FR2904555A1 - Use of a vegetable extract e.g. obtained from genus Linum made of proteic/peptidic compounds, to enhance the augmentation of melanin synthesis in melanocytes of the epidermis or hair bulb and improves the natural pigmentation of the skin - Google Patents

Abstract

Use of a vegetable extract (I) obtained from genus Linum, genus Zea, genus Helianthus or the species Glycine max or Brassica napus mainly made of proteic/peptidic compounds, optionally in combination with another active agent, is claimed in the preparation of cosmetic, dermatologic and/or pharmaceutical composition, to enhance the augmentation of melanin synthesis in melanocytes of the epidermis or hair bulb and improves the natural pigmentation of the skin. ACTIVITY : Dermatological. MECHANISM OF ACTION : Melanogenesis stimulator. The ability of (I) to enhance the augmentation of the melanin synthesis in melanocytes of the epidermis was tested using human skin biopsies. The result showed that there was a sharp increase in the melanin synthesis and a stimulation of the whole process of melanin distribution in epidermis (after 48 hours of the treatment).

Description

i

The present invention relates to the use in a cosmetic composition or for the preparation of a pharmaceutical composition, of an effective amount of rapeseed extract; the extract or the composition being intended to promote the increase of melanin synthesis in the melanocytes of the epidermis or hair bulb, with a view to giving it a tanned appearance, or to prepare the skin for exposure to the sun, or for therapeutic purposes, for repigmenting depigmented skin, for example in the case of vitiligo, or for pigmenting hair or hair, in particular in the treatment and prevention of canities.

The color of human hair and skin is a function of various factors including seasons of the year, race, sex and age. It is mainly determined by the concentration of melanin produced by melanocytes. Melanocytes are specialized cells that, via particular organelles, melanosomes, synthesize melanin. The synthesis of melanin or melanogenesis is a complex process whose precise mechanisms are not yet elucidated and which schematically involves the following steps:

Tyrosine ^ Dopa ^ Dopaquinone ^ Dopachrome ^ Melanin

In the epidermis, the melanocyte is involved in the epidermal melanic unit which comprises a melanocyte surrounded by about 40 neighboring keratinocytes. As melanin is synthesized in the melanosomes, they move from the perinuclear region to the end of the melanocyte dendrites. By phagocytosis, the end of the dendrites is captured by keratinocytes, degraded membranes and redistributed melanosomes in the keratinocytes, where they will provide protection up to the natural desquamation of the cells. The production of melanin, as well as its transport, is regulated by various factors such as, for example, UV radiation, hormones or chemicals. Thus, an increase in exposure to UV radiation causes the synthesis of pigments and browning of the skin. The pigmentation of hair and hair requires the presence of melanocytes in the bulb of the hair follicle. The hair follicle is a tubular invagination of the epidermis that penetrates to the deep layers of the dermis. The melanocytes in the bulb of the hair follicle are in an active state, that is, they synthesize melanin. These pigments are transmitted to the keratinocytes intended to form the hair shaft, which will lead to the growth of a pigmented hair or hair. It is accepted that canitia (natural whitening of hair) is associated with a decrease of melanin in the hair shaft.

Nowadays, it is important to look good and tanned skin is always a sign of good health. However, natural tanning is not always without risk insofar as it requires prolonged exposures to UV radiation, which are likely in return to induce an alteration of skin cells, especially in the case of individuals of clear phototypes. The skin ages prematurely, becomes dry and is characterized by many wrinkles and age spots. It is therefore desirable to find an alternative to natural tanning that is compatible with the health requirements of individuals. On the other hand, we know that in most populations the maintenance of a constant coloring of the hair, sign of youth, is a strong aspiration. The search for compounds that can promote the synthesis of melanin in the skin and hair is a concern of dermatology and cosmetics. These new compounds are particularly useful as an alternative to sun exposure, to prepare the skin and protect it from the sun's rays, to obtain a tan more intense after exposure to the sun, to prolong the natural pigmentation of the skin after exposure to the sun. sun or to prevent and / or limit and / or stop the development of canities and even maintain the natural pigmentation of hair and / or gray or white hairs.

By natural pigmentation of the skin is meant the coloring of the skin or hair determined by the melanin concentration.

In this regard, many solutions have been proposed by adding exogenous dyes, the best known of which is dihydroxyacetone, or DHA. However, only the stimulation of the pigmentation of the skin and / or the hair by the natural way allows a real protection vis-à-vis the UV radiations and remains the ideal way of stimulation of the pigmentation. Thus, it has been proposed in the prior art the preparation and use of activators of melanin biosynthesis (FR828097, FR 2831438, FR 2845285) involving hormones (alpha MSH or its derivatives WO2006037188) or prostaglandins ( WO9511003).

