KR102322974B1 - Compositions for Improving Skin Wrinkles Using an Extract of Boehmeria tricuspis var. unicuspis - Google Patents

Abstract

The present invention discloses a composition for improving skin wrinkles using a turtle tail extract showing elastase inhibitory activity.

Description

Compositions for Improving Skin Wrinkles Using an Extract of Boehmeria tricuspis var. unicuspis}

The present invention relates to a composition for improving skin wrinkles using an extract of a turtle tail ( Boehmeria tricuspis var. unicuspis ).

The skin accounts for about 16% of the human body, and because it is in direct contact with the external environment, it 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 a thin protective layer composed of keratinocytes, which are mainly made of keratin, melanocytes that produce and secrete melanin, immune cells such as Langerhans cells, and Merkel's copuscles. It prevents external stimuli and pathogens from entering, regulates body temperature, and maintains moisture and lipid components. The dermis is a connective tissue beneath the epidermis and is mostly composed of a network of macromolecules called extracellular matrix. This extracellular matrix is made from fibroblasts and consists of fibrous proteins such as collagen and elastin, and polysaccharides such as hyaluronic acid.

As we age, skin cells are damaged due to various contaminants, strong ultraviolet rays, stress, and nutritional deficiencies. 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, and it occupies 90% of the dermal layer (J Am Acad Dermatol, 17(4):610-613. 2001) and gives skin strength and tension. It serves to protect the skin from external stimuli. In addition, elastin in the dermal layer accounts for about 2%, which is less than collagen, but plays a role in supporting collagen fibers. It has been reported in many recent studies that the 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 are degraded by collagenase or elastase. As people age or are exposed to UV rays, the action and cell number of fibroblasts decreases, the amount of collagen or elastin synthesized decreases, and the action of collagenase or elastase that decomposes them increases. Once the elasticity of the skin is reduced by collagen and elastin, it is very difficult to recover. Accordingly, research for improving skin wrinkles by inhibiting elastase activity, which increases with age, is being actively conducted.

Currently, as a substance that inhibits skin wrinkle formation, 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) Efficacy has been 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), flavonoids ( Francesco B et al., Int J Pharm 145: 87-94.1996), red bean extract (Korean Patent No. 101008833), Yeongyo extract (Korean Patent No. 100825450), etc. Wrinkle improvement and skin protection effects were explored. became However, some substances have low stability or cause skin irritation, so there is a problem with safety, so their use is limited. Accordingly, the search for substances with excellent anti-wrinkle activity, safety and stability is continuing.

The present invention discloses the elastase inhibitory activity of a turtle tail extract.

It is an object of the present invention to provide a composition for improving skin wrinkles using a turtle tail extract.

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

The present invention has been completed by confirming that the green turtle tail extract has elastase inhibitory activity, as confirmed in the following Examples and Experimental Examples.

In consideration of the above, the present invention can be identified as a composition for improving skin wrinkles including an active ingredient of the turtle tail extract.

In the present specification, the term "grass turtle tail extract" refers to extracting green turtle tail leaves, branches, above-ground parts, rhizomes, roots, underground parts, or mixtures thereof with water, 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 these It refers to an extract obtained by leaching using a mixed solvent, an extract obtained using a supercritical extraction solvent such as carbon dioxide, pentane, or a fraction obtained by fractionating the extract. Thus, any method such as chilling, reflux, heating, ultrasonic radiation, and supercritical extraction can be applied. In the case of a fractionated extract, a fraction obtained by suspending the extract in a specific solvent and mixing and standing still with a solvent having a different polarity, and adsorbing the crude extract to a column filled with silica gel, etc. It is meant to include the fraction obtained as a mobile phase. In addition, the meaning of the extract includes a concentrated liquid extract or solid extract from which the extraction solvent is removed by freeze drying, vacuum drying, hot air drying, spray drying, or the like. Preferably, an extract obtained by using water, an alcohol having 1 to 4 carbon atoms or a mixed solvent thereof as an extraction solvent, more preferably an extract obtained by using a mixed solvent of water and an alcohol having 1 to 4 carbon atoms as an extraction solvent do.

