KR20200047477A - Compositions for Improving Skin Wrinkles and Skin Whitening Using an Extract of Polygonum japonica - Google Patents

Abstract

Disclosed in the present invention is a composition for alleviating skin wrinkles and for skin whitening using an extract of Persicaria japonica which shows elastase inhibitory activity, and also shows tyrosinase inhibitory activity. An objective of the present invention is to provide the composition for alleviating skin wrinkles and for skin whitening using the extract of Persicaria japonica. The composition can be commercialized as food, cosmetics, drugs, etc.

Description

Composition for Improving Skin Wrinkles and Skin Whitening Using an Extract of Polygonum japonica

The present invention relates to a composition for improving skin wrinkles and whitening skin using an extract of Polygonum japonica.

Skin occupies about 16% of the human body, and is directly in contact with the external environment, and plays an important role in protecting the human body from external harmful factors such as temperature, humidity, and ultraviolet rays. The skin is composed of the epidermis, dermis, and subcutaneous tissue under the keratin. The epidermis is composed mainly of keratinocytes made of keratin, immune cells such as melanocytes that produce and secrete melanin, and Langerhans cells, and a thin protective layer composed of perceptual cells (Merkel's copuscles). It prevents external stimulation and invasion of pathogens and regulates body temperature and maintains moisture and lipid components. The dermis is a connective tissue under the epidermis and is mostly composed of a network of macromolecules called extracellular matrix. This extracellular epilepsy is made from fibroblasts and is composed of fibrous proteins such as collagen and elastin and polysaccharides such as hyaluronic acid.

With age, skin cells are damaged due to various contaminants, strong ultraviolet rays, stress, and malnutrition, and cell proliferation is not smooth, resulting in wrinkles, loss of elasticity, pigmentation and keratinization in the skin ( Gilchrest BA, J. Am. Acad. Dermatol, 21, 610. 1989).

Collagen is the most important protein for maintaining skin moisture and maintaining skin flexibility and elasticity. It accounts for 90% of the dermal layer (J Am Acad Dermatol, 17 (4): 610-613. 2001) and gives skin strength and tension To protect the skin from external stimuli. In addition, elastin in the dermal layer occupies about 2%, so it is less than collagen, but it plays a role in supporting collagen fibers, and many studies have reported that deficiency, aggregation, and loss of elastin fibers play an important role in the mechanism of skin wrinkle formation. (Weihermann AC et al., Int J Cosmet Sci. 2017 Jun; 39 (3): 241-247; Mora Huertas AC et al., Biochimie. 2016 Sep-Oct; 128-129: 163-73).

Collagen and elastin are synthesized in fibroblasts and degraded by collagenase or elastase. With age or exposure to UV light, the action of fibroblasts and the number of cells decreases, reducing the amount of collagen or elastin synthesis and increasing the action of collagenase or elastase to break them down. The elasticity of the skin due to collagen and elastin is very difficult to recover after being reduced once. Accordingly, research to improve skin wrinkles by inhibiting increasing elastase activity with age has been actively conducted.

Retinoic acid and retinol (Simon C et al., J Invest Dermatol 98: 248-260. 1992; Elaine S et al., J Invest Dermatol 96: 975-978. 1991) The effect is proven, dehydroepiandrosterone (Shin MH et al., J Invest Dermatol 124: 315-323.2005), ginsenoside Rg3 extracted from ginseng (Kim SW et al., J Soc Cosmet Scientists Korea 30: 221-225.2004), flavonoid ( Francesco B et al., Int J Pharm 145: 87-94.1996), red bean extract (Korea Patent No. 101008833), yeonkyo extract (Korea Patent No. 100825450), etc. Became. However, some substances have limitations in their use because they have low stability or cause skin irritation and safety problems. Accordingly, the search for substances having excellent wrinkle improvement activity effects and safety and stability continues.

