BR112013002215B1 - COSMETIC USE OF GREEN COFFEE GRAINS AND METHOD, KIT FOR REGULATION OF SKIN PIGMENTATION DISORDERS, AND NON-THERAPEUTIC METHOD FOR COSMETIC TREATMENT - Google Patents

Abstract

use of green coffee beans to regulate skin pigmentation disorders. The present invention generally relates to the field of food supplements and / or food products for cosmetic purposes. More specifically, the present invention aims to provide an ingredient containing green coffee beans or an extract thereof for prevention and / or treatment of skin hypergmentation, skin color imperfections such as age points and other skin disorders characterized by abnormal pigments. The present invention also aims to improve skin tone as well as to provide a skin whitening or bleaching agent.

Description

Patent Descriptive Report for "COSMETIC USE OF GREEN COFFEE GRAINS AND METHOD, SKIN PIGMENTATION DISORDER KIT, AND NON-THERAPEUTIC METHOD FOR COSMETIC TREATMENT". The present invention relates in general to the field. food supplements and / or food products for cosmetic purposes More specifically, the present invention aims to provide an ingredient containing green coffee beans or an extract thereof for the prevention and / or treatment of skin hyperpigmentation, skin color imperfections such as as age points and other skin disorders characterized by abnormal pigments The present invention also aims at improving skin tone as well as providing a skin whitening or bleaching agent.

Background of the Invention Skin color is primarily determined by the amount and type of melanin, a brown pigment present in the skin. Smaller amounts of melanin result in lighter skin color while larger amounts result in darker skin color. Also, hyperpigmentation in the skin is caused by overexpression or accumulation of melanin in the skin. As a result, the course involved in melanin production has been targeted by many inhibitors in order to reduce the levels produced. One of the main enzymes involved in the course of melanin is tyrosinase. Melanin synthesis is a process under hormonal control, including melanocyte stimulating hormone (MSH) (Me-lanocyte Stimulating Hormone) and adrenocorticotropic hormone (ACTH) (Adrenocorticotropic Hormone) peptides that are produced from the pro-opiomelanocortin precursor. . It is stimulated by DNA damage that is caused by UVB radiation as well.

So sun exposure, over time, can induce many biochemical skin reactions, leading to sunburn and tanning, for example. Other consequences of sun exposure accumulate over time. These changes can result in the development of age spots and create a mottled, uneven skin tone. Unfortunately, many of the commercially available products on the market today are either only marginally effective or contain active agents that are unstable and lose their potency when incoipoised to a finial form. The ability to modify the expression of skin pigment content to promote a uniform skin tone or lightening skin tone is highly desirable in today's society. Many people want to change their skin tone, reduce age points, etc., or just for purely cosmetic reasons.

As a result, efforts to develop effective compositions have focused on agents that inhibit tyrosinase activity. For example, a variety of tyrosinase inhibitors such as hydroquinone, vitamin C, cysteine, kojic acid, arbutin and glutathione among others have been proposed in topical compositions. Also, a variety of dermatological compositions have been suggested for improving the appearance of pigment disorders such as those seen in melasma, freckles, vitiligo, piebaldism, phenylketonuria and the like and / or for cosmetic purposes.

Also, the use of skin whitening compositions is widely expanded. However, they either destroy melanin or inhibit its formation. Many of these contain harsh chemical agents such as peroxides, acids or formaldehyde or thiolated materials. Less astringent therapies have other disadvantages.

Topical retinoids and topical corticosteroids have been suggested as hypopigmentation agents, as well as laser treatment and chemical exfoliations, but these have few desirable responses.

Other compositions have suggested the use of natural materials on the skin, which in some cases have been used for centuries in Asia or Europe to whiten skin and skin areas or to enhance the appearance of good skin. These include the use of lemon, orange, cucumber, ginkgo, carob, pomegranate, geranium herb, cinnamon, sweet marjoram, rosemary, etc. In order to combat abnormal pigment-related disorders or to lighten skin tone, several compounds that, when applied topically to the skin, are able to reduce thyrokinase activity and consequently limiting melanin production, were then proposed. Unfortunately, currently available treatments are not entirely satisfactory, in particular in terms of the coiateral effects that are often associated with them, such as irritating side effects with certain topical agents.

