MX2014009188A - Use of starfruit extract as a cpt-1 modulator and compositions thereof. - Google Patents

Abstract

The present invention describes methods for improving the appearance of skin, particularly, treating, ameliorating, preventing, delaying, and/or improving one or more signs of excess accumulation and/or production of subcutaneous fat, such as cellulite, and conditions related thereto, by topically applying compositions comprising Carnitine Palmitoyl Transferase-1 (CPT-1) stimulating aqueous extract of the leaf of Averrhoa carambola, optionally with other anti-lipid agents.

Description

USE OF CARAMBOLA EXTRACT AS A CPT-1 AND MODULATOR COMPOSITIONS OF THE SAME FIELD OF THE INVENTION The present invention relates generally to compositions containing Averrhoa Carambola leaf extract (also known as carambola) for topical application to the skin that modulate the expression of Carnitine Palmitoyl Transferase-1 (CPT-1). The compositions of the present invention comprise at least one anti-lipid agent and provide benefits to the skin, in particular, by improving the condition and appearance of the skin affected by cellulite. More particularly, the compositions of the present invention comprise an aqueous carambola extract that stimulates the expression of CPT-1, an enzyme important for the oxidation of fat.

BACKGROUND OF THE INVENTION Consumers continually seek to improve the appearance of their skin, and in particular, seek to improve the appearance of the skin affected by unwanted deposition and / or accumulation of fat, including cellulite. There is active interest in the cosmetics industry to develop products that can be applied topically to the skin and provide anti-cellulite and anti-adiposity benefits, as well as other anti-lipid benefits. Cosmetic products that improve the appearance of the skin are increasingly demand as well as consumers who seek incrementally to mitigate and delay the signs of excess accumulation and / or production of subcutaneous fat.

Cellulite is the non-uniform, lumpy type of subcutaneous fat that tends to accumulate in the buttocks, thighs and extremities of many women. It is considered unpleasant because it gives the tissues that involve the skin an "orange peel" or "cottage cheese" appearance. The compression of the skin, as when sitting or crossing the legs, produces a "mattress appearance" with bulges and bites of the fatty layer. Fat nodules can feel trapped inside the hardened connective tissue. The histology of the skin affected by cellulitis indicates that cellulitis results from a combination of enlarged fatty tissue and weak dermal structure and connective tissue septa. The accumulation of excess fat increases the volume of adipocytes, which bulge in a weakened dermis to create the characteristic irregularities in the appearance of the epidermal surface. A number of factors can cause cellulite, including, for example, hereditary, intestinal, circulatory, lymphatic, hormonal and lifestyle factors. The diet to reduce fat intake, exercise to increase fat metabolism and prevent the accumulation of cellulite, and a massage and hydrotherapy to stimulate drainage lymphatic can help reduce the appearance of cellulite. However, these means to combat cellulite or subcutaneous fat are limited, and the need remains for additional procedures.

There is a need in the art for compositions and methods to improve the appearance of the skin, including the treatment, control, handling, amelioration, prevention, inhibition, retardation and / or reduction of excess accumulation and / or production of subcutaneous fat, including cellulite, acne and / or oily skin.

Therefore, it is an object of the invention to provide new ingredients to treat, ameliorate, prevent, inhibit, retard and / or reduce the signs of excess accumulation and / or production of subcutaneous fat. The novel methods and compositions, as well as their mode (s) of action, are described herein to treat conditions related to the accumulation of fat and / or the production of subcutaneous fat, including cellulite, as well as formulations for the skin that they comprise the same, and other personal care products for the skin.

The above discussion is presented only to provide a better understanding of the nature of the problems confronted in the art and should not be considered in any way as an admission as to the prior art, nor should the citation of any reference in the present is considered as an admission that such a reference constitutes the "prior art" for the present application.

BRIEF DESCRIPTION OF THE INVENTION The protuberance of fatty tissue enlarged in the dermis is one of the major factors that contribute to the appearance of cellulite. One of the procedures to improve cellulite is to stimulate the breakdown of fats and reduce the amount of fat and / or lipids in adipocytes, or fat cells. Carnitine Palmitoyl Transferase-1 (CPT-1) is a mitochondrial enzyme that catalyzes the conjugation of carnitine to fatty acids, which is the limiting stage of the oxidation rate of fatty acid (decomposition of fatty acid). Without wishing it to be limited by theory, it is believed that an increase in the expression of CPT-1 leads to a reduction in lipid accumulation in fat cells, which in turn decreases the size of the adipose tissue and helps to improve the appearance of the skin affected by cellulite.

Prior to this invention, it was not known that a stimulator of CPT-1 expression could reduce the accumulation of lipid in fat cells. Surprisingly, it was discovered that aqueous extracts of the leaf of Averrhoa carambola (also known as "carambola" afterwards in the present used interchangeably) stimulate CPT-1 expression and lead to the accumulation of reduced lipid in fat cells. In particular, compositions comprising aqueous extracts of the Averrhoa carambola leaf have surprisingly been found to reduce fat accumulation and adipocyte differentiation, offering combined mechanisms of action to combat undesired subcutaneous fat, and in particular cellulite. . In addition, carambola extract may be beneficial in treating other skin conditions characterized by excess lipids, eg, acne or oily skin.

The Averrhoa carambola, also known as Carambola, is a species of woody plant in the family Oxalidaceae. This evergreen tree is native to Southeast Asia and the subcontinent of India. The Averrhoa carambola is a small tree or shrub, with flowers from pink to red-purple. The flowers are small and bell-shaped, with five petals that have whitish edges. Flowers often occur in the year under tropical conditions. The tree is grown in tropical and semitropical regions for its edible fruits and medicinal uses.

While the leaf extract of Averrhoa carambola has been described in the treatment of wrinkles (JP 2003/3009893, JP 2002/226323, and JP 2003/055244), and also in Inhibition of testosterone 5-a-reductase (JP 2002 / 241296A), the extract of Averrhoa carambola has never been described to combat unwanted subcutaneous fat and / or cellulitis.

In one aspect of the invention, the cosmetic compositions (or personal care products) are provided to improve the appearance of the skin comprising a Carnitine Palmitoyl Transferase-1 (CPT-1) stimulator in a cosmetically acceptable vehicle in an amount effective to decrease adipocyte differentiation and / or intracellular triglyceride production and / or accumulation in adipocytes in the area of the skin. In some embodiments, the CPT-1 stimulator is an extract of Averrhoa carambola, in particular, an extract. watery leaves, stems, and flowers (or combinations thereof) of the plant. In one aspect of the invention, the CPT-1 stimulator is an aqueous extract of Averrhoa carambola leaves and stimulates the expression of the CPT-1 gene.

In some embodiments of the invention, methods are provided for treating a condition of the skin characterized by excess lipids, oily skin and / or oily scalp, comprising topically applying to skin in need thereof an effective amount of an extract. aqueous stimulation of CPT-1 from Averrhoa carambola leaf in a cosmetically acceptable vehicle for a sufficient time to improve the appearance of the skin.

In some embodiments, the cosmetic composition further comprises at least one other anti-lipid agent, the anti-lipid agent which is selected from the group consisting of a phosphodiesterase inhibitor, an adenylate cyclase activator, a lipolysis stimulator, an beta-adrenergic receptor, an alpha-2-adrenergic receptor antagonist, a xanthine analogue, forskolin, an extract of forskohlii, an extract of hawthorn, an extract of cola, isoproterenol, yohimbine, Ginkgo biloba extract, oil of goatee , caffeine, a collagen stimulator, an elastin stimulator, carnitine, creatine, and combinations thereof.

In another aspect, the invention relates to methods for improving the appearance of the skin affected by undesired subcutaneous fat, such as cellulite, which comprises applying topically to the skin a cosmetic composition comprising one or more modulators of CPT-1 in a vehicle. cosmetically acceptable in an amount effective to decrease adipocyte differentiation and / or intracellular triglyceride production and / or accumulation in adipocytes in the area of the skin. In some embodiments, the CPT-1 stimulator is an extract of Averrhoa carambola, in particular, an aqueous extract and / or ethanol from the leaves, stems and flowers of the plant, particularly the leaves. For example, an effective amount of Averrhoa carambola extract in a cosmetically acceptable vehicle can be applied to the skin for a sufficient length of time to improve the appearance of the skin.

In some embodiments, the composition is applied to the cellulite found in at least one of the region of the thigh, buttocks, abdomen, hip or arm upper arm. In some embodiments, the composition is left in the application area, for example, as a composition left over. In some embodiments, the composition is applied in accordance with a treatment regimen, such as at least one application once a day for a period of at least 4 weeks. In some embodiments, the treatment regimen comprises at least one application once a day for a period of at least 2 weeks. In particular embodiments, methods are provided wherein sufficient time to improve the appearance of the skin comprises a period of at least 2 weeks, and wherein the aqueous extract is applied at least once a day. In other modalities, the composition is applied two or three times a day.

A method is also provided to reduce the re-occurrence of cellulite in an area previously affected by cellulite, which comprises applying topically to the same an effective amount of an aqueous extract of stimulation of CPT-1 from the leaf of Averrhoa carambola in a cosmetically acceptable vehicle.

Yet another aspect relates to methods for reducing the deposition of unwanted fat comprising topically applying to an area affected by the deposition of unwanted fat and / or accumulating an effective amount of an aqueous extract of CPT-1 stimulation of the Averrhoa leaf. carambola in a cosmetically acceptable vehicle, for a sufficient time to reduce unwanted fat.

Another embodiment of the invention provides a personal care or cosmetic composition for treating a condition of the skin characterized by excess lipids comprising an effective amount of an aqueous stimulation extract of CPT-1 from the leaf of Averrhoa carambola in a vehicle cosmetically acceptable Another embodiment of the invention provides compositions for treating a condition of the skin characterized by excess lipids, comprising an effective amount of an aqueous stimulation extract of CPT-1 from the leaf of Averrhoa carambola in a cosmetically acceptable vehicle, wherein the Aqueous extract has an HPLC analysis according to Figure 1.

