agent that is active on lipolysis and as an adipocyte differentiation inhibitor, for the production of a slimming composition.
Description
La présente invention concerne l'utilisation d'un extrait végétal choisi dans le groupe formé par la famille des Balanitaceae et par le genre Vitellaria pour des compositions cosmétiques topiques ou orales, pharmaceutiques ou nutraceutiques à action amincissante iipolytique. The present invention relates to the use of a plant extract selected from the group consisting of the Balanitaceae family and the Vitellaria genus for topical or oral cosmetic, pharmaceutical or nutraceutical compositions with lipidic slimming action.
L'un des principaux objets de la présente invention consiste en la découverte, de façon surprenante et inattendue, d'extraits végétaux capables simultanément de stimuler la lipolyse et d'inhiber la différenciation adipocytaire, de sorte à optimiser l'action amincissante en utilisant deux voies biologiques et biochimiques différentes à partir d'un seul et même extrait végétal. Ainsi, les extraits végétaux choisis dans le groupe formé par la famille des Balanitaceae et par le genre Vitellaria stimulent la production de Zinc-alpha2-glycoprotéine (ZAG), un LMF ou facteur de mobilisation des lipides (ST RUSSELL Biochim. Biophys. Actu. 2004 1636 : 59-68) et inhibent l'activité de la Glucose-6- Phosphate Déshydrogénase (G6PDH), une enzyme qui intervient dans la conversion pré-adipocyte/adipocyte (LM SHANTZ et Al. PNAS 1989 ; 86 : 3852- 3856), comme déjà démontré dans le brevet EP0872244. One of the main objects of the present invention is the discovery, surprisingly and unexpectedly, of plant extracts capable of simultaneously stimulating lipolysis and inhibiting adipocyte differentiation, so as to optimize the slimming action by using two different biological and biochemical pathways from a single plant extract. Thus, the plant extracts selected from the group consisting of the family Balanitaceae and the genus Vitellaria stimulate the production of Zinc-alpha2-glycoprotein (ZAG), an LMF or lipid mobilization factor (ST RUSSELL Biochim Biophys. 2004 1636: 59-68) and inhibit the activity of Glucose-6-Phosphate Dehydrogenase (G6PDH), an enzyme involved in pre-adipocyte / adipocyte conversion (LM SHANTZ et al., PNAS 1989; 86: 3852-3856). ), as already demonstrated in EP0872244.
Une partie de la graisse du corps humain est stockée sous forme de triglycérides dans les cellules de l'hypoderme appelées adipocytes. L'amincissement accompagne une diminution de la graisse stockée dans les adipocytes. Les adipocytes sont des cellules très actives, elles jouent un rôle prépondérant dans le contrôle de l'équilibre énergétique de l'organisme. Les adipocytes assurent le métabolisme des graisses. L'anabolisme des graisses, la lipogénèse, se traduit par un processus de stockage des corps gras sous forme de triglycérides sous l'action de réactions enzymatiques à l'intérieur des adipocytes. La lipogénèse est régulée positivement par l'insuline et se fait soit par captage dans le sang des acides gras issus de lipoprotéines (chylomicrons ou de liproprotéines de très basse densité VLDL) et leur hydrolyse par la lipoprotéine lipase, soit par néosynthèse dans la cellule à partir du glucose. La lipogénèse conduit ainsi au stockage des graisses sous forme de triglycérides dans les adipocytes. Le catabolisme des graisses, la lipolyse, se traduit par une
mobilisation des triglycérides et leur dégradation sous l'action d'enzyme, les triglycérides lipases. Elles sont activées par l'AMP cyclique. L'AMP cyclique est régulée par L'Adenylate Cyclase, cette dernière est, par ailleurs, réprimée par hydrolyse en 5ΆΜΡ via la Phosphodiestérase. La lipolyse conduit ainsi à la libération d'acides gras et au déstockage des adipocytes. Part of the fat of the human body is stored as triglycerides in the cells of the hypoderm called adipocytes. Thinning accompanies a decrease in fat stored in adipocytes. The adipocytes are very active cells, they play a preponderant role in the control of the energy balance of the body. The adipocytes ensure the metabolism of fats. Fat anabolism, lipogenesis, results in a process of storage of fatty substances in the form of triglycerides under the action of enzymatic reactions inside the adipocytes. Lipogenesis is upregulated by insulin and is either by the uptake into the blood of fatty acids derived from lipoproteins (chylomicrons or very low density lipoproteins VLDL) and their hydrolysis by lipoprotein lipase, or by neosynthesis in the cell. from glucose. Lipogenesis thus leads to the storage of fats in the form of triglycerides in adipocytes. The catabolism of fats, lipolysis, results in a mobilization of triglycerides and their degradation under the action of enzyme, triglycerides lipases. They are activated by cyclic AMP. The cyclic AMP is regulated by Adenylate Cyclase, the latter is, moreover, repressed by 5 hydr hydrolysis via phosphodiesterase. Lipolysis thus leads to the release of fatty acids and the destocking of adipocytes.
Si le métabolisme est déséquilibré dans le sens de la lipogénèse, il se produit alors dans les adipocytes une accumulation de triglycérides qui se traduit progressivement par un épaississement de l'hypoderme. La peau se déforme en surface de manière irrégulière et donne l'aspect « d'une peau d'orange ». Cette déformation est disgracieuse, elle affecte la silhouette, elle évolue en embonpoint et peut conduire à l'obésité. If the metabolism is imbalanced in the direction of lipogenesis, then there occurs in the adipocytes an accumulation of triglycerides which gradually results in a thickening of the hypodermis. The skin deforms unevenly on the surface and gives the appearance of "orange peel". This deformity is unsightly, it affects the silhouette, it evolves in overweight and can lead to obesity.
Pour lutter contre cette adiposité différents axes ont été explorés et expérimentés pour moduler le métabolisme des graisses et privilégier la lipolyse, ou pour affecter la capacité de stockage des adipocytes. To fight against this adiposity various axes have been explored and experimented to modulate the fat metabolism and privilege lipolysis, or to affect the storage capacity of adipocytes.
Les différents axes sont : The different axes are:
- Soit le blocage du transport du glucose à l'intérieur de l'adipocyte. - Or blocking the transport of glucose inside the adipocyte.
- Soit l'inhibition des lipoprotéines lipases. - The inhibition of lipoprotein lipases.
- Soit l'activation des triglycérides lipases (lipase hormonosensible), par stimulation de la production d'AMP cyclique sous contrôle de l'Adénylate - The activation of triglyceride lipases (hormone-sensitive lipase) by stimulating the production of cyclic AMP under the control of adenylate
Cyclase, ou par inhibition de sont hydrolyse en bloquant la phosphodiestérase. Cyclase, or by inhibition of are hydrolyzed by blocking phosphodiesterase.
- Soit l'utilisation d'antagonistes des récepteurs du neuropeptide Y (NPY) dont l'implication dans la lipolyse a été démontrée (P. Valet, J. Clin. Invest., 1990, 85, 291-295). Or the use of neuropeptide Y (NPY) receptor antagonists whose involvement in lipolysis has been demonstrated (P. Valet, J. Clin Invest, 1990, 85, 291-295).
- Soit l'utilisation d'antagonistes des récepteurs a2 adrénergiques ou des agonistes des récepteurs 33-adrénergiques pour stimuler la production d'AMP cyclique. Either the use of α 2 -adrenergic receptor antagonists or β-adrenergic receptor agonists to stimulate the production of cyclic AMP.
- Soit la prévention de la différenciation adipocytaire par stimulation de la G6PDH ou par inhibition des métalloprotéinases 2 et/ou 9 selon le brevet de CLARINS FR 286707A1.
- Soit l'utilisation de modulateurs de l'Aquaporine adipeuse (AQPap) pour diminuer le volume des adipocytes et pour augmenter la sortie du glycérol selon le brevet L'OREAL FR 2863492A1. Les inventeurs de la présente invention ont maintenant découvert de façon surprenante et inattendue que les extraits végétaux choisis dans le groupe formé par la famille des Balanitaceae et par le genre Vitellaria agissent à la fois sur un agoniste, la ZAG, des récepteurs 3-adrénergiques, et sur la prévention de la différenciation adipocytaire par inhibition de l'activité de la G6PDH. - Either the prevention of adipocyte differentiation by stimulation of G6PDH or by inhibition of metalloproteinases 2 and / or 9 according to the patent of CLARINS FR 286707A1. - Either the use of modulators Aquaporin adipose (AQPap) to reduce the volume of adipocytes and to increase the glycerol output according to the patent L'OREAL FR 2863492A1. The inventors of the present invention have now surprisingly and unexpectedly discovered that plant extracts selected from the group consisting of the family Balanitaceae and the genus Vitellaria act on both an agonist, ZAG, 3-adrenergic receptors, and on the prevention of adipocyte differentiation by inhibition of G6PDH activity.
La différenciation adipocytaire consiste à transformer les pré-adipocytes, eux- mêmes issus des fibroblastes du derme, non fonctionnels sur le plan du contrôle du métabolisme lipidique, en adipocytes fonctionnels, c'est-à-dire capables de stocker les lipides par lipogénèse, et capables de les déstocker par lipolyse. Adipocyte differentiation consists of transforming the pre-adipocytes, themselves derived from dermal fibroblasts, which are non-functional in terms of lipid metabolism control, into functional adipocytes, that is to say capable of storing lipids by lipogenesis. and able to destock them by lipolysis.
La famille des Balanitaceae est représentée par un seul genre Balanites. Le genre Balanites est essentiellement représenté par les espèces Balanites aegyptiaca, Balanites maughamii et Balanites wilsoniana. Ces espèces sont des arbres et arbustes tropicaux absents en Amérique. Ils se caractérisent par leur teneur élevée en sapogénines notamment au niveau de leurs fruits entre 1 et 9%. Leurs graines sont oléagineuses. La famille des Balanitaceae trouve déjà des applications cosmétiques visant à diminuer la teneur en mélanine et plus généralement visant à éclaircir la peau comme démontré et publié par la demanderesse dans le brevet FR 0902932. Par conséquent, il n'a été révélé dans la littérature aucune utilisation d'au moins une plante appartenant à la famille Balanitaceae dans ou pour la préparation d'une composition topique ou orale destinée à mincir. The family Balanitaceae is represented by a single genus Balanites. The genus Balanites is mainly represented by the species Balanites aegyptiaca, Balanites maughamii and Balanites wilsoniana. These species are tropical trees and shrubs absent in America. They are characterized by their high content of sapogenins especially at the level of their fruits between 1 and 9%. Their seeds are oleaginous. The Balanitaceae family has already found cosmetic applications aimed at decreasing the melanin content and more generally aimed at lightening the skin as demonstrated and published by the applicant in patent FR 0902932. Therefore, it has not been revealed in the literature any use of at least one plant belonging to the family Balanitaceae in or for the preparation of a topical or oral composition intended for thinning.
