MX2013001078A - Use of green coffee beans for regulating skin pigmentation disorders. - Google Patents

Abstract

The present invention relates generally to the field of food supplements and/or food products for cosmetic purpose. More specifically, the present invention aims to provide an ingredient containing green coffee beans or an extract thereof for preventing and/or treating hyper-pigmentation of skin, skin color imperfections such as age-spots and other skin disorders characterized by abnormal pigments. The present invention also aims at improving skin tone as well as providing a skin lightening or whitening agent.

Description

USE OF GREEN COFFEE BEANS TO REGULATE DISORDERS OF PIGMENTATION OF THE SKIN Field of the invention The present invention relates generally to the field of food supplements and / or food products for cosmetic purposes. More specifically, the present invention focuses on providing an ingredient containing green coffee beans or an extract thereof to prevent and / or treat hyper-pigmentation of the skin, imperfections in the color of the skin such as age spots and Other dermatological disorders characterized by abnormal pigmentation. The present invention also focuses on improving skin tone as well as providing a skin whitening or lightening agent.

BACKGROUND OF THE INVENTION The color of the skin is determined mainly by the amount and type of melanin, a brown pigment present in the skin. Lower amounts of melanin result in a lighter skin color while higher amounts translate to a darker skin color. Also, hyper-pigmentation of the skin is caused by overexpression or accumulation of melanin in the skin. As a result, the pathway involved in the production of melanin has been the target of many inhibitors to reduce the levels produced. One of the main enzymes involved in the melanin pathway is tyrosinase.

Melanin synthesis is a hormone-controlled process, including melanocyte-stimulating hormone (MSH) and adrenocorticotropic hormone (ACTH) peptides that are produced from the propiomelanocortin precursor. It is stimulated by DNA damage that is caused by UVB radiation as well.

In this way, exposure to the sun over time can induce many biochemical reactions in the skin, leading to sunburns 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 non-uniform and mottled skin tone. Unfortunately, many of the commercially available products in the current market are either only marginally effective, or contain active agents that are unstable and lose their potency when incorporated into a final formula.

The ability to modify the expression of pigment content in the skin, to promote a uniform skin tone or to lighten the skin tone, is highly desired in today's society. Many people want to modify their skin tone, reduce aging spots, etc., or simply for 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 to improve the appearance of pigmentation disorders such as those observed in melasma, freckles, vitiligo, piebaldism, phenylketonuria and the like and / or for cosmetic purposes.

Likewise, the use of skin bleaching compositions has expanded widely. However, whether they destroy melanin or inhibit its training. Many of them contain aggressive chemicals such as peroxides, acids or formaldehyde, or thiolated materials. Less severe therapies have other disadvantages.

Topical retinoids and topical corticosteroids have been suggested as hypo-pigmentation agents, as are laser treatment and chemical peels, but these fall short of the desirable responses.

Other compositions suggested the use in the skin of natural materials, which in some cases have been used for centuries in Asia or Europe to whiten skin and areas of the skin, or to increase the appearance of the finished skin. These include the use of lemon, orange, cucumber, ginkgo, carob, pink fruit, geranium herb, cinnamon, sweet marjoram, rosemary, etc.

To combat disorders related to abnormal pigment or to lighten skin tone, several compounds that when applied topically to the skin are able to reduce the activity of tyrosinase and consequently limit the production of melanin, have been proposed in this way . Unfortunately, currently available treatments are not completely satisfactory, particularly in terms of the side 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 that do not have the disadvantages of those described in the prior art. In particular, it would be highly desirable to develop nutritional cosmetic compositions to be administered by oral route 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 to treat and / or prevent skin pigmentation disorders, in particular those due to environmental factors or aging.

The object of the present invention is to satisfy these needs.

BRIEF DESCRIPTION OF THE INVENTION The present inventors were able to achieve this goal by providing a food or food supplement composition comprising at least one ingredient containing green coffee beans or an extract thereof.

Thus, according to a first aspect, 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 pigmentation of the skin. These skin disorders are in particular those due to age or to environmental factors (eg, UV), such as age spots. They can also be dermatological disorders that are observed in asthma, freckles, vitiligo, piebaldism, phenylketonuria and the like.