It is known that melanin is synthesized from melanocytes, which are color cells present in the base layer in the skin (epidermis), and is metastasized to peripheral keratinocytes, and is known to exhibit human skin color. When the skin receives sunlight, melanin is produced by chemical reactions in melanocytes, pigment-forming cells. The main role of melanin is to protect the inside of the skin by removing free radicals and free radicals generated by the skin (Brain Research Bulletin 10 (6): 847 851, 1983; Mutation Research) 571 (1): 121-2, 2005; Nature. 22; 445 (7130): 843-50. 2007). However, overexpression of melanin significantly affects not only skin health such as skin darkening, pigmentation, blemishes, freckles, skin cancer, but also aesthetics (Pigment Cell Res 10, 127-138. 1997; Vet Dermatol. 2003 Apr; 14 (2) ): 57-65.).

The starting material for melanin is tyrosine, a type of amino acid normally present in the human body. Tyrosine is oxidized in the melanocytes by an enzyme called tyrosinase to turn into dopa (dihydroxy phenylalanine, DOPA), and dopa further oxidizes to produce dopaquinone (DOPA-Quinone). And when dopaquinone encounters cysteine, cysteinyldopa is produced, resulting in a reddish-brown pheomelanin. The produced melanin is then carried on a melanosome and delivered to keratinocytes (Pigment Cell Res. 12 (1): 4-12.1999 .; Cell Mol Biol (Noisy-le-grand). 45 (7): 981 -90.1999; An Bras Dermatol. 88 (1): 76-3. 2013).

Accordingly, the basic mechanisms of pharmaceuticals formulated in whitening cosmetics for the purpose of preventing or alleviating pigmentation are inhibiting tyrosinase action, inhibiting tyrosinase production, inhibiting melanin-producing mediator, reducing and inhibiting strong oxidation of melanin, excretion of melanin And promotes UV protection. Representative materials that inhibit the activity of tyrosinase include arbutin and kojic acid. Materials that directly destroy melanin include hydroquinone and mercury, but mercury is prohibited as a toxic substance. Whitening agents that reduce the produced melanin include vitamin C, glutathione, and magnesium ascorbate phosphate (J Cosmet Sci.65 (6): 365-75. 2014; Int J Cosmet Sci.37 ( 6): 567-73. 2015; Yakugaku Zasshi. 128 (8): 1203-7. 2008; Int J Cosmet Sci. 27 (3): 147-53. 2005; Acta Derm Venereol.63 (3): 209- 14.1983; Skin Pharmacol Appl Skin Physiol. 13 (3-4): 143-9. 2000; J Cosmet Laser Ther. 15 (2): 107-13. 2013.).

As interest in whitening has increased, the development of whitening cosmetics with more excellent effects in addition to the well-known substances has been actively conducted, but synthetic whitening materials have problems such as decomposition, coloring, odor, stability and safety during use. have. Therefore, recently, studies on natural whitening agents that do not affect cells and reduce melanin synthesis have been actively conducted.

The present invention discloses a skin wrinkle improving activity and a skin whitening activity of the extract of white flowers.

An object of the present invention is to provide a composition for improving skin wrinkles and whitening skin using an extract of white flowers.

Other or specific objects of the present invention will be presented below.

The present invention was completed by confirming that the extract of the white flower quenched showed elastase inhibitory activity and also showed tyrosinase inhibitory activity, as confirmed in the Examples and Experimental Examples below.

In view of the above, the present invention can be identified as a composition for improving skin wrinkles containing an extract as a white flower in one aspect as an active ingredient, and in another aspect as a composition for skin whitening comprising an extract as a white flower as an active ingredient Can grasp.

On the other hand, as confirmed in the Examples and Experimental Examples below, the present inventors macrophages (Ito T., et al., Curr Drug Traget Inflamm Allergy, 2 (3): 257-265, which play a pivotal role in the inflammatory response. 2003) After inducing the inflammatory reaction by treating LPS (lipopolysaccharide), the white flower extract was treated by concentration to evaluate the level of nitrogen oxide (NO) production. Inhibition was confirmed (IC ₅₀ = 45.29 µg / ml), and it was confirmed that there was no specific cytotoxicity even at the highest treatment concentration of 100 µg / ml.