C'est justement ce type d'utilisation qui fait l'objet de la présente invention. Le genre Vitellaria appartient à la famille des Sapotaceae, ce genre n'est constitué que d'une seule espèce Vitellaria paradoxa CF. Gaertn. Il s'agit d'un
arbre tropical africain, aussi appelé Karité ou Butyrospermum parkii. Ses graines sont oléagineuses, et fournissent le beurre de karité. Cette plante est très largement connue et utilisée dans diverses applications cosmétiques. Traditionnellement les femmes d'Afrique de l'ouest et d'Afrique centrale utilisent le beurre de karité de manière topique pour entretenir et hydrater leur peau et celle de leur bébé. Elles utilisent également ce beurre comme huile de massage pour décontracter les muscles et apaiser les articulations douloureuses. De manière plus originale à la saison sèche en période de vent, et plus particulièrement lorsque l'atmosphère est chargée de poussière, il est souvent observé que ces populations africaines s'enduisent l'intérieur des narines de beurre de karité pour éviter de tomber malade. Dans les produits dermo- cosmétiques, depuis très longtemps, le beurre de karité est un ingrédient largement utilisé dans les phases grasses des émulsions huile dans eau, les émulsions eau dans huile, les baumes ou les huiles cosmétiques. Par ailleurs, le brevet FR 2859103 déposé par SILAB décrit un actif notamment cosmétique issu du tourteau de karité ayant des propriétés anti-radicalaires et détoxifiantes ; le brevet FR 2912055 déposé par IDENOV LAB décrit un extrait de Karité riche en acide gallique participant à calmer l'irritation de la peau ; le brevet FR 2698785 déposé par THREL Jean-Noël montre qu'un extrait de karité permet de potentialiser un activateur de l'Adénylate Cyclase sur un modèle mélanocytaire de sorte à contribuer indirectement à la synthèse de mélanine ; dans le brevet FR 2676645 SILAB démontre que les insaponifiables de beurre de karité permettent d'améliorer l'efficacité des filtres solaires ; dans le brevet FR 2809011 SEDERMA décrit l'utilisation de beurre de karité en cosméto-textile sous forme encapsulé ; dans le brevet FR2779645 SEDERMA démontre l'utilisation de karité combiné à un extrait de café pour favoriser la cicatrisation et générer un effet apaisant sur la peau. Par conséquent, il n'a été révélé dans la littérature aucune utilisation d'au moins une plante appartenant au genre Vitellaria dans ou pour la préparation d'une composition topique ou orale destinée à mincir. It is precisely this type of use which is the subject of the present invention. The genus Vitellaria belongs to the family Sapotaceae, this genus consists of only one species Vitellaria paradoxa CF. Gaertn. This is a African tropical tree, also called Shea or Butyrospermum parkii. Its seeds are oleaginous, and provide shea butter. This plant is very widely known and used in various cosmetic applications. Traditionally women in West and Central Africa use shea butter topically to maintain and hydrate their skin and that of their baby. They also use this butter as a massage oil to relax muscles and soothe aching joints. In a more original way during the dry season during windy periods, and especially when the atmosphere is dusty, it is often observed that these African populations smear themselves inside the nostrils of shea butter to avoid getting sick. . In dermo-cosmetic products, for a very long time, shea butter has been widely used in the oily phases of oil-in-water emulsions, water-in-oil emulsions, balms or cosmetic oils. Furthermore, the patent FR 2859103 filed by SILAB describes an especially cosmetic active derived from shea cake having anti-radical and detoxifying properties; the patent FR 2912055 filed by IDENOV LAB describes a shea extract rich in gallic acid participating in calming skin irritation; patent FR 2698785 filed by THREL Jean-Noël shows that a shea extract can potentiate an activator of Adenylate Cyclase on a melanocyte model so as to contribute indirectly to the synthesis of melanin; in patent FR 2676645 SILAB demonstrates that unsaponifiables of shea butter can improve the effectiveness of sunscreens; in FR 2809011 SEDERMA discloses the use of cosmetically textile shea butter in encapsulated form; in FR2779645 patent SEDERMA demonstrates the use of shea combined with a coffee extract to promote healing and generate a soothing effect on the skin. Therefore, it has not been revealed in the literature any use of at least one plant belonging to the genus Vitellaria in or for the preparation of a topical or oral composition intended for thinning.
C'est justement ce type d'utilisation qui fait l'objet de la présente invention.
Dans un premier mode de réalisation de l'invention, la composition est une composition cosmétique topique ou orale, pharmaceutique ou nutraceutique qui contient au moins une fraction végétale lipophile choisie dans le groupe formé par le genre Vitellaria comme agent actif contre l'adiposité. It is precisely this type of use which is the subject of the present invention. In a first embodiment of the invention, the composition is a topical or oral cosmetic, pharmaceutical or nutraceutical composition which contains at least one lipophilic vegetable fraction chosen from the group formed by the genus Vitellaria as an active agent against adiposity.
Par agent actif contre l'adiposité, les inventeurs désignent un agent actif permettant de réduire le stock adipeux conduisant à un effet minceur. Par agent actif contre l'adiposité, les inventeurs désignent un agent actif pour mincir. Dans un deuxième mode de réalisation de l'invention, la composition est une composition cosmétique topique ou pharmaceutique qui contient au moins une fraction végétale lipohile choisie dans le groupe formé par la famille des Balanitaceae comme agent actif contre l'adiposité. Dans un troisième mode de réalisation de l'invention, la composition est une composition cosmétique topique ou orale, ou pharmaceutique qui contient comme agent actif minceur et lipolytique au moins une fraction végétale lipophile choisie dans le groupe formé par le genre Vitellaria. By active agent against adiposity, the inventors designate an active agent for reducing the adipose stock leading to a slimming effect. By active agent against adiposity, the inventors designate an active agent to slim down. In a second embodiment of the invention, the composition is a topical or pharmaceutical cosmetic composition which contains at least one lipohile vegetable fraction selected from the group consisting of the Balanitaceae family as an active agent against adiposity. In a third embodiment of the invention, the composition is a topical or oral cosmetic or pharmaceutical composition which contains as slimming and lipolytic active agent at least one lipophilic vegetable fraction chosen from the group formed by the genus Vitellaria.
Dans ce mode de réalisation, de préférence, ledit ou au moins l'un des agent(s) actif(s) minceur est un extrait lipophile de graines de végétal du genre Vitellaria espèce paradoxa présent dans la composition à une concentration exprimée en pourcentage en poids rapporté au poids total de la composition comprise entre 0.0001 et 10%, de préférence voisine de 0.05% selon l'extrait testé Dans un quatrième mode de réalisation de l'invention, la composition est une composition cosmétique topique ou pharmaceutique qui contient comme agent actif minceur et lipolytique au moins une fraction végétale lipophile choisie dans le groupe formé par la famille des Balanitaceae. In this embodiment, preferably, said or at least one of the active agent (s) active slimming is a lipophilic extract of plant seeds of the genus Vitellaria species paradoxa present in the composition at a concentration expressed as a percentage of weight relative to the total weight of the composition of between 0.0001 and 10%, preferably close to 0.05% according to the tested extract In a fourth embodiment of the invention, the composition is a topical or pharmaceutical cosmetic composition which contains as agent slimming and lipolytic active agent at least one lipophilic plant fraction selected from the group consisting of the family Balanitaceae.
Dans ce mode de réalisation, de préférence, ledit ou au moins l'un des agent(s) actif(s) minceur est un extrait lipophile de graines de végétal de la famille des Balanitaceae de préférence genre Balanites espèce aegyptiaca présent dans la
composition à une concentration exprimées en pourcentage en poids rapporté au poids total de la composition comprise, de préférence, entre 0.0001 et 10%, de préférence voisine de 0,5% selon l'extrait testé. In this embodiment, preferably, said or at least one of the slimming active agent (s) is a lipophilic extract of plant seeds of the Balanitaceae family, preferably genus Balanites species aegyptiaca present in the plant. composition at a concentration, expressed as a percentage by weight relative to the total weight of the composition, preferably between 0.0001 and 10%, preferably around 0.5%, depending on the extract tested.
Quel que soit le mode de réalisation, la composition nutraceutique, pharmaceutique ou cosmétique orale contient à chaque fois au moins un agent actif formé d'un extrait végétal lipophile de graines du genre Vitellaria espèce paradoxe, incorporé dans un véhicule nutraceutiquement ou pharmaceutiquement acceptable compatible avec une ingestion orale, présent dans la composition à une concentration exprimée en pourcentage en poids rapporté au poids total de la composition comprise, de préférence, entre 0.0001 et 100%, de préférence voisine de 1 % selon l'extrait testé. Whatever the embodiment, the oral nutraceutical, pharmaceutical or cosmetic composition contains in each case at least one active agent formed of a lipophilic plant extract of seeds of the genus Vitellaria species paradox, incorporated in a nutraceutically or pharmaceutically acceptable vehicle compatible with oral ingestion, present in the composition at a concentration expressed as a percentage by weight relative to the total weight of the composition, preferably between 0.0001 and 100%, preferably around 1% depending on the extract tested.
La composition peut comprendre en outre tout additif usuellement utilisé dans le domaine cosmétique oral, nutraceutique ou pharmaceutique, tel que des séquestrants, des anti-oxydants, des conservateurs, des charges, des électrolytes, des humectants, des colorants, des bases ou des acides usuels, des minéraux, des arômes, des huiles essentielles, des actifs nutraceutiques ou pharmaceutiques, des lubrifiants, des édulcorants, des vitamines, des acides gras essentiels, des huiles végétales ou minérales, des agents sucrants. Bien entendu, l'homme du métier veillera à choisir ce ou ces éventuels composés complémentaires et/ou leur quantité de manière telle que les propriétés avantageuses de la composition selon l'invention ne soient pas ou substantiellement pas altérées. Ces additifs peuvent être présents dans la composition à raison de 0% à 99.9999% en poids par rapport au poids total de la composition. The composition may furthermore comprise any additive usually used in the oral, nutraceutical or pharmaceutical cosmetic field, such as sequestering agents, antioxidants, preservatives, fillers, electrolytes, humectants, dyes, bases or acids. Uses, minerals, flavors, essential oils, nutraceutical or pharmaceutical active ingredients, lubricants, sweeteners, vitamins, essential fatty acids, vegetable or mineral oils, sweeteners. Of course, those skilled in the art will take care to choose this or these optional additional compounds and / or their amount in such a way that the advantageous properties of the composition according to the invention are not or substantially not impaired. These additives may be present in the composition in a proportion of from 0% to 99.9999% by weight relative to the total weight of the composition.
