KR102262362B1 - Composition for improving skin conditions comprising an extract of oriental melon stem or cucumber stem - Google Patents

Abstract

The present invention provides a composition for improving skin condition comprising one or more extracts or fractions thereof selected from the group consisting of melon stems and cucumber stems, wherein the improvement of the skin condition is anti-inflammatory, trouble improvement, whitening and complexion improvement from the group consisting of It relates to a composition that is one or more selected. In addition, the present invention is for preventing or treating at least one selected from the group consisting of skin inflammatory diseases, skin troubles, and skin hyperpigmentation comprising one or more extracts or fractions thereof selected from the group consisting of melon stems and cucumber stems. It relates to pharmaceutical compositions.

Description

Composition for improving skin conditions comprising an extract of oriental melon stem or cucumber stem

The present invention relates to a composition for improving skin condition comprising one or more extracts or fractions thereof selected from the group consisting of melon stem and cucumber stem as an active ingredient, and a method for improving skin condition using the same. In addition, the present invention provides a pharmaceutical composition for preventing or treating skin diseases containing one or more extracts or fractions thereof selected from the group consisting of melon stems and cucumber stems as an active ingredient, and preventing or treating skin diseases using the pharmaceutical composition It's about how to treat.

Inflammation is the body's immune response to a wound or disease, and oxidative stress such as ultraviolet rays, active oxygen, and free radicals activates inflammatory factors, causing various diseases and aging of the skin. Vasoactive polypeptides such as kinin, plasmin, and complement act as vasodilators, contractiles, and chemotaxis, and in addition, lymphocytic such as interleukin-6 (IL-6) Phosphorus and arachidonic acid are responsible for the inflammatory response. Arachidonic acid is metabolized to prostaglandin and leukotriene, which are inflammatory mediators, through two pathways, cyclooxygenase or lipooxygenase, and mediates various inflammatory