In addition, as used herein, the term "active ingredient" refers to a component capable of exhibiting the desired activity alone or in combination with a carrier that has no activity by itself.

The composition of the present invention may contain the active ingredient in an arbitrary amount (effective amount) as long as it can exhibit a wrinkle improvement effect, etc. depending on the formulation and purpose of formulation, and a typical effective amount is 0.001 weight based on the total weight of the composition. % to 15% by weight. Here, the term "effective amount" refers to the intended medical and cosmetic effects such as wrinkle improvement when the composition of the present invention is administered to a mammal, preferably a human subject, during the administration period according to the suggestion of a medical professional. It refers to the amount of active ingredient included in the composition of the present invention. Such effective amounts can be determined empirically within the ordinary ability of one of ordinary skill in the art.

In addition to the active ingredient, the composition of the present invention has similar activities such as skin whitening activity, skin hypersensitivity reaction suppression activity, skin protection activity (skin damage suppression by ultraviolet rays, skin moisturizing, etc.) In order to enhance the convenience of administration, ingestion, and use through addition, any compound or natural extract known to have the activity and safety has already been verified in the art may be additionally included.

These compounds or extracts include pharmacopoeia of each country (“Korea Pharmacopoeia” in Korea), health functional food regulations of each country (“health functional food standards and specifications” announced by the Ministry of Food and Drug Safety in Korea), functional cosmetics regulations of each country (the Ministry of Food and Drug Safety notice in Korea). Compounds or extracts listed in the compendium such as "Standards and Test Methods for Functional Cosmetics," etc.) In accordance with the laws of each country governing the manufacture and sale of functional foods (the “Health Functional Food Act” in Korea), each country’s laws governing the manufacture and sale of compounds or extracts and functional cosmetics whose functionality has been recognized (the “Cosmetics Act” in Korea). '), compounds or extracts whose functionality is recognized are included.

Such ingredients include, for example, retinol, retinyl palmitate, adenosine, polyethoxylated amide, recognized as a skin wrinkle improvement ingredient in the Cosmetics Code (Korean Ministry of Food and Drug Safety Notification, 「Standards and Test Methods for Functional Cosmetics」) according to the Korean Cosmetics Act. dromethrazole, dromethrizole trisiloxane, digalloyl trioleate, dimethicodiethylbenzalmalonate, diethylhexylbutamidotriazone, Arbutin, niacinamide, ascorbyl glucoside, alpha-bisabolol, Oil Soluble Licorice (Glycyrrhiza) Extract recognized as skin whitening ingredients in the same cosmetics industry, UV protection in accordance with the Korean Health Functional Food Act Complex extracts such as pine bark extract recognized as ingredients, phosphatidylserine, finger root extract powder, and complex extracts such as red ginseng and cornus oil are recognized as functional ingredients for improving sensitive skin condition according to the Korean Health Functional Food Act. L. sakei Probio 65, gamma-linolenic acid-containing oils and fats, L. plantarum CJLP133, a lactic acid bacterium derived from fruits and vegetables, and ATP probiotics. One or more of these compounds or natural extracts may be included in the composition of the present invention together with its active ingredient.

In a specific aspect, the composition of this invention can be grasped|ascertained as a food composition.

The food composition of the present invention may be prepared in any form, for example, beverages such as tea, juice, carbonated beverages, and ionic beverages, processed oils such as milk and yogurt, gums, rice cakes, Korean sweets, bread, confectionery, noodles, etc. Foods, tablets, capsules, pills, granules, liquids, powders, flakes, pastes, syrups, gels, jellies, and health functional food preparations such as bars can be prepared.