On the other hand, there are pathologies related to pigmentation such as vitiligo which is an autoimmune disease characterized by the appearance on the skin of white patches related to a lack of pigmentation or pityriasis versicolor, a superficial mycosis. causing the appearance of light spots that may appear immediately or after exposure to the sun.

The main objective of the present invention is to provide a new active ingredient that significantly promotes the synthesis of melanin in the melanocytes of the epidermis and hair bulb. The inventors have indeed demonstrated a biological activity and, more particularly dermatological and cosmetic, a rapeseed extract. Cosmetic compositions containing extracts of Brassicaceae have already been proposed in earlier documents. Thus, for example, patent FR 2802417 describes a cosmetic and / or pharmaceutical preparation containing an effective amount of a Brassicaceae extract and a fatty substance and or emulsifiers. However, to the knowledge of the Applicant, it has never been described, in the prior art, the use of a plant protein hydrolyzate belonging to the cruciferous family, as an active ingredient to increase the synthesis. melanin in melanocytes in cosmetics and / or in dermatology and or in pharmaceuticals.

By pro-pigmenting active agent is meant a compound capable of promoting the increase of melanin synthesis in the melanocytes of the epidermis or hair bulb.

By hair and hair is meant all the hairy appendages and in particular also the eyelashes and the eyebrows.

The compositions according to the invention may be applied by any appropriate route, in particular oral, parenteral or external topical, and their formulation will be adapted by those skilled in the art, in particular for cosmetic or dermatological compositions. Advantageously, the compositions according to the invention are intended for topical administration. They contain a physiologically acceptable medium, in particular a cosmetologically or pharmaceutically acceptable medium, in particular a dermatologically acceptable medium.

Thus, the subject of the invention is primarily the use in a composition, or for the preparation of such a composition, of an effective amount of extract; the extract or the composition being intended to promote the increase of melanin synthesis in the melanocytes of the epidermis or hair bulb. The term "extract" refers to any isolated substance or preparation obtained from plant material. It is obtained, for example, by dissolving the active components by means of solvents (such as water, alcohol, etc.) then by concentration and purification of these active ingredients, for example by evaporation of the solvents. Any method of extraction or purification known to those skilled in the art can be used to prepare the extract according to the invention.

To carry out the extraction, it is possible to use the entire folding, or a specific part of the plant (leaf, grain, etc.). More particularly according to the invention, one of the many plants of the family Cruciferae (Latinized in Cruciferae) is used. About 3200 species are distributed in 375 genera worldwide. Crucifers are also called Brassicaceae. These plants are found mainly in the temperate regions of the northern hemisphere and, more particularly, in the mediterranean margin. Crucifers get their name from the cross arrangement of their sepals and petals. They are herbaceous, perennial, annual and quite commonly biennial.

As a plant belonging to this family include field crops, oleaginous, such as rapeseed (Brassica napus, var. oleifera); food plants like all varieties of "cabbage" (of the genus Brassica); condiments such as mustard (of the genus Sinapis); Or plants of ornamental interest such as the wallflower or the basket of gold (of the genus Alyssum).

Any method of extraction or purification known to those skilled in the art can be used to prepare the hydrolyzate according to the invention. For example, in a first step, crucifer seeds, such as rapeseeds, can be delipidated by simple pressing and / or by the action of a conventional organic solvent (for example an alcohol, a hexane or acetone). After drying of the product thus obtained, a residue enriched in proteins commonly known as cake is obtained.

According to another technique, it is possible to envisage carrying out the extraction of a protein fraction obtained from this cake. The actual protein extraction step is carried out in an aqueous medium, neutral or basic. Preferably, according to the invention, the extraction of the proteins will be carried out in aqueous medium, slightly basic, and hot. Proteins will be recovered by precipitation or concentration. The hydrolysis step of the proteins is carried out by proteases of plant origin such as, for example, papain or bromelain; or by so-called enzymes industrials such as alkalases, flavourzyme ... The culture medium thus hydrolyzed is centrifuged, filtered until a hydrolyzate of cruciferous proteins is obtained.

