KR20170067287A - Composition for improving the skin - Google Patents

Abstract

The present invention relates to a composition comprising picetine as an active ingredient, and the composition of the present invention has an effect of improving or preventing aging of skin, wrinkles, lowering of elasticity and lowering of moisture content, ) And sulfosuccinic acid glycosaminoglycan, thereby reducing the wrinkles, aging, elasticity, etc. of the skin fundamentally and improving and preventing it. It is derived from a natural substance and has low toxicity and side effects, Or as an effective ingredient such as food.

Description

[Composition for improving the skin]

The present invention relates to a cosmetic, a health functional food and a pharmaceutical composition for improving skin.

The skin is an important body which is responsible for various physiological functions such as a function for protecting the human body from the external environment, a barrier function for preventing the internal moisture and useful components from flowing out, a temperature control function, and an excretion function. As the aging of an individual progresses, the skin is also aged to lose this important function. In general, the main causes of skin aging are largely divided into extrinsic factors such as intrinsic factors explained by the increase in natural age and sunlight damage have. As a result of skin aging caused by these internal and external factors, wrinkle formation and elasticity decrease phenomenon are caused mainly due to damage and change of the dermal layer.

The structure of the skin is largely divided into the epidermal layer, the dermal layer, and the subcutaneous fat layer. The dermis is a substantial skin that makes up 90% of the skin and consists of a matrix that fills the connective tissue between the collagen fibers and the elastic fibers and between the cells and the connective tissue. Collagen fibers are produced in fibroblasts, and their important functions are mechanical rigidity of the skin, resistance of connective tissues, adhesion of tissues, and support of cell adhesion. Such collagen is reduced in its amount and deteriorated in its structure as it ages, and it has been pointed out as a main cause of endogenous skin aging and wrinkles. In addition, collagen fiber damage caused by ultraviolet rays may be a cause of exogenous skin aging and wrinkles. Elastic fibers are important materials to maintain the elasticity of the skin. When it is denatured due to various causes, the skin elasticity is reduced. Substrate is a substance filling the dendritic connective fibers and cells, and is present in the form of gel without morphology. Glycosaminoglycan, which is a hydrophilic polysaccharide that forms a substrate, is also called a mucopolysaccharide because it exists in the form of a mucus dissolved in water.

Glycosaminoglycan (GAG) is a structure in which disaccharide-type sugars are repeatedly connected to each other to form hyaluronic acid, chondroitin sulfate, heparan sulfate, heparin, keratan sulfate sulfate, and dermatan sulfate. GAG can be roughly classified into two types: Hyaluronic acid (GAG) that does not contain a sulfate group, and the remaining 5 species including a sulfate group.

GAG is a major component of extracellular marix (ECM) in the skin and plays a role in filling void spaces between collagen fibers and elastic fibers, which are a large part of ECM, and recognizes changes in surrounding proteins or cells, Lt; / RTI > This affects the growth and differentiation of cells and their normal function. In addition, GAG has an excellent binding ability with water molecules and plays an important role in maintaining moisture of the skin. As the skin aging progresses due to internal or external causes, the amount of GAG present in the dermis decreases and the ability to newly synthesize GAG decreases. This increases the void space of the dermis to reduce wrinkles, reduce skin elasticity, The results are retrieved.

The wrinkle preventing and improving cosmetic materials that are used to improve the aging and wrinkles of the skin are products containing vitamin A (retinol) or retinyl palmitate. However, the products containing these raw materials are not only sensitive to changes over time, but also have a limited amount of use due to problems of stability such as skin irritation and redness when they are penetrated or decomposed into the skin at an effective concentration or more, And the moisturizing effect was insignificant.

In order to solve such a problem, the inventors of the present invention have found that, in order to prevent aging of the skin and to prevent aging of the skin, The inventors of the present invention have conducted continuous research on the skin improving agent capable of suppressing the occurrence of wrinkles and confirmed that picetin is excellent in the effect of promoting the synthesis of sulfosized glycosaminoglycan and collagen type I of skin cells, .

Accordingly, it is an object of the present invention to provide a cosmetic composition, a pharmaceutical composition and a food composition having a skin-improving effect.

In order to achieve the above object, the present invention provides a cosmetic composition comprising fisetin or a derivative thereof as an active ingredient.

The composition may be for promoting the synthesis of sulfated Glycosaminoglycan.

The composition may be for promoting collagen synthesis.

The composition may be for aging the skin, wrinkling the skin, lowering the elasticity of the skin, lowering the moisture content of the skin, or improving or preventing aging.

The amount of the phytetin contained in the composition may be 1 x 10 < ^-5 > to 10 wt% of the total composition.

The cosmetic composition may be in the form of a solution, a suspension, an emulsion, a paste, a gel, a cream, a lotion, a powder, a soap, a surfactant-containing cleansing oil, a foundation, a cosmetic liquid, a cosmetic ointment, , A make-up remover, and a detergent.