It would then be highly desirable to have alternative preparations which did not have the drawbacks of those described in the prior art. In particular, it would be highly desirable to develop orally administered nutritional cosmetic compositions that have improved stability and efficacy to promote a uniform skin tone or to lighten skin tone.

There also remains a need for active agents that are effective for treating and / or preventing skin pigmentation disorders, particularly those due to environmental factors or aging. The object of the present invention is to satisfy these needs.

Summary of the Invention The present inventors have been able to achieve this by providing a food composition or food supplement comprising at least one ingredient containing green coffee beans or an extract thereof.

Accordingly, according to a first object, the invention relates to the cosmetic use of an effective amount of at least one ingredient containing green coffee beans or an extract thereof as an active agent for treating and / or preventing disorders of skin pigmentation. Such skin disorders are in particular due to age or environmental factors (eg, UV) such as age points. They may also be skin disorders that are observed in melasma, freckles, vitiligo, piebaldism, phenylketonuria and the like.

The present inventors have found that green coffee effectively suppresses melanin formation, melanogenesis, despite the fact that extracts show little to no inhibition of tyrosinase activity. This result is surprising and unexpected considering the pivotal role of tyrosinase in melanogenesis and the focus of developmental efforts on the technique to inhibit this enzyme.

For the purpose of the present invention, the term "skin" is intended to mean the skin of the face or body.

For the purpose of the present invention, the term "effective amount" is intended to mean an amount sufficient to achieve the expected effect.

For the purpose of the present invention, the term "prevent" is intended to reduce the risk of occurrence of the manifestation of the disorder under consideration. The present invention also relates to the cosmetic use of the above mentioned ingredient as an active agent for treating and / or preventing skin pigment imperfections. As a result, the color becomes brighter and more homogeneous, with no areas of dyschromia or drying. The present invention also relates to the cosmetic use of an effective amount of at least one ingredient containing green coffee beans or an extract thereof according to the invention as an active agent for bleaching or lightening skin tone.

The present inventors have also found that the ingredient according to the invention further improves skin hydration and / or barrier function.

A use according to the present invention may also comprise the use of at least one ingredient containing green coffee beans or an extract thereof, in combination with an effective amount of at least one active agent to further improve skin hydration or aging. particularly as described below.

According to another of its aspects, the object of the invention is a method, in particular a cosmetic method, for treating and / or preventing skin tone imperfections and disorders associated with hyperpigmentation, in particular aesthetic disorders, in a subject comprising at least one step of administering to said subject at least one ingredient containing green coffee beans or an extract thereof according to the invention.

The compositions according to the present invention are orally administrable. This has the advantage of acting globally on the entire skin in its deep layers (dermis, hypodermis) by means of a rapid and relatively non-restrictive mode of administration. Specifically, metabolites and other active nutrients are in particular distributed within the dermal matrix through the bloodstream. Oral administration also has the advantage of a fast and relatively non-restrictive mode of administration.

Detailed Description of the Invention According to a first object, the present invention provides for the use of green coffee beans.

In the following text, "coffee beans" shall be understood to mean beans obtained by wet (fermentation, washing) or by dry (drying followed by mechanical stripping) starting from the "cherry" of coffee after stripping as above. described. "Extract" shall be understood to mean all compounds obtained from an alcoholic, aqueous-alcoholic or aqueous extraction of a crude product. The coffee tree species selected for the preparation of the coffee bean extracts used in the compositions are advantageously selected from the Coffea species. Coffee trees are small trees with soft, evergreen, leathery, bright leaves (10-15 x 4-6 cm). The fragrant white flowers are grouped in spirals at the angle formed by the leaf and the branch of the leaves. The fruit is a green drupe that turns red at maturity and usually contains two planar-convex berries that are contiguous across its planar face. Although only two species provide the essential needs of the coffee market (C. arabica and C. cane-phorá), many coffee tree species exist in the wild in the rainforests of East Africa. Coffee "bean" is obtained through the wet (fermentation, washing) or dry (drying, followed by mechanical peeling) pathways by breaking off a coffee "cherry", ie from the ridges. Pulp reduction removes the red pericarp and fleshy mesocarp; it leads to the "shell" of the coffee. It is after peeling (removal of the lignified endocarp) that the "bean" of coffee (or beans) is obtained. Green coffee may be derived from Arabica and Robusta or it may be a mixture of Arabica and Robusta. The green coffee portion may be at least partially decaffeinated. This is to provide products whose caffeine level can be modulated from caffeine free to regular caffeine level.