Another embodiment of the invention provides compositions for treating a skin condition characterized by excess lipids, comprising an effective amount of an aqueous stimulation extract of CPT-1 from the Averrhoa carambola leaf in a cosmetically acceptable vehicle, wherein the aqueous extract comprises less than 0.1% by weight of phenolic compounds and by at least 20% by weight of carbohydrates.

These and other aspects of the present invention will be better understood by reference to the following detailed description.

- BRIEF DESCRIPTION OF THE DRAWINGS Figure 1 shows an HPLC analysis of a leaf extract of Averrhoa carambola that stimulates CPT-1 according to the invention.

Figure 2 shows an HPLC analysis of a leaf extract of Averrhoa carambola which down-regulates CPT-1.

DETAILED DESCRIPTION It has surprisingly been found that compositions comprising one or more substances that stimulate the expression of Carnitine Palmitoyl Transferase-1 (CPT-1) remarkably improve the appearance of the skin affected by the deposition of unwanted fat and / or accumulation, including skin affected by cellulite, when applied topically to it. In particular, cosmetic compositions comprising extracts, of p Preference aqueous extracts, from Averrhoa carambola can be used in such methods to improve the appearance of the skin affected by cellulite, as well as reduce the re-occurrence of cellulite in the area previously affected and / or to reduce obesity in areas affected by the accumulation of unwanted fat and / or deposition.

Extracts and Stimulation Compositions of CPT-1 One aspect of the present invention relates to compositions for topical application comprising carambola extracts that stimulate CPT-1 to treat, ameliorate, inhibit, retard, reduce the incidence or risk of, and / or reduce signs of excess accumulation and / or production of subcutaneous fat. Improving the appearance of the skin affected by cellulite and / or combating the signs of unwanted subcutaneous fat may include, without limitation, one or more of the following: (a) reduction in the appearance of bulging and / or non-uniformity of cellulite; (b) reduction in the appearance of cellulite bites in compression; (c) reduction in the degree of area affected by cellulitis; (d) prevention or delay in the recurrence of cellulitis; (e) acne prevention or treatment; (f) prevention or treatment of oily skin; (g) reduction in subcutaneous fat deposition and / or accumulation; (h) improvement in collagen deposition; and (i) improvement in connective tissue resistance.

The improvements can be measured by methods known in the art, including, for example, by consumer panel testing. Methods for improving the appearance of the skin according to the invention include the reduction of the appearance of cellulite on the affected skin in this way. The methods according to the invention may also include the improvement of the smoothness or skin tone affected by cellulitis. In practice, the compositions of the invention are applied to the skin in need of treatment, i.e., the skin suffering from a deficiency or loss in any of the above skin attributes or which would otherwise benefit from improvement in the skin. any of the above skin attributes.

A "CPT-l stimulator" refers to any agent that decreases the level of triglycerides in human adipocytes via one or more routes mediated by CPT-1. In some embodiments, the CPT-1 stimulator reduces triglycerides in the serum. The decrease in the levels of triglyceride can refer to a decrease in adipocyte proliferation and / or differentiation and / or production of intracellular lipid and / or triglyceride, storage, and / or accumulation in adipocytes, and an increase in oxidation and / or degradation and / or lipolysis of the fatty acid; and / or the reduced expression of lipogenic genes, in vitro or in vivo, and can be measured by any means known in the art, or as described herein. For example, the CPT-1 stimulation carambola extract can act to decrease triglyceride production within human adipocytes (see, for example, Example 1 below), or the CPT-1 stimulation carambola extract can act to lower triglycerides in the serum. In some embodiments, the triglyceride levels are decreased by at least about 30%, at least about 40%, at least about 50%, at least about 60%, at least about 70%, at least about 75 %, or at least approximately 100%, compared to the triglyceride level in the absence of the carambola extract. As another example, stimulation of CPT-1 can also be measured directly, for example, by measuring an increase in expression of the CPT-1 gene, where the CPT-1 stimulator acts to increase the expression of the CPT-1 gene within of human adipocytes. See, for example, Example 2 below. In some embodiments, expression of the CPT-1 gene is increased by at least about 10%, at least about 20%, at least about 25%, at least about 30%, at least about 35%, at least about 40%, at least about 50%, or at least about 100%, compared to the expression level of the CPT-1 gene in the absence of the CPT-1 stimulation carambola extract.

It is understood that a CPT-1 stimulator can give rise to an effective decrease in triglyceride levels by any means, for example, by increasing the transcribed CPT-1 mRNA and / or by increasing the expressed CPT-1 protein and / or by decreasing the post-translational processing of the CPT-1 protein in adipocytes. Activation mechanisms can include up-regulation of a CPT-1 agonist; Down-regulation of a CPT-1 antagonist; the increase in the stability of CPT-1 RNA and / or protein, and / or the increase in the dimerization of CPT-1 with ligands that affect the activation of CPT-1. The CPT-1 stimulator can refer to an extract, for example, an extract of Averrhoa carambola, which contains a number of active compounds, one or more of which modulate CPT-1. In a preferred embodiment, the CPT-1 stimulator is a carambola extract and increases the amount of the CPT-1 protein.

In preferred embodiments, the CPT-1 stimulator is an extract of Averrhoa carambola (carambola), more particularly an aqueous extract. The carambola Averrhoa is also known as Carambola and by the common name of "carambola". The Averrhoa carambola is a species of woody plant in the family Oxalidaceae. It originates from the Philippines, where it is called "balimbing" or "saranate", depending on its acidity. Another common name is "belimbing" (Indonesia, Malaysia, India and Sri Lanka). The tree and its fruit are popular throughout Southeast Asia, the South Pacific, parts of East Asia and are also cultivated throughout the tropics, such as Costa Rica, Peru, Colombia, Trinidad, Ecuador, Guyana, Republic Dominican Republic and Brazil, and in the United States, in South Florida and in Hawaii. Averrhoa carambola is a small tree or shrub, with pink to red-purple flowers. The flowers are small and bell-shaped, with five petals that have whitish edges. Flowers often occur throughout the year under tropical conditions. The tree is grown in tropical and semi-tropical regions for its edible fruits and medicinal uses. Averrhoa carambola is believed to be rich in antioxidants and vitamin C and low in sugar, sodium and acids. It is also a potent source of both primary and secondary polyphenolic antioxidants. Averrhoa carambola has both antioxidant activities and Antimicrobial: the purification of NO by the extract of the fruit is dependent on the concentration and the stage of maturation. The extracts have antimicrobial activity against E. coli, Salmonella typhi, Staphylococcus aureus and Bacillus cereus.

For use in the compositions of this disclosure, the plant, plant components, and / or active ingredients are preferably derived directly from the plant. The components may be in a pure form, a semi-pure form, or unpurified form. In preferred embodiments, the Averrhoa carambola extract comprises an aqueous, alcoholic, or hydroalcoholic extract. In more preferred embodiments, the components are in the form of an extract obtained by extraction with polar solvent, such as by using aqueous extraction.

The solvent extraction includes collecting the raw materials of the plant containing the desired constituent (s), particularly those above ground, such as leaves, stems, flowers, bark, and the like. These plant materials are ground to small particle sizes, and then placed in an extraction machine through an entry for raw materials by a free-loading machine. The raw material of the plant is pushed into the extraction machine by means of a propeller, and slowly moves the raw material of the plant forward. The solvent can be added to the machine through a solvent inlet at the top of a waste discharge outlet. Due to the difference in gravity and balance, the solvent flows into the raw material inlet, soaks the materials, and flows out the opposite side of the solvent inlet. Since the materials of the plant and the solvent move in opposite directions to each other, the materials of the plant are constantly submerged in a solution containing a low concentration of extract. As a result of the equilibrium, high performance of the constituent (s) of the plant can be achieved by continuously extracting the material from the plant against the low concentration solution. The concentration of the plant material in a solvent extraction can be from about 5 g / L to about 50 g / L, preferably from about 10 g / L to about 30 g / L, much more preferably at least 20 g / L. g / L.

The extraction time can be adapted to remove the constituents of the plant, for example between approximately 1-8 hours is typical, more preferably that is between approximately 2-6 hours, and much more preferably which is between approximately 3-5 hours. hours. The extraction temperature can be chosen according to the solvent and the extraction method that is used, but it can be between about 20 ° C to about 90 ° C (including extraction at room temperature), between about 40 ° C to about 70 ° C, or between about 50 ° C to about 60 ° C. The collected extract is then finely filtered to remove the debris, and can be used directly, or it can be concentrated, for example, by distillation of the solvent, by lyophilization, or by any other conventional process. The extract can also be provided in powder form by removing substantially all of the solvent.

Briefly, a polar or aqueous solvent extraction method involves washing and extracting the material from the plant using water, an aqueous solution, or another polar solvent. Non-limiting examples of polar solvents include, but are not limited to, water; alcohols (such as methanol, ethanol, propanol, butanol and the like); glycols; ethers (such as diethyl ether, dipropyl ether, and the like); esters (such as butyl acetate, ethyl acetate, and the like); ketones (such as acetone, methyl ethyl ketone, and the like); organic acids including acetic acid, and the like; dimethyl sulfoxide; acetonitrile; other organic solvents; and combinations thereof. Other suitable solvents include physiological saline, solution phosphoric acid buffer and phosphate buffer saline solution and the like. In some preferred embodiments, water is used as the polar solvent. Methods well known in the art can be used for extraction with polar solvent.

Similarly, an organic solvent extraction method involves washing and extracting the plant material using an organic solvent. Non-limiting examples of organic solvents include methanol, ethanol, isopropanol, dichloromethane, chloroform, hexane, xylene, and petroleum ether. Methods well known in the art can be used for extraction with organic solvent.

In some embodiments, extraction comprises aqueous-organic extraction. Generally, extraction with aqueous-organic solvent initially involves collecting raw materials from parts of the plant, particularly parts above the ground, such as leaves, stems, flowers, bark, and the like, which are milled into small particle sizes. . The milled plant material is soaked in aqueous solution that is acidic or alkaline, depending on the solubility and stability of the desired extract under acidic or alkaline (basic) conditions. For extraction under acidic conditions, an acid, such as hydrochloric acid or sulfuric acid is added to water, for example, at a concentration of about 3% (w / v).