This hydrolyzate is dissolved in one or more solvents. In particular, aqueous solvents may be mentioned. By aqueous solvent is meant any solvent consisting wholly or partially of water. We can mention the water itself, hydroalcoholic solvents in all proportions or solvents consisting of water and a compound such as propylene glycol or butylene glycol in all proportions. Plant protein hydrolysates belonging to the cruciferous family are analyzed for their content of proteinaceous compounds. Protein compounds are understood to mean the protein fragments, the peptides and the free amino acids present in the mixture. The peptides, amino acids and protein fragments are determined according to conventional techniques, which are well known to those skilled in the art. Thus, according to an advantageous embodiment of the invention, the hydrolyzed extract contains a quantity of protein compounds representing between 30 and 90% of the total weight of the dry matter, more particularly this amount is between 50 and 80% total weight of the dry matter.

The invention has the second object the use in a cosmetic composition, or for the preparation of a pharmaceutical composition, of an effective amount of extract; the extract or the composition being intended to promote the pigmentation of the hairs and / or the hair.

The invention also relates to the use in a cosmetic composition, or for the preparation of a pharmaceutical composition, of an effective amount of extract; the extract or the composition being intended to prepare the skin for exposure to the sun.

The invention also relates to the use in a cosmetic composition, or for the preparation of a pharmaceutical composition, of an effective amount of extract; the extract or the composition being intended, by increasing melanin synthesis, to protect the skin from sunlight.

According to another form of the invention, the use of the rapeseed extract or the composition containing it is intended to protect the skin from environmental stress. According to an advantageous embodiment of the invention, the extract is first solubilized in one or more cosmetically or pharmaceutically acceptable solvents such as water, glycerol, propylene glycol, butylene glycol, ethoxylated or propoxylated diglycols, and the like. ethanol, propanol or isopropanol.

According to yet another advantageous embodiment of the invention, the rapeseed extract is previously solubilized in a cosmetic or pharmaceutical vector such as liposomes or adsorbed on powdery organic polymers, mineral supports such as talcs and bentonites, and more generally solubilized in, or attached to, any cosmetically or pharmaceutically acceptable carrier.

To give an order of magnitude, in the cosmetic or dermatological compositions of the present invention, the rapeseed extract is used in an amount representing from 0.0001% to 20% of the total weight of the composition, and preferably in an amount representing from 0.05% to 5% of the total weight of the composition.

In addition to the major advantage of the pigmentation of the skin in the sun protection, a pro-pigmenting compound according to the invention offers outlets in self-tanning products and promoting tanning. For this, the invention relates to the use of rapeseed extract for the manufacture of products for artificial tanning and / or browning of the skin.

The invention also relates to the use of rapeseed extract for improving the intensity and / or the homogeneity and / or the persistence of the coloration produced on the skin and / or the hair.

The invention also relates to the use of rapeseed extract for reducing pigmentary disorders associated with hypopigmentation of the skin, especially vitiligo.

Preferably, the compositions according to the present invention will be in a form suitable for topical administration to the skin, and cover all cosmetic or dermatological forms. These compositions must therefore contain a cosmetically and / or dermatologically acceptable medium, that is to say compatible with the skin, hair or hair. These compositions may especially be in the form of creams, O / W, W / O emulsions or multiple emulsions, solutions, suspensions, gels, milks, lotions, sticks or powders, suitable for application to the skin, lips and / or hair.

These compositions comprise the excipients necessary for their formulation, such as solvents, thickeners, diluents, surfactants, antioxidants, dyes, preservatives, perfumes.

Of course, those skilled in the art will take care to choose any additional compounds, active or non-active, and / or their quantity, so that the advantageous properties of the mixture are not, or not substantially, impaired by the addition considered.

The composition that may be used according to the invention may in particular consist of a composition for hair care, and in particular a shampoo, a conditioner, a setting lotion, a treatment lotion, a cream or a styling gel, a restructuring lotion for hair, a mask, etc. The cosmetic composition according to the invention can be used in particular in treatments using an application that is followed or not followed by rinsing, or in the form of shampoo.

It can also be in the form of dye or mascara to be applied with a brush or a comb, in particular on eyelashes, eyebrows or hair.

Advantageously, the compositions that can be used according to the invention also contain at least one other agent that promotes the pigmentation of the skin, hair and / or hair. Such compounds are in particular tyrosinase substrates, such as tyrosine or L-DOPA, prostaglandins, or activating compounds of the cAMP pathway such as pro-opiomelanocortin derivatives, adenosine, or forkoline or its derivatives. Mention may also be made of plant extracts such as citrus aurantium (bitter orange) or chrysanthemum (Chrysanthemum morifolium), described in particular in patents FR 2845285 and EPI 014934.