The present invention also provides cosmetics comprising fisetin or a derivative thereof as an active ingredient.

In addition, the present invention provides a pharmaceutical composition for preventing and treating skin damage diseases comprising fisetin or a derivative thereof as an active ingredient.

The skin damage disease may be selected from the group consisting of skin erythema, skin aging, skin wrinkles, skin capillaries, skin elasticity reduction, and skin moisture-containing degradation.

The pharmaceutical composition may be in a form selected from the group consisting of ointments, creams, tablets, pills, powders, granules, capsules, suspensions, solutions, emulsions, syrups, aqueous solutions, non-aqueous solutions, suspensions, For the prevention and treatment of injured diseases.

Further, the present invention provides a health functional food composition for improving or preventing skin aging, skin wrinkles, reduced skin elasticity, or reduced skin moisture content comprising fisetin or a derivative thereof as an active ingredient.

The present invention relates to a composition comprising picetin as an active ingredient, which has the effect of improving or preventing skin aging, wrinkles, reduced elasticity and moisture content, and more specifically, a skin collagen type I and a sulfated glycosaminoglycan The present invention relates to a cosmetic composition, cosmetic composition, cosmetic composition, cosmetic composition, cosmetic composition, cosmetic composition, cosmetic composition, cosmetic composition, cosmetic composition, cosmetic composition, And can be very usefully used in food compositions.

The present invention relates to a cosmetic composition comprising fisetin or a derivative thereof as an active ingredient.

The picetine may be represented by the following formula (1).

[Chemical Formula 1]

The compound of the above formula (I) is named 2- (3,4-dihydroxyphenyl) -3,7-dihydroxyphenyl-3,7-dihydroxychromene -4-one), and the generic name is fisetin.

The above-mentioned picetin corresponds to one of the kinds of the fluroborides, and means a compound having C ₁₅ H ₁₀ O ₆ , molecular weight = 286. The above-mentioned pedin generally has yellow needle-like crystals, the melting point is 360 ° C or higher, and recrystallized in diluted acetic acid may contain 6 molecules of crystal number. Can be extracted and purified from extracts of natural products.

The above-mentioned picetine can be chemically synthesized through various organic chemistry methods known in the art, and can be easily obtained from plants and the like. The picetin used in the present invention was purchased from Sigma-Aldrich (USA).

The derivatives of picetine are all meant to show effects similar to those of the picetin of the present invention among the compounds in which some structures of picetin are substituted or changed.

The above-mentioned picetin is useful as an effective ingredient for suppressing, treating and improving wrinkles caused by wrinkles associated with reduction of collagen and lowering of elasticity, degradation of synthesis of sulfated glycosaminoglycan, which is another constituent of extracellular matrix, And can be used as an effective ingredient for wound healing due to its excellent healing effect on wounds generated in skin and the like. In addition, since the pysetin maintains excellent efficacy even when contained in a small amount, it can be used in various formulations as an effective ingredient for improving or preventing skin wrinkles, skin elasticity reduction or skin aging in medicines or cosmetics, have.

The picetin was found to promote the biosynthesis of the sulfated glycosaminoglycan and the collagen type I, thereby exhibiting the effect of keeping collagen type I and extracellular matrix constituents of the skin compact.

In order to examine the effect of picetin on human fibroblasts and keratinocytes in a specific embodiment, it was found that when picetin was treated with fibroblasts derived from human body, the production of collagen type I and sulfosuccinic glycosaminoglycan (Table 1 and Table 2). In order to examine the effect of the present invention on the expression of HAS-2 and HAS-3 in the picetin, picetine may promote the expression of HAS-2 and HAS-3. The expression of HAS-2 and HAS-3 was increased when treated with picetine (Table 3).

Accordingly, the cosmetic composition of the present invention may be a cosmetic composition for promoting synthesis of sulfated Glycosaminoglycan and / or promoting collagen synthesis.

In addition, the cosmetic composition of the present invention may be a cosmetic composition for moisturizing the skin.

The cosmetic composition containing the above phytetin can increase the production of glycosaminoglycans sulfated in the skin, accelerate the production of type I collagen and enhance the expression of HAS, thereby improving the skin, May be for improving or preventing skin aging, wrinkles of skin, lowering of skin elasticity, or lowering of skin moisture content.

It was experimentally confirmed that when the composition of the present invention was used, the skin moisture content and moisture retention capacity were increased (Table 4), and it was experimentally confirmed that skin elasticity improvement and anti-aging skin wrinkle prevention or improvement effect were excellent 5).

The term " skin aging " refers to a phenomenon of skin elasticity reduction, gloss reduction, wrinkle formation, weakening of regenerative power, or severe drying, which may be caused by time or external environment, Reduced extracellular matrix components, such as glycosaminoglycans, can be caused by a reduction in skin elasticity or wrinkles.