For extraction under alkaline conditions, an alkali such as sodium hydroxide or sodium carbonate is added to the water. The extraction time and the extraction temperature are typically similar to those used in the organic solvent extraction method described above.

The extract is then collected and finely filtered to remove the debris. Alkaline agents (eg, ammonia) or acidifying agents (eg, sulfuric acid) can be added to the extract to neutralize the solution by adjusting the pH, depending on the acidity or alkalinity of the extract collected. The aqueous extract can be used directly, concentrated or dried. Alternatively, the organic solvent may be added to the neutralized solution to transfer the active ingredients from an aqueous phase to an organic phase. Examples of such organic solvents include, but are not limited to, ethanol, isopropanol, butanol, pentanol, hexanol, and xylene. The extract comprising the transferred extract assets dissolved in the organic solvent can be used directly, used as a concentrate, or dried.

Different plants that contain different constituents can be mixed and extracted with one another. This mixed extraction process is preferably used if two or more plants containing constituents having similar solubility in the solvent used are extracted. extraction, such as ethanol. The mixture of extracts can be concentrated and stored in an appropriate solvent.

In some modalities, the extract is obtained from the leaves, stems and flowers of the plants of Averrhoa carambola. In some preferred embodiments, the extracts are obtained by drying the plant material and by subsequently extracting the dried plant using a solvent, for example, a polar solvent can be used. Suitable polar solvents include, but are not limited to, water; alcohols (such as methanol, ethanol, propanol, butanol and the like); glycols; ethers (such as diethyl ether, dipropyl ether, and the like); esters (such as butyl acetate, ethyl acetate, and the like); ketones (such as acetone, methyl ethyl ketone, and the like); organic acids including acetic acid, and the like; dimethyl sulfoxide; acetonitrile; other organic solvents; and combinations thereof. Other suitable solvents include physiological saline, phosphoric acid buffer and phosphate buffer saline and the like. In some preferred embodiments, ethanol and / or water is used as the polar solvent.

Preferably, the extract of Averrhoa carambola is obtained by extracting leaves, flowers, stems of Averrhoa carambola with water, ethanol, or a mixture thereof. The solvent systems optionally may comprise from about 10 volume% to about 90 volume% ethanol, and from about 10 volume% to about 90 volume% water; from about 25% by volume to about 75% by volume of ethanol and from about 25% by volume to about 75% by volume of water; from about 45% by volume to about 55% by volume of ethanol and from about 45% by volume to about 55% by volume of water; or with a 50:50 (by volume) mixture of ethanol and water.

Preferably, the extract of Averrhoa carambola is obtained by solubilizing the leaves of Averrhoa carambola powder, followed by enzymatic hydrolysis (for example, by a carbohydrase). Enzyme activity can be inactivated by heat treatment. A preferred adjuvant is added to remove the phenolic compounds, so that the amount of phenolic compounds is less than 2%, less than 1%, or much more preferably less than 0.1% of the dry weight of the final carambola Averrhoa extract. The resulting caraway extract Averrhoa preferably contains a total sugar content between about 20% and 64% based on the weight of the dry matter, preferably at least 20% total sugar content with respect to the weight of the material dry Alternatively, the total sugar content is about 3.2 g / L to about 36 g / L, preferably between about 8 g / L and about 16 g / L, compared to the volume of the resulting active extract. Other preferred characteristics of the Averrhoa carambola extract are: dry matter of between about 10 and about 90 g / L, preferably between about 25 and about 40 g / L; a pH of between about 3.0 and about 5.0, preferably between about 3.0 and about 4.0; protein content of about 8.3 to about 23% by weight of the dry matter; a crude ash content of about 22.5 to about 39% by weight percent of the dry matter in the extract; and uronic acid from about 5 to about 17% by weight of the dry matter in the extract. The particularly preferred caramel leaf extracts according to the invention have at least 20% carbohydrates by weight and no polyphenol compounds, or substantially undetectable polyphenol compounds.

Additional suitable extraction processes are described in PCT Publications WO 03/079816 (which describes a process for the preparation of tomato extracts), WO 04/014404 (which describes a process for the preparation of an extract of Echinacea angustifolia) and WO 04/014958 (describing the extraction of a polysaccharide from the roots of Echinacea angustifolia), all of which are incorporated herein by reference in their entirety.

In other embodiments, the carambole Averrhoa extract, as referred to herein, includes "synthetic" extracts, ie, where various combinations of known plant components and / or constituents combine to substantially mimic the composition and / or activity of an extract of plant of natural origin. Such synthetic extracts are included in the terms "extract" or "plant extract". The synthetic extracts will have two or more, three or more, four or more active ingredients in common with a natural plant. Much more preferably, the synthetic extracts will have substantially the same number of active ingredients as a natural extract of the plant. The correspondence of the numerical incidence of active ingredients between the synthetic extracts and the extract of plant or natural plant can be described in terms of "percent of commonality". Preferably, the synthetic extract has approximately 50% or more commonality to the chemical composition of a plant extract or natural plant. In other words, the synthetic extract has approximately 50% more of the active ingredients found in the plant or a natural plant extract. More preferably, the chemical composition of the synthetic extract has approximately 70% or more commonality to the composition chemistry of a plant or a natural plant extract. Optimally, a synthetic extract has approximately 90% or more commonality to the chemical composition of a plant or a natural plant extract. The plant or natural plant extract for comparison is derived, for example, from the Averrhoa carambola plant, for example, as described herein.

The Averrhoa carambola plant may be in any form that includes, but is not limited to, the entire plant, a dried plant, a ground plant, or parts thereof, including, but not limited to, seeds, needles, leaves, roots, bark, cones, stems, rhizomes, callus cells, protoplasts, organs and organ systems, and meristems, an extract, a dry extract, a synthetic extract or components and / or constituents found in, or isolated from, the plant and / or portions of the plant, or extracts derived either directly or synthetically from the plant, or any combination thereof.

Substances found in some extracts of Averrhoa carambola include abscisic acid derivatives and abscisic alcohol, vomifolol, roseoside, epicatechin, 2,5-dimethoxy-3-undecylphenol and 5-methoxy-3-undecylphenol, 5-O-methylembelain, and 2-dehydroxy-5-0-methylenembene, among others (Araho, D. et al., Nat. Med. 59: 113-16, 2005; Xu et al., 2004; Chakthong, et al. Chínese Chem. Lett 21 (9): 1094-96, 2010, D.C. Guna Ardena, Proc. Peradeniya Univ. Res. Sessions, 2007). Some embodiments may include one or more of these substances, while others may be free, or substantially free, of one or more of these substances.

The cosmetic compositions of the present invention generally comprise an amount of a CPT-1 stimulator, for example, an amount of Averrhoa carambola extract, effective to improve the appearance of human skin in an area to which it is applied topically. In preferred embodiments, the compositions comprise an effective amount of carambola extract to decrease adipocyte differentiation and / or intracellular triglyceride production and / or accumulation of adipocytes in the skin area.

In certain preferred embodiments, the cosmetic composition comprises an amount of carambola extract of about 0.001% by weight to about 50% by weight based on the total weight of the composition; preferably from about 0.01% by weight to about 25% by weight based on the total weight of the composition; more preferably from about 0.1% by weight to about 10% by weight based on the total weight of the composition, and even more preferably from about 0.1% by weight to about 1% by weight, or about 0.5% by weight, in basis to weight total of the composition. In one embodiment, a cosmetic composition comprises an amount of carambola extract of about 0.01% by weight to about 5% by weight based on the total weight of the composition. The above amounts refer to an "active amount" of a CPT-1 stimulator, such as the amount of carambola extract or Averrhoa carambola extract. The term "active amount" refers to the amount of starch equivalent to the concentration of absent dry solvent, solvent, carrier, filler or the like. The cosmetic compositions described herein find use as anti-lipid agents, for example, as detailed below.

Cosmetic Use of CPT-1 Modulation Compositions Another aspect of the present invention relates to the cosmetic use of compositions comprising a CPT-1 stimulator, particularly an aqueous carambola extract, where the carambola extract stimulates the expression of CPT. -1. Such compositions act to lessen, inhibit, retard, reduce, and / or improve the signs of excess accumulation and / or production of subcutaneous fat, and therefore find use as potent anti-lipid products, and, in particular, anti-aging products. -cellulitis.

An "anti-lipid" agent or product, as used herein, refers to any substance that acts to decrease triglyceride levels in adipocytes, such as by giving rise to one or more of a decrease in adipocyte proliferation and / or adipocyte differentiation; a decrease in the production of intracellular lipid and / or triglyceride, storage, and / or accumulation, an increase in the oxidation, degradation and / or lipolysis of fatty acid; and / or reduced expression of lipogenic genes, in vi tro or in vivo. An "anti-cellulite" agent is the product, as used herein, is a substance that exerts anti-lipid effects to produce a visible or palpable improvement in the skin affected by cellulite.

In some embodiments, a method is provided for improving the appearance of the skin affected by the production of subcutaneous fat and / or accumulation, such as in the case of cellulitis, where the method comprises applying topically to the affected skin at least one stimulator. of CPT-1 such as carambola extract, in a cosmetically acceptable vehicle. The composition will comprise an effective amount of the substance. An "effective amount" or an "effective amount" to improve the appearance of the skin refers to the active amount of a CPT-1 stimulator such as a sufficient carambole extract to produce a visible improvement in the skin affected by the fat. undesired subcutaneous when applied to the skin for a sufficient time. Such improvements include, without limitation, the following: (a) reduction in the appearance of bulging and / or non-uniformity of cellulite; (b) reduction in the appearance of cellulite bites in compression; (c) reduction in the degree of area affected by cellulite; (d) prevention or delay in the recurrence of cellulitis / (e) acne prevention or treatment; (f) prevention or treatment of oily skin; (g) reduction in subcutaneous fat deposition and / or accumulation; (h) improvement in collagen deposition; and / or (i) improvement in connective tissue resistance.