In particular, a coffee bean extract may be obtained by aqueous, aqueous-alcoholic or alcoholic extraction of coffee beans and preferably by extraction with the aid of methanol, ethanol or propanol. Preferably, it does not contain the coffee bean fractions that can be extracted by nonpolar solvents. Methods for preparing decaffeinated coffee extracts are well known in the art.

The compositions according to the invention may be in any of the dosage forms normally available for the selected administration method. The carrier may be diverse in nature depending on the type of composition under consideration. Accordingly, the composition may be any food or pharmaceutical product or a cosmetic product for oral application. Examples for food or pharmaceutical carriers complete nutritional formula, dairy products such as ieite, yogurt, cheese, fermented milk, fermented milk products, ice cream, cereal products or fermented cereal products, dairy powders milk, baby formulas, chilled or shelf-stable drinks, confectionery, chocolate or cereal foods, animal feed, in particular for domestic animals. In particular, chicory or extract thereof may be incorporated into any other form of food supplement or fortified food, for example, post-compacted or uncompressed food bars. The powders may be diluted with water, soda, milk products or soy derivatives or incorporated into food bars. The food product may also further comprise a protein source, a carbohydrate source, a lipid source, a mineral source and / or a vitamin source. The presence of proteins, carbohydrates, lipids, minerals and / or vitamins can have several advantages. These compounds generally contribute to the taste and mouthfeel of the final product. They also provide the body with nutrients that it may urgently need when it is affected by skin disorders. They also allow formulation of the product of the present invention as a complete nutritional formula so that no additional nutrition is required.

The individual ingredients may comprise any type of edible compound. Typical ingredients for food compositions, in particular beverages, are well known in the art, for example, milk, cream, coffee bleachers and coffee creams. Alternatively, the ingredients could also be a salad dressing or parts thereof, for example. Such compounds are used by consumers to modify, for example, the aroma, appearance and texture of a composition. The ingredients may be in liquid or dry form, for example as powders, which are dissolved and / or suspended in a beverage. The invention also provides a coffee beverage product, such as (a) a roasted and ground coffee product, (b) a soluble coffee product, (c) a single portion coffee pad, tablet or capsule, (d ) a ready-to-drink coffee product or (e) any other suitable coffee product, comprising the coffee product as defined herein as an ingredient.

Soluble coffee or instant coffee, as it is otherwise known, is very well known and has been commercially produced for many decades. It is made from roasted and ground coffee in a variety of ways, all well-known to those skilled in the art. The present invention is particularly suitable for use as a soluble coffee product or any product which is based on or derived from a soluble coffee product. For example, the coffee product may also be used in so-called ready-to-drink beverages. Examples of ready-to-drink beverages for which the product of the present invention is suitable include two-in-one beverages comprising a coffee component together with a natural or artificial sweetener component, the components being optionally prediluted with a liquid such as water or milk. In this case, the coffee component may comprise the coffee product of the present invention.

Three-in-one beverages comprising coffee, a sweetener and a whitener such as milk, a liquid cream or a solid cream (for example, powder) may comprise the coffee product of the present invention.

Further, any beverage comprising soluble coffee as an ingredient may comprise the coffee product of the present invention. The composition may further comprise additional ingredient suitable for inclusion in a food composition. Common ingredients may, for example, be sugars, artificial sweeteners, emulsifiers, stabilizers, thickeners, flow agents, colorants, flavors, flavorings and the like. Suitable artificial sweeteners include saccharin, cyclamates, acetosulfame, L-aspartyl based sweeteners such as aspartame and mixtures thereof. Suitable emulsifiers include monoglycerides, diglycerides, lecithin, diacetyl tartaric acid esters of monodiglycerides, emulsifying starches and mixtures thereof. Suitable stabilizers include dipotassium phosphate and sodium citrate. A suitable flow agent is sodium silica aluminate. In one embodiment, the composition comprises milk protein and / or vegetable protein. In a further embodiment the composition comprises milk fat and / or vegetable fat.

Further, the present invention may be used as an ingredient for standard preparation, espresso, coffee-based beverage preparations to be used as a main portion or single beverage portion for home preparation.