The term " skin wrinkles " of the present invention refers to the skin of the skin, which may be caused by a gene, a decrease in collagen present in the skin dermis, an external environment, etc., and an elastin and collagen, Skin wrinkles are produced when glycosaminoglycan sulfated to help.

The term " skin elasticity " is expressed by elastic fibers composed of elastin existing in the dermal layer. Such elastic fibers have a very low elastic modulus such as rubber, and are easily deformed by a small force. When removed, it easily returns to the original shape. The reduction of the sulfated glycosaminoglycan reduces collagen and elastin as well as makes it difficult to maintain the structure, resulting in reduced skin elasticity.

The term " moisturizing " means maintaining the homeostasis of the living body by appropriately adjusting water loss (moisture evaporation) and the like, and when the glycosaminoglycan sulfate sulfated together with hyaluronic acid in the skin is reduced, water loss may occur.

The term " prevention " refers to inhibiting or retarding skin aging or wrinkle formation, elasticity, or moisture content reduction, regardless of the cause of aging using the composition of the present invention, Refers to inhibiting or delaying the action of glycosaminoglycans sulfated and collagen type I in keratinocytes through the action of promoting biosynthesis of collagen type I.

The term " improvement " means any action that improves or alleviates the skin condition by maintaining or strengthening the ability of the skin to develop wrinkles, aging, and elasticity. Specifically, It means not only the reduction of elastin and collagen, but also the maintenance of their structure to improve the wrinkles, aging, elasticity or moisture content of the skin.

The content of phycetin contained in the composition may be included in an effective amount.

The term " effective amount " means the amount of picetin that can inhibit or delay the development of skin aging or wrinkles, or alleviate already formed wrinkles.

The effective amount of the picetin contained in the wrinkle-improving composition of the present invention will vary depending on the form in which the composition for improving wrinkles is commercialized, the method in which the picetin is applied to the skin, and the time on the skin. For example, when the composition for wrinkle improvement is commercialized as a medicament for dermatological treatment due to the formation of wrinkles of the skin, it may contain picetin at a higher concentration than that of a cosmetic product that is routinely applied to skin . In the case of a wash-off type cosmetic product such as a make-up removing agent, a detergent and the like in which the active ingredient remains on the skin in a short period of time even when it is commercialized as a cosmetic product, it may contain a relatively high concentration of phycetin. On the other hand, in the case of leave-on type cosmetics such as lotion, cream, essence, etc., in which the active ingredient remains on the skin for a long period of time, will be.

The content of the phytetin contained in the composition may be specifically 1 x 10 < ^-5 > to 10 wt% of the total composition. When the concentration of the component is less than 0.00001% by weight, the effect is difficult to obtain, and when the concentration exceeds 10% by weight, the overall processability of the composition such as solubility in a solvent is lowered and the use of the composition for various purposes have.

The preferred concentration of phycetin contained in the composition is 0.1 μg / ml to 100 μg / ml, more preferably 1 μg / ml to 50 μg / ml, still more preferably 5 μg / ml to 25 μg / ml Lt; / RTI >

The cosmetic composition may be used in any form that can be applied to the skin. Specific examples include solutions, suspensions, emulsions, pastes, gels, creams, lotions, powders, soaps, surfactant-containing cleansers, oils, foundations, lotions, cosmetic oils, sprays, packs, sunscreens, makeup bases, Removing agents and detergents, and is not limited to the above examples.

In addition, the cosmetic composition can be used as an external preparation for skin for enhancing skin elasticity, preventing skin aging, and improving skin wrinkles.

In one embodiment of the present invention, it has been confirmed that when picetin is manufactured into an external ointment or an essence formulation and applied to human skin, it exhibits excellent skin wrinkle-reducing effect. In particular, it has been confirmed that picetin exhibits excellent wrinkle-reducing effect even when applied at a low concentration level, that is, in a small amount.

The cosmetic composition containing picetine according to the present invention can be used as a cosmetically acceptable carrier, diluent, adjuvant, coloring agent, stabilizer, flavoring agent, surfactant, oil, humectant, alcohol, A pH adjuster and an ultraviolet screening agent. When the composition is used as a composition for external use on the skin, it may be in any form that can be applied to a skin such as a liquid, oil, cream, ointment, stick, pack, pasta, Is also available.

The cosmetic composition may further comprise a cosmetically acceptable excipient to facilitate its use and handling. The cosmetically acceptable excipient includes a surfactant, an emulsifier, a soap acid, a solvent, a binder, a diluent, a lubricant, a stabilizer, a perfume, water, a lower alcohol, a thickener, a chelating agent, a pigment, a preservative, a colorant, Antioxidants, antifoaming agents, antimicrobial agents, antifouling agents, enzymes, plant or mineral oils, fats, fluorescent substances, fungicides, flocculants, humectants, fragrances, fragrance carriers, preservatives, proteins, silicones, Blockers, vitamins, plant extracts or waxes. These may be used alone or in combination of two or more.