The compositions of the invention can be applied to the skin in need of treatment, such as the skin suffering from a deficiency or loss in any of the above attributes or that would otherwise benefit from the anti-lipid effects of the composition, for example, as described herein. For example, the CPT-1 stimulator, such as an aqueous leaf extract of Averrhoa carambola, can be provided in a cosmetically acceptable vehicle, topically applied to an area of the skin, and to remain in the area in an effective amount to treat and / or prevent an undesired skin characteristic or condition, and / or to improve the aesthetic appearance of the skin. Topical application facilitates the targeted delivery of the active components, for example, without the requirement of an injection or the expert ability of a health professional. While topical compositions are a preferred embodiment according to the invention, oral formulations are also contemplated.

"Treatment" as used herein, as well as related terms such as "treating" or "treating", refers to eradicating, reducing, ameliorating, or reversing one or more of the undesired characteristics associated with the condition of the skin that is treated, such that the consumer perceives an improvement in the appearance of the skin or other treatment benefit with respect to the condition. "Prevention" as used herein, as well as related terms, such as "preventing" or "preventing", refers to providing the skin not yet affected by the condition with a benefit that serves to prevent, retard, anticipate, minimize or reduce the recurrence of one or more unwanted characteristics associated with the condition of the skin that is prevented. Such preventive benefits include, for example, the retardation of the development and / or recurrence of the condition, or the reduction of the duration, severity, or intensity of one or more undesired characteristics associated with the condition if it develops eventually.

Methods of Use of the Proposals The cosmetic compositions taught herein, according to the methods of the invention, can be applied to an area of the skin affected by cellulite to improve the appearance of the skin. An improvement may involve a reduction in the appearance of bulging and / or non-uniformity, characteristic of cellulite, preferably reducing what is known as the "cottage cheese" or "orange peel" appearance. In addition, areas of cellulite tend to bulge, prick and curl when squeezed or compressed, such as when legs are crossed when sitting, which can worsen the appearance of cellulite areas. In some modalities, an improvement involves a reduction in this appearance of cellulite bites in the compression, so that the appearance of cellulite in the legs appears even when sitting cross-legged. An improvement may also involve the reduction of the depth and / or visible intensity of cellulite.

Cellulite tends to accumulate in certain regions of the body, for example, in the thighs and buttocks of many women, as well as in the abdomen, hip and / or region of the body. upper arm. In some modalities, the degree of the area affected by cellulite is reduced, such that the smaller areas of the thigh, buttocks, abdomen, hip and / or the region of the upper arm remain visibly affected. In preferred embodiments, one or more of such regions becomes free of visible signs of cellulitis after treatment with a composition described herein.

In some embodiments, a method is provided to reduce the re-occurrence of cellulite in an area that was previously affected by cellulite, but that shows little or no signs of cellulite. The reduction of the re-occurrence refers to the delay of the recurrence of any cellulitis on a previously affected area, or the reduction of the degree of cellulite that re-appears in the area, such that any recurrent cellulitis is less noticeable than the previous amounts .

The compositions for use in the method of the present invention will comprise a CPT-1 stimulator, such as carambola extract, in an amount sufficient to reduce intracellular triglyceride levels in adipocytes in a given area of the skin when applies topically to it. As used herein, the reduction of triglyceride level and related expressions refers to a decrease in adipocyte differentiation and / or triglyceride production intracellular, storage, and / or accumulation in the adipocytes, and / or an increase in the oxidation of fatty acid; and / or the reduced expression of lipogenic genes, in vitro or in vivo, to decrease the triglyceride content in an area of the skin, preferably the improvement of the appearance of the skin to a discernible degree. For example, in some embodiments, the level of triglycerides is decreased by at least about 30%, at least about 40%, at least about 50%, at least about 60%, at least about 70%, so less about 75%, or at least about 100%, compared to the triglyceride level in the absence of the CPT-1 stimulation carambola extract. Triglyceride levels in subcutaneous adipocytes can be determined by appropriate assays, eg, in vitro assays described herein or known in the art. For example, Example 1 below provides experimental details of assays for measuring intracellular triglyceride levels in human adipocytes.

While not wishing to be bound by theory, the compositions described herein act by a number of mechanisms of action to effect improvement in the appearance of the skin affected by the undesired subcutaneous fat. The compositions comprising carambola extracts act as stimulators of CPT-1. The enzyme Carnitine Palmitoyl Transferase-1 (CPT-1), also known as carnitine acyl transferase I, or CAT-1, is a mitochondrial enzyme. That is part of a family of enzymes called carnitine acyltransferases. Three isoforms of CPT-1 are currently known: CPT1A, CPT1B and CPT1C. CPT-1 is associated with the outer mitochondrial membrane and mediates the transport of long-chain fatty acids through the membrane by binding them to carnitine. Its role in fatty acid metabolism makes CPT-1 important in many metabolic disorders such as type 2 diabetes and insulin resistance. Such diseases, along with many other health problems, cause levels of free fatty acid (FFA) in humans to become elevated, fat accumulates in skeletal muscle, and a decrease in the ability of muscles to oxidize fatty acids . CPT-1 has been implicated in playing a critical role in these symptoms. Its importance in fatty acid metabolism makes CPT-1 a potentially useful enzyme to focus on the development of treatments for many other metabolic disorders, too. The stimulation carambola extract of CPT-1 can act to break down fat deposits, even in mature fat cells. In addition, this extract may be beneficial in treating other conditions of the skin characterized by excess lipids, for example, acne or oily skin.

In this way, without wishing to be limited by theory, the compositions described herein may act to combat the signs of cellulitis via a mechanism of action. The stimulation carambola extracts of CPT-1 work to decrease the deposition of subcutaneous fat and / or accumulation and / or decrease of adipocyte differentiation. CPT-1 is a marker of adipocyte differentiation, and acts to reduce the differentiation of adipocytes. A stronger dermal structure reduces the likelihood of "globularization" of fat nodules between connective tissue fibers or septa, which are thought to lead to the unpleasant appearance characteristic of cellulite. In addition, lower levels of subcutaneous fat also reduce the likelihood of such globularity. As cellulite is believed to result from a combination of enlarged fat tissue and weak dermal structure, combating cellulite through multiple procedures, as described herein, may provide superior results with products that use only one procedure . Accordingly, the invention provides novel mechanisms of action to improve the appearance of cellulite, and thus potent anti-cellulite compositions for use herein.

In some embodiments, cosmetic compositions to combat signs of undesired subcutaneous fat in addition, they comprise additional anti-lipid agents. For example, the cosmetic composition comprising a CPT-1 stimulation carambola extract in an effective amount (or effective amounts) to improve the appearance of the skin further comprise at least one anti-lipid agent, including another agent anti-cellulitis It is contemplated that synergistic improvements can be obtained with such combinations, in some modalities.

Exemplary anti-cellulitis agents include, without limitation, phosphodiesterase inhibitors, such as xanthine analogues, caffeine, aminophylline and theophylline; adenylate cyclase activators, such as forskolin and Coleus forskohlii extract; lipolysis stimulators, such as hawthorne extract and cola extract; beta-adrenergic receptor agonists, such as isoproterenol; alpha-2-adrenergic antagonists, such as yohimbine and Ginkgo biloba extract; knob oil (see, for example, US 7,410,658); carnitine and / or creatine (see, for example, US 2007/0264205 entitled "Cosmetic Composition having Carnitine Creatine and Methods for Using", incorporated herein by reference in its entirety). In some embodiments, additional assets include a collagen stimulator and / or an elastin stimulator, for example, a substance that stimulates the production of elastin, and / or a glycosaminoglycan. Examples of collagen, elastin and glycosaminoglycan improvers include, for example, fennel extract, carrot extract, and alfalfa extract. In some embodiments, additional assets include a collagenase inhibitor and / or elastase inhibitor. In some embodiments, the invention relates to the synergistic action of one or more compositions described herein with knob oil, for example, to provide enhanced anti-cellulite benefits to the skin.

In some embodiments, the cosmetic compositions further comprise at least one collagen and / or elastin stimulator. Such collagen or elastin stimulators are effective in, for example, providing improvement in the production of procollagen and / or collagen and / or improvement in the maintenance and remodeling of elastin.

Benefits antl-celulltis and adiposity In some embodiments, a method is provided to reduce obesity and / or increase weight loss and / or help reduce body size. The method comprise applying topically to an area affected by unwanted fat deposition of an effective amount of an Averrhoa carambola extract from CPT-1 stimulation, in a cosmetically acceptable vehicle, for a sufficient time to reduce unwanted fat. . The activities CPT-1 stimulation of the composition can reduce fat accumulation and / or adipocyte differentiation, as described herein, to reduce weight, preferably in targeted areas. Such areas can be "problem areas" of which the consumer finds it difficult to lose weight through diet and / or general exercise. Other methods for treating unwanted fat deposition have been described and can be used with the Averrhoa Carambola stimulation extract of CPT-1 described herein. See, for example, O 04/047746.

In some other embodiments, it is contemplated that the compositions described herein, such as cosmetic compositions comprising an extract of Averrhoa carambola, will exhibit one or more benefits in aesthetic appearance, selected from the following: (a) treatment, reduction and / or prevention of fine lines or wrinkles; (b) reduction of the pore size of the skin, (c) improvement in the thickness, fatness, and / or tightness of the skin; (d) improvement in the flexibility and / or softness of the skin; (e) improvement in skin tone, radiance and / or clarity; (f) improvement in procollagen production and / or collagen; (g) improvement in the maintenance and remodeling of collagen and / or elastin; (h) improvement in skin texture and / or promotion of retexturization; (i) improvement in repair and / or skin barrier function; (j) improvement in the appearance of the contours of the skin; (k) restoration of luster and / or brilliance of the skin; (1) replenishment of essential nutrients and / or constituents in the skin; (m) decrease due to aging and / or menopause; (n) improvement in skin moistening; (o) increase in the elasticity and / or resilience of the skin; (p) treatment, reduction, and / or prevention of skin hanging; I (q) reduction of pigment points.