If the product is a nutritional supplement for oral administration, it may be present in capsules, Qeiatin capsules, soft capsules, tablets, sugar-coated tablets, pills, pastes or pastilles, gums or solutions or emulsions for drinking, a syrup or a gel. Such a supplement could also include a sweetener, a stabilizer, an antioxidant, an additive, a taste and / or a colorant. The formulation thereof is carried out by standard methods for producing sugar coated tablets, gel capsules, gels, controlled release hydrogels, emulsions, tablets or capsules.

In this regard, the adjuvant for oral compositions, in particular for food supplements, is known to the person skilled in the art. Mention may be made, among others and for purely illustrative purposes, of lubricants such as magnesium stearate, instant solubilizing products, gelling agents, thickeners, humectants, fatty and / or aqueous compounds, preservatives, texturizing, flavoring and / or agents coatings, antioxidants and coloring materials commonly used in food. The composition according to the present invention may further contain lipids, polyphenols, taurine, probiotic microorganisms, vitamins and / or trace elements. If probiotics are used, they may be included in a living, semi-active or deactivated form, for example as a lyophilized powder.

Also culture supernatants of the microorganisms may be included in the composition. They may be selected from the group consisting of lactic acid bacteria, in particular Lactobacilli and / or Biophidobacteria, and are more preferably selected from the group consisting of Lactobacillus johnsonii, Lactobacillus rhamno-sus, Lactobacillus paracaseus, Lactobacilli, Bifidobacterium bifidum, Bifidobacterium brief, Animal Bifidobacterium, Infant Bifidobacterium, Bifidobacterium dolescentis and Bifidobacterium pseudocatenulatum. According to a more preferred embodiment, the strains used are Lactobacillus johnsonií (La1) deposited on June 30, 1992 under the Budapest Treaty with the Pasteur Institute and receiving deposit no. CNCM 1-1225 or Lactobacillus paracasei (ST11) filed January 12, 1999 with the Institute Pasteur in accordance with the Budapest Treaty and receiving deposit no. CNCM 1-2116. The following compounds may, for example, be used alone or in combination: zinc and its salts including zinc sulfate and zinc glucanate, vitamins B5, B6, B8, C, E or PP, p-carotene and carotenoids, garlic extracts in particular in the form of allyl sulfide or garlic oil, selenium, curcumin, curcumininoids, niacin, lithospermic acid and adenosine. It is understood that one skilled in the art will select such active compounds and, where possible, combine them in such a manner as to enhance the expected effects of the composition which is the object of the invention by preventing the desired activity of interest from being inhibited or attenuated.

Usage The products of the invention may be used efficiently for treating or preventing skin pigmentation disorders or cosmetically lightening skin tone, for example by decreasing melanin production. In fact, extracts of green coffee beans have been shown to decrease melanin synthesis in vitro (Example 1, Figure 1). Tyrosinase production was also decreased, but to a limited degree (Fig-Frog 2), suggesting that the decrease in melanin was not due to the decrease in tyrosinase, but rather to mechanisms acting upstream or downstream of this enzyme.

The ingredients according to the present invention further have a positive effect on skin barrier reinforcement and maintenance of skin hydration.

As a result, pigment imperfections are reduced, the color becomes brighter and more homogeneous, with no areas of discoloration or dryness.

Accordingly, according to one object, the invention relates to the cosmetic use of an effective amount of at least one ingredient containing green coffee beans as an active agent for treating and / or preventing skin pigmentation disorders, in particular. those due to age or environmental factors such as üV. The present invention also relates to the cosmetic use of an effective amount of at least one ingredient containing green coffee beans as an active agent for skin tone whitening or bleaching, which is particularly desirable for the Asian population.

A use according to the present invention may also comprise the use of at least one ingredient containing green coffee beans in combination with an effective amount of at least one active agent for improving skin hydration or skin aging, in particular as described below.

According to another aspect, the object of the present invention is a method, in particular a cosmetic method, for treating and / or preventing skin tone imperfections and / or disorders associated with hyperpigmentation, in particular aesthetic disorders, in a subject comprising at least one step of administering to said subject at least one ingredient containing green coffee beans according to the invention. The cosmetic treatment method of the invention may be carried out in particular by oral administration of at least an effective amount of at least one ingredient containing green coffee beans according to the invention. Oral administration comprises ingestion, in one or more administrations, of an oral composition as defined above.