Nitric oxide is synthesized from L-arginine by the action of nitric oxide synthase (NOS), and NOS has several isoforms. BNOS (brain NOS) present in the brain, nNOS (neuronal NOS) present in the nervous system, and eNOS (endothelial NOS) present in the vascular endothelial system are always expressed at a certain level in the body, and monoxide produced in small amounts by these Nitrogen (NO) plays an important role in maintaining homeostasis by performing various physiological reactions related to blood pressure regulation, neurotransmission, learning, and memory. On the other hand, iNOS (induced NOS), whose expression is induced by a certain stimulus, generates excessive NO, and nitric oxide, which is excessively generated by iNOS, reacts with superoxide to form peroxynitrite. It acts as a powerful oxidizing agent and damages cells, thereby engaging in various pathological processes including inflammation and cancer (Gupta SC et al., Exp Biol Med., 236: 658-671, 2011; Riehemann et al., FEBS Lett., 442: 89-94, 1999; Stamler et al., Science, 258: 1898-1902, 1992).

In consideration of the above, the present invention can provide a composition for inhibiting nitric oxide production, which includes an extract as an active ingredient in another aspect in another aspect. This composition of the present invention can be usefully used for inflammatory diseases caused by excessive production of nitrogen oxide. Such inflammatory diseases include asthma, allergic and non-allergic rhinitis, chronic and acute rhinitis, chronic and acute gastritis or enteritis, ulcerative gastritis, acute and chronic nephritis, acute and chronic hepatitis, chronic obstructive pulmonary disease, pulmonary fibrosis, hypersensitivity Colorectal syndrome, inflammatory pain, migraine, headache, back pain, fibromyalgia, fascia disease, viral infections (such as type C infection), bacterial infections, fungal infections, burns, wounds caused by surgical or dental surgery, prostaglas Dean E hypersyndrome, atherosclerosis, gout, arthritis, rheumatoid arthritis, ankylosing spondylitis, Hodgkin's disease, pancreatitis, conjunctivitis, iris, scleritis, uveitis, dermatitis (including atopic dermatitis), eczema, multiple sclerosis, etc. have.

On the other hand, in the present specification, the term "white flower extract" refers to white flower extract outpost, leaves, stems, ground parts, roots, roots, underground parts, seeds or mixtures thereof, water, and lower alcohols having 1 to 4 carbon atoms (methanol, ethanol, butanol). Etc.), methylene chloride, ethylene, acetone, hexane, ether, chloroform, ethyl acetate, butyl acetate, N, N-dimethylformamide (DMF), dimethyl sulfoxide (DMSO), 1,3-butylene glycol, propylene glycol Or it means the extract obtained by leaching using these mixed solvents, the extract obtained using a supercritical extraction solvent such as carbon dioxide, pentane, or a fraction obtained by fractionating the extract, and the extraction method is the polarity of the active substance, the degree of extraction, preservation In consideration of the degree, any method such as cold acupuncture, reflux, warming, ultrasonic radiation, and supercritical extraction can be applied. In the case of fractionated extracts, the fractions obtained by suspending the extracts in a specific solvent and mixing and policing with a solvent of different polarity, adsorb the crude extract on a column filled with silica gel, etc., and then use a hydrophobic solvent, a hydrophilic solvent or a mixed solvent thereof. It means that it contains the fraction obtained as a mobile phase. In addition, the meaning of the extract includes a concentrated liquid extract or a solid extract in which the extraction solvent is removed by a method such as freeze drying, vacuum drying, hot air drying, spray drying, and the like. Preferably, it means an extract obtained by using water, lower alcohol having 1 to 4 carbon atoms (methanol, ethanol, butanol, etc.) or a mixed solvent thereof.

In addition, in the present specification, "active ingredient" refers to a component that can exhibit the desired activity alone or itself can exhibit activity with an inactive carrier.

In addition to the active ingredient, the composition of the present invention has similar activity, such as skin wrinkle improvement effect or skin whitening effect, enhancing or strengthening, or inhibiting skin hypersensitivity reaction, skin protection activity (suppressing skin damage caused by ultraviolet rays, moisturizing skin, etc.) In order to enhance the convenience of intake, intake, and use through addition, it may further include any compound or natural extract already known in the art for safety and having a corresponding activity.