Such compounds are also found in the family of exogenous dyes of the superficial layers of the epidermis, such as dihydroxyacetone (DHA), erythrulose, extracts of henna leaves, described in particular in patents EP 0742002 and FR2779958. The invention relates to a cosmetic process for increasing the synthesis of melanin in melanocytes and promoting the natural pigmentation of the skin and the hair, which consists in applying the composition as defined above to the skin or the hair.

The invention relates to a cosmetic treatment method for preventing or treating hair and hair whitening, comprising applying to the skin the composition as defined above.

Other advantages and features of the invention will appear better on reading the examples given for illustrative and non-limiting purposes.

Example 1 Preparation of an extract of plant proteins belonging to the genus cruciferous.

In a first step, 1 kg of the rapeseeds are delipidated by the action of an organic solvent: hexane. After drying the product, a residue enriched in proteins (the cake) is obtained. The cake is then diluted in a slightly basic aqueous solution and then hydrolyzed by adding an enzyme: papain, at 60 ° C. for 4 hours with stirring. This mixture is then heated to 80 ° C, centrifuged and filtered until a clear solution is obtained. It is then concentrated under vacuum, then filtered again on filter plates and sterilizing cartridge.

A brown-colored hydrolyzate titrating at 30 g / l of protein-like compounds is then obtained. The hydrolyzed extract contains a quantity of protein compounds representing approximately 65% of the total weight of the dry matter. This hydrolyzate is redissolved in dipropylene glycol.

Example 2 Ex Vivo Study of the Effect of Cruciferous Extract on Melanin Synthesis

The purpose of this ex vivo study is to demonstrate the increase in melanization provided by the salt extract of the invention.

Protocol: Human skin biopsies 6 mm in diameter are maintained in culture ex vivo in the presence of a specific medium (DMEM lg / L, HAMF12, SVF and antibiotics) on inserts deposited in 6-well plates. The biopsies are cultured for 48 hours and receive or not 2 applications per day of extract according to the invention at a concentration of 1%. The biopsies are then fixed in 9% formalin, NaCl (150 mM) for 10 hours and then included in the paraffin. Skin sections 3 μm thick are then made and the melanin is stained specifically by the Fontana-Masson technique.

Results: Skin sections that did not receive the application of extract according to the invention have a low intensity coloration. On the other hand, the skin sections having received the extract applications according to the invention exhibit a markedly increased color intensity. In addition, melanin is located in the basal layer, but also transported in the supra-basal layers.

Conclusions: 48 hours of treatment led to a strong increase of melanin synthesis by melanocytes and to stimulate the whole process of distribution of melanin in the epidermis.

Example 3 Preparation of compositions

These compositions were obtained by simple mixing of the various components. The quantities indicated are given as a percentage of weight.

1 - Oil-in-water emulsion

Oil phase: m Montanov 68 (Cetearyl Alcohol and Cetearyl Glucoside) 5.00% m Jojoba Oil 5.00% m Vaseline Oil 5.00% m Isopropyl Palmitate 7.00%

Water phase: m Glycerine 5.00% m Allantoin 0.10% m Extract according to the invention 1.00% m Sepigel 305 (Polyacrylamide and C13-14 Isoparaffin and Laureth-7) 0.30% m Preservative 0.50% 0.50% qsp 100%

Eau perfume

2- Gel

Carbopol Ultrez 10 (2% solids)

triethanolamine

Extract according to the invention

Tory

EDTA (sequestering)

Perfume

Water

3- Lotion

B Mono Propylene Glycol B Allantoine

B Glycerin m Cetiol HE (PEG-7 Glyceryl Cocoate)

B Extract according to the invention

B Conservative B Perfume

Handsome

4-self-tanning oil-in-water emulsion

Oily phase: B Glycerol mono / distearate mixture

B Stearyl alcohol

B Stearic acid palm oil

B Poly dimethylsiloxane

B Poly dimethylsiloxane mixture alpha-omega dihydroxyl / cyclopentadimethylsiloxane (14.7 / 85.3)

B Lauroyl isopropyl sarconisate

Aqueous phase :

B Dihydroxyacetone

B Glycerin

25.00%

0.50%

5.00%

0.20%

0.10%

0.50% qsp 100%

1.00%

0.30%

1.00%

1.00%

0.5%

0.20%

0.50% qsp 100%

2.00%

1.00%

1.50%

2.00%

3.00%

15.00%

5.00% 5.00% B Hexadecyl alcohol phosphate, potassium salt 1.00%

B Polyacrylic acid 0.30%

B Triethanolamine qsp pH: 7

B dl-alpha-tocopheryl acetate 0.50%

B Extract according to example 1 1.00%

B Demineralized water qs 100.00%

Phase huileuse : B Polydiméthyl/methylcetyl methylsiloxane oxyéthyléné5-self-tanning water-in-oil emulsion