The present inventors have discovered that green coffee beans effectively suppress melanin formation, melanogenesis, despite the fact that the extracts show little to no inhibition of tyrosinase activity. This result is surprising and unexpected considering the central role of tyrosinase in melanogenesis and the focus of the development efforts in the technique for inhibiting this enzyme.

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

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

For the purposes of the present invention, the term "prevent" is intended to mean reducing the risk of manifestation of the disorder being considered.

The present invention is also directed towards the cosmetic use of the above-mentioned ingredient, as an active agent for treating and / or preventing imperfections of skin pigmentation. As a result, the complexion becomes brighter and more homogeneous, without areas of dyschromia, or dryness.

The present invention is also directed towards 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 whitening or lightening the tone of the skin.

The present inventors have also discovered that the ingredient according to the invention further improves hydration and / or skin 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 the hydration of skin or aging of the skin, in particular as described below.

According to other of its aspects, the object of the invention is a method, in particular a cosmetic method, for treating and / or preventing imperfections in skin tone and the disorders associated with hyper-pigmentation, in particular aesthetic disorders, in a individual, comprising at least one step of administering to the individual, at least one ingredient that contains green coffee beans or an extract thereof according to the invention.

The compositions according to the present invention may be 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 distributed in particular within the dermal matrix via the bloodstream. Oral administration also has the advantage of a rapid and relatively non-restrictive mode of administration.

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

In the following text "coffee beans" should be understood as meaning the grain obtained by the wet route (fermentation, washing) or by the dry route (drying after mechanical dehulling) starting from the "cherry" of coffee, after of the dehulling as described above.

"Extract" is to be understood as meaning all the compounds obtained by starting from an alcoholic or aqueous-alcoholic extraction of a crude product. The coffee tree species selected for the preparation of the coffee bean extracts used in the compositions are suitably selected from the Coffea species.

Coffee trees are small trees with glossy leathery, perennial and smooth marginal leaves (10-15 x 4-6 cm). The fragrant and white flowers are grouped in spirals in the armpit of the leaves. The fruit is a green drupe, which turns red when ripe and normally contains two flat-convex berries that become contiguous through its flat surface. Although only two species supply the needs Essential coffee market factors (C. arabica and C. canephora), many coffee tree species exist in the wild state in the tropical forests of West Africa.

The "grain" of coffee is obtained by the wet route (fermentation, washing) or the dry route (drying, followed by mechanical dehulling) starting from the "cherry" of coffee, that is, of the drupes. The reduction to pulp eliminates the red pericarp and the fleshy mesocarp; It leads to the "husk" of coffee. It is after peeling (removal of the lignified endocarp) that the "cherry" (or grain) of coffee is obtained.

Green coffee can be derived from Arabica or Robusta, or it can be a mixture of Arabica and Robusta. The green coffee portion can be at least partially decaffeinated. This is to provide caffeine level products that can be modulated from caffeine-free to regular caffeine level.

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

The compositions according to the invention can be in any of the medical forms normally available for the selected administration method. The carrier can be of different nature depending on the type of composition under consideration. Accordingly, the composition can be any food or pharmaceutical product, or a cosmetic product for oral application. Examples of pharmaceutical foods or carriers are complete nutritional formulas, dairy products such as milk, yogurt, cheese, fermented milks, milk-based fermented products, ice cream, cereal-based products or products based on fermented cereals, milk-based powders, formulas for infants or babies, cold drinks or stable on shelf, confectionery type food products, chocolate or cereal, animal feed, in particular for domestic animals. In particular, the chicory or extract thereof can be incorporated into any other form of food supplement or enriched food, for example food sticks or compacted or non-compacted powders. The powders can be diluted in water, soda, dairy products or soybean derivatives, or incorporated into food bars.

The food product may also comprise a protein source, a carbohydrate source, a lipid source, a mineral source and / or a source of vitamins. 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 require when it is affected by skin disorders. They also allow formulating 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 bleaches and coffee cream substitutes. Alternatively, the ingredients could also be a dressing for salads or parts thereof, for example. These compositions 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 sachet, 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 produced commercially for many decades. It is produced from roasted and ground coffee in a variety of ways, all of which are well known to the person skilled in the art.