These compounds or extracts include the National Pharmacopoeia ("Korea Pharmacopoeia" in Korea), the national health functional food fair (in Korea, the "Ministry of Food and Drug Administration" is the "Standards and Standards for Health Functional Food"), the functional cosmetic fair in each country (Korea Food and Drug Administration Notification Compounds or extracts listed in the fair, such as "Standards and Test Methods for Functional Cosmetics"), compounds or extracts that have been approved as items in accordance with the laws of each country governing the manufacture and sale of pharmaceuticals ("Pharmacist Law" in Korea), health Laws governing the manufacture and sale of functional foods in accordance with the laws of each country governing the manufacture and sale of functional foods (in Korea, the 「Act on Health Functional Foods」) ”) Includes compounds or extracts whose functionality is recognized.

These ingredients include, for example, arbutin, niacinamide, ascorbyl glucoside, alpha-bisabolol, and oil-soluble licorice, recognized as skin whitening ingredients in the Cosmetics Fair (Korea Food and Drug Administration notice, `` Standards and Specifications for Functional Cosmetics '') UV protection in the Korean cosmetic industry, such as retinol, retinyl palmitate, adenosine, polyethoxylated amide, etc., which have been recognized as ingredients for improving skin wrinkles in the same Korean cosmetic industry, such as extract (Oil Soluble Licorice (Glycyrrhiza) Extract) Compounds such as drometrizole, drometrizoletrisiloxane, digalloyltrioleate, dimethycodiethyl benzalmalonate, diethylhexylbutamidotriazone, pine bark extract, phosphatidylserine, fingerroot Extract powders, and complex extracts such as red ginseng and cornus officinalis. Law in accordance with the Examples of the "sensitive skin condition improved, the functional components may include L. sakei Probio 65, gamma-linolenic acid-containing oil, derived from lactic acid bacteria in gwachae L.plantarum CJLP133, probiotics such as ATP. These compounds or natural extracts may be included in the composition of the present invention together with one or more of its active ingredients.

The composition of the present invention may contain the active ingredient in any amount (effective amount) as long as it can exhibit wrinkle improvement activity, skin whitening activity, NO production inhibitory activity, etc. intended to be treated according to use, formulation, formulation purpose, etc. , A typical effective amount will be determined within the range of 0.001% to 15% by weight based on the total weight of the composition. Here, the "effective amount" is intended to improve wrinkles, skin whitening effect, NO production suppression effect, etc. when the composition of the present invention is administered to a mammal, preferably a human, or a human subject to which the application is applied, by a recommendation such as medical or skin experts. It refers to the amount of active ingredient contained in the composition of the present invention, which can exhibit a dermatological and medical effect. Such an effective amount can be determined empirically within the ordinary skill in the art.

In the specific aspect, the composition of the present invention can be grasped as a food composition.

The food composition of the present invention can be produced in any form, such as tea, juice, carbonated beverages, beverages such as ionic beverages, processed oils such as milk, yogurt, gums, rice cakes, Chinese medicines, breads, cookies, noodles, etc. Food, tablets, capsules, pills, granules, liquids, powders, flakes, pastes, syrups, gels, jelly, bars, etc. can be prepared as health functional food formulations.

In addition, the food composition of the present invention can be classified into any product as long as it complies with the enforcement regulations at the time of manufacturing and distribution in the legal and functional classification. For example, it is a health functional food pursuant to the law of the country of exclusion governing the manufacture and sale of health functional food (in Korea, it is the 「Act on Health Functional Food」), or the law of an exempt country governing the manufacture and sale of food (in Korea It can be confectionery, soybean, soy milk, fermented beverage, special purpose food, etc. according to each food type according to the food fair (in accordance with the Food Sanitation Act) (in Korea, the Korean Food and Drug Administration's "Standards and Standards for Food").