Oily phase: B Polydimethyl / methylcetyl methylsiloxane oxyethylenated

B Phenyl trimethylsiloxy trisiloxane

B Lauroyl isopropyl sarcosinate

B Isohexadecane

B Cyclopenta dimethylsiloxane Aqueous phase:

B Dihydroxyacetone

B Glycerin

B magnesium sulphate

B Extract according to example 1 B Demineralized water

2.00%

3.00%

10.00%

5.00%

3.00%

2.00%

5.00%

0.70%

1.00% qsp 100.00%

5.00%

0.40%

13.00%

7.00%

5.00%

0.25%

qsp 100.00 %1.00%

qsp 100.00%

6- Self-tanning lotion

B Dihydroxyacetone

B Freeze-dried extract of ^' Εclipta prostata B 96% Ethanol

B Ethoxydiglycol

B PPG-1-PEG-9-Lauryl Glycol Ether

B Parabens

B Extract according to example 1 B Demineralized water 66.80%

5.00%

0.30%

0.30%

2.00%

2.00%

2.00%

2.00%

1.00%

1.00%

1.00%

1.00%

0.25%

0.1%

0.1%

10.975%

2.00%

0.60%

0.40%

0.05%

1.00 %0.025%

1.00%

7- Oil emulsion in self-tanning water

Handsome

B Ethoxydiglycol

B Xanthan gum B Cetyl hydroxyethylcellulose

B Cetyl alcohol

B Stearyl alcohol

B Octyl palmitate

B Glucam P-20 Distearate B Steareth-20

B Dimethicone

B Polysorbate 60

B Dimethicone Copolyol / IPDI Copolymer

B Glycerylstearate and PEG-100 Stearate B Actiplex 335 Lipo OP

B Tocopheryl acetate

B Water fl Dihydroxyacetone fl Nipaguard MPA fl Panthenol, 50% aqueous fl Sorbic acid fl Sodium metabisulfite fl Extract according to Example 1

Claims (6)

Use of an effective amount of at least one plant extract obtained from plants of the brassica genus, alone or in combination with at least one other active agent, in or for the preparation of a cosmetic and / or dermatological composition and or pharmaceutical, the extract or the composition containing it being intended to promote the increase of melanin synthesis in the melanocytes of the epidermis or hair bulb and improve the natural pigmentation of the skin. 2. Use according to claim 1, characterized in that the plants belong to the species Brassica napus (rapeseed). 3. Use according to one of the preceding claims, characterized in that the composition is in a form suitable for topical application comprising a cosmetically or dermatologically acceptable medium. 4. Use according to any one of the preceding claims, characterized in that the rapeseed extract is used in an amount representing from 0.0001% to 20% of the total weight of the composition, and preferably in an amount representing from 0 , 5% to 5% of the total weight of the composition. 5. Use according to any one of the preceding claims, characterized in that the composition further contains at least one exogenous dye of the surface layers of the epidermis and / or at least one pro-pigmenting active agent different from said rapeseed extract, selected from tyrosinase substrates or prostaglandins or activating compounds of the cAMP pathway or plant extracts pigmenting. 6. Use according to any one of the preceding claims, characterized in that the extract or the composition containing it is intended, by increasing melanin synthesis, to prepare the skin for exposure to the sun or to protect the skin. radiation from the sun. 7. Use according to any one of the preceding claims characterized in that the extract or composition containing it is intended to protect the skin from external aggressions, in particular UV rays. 8. Use according to any one of the preceding claims characterized in that the extract or the composition containing it are intended for artificial tanning and or browning of the skin. 9. Use according to any one of the preceding claims characterized in that the extract or the composition containing it are intended to improve the intensity and / or homogeneity and or the persistence of the pigmentation of the skin and / or hair. 10. Use according to any one of the preceding claims characterized in that the extract or the composition containing it is intended to attenuate a pigmentary disorder of the skin, especially vitiligo. 11. Use according to any one of the preceding claims characterized in that the extract or the composition containing it are intended to prevent or treat the whitening of the hair and / or hair. 12. Cosmetic treatment process intended to promote the increase of melanin synthesis in melanocytes, characterized in that a composition as defined according to any one of Claims 1 to 5 is applied topically to the zone to be treated. .