Based on the teachings provided herein, one of skill in the art will recognize other cosmetic and / or pharmaceutical applications for the compositions described herein, and such applications are also contemplated as being within the scope of the present invention. invention. For example, the compositions described herein may also find use in personal care products, such as skin care or hair care products, where it is desirable to produce an improvement in the appearance of the skin or hair, as described herein, in the application of the product. It is contemplated, for example, that the compositions described herein may find use in lotion and / or toner formulations that decrease the appearance of cellulite and other undesired subcutaneous fat on various body surfaces. It is contemplated, for example, that the compositions described herein may find use in hair care formulations that improve the appearance of hair by decreasing sebum and / or oil and / or unwanted fattyness on the hair.

Personal care products for the skin according to the invention include, for example, body lotions, body tonics, and the like. Hair care products according to the invention include, for example, shampoo, conditioner, aerosol spray, pump spray, mousse, foam, solution, serum, or the hair care composition can be incorporated into a wipe Treatment regimens The invention provides methods to improve the appearance of the skin by topically applying a composition comprising a CPT-1 stimulation carambola extract having the composition on an area of the skin for a sufficient period of time to improve the appearance of the skin, as described in FIG. I presented. The composition will typically be applied to the skin in accordance with a treatment regimen. The treatment regimen may comprise application of one, two, or three times daily for as long as necessary to achieve the desired results, such as the anti-cellulite benefits described herein. This treatment regimen may comprise the daily application or the application of a daily yes and no, for at least about one week, at least about two weeks, at least about three weeks, at least about four weeks, per at least about six weeks, at least about eight weeks, at least about twelve weeks, or more. In some embodiments, the composition is applied more than once a day during the aforementioned periods of time, for example, twice a day, preferably once in the morning and once again in the evening before sleep. The composition is preferably massaged throughout the area being treated, for example, on the thighs, buttocks, hips, abdomen, upper arms and the like.

Also chronic treatment regimens are contemplated, for example, with respect to prophylactic treatments directed at preventing one or more signs of cellulite from the skin or other undesired subcutaneous fat.; as well as with respect to the reduction and / or prevention of the recurrence of cellulitis in an area previously affected in this way. The treatment and / or prophylactic regimen may also depend on the concentration of the CPT-1 stimulation carambola extract that is used, for example, since different concentrations may produce anti-cellulite skin benefits more quickly than others. Treatment regimens according to the invention optionally may include additional exercise, diet modulation and increased water intake.

The compositions are generally applied topically to the skin for a period of time sufficient to improve the appearance of the skin affected by cellulite or other undesired subcutaneous fat. In some embodiments, the compositions are left on the skin as a "left over" composition, whereby it is proposed that they be applied in a formulation that allows to remain on the skin without being deliberately washed and / or rubbed for a certain period of time . For example, the composition can be left on the skin for one day, overnight, or for at least about 18 hours, for at least about 12 hours, for at least about 8 hours, or for at least about 4 hours.

Formulations of Excerpts from Averrhoa Carambola CPT-1 stimulators, such as the aqueous extracts of the Averrhoa carambola leaf, can be used to formulate cosmetic compositions, as is known in the art. The cosmetic compositions find use in anti-cellulite and anti-lipid products, preferably formulated for topical application to the skin, for example, with a cosmetically acceptable vehicle. Formulations for cosmetic compositions comprising Averrhoa carambola extracts of CPT-1 stimulation are described in more detail below.

According to the invention, caraway extracts of Averrhoa stimulation of CPT-1 can be formulated in a variety of product forms. The compositions can be prepared in targeted delivery systems, for example, creams, lotions, gels, toners, serums, transdermal patches and the like, particularly for topical administration. For example, the invention encompasses compositions comprising a cosmetically or dermatologically acceptable formulation that is suitable for contact with the tissue of the living animal, particularly human tissue, with virtually no or little physiological effect adverse to the user. The invention it also encompasses compositions for oral delivery. The compositions encompassed by this invention can be provided in any cosmetically and / or dermatologically suitable form, preferably as a lotion or cream, but also in an anhydrous or aqueous base, as well as in a sprayable liquid form. Other forms of cosmetic product suitable for the compositions include, for example, an emulsion, a cream, a balsam, a glitter, a lotion, a mask, a serum, a toner, an ointment, a mouse, a patch, an ointment, a solution, a spray, a wax-based bar, a washcloth, a shampoo, a conditioner and / or a foam.

In some particular embodiments, the cosmetic composition comprising an aqueous extract of Averrhoa carambola from CPT-1 stimulation is provided in the form of a cream for topical application to the affected skin, previously affected, or likely to be affected by cellulite. In some particularly preferred embodiments, the cream comprising the aqueous carambole stimulation extract of CPT-1 is supplied together with a gel for use with the cream, for example, by following the application of the cream with the application of the gel to the the same area of the skin. The gel preferably provides hardening polymers to increase the cellulite reduction effects of the cream. In more preferred embodiments, the gel provides a Cooling sensation to the skin when applied to the skin after the application of the cream. The cream and the gel can be provided in different containers, or in different compartments of the same container. In some embodiments, the cream and gel are provided in a "tube-in-a-tube" that delivers the cream and gel together. This allows the cream and gel to be mixed in the supply, for example, immediately before application to the skin.

In addition, contemplated compositions may include one or more cosmetically acceptable, compatible adjuvants commonly used and known to the skilled artisan, such as colorants, fragrances, emollients, humectants, preservatives, vitamins, chelates, thickeners, goatee oil or seed oil. knob (WO 01/66067 to "M thod of Treating to Skin Condition", incorporated herein by reference) and the like, as well as other botanicals such as aloe, chamomile and the like.

Also encompassed by the invention are transdermal delivery modes, such as patches and the like, with or without suitable penetration enhancers. The methods and compositions incorporated by the invention provide a means whereby the extract of Averrhoa carambola stimulation of CPT-1 can be administer effectively in a transdermal system or device. Examples of such devices are known in the art, for example, as described in U.S. Patent Nos. 5,146,846; 5,223,262; 4,820,724; 4,379,454; and 4,956,171, all of which are incorporated herein by reference and such descriptions are not intended to be limiting. In a preferred method, topical application is through a vehicle, carrier or sustained release diluent, for example, using a topically applied sustained release patch. Preferably, when a topical patch is used, the patch is applied to the desired area for a prolonged period of time, such as, for example, at least about 4 hours, at least about 8 hours, at least about 12 hours , at least about 16 hours, or at least about 24 hours. In some embodiments, the extended period of time is all day, for example, from the morning to the time of sleep, or during the night, for example, while the user is sleeping.

The aqueous stimulation extracts of CPT-1 from the carambole Averrhoa leaf of the present invention are preferably contained in a cosmetically or dermatologically acceptable vehicle, medium, diluent or carrier, which provides a topical formulation for use in the treatment, amelioration, prevention, inhibition, delay, and / or reduction of the signs of excess accumulation and / or production of subcutaneous fat, which include the improvement of the appearance of the skin affected by cellulitis.

In some embodiments, the topical formulation comprises a cosmetically acceptable vehicle (medium, diluent or carrier) that is compatible with human skin. The cosmetically acceptable vehicle may comprise an aqueous phase, an oil phase, alcohol or aqueous / alcohol based solutions, ointments, lotions, gels, wax-in-water or water-in-oil emulsions, oil-in-water, or water-oil-water emulsions, for example, which have the appearance of creams, gels, microemulsions or aerosols.

The aqueous phase is a mixture of one or more water-soluble or water-dispersible substances, which may be liquid, semi-solid or solid at room temperature (25 ° C). The vehicle comprises, or may be in the form of, a suspension, dispersion or solution in water or in an aqueous-alcoholic vehicle, which may contain a thickener or gelling agent. A person skilled in the art can select the appropriate cosmetic form, the ingredients contained therein, as well as the methods for preparing it, on the basis of knowledge possessed by the skilled person.

In some embodiments, the cosmetically acceptable vehicle may include an aqueous phase which may contain water, or a mixture of water and water. at least one hydrophilic organic solvent, in particular an alcohol, especially a linear or branched lower monoalcohol containing from 2 to 5 carbon atoms, for example, ethanol or propanol; a polyol, for example, propylene glycol, sorbitol, glycerol, diglycerol, panthenol, or polyethylene glycol; and mixtures thereof. The aqueous phase may represent from about 0.5% by weight to about 99.99% by weight, based on the total weight of the composition.

In some embodiments, when the composition of the invention is in the form of an emulsion, the composition may also optionally comprise a surfactant, preferably in an amount of about 0.1 wt% to about 30 wt%, and in particular about 1% by weight to about 20% by weight, based on the total weight of the composition.

In some embodiments, the composition may also comprise a thickening polymer such as an amphiphilic polyurethane, a polyacrylic homopolymer or copolymer, a polyester and / or a hydrocarbon-based resin.

The invention also contemplates formulations which may comprise an oil phase containing oil-soluble or oil-dispersible substances, which are liquid at room temperature (25 ° C) and / or oily substances or Waxes that are solid at room temperature, such as waxes, semi-solids, gums and mixtures thereof. The waxes may include hydrocarbon-based waxes, fluoro waxes and / or silicone waxes and may be of plant, mineral, animal, and / or synthetic origin. The formulations typically comprise from about 0 wt% to about 20 wt% waxes, based on the total weight. The gums used are generally polydimethylsiloxanes (PDMS), high molecular weight cyclics, cellulose gums or polysaccharides, and the semi-solid materials are generally hydrocarbon-based compounds, such as, but not limited to, lanolins and derivatives thereof. . This oily phase may also contain organic solvents.