Food composition of the present invention may include a food additive in addition to the active ingredient. Food additives can be generally understood as substances added to foods, mixed or infiltrated in the manufacture, processing, or preservation of foods, and their safety must be ensured because they are consumed daily and for a long time with foods. Food additives in accordance with national laws governing the manufacture and distribution of food ("Food Sanitation Act" in Korea) are limited in terms of ingredients or functions in terms of safety and food additives. In the Korean Food Additives Fair (Korea Food and Drug Administration's notice, `` Food Additive Standards and Standards ''), food additives are classified into chemical synthetic products, natural additives and mixed preparations in terms of ingredients, and these food additives are sweeteners and flavors in terms of functionality It is divided into agents, preservatives, emulsifiers, acidulants, and thickeners.

Sweeteners are used to impart a moderate sweetness to food, and both natural and synthetic can be used in the composition of the present invention. Preferably, a natural sweetener is used, and examples of the natural sweetener include sugar sweeteners such as corn syrup solids, honey, sucrose, fructose, lactose, and maltose.

Flavoring agents can be used to enhance the taste or aroma, and both natural and synthetic can be used. Preferably, it is the case of using a natural thing. In addition to flavor, when using natural ones, the purpose of enhancing nutrition can also be combined. As a natural flavoring agent, it may be obtained from apples, lemons, citrus fruits, grapes, strawberries, peaches, etc., or may be obtained from green tea leaves, perilla, large leaves, cinnamon, chrysanthemum leaves, jasmine, and the like. In addition, those obtained from ginseng (red ginseng), bamboo shoots, aloe vera, and ginkgo can be used. Natural flavoring agents may be liquid concentrates or solid extracts. In some cases, synthetic flavoring agents may be used, and synthetic flavoring agents may include esters, alcohols, aldehydes, terpenes, and the like.

As a preservative, sodium sorbate, sodium sorbate, potassium sorbate, calcium benzoate, sodium benzoate, potassium benzoate, EDTA (ethylenediaminetetraacetic acid), etc. can be used, and as an emulsifier, acacia gum, carboxymethylcellulose, xanthan gum, Pectin and the like, and as the acidulant, arithmetic, malic acid, fumaric acid, adipic acid, phosphoric acid, gluconic acid, tartaric acid, ascorbic acid, acetic acid, phosphoric acid and the like can be used. The acidulant may be added so that the food composition has an appropriate acidity for the purpose of suppressing the growth of microorganisms in addition to the purpose of enhancing taste.

As a thickener, a suspending agent, sedimentation agent, gel forming agent, swelling agent, etc. may be used.

The food composition of the present invention may include bioactive substances or minerals known in the art for the purpose of supplementing and reinforcing functional and nutritional properties in addition to the food additives described above, and guaranteed stability as food additives.

Examples of such bioactive substances include catechins contained in green tea, vitamins such as vitamin B1, vitamin C, vitamin E, and vitamin B12, tocopherol, dibenzoyl thiamine, and the like, and calcium preparations such as calcium citrate and magnesium stearate as minerals Magnesium preparations such as iron, iron preparations such as iron citrate, chromium chloride, potassium iodide, selenium, germanium, vanadium, zinc, and the like.

The food composition of the present invention may include the food additives as described above in an appropriate amount to achieve the purpose of addition according to the product type.

With regard to other food additives that may be included in the food composition of the present invention, it is possible to refer to national foods or food additives.

The composition of the present invention can be identified as a pharmaceutical composition in other specific embodiments.

In particular, when the composition for skin whitening of the present invention is identified as a pharmaceutical composition, the target disease may be understood as skin hyperpigmentation, and specific examples of such hyperpigmentation include freckles, senile plaques, liver spots, spots, brown or black spots, and sunlight Hyperpigmentation after use of medications such as plaques, blue melasma, calcium antagonists, sequelae following sclerotherapy, gestational chloasma, and black derma in women taking oral contraceptives , Hyperpigmentation, phototoxic reaction, or other similar small, fixed pigmented lesions after inflammation due to wounds or dermatitis, including scratches and burns, but is not limited thereto.