It can comprise a single application. According to another embodiment, the application is repeated, for example, 2 to 3 times a day, for a day or more, and generally for an extended period of at least 4, or even 1 to 15, weeks.

Further, combinations of treatment with optionally oral or topical forms may be desired in order to supplement or enhance the activity of the ingredients as defined by the invention.

Accordingly, a topical or oral treatment with a green coffee bean-containing composition according to the invention, combined with an oral or topical composition optionally containing another active ingredient, in parentifying a probiotic microorganism, or other probiotic in form. dead, alive or semi-active or a moisturizing or anti-aging agent, could be thought of as a case. The ingredients are mixed prior to formulation in the order and under conditions readily determined by those skilled in the art. The proportion of coffee bean extract in the composition will, of course, be determined as a function of the desired effect and mode of administration of the composition.

The daily doses of orally administered green coffee bean extract may preferably be from 0.1 to 27 g / day, depending on the type of product and caffeine content, more preferably 0.5 to 18 g / day. most preferably still 1 to 3 g / day. The present inventors have found that the effectiveness of green coffee bean extracts according to the present invention is generally dose dependent and follows a dose response curve. If generally mild skin disturbance or damage is to be prevented and the product will be used frequently, very small amounts will be sufficient to achieve the desired effect. If a severe skin pigment disorder has to be treated, larger amounts will be more appropriate, although also small amounts will have an effect.

Preferably, the composition intended for oral administration contains a coffee bean extract in an amount ranging from 1% to 100% by weight of the composition and preferably from 10% to 80% by weight of the composition depending on the form. of product.

Additional advantages and features of the present invention are apparent from the following Examples and Figures. The examples below are then given by way of non-limiting illustration of the field of the invention. In these examples, unless otherwise noted, percentages are percentages by weight, and ranges of values written in the form "between ... and ..." include specified upper and lower limits.

Figures Figure 1: Evaluation of melanin production by murine melanocytes pretreated with green coffee strains.

Figure 2: Evaluation of tyrosinase production by murine melanocytes pretreated with green coffee extracts.

Figure 3: Evaluation of filaggrin synthesis by human primary e-pyoderma keratinocytes pretreated with different green coffee extracts.

Figure 4: Evaluation of hyaluronic acid secretion by human primary epidermal keratinocytes pretreated with green coffee extracts.

Figure 5: CD44 production by human epidermal keratinocytes pretreated with different green coffee extracts.

EXAMPLES

Example 1: Effects on Skin Pigmentation In order to evaluate the potential beneficial effect of ingredients with respect to skin des- or pro-pigmentation the applicant used 2D murine melanocyte culture (B16) and 2 tests were performed: 1-evaluation melanin production and 2-tyrosinase production evaluation. 1. Cell Culture Conditions B16 cells were cultured in DMEM 1 g / l of phenol-free red glucose supplemented with 10% fetal bovine serum in a humidified chamber at 37 ° C and containing 5% CO2. 2. Melanin Production by Murine B16 Melanocyte Cell Line Cells were incubated with the selected ingredients or test references (Kojic acid at 400 pg / mL) for 72 hours in the presence or absence of NDP-MSH, an analog of MSH. Total amount of melanin (extracellular and intracellular) was assessed by measuring the optical density at 405 nm of each sample against melanin standards in the presence or absence of NDP-MSH. 3. Tyrosinase Production by Murine B16 Melanocyte Cell Line Cells were incubated with the selected ingredients or test references (Kojic acid at 400 pg / ml) for 4 hours. Tyrosinase production was assessed by immunostaining. INGREDIENTS: Applicant has tested decaffeinated green coffee extracts from Robusta and Arabica, Svetol® (provided by Naturex); Oryza P-extract and a green coffee extracted in water. The concentrations tested for each green coffee extract are shown in Table 1. ____________________________ Table 1: Cytotoxicity of green coffee extracts on human primary dermal fibroblasts and human primary epidermal keratinocytes. The applicant worked with the highest non-toxic concentration with respect to normalizing as many conditions as possible between the different extracts to be even better able to compare them. In this way, coffee extracts were tested at a concentration of 40 pg / mL. Results Results are expressed as a percentage with respect to the control. Test reference (Kojic acid) induced, as expected, a decrease in melanin content. Figure 1 shows melanin production by B16 melanocytes treated for 72 hours with the selected ingredients. The applicant generally observed that coffee extracts had some potential for depigmentation of the peel, as they were able to decrease melanin and tyrosinase production in vitro compared to control conditions (Figures 1 and 2).