Quel que soit le mode de réalisation, la composition topique contient à chaque fois au moins un agent actif formé d'un extrait végétal, tel que mentionné ci- dessus incorporé dans un véhicule pharmaceutiquement ou cosmétiquement acceptable compatible avec une application topique. La composition peut comprendre en outre tout additif usuellement utilisé dans le domaine cosmétique topique ou pharmaceutique, tel que des séquestrants, des antioxydants, des filtres solaires, des conservateurs, des charges, des électrolytes,
des humectants, des colorants, des bases ou des acides usuels, des minéraux, des parfums, des huiles essentielles, des actifs cosmétiques, des hydratants, des vitamines, des acides gras essentiels, des huiles végétales ou minérales, des silicones ou leurs dérivés, des sphingolipides, des composés auto- bronzants, des agents apaisants et protecteurs de la peau. Bien entendu, l'homme du métier veillera à choisir ce ou ces éventuels composés complémentaires et/ou leur quantité de manière telle que les propriétés avantageuses de la composition selon l'invention ne soient pas ou substantiellement pas altérées. Ces additifs peuvent être présents dans la composition à raison de 0% à 99.9999% en poids par rapport au poids total de la composition. Whatever the embodiment, the topical composition contains in each case at least one active agent formed of a plant extract, as mentioned above incorporated in a pharmaceutically or cosmetically acceptable vehicle compatible with a topical application. The composition may furthermore comprise any additive usually used in the field of topical or pharmaceutical cosmetics, such as sequestering agents, antioxidants, sunscreens, preservatives, fillers, electrolytes, humectants, dyes, bases or common acids, minerals, perfumes, essential oils, cosmetic active ingredients, moisturizers, vitamins, essential fatty acids, vegetable or mineral oils, silicones or their derivatives, sphingolipids, self-tanning compounds, soothing and protective agents for the skin. Of course, those skilled in the art will take care to choose this or these optional additional compounds and / or their amount in such a way that the advantageous properties of the composition according to the invention are not or substantially not impaired. These additives may be present in the composition in a proportion of from 0% to 99.9999% by weight relative to the total weight of the composition.
La composition cosmétique topique ou pharmaceutique de contrôle de la lipolyse et de la différenciation adipocytaire est applicable par voie topique et se présente sous la forme d'huile ou de lotion ou de gel ou d'émulsion huile dans eau ou d'émulsion eau dans huile ou de crème. The topical or pharmaceutical cosmetic composition for controlling lipolysis and adipocyte differentiation is applicable topically and is in the form of an oil or lotion or an oil-in-water gel or emulsion or a water-in-oil emulsion. or cream.
La composition cosmétique orale, nutraceutique ou pharmaceutique de contrôle de la lipolyse et de la différenciation adipocytaire est ingérable sous forme de sirop, de gélule, de poudre, d'ampoule, de solution buvable, d'huile, d'émulsion huile dans eau ou eau dans huile, de pâte, de chocolat ou de biscuit. The oral, nutraceutical or pharmaceutical cosmetic composition for controlling lipolysis and adipocyte differentiation is ingestable in the form of syrup, capsule, powder, ampoule, oral solution, oil, oil-in-water emulsion or water in oil, dough, chocolate or biscuit.
La composition pharmaceutique de contrôle de la lipolyse et de la différenciation adipocytaire selon l'invention peut se présenter sous forme injectable. La forme injectable de contrôle se présente sous la forme de lotion ou de gel ou d'émulsion huile dans eau ou eau dans huile ou d'huile. The pharmaceutical composition for controlling lipolysis and adipocyte differentiation according to the invention may be in injectable form. The injectable form of control is in the form of lotion or gel or emulsion oil in water or water in oil or oil.
L'invention a encore pour objet un procédé de contrôle de la lipolyse et de la différenciation adipocytaire à des fins cosmétiques pour mincir chez un mammifère comprenant au moins une étape d'administration parentérale d'une quantité efficace d'un extrait de végétal lipophile choisi dans le groupe formé par la famille des Balanitaceae et par le genre Vitellaria. Des exemples de formulation ci-dessous permettent d'illustrer les compositions selon l'invention sans toutefois en limiter la portée. Des exemples illustrant
l'activité de stimulation de la production de Zinc-alpha2-glycoprotéine (ZAG) et d'inhibition de l'activité de la Glucose-6-Phosphate Déshydrogénase (G6PDH) des différentes compositions selon l'invention sont également décrits, ainsi que des exemples illustrant l'activité de stimulation de la lipolyse. Dans les compositions ci-après, les proportions des différents constituants sont exprimées en pourcentage en poids par rapport au poids total de la composition. The invention also relates to a method for controlling lipolysis and adipocyte differentiation for cosmetic purposes for thinning in a mammal comprising at least one step of parenteral administration of an effective amount of a selected lipophilic plant extract in the group formed by the family Balanitaceae and the genus Vitellaria. Examples of formulation below allow to illustrate the compositions according to the invention without however limiting the scope. Examples illustrating the activity of stimulating the production of Zinc-alpha2-glycoprotein (ZAG) and of inhibiting the activity of Glucose-6-Phosphate Dehydrogenase (G6PDH) of the various compositions according to the invention are also described, as well as examples illustrating the activity of stimulation of lipolysis. In the compositions below, the proportions of the various constituents are expressed as a percentage by weight relative to the total weight of the composition.
Exemple 1 : Example 1
Un exemple de composition cosmétique topique amincissante se présentant sous forme de crème et contenant un extrait lipohile de Balanites, en particulier de Balanites aegyptiaca va être décrit. An example of a cosmetic topical slimming composition in the form of a cream containing a lipohile extract of Balanites, in particular Balanites aegyptiaca, will be described.
L'extrait lipohile végétal utilisé est issu des graines oléagineuses de Balanites. Ces graines sont traitées, en particulier décoquées afin de séparer la coque de l'amande. L'amande est ensuite délipidée de préférence par pressage à froid ou à chaud des amandes, ou par extraction avec un solvant apolaire tel que, entre autres, l'hexane, ou par extraction au C02 supercritique afin de séparer la fraction lipidique des amandes. Cette fraction lipidique subit, soit selon un premier mode d'extraction, une extraction avec un solvant alcoolique polaire comme entre autres l'éthanol ou le méthanol contenant entre 0.01 % et 10% d'eau, et préférentiellement entre 3 et 6 % d'eau, soit, selon un second mode d'extraction, une extraction à l'eau en état supercritique. Selon le premier mode d'extraction, par décantation, le surnageant de cette extraction contient la fraction active de l'extrait lipohile selon l'invention et peut intégrer la composition à une concentration comprise, de préférence, dans la plage 0.001 % à 10%, selon le second mode d'extraction, l'extrait directement obtenu contient la fraction active de l'extrait lipohile selon l'invention et peut intégrer la composition à une concentration comprise, de préférence, dans la plage 0.001 % à 1 %. Selon l'un quelconque mode d'extraction, l'extrait obtenu peut ainsi être directement intégré dans la composition cosmétique topique ou, selon
le premier mode d'extraction, peut être séché par sublimation du solvant alcoolique polaire, notamment sous vide afin d'obtenir un extrait concentré dépourvu de solvant. Selon l'un quelconque mode d'extraction, l'extrait concentré, dépourvu de solvant, est un liquide plus ou moins épais ou visqueux qui peut figer à température ambiante, il est lipophile et s'incorpore dans la phase grasse ou huileuse de la composition. Cet extrait concentré est intégré dans la composition à une concentration comprise, de préférence, dans la plage 0.001 % à 1 %. The vegetable lipohil extract used is derived from the oilseed seeds of Balanites. These seeds are processed, in particular decocated to separate the shell from the kernel. The almond is then delipidated preferably by cold pressing or hot almonds, or by extraction with an apolar solvent such as, inter alia, hexane, or by supercritical CO2 extraction to separate the lipid fraction of almonds. This lipid fraction undergoes, either according to a first extraction method, an extraction with a polar alcoholic solvent such as, among others, ethanol or methanol containing between 0.01% and 10% of water, and preferably between 3 and 6% of water. water, or, according to a second mode of extraction, extraction with water in supercritical state. According to the first extraction method, by decantation, the supernatant of this extraction contains the active fraction of the lipohile extract according to the invention and can integrate the composition at a concentration preferably in the range 0.001% to 10% according to the second method of extraction, the directly obtained extract contains the active fraction of the lipohile extract according to the invention and can integrate the composition at a concentration preferably in the range 0.001% to 1%. According to any method of extraction, the extract obtained can thus be directly integrated into the topical cosmetic composition or, according to the first extraction mode can be dried by sublimation of the polar alcoholic solvent, in particular under vacuum to obtain a concentrated extract free of solvent. According to any method of extraction, the concentrated extract, devoid of solvent, is a more or less thick or viscous liquid which can set at room temperature, it is lipophilic and is incorporated in the oily or oily phase of the composition. This concentrated extract is incorporated into the composition at a concentration preferably in the range 0.001% to 1%.