When the cosmetic composition is formulated into cosmetics, it may contain known dermatologically acceptable excipients that act as a carrier for the active ingredient. Specifically, the cosmetic composition may include International cosmetic ingredient dictionary, 6th ed., The cosmetic, Toiletry and Fragrance Association , Inc., Washington, 1995, which is incorporated herein by reference in its entirety. Which are incorporated herein by reference.

The present invention also relates to cosmetics comprising fisetin or a derivative thereof as an active ingredient.

The cosmetic may be any one selected from the group consisting of lotion, essence, skin, lotion, cream, and pack.

Examples of the cosmetics include a skin, a skin softener, a skin toner, an astringent, a lotion, a milk lotion, a moisturizing lotion, a nutrition lotion, a massage cream, a nutrition cream moisturizer cream, a hand cream, a purity, essence, Cleansing lotion, cleansing cream, body lotion and body cleanser, but the present invention is not limited thereto.

The present invention also relates to a pharmaceutical composition for preventing or treating skin damage diseases comprising fisetin or a derivative thereof as an active ingredient.

The present invention also relates to a medicament or a quasi-drug comprising the above pharmaceutical composition.

The pharmaceutical composition refers to a medicament for the purpose of diagnosing, treating, alleviating, treating or preventing an illness in an animal including a human being.

The skin damage disease refers to a disease caused by damage to the skin. Specifically, the skin damage disease is selected from the group consisting of erythema, skin aging, skin wrinkles, skin capillary blood vessels, skin elasticity reduction, It can be one.

The preferred dosage of the pharmaceutical composition of the present invention varies depending on the age, sex, weight, symptom, degree of disease, drug form, administration route and period of time of the subject, but can be appropriately selected by those skilled in the art. For the desired effect, the pharmaceutical composition of the present invention is preferably administered at 0.01 to 1000 mg / day. The administration can be done once a day or several times. In addition, the dose may be increased or decreased according to age, sex, weight, degree of disease, route of administration, and the like. Accordingly, the dose does not limit the scope of the present invention in any aspect.

The composition can be administered to mammals such as rats, mice, livestock, humans, and the like in a variety of routes including parenteral, oral, and the like, all manner of administration being expected, for example oral, rectal or intravenous, , Subcutaneous, intrauterine or intracerebroventricular injection.

The pharmaceutical composition for prevention or treatment of skin damage diseases according to the present invention may contain the above-mentioned phytetin as an active ingredient singly, and may be formulated into pharmaceutically acceptable carriers, excipients, diluents and / Or a subcomponent.

More specifically, in addition to the above-mentioned active ingredients, there may be further added nutritional agents, vitamins, electrolytes, flavors, coloring agents, aggravating agents, pectic acid and salts thereof, alginic acid and salts thereof, organic acids, protective colloid thickening agents, pH adjusting agents, Glycerin, alcohols, carbonating agents used in carbonated drinks, and the like.

The term "pharmaceutically acceptable" as used herein means physiologically acceptable and does not normally cause an allergic reaction such as gastrointestinal disorder, dizziness, or the like when administered to an animal, preferably a human. The pharmaceutically effective amount may be appropriately changed depending on the disease and its severity, the age, body weight, health condition, sex, administration route and treatment period of the patient.

Examples of the pharmaceutically acceptable carrier, excipient or diluent include lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, acacia rubber, alginate, gelatin, calcium phosphate, calcium silicate, Cellulose, methylcellulose, microcrystalline cellulose, polyvinylpyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate and mineral oil, propylhydroxybenzoate, talc, magnesium stearate and mineral oil , Dextrin, calcium carbonate, dextrin, calcium carbonate, propylene glycol, liquid paraffin, and physiological saline. However, it is not limited thereto, and any conventional carrier, excipient or diluent may be used.

The components may be added to the active ingredient picetine either independently or in combination.

The formulations of the pharmaceutical compositions may vary depending on the method of use and may be formulated using methods well known in the art to provide rapid, sustained or delayed release of the active ingredient after administration to the mammal . Examples of the formulations may be formulations selected from the group consisting of ointments, creams, tablets, pills, powders, granules, capsules, suspensions, solutions, emulsions, syrups, aqueous solutions, nonaqueous solutions, suspensions and emulsions .

The formulation may further contain an excipient such as an ordinary filler, an extender, a binder, a disintegrant, a surfactant, an anticoagulant, a lubricant, a wetting agent, a flavor, an emulsifier, an antiseptic, a sweetener, a fragrance or a preservative.