Suitable oily materials that are liquid at room temperature, often referred to as oils, include hydrocarbon based oils of animal origin such as perhydrosqualene; hydrocarbon-based plant oils such as liquid triglycerides of fatty acids of 4 to 10 carbon atoms, for example, triglycerides of heptanoic or octanoic acid, or oils such as sunflower oil, corn oil, soybean oil, oil of grape seed, castor oil, avocado oil, triglycerides of caprylic / capric acid, or jojoba oil; linear or branched hydrocarbons of mineral or synthetic origin, such as liquid paraffin and derivatives of them, or oil jelly; and synthetic ethers, in particular esters of fatty alcohols, specifically, for example, isopropyl myristate, 2-ethylhexyl palmitate, 2-octyldodecyl stearate, isostearyl isostearate; hydroxylated esters such as isostearyl lactate, octyl hydroxystearate, octyldodecyl hydroxystearate, heptanoates, octanoates and decanoates of fatty alcohols; polyol esters such as propylene glycol dioctanoate, neopentyl glycol diheptanoate, diethylene glycol diisononanoate, and pentaerythritol esters; fatty alcohols containing from 12 to 26 carbon atoms such as octyldodecanol, 2-butyloctanol, 2-hexyldecanol, 2-undecylpentadecanol, oleyl alcohol; fluoro oils partially based on hydrocarbon and / or fluorosilicone oils; silicone oils such as polydimethylsiloxane (PD S) linear or cyclic, volatile or non-volatile which are liquid or semi-solid at room temperature, such as cyclomethicones and dimethicones, optionally comprising a phenyl group, for example phenyl trimethicones, siloxanes, and mixtures of the same. These oils are usually present in an amount from about 0 wt% to about 90 wt%, preferably from about 1 wt% to about 80 wt% by weight of the oil phase.

The oil phase of the formulation can also understand one or more cosmetically acceptable organic solvents. These solvents are present in an amount of from about 0% by weight to about 60% by weight, preferably from about 1% by weight to about 30% by weight, based on the total weight of the composition, and can be selected from the group which consists of lipophilic organic solvents, amphiphilic organic solvents, and mixtures thereof. Suitable solvents that can be used in the composition of the invention include acetic acid esters such as methyl, ethyl, butyl, amyl or 2-methoxyethyl acetate; isopropyl acetate; hydrocarbons such as toluene, xylene, p-xylene, hexane or heptane; ethers containing at least 3 carbon atoms, and mixtures thereof. In some other embodiments, the compositions may be in the form of vesicular dispersions containing ionic and / or nonionic lipids, as described above.

In yet other embodiments, the compositions are formulated into liposomes or microspheres, which may comprise other additives or substances, and / or which may be modified to target or remain more specifically at the site after administration. (See, for example, U.S. Patent No. 5,770,222 to Unger et al., Incorporated herein by reference).

The formulations for use in the methods Inventives may further comprise any ingredient conventionally used in the cosmetics field. These ingredients include, for example, preservatives, aqueous phase thickeners (polysaccharide biopolymers, synthetic polymers), fatty phase thickeners, fragrances, hydrophilic and lipophilic active agents, and mixtures thereof. The amounts of these various ingredients are those conventionally used in the cosmetics field to achieve their intended purpose, and typically range from about 0.01% by weight to about 20% by weight, based on the total weight of the composition or formulation. The nature of these ingredients and their amounts will be selected to be compatible with the production and applications proposed in the compositions, as described herein.

In some embodiments, the formulation may optionally comprise an additional particulate phase, typically present in an amount of from about 0 wt.% To about 30 wt.%, Based on the total weight of the composition or formulation, preferably about 0.05 wt. weight to about 20% by weight, and which may comprise pigments and / or pearlescent agents and / or fillers used in cosmetic compositions.

Suitable inorganic pigments include, but they are not limited to titanium oxide, zirconium oxide and cerium oxide, as well as zinc oxide, iron oxide, chromium oxide and ferric blue. Suitable organic pigments include barium, strontium, calcium and aluminum and carbon black lacquers. Suitable pearlescent agents include mica coated with titanium oxide, with iron oxide or with natural pigment. The fillers are normally present in an amount of from about 0 wt% to about 20 wt%, based on the total weight of the composition or formulation, preferably from about 0.1 wt% to about 10 wt%. Suitable fillers include talc, silica, zinc stearate, mica, kaolin, nylon (particularly orgasol) powder, polyethylene powder, TEFLON ™, starch, boron nitride, copolymer microspheres such as Expancel (Nobel Industrie), Polytrap ( Dow Corning), and silicone resin micro-accounts (Tospearl from Toshiba).

In some particular embodiments, the compositions for topical application may be in the form of a personal skin care product, preferably for the thighs, buttocks, legs, hips, abdomen, extremities, upper arms and / or other areas of the skin. body. Non-limiting examples include creams or lotions, balms, ointments, gels, masks, artificial tanning compositions, patches or a solid that is emptied or mold as a bar or a round shape, for example.

In some embodiments, topical formulations may also include one or more antioxidants. An antioxidant works, among other things, to purify the free radicals of the skin, protect the skin from environmental aggressors. Examples of antioxidants that can be used in the present compositions and formulations include compounds containing phenolic hydroxy functions, such as ascorbic acid and its derivatives / esters; Thiodipropionic acid and its esters; vitamins A, C, or E; polyphenols, beta-carotene; catechins; curcumin; ferulic acid derivatives (e.g., ethyl ferulate, sodium ferulate); gallic acid derivatives (e.g., propyl gallate); lycopene; reductive acid; rosmarinic acid; tannic acid; tetrahydrocurcumin; tocopherol and its derivatives; uric acid; or any of the mixtures thereof. Other suitable antioxidants are those having one or more thiol (-SH) functions, in either reduced or non-reduced form, such as glutathione, lipoic acid, thioglycolic acid, and other sulfhydryl compounds. The antioxidant may be inorganic, such as bisulfites, metabisulfites, sulfites, or other inorganic salts and sulfur-containing acids. The compositions of the present invention may have an antioxidant of preferably from about 0.001% by weight to about 10% by weight, and more preferably from about 0.01% by weight to about 5% by weight, based on the total weight of the composition or formulation.

In some embodiments, topical formulations may also include one or more of the following: a skin penetration enhancer, an emollient, a skin fortifier, an exfoliation promoter, and an optical diffuser. Details regarding these and other suitable cosmetic ingredients can be found in the International Cosmetic Ingredient Dictionary and Handbook, Manual, 10th Edition (2004), published by the Cosmetic, Toiletry, and Fragrance Association (CTFA), p. 2177-2299, which is incorporated herein by reference in its entirety.

An emollient provides the functional benefits of increasing the smoothness of the skin and can help improve the appearance of skin affected by cellulite and other unwanted subcutaneous fat. Examples of emollients include isopropyl myristate, petrolatum, isopropyl lanolate, silicones (eg, methicone, dimethicone), oils, mineral oils, fatty acid esters, or any of mixtures thereof. The preferred emollient is present from about 0.1 wt% to about 50 wt% of the total weight of the composition or formulation.

A skin fortifier serves as an enhancer of collagen to the skin. An example of a suitable and preferred skin fortifier is palmitoyl oligopeptide. Other skin fortifiers are collagen and / or glycosaminoglycan (GAG) enhancing agents. The skin fortifier of preference is present in about 0.1% by weight to about 20% by weight of the total weight of the composition or formulation.

In some embodiments, the formulations may have one or more exfoliation promoters. Suitable examples of exfoliation promoters include alpha hydroxy acids (AHA); benzoyl peroxide; beta hydroxy acids; acid ketoes, such as pyruvic acid, 2-oxopropanoic acid, 2-oxobutanoic acid and 2-oxo-pentanoic acid; oxa acids as described in U.S. Patent Nos. 5,847,003 and 5,834,513 (the descriptions of which are incorporated herein by reference); salicylic acid; urea; or any of the mixtures thereof. Preferred exfoliation promoters are 3, 6, 9-trioxaundecanedioic acid, glycolic acid, lactic acid, or any of mixtures thereof. When one embodiment of the invention includes an exfoliation promoter, the formulation may have from about 0.1 wt% to about 30 wt%, preferably from about 1 wt% to about 15 wt%, and more preferably about 1% by weight a about 10% by weight, of the exfoliation promoter based on the total weight of the composition or formulation.

An optical diffuser is a particle that changes the surface optometry of the skin, resulting in a visual blurring and smoothing of, for example, lines and wrinkles, as well as bulging and non-uniformity caused by cellulite and other undesired subcutaneous fat. Examples of optical diffusers that can be used in the present invention include, but are not limited to, boron nitride, mica, nylon, polymethyl methacrylate (PMMA), polyurethane powder, sericite, silica, silicone powder, talc, TEFLON ™, titanium dioxide, zinc oxide, or any of the mixtures thereof. The optical diffuser is preferably present at about 0.01% by weight to about 20% by weight, based on the total weight of the composition or formulation.

In some embodiments, the formulations may have one or more retinoids. Exemplary retinoids include, without limitation, retinoic acid (e.g., all-trans or 13-cis) and derivatives thereof, retinol (Vitamin A) and esters thereof, such as retinyl palmitate, retinyl acetate and propionate. retinol, and salts thereof.

In some embodiments, the formulations may have one or more sunscreen protectors. A solar filter protects the skin from damage by ultraviolet rays. In an illustrative embodiment of the invention, the sunscreen will provide protection against both UVA and UVB, by using either a single sunscreen or a combination of sunscreens. Among the sunscreens that may be employed in the present compositions are avobenzone, cinnamic acid derivatives (such as octylmethoxy cinnamate), octyl salicylate, oxybenzone, titanium dioxide, zinc oxide, or any of the mixtures thereof. The sunscreen may be present in an amount of about 1% by weight to about 30% by weight of the total weight of the composition. The compositions of the invention having sunscreen give rise to additional improvements to the aesthetic appearance of the skin, including at least one of the following: minimization of sunburn and / or reduction of redness.