La composition peut présenter une formulation telle que suit : The composition may have a formulation as follows:
Ingrédients % Ingredients%
Eau QSP QSP Water
Gomme de Xanthane 0,7 Xanthan Gum 0.7
Glyceryl Stéarate 4,3 Glyceryl Stearate 4.3
Alcool ceterarylique et glucoside 2 Ceteraryl alcohol and glucoside 2
cetearylique cetearylic
Huile de sésame 6 Sesame oil 6
Huile de tournesol 5 Sunflower oil 5
Dicaprylyl carbonate 3 Dicaprylyl carbonate 3
Huile de jojoba 1 Jojoba oil 1
Glycérine 1 Glycerin 1
Acide sorbique 0,35 Sorbic acid 0.35
Benzoate de sodium 0,5 Sodium benzoate 0.5
Vitamine E 0,2 Vitamin E 0.2
Parfum 0,5 Perfume 0.5
Extrait lipophile Balanites aegyptiaca 0,5 Lipophilic extract Balanites aegyptiaca 0.5
testé
Exemple 2 : tested Example 2
Un exemple de composition cosmétique « anti-poche » en contour des yeux se présentant sous forme de sérum et contenant un extrait lipohile de Vitellaria, en particulier de Vitellaria paradoxa va être décrit. L'extrait lipohile végétal utilisé est issu des graines oléagineuses de Vitellaria. Ces graines sont traitées, en particulier décoquées afin de séparer la coque de l'amande. L'amande est ensuite délipidée de préférence après broyage mécanique, par exemple, par pressage à froid ou à chaud des amandes, ou par extraction avec un solvant apolaire tel que, entre autres, l'hexane, ou par extraction au C02 supercritique afin d'isoler la fraction lipidique des amandes en tout ou partie. Cette fraction lipidique subit alors, soit une extraction avec un solvant alcoolique polaire, selon un premier mode d'extraction, comme entre autres l'éthanol ou le méthanol contenant entre 0.01% et 10% d'eau, et préférentiellement entre 3 et 6 % d'eau, soit une extraction à l'eau en état supercritique, selon un second mode d'extraction. Par décantation, le surnageant selon le premier mode d'extraction, ou le produit directement extrait selon le second mode d'extraction, contient la fraction active de l'extrait lipohile selon l'invention. Selon l'un quelconque mode d'extraction, l'extrait obtenu peut ainsi être directement intégré, avec ou sans solvant, à la composition cosmétique ou, selon le premier mode d'extraction, peut être séché par sublimation du solvant alcoolique polaire, notamment sous vide, afin d'obtenir un extrait concentré dépourvu de solvant. L'extrait concentré, dépourvu de solvant, selon le premier mode d'extraction ou l'extrait direct selon le second mode d'extraction, est un liquide plus ou moins épais ou visqueux qui peut figer à température ambiante, il est liposoluble et s'incorpore dans la phase grasse ou huileuse de la composition. Cet extrait concentré selon le premier mode d'extraction ou l'extrait direct selon le second mode d'extraction, est intégré dans la composition à une concentration, de préférence, comprise dans la plage 0.0001 % à 3%.
La composition peut présenter une formulation telle que suit : An example of an "anti-pocket" cosmetic composition in the contour of the eyes that is in the form of serum and containing a lipohile extract of Vitellaria, in particular Vitellaria paradoxa, will be described. The vegetable lipohile extract used is derived from the oil seeds of Vitellaria. These seeds are processed, in particular decocated to separate the shell from the kernel. The almond is then delipidated, preferably after mechanical grinding, for example by cold or hot pressing of the almonds, or by extraction with an apolar solvent such as, inter alia, hexane, or by extraction with supercritical CO 2 in order to isolate the lipid fraction of almonds in whole or in part. This lipid fraction is then subjected to either an extraction with a polar alcoholic solvent, according to a first extraction method, such as, among others, ethanol or methanol containing between 0.01% and 10% of water, and preferably between 3 and 6%. of water, ie extraction with water in supercritical state, according to a second mode of extraction. By decantation, the supernatant according to the first extraction method, or the product directly extracted according to the second extraction mode, contains the active fraction of the lipohile extract according to the invention. According to any method of extraction, the extract obtained can thus be directly integrated, with or without a solvent, into the cosmetic composition or, according to the first extraction method, can be dried by sublimation of the polar alcoholic solvent, in particular under vacuum, to obtain a concentrated extract devoid of solvent. The concentrated extract, devoid of solvent, according to the first extraction method or the direct extract according to the second extraction method, is a more or less thick or viscous liquid which can set at room temperature, it is fat soluble and incorporates in the oily or oily phase of the composition. This concentrated extract according to the first extraction method or the direct extract according to the second extraction mode, is incorporated in the composition at a concentration, preferably in the range 0.0001% to 3%. The composition may have a formulation as follows:
Exemple 3 : Un exemple de composition nutraceutique amincissante se présentant sous forme de poudre et contenant un extrait lipohile de Vitellaria, en particulier de Vitellaria paradoxa va être décrit. Selon l'invention, selon la réglementation européenne actuelle en vigueur, seul un extrait lipohile de Vitellaria paradoxa peut faire l'objet d'une composition nutraceutique. L'extrait lipohile végétal utilisé est issu des graines oléagineuses de Vitellaria. Ces graines sont traitées, en particulier décoquées afin de séparer la coque de l'amande. L'amande est ensuite délipidée de préférence après broyage
mécanique, par exemple, par pressage à froid ou à chaud des amandes, ou par extraction avec un solvant apolaire tel que, entre autres, l'hexane, ou par extraction au C02 supercritique afin d'isoler la fraction lipidique des amandes en tout ou partie. Cette fraction lipidique subit alors, soit une extraction avec un solvant alcoolique polaire, selon un premier mode d'extraction, comme entre autres l'éthanol ou le méthanol contenant entre 0.01% et 10% d'eau, et préférentiellement entre 3 et 6 % d'eau, soit une extraction à l'eau en état supercritique, selon un second mode d'extraction. Par décantation, le surnageant selon le premier mode d'extraction, ou le produit directement extrait selon le second mode d'extraction, contient la fraction active de l'extrait lipohile selon l'invention. Selon l'un quelconque mode d'extraction, l'extrait obtenu peut ainsi être directement intégré, avec ou sans solvant, à la composition cosmétique ou, selon le premier mode d'extraction, peut être séché par sublimation du solvant alcoolique polaire, notamment sous vide, afin d'obtenir un extrait concentré dépourvu de solvant. L'extrait concentré, dépourvu de solvant, selon le premier mode d'extraction ou l'extrait direct selon le second mode d'extraction, est un liquide plus ou moins épais ou visqueux qui peut figer à température ambiante, il est liposoluble et s'incorpore dans la phase grasse ou huileuse de la composition. Cet extrait concentré selon le premier mode d'extraction ou l'extrait direct selon le second mode d'extraction, est intégré dans la composition à une concentration, de préférence, comprise dans la plage 0.0001 % à 3%. EXAMPLE 3 An example of a slimming nutraceutical composition in the form of a powder containing a lipohile extract of Vitellaria, in particular Vitellaria paradoxa, will be described. According to the invention, according to current European regulations in force, only a lipohile extract of Vitellaria paradoxa can be the subject of a nutraceutical composition. The vegetable lipohile extract used is derived from the oil seeds of Vitellaria. These seeds are processed, in particular decocated to separate the shell from the kernel. The almond is then delipidated preferably after grinding mechanical, for example, by cold pressing or hot almonds, or by extraction with an apolar solvent such as, inter alia, hexane, or supercritical CO2 extraction to isolate the lipid fraction of almonds in all or part. This lipid fraction is then subjected to either an extraction with a polar alcoholic solvent, according to a first extraction method, such as, among others, ethanol or methanol containing between 0.01% and 10% of water, and preferably between 3 and 6%. of water, ie extraction with water in supercritical state, according to a second mode of extraction. By decantation, the supernatant according to the first extraction method, or the product directly extracted according to the second extraction mode, contains the active fraction of the lipohile extract according to the invention. According to any method of extraction, the extract obtained can thus be directly integrated, with or without a solvent, into the cosmetic composition or, according to the first extraction method, can be dried by sublimation of the polar alcoholic solvent, in particular under vacuum, to obtain a concentrated extract devoid of solvent. The concentrated extract, devoid of solvent, according to the first extraction method or the direct extract according to the second extraction method, is a more or less thick or viscous liquid which can set at room temperature, it is fat soluble and incorporates in the oily or oily phase of the composition. This concentrated extract according to the first extraction method or the direct extract according to the second extraction mode, is incorporated in the composition at a concentration, preferably in the range 0.0001% to 3%.
La composition peut présenter une formulation telle que suit : Pulpe d'acérola déshydratée 99% Extrait lipohile Vitellaria paradoxa testé 1 % The composition may have a formulation as follows: Dehydrated acerola pulp 99% Lipohile extract Vitellaria paradoxa tested 1%
Exemple 4 : Example 4
Un exemple de composition nutraceutique amincissante se présentant sous forme de chocolat noir et contenant un extrait lipohile de Vitellaria, en particulier
de Vitellaria paradoxa va être décrit. Selon l'invention, selon la réglementation européenne actuelle en vigueur, seul un extrait lipohile de Vitellaria paradoxa peut faire l'objet d'une composition nutraceutique. An example of a slimming nutraceutical composition in the form of dark chocolate and containing a lipohil extract of Vitellaria, in particular of Vitellaria paradoxa will be described. According to the invention, according to current European regulations in force, only a lipohile extract of Vitellaria paradoxa can be the subject of a nutraceutical composition.
L'extrait lipohile végétal utilisé est issu des graines oléagineuses de Vitellaria. Ces graines sont traitées, en particulier décoquées afin de séparer la coque de l'amande. L'amande est ensuite délipidée de préférence après broyage mécanique, par exemple, par pressage à froid ou à chaud des amandes, ou par extraction avec un solvant organique apolaire tel que, entre autres, l'hexane, ou par extraction au C02 supercritique afin d'isoler la fraction lipidique des amandes en tout ou partie. Cette fraction lipidique subit alors, soit une extraction avec un solvant alcoolique polaire, selon un premier mode d'extraction, comme entre autres l'éthanol ou le méthanol contenant entre 0.01 % et 10% d'eau, et préférentiellement entre 3 et 6 % d'eau, soit une extraction à l'eau en état supercritique, selon un second mode d'extraction. Par décantation, le surnageant selon le premier mode d'extraction, ou le produit directement extrait selon le second mode d'extraction, contient la fraction active de l'extrait lipohile selon l'invention. Selon l'un quelconque mode d'extraction, l'extrait obtenu peut ainsi être directement intégré, avec ou sans solvant, à la composition cosmétique ou, selon le premier mode d'extraction, peut être séché par sublimation du solvant alcoolique polaire, notamment sous vide, afin d'obtenir un extrait concentré dépourvu de solvant. L'extrait concentré, dépourvu de solvant, selon le premier mode d'extraction ou l'extrait direct selon le second mode d'extraction, est un liquide plus ou moins épais ou visqueux qui peut figer à température ambiante, il est liposoluble et s'incorpore dans la phase grasse ou huileuse de la composition. Cet extrait concentré selon le premier mode d'extraction ou l'extrait direct selon le second mode d'extraction, est intégré dans la composition à une concentration, de préférence, comprise dans la plage 0.0001 % à 100%. The vegetable lipohile extract used is derived from the oil seeds of Vitellaria. These seeds are processed, in particular decocated to separate the shell from the kernel. The almond is then delipidated, preferably after mechanical grinding, for example by cold or hot pressing of the almonds, or by extraction with an apolar organic solvent such as, inter alia, hexane, or by extraction with supercritical CO 2 so to isolate the lipid fraction of almonds in whole or in part. This lipid fraction is then subjected to either an extraction with a polar alcoholic solvent, according to a first extraction method, such as, among others, ethanol or methanol containing between 0.01% and 10% of water, and preferably between 3 and 6%. of water, ie extraction with water in supercritical state, according to a second mode of extraction. By decantation, the supernatant according to the first extraction method, or the product directly extracted according to the second extraction mode, contains the active fraction of the lipohile extract according to the invention. According to any method of extraction, the extract obtained can thus be directly integrated, with or without a solvent, into the cosmetic composition or, according to the first extraction method, can be dried by sublimation of the polar alcoholic solvent, in particular under vacuum, to obtain a concentrated extract devoid of solvent. The concentrated extract, devoid of solvent, according to the first extraction method or the direct extract according to the second extraction method, is a more or less thick or viscous liquid which can set at room temperature, it is fat soluble and incorporates in the oily or oily phase of the composition. This concentrated extract according to the first extraction mode or the direct extract according to the second extraction mode is incorporated in the composition at a concentration, preferably in the range 0.0001% to 100%.