In general, solid dosage forms for oral administration include tablets, pills, soft or hard capsules, pills, powders and granules, which may contain one or more Excipients such as starch, calcium carbonate, sucrose or lactose, gelatin, and the like. In addition to simple excipients, lubricants such as magnesium stearate and talc may also be used.

In addition, liquid preparations for oral administration include suspensions, solutions, emulsions, and syrups. In addition to water or liquid paraffin, which is a commonly used simple diluent, various excipients, for example, Wetting agents, sweetening agents, perfumes, preservatives, and the like.

Examples which may be mentioned for skin administration are suitable for the production of dusting powders, emulsions, suspensions, oils, sprays, ointments, ointments, creams, pastes, gels, foams or solutions, and may be formulated as transdermal therapeutics (TTS) ) And / or excipients. The topical pharmaceutical preparations of the present invention may be semi-solid formulations, in particular ointments (ointments, suspension ointments), creams, gels or pastes. Lactic alcohol, cetyl alcohol, stearyl alcohol, fatty acids such as palmitic acid or stearic acid, liquid or solid paraffin or ozokerite, liquid or solid waxes, for example, For example, isopropyl myristate, natural or partially synthetic fats such as coconut fatty acid triglycerides, hydrogenated oils such as hydrogenated peanut or castor oil, or fatty acid partial esters of glycerol, such as glycerol monostearate or glycerol There is distearate. Suitable emulsifiers include surfactants, such as nonionic surfactants, such as polyalcohols or fatty acid esters of ethylene oxide adducts thereof, such as polyglycerol fatty acid esters or polyoxyethylene sorbitan fatty acid esters, sorbitan fatty acid esters such as Sterol or polyoxyethylene fatty alcohol ethers or fatty acid esters such as sorbitan oleate and / or sorbitan isostearate, such as, for example, an alkali metal salt of an anionic surfactant, for example a fatty alcohol sulfonate, Such as sodium lauryl sulfate, sodium cetyl sulfate or sodium stearyl sulfate, which are generally used in the presence of the fatty alcohols described above, for example cetyl alcohol or stearyl alcohol. Among them, it is possible to add an agent for preventing the drying of the cream, for example, a polyalcohol such as glycerol, sorbitol, propylene glycol and / or polyethylene glycol to the aqueous phase or to add a preservative, perfume or the like to the aqueous phase.

The pharmaceutical preparations of the present invention may be paraffinic, especially low viscosity paraffin, which may be an anhydrous ointment and which is suitable for topical use and is liquid at body temperature, or which contains the natural or partially synthetic fat, for example coconut fatty acid triglycerides Sorbitan monostearate and distearate, silicones such as polymethylsiloxane, such as hexamethyldisiloxane, or octamethyl triisostearate, such as, for example, glycerol monostearate and distearate, Siloxanes, and may contain, for example, fatty alcohols associated with aqueous creams and increasing water absorption capacity, and sterols, wool waxes, other emulsifiers and / or other additives.

In the present invention, when the pharmaceutical composition is formulated into pharmaceuticals, reference is made to Remington's Pharmaceutical Science, Mack Publishing Company, Easton PA, which is incorporated herein by reference.

In addition, the pharmaceutical composition of the present invention can be used alone for improving, alleviating, treating or preventing skin, or in combination with methods using surgery, hormone therapy, drug therapy and biological response modifier.

The numerical values set forth herein should be construed to cover equivalent ranges unless otherwise indicated.

Further, the present invention relates to a health functional food composition for improving or preventing skin aging, skin wrinkles, skin elasticity reduction, or skin moisture content, which comprises fisetin or a derivative thereof as an active ingredient.

The term "food" means a natural or processed product containing one or more nutrients. Preferably, the food refers to a state in which the food can be directly eaten through a certain degree of processing. In general terms, Functional foods, beverages, food additives and beverage additives.

The food may be, for example, various foods, beverages, gums, tea, a vitamin complex, a health functional food, and the like. In addition, in the present invention, the food may contain special nutritional foods (e.g., crude oil, spirits, infant food, etc.), meat products, fish products, tofu, jelly, noodles (Such as soy sauce, soybean paste, hot pepper paste, mixed sauce), sauces, confectionery (eg snacks), dairy products (eg fermented milk, cheese), other processed foods, kimchi, pickled foods (E.g., fruit and vegetable beverages, two oils, fermented beverages, etc.), natural seasoning (e.g., ramen soup, etc.).

The food, the functional food, the health functional food, the beverage, the food additive and the beverage additive can be produced by a usual production method.

In the present invention, the health functional food refers to a food group imparted with added value to function or express the function of the food by physical, biochemical, biotechnological techniques, etc., or to control the biological defense rhythm of the food composition, Means a food which is processed and designed so that the body control function related to restoration and the like is sufficiently expressed to the living body.

The health functional food may include food-acceptable food supplementary additives, and may further include suitable carriers, excipients and diluents conventionally used in the production of health functional foods.