In addition, the food composition of the present invention may have any product classification in terms of legal and functional classification as long as it conforms to the enforcement laws at the time of manufacture and distribution. For example, it is a health functional food according to Korea's "Health Functional Food Act", or confectionery, beans, tea, and beverages according to each food type according to the Food Ordinance of Korea's Food Sanitation Act (Ministry of Food and Drug Safety Notification "Food Standards and Specifications") , food for special use, and the like.

The food composition of the present invention may contain food additives in addition to the active ingredients thereof. Food additives can be generally understood as substances that are added to and mixed with or infiltrated into food in manufacturing, processing, or preserving food. Food additives with guaranteed safety are limited in terms of ingredients or functions in the Food Additives Ordinance in accordance with the laws of each country that regulates the manufacture and distribution of food (“Food Sanitation Act” in Korea). In the Korean Food Additives Code (“Food Additive Standards and Specifications” notified by the Ministry of Food and Drug Safety), food additives are classified into chemically synthetic products, natural additives, and mixed preparations in terms of ingredients. It is classified into an agent, a preservative, an emulsifier, an acidulant, and a thickener.

The sweetener is used to impart appropriate sweetness to food, and both natural and synthetic ones may be used in the composition of the present invention. Preferably, a natural sweetener is used. Examples of the natural sweetener include sugar sweeteners such as corn syrup solids, honey, sucrose, fructose, lactose, and maltose.

Flavoring agents may be used to improve taste or aroma, and both natural and synthetic ones may be used. Preferably, it is a case where a natural thing is used. In the case of using a natural one, the purpose of nutritional enhancement in addition to flavor may be concurrently used. The natural flavoring agent may be obtained from apples, lemons, tangerines, grapes, strawberries, peaches, or the like, or obtained from green tea leaves, horseradish leaves, bamboo leaves, cinnamon, chrysanthemum leaves, jasmine, and the like. In addition, those obtained from ginseng (red ginseng), bamboo shoots, aloe vera, ginkgo biloba, etc. can be used. The natural flavoring agent may be a liquid concentrate or a solid extract. Optionally, a synthetic flavoring agent may be used, and the synthetic flavoring agent may be an ester, an alcohol, an aldehyde, a terpene, or the like.

As a preservative, sodium calcium 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 etc. are mentioned, and acidulant, malic acid, fumaric acid, adipic acid, phosphoric acid, gluconic acid, tartaric acid, ascorbic acid, acetic acid, phosphoric acid, etc. can be used as an acidulant. Acidulant may be added so that the food composition has an appropriate acidity for the purpose of inhibiting the growth of microorganisms in addition to the purpose of enhancing the taste.

As the thickening agent, a suspending agent, a settling agent, a gel-forming agent, a bulking agent, and the like can be used.

The food composition of the present invention may contain, in addition to the food additives as described above, physiologically active substances or minerals known in the art for the purpose of supplementing and reinforcing functionality and nutrition and guaranteed stability as food additives.

Examples of such physiologically active substances include catechins contained in green tea and the like, vitamins such as vitamin B1, vitamin C, vitamin E, and vitamin B12, tocopherol, dibenzoylthiamine, and the like. Magnesium preparations, such as iron preparations, such as iron citrate, chromium chloride, potassium iodide, selenium, germanium, vanadium, zinc, etc. are mentioned.

In the food composition of the present invention, the food additives as described above may be included in an appropriate amount to achieve the purpose of the addition according to the type of product.

In relation to other food additives that may be included in the food composition of the present invention, reference may be made to the national food regulations or food additives regulations.

The composition of the present invention may be identified as a pharmaceutical composition in another specific embodiment.

The pharmaceutical composition of the present invention may be prepared as 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 topical route, oral route, intravenous route, intramuscular route, and direct absorption through mucosal tissue, and two or more routes may be used in combination. An example of the combination of two or more routes is a case in which two or more formulations of drugs according to the route of administration are combined. For example, one drug is first administered by an intravenous route and the other drug is secondarily administered by a local route.