La composition peut présenter une formulation telle que suit :
Poudre de Cacao The composition may have a formulation as follows: Cocoa powder
Beurre de Cacao Cocoa butter
Extrait feuilles Stevia rebaudiana Leaf extract Stevia rebaudiana
Extrait lipohile Vitellaria paradoxa testé Comme l'illustrent les résultats d'activité ci-après, les compositions contenant des extraits de Balanites aegyptiaca (Balanitaceae) et Vitellaria paradoxa (Sapotaceae) sont des compositions qui induisent le destockage des graisses chez les mammifères. Ce destockage s'explique par stimulation de la lipolyse par le fait de l'augmentation de production de Zinc-alpha 2-glycoprotéine (ZAG), un L F ou facteur de mobilisation des lipides qui en se liant sur les récepteurs β3 adrenergiques des adipocytes modifie une protéine G de sorte à activer l'Adénylate Cyclase. L'Adénylate Cyclase transforme alors ΑΤΡ en AMPc qui active une protéine kinase. Cette protéine kinase active une lipase qui dégrade le triacylglycerol stocké en acides gras. La ZAG active ainsi la cascade enzymatique qui conduit à la lipolyse. La ZAG stimule donc la lipolyse de manière directe en surexprimant l'AMPc. Ce destockage des graisses s'explique également par inhibition de la différenciation des pré-adipocytes par inhibition de la Glucose 6 phosphodihydrogénase (G6PDH). Lipohil extract Vitellaria paradoxa tested As illustrated by the results of activity below, the compositions containing extracts of Balanites aegyptiaca (Balanitaceae) and Vitellaria paradoxa (Sapotaceae) are compositions that induce destocking of fats in mammals. This destocking is explained by stimulation of lipolysis due to the increased production of Zinc-alpha 2-glycoprotein (ZAG), an LF or lipid mobilization factor which binds to the adrenergic β3 adrenergic receptors. a G protein so as to activate Adenylate Cyclase. Adenylate Cyclase then transforms ΑΤΡ into cAMP that activates a protein kinase. This protein kinase activates a lipase that degrades the triacylglycerol stored in fatty acids. ZAG thus activates the enzymatic cascade which leads to lipolysis. ZAG therefore stimulates lipolysis directly by overexpressing cAMP. This destocking of fats is also explained by inhibition of differentiation of pre-adipocytes by inhibition of Glucose 6 phosphodihydrogenase (G6PDH).
Les utilisations de ces compositions sont diverses et variées. The uses of these compositions are diverse and varied.
Selon un premier mode d'application, en applications topiques, les extraits selon l'invention peuvent être utilisés dans les produits amincissants, lipolytiques, anti-cellulites, raffermissants, toniques, anti-poches sous les yeux, et plus généralement dans les produits destinés à améliorer et affiner la silhouette, le visage et le buste. Ces compositions peuvent être sous forme de capsules collées sur des fibres textiles de vêtements amincissants ou de textiles imprégnés de capsules en contact avec la peau ou de polymères imprégnés de capsules en contact avec la peau, de capsules intégrées dans des produits de massage, d'huiles de massage, d'émulsion huile dans eau, d'émulsion eau dans huile, de sérum, de lotion, de gel, de savon, dans les
produits dermocosmétiques, dans les produits de maquillage, comme co-actifs dans les produits raffermissants, tenseurs et anti-âges. According to a first mode of application, in topical applications, the extracts according to the invention can be used in slimming, lipolytic, anti-cellulite, firming, toning, anti-puffiness products under the eyes, and more generally in products intended for to improve and refine the silhouette, the face and the bust. These compositions may be in the form of capsules glued to textile fibers of slimming garments or of textile impregnated with capsules in contact with the skin or of polymers impregnated with capsules in contact with the skin, of capsules incorporated in massage products, of massage oils, oil-in-water emulsion, water-in-oil emulsion, serum, lotion, gel, soap, in dermocosmetic products, in makeup products, as co-active in firming, tensor and anti-aging products.
Pour être efficaces, et compte-tenu de la rémanence de leur activité, les produits cosmétiques non rincés comprenant ces actifs sont à utiliser préférentiellement au minimum deux fois par semaine en cure de trois mois. Les compositions cosmétiques rincées comprenant ces actifs sont à utiliser préférentiellement au minimum deux fois par jour, en cure de trois mois. To be effective, and taking into account the persistence of their activity, non-rinsed cosmetic products comprising these active ingredients are to be used preferably at least twice a week in a three-month course. The rinsed cosmetic compositions comprising these active ingredients are to be used preferably at least twice a day, in course of three months.
Les produits cosmétiques comprenant ces actifs peuvent être utilisés chaque jour. Cosmetics including these assets can be used every day.
Selon un second mode d'application, Per os, dans le domaine nutraceutique, seul l'extrait lipophile de Vitellaria paradoxa peut être utilisé de manière « alimentaire » compte tenu de la réglementation européenne actuelle, et donc incorporer des compositions amincissantes selon l'invention. Selon le second mode d'application, l'extrait lipohile de Vitellaria paradoxa selon l'invention peut incorporer des compositions amincissantes, ou contre l'adiposité, nutraceutiques et pharmaceutiques. Ces compositions peuvent être sous forme de poudres, de gels, de lotions, de pâtes, de gommes, de chocolats, de gélules, de capsules, d'émulsions huile dans eau, d'émulsion eau dans huile, d'huiles ou d'ampoules. According to a second embodiment, Per os, in the nutraceutical field, only the lipophilic extract of Vitellaria paradoxa can be used in a "food" manner in view of current European regulations, and therefore incorporate slimming compositions according to the invention. . According to the second mode of application, the lipohile extract of Vitellaria paradoxa according to the invention may incorporate slimming compositions, or against adiposity, nutraceuticals and pharmaceuticals. These compositions may be in the form of powders, gels, lotions, pastes, gums, chocolates, capsules, capsules, oil-in-water emulsions, water-in-oil emulsions, oils or bulbs.
Selon un troisième mode d'application, par injection, dans le domaine pharmaceutique, les extraits selon l'invention peuvent incorporer des compositions injectables. Ces compositions peuvent être sous formes de poudres à diluer extemporanément, de gel, de lotion, de sérum, d'émulsion huile dans eau ou eau dans huile. According to a third mode of application, by injection, in the pharmaceutical field, the extracts according to the invention can incorporate injectable compositions. These compositions may be in the form of extemporaneously dilutable powders, gel, lotion, serum, oil-in-water or water-in-oil emulsion.
Les extraits retenus pour la démonstration sont des extraits issus d'une extraction hydroalcoolique de la fraction lipidique des graines des végétaux, puis concentrés par évaporation sous vide de l'éthanol et de l'eau au moyen d'un système « rotavapor ». The extracts selected for the demonstration are extracts from a hydroalcoholic extraction of the lipid fraction of the seeds of the plants, then concentrated by vacuum evaporation of ethanol and water using a "rotavapor" system.
Ainsi, l'extrait lipohile de la fraction lipidique des graines de Balanites aeqyptiaca présente une composition telle que suit :
Fraction lipidique de la graine 50% Ethanoi 96° 50% Thus, the lipohile extract of the lipid fraction of Balanites aeqyptiaca seeds has a composition as follows: Lipid fraction of the seed 50% Ethanoi 96 ° 50%
La composition étant exprimée en pourcentage en poids par rapport au poids total de ladite composition. The composition being expressed as a percentage by weight relative to the total weight of said composition.
Cet extrait est maintenu sous agitation à l'obscurité pendant 4 heures à température ambiante. Cet extrait est mis à décanter à l'obscurité à température ambiante pendant 24 heures. Le surnageant est récupéré. This extract is kept stirring in the dark for 4 hours at room temperature. This extract is allowed to settle in the dark at room temperature for 24 hours. The supernatant is recovered.
Le surnageant est alors concentré par évaporation de l'éthanol 96° dans un système « rotavapor » à 40°c, sous vide. L'extrait concentré résultant est appelé dans ce qui suit « EXTRAIT LIPOHILE BALANITES AEGYPTIACA TESTE ». The supernatant is then concentrated by evaporation of the 96 ° ethanol in a "rotavapor" system at 40 ° C. under vacuum. The resulting concentrated extract is referred to in the following as "LIPOHILE EXTRACT BALANITES AEGYPTIACA TEST".
L'extrait lipohile de la fraction lipidique des graines de Vitellaria paradoxa présente une composition telle que suit : The lipohile extract of the lipid fraction of the seeds of Vitellaria paradoxa has a composition as follows:
Fraction lipidique de la graine 50% Lipid fraction of the seed 50%
Ethanoi 96° 50% Ethanoi 96 ° 50%
La composition étant exprimée en pourcentage en poids par rapport au poids total de ladite composition. The composition being expressed as a percentage by weight relative to the total weight of said composition.
Cet extrait est maintenu sous agitation à l'obscurité pendant 4 heures à température ambiante. Cet extrait est mis à décanter à l'obscurité à température ambiante pendant 24 heures. Le surnageant est récupéré. This extract is kept stirring in the dark for 4 hours at room temperature. This extract is allowed to settle in the dark at room temperature for 24 hours. The supernatant is recovered.
Le surnageant est alors concentré par évaporation de l'éthanol 96° dans un système « rotavapor » à 40°c, sous vide. L'extrait concentré résultant est appelé dans ce qui suit « EXTRAIT LIPOHILE VITELLARIA PARADOXA TESTE ». The supernatant is then concentrated by evaporation of the 96 ° ethanol in a "rotavapor" system at 40 ° C. under vacuum. The resulting concentrated extract is referred to in the following as "EXTRACT LIPOHILE VITELLARIA PARADOXA TEST".