The pharmaceutical composition of the present invention may be prepared in an oral dosage form or a parenteral dosage form according to the route of administration by a conventional method known in the art, including a pharmaceutically acceptable carrier in addition to the active ingredient. Here, the route of administration may be any suitable route including a local route, an oral route, an intravenous route, an intramuscular route, and direct absorption through mucosal tissue, and two or more routes may be used in combination. An example of a combination of two or more routes is when two or more formulations of the drug are combined according to the route of administration, for example, when one drug is administered by intravenous route and the second drug is administered by topical route.

Pharmaceutically acceptable carriers are well known in the art depending on the route of administration or formulation, and specifically refer to the pharmacopeia of each country, including "Korea Pharmacopoeia".

When the pharmaceutical composition of the present invention is prepared in an oral dosage form, powders, granules, tablets, pills, dragees, capsules, liquids, gels, syrups, suspensions, wafers according to methods known in the art with suitable carriers And the like. Examples of suitable carriers at this time include sugars such as lactose, glucose, sucrose, dextrose, sorbitol, mannitol, xylitol, starches such as corn starch, potato starch, wheat starch, cellulose, methylcellulose, ethylcellulose, sodium carboxymethylcellulose, Celluloses such as hydroxypropyl methylcellulose, polyvinyl pyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, magnesium stearate, mineral oil, malt, gelatin, talc, polyol, vegetable oil, ethanol, green Serol, etc. are mentioned. In the case of formulation, if necessary, suitable binders, lubricants, disintegrants, colorants, diluents, etc. may be included. Suitable binders include starch, magnesium aluminum silicate, starch ferist, gelatin, methylcellulose, sodium carboxymethylcellulose, polyvinylpyrrolidone, glucose, corn sweetener, sodium alginate, polyethylene glycol, wax, etc., and lubricants include oleic acid Sodium, sodium stearate, magnesium stearate, sodium benzoate, sodium acetate, sodium chloride, silica, talcum, stearic acid, magnesium salts and calcium salts thereof, polydetylene glycol, and the like, and starch and methyl cellulose as disintegrants , Agar, bentonite, xanthan gum, starch, alginic acid or its sodium salt. Moreover, lactose, dextrose, sucrose, mannitol, sorbitol, cellulose, glycine etc. are mentioned as a diluent.

When the pharmaceutical composition of the present invention is prepared in a parenteral dosage form, it may be formulated in the form of injections, transdermal administrations, nasal inhalants and suppositories according to methods known in the art with suitable carriers. When formulated as an injectable agent, an aqueous isotonic solution or suspension may be used as a suitable carrier. Specifically, an isotonic solution such as PBS (phosphate buffered saline) containing triethanol amine, sterile water for injection, or 5% dextrose may be used. . When formulated as a transdermal dosage form, it can be formulated in the form of ointments, creams, lotions, gels, external solutions, pasta, linen agents, aerosols, and the like. For nasal inhalers, dichlorofluoromethane, trichlorofluoromethane, dichlorotetrafluoroethane, carbon dioxide, etc. can be formulated in the form of an aerosol spray using a suitable propellant. witepsol), tween 61, polyethylene glycols, cacao butter, laurin, polyoxyethylene sorbitan fatty acid esters, polyoxyethylene stearate, sorbitan fatty acid esters, and the like.

Regarding the specific formulation of the pharmaceutical composition, it is known in the art, and for example, see Remington's Pharmaceutical Sciences (19th ed., 1995) and the like. The above documents are regarded as part of this specification.

Preferred dosages of the pharmaceutical compositions of the present invention range from 0.001 mg / kg to 10 g / kg per day, preferably 0.001 mg / kg to 1 g per day, depending on the patient's condition, weight, sex, age, patient severity, and route of administration. / kg range. Administration can be made once a day or divided into several times. Such dosages should not be construed as limiting the scope of the invention in any aspect.

In another specific aspect, the composition of the present invention can be identified as a cosmetic composition. When the anti-inflammatory composition of the present invention is identified as a cosmetic composition, its use may be understood as relief of inflammatory skin irritation.