Pharmaceutically acceptable carriers are well known in the art depending on the route of administration or formulation, and specifically, reference may be made to the pharmacopeias of each country including the "Korea Pharmacopoeia".

When the pharmaceutical composition of the present invention is prepared as an oral dosage form, powders, granules, tablets, pills, dragees, capsules, liquids, gels, syrups, suspensions, wafers, together with a suitable carrier according to methods known in the art. It can be prepared in a formulation such as Examples of suitable carriers include sugars such as lactose, glucose, sucrose, dextrose, sorbitol, mannitol, and xylitol, starches such as corn starch, potato starch, wheat starch, cellulose, methylcellulose, ethylcellulose, sodium carboxymethylcellulose, Cellulose such as hydroxypropylmethylcellulose, polyvinylpyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, magnesium stearate, mineral oil, malt, gelatin, talc, polyol, vegetable oil, ethanol, grease Serol etc. are mentioned. In the case of formulation activity, an appropriate binder, lubricant, disintegrant, colorant, diluent, etc. may be included as needed. Suitable binders include starch, magnesium aluminum silicate, starch ferrist, gelatin, methylcellulose, sodium carboxymethylcellulose, polyvinylpyrrolidone, glucose, corn sweetener, sodium alginate, polyethylene glycol, wax, and the like, and oleic acid as lubricant. sodium, sodium stearate, magnesium stearate, sodium benzoate, sodium acetate, sodium chloride, silica, talcum, stearic acid, its magnesium and calcium salts, polyethylene glycol, and the like. , agar, bentonite, xanthan gum, starch, alginic acid or its sodium salt. Examples of the diluent include lactose, dextrose, sucrose, mannitol, sorbitol, cellulose, glycine, and the like.

When the pharmaceutical composition of the present invention is prepared for parenteral use, it may be formulated in the form of injections, transdermal administrations, nasal inhalants and suppositories together with suitable carriers according to methods known in the art. When formulated as an injection, an aqueous isotonic solution or suspension may be used as a suitable carrier, and specifically, PBS (phosphate buffered saline) containing triethanolamine, sterile water for injection, or isotonic solution such as 5% dextrose may be used. . When formulated for transdermal administration, it can be formulated in the form of ointments, creams, lotions, gels, external solutions, pasta agents, liniment agents, air rolls, and the like. In the case of nasal inhalants, it can be formulated in the form of an aerosol spray using a suitable propellant such as dichlorofluoromethane, trichlorofluoromethane, dichlorotetrafluoroethane, carbon dioxide, and the like. witepsol), tween 61, polyethylene glycols, cacao fat, laurin fat, polyoxyethylene sorbitan fatty acid esters, polyoxyethylene stearate, sorbitan fatty acid esters, and the like can be used.

Specific formulations of pharmaceutical compositions are known in the art, and reference may be made to, for example, Remington's Pharmaceutical Sciences (19th ed., 1995). This document is considered a part of this specification.

A preferred dosage of the pharmaceutical composition of the present invention is in the range of 0.001 mg/kg to 10 g/kg per day, preferably 0.001 mg/kg to 1 g, depending on the patient's condition, weight, sex, age, patient's severity, and administration route. It can be in the range /kg. Administration may be performed once or divided into several times a day. Such dosages should not be construed as limiting the scope of the invention in any respect.

In another specific embodiment, the composition of the present invention can be identified as a cosmetic composition.

Even when the composition of the present invention is identified as a cosmetic composition, the cosmetic composition can be classified into any product in terms of its use or by law, and specifically functional cosmetics, non-functional products having uses such as improvement of skin troubles and improvement of atopic dermatitis It may be general cosmetics and the like. The product form may also take any product form, specifically solution, suspension, emulsion, paste, gel, cream, lotion, powder, soap, surfactant-containing cleansing, oil, powder foundation, emulsion foundation, wax It can take the form of products such as foundation and spray. In the specific product form, it may be in the form of a flexible lotion, a nourishing lotion, a nourishing cream, a massage cream, an essence, an eye cream, a cleansing cream, a cleansing foam, a cleansing water, a pack, a spray, or a powder.