Les résultats ci-après illustrent l'effet dose des actifs « EXTRAIT LIPOHILE BALANITES AEGYPTIACA TESTE » et « EXTRAIT LIPOHILE VITELLARIA PARADOXA TESTE » pour leur capacité à moduler la production de ZAG dans un modèle de kératinocytes épidermiques humains normaux adultes. Des monocouches de kératinocytes humains normaux ont été obtenues en cultivant des cellules issues d'une plastie abdominale réalisée chez une femme de 45 ans. Les kératinocytes ont été incubés pendant 48 heures à
37°C, sous atmosphère humide et à 5% de CO2, en absence (Témoin) ou en présence de dexaméthasone à 10μ ( produit de référence ) ou en présence de concentrations croissantes des actifs à l'essai. Ces concentrations (V/V) sont exprimées en volume de l'actif par rapport au volume total du milieu d'incubation dans lequel l'actif est stabilisé. The following results illustrate the dose effect of the active ingredients "EXTRACT LIPOHILE BALANITES AEGYPTIACA TEST" and "EXTRACT LIPOHILE VITELLARIA PARADOXA TEST" for their ability to modulate the production of ZAG in a model of normal adult human epidermal keratinocytes. Monolayers of normal human keratinocytes were obtained by culturing cells from an abdominoplasty performed in a 45-year-old woman. The keratinocytes were incubated for 48 hours at 37 ° C, under humid atmosphere and at 5% CO2, in absence (control) or in the presence of dexamethasone at 10 μ (reference product) or in the presence of increasing concentrations of test assets. These concentrations (V / V) are expressed in volume of the active relative to the total volume of the incubation medium in which the asset is stabilized.
« EXTRAIT LIPOHILE BALANITES AEGYPTIACA TESTE » = SNHBCO2 : SNHBCO2 → 0.001 ; 0.005 ; 0.01 % (VA/) "LIPOHILE EXTRACT BALANITES AEGYPTIACA TEST" = SNHBCO2: SNHBCO2 → 0.001; 0.005; 0.01% (VA /)
« EXTRAIT LIPOHILE VITELLARIA PARADOXA TESTE » = SNBKSTBF : SNBKSTBF → 0.001 ; 0.005 ; 0.01 % (V/V) "LIPOHILE EXTRACT VITELLARIA PARADOXA TEST" = SNBKSTBF: SNBKSTBF → 0.001; 0.005; 0.01% (V / V)
L'« EXTRAIT LIPOHILE BALANITES AEGYPTIACA TESTE » = SNHBCO2 est d'abord dilué à 50% dans du DMSO (VA/), pour être ainsi dilué dans le milieu de culture. L'« EXTRAIT LIPOHILE VITELLARIA PARADOXA TESTE » = SNBKSTBF est d'abord dilué à 10% du DMSO (P/V), pour être ainsi dilué dans le milieu de culture. The "LIPOIL EXTRACT BALANITES AEGYPTIACA TEST" = SNHBCO2 is first diluted to 50% in DMSO (VA /), to be diluted in the culture medium. The "LIPOHIL EXTRACT VITELLARIA PARADOXA TEST" = SNBKSTBF is first diluted to 10% DMSO (P / V), to be diluted in the culture medium.
A la fin de la période d'incubation, la ZAG est quantifiée dans les milieux de culture à l'aide d'un kit ELISA sensible et spécifique, et les protéines contenues dans les lysats cellulaires sont quantifiées par une méthode spectrocolorimétrique faisant appel au bleu de Coomassie (Bradford M. 1976 Anal. Biochem., 72, 248-254). Les résultats sont donnés sous la forme d'un rapport « ng de ZAG / mg de protéines totales du tapis cellulaire » (moyennes +/- la déviation standard, S.D.). La significativité statistique des différences observées entre les conditions « contrôle » et « produit de référence » ou « DMSO » est évaluée par un test de Student (Student t-test ; p < 0.05). La significativité statistique des différences observées entre les conditions « contrôle » et « produit à l'essai », est évaluée produit par produit, par une analyse de la variance à un facteur (One Way ANOVA), suivie, lorsque cela est nécessaire, d'un test de Holm-Sidak ou de Dunn's (p < 0.05). Les résultats présentés dans la figures 1 concernent les actifs « EXTRAIT LIPOHILE BALANITES AEGYPTIACA TESTE » et « EXTRAIT LIPOHILE VITELLARIA
PARADOXA TESTE » et montrent que dans les conditions expérimentales retenues après 48 heures d'incubation, les actifs « EXTRAIT LIPOHILE BALANITES AEGYPTIACA TESTE » et « EXTRAIT LIPOHILE VITELLARIA PARADOXA TESTE » induisent une augmentation significative de la production kératinocytaire de ZAG. Ces résultats sont validés par le fait que la dexaméthasone à 10μ , utilisée comme produit de référence, augmentait significativement, de manière attendue, la production kératinocytaire de ZAG. At the end of the incubation period, the ZAG is quantified in the culture media using a sensitive and specific ELISA kit, and the proteins contained in the cell lysates are quantified by a spectrocolorimetric method using blue Coomassie (Bradford M., 1976 Anal Biochem., 72, 248-254). The results are given in the form of a ratio "ng of ZAG / mg of total proteins of the cell layer" (averages +/- standard deviation, SD). The statistical significance of the differences observed between the conditions "control" and "reference product" or "DMSO" is evaluated by a Student's test (Student t-test, p <0.05). The statistical significance of the observed differences between the conditions "control" and "product under test" is evaluated product by product, by a one-way analysis of variance (One Way ANOVA), followed, where necessary, by a Holm-Sidak or Dunn's test (p <0.05). The results presented in FIG. 1 relate to the active ingredients "EXTRACT LIPOHILE BALANITES AEGYPTIACA TESTE" and "EXTRACT LIPOHILE VITELLARIA". PARADOXA TEST "and show that under the experimental conditions retained after 48 hours of incubation, the active ingredients" EXTRACT LIPOHILE BALANITES AEGYPTIACA TEST "and" EXTRACT LIPOHILE VITELLARIA PARADOXA TEST "induce a significant increase in the keratinocyte production of ZAG. These results are validated by the fact that dexamethasone at 10 μ, used as reference product, significantly increased, as expected, the keratinocyte production of ZAG.
- "SNHBCO2" à 0,005 % → + 42,3 % (p<0,05) - "SNHBCO2" at 0.005% → + 42.3% (p <0.05)
- "SNHBCO2" à 0,01 % → + 30,1 % (p<0,05) - "SNBKSTBF" à 0,005 % → + 14,5 % (p<0,05) - "SNHBCO2" at 0.01% → + 30.1% (p <0.05) - "SNBKSTBF" at 0.005% → + 14.5% (p <0.05)
- "SNBKSTBF" à 0,01 % → + 55,7 % (p<0,05) - "SNBKSTBF" at 0.01% → + 55.7% (p <0.05)
- "Dexaméthasone" à 10 μΜ → + 27 % (p<0,05) - "Dexamethasone" at 10 μΜ → + 27% (p <0.05)
Les résultats ci-après illustrent l'effet dose des actifs « EXTRAIT LIPOHILE BALANITES AEGYPTIACA TESTE » et « EXTRAIT LIPOHILE VITELLARIA PARADOXA TESTE » pour leur capacité à moduler l'activité de la G6PDH dans un modèle IN VITRO acellulaire. La Glucose-6-Phosphate Deshydrogénase utilisée provient de la société SIGMA-ALDRICH. La G6PDH est incubée avec une solution de glucose, d'ATP, de NAD et d'hexokinase, en présence ou non des actifs à l'essai : The results below illustrate the dose effect of the active ingredients "EXTRACT LIPOHILE BALANITES AEGYPTIACA TEST" and "EXTRACT LIPOHILE VITELLARIA PARADOXA TEST" for their ability to modulate the activity of G6PDH in an acellular IN VITRO model. The Glucose-6-phosphate dehydrogenase used is from SIGMA-ALDRICH. G6PDH is incubated with a solution of glucose, ATP, NAD and hexokinase, with or without the active ingredients tested:
Hexokinase hexokinase
Glucose + ATP ► Glucose-6-Phosphate + ADP Glucose + ATP ► Glucose-6-Phosphate + ADP
G6PDH G6PDH
G6PD + NAD ► 6-PHOSPHOGLUCONATE + NADH G6PD + NAD ► 6-PHOSPHOGLUCONATE + NADH
La variation de l'absorbance à 340 nm est directement proportionnelle à l'activité de la G6PDH. La solution de G6PDH est incubée pendant 5 minutes à
température ambiante en présence des substrats, et en absence (tampon seul) ou en présence d'EDTA (produit de référence) ou de concentrations croissantes des actifs. The change in absorbance at 340 nm is directly proportional to the activity of G6PDH. The G6PDH solution is incubated for 5 minutes at ambient temperature in the presence of substrates, and in the absence (buffer alone) or in the presence of EDTA (reference product) or increasing concentrations of active ingredients.
« EXTRAIT LIPOHILE BALANITES AEGYPTIACA TESTE » = SNHBC02 : SNHBC02 → 0.001 ; 0.005 ; 0.01 ; 0.05 ; 0.1 ; 0.5 et 1 % (VA/)"LIPOHILE EXTRACT BALANITES AEGYPTIACA TEST" = SNHBC02: SNHBC02 → 0.001; 0.005; 0.01; 0.05; 0.1; 0.5 and 1% (VA /)
Ces concentrations (VA/) sont exprimées en volume de l'actif par rapport au volume total du milieu d'incubation dans lequel l'actif est stabilisé. These concentrations (VA /) are expressed as the volume of the active relative to the total volume of the incubation medium in which the asset is stabilized.
« EXTRAIT LIPOHILE VITELLARIA PARADOXA TESTE » = SNBKSTBF : SNBKSTBF → 0.001 ; 0.005 ; 0.01 ; 0.05 ; 0.1 ; 0.5 et 1 % (P/V)"LIPOHILE EXTRACT VITELLARIA PARADOXA TEST" = SNBKSTBF: SNBKSTBF → 0.001; 0.005; 0.01; 0.05; 0.1; 0.5 and 1% (W / V)
Ces concentrations (PAZ) sont exprimées en poids de l'actif par rapport au volume total du milieu d'incubation dans lequel l'actif est stabilisé. These concentrations (PAZ) are expressed by weight of the active ingredient relative to the total volume of the incubation medium in which the active agent is stabilized.
Un « blanc produit » est réalisé en absence de G6PDH, pour chacune des concentrations des produits testés afin de tenir compte d'une éventuelle absorbance à 340 nm des actifs à l'essai. A "white product" is produced in the absence of G6PDH, for each of the concentrations of the products tested to take into account a possible absorbance at 340 nm of the test assets.