Even if the composition of the present invention is identified as a cosmetic composition, the cosmetic composition may have any product classification in accordance with its use, and in particular, it has functionalities such as improving skin trouble, enhancing skin whitening, and improving atopic dermatitis. Cosmetics, non-functional general cosmetics, and the like. As for the product form, any product form can be taken, specifically, solutions, suspensions, emulsions, pastes, gels, creams, lotions, powders, soaps, surfactant-containing cleansing, oils, powder foundations, emulsion foundations, waxes It can take the form of products such as foundations and sprays. In a specific product form, it may be flexible lotion, nutrition lotion, nutrition cream, massage cream, essence, eye cream, cleansing cream, cleansing foam, cleansing water, pack, spray or powder formulation.

The cosmetic composition of the present invention may include, in addition to its active ingredients, ingredients commonly used in cosmetic compositions, such as stabilizers, solubilizers, surfactants, vitamins, pigments and conventional auxiliary agents such as colorants and carriers.

When the formulation of the present invention is a paste, cream or gel, animal oil, vegetable oil, wax, paraffin, starch, trakant, cellulose derivative, polyethylene glycol, silicone, bentonite, silica, talc or zinc oxide, etc. may be used as a carrier component. You can.

When the formulation of the present invention is a powder or a spray, lactose, talc, silica, aluminum hydroxide, calcium silicate or polyamide powder can be used as a carrier component, and in the case of a spray, additionally chlorofluorohydrocarbon, propane / Propellant such as butane or dimethyl ether.

When the formulation of the present invention is a solution or emulsion, a solvent, solubilizer or emulsifier is used as a carrier component, specifically water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene glycol, 1,3-butyl glycol oil, glycerol aliphatic ester, polyethylene glycol, fatty acid ester of sorbitan, and the like can be used.

When the formulation of the present invention is a suspension, liquid diluents such as water, ethanol or propylene glycol as carrier components, ethoxylated isostearyl alcohol, suspending agents such as polyoxyethylene sorbitol esters, polyoxyethylene sorbitan esters, and microcrystals Sex cellulose, aluminum metahydroxide, bentonite, agar and the like can be used.

When the formulation of the present invention is a surfactant-containing cleansing, aliphatic alcohol sulfate, aliphatic alcohol ether sulfate, sulfosuccinic acid monoester, isethionate, imidazolinium derivatives, methyltaurate, sarcosinate, fatty acid amide as a carrier component Ether sulfates, alkylamidobetaines, aliphatic alcohols, fatty acid glycerides, fatty acid diethanolamides, vegetable oils, lanolin derivatives or ethoxylated glycerol fatty acid esters and the like can be used.

The cosmetic composition of the present invention can be prepared according to the manufacturing method of a cosmetic composition that is conventionally performed in the art, except that it contains an active ingredient that exhibits skin wrinkle improvement activity and skin whitening activity.

As described above, according to the present invention, it is possible to provide a composition for improving skin wrinkles and a skin whitening composition using an extract of white flowers.

Such a composition of the present invention can be commercialized as food, cosmetics, and drugs.

Figure 1 is a result showing the elastase inhibitory activity of the extract of white flowers.
Figure 2 is a result showing the tyrosinase inhibitory activity of the white flower yeokkyeot extract.

Hereinafter, the present invention will be described with reference to Examples and Experimental Examples. However, the scope of the present invention is not limited to these examples and experimental examples.

<Example> Preparation of extracts of white flowers

After adding 20% by weight of 70% ethanol to the white flower Yeo Yeok (outpost) powder and leaching it for 24 hours, it was filtered with Whatman paper filter paper No.2, and the filtrate was concentrated under reduced pressure to prepare a white flower Yeogyeot extract.

<Experimental Example> Elastase inhibitory activity experiment, tyrosinase inhibitory activity experiment, etc.

<Experimental Example 1> Elastase inhibitory activity experiment

After adding a sample diluted by concentration to 50 mM Tris-Cl buffer (pH 8.5), 1 mg / ml N-succinyl- (Ala) ₃ -p-nitroanilide of substrate was added to 50 mM Tris-Cl buffer (pH 8.5). 0.6 U / ml PPE (porcine pancreas elastase) was added, mixed well, and reacted at 25 ° C to measure absorbance at 405 nm using an ELISA reader. The results are shown in FIG. 1 as a percentage of the sample-untreated group. Ursolic acid was used as a positive control.