The cosmetic composition of the present invention may include components commonly used in cosmetic compositions in addition to the active ingredient, for example, conventional adjuvants such as stabilizers, solubilizers, surfactants, vitamins, pigments and fragrances, and carriers.

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

When the formulation of the present invention is a powder or a spray, lactose, talc, silica, aluminum hydroxide, calcium silicate or polyamide powder may be used as a carrier component, and in particular, in the case of a spray, additional chlorofluorohydrocarbon, propane /may contain propellants 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-butylglycol oil, glycerol aliphatic ester, polyethylene glycol, fatty acid ester of sorbitan, and the like may be used.

When the formulation of the present invention is a suspension, as a carrier component, a liquid diluent such as water, ethanol or propylene glycol, a suspending agent such as ethoxylated isostearyl alcohol, polyoxyethylene sorbitol ester, polyoxyethylene sorbitan ester, 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 agent, aliphatic alcohol sulfate, aliphatic alcohol ether sulfate, sulfosuccinic acid monoester, isethionate, imidazolinium derivative, methyltaurate, sarcosinate, fatty acid amide as carrier components Ether sulfate, alkylamidobetaine, fatty alcohol, fatty acid glyceride, fatty acid diethanolamide, vegetable oil, lanolin derivative or ethoxylated glycerol fatty acid ester and the like can be used.

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

As described above, according to the present invention, it is possible to provide a composition for improving skin wrinkles using a turtle tail extract.

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

1 is a result of an elastase inhibitory activity experiment.

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 grass turtle tail extract

After adding 20 times the weight of 70% ethanol to the dried grass turtle tail (extraction part: eggplant) pulverized powder, leaching for 24 hours, filtering with Whatman paper filter paper No. 2, and concentrating the filtrate under reduced pressure and freeze-drying to prepare a grass turtle tail extract.

<Experimental Example> Wrinkle improvement activity test - Elastase inhibitory activity measurement

After adding samples diluted by concentration to 50 mM Tris-Cl buffer (pH 8.5), 1 mg/ml of the substrate N-succinyl-(Ala) _3- p-nitroanilide was added to 50 mM Tris-Cl buffer (pH 8.5). 0.6U/ml PPE (porcine pancreas elastase) was added, mixed well, and reacted at 25°C, and absorbance was measured at 405 nm using an ELISA reader. By measuring the elastase inhibitory ability compared to the control group, which is the sample untreated group, IC ₅₀ , which is the 50% inhibitory concentration of elastase, was obtained. As a positive control, ursolic acid was used. _{While the results are shown in FIG. 1 , the IC 50} , which is the 50% inhibitory concentration of elastase, is shown in Table 1 below. The results are the results of three repeated experiments for each concentration.

Elastase inhibitory activity (IC ₅₀ , μg/ml) division Elastase inhibition assay (μg/ml)) Grass turtle tail (branch) extract 886.25 ursolic acid 42.62

As confirmed in FIG. 1 and Table 1, the turtle tail extract showed elastase inhibitory activity in a concentration-dependent manner, and its IC ₅₀ was found to be 886.25 μg/ml. _{The IC 50} of ursolic acid as a positive control was 42.62 μg/ml.

Claims (4)

A composition for improving skin wrinkles comprising, as an active ingredient, a water and ethanol mixed solvent extract of grass turtle tail eggplant having elastase inhibitory activity.
According to claim 1,
The mixed solvent of water and ethanol is 70% ethanol composition.
3. The method of claim 1 or 2,
The composition is a food composition, characterized in that the composition.
3. The method of claim 1 or 2,
The composition is a cosmetic composition, characterized in that the composition.

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