L'« EXTRAIT LIPOHILE BALANITES AEGYPTIACA TESTE » = SNHBCO2 est d'abord dilué à 50% dans du DMSO (VA/), pour être ainsi dilué dans le milieu de culture. L'« EXTRAIT LIPOHILE VITELLARIA PARADOXA TESTE » = SNBKSTBF est d'abord dilué à 10% du DMSO (P V), pour être ainsi dilué dans le milieu de culture. The "LIPOIL EXTRACT BALANITES AEGYPTIACA TEST" = SNHBCO2 is first diluted to 50% in DMSO (VA /), to be diluted in the culture medium. The "LIPOHIL EXTRACT VITELLARIA PARADOXA TEST" = SNBKSTBF is first diluted to 10% of DMSO (P V), to be diluted in the culture medium.
L'amplitude de la réaction enzymatique est évaluée après 5 minutes d'incubation en présence de substrat et des produits à l'essai, par spectrocolorimétrie en faisant lecture de l'absorbance des milieux réactionnels à 340 nm. Pour chaque concentration testée, l'effet du produit à l'essai sur l'activité de la G6PDH est calculé selon la formule suivante : Q , [ DO;*; en présence de ."inhibiteur χ 100 The amplitude of the enzymatic reaction is evaluated after 5 minutes of incubation in the presence of substrate and of the products under test, by spectrocolorimetry by reading the absorbance of the reaction mediums at 340 nm. For each concentration tested, the effect of the test product on the activity of G6PDH is calculated using the following formula: Q, [OD; *; in the presence of. " inhibitor χ 100
I DOse sa absence de 1 mlnbitew I DOs his absence of 1 mlnbitew
Les résultats sont donnés sous la forme de pourcentage d'activité de la G6PDH par rapport au témoin (moyennes +/- la déviation standard, S.D.). La significativité statistique des différences observées entre les conditions
« contrôle » et « produit de référence » ou « DMSO 1 %» est évaluée par un test de Student (Student t-test ; p < 0.001 ) et par une analyse de la variance à un facteur (One Way ANOVA), suivie d'un test de Holm-Sidak (p : < 0.05). La significativité statistique des différences observées entre les conditions « contrôle » et « produit à l'essai », est évaluée produit par produit, par une analyse de la variance à un facteur (One Way ANOVA), suivie, lorsque cela est nécessaire, d'un test de Holm-Sidak (p < 0.05). The results are given as a percentage of G6PDH activity relative to the control (averages +/- standard deviation, SD). The statistical significance of the differences observed between the conditions "Control" and "reference product" or "DMSO 1%" is evaluated by a Student t-test (p <0.001) and a one-way analysis of variance (One Way ANOVA), followed by a Holm-Sidak test (p: <0.05). The statistical significance of the observed differences between the conditions "control" and "product under test" is evaluated product by product, by a one-way analysis of variance (One Way ANOVA), followed, where necessary, by a Holm-Sidak test (p <0.05).
Les résultats présentés dans la figure 2 concernent les actifs « EXTRAIT LIPOHILE BALANITES AEGYPTIACA TESTE » et « EXTRAIT LIPOHILE VITELLARIA PARADOXA TESTE » et montrent que dans les conditions expérimentales retenues après 5 minutes d'incubation, les actifs « EXTRAIT LIPOHILE BALANITES AEGYPTIACA TESTE » et « EXTRAIT LIPOHILE VITELLARIA PARADOXA TESTE » inhibent significativement l'activité de la G6PDH. Ces résultats sont validés par le fait que l'EDTA à 5 mM, utilisé comme produit de référence, inhibait significativement, de manière attendue, la réaction enzymatique après 5 minutes d'incubation. The results presented in FIG. 2 relate to the active ingredients "EXTRACT LIPOHILE BALANITES AEGYPTIACA TEST" and "EXTRACT LIPOHILE VITELLARIA PARADOXA TEST" and show that under the experimental conditions selected after 5 minutes of incubation, the active ingredients "EXTRACT LIPOHILE BALANITES AEGYPTIACA TESTE" and "LIPOHILE EXTRACT VITELLARIA PARADOXA TESTE" significantly inhibit the activity of G6PDH. These results are validated by the fact that the 5 mM EDTA, used as a reference product, significantly inhibited the enzyme reaction in an expected manner after 5 minutes of incubation.
- "SNHBCO2" à 0,005 % → - 39 % (p<0,05) - "SNHBCO2" at 0.005% → - 39% (p <0.05)
- "SNHBCO2" à 0,01 % → - 47,8 % (p<0,05) - "SNBKSTBF" à 0,01 % → - 35,5 % (p<0,05) - "SNHBCO2" at 0.01% → - 47.8% (p <0.05) - "SNBKSTBF" at 0.01% → - 35.5% (p <0.05)
- "SNBKSTBF" à 0,05 % → - 74,3 % (p<0,05) - "SNBKSTBF" at 0.05% → - 74.3% (p <0.05)
- "EDTA" à 5 μΜ → - 83 % (p<0,05) - "EDTA" at 5 μΜ → - 83% (p <0.05)
Les résultats ci-après illustrent l'effet dose des actifs « EXTRAIT LIPOHILE BALANITES AEGYPTIACA TESTE » et « EXTRAIT LIPOHILE VITELLARIA PARADOXA TESTE » pour leur capacité à moduler l'activité lipolytique dans un modèle d'adipocytes humains normaux adultes en suspension. Des adipocytes humains ont été dissociés à partir d'une plastie abdominale réalisée chez une femme de 62 ans, puis incubés en présence ou non des actifs à l'essai. Les
adipocytes ont été incubés 2 heures à 37°C, sous agitation, en absence (milieu incubation seul) ou en présence des produits de référence, ou de concentrations croissantes des produits à l'essai Les kératinocytes ont été incubés pendant 48 heures à 37°C, sous atmosphère humide et à 5% de CO2, en absence (Témoin) ou en présence de dexaméthasone à 10μΜ ( produit de référence ) ou en présence de concentrations croissantes des actifs à l'essai. The following results illustrate the dose effect of the active ingredients "EXTRACT LIPOHILE BALANITES AEGYPTIACA TEST" and "EXTRACT LIPOHILE VITELLARIA PARADOXA TEST" for their ability to modulate lipolytic activity in a model of normal adult human adipocytes in suspension. Human adipocytes were dissociated from a tummy tuck performed in a 62-year-old woman, and then incubated with or without test assets. The Adipocytes were incubated for 2 hours at 37 ° C., with shaking, in the absence (medium incubation alone) or in the presence of the reference products, or with increasing concentrations of the products under test. The keratinocytes were incubated for 48 hours at 37 ° C. C, in a humid atmosphere and at 5% CO2, in absence (control) or in the presence of dexamethasone at 10 μΜ (reference product) or in the presence of increasing concentrations of the test substances.
« EXTRAIT LIPOHILE BALANITES AEGYPTIACA TESTE » = SNHBCO2 : "LIPOHILE EXTRACT BALANITES AEGYPTIACA TEST" = SNHBCO2:
SNHBCO2 → 0.001 ; 0.01 ; 0.1 % (P/V) SNHBCO2 → 0.001; 0.01; 0.1% (W / V)
Ces concentrations (PA ) sont exprimées en poids de l'actif par rapport au volume total du milieu d'incubation dans lequel l'actif est stabilisé. These concentrations (PA) are expressed as the weight of the active ingredient relative to the total volume of the incubation medium in which the active agent is stabilized.
« EXTRAIT LIPOHILE VITELLARIA PARADOXA TESTE » = SNBKSTBF : SNBKSTBF → 0.001 ; 0.01 ; 0.1 % (P/V) "LIPOHILE EXTRACT VITELLARIA PARADOXA TEST" = SNBKSTBF: SNBKSTBF → 0.001; 0.01; 0.1% (W / V)
Ces concentrations (PA ) sont exprimées en poids de l'actif par rapport au volume total du milieu d'incubation dans lequel l'actif est stabilisé. These concentrations (PA) are expressed as the weight of the active ingredient relative to the total volume of the incubation medium in which the active agent is stabilized.
SNHBCO2 est préparé à partir d'une solution mère à 50% dans du DMSO (VA/), pour être alors dilué directement dans le milieu de culture, avec une concentration maximale de DMSO de 0.01 % (VA/). SNBKSTBF est préparé à partir d'une solution mère à 10% dans du DMSO (PA/), pour être alors dilué directement dans le milieu de culture, avec une concentration maximale de DMSO de 1 % (VA/). SNHBCO2 is prepared from a 50% stock solution in DMSO (VA /), then diluted directly in the culture medium, with a maximum concentration of DMSO of 0.01% (VA /). SNBKSTBF is prepared from a 10% stock solution in DMSO (PA /), and then diluted directly in the culture medium with a maximum concentration of DMSO of 1% (VA /).
Les activateurs de références utilisés vis-à-vis de l'activité lipolytique sur adipocytes sont la caféine et la théophylline à 10"4M. The reference activators used with respect to lipolytic activity on adipocytes are caffeine and theophylline at 10 -4 M.
A la fin de la période d'incubation, les acides gras non estérifiés (AGNE) sont quantifiés dans les milieux d'incubation à l'aide d'une technique spectrophotométrique sensible et spécifique. At the end of the incubation period, the non-esterified fatty acids (EAFA) are quantified in the incubation media using a sensitive and specific spectrophotometric technique.
Les résultats sont donnés sous la forme de concentrations (en μΜ) d'AGNE présents dans les milieux d'incubation des adipocytes (moyennes +/- la dérivation standard, S.D.). La significativité statistique des différences observées entre les conditions « contrôle » et « produit de référence » est évaluée par un test de Student (Student t-test, p< 0.001 ). La significativité
statistique des différences observées entre les conditions « Témoin » et « Produits à l'essai », est évaluée produit par produit, par une analyse de la variance à un facteur (One Way ANOVA), suivie, lorsque cela est nécessire d'un test de Holm-Sidak (p< 0.05). The results are given in the form of concentrations (in μΜ) of AGNE present in the incubation medium of the adipocytes (average +/- standard derivation, SD). The statistical significance of the differences observed between the conditions "control" and "reference product" is evaluated by a Student's test (Student t-test, p <0.001). Significance statistic of the differences observed between the conditions "Witness" and "Products under test", is evaluated product by product, by a one-way analysis of variance (One Way ANOVA), followed, when this requires a test from Holm-Sidak (p <0.05).