As can be seen in FIG. 1, the extract of white flowers showed an elastase inhibitory activity in a concentration-dependent manner, and showed an inhibitory activity close to 80% even at the lowest treatment concentration of 100 μg / ml, resulting in an IC ₅₀ of 100 μg / ml.

<Experimental Example 2> Tyrosinase inhibitory activity experiment

After adding a sample diluted by concentration to 0.1 M potassium phosphate buffer (pH 6.5) and 1250 unit / ml mushroom-derived tyrosinase, mix well by adding 1.5 mM L-tyrosine as a substrate, and react at 37 ° C for 20 minutes, then 490 nm Absorbance is measured using an ELISA reader. Arbutin was used as a positive control, and the results are shown in FIG. 2 as a percentage of the sample-untreated group.

As can be seen in FIG. 2, the white flower extract showed tyrosinase inhibitory activity in a concentration-dependent manner, and the IC ₅₀ was 431.12 μg / ml.

<Experiment 3> Anti-inflammatory activity experiment-NO production inhibitory activity experiment in macrophages

In order to evaluate the anti-inflammatory activity of the extract of the above Example in RAW264.7 cell, which is a mouse macrophage cell, it was dispensed with a cell number of 5 × 10 ⁴ cells / well in a 96 well plate and 24 hours under conditions of 37 ° C. and 5% CO ₂ . While incubating. After treating the sample in a 96 well plate for each concentration for 1 hour, 1 μg / ml of LPS (Lipopolysacharide) was treated and cultured for 24 hours to be used for anti-inflammatory activity evaluation. To evaluate anti-inflammatory activity through NO assay, griess A and B reagents were used, and 1% sulfanilamide and 0.1% N- (1-naphtyl) ethylenediamine dihydrochloride reagent were mixed in a 1: 1 ratio. After processing the sample in a 96 well plate, supernatant of the medium cultured for 24 hours at 37 ° C and 5% CO ₂ was mixed with griess (A + B) reagent in a 1: 1 ratio of 50 μl each and stored at room temperature for 10 minutes. After that, by measuring the ELISA at 540 nm, the inhibition of NO production was compared to the control group, which is a sample-free group, and IC ₅₀ was obtained. As a result, IC ₅₀ was found to be 45.29 μg / ml.

Cytotoxicity was measured by MTT method. Specifically, the medium remaining in the 96 well plate was removed, and serum free medium containing 10% of 5 mg / ml MTT solution was added to each 100ul per well, and then placed in a 37 ° C, 5% CO ₂ incubator to react for 2 hours. After removing the medium, DMSO was added to 100 µl / well and dissolved in a shaker for 15 minutes to measure the absorbance at 540 nm using an ELlSA reader to determine the cell viability to confirm the toxicity of the sample. There was no particular cytotoxicity at the highest treatment concentration of 100 μg / ml.

Claims (12)

A composition for improving skin wrinkles, which contains an extract of white flowers.
According to claim 1,
The extract is a composition characterized in that water, ethanol, or a mixed solvent extract thereof
The method according to claim 1 or 2,
The composition is characterized in that the pharmaceutical composition.
The method according to claim 1 or 2,
The composition is characterized in that the food composition.
The method according to claim 1 or 2,
The composition is characterized in that the cosmetic composition.
A composition for skin whitening that contains an extract of white flowers as an active ingredient.
The method of claim 6,
The extract is a composition characterized in that water, ethanol, or a mixed solvent extract thereof
The method of claim 6 or 7,
The composition is characterized in that the pharmaceutical composition.
The method of claim 6 or 7,
The composition is characterized in that the food composition.
The method of claim 6 or 7,
The composition is characterized in that the cosmetic composition.
A composition for inhibiting NO production, comprising an extract as a white flower.
The method of claim 11,
The extract is a composition characterized in that the extract of water, ethanol, or a mixed solvent thereof.

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