In some embodiments, the formulation may also have one or more of the following cosmetic, pharmaceutical agents, excipients, ingredients or adjuvants; anesthetics; antibiotics, for example, erythromycin and tetracyclines; salicylic acids; anti-allergenic; antifungals; antiseptics; anti-irritants; anti-inflammatory agents; antimicrobials; analgesics; nitric oxide synthase inhibitors; insect repellents; self-tanning agent; penetration enhancers in the skin; skin cooling agents; chelating agents; dyes, including dyes, lacquers and pigments that can be untreated or chemically treated on the surface to improve wettability or some other property; demulcent; emulsifiers; fragrances; humectants; lubricants; skin protectors; humidifiers; pH adjusters; conservatives; stabilizers; surfactants; thickeners; film formers; plasticizers; viscosity modifiers; vitamins; stimulators of blood flow; or any of the mixtures thereof. The amounts of these various substances are those that are conventionally used in the cosmetic or pharmaceutical fields to achieve their intended purposes, for example, they may constitute from about 0.01% by weight to about 20% by weight of the total weight of the composition or formulation.

Emulsifiers are typically present in the compositions or formulations of the invention in an amount of about 0.01% by weight to about 30% by weight, and preferably from about 0.5% by weight to about 30% by weight, based on the total weight of the composition. In some other embodiments, the composition or formulation is free or substantially free of emulsifiers.

Non-limiting examples of thickening agents Suitable include xanthan gum, hydroxypropyl cellulose, hydroxyethyl cellulose, carbomer, acacia gum, Sepigel 305 (available from Seppic Co., France), and clays such as magnesium aluminum silicate.

The topical compositions of the present invention may include, and their utility may be increased, by one or more humectants, such as ureas, pyrrolidone carboxylic acids, amino acids, sodium hyaluronates, certain polyols, and other compounds with hygroscopic properties.

The general activity and the softness to the skin of the compositions according to the invention can also be increased by neutralization to a pH of from about 3.5 to about 8.0, much more preferably a pH of from about 3.5 to about 5.5. This neutralization is preferably carried out with one or more of ammonium hydroxide, potassium hydroxide, sodium hydroxide, arginine or other amino acids and / or triethanolamine.

All terms cited herein are proposed to have their ordinary meaning unless otherwise provided. As used herein, "% by weight" or "% by weight" refers to the weight percent of a component relative to the total weight of the composition or formulation (i.e., including any of carriers, vehicles, solvents, emollients, fillers, or other components added before application to the skin) unless otherwise specified.

EXAMPLES Example 1: Procedure of Extraction of the Leaf of Averrhoa carambola and the HPLC Analysis of the Leaf Excerpts of Averrhoa carambola from two Protocols The carambola Averrhoa can be extracted from natural raw materials by using aqueous-organic solvent extraction methods as is known in the art, for example, as discussed below.

An aqueous extract of CPT-1 stimulation was obtained by extracting the leaves of the Averrhoa carambola plant using an aqueous extraction scheme. Briefly, the leaves of Averrhoa carambola were first ground to produce a powder.

The ground powder was then solubilized in water at a concentration between about 10 and about 90 g / L, preferably between about 25 and about 40 g / L, at a temperature between about 40 ° C and 60 ° C. The aqueous solution was subjected to enzymatic hydrolysis directed to the carbohydrates using any of a number of commercially available hydrolases or carbohydrases. The residual enzymatic activity is inactivated by heat treatment for about 4 hours. An adjuvant such as polyvinylpolypyrrolidone (PVPP) was added to remove the polyphenolic compounds. The soluble and insoluble phases were separated by decantation, filtration and / or centrifugation and collection of the soluble fraction (filtrate or soluble phase). The filtration eliminated molecules of high molecular weight, that is, above 20,000 Da. The active fraction was then concentrated by methods known in the art, such as by rotovap, lyophilization, or freeze drying. The resulting concentrated liquid phase was sterilized by membrane filtration through a 0.22 micron filter. The total concentrated extract gave an aqueous extract (stimulation extract of CPT-1) from Averrhoa carambola in the form of an amber, clear liquid.

The stimulation extract of CPT-1 was characterized by having 36.2 g / L of dry matter (obtained by drying in oven at 105 ° C until the constant weight was obtained); a pH of 3.6 (measured potentiometrically at room temperature); 56.1% total sugar content by weight of the dry matter (Dubois et al., Analytical Chemistry 28 (3): 350-356 (1956)); 26.2% crude ash content by weight of the dry matter (obtained by incineration at 550 ° C in an electric muffle furnace and deducting the tared container, VULCAN ™ 3.550-NDI); 8.6% protein content by weight of dry matter (measured according to Kjeldhal's method, Official Methods of Analysis of AOAC International, 12th Ed., Pages 15-60 (1975)); 6.6% of uronic acid by weight of dry matter, and 0.0015% of polyphenol content by weight of dry matter. The determination of uronic acid was made by reacting uronic present with sodium tetraborate, producing a pink color in the presence of meta-hydroxydiphenyl that was quantified by spectrophotometry at 520 nm against a standard range of galacturonic acid from 10 to 100 mg / L (the results were expressed in terms of galacturonic acid). The phenolic compounds were quantified by the reaction in the presence of potassium ferricyanide, the formation of color compounds detected at 715nm using a standard range of gallic acid from 40 to 120 mg / L.

A methanolic extract of CPT-1 inhibition was obtained by extracting the leaves of the Averrhoa carambola plant using an extraction scheme with methanol. Briefly, the Averrhoa carambola leaves were first manually ground into small particles resulting in a powder. The ground powder was then extracted with 25% methanol. Alternatively, the homogenized plant material can be combined with an equivalent volume of methanol, stirred in a sealed container for 30-120 minutes at 200 rpm, and centrifuged for 10 min, in order to form a clear methanol layer in the higher.

After filtration and evaporation in vacuo, the total concentrated extract was lyophilized (or concentrated by other means known in the art) to give a methanol extract of Averrhoa carambola.

For sampling purposes, leaf extracts of Averrhoa carambola were dispersed in 25% methanol at approximately 5mg / mL. The soluble UV absorbing components were separated and analyzed by HPLC. The column of the HPLC instrument was Zorbax SB-C18, 7.5 cm long x 4.6 mm I.D. of stainless steel, particle size of 3.5 microns, and the detector was the UV absorbance of the diode array, at 260 nm, 300 nra and 360 nm. The conditions of HPLC analysis were as follows: Mobile Phase Gradient: 0 Minutes 15% methanol (Solvent B) / 85% water with 1% acetic acid (Solvent A). 10 minutes 95% methanol / 5% water with 1% acetic acid. 15 minutes 95% methanol / 5% water with 1% acetic acid. 15. 01 Minutes 5% methanol / 85% water with 1% acetic acid. 19 Minutes 15% methanol / 85% water with 1% acetic acid.

Flow Expense: 1.5 mL / min.

Column temperature: 40 ° C Volume of Sample Injection: 20 μ ?.

Run Time: 19 min The HPLC spectra of a sample of a leaf extract of Averrhoa carambola from aqueous CPT-1 stimulation (Figure 1) and a leaf extract of Averrhoa carambola from methanolic CPT-1 inhibition (Figure 2) show different peak patterns under the same elution conditions, indicating chemical differences between the two extracts.

Example 2: Stimulation of CPT-1 Gene Expression by Averrhoa Leaf Extract Carambola The human pre-adipocytes were allowed to differentiate into adipocytes in the adipocyte differentiation medium for 7 days. On Day 8, the Adipocyte Differentiation Medium was replaced with the Adipocyte Maintenance Medium containing the leaf extract of Averrhoa carambola for another 7 days as described above. The leaf extract of Averrhoa carambola in the percentages by weight indicated was added every other day. At the end of the treatment, the RNA was extracted from the adipocytes using the RNA Easy mini equipment (Qiagen, CA). 200 ng of total RNA was used to generate 20 microL of cDNA using the high capacity cDNA reverse transcription equipment (Applied Biosystem: Cat # 4368814). Reverse transcriptase, the buffer, dNTP, random primer, and the RNase inhibitor were diluted with the RNA according to the manufacturer's protocol. One microliter of cDNA was used in RTL-PCR reactions of microL. Briefly, 10 μ? of the Master TaqMan Expression Master Mix (Applied Biosystems; Cat # 4369016), 8 μ? of H20, 1 μ? of cDNA and 1 μ? of either the CPT-1 primer (Applied Biosystem; Hs03046298_sl) or 18S (Applied Biosystem; 4333760-1001032) as a maintenance gene were mixed in a 96-well polypropylene plate (Agilent Technologies, Cat # 410088). The RTq-PCR conditions were an incubation step at 50 ° C for 2 minutes and an enzyme activation step at 95 ° C for 10 minutes; followed by 45 cycles of 95 seconds for 30 seconds and 60 ° C for 1 minute. The CT value was obtained from the Stratagene MX2005P software.

All samples were run in triplicate and normalized to 18S, and the results were expressed as a percentage of the control, as presented in Tables 1 and 2.

Table 1, Expression of the CPT-1 Gene Table 2, Expression of the CPT-1 Gene Human adipocytes treated with it% by weight of the leaf extract of Averrhoa carambola acuoso showed a% significant increase in the expression of the CPT-1 gene with the aqueous leaf extract of Averrhoa carambola, as indicated in Table 1. In marked contrast, an extract of leaf extract of Averrhoa carambola with methanol showed a decrease in the expression of the CPT-1 gene, as indicated in Table 3. This discovery is surprising and indicates that the two leaf extracts of Averrhoa carambola, obtained by way of aqueous extraction (data summarized in Table 1), or obtained by the methanol extraction route (data summarized in Table 2), have different chemical compositions.

Example 3: Reduction of Intracellular Triglycerides by Extract of Leaf of Averrhoa carambola Primary cryopreserved human pre-adipocytes harvested from the subcutaneous adipose tissue of a healthy woman were obtained from Zen-Bio (Research Triangle Park, NC). Following the manufacturer's instructions, the pre-adipocytes were cultured in the pre-adipocyte medium containing DMEM / F-12 from Ham (1: 1, v / v), HEPES (pH 1.4), fetal bovine serum, penicillin, streptomycin, and amphotericin B (Zen-Bio), in an incubator at 37 ° C humidified with 5% C02. After reaching 90% confluence, the pre-adipocytes were allowed to differentiate into adipocytes by adding the Adipocyte Differentiation Medium containing DMEM / F-12 from Ham (1: 1, v / v), HEPES, pH 7.4, serum fetal bovine, biotin pantothenate, human insulin, dexamethasone, isobutylmethylxanthine, penicillin, streptomycin and amphotericin B (Zen-Bio).