Les résultats présentés dans la figure 3 concernent les actifs « EXTRAIT LIPOHILE BALA ITES AEGYPTIACA TESTE » et « EXTRAIT LIPOHILE VITELLARIA PARADOXA TESTE » et montrent que dans les conditions expérimentales retenues après 2 heures d'incubation à 37°C, les actifs « EXTRAIT LIPOHILE BALANITES AEGYPTIACA TESTE » et « EXTRAIT LIPOHILE VITELLARIA PARADOXA TESTE » augmentent significativement la lipolyse. Ces résultats sont validés par le fait que la caféine et la Théophylline, utilisées comme produits de référence, augmentaient significativement, de manière attendue, la libération d'AGNE dans les milieux d'incubation des adipocytes en suspension. The results presented in FIG. 3 relate to the active ingredients "EXTRACT LIPOHIL BALA ITES AEGYPTIACA TEST" and "EXTRACT LIPOHILE VITELLARIA PARADOXA TEST" and show that under the experimental conditions retained after 2 hours of incubation at 37 ° C., the active ingredients "EXTRACT LIPOHILE BALANITES AEGYPTIACA TEST "and" EXTRACT LIPOHIL VITELLARIA PARADOXA TEST "significantly increase lipolysis. These results are validated by the fact that caffeine and theophylline, used as reference products, significantly increased, as expected, the release of AGNE in the incubation medium of the adipocytes in suspension.
- "SNHBCO2" à 0,01 % → + 34 % (p<0,05) - "SNHBCO2" at 0.01% → + 34% (p <0.05)
- "SNHBCO2" à 0,1 % → + 64 % (p<0,05) - "SNHBCO2" at 0.1% → + 64% (p <0.05)
- "SNBKSTBF" à 0,001 % → + 60 % (p<0,05) - "SNBKSTBF" at 0.001% → + 60% (p <0.05)
- "SNBKSTBF" à 0,01 % → + 70 % (p<0,05) - "Caféine" à 10"4M → + 67 % (p<0,001 ) - "SNBKSTBF" at 0.01% → + 70% (p <0.05) - "Caffeine" at 10 "4 M → + 67% (p <0.001)
- "Théophylline" à 1(T* → + 125 % (p<0,001 )
- "Theophylline" at 1 (T * → + 125% (p <0.001)
Claims
1 . Extrait de végétal choisi dans le groupe formé par la famille des Balanitaceae et par le genre Vitellaria de la famille des Sapotaceae pour son utilisation à la fois comme agent de stimulation de la lipolyse et comme inhibiteur de la différenciation adipocytaire pour la fabrication de composition à action amincissante. 1. Plant extract selected from the group consisting of the family Balanitaceae and the genus Vitellaria from the family Sapotaceae for its use both as a lipolysis stimulating agent and as an inhibitor of adipocyte differentiation for the manufacture of action composition slimming.
2. Composition amincissante, caractérisée en ce qu'elle contient à la fois comme agent actif sur la lipolyse et comme inhibiteur de la différenciation adipocytaire au moins un extrait de végétal choisi dans le groupe formé par la famille des Balanitaceae et par le genre Vitellaria de la famille des Sapotaceae. 2. Slimming composition, characterized in that it contains both as active agent on lipolysis and as an inhibitor of adipocyte differentiation at least one plant extract selected from the group consisting of the family Balanitaceae and the genus Vitellaria of the Sapotaceae family.
3. Composition amincissante selon la revendication 2, caractérisée en ce que, ladite composition est une composition pharmaceutique qui contient au moins un extrait de végétal choisi dans le groupe formé par la famille des Balanitaceae et par le genre Vitellaria de la famille des Sapotaceae comme agent actif sur la lipolyse et comme inhibiteur de la différenciation adipocytaire, en quantité efficace pour traiter ou prévenir les disgrâces de l'adiposité tels que la « peau d'orange » ou l'embonpoint de la silhouette. 3. slimming composition according to claim 2, characterized in that, said composition is a pharmaceutical composition which contains at least one plant extract selected from the group consisting of the family Balanitaceae and the genus Vitellaria family Sapotaceae as agent active on lipolysis and as an inhibitor of adipocyte differentiation, in an amount effective to treat or prevent disgrace of adiposity such as "orange peel" or being overweight.
4. Composition amincissante selon la revendication 2, caractérisée en ce que, ladite composition contient au moins un extrait de végétal choisi dans le groupe formé par la famille des Balanitaceae et par le genre Vitellaria de la famille des Sapotaceae comme agent actif sur la lipolyse et comme inhibiteur de la différenciation adipocytaire, en quantité efficace pour traiter ou prévenir les disgrâces de l'adiposité tels que la « peau d'orange » ou l'embonpoint de la silhouette. 4. slimming composition according to claim 2, characterized in that, said composition contains at least one plant extract selected from the group consisting of the family Balanitaceae and the genus Vitellaria family Sapotaceae as an active agent on lipolysis and as an inhibitor of adipocyte differentiation, in an amount effective to treat or prevent disgrace of adiposity such as "orange peel" or overweight silhouette.
5. Composition amincissante selon la revendication 2, caractérisée en ce que, ladite composition est une composition nutraceutique qui contient au moins un extrait de végétal choisi dans le genre Vitellaria de la famille des Sapotaceae comme agent actif sur la lipolyse et comme inhibiteur de la différenciation adipocytaire, en quantité efficace pour traiter ou prévenir les disgrâces de l'adiposité tels que la « peau d'orange » ou l'embonpoint de la silhouette. 5. slimming composition according to claim 2, characterized in that, said composition is a nutraceutical composition which contains at least one plant extract selected from the genus Vitellaria of the Sapotaceae family as an active agent on lipolysis and as an inhibitor of differentiation adipocyte, in an amount effective to treat or prevent disgrace of adiposity such as "orange peel" or overweight silhouette.
6. Composition amincissante selon la revendication 3, caractérisée en ce qu'elle est applicable par voie injectable et se présente sous formes de gel, de lotion, d'émulsion huile dans eau ou eau dans huile. 6. Slimming composition according to claim 3, characterized in that it is applicable by injection and is in the form of gel, lotion, oil in water emulsion or water in oil.
7. Composition amincissante selon la revendication 4, caractérisée en ce qu'elle est applicable par voie topique et se présente sous forme de capsules intégrées dans des produits de massage, d'huiles de massage, d'émulsion huile dans eau, d'émulsion eau dans huile, de lotion, de gel. 7. Slimming composition according to claim 4, characterized in that it is applicable topically and is in the form of capsules embedded in massage products, massage oils, oil-in-water emulsion, emulsion water in oil, lotion, gel.
8. Composition amincissante selon la revendication 5, caractérisée en ce qu'elle est applicable par voie orale et se présente sous forme de poudres, de gels, de pâtes, de chocolats, de gélules, d'émulsions huile dans eau, d'émulsion eau dans huile, d'huiles, d'ampoules. 8. slimming composition according to claim 5, characterized in that it is applicable orally and is in the form of powders, gels, pastes, chocolates, capsules, oil-in-water emulsions, emulsion water in oil, oils, bulbs.
9. Composition amincissante selon les revendications 3 et 4, caractérisée en ce que ledit ou au moins l'un des agent(s) actif(s) est un extrait lipohile de graines de végétal de la famille des Balanitaceae de préférence genre Balanites espèce aegyptiaca présent dans ladite composition à une concentration exprimée en pourcentages en poids rapporté au poids total de la composition comprise entre 0.0001 % et 1 %, de préférence voisine de 0.1 % selon l'extrait testé ou un extrait de graines de végétal du genre Vitellaria appartenant à la famille de Sapotaceae de préférence espèce paradoxa présent dans ladite composition à une concentration exprimée en pourcentages en poids rapporté au poids total de la composition comprise entre 0.0001 % et 3%, de préférence voisine de 0.05% selon l'extrait testé . 9. slimming composition according to claims 3 and 4, characterized in that said or at least one of the active agent (s) is a lipophilic extract of plant seeds of the family Balanitaceae preferably genus Balanites species aegyptiaca present in said composition at a concentration expressed in percentages by weight relative to the total weight of the composition of between 0.0001% and 1%, preferably close to 0.1% according to the extract tested or an extract of plant seeds of the genus Vitellaria belonging to the Sapotaceae family preferably paradoxa species present in said composition in a concentration expressed in percentages by weight relative to the total weight of the composition of between 0.0001% and 3%, preferably close to 0.05% according to the extract tested.
10. Composition amincissante selon la revendication 5, caractérisée en ce que ledit agent actif est un extrait de graines de végétal du genre Vitellaria appartenant à la famille des Sapotaceae de préférence espèce paradoxa présent dans ladite composition à une concentration exprimée en pourcentages en poids rapporté au poids total de la composition comprise entre 0.0001 % et 3%, de préférence voisine de 1 % selon l'extrait testé . 10. Slimming composition according to claim 5, characterized in that said active agent is an extract of plant seeds of the genus Vitellaria belonging to the Sapotaceae family, preferably paradoxa species present in said composition in a concentration expressed in percentages by weight relative to total weight of the composition of between 0.0001% and 3%, preferably around 1% according to the extract tested.
11. Procédé de contrôle à des fins cosmétiques pour mincir comprenant au moins une étape d'administration parentérale d'une quantité efficace d'un extrait de végétal choisi dans le groupe formé par la famille des Balanitaceae et par le genre Vitellaria appartenant à la famille des Sapotaceae. 11. A method for controlling cosmetic purposes for thinning comprising at least one step of parenteral administration of an effective amount of a plant extract selected from the group consisting of the family Balanitaceae and the genus Vitellaria belonging to the family Sapotaceae.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
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FR1003063A FR2962907B1 (en) | 2010-07-21 | 2010-07-21 | PLANT EXTRACT FOR MANUFACTURING SLIMMING COMPOSITION AND METHOD FOR CONTROLLING MINCIR USING SUCH COMPOSITION |
FR1003063 | 2010-07-21 |
Publications (1)
Publication Number | Publication Date |
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WO2012017141A1 true WO2012017141A1 (en) | 2012-02-09 |
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Family Applications (1)
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PCT/FR2011/000430 WO2012017141A1 (en) | 2010-07-21 | 2011-07-20 | Plant extract for the production of a slimming composition and method of control for slimming using such a composition |
Country Status (2)
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FR (1) | FR2962907B1 (en) |
WO (1) | WO2012017141A1 (en) |
Families Citing this family (1)
Publication number | Priority date | Publication date | Assignee | Title |
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FR2987999B1 (en) | 2012-03-15 | 2014-10-03 | Fabre Pierre Dermo Cosmetique | COSMETIC USE OF BALANITE ALMOND EXTRACT TO IMPROVE HAIR RESISTANCE |
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2010
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FR2962907B1 (en) | 2015-05-08 |
FR2962907A1 (en) | 2012-01-27 |
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