In the present invention, beverage means a general term for drinking or enjoying a taste, and is intended to include a health functional beverage.

The above-mentioned beverage is not particularly limited as long as it contains the above-mentioned extract as an active ingredient as an essential ingredient at the indicated ratio, and may contain various flavors or natural carbohydrates as an additional ingredient such as ordinary beverages.

Examples of the natural carbohydrates include polysaccharides such as disaccharides such as monosaccharides such as glucose and fructose, maltose and sucrose, dextrin and cyclodextrin, and sugar alcohols such as xylitol, sorbitol and erythritol . The flavor may be a natural flavor such as tautatin or a stevia extract such as rebaudioside A or glycyrrhizin or a synthetic flavor such as saccharin, aspartame and the like.

The amount of the natural carbohydrate to be added may generally be about 1 to 20 g, preferably 5 to 12 g per 100 ml of the food composition of the present invention. In addition, the composition of the present invention may further contain flesh for the production of natural fruit juice, fruit juice drink, and vegetable drink.

In addition to the above, the food composition of the present invention can be used as a flavoring agent such as a variety of nutrients, vitamins, minerals (electrolytes), synthetic flavors and natural flavors, coloring agents and thickening agents (cheese, chocolate etc.), pectic acid and its salts, Salts thereof, organic acids, protective colloid thickeners, pH adjusting agents, stabilizers, preservatives, glycerin, alcohols, carbonating agents used in carbonated drinks, and the like.

These components can be used independently or in combination. The proportion of such an additive is not critical, but may be selected in the range of 0 to 2,000 parts by weight per 100 parts by weight of the extract of the present invention.

The health-functional beverage is used to control the bio-defense rhythm of the beverage group or beverage composition to which the added value is imparted so that the function of the beverage functions for a specific purpose by physical, biochemical, biotechnological, or the like, Means a beverage which has been designed so as to sufficiently express the body controlling function related to the living body.

The health functional beverage is not particularly limited to the other ingredients other than the picetine of the present invention as an essential ingredient at the indicated ratio, and may contain various flavors or natural carbohydrates as an additional ingredient such as ordinary beverages.

Examples of the natural carbohydrates include polysaccharides such as disaccharides such as monosaccharides such as glucose and fructose, maltose and sucrose, dextrin and cyclodextrin, and sugar alcohols such as xylitol, sorbitol and erythritol . The flavor may be a natural flavor such as tautatin or a stevia extract such as rebaudioside A or glycyrrhizin or a synthetic flavor such as saccharin, aspartame and the like.

The amount of the natural carbohydrate to be added may generally be about 1 to 20 g, preferably 5 to 12 g per 100 ml of the food composition of the present invention. In addition, the composition of the present invention may further contain flesh for the production of natural fruit juice, fruit juice drink, and vegetable drink.

In addition to the above, the food composition of the present invention can be used as a flavoring agent such as a variety of nutrients, vitamins, minerals (electrolytes), synthetic flavors and natural flavors, coloring agents and thickening agents (cheese, chocolate etc.), pectic acid and its salts, Salts thereof, organic acids, protective colloid thickeners, pH adjusting agents, stabilizers, preservatives, glycerin, alcohols, carbonating agents used in carbonated drinks, and the like. These components can be used independently or in combination. The proportion of such additives is not so critical, but may be selected in the range of 0 to 20 parts by weight per 100 parts by weight of the picetin of the present invention.

The health functional food may further contain food additives and the suitability of the food additives as a food additive is not limited to the standards and standards relating to the relevant items in accordance with the general provisions of the Food Additives Ordinance approved by the Food and Drug Administration, .

The extract of the present invention, which is added to foods containing beverages in the process of producing the health functional food of the present invention, can suitably increase or decrease its content as needed, and is preferably 0.00001 to 10 wt% As shown in Fig.

The invention also relates to the use of picetine for the manufacture of said cosmetic, pharmaceutical or food composition and to a method for improving the skin comprising applying or taking an effective amount of picetin to the skin.

Hereinafter, preferred embodiments of the present invention will be described in order to facilitate understanding of the present invention. However, the following examples are provided to further understand the present invention, and the present invention is not limited by the examples.

[ Example  1] Confirmation of promoting the synthesis of collagen type I in human fibroblasts

Pysetin was added to the culture medium of human fibroblasts to confirm the promoting effect of collagen synthesis at the cellular level. The picetin used was purchased from Sigma Aldrich (USA). The synthesized collagen was quantitated using a PICP EIA kit (Procollagen Type I C-Peptide Enzyme Immuno Assay Kit).

In the experiment, the final concentration of phy- ethin was 10 μg / ml and 20 μg / ml. Picetine was added to the culture medium of human-derived fibroblasts (DMEM medium) and cultured for 48 hours. After culturing, the degree of collagen synthesis was measured at 450 nm using a PICP EIA kit using a spectrophotometer at each concentration.