The present invention is particularly suitable for use as a soluble coffee product or any product that is based on, or derived from, a soluble coffee product. For example, the coffee product can 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 which comprise a coffee component together with a natural or artificial sweetening component, the components being optionally pre-diluted with such a liquid. like water or milk. In this case, the coffee component may comprise the coffee product of the present invention.

The three-in-one beverages, which comprise coffee, a sweetener and a bleach such as milk, a liquid cream substitute or a solid cream substitute (eg powder), can comprise the coffee product of the present invention.

In addition, any beverage comprising soluble coffee as an ingredient may comprise the coffee product of the present invention.

The composition may further comprise additional ingredients suitable for inclusion in a food composition. The usual ingredients they can be for example sugars, artificial sweeteners, emulsifiers, stabilizers, thickeners, flow agents, dyes, flavors, flavors 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 mono-diglycerides, 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.

In addition, the present invention can be used as an ingredient for standard and express coffee-based beverage preparations that will be used as a complete or individual beverage portion for home preparation.

If the product is a nutritional supplement for oral administration, it may be present in capsules, gelatin capsules, soft capsules, tablets, sugar-coated tablets, pills, pastes or pills, gums or drinkable solutions or emulsions, a syrup or a gel. This supplement may also include a sweetener, a stabilizer, an antioxidant, an additive, a flavoring agent and / or a colorant. The formulation thereof is carried out by means of the normal 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 dietary 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 dissolving products, gelling agents, thickeners, humectants, fatty and / or aqueous compounds, preservatives, texturizing agents, flavorings and / or coating, antioxidants and coloring materials normally used in food.

The composition according to the present invention may also contain lipids, polyphenols, taurine, probiotic microorganisms, vitamins and / or oligo-elements. If probiotics are used, they can be included in a living, semi-active or deactivated form, for example, as a lyophilized powder.

Culture supernatants of the microorganisms can also be included in the composition. They may be selected from the group consisting of lactic acid bacteria, in particular lactobacilli and / or bifidobacteria, and are most preferably selected from the group consisting of Lactobacillus johnsonii, LactobacHus reuteri, Lactobacillus rhamnosus, Lactobacillus paracasei, Lactobacillus casei, Bifidobacterium bifidum, Bifidobacterium breve, Bifidobacterium animáis, Bifidobacterium infantis, Bifidobacterium dolescentis and Bifidobacterium pseudocatenulatum. According to a more preferred embodiment, the strains used are Lactobacillus johnsonii (La1) deposited on June 30, 1992, under the Budapest Treaty at the Pasteur Institute and which received the deposit No. CNCM 1-1225 or Lactobacillus paracasei (ST1 ) deposited on January 12, 1999, at the Pasteur Institute in accordance with the Budapest Treaty and which received the deposit No. CNCM 1-21 16. The following compounds can be used, for example 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, the curcuminoids, niacin, lithospermic acid and adenosine. It is understood that the specialist will select these active compounds and, where possible, the will combine in such a way as to improve the expected effects of the composition which is the objective of the invention by preventing the activity of desired interest from being inhibited or attenuated.

Use The products of the invention can be used efficiently to treat or prevent skin pigmentation disorders or to cosmetically lighten the skin tone, for example, by reducing the production of melanin. In fact, extracts of green coffee beans showed in vitro reduction of melanin synthesis (example 1, figure 1). Tyrosinase production was also reduced but to a limited extent (Figure 2), suggesting that the reduction in melanin was not due to the inhibition of tyrosinase but rather to mechanisms that act up or down this enzyme.

The ingredients according to the present invention also have a positive effect in reinforcing the skin barrier and maintaining skin hydration.

As a result, pigmentation imperfections are reduced, the complexion becomes brighter and more homogeneous, without areas of dyschromia, or dryness.

Thus, according to one aspect, 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 UV.

The present invention is also directed towards the cosmetic use of an effective amount of at least one ingredient containing green coffee beans as an active agent for whitening or lightening the skin tone, 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 to improve skin hydration or aging of the skin. skin, in particular as described herein.