Example 2: Effect on Skin Barrier Function and Hydration The potential beneficial effect of the Extracts of Example 1 with respect to skin barrier function and skin hydration was evaluated using 2D culture of human primary epidermal keratinocytes and we performed 3 tests. : 1-evaluation of filaggrin synthesis, 2-evaluation of hyaluronic acid secretion and 3-evaluation of CD44 (hyaluronic acid receptor) production by human primary epidermal keratinocytes.

Human Epidermal Keratinocyte Cell Culture Conditions were cultured in SFM control-medium keratinocytes in a humidified chamber at 37 ° C and containing 5% CO2. Synthesis of Filaggrin by Human Epidermal Keratinocytes Cells were incubated with the selected ingredients or test references (1.5 mM CaCh) for 144 hours. Filaggrin production was evaluated by immunostaining. Hyaluronic Acid Secretion by Human Epidermal Keratinocytes Cells were incubated with the selected ingredients or test references (10 "7 M retinoic acid) for 72 hours. The release of hyaluronic acid by human epidermal keratinocytes in supernatants was quantified. CD44 production by Human Epidermal Keratinocytes Cells were incubated with the selected ingredients or test references (10'7 M retinoic acid) for 72 hours CD44 production by human epidermal keratinocytes was evaluated by immunostaining.

Results The results are shown in Figures 3, 4 and 5. Green coffee seemed to increase filaggrin production (Figure 3). Decaffeinated green coffee extracts Robusta and Arabica moderately increased secretion of hyaluronic acid (128% and 120% of control, respectively) (Figure 4), an in vivo skin cell secreted glycosaminoglycan that helps maintain proper hydration through attraction and water trapping in extracellular spaces. While Oryza and green coffee extracted in water increased (148% and 132% of the control, respectively) the production of CD44, the hyaluronic acid receptor (Figure 5). A stronger skin barrier ensures better body protection against environment and pathogen attack. It also limits water loss through the epidermis, thereby ensuring proper skin hydration.

Claims (14)

Cosmetic use of an effective amount of green coffee beans, or at least one extract thereof, characterized in that it is as an active agent for the preparation of an oral composition for the treatment and / or prevention of pigment disorders of the skin and / or skin pigment imperfections. Use according to claim 1, characterized in that the skin pigmentation disorders are those observed in melasma, freckles, vitiligo, piebaldism, phenylketonuria and the like and / or age points. Use according to claim 1 or 2, characterized in that it is for the improvement of skin tone and / or skin color. Use according to any one of claims 1 to 3, characterized in that it is for lightening and / or whitening skin tone. Use according to any one of claims 1 to 4, characterized in that the composition enhances skin hydration. Use according to any one of claims 1 to 5, characterized in that the composition enhances the barrier function of the skin. Use according to any one of claims 1 to 6, characterized in that the extract is derived from coffee beans selected from the species Coffea arabica, Coffea robusta, Coffea canephora or Coffea ibérica. Use according to any one of claims 1 to 7, characterized in that the coffee beans are decaffeinated. Use according to any one of claims 1 to 8, characterized in that the coffee bean extract represents from 1% to 100% of the total weight of the composition. Use according to any one of claims 1 to 9, characterized in that said composition is a food product, a beverage, a food supplement, a nutraceutical, or a medicament. Use according to any one of claims 1 to 10, characterized in that the composition further comprises at least one type of food grade microorganism. Use according to claim 11, characterized in that the microorganisms are probiotics. A non-therapeutic method for cosmetic treatment which is of use for treating and / or preventing skin pigment disorders and / or skin pigment imperfections, characterized in that it comprises at least one step of administration to an individual. , of an effective amount of green coffee beans, or at least one extract thereof. A kit for treating and / or preventing skin pigment disorders and / or skin pigment imperfections, characterized in that it comprises an oral treatment with a composition containing green coffee beans, or at least one extract thereof, combined with an oral or topical composition optionally containing a probiotic microorganism, or a moisturizing or anti-aging agent.