For the comparison of the effects, the degree of collagen synthesis was measured in the same manner in the culture medium of the fibroblasts to which nothing was added (control group) and the sample to which TGF-beta was added so as to have a final concentration of 10 ng / ml.

The increase rate of collagen production was calculated as a ratio of relative collagen production to the control group, and the results are shown in Table 1 below.

sample Collagen production (ng / ml)) Growth rate (%) Control group 178 - TGF-beta 10 ng / ml 470 164 Picetine 10 / / ml 297 67 Picetin 20 / / ml 335 88                                                  (Number of repetitions = 4)

[ Example  2] in human fibroblasts Sulfation Of glycosaminoglycan  Confirmation of synthesis promotion effect

Pysetin was added to the culture medium of human fibroblast to confirm the effect of promoting the synthesis of sulfosuccinic acid glycosaminoglycans at the cellular level. Measurement of glycosaminoglycan sulfate was quantitated using Blyscan glycosaminoglycan assay kit (Biocolor).

In the experiment, the final concentrations of picetin were 1 ㎍ / ml, 10 ㎍ / ml, and 20 ㎍ / ml. Pysetine was added to the human fibroblast culture medium (DMEM medium) for 24 hours, and then the culture broth was taken. The amount of total sulfated glycosaminoglycan was measured at each concentration by the Blyscan glycosaminoglycan assay kit And measured at 656 nm using a photometer.

The production increase rate of the sulfated glycosaminoglycan was calculated by the ratio of the amount of the sulfated glycosaminoglycan produced relative to the culture medium (control) of the fibroblasts to which nothing was added, and the results are shown in Table 2 below.

Samples (/ / ml) Production amount of glycosaminoglycan sulfate (ng / ml) Growth rate (%) Control group 0.46 -  1 g / ml of picetin 0.54 17 Picetine 10 / / ml 1.56 239.1 Picetin 20 / / ml 4.00 769.5                                                 (Number of repetitions = 4)

As shown in Table 2 above, it was confirmed that excellent synthesis effect of glycosaminoglycan sulfated sulfide was obtained at 10 占 퐂 / ml and 20 占 퐂 / ml, respectively, as compared with the control group not treated with picetin.

[ Example  3] Increased expression of hyaluronic acid synthase (HAS) gene by picetin in human keratinocytes

Human keratinocytes were cultured in DMEM medium containing 10% fetal bovine serum at a concentration of 1 × 10 ⁶ cells / ml, and 3000 μl of each was dispensed into a 6-well plate for 18 hours. Washed twice with non-DMEM medium. Picetine was treated at 1 ppm for 24 hours. Cells were recovered and total RNA was extracted with RNeasy mini kit (Qiagen), and 1 μg of RNA was quantified and reverse transcribed using GeneAmp ^® RNA PCR kit (Applied Biosystems). The reverse transcription reaction was performed using a Mycycler ^® PCR instrument (Biorad).

Quantitative real time PCR was performed using 2 μl of the reverse transcription reaction solution and Taqman ^® probe (Invitrogen, USA, HS02511055_S1, HS03929097_g1) of HAS-2, HAS-3 and GAPDH (Glyceraldehyde-3-phosphate dehydrogenase). Real time PCR was performed using a CFX96 Touch ^TM Real-Time PCR Detection System instrument (Biorad). Experimental results obtained by real time PCR were calculated by the method described in Livak KJ et al. (Methods, 2001, 25, 402-408) on the basis of the housekeeping gene GAPDH.

In addition, mRNA expression level of the picetin-treated experimental group was quantified with reference to the amount of mRNA expression of the negative control group (100%), and it is shown in Table 3.

sample No treatment
(Negative control) Glucosamine
100 ppm Physetine
1 ppm Physetine
10 ppm HAS-2
Expression level (%) 100 114 111 131 HAS-3
Expression level (%) 100 125 119 140

* Number of repetitions = 4

As shown in Table 3, the expression of hyaluronic acid synthase, particularly HAS-2 and HAS-3, was increased in keratinocytes derived from human body by treatment with phytoethin. In addition, picetine showed expression of HAS-2 and HAS-3 similar to the positive control even 100 times smaller than that of the positive control, and expression was 10 times smaller than that of the control group. It was confirmed that there is a moisturizing effect on the reduction of the excellent skin moisture retention even with a small amount of picetine.

[ Manufacturing example  1 and Comparative Example  1] Manufacture of ointment for external skin

Skin external ointment containing picetine as an active ingredient was prepared according to a conventional method as shown in the composition of Table 4 below. In addition, the ointment for external use for skin prepared from the other ingredients except for the active ingredient was prepared in Comparative Example 1.