To treat the adipocytes with the leaf extract of Averrhoa carambola, the aqueous extract (obtained according to the process of Example 1) was dissolved in the adipocyte differentiation medium (in two concentrations) and then added in cell culture during 7 days. The untreated adipocytes were used as a control. After 7 days of incubation, the Adipocyte Differentiation Medium was replaced with the Maintenance Medium containing carambole Averrhoa leaf extract, Ham DMEM / F-12 (1: 1, v / v), HEPES, pH 7.4 , fetal bovine serum, biotin pantothenate, human insulin, dexamethasone, penicillin, streptomycin and amphotericin B, and the adipocytes continued under incubation for another 7 days. The Triglyceride production in adipocytes was determined by using a triglyceride assay type (Zen-Bio). Briefly, the adipocytes were rinsed with a buffer buffer for washing and lysed in a lysis buffer after removal of the medium. The intracellular triglycerides were released in the lysis buffer and converted to glycerol-1-phosphate, which was subsequently oxidized to di-hydroxy acetone phosphate and hydrogen peroxide. The hydrogen peroxide was reacted with 4-aminoantipyrine (4-AAP) and N-ethyl-N- (3-sulfopropyl) -m-anisidine sodium (ESPA) to generate a quinoneimine dye, which shows a maximum of absorbency at 540 nm. The increase in absorbance at 540 nm is directly proportional to the intracellular levels of triglycerides in the adipocytes. The results are presented in Table 3 below.

Table 3, Intracellular Triglyceride Levels The human adipocytes treated with it% by weight indicated of leaf extract of Averrhoa carambola showed a% of significant ease in the levels of intracellular triglyceride, as indicated in Table 3.

Example 4: Exemplary compositions An oil-in-water emulsion cosmetic composition of sample according to the invention was formulated in accordance with Table 4.

Table 4, Sample Cosmetic Composition The leaf extract of Averrhoa carambola was a leaf extract of Averrhoa carambola for stimulation of Aqueous CPT-1 obtained as described in Example 3. Certain optional ingredients are indicated by a range that includes zero percent.

Other cosmetic compositions comprising an extract of Averrhoa carambola for topical application to the skin can be formulated by methods known in the art. cosmetic A cream comprising an extract of Averrhoa carambola can optionally be administered together with a cosmetic composition of a gel for optimal results. Suitable ingredients for such formulations are found in the INCI Ingredient Dictionary and Handbook, 11th edition, 2006, and in the International Cosmetic Ingredient Dictionary and Handbook, 10th edition (2004), published by the Cosmetic, Toiletry, and Fragrance Association (CTFA) , the descriptions of which are incorporated herein by reference in their entirety.

Example 5: Consumer Study A consumer test, double blind, monadic, was conducted using a composition according to the invention (as described in Table 4) over a period of four weeks among 120 women aged 25-59, in five geographically dispersed locations in the United States. This study was conducted through an independent consumer research agency, in accordance with the best practices of the consumer use test and the ASTM International guidelines to support the claims. Respondents were instructed to use the composition at home twice a day for four weeks, and were interviewed by telephone after 1 week, 2 weeks and 4 weeks of composition use twice a day. All the data is They returned to the independent research agency for processing and analysis using ANOVA. According to the results of the study, 61% of the respondents agreed that the composition remarkably reduces the appearance of cellulite; | 72% of respondents agreed that the composition makes their skin feel more toned and had the freedom and confidence to use what they will want; 66% of the respondents agreed that the depth and intensity of their cellulite was reduced in only two weeks; and 59% of the respondents agreed that even their most unchanged or stubborn cellulite was visibly improved in just two weeks. These results were significant in a confidence interval of 90%.

All references including patent applications and publications cited herein are incorporated herein by reference in their entirety and for all purposes to the same degree as if each publication or patent or individual patent application was specifically and individually indicated to be incorporated by reference in its entirety for all purposes. Many modifications and variations of this invention can be made without departing from its spirit and scope, as will be apparent to those skilled in the art. The specific modalities described they are hereby provided by way of example only, and the invention is to be limited only by the terms of the appended claims, together with the full scope of equivalents to which such claims are authorized.

Claims (33)

1. A method for treating a skin condition represented by excess lipids, characterized in that it comprises applying topically to the skin in need thereof an effective amount of an aqueous extract of stimulation of Carnitine Palmitoyl Transferase-1 (CPT-1) of the leaf of Averrhoa carambola in a cosmetically acceptable vehicle for a sufficient time to improve the appearance of the skin.

2. The method in accordance with the claim 1, characterized in that the aqueous extract has an HPLC analysis according to Figure 1.

3. The method according to claim 1, characterized in that the aqueous extract comprises less than 0.1% by weight of phenolic compounds and at least 20% by weight of carbohydrates.

. The method according to claim 1, characterized in that the condition of the skin is cellulite.

5. The method according to claim 1, characterized in that the condition of the skin is acne.

6. The method according to claim 1, characterized in that the condition of the skin is oily skin.

7. The method according to claim 1, characterized in that the aqueous extract also comprises at least one other anti-lipid agent.

8. The method according to claim 7, characterized in that the at least one other anti-lipid agent comprises at least one agent selected from the group consisting of a phosphodiesterase inhibitor, an adenylate cyclase activator, a lipolysis stimulator, an agonist of the beta-adrenergic receptor, an alpha-2-adrenergic receptor antagonist and combinations thereof.

9. The method according to claim 7, characterized in that the at least one other anti-lipid agent comprises at least one agent selected from the group consisting of a xanthine analogue, forskolin, a forskohlii extract, a Hawthorne extract, an extract of cola, isoproterenol, yohimbine, Ginkgo biloba extract, perilla oil, and combinations thereof.

10. The method according to claim 4, characterized in that the cellulitis is found in at least one of a thigh, buttocks, abdomen, hip and / or upper arm region.

11. The method according to claim 1, characterized in that sufficient time to improve the appearance of the skin comprises a period of at least 2 weeks, and wherein the aqueous extract is applied at least once a day.

12. The method according to claim 2, characterized in that the aqueous extract is applied two or three times a day.

13. A method for reducing the deposition of unwanted fat and / or accumulation, characterized in that it comprises applying topically to an affected area an effective amount of an aqueous extract of stimulation of CPT-1 from the leaf of Averrhoa carambola in a cosmetically acceptable vehicle, during a enough time to reduce unwanted fat.

14. A composition for treating a condition of the skin represented by excess lipids, characterized in that it comprises an effective amount of an aqueous extract of stimulation of CPT-1 from the leaf of Averrhoa carambola in a cosmetically acceptable vehicle.

15. The composition according to claim 14, characterized in that the composition further comprises at least one other anti-lipid agent selected from the group consisting of a xanthine analogue, forskolin, a forskohlii extract, a Hawthorne extract, a tail extract , isoproterenol, yohimbine, Ginkgo biloba extract, perilla oil, and combinations thereof.

16. A composition for treating a condition of the skin represented by excess lipids, characterized in that it comprises an effective amount of an aqueous extract of stimulation of CPT-1 from the Averrhoa carambola leaf in a cosmetically acceptable vehicle, wherein the aqueous extract has an HPLC analysis according to Figure 1.

17. The composition according to claim 16, characterized in that the composition further comprises at least one other anti-lipid agent selected from the group consisting of a xanthine analogue, forskolin, a forskohlii extract, a Hawthorne extract, a tail extract , isoproterenol, yohimbine, Ginkgo biloba extract, perilla oil, and combinations thereof.

18. The composition according to claim 16, characterized in that the composition further comprises at least one collagen and / or elastin stimulator.

19. A composition for treating a condition of the skin represented by excess lipids, characterized in that it comprises an effective amount of an aqueous extract of stimulation of CPT-1 from the leaf of Averrhoa carambola in a cosmetically acceptable vehicle, wherein the aqueous extract comprises minor than 0.1% by weight of phenolic compounds and at least 20% by weight of carbohydrates.

20. The use of an aqueous extract of the Averrhoa carambola leaf, characterized in that it is for the treatment of excess lipids, where the aqueous extract it comprises less than 0.1% by weight of phenolic compounds and at least 20% by weight of carbohydrate.

21. The use according to claim 20, characterized in that the treatment is comprised of the up-regulation of the expression CPT-1.

22. The use according to claim 21, characterized in that the up-regulation of CPT-1 expression is tested by a measurable increase in mRNA transcription associated with CPT-1.

23. The use according to claim 22, characterized in that upregulation of CPT-1 expression is assayed by a measurable increase in protein expression associated with CPT-1.

24. The use according to claim 20, characterized in that the treatment is comprised of the reduction of lipid accumulation in the adipocytes.

25. The use according to claim 20, characterized in that the treatment is comprised of the reduction in the differentiation of adipocytes.

26. The use according to claim 20, characterized in that the treatment is comprised of the reduction in the accumulation of adipocytes.

27. The use according to claim 20, characterized in that the treatment is comprised of the reduction in the production, storage and / or accumulation of intracellular triglyceride.

28. The use according to claim 27, characterized in that the treatment is further comprised of the reduction in triglycerides in the serum.

29. The use according to claim 20, characterized in that the treatment is comprised of the reduction of subcutaneous fat.

30. The use according to claim 20, characterized in that the treatment is comprised of the reduced expression of lipogenic genes.

31. The use according to claim 20, characterized in that the treatment is comprised of the increased oxidation of fatty acids.

32. The use according to claim 20, characterized in that the aqueous extract is obtained by the aqueous solubilization of the Averrhoa carambola leaf powder to form a mixture, followed by the enzymatic hydrolysis of the mixture and the separation of the aqueous phase from the mixture. , which results in the aqueous leaf extract of Averrhoa carambola.

33. The use according to claim 20, characterized in that the aqueous extract has an HPLC analysis according to Figure 1.