According to another of its aspects, the object of the invention is a method, in particular a cosmetic method, for treating and / or preventing imperfections of skin tones and / or disorders associated with hyper-pigmentation, in particular aesthetic disorders, in an individual, comprising at least one step of administering to the individual, at least one ingredient containing green coffee beans according to the invention.

The cosmetic treatment method of the invention can be carried out in particular by orally administering at least an effective amount of at least one ingredient containing green coffee beans according to the invention. The oral administration comprises ingesting, in one or more consumptions, 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 one or more, and generally for a prolonged period of at least 4, or even 1 to 15 weeks.

In addition, combinations of treatment with, optionally, oral or topical forms may be contemplated to complement or reinforce the activity of the ingredients defined by the invention.

Thus, a topical or oral treatment with a composition containing roasted coffee beans according to the invention, combined with an oral or topical composition optionally containing another active ingredient, in particular a probiotic microorganism, or other probiotics in dead form , live or semi-active or a moisturizing or anti-aging agent could be imagined as a kit. The ingredients are mixed, before they are formulated, in the order and under the conditions easily determined by those skilled in the art.

The proportion of coffee grain extract in the composition will of course be determined as a function of the desired effect and the mode of administration of the composition.

The daily doses of green coffee beans extract administered by the oral route may preferably comprise between 0.1 and 27 g / day depending on the type of product and the caffeine content, most preferably 0.5 to 18 g / day, even more preferably 1 at 3 g / day. The present inventors have found that the effectiveness of the green coffee bean extracts according to the present invention generally depends on the dose and follows a dose response curve. If slight disorders or skin damage are 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 pigmentation disorder is to be treated, larger amounts will be more adequate, although small amounts will also produce an effect.

Preferably, the composition designed for oral administration contains an extract of coffee beans 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 the product.

Advantages and additional features of the present invention are apparent from the following examples and figures. The examples here are then presented by way of non-limiting illustration of the scope of the invention. In these examples, unless otherwise indicated, the percentages are percentages by weight and the ranges of values written in the form "between ... and ..." include the specified upper and lower limits.

Brief description of the figures Figure 1: Evaluation of melanin production by murine melanocypre-treated with green coffee extracts.

Figure 2: Evaluation of tyrosinase production by murine melanocypre-treated with green coffee extracts.

Figure 3: Evaluation of filaggrin synthesis by human primary epidermal keratinocypre-treated with different green coffee extracts.

Figure 4: Evaluation of the secretion of hyaluronic acid by human primary epidermal keratinocypre-treated with green coffee extracts.

Figure 5: Production of CD44 by human epidermal keratinocypre-treated with different green coffee extracts.

EXAMPLES Example 1 Effect on skin pigmentation To evaluate the potential beneficial effect of the ingredients towards de-or pro-pigmentation of the skin, we used a 2D culture of murine melanocy(B16) and carried out 2 s: 1 - evaluation of melanin production and 2- evaluation of the production of tyrosinase. 1. Cell culture conditions B16 cells were cultured in DMEM 1 g / L glucose without phenol red supplemented with 10% fetal calf serum, in a chamber humidified at 37 ° C and containing 5% C02. 2. Melanin production by cell line of B16 kidney melanoma The cells were incubated with the selected ingredients or the references (kojic acid at 400 μg / mL) for 72 hours, in the presence or absence of NDP-MSH, an analogue of MSH. The total amount of melanin (extracellular or intracellular) was evaluated 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 the murine melanocyte cell line B16 The cells were incubated with the selected ingredients or the references (kojic acid at 400? / ???) for 48 hours. Tyrosinase production was evaluated by immunological labeling.

INGREDIENTS: We have ed extracts of green coffee of Robusta and Arabica, Svetol® (provided by Naturex) and Oryza's Extract-P and a green coffee extracted with water. The concentrations ed for each coffee extract are indicated in table 1.

Table 1 Cytotoxicity of green coffee extracts in human primary dermal fibroblasts and in human primary epidermal keratinocytes We have worked with the highest non-cytotoxic concentration, with respect to normalizing as much as possible the conditions between the different extracts in order to be able to compare them. Thus, coffee extracts have been ed at a concentration of 40 μ9 /? T ?? _.