Composition (% by weight) Production Example 1 (% by weight) Comparative Example 1 (% by weight) Physetine 0.2 0 Diethyl sebacate 8 8 Nonsense 5 5 Polyoxyethylene oleyl ether phosphate 6 6 Sodium benzoate One One vaseline to 100 to 100

[ Manufacturing example  2 and Comparative Example  2] Production of Essence

A cosmetic composition was prepared in the same manner as in Production Example 2, except that the cosmetic essence was prepared in the same manner as in Production Example 2, except that the active ingredient was not included in the formulation of the skin aging-preventing and wrinkle- Respectively. The detailed composition is shown in Table 5 below.

Composition (% by weight) Production Example 2 (% by weight) Comparative Example 2 (% by weight) Physetine 0.5 0 glycerin 10.0 10.0 Sodium hyaluronate aqueous solution (1%) 5.0 5.0 Polyoxyethylene hardened castor oil 1.0 1.0 Methyl paraoxybenzoate 0.1 0.1 Spices 0.05 0.05 Purified water to 100 to 100

[ Experimental Example  1] Confirm skin wrinkle improvement effect through panel test

For the essences of Preparation Example 2 and Comparative Example 2, the skin wrinkle-reducing effect was tested as follows for healthy 35- to 50-year-old women.

30 women aged 35 to 50 years were divided into two groups of 15 persons each. Group 1 contained the essence of Preparation Example 2 containing 0.5% of pysetin, Group 2 was the essence of Comparative Example 2, For 3 months. After 3 months, the improvement of skin wrinkles was evaluated by questionnaires. The subjects' questionnaires were compared with those before use with respect to improvement of skin wrinkles and elasticity. No improvement, slight improvement, and considerable improvement were determined in three stages, and the results are shown in Table 6 below.

Category (persons) No improvement Slight improvement A significant improvement Production Example 2 One 7 7 Comparative Example 2 9 4 2

As shown in Table 6, when the essence of Production Example 2 containing 0.5% of picetin was used, it was confirmed that the effect of improving skin wrinkles was superior to that of the essence of Comparative Example 2 which was not used.

[ Experimental Example  2] Through image analysis Cosmetics  Wrinkle improvement test of essence

The wrinkle-improving effect was evaluated for the essences of Preparation Example 2 and Comparative Example 2 through image analysis.

Specifically, the replica under the eye was sampled (Xantopren, Bayer) before the experiment was started, and the replica was sampled from the same site under the eyes immediately after the experiment was completed. The density of skin wrinkles was measured by analysis. The reduction rate of the skin wrinkle density by image analysis is a value obtained by averaging the ratio of the skin wrinkle density after use to the skin wrinkle density before use of the essence, and the measurement results are shown in Table 7 below.

Skin Wrinkle Density Reduction (%) Comparative Example 2 14 Production Example 2 56

As shown in Table 7, when the essence of Preparation Example 2 containing picetin was used, it was found that the effect of improving skin wrinkles was superior to that of Comparative Example 2 containing no picetin. No skin irritation or side effects due to the essence of Preparation Example 2 were found in the above test procedure.

Claims (11)

A cosmetic composition comprising fisetin or a derivative thereof as an active ingredient. The method according to claim 1,
Wherein said composition is for promoting the synthesis of sulfated Glycosaminoglycan. The method according to claim 1,
Wherein said composition is for promoting collagen synthesis. The method according to claim 1,
Wherein the composition is adapted for improving or preventing skin aging, wrinkles, skin elasticity or skin moisture content. The method according to claim 1,
Wherein the content of the phytetin contained in the composition is 1 x 10 < ^-5 > to 10 wt% of the total composition. 6. The method according to any one of claims 1 to 5,
The cosmetic composition may be in the form of a solution, a suspension, an emulsion, a paste, a gel, a cream, a lotion, a powder, a soap, a surfactant-containing cleansing oil, a foundation, a cosmetic liquid, a cosmetic ointment, , A makeup removing agent, and a detergent. Cosmetics containing fisetin or a derivative thereof as an active ingredient. A pharmaceutical composition for the prevention and treatment of skin damage diseases comprising fisetin or a derivative thereof as an active ingredient. 9. The method of claim 8,
Wherein said skin damage disease is selected from the group consisting of erythema, aging of the skin, wrinkles of the skin, capillaries of the skin, skin elasticity reduction and skin moisture-containing degradation. 9. The method of claim 8,
The pharmaceutical composition may be in a form selected from the group consisting of ointments, creams, tablets, pills, powders, granules, capsules, suspensions, solutions, emulsions, syrups, aqueous solutions, non-aqueous solutions, suspensions, A pharmaceutical composition for preventing and treating injurious disease. A composition for health functional food comprising fisetin or a derivative thereof as an active ingredient for improving or preventing skin aging, wrinkles, reduced skin elasticity, reduced skin moisture content, or aging.