Results The results are expressed as a percentage in relation to the control. The reference (kojic acid) induced, as expected, a reduction in the melanin content. Figure 1 shows the production of melanin by B16 melanocytreated for 72 hours with the selected ingredients.

We have observed in general that the coffee extracts had some potential for depigmentation of the skin since they were able to reduce the production of melanin and tyrosinase in vitro in comparison with the 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 towards skin barrier function and hydration of the skin was evaluated using 2D culture of human primary epidermal keratinocyand we carried out 3 s: 1-evaluation of filaggrin synthesis, 2 - evaluation of hyaluronic acid secretion and 3- evaluation of the production of CD44 (hyaluronic acid receptor) by human primary epidermal keratinocy Cell culture conditions Human epidermal keratinocytes were cultured in control medium of keratinocytes-SFM, in a chamber humidified at 37 ° C and containing 5% C02.

Synthesis of filaqrin by human epidermal keratinocytes The cells were incubated with the selected ingredients or the test references (CaCl2 at 1.5 mM) for 144 hours. Filagrin production was evaluated by immunolabeling.

Secretion of hyaluronic acid by human epidermal keratinocytes The cells were incubated with the selected ingredients or the test references (retinoic acid at 10 ~ 7 M) for 72 hours. The release of hyaluronic acid by human epidermal keratinocytes in supernatants was quantified by ELISA assay.

Production of CD44 by human epidermal keratinocytes The cells were incubated with the selected ingredients or the test references (retinoic acid at 10"7 M) for 72 hours The production of CD44 by human epidermal keratinocytes was evaluated by immunolabeling.

Results The results are shown in figures 3, 4 and 5. Green coffee appeared to increase filaggrin production (figure 3). Robusta and Arabica decaffeinated green coffee extracts moderately increased the secretion of hyaluronic acid (128% and 120% of the control respectively) (Figure 4), a glycosaminoglycan secreted by dermal cells in vivo that helps maintain adequate hydration by attracting and trapping water in the extracellular spaces. While Oryza and green coffee extracted with 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 protection of the body against the environment and the attack of pathogens. It also limits the loss of water through the epidermis, thus ensuring adequate dermal hydration.

Claims (13)

1 . Cosmetic use of an effective amount of at least green coffee beans or an extract thereof, as an active agent in the preparation of an oral composition for treating and / or preventing disorders of skin pigmentation and / or skin imperfections .

2. The use according to one of the preceding claims, wherein the disorders of the skin are those observed in melasma, freckles, vitiligo, piebaldism, phenylketonuria and the like, and / or stains by age.

3. The use according to one of the preceding claims for improving the skin tone and / or complexion of the skin.

4. The use according to one of the preceding claims for clarifying and / or whitening the skin tone.

5. The use according to one of the preceding claims, wherein the composition further improves the hydration of the skin.

6. The use according to one of the preceding claims, wherein the composition further improves the barrier function of the skin.

7. The use according to one of the preceding claims, in which the extract is derived from coffee beans selected from the Coffea arábica, Coffea robusta, Coffea canephora or Coffea ibérica species.

8. The use according to one of the preceding claims, wherein the coffee beans are decaffeinated.

9. The use according to one of the preceding claims, wherein the coffee bean extract represents from 1% to 100% of the total weight of the composition.

10. The use according to any of the preceding claims, wherein the composition is a food product, a beverage, a food supplement, a nutraceutical or a medicine.

The use according to one of the preceding claims, wherein the composition further comprises at least one type of food grade microorganisms, in particular probiotics, in dead, living or semi-active form.

12. A method of cosmetic treatment that is useful for treating and / or preventing skin pigmentation disorders and / or skin imperfections, characterized in that it comprises at least one step of administering to an individual an effective amount of at least grains of green coffee or an extract thereof.

13. A kit for treating and / or preventing skin pigmentation disorders and / or skin imperfections, characterized in that it comprises an oral treatment with a composition containing at least green coffee beans or an extract thereof, combined with an oral composition or topical optionally containing a probiotic microorganism in dead, living or semi-active form, or a moisturizing or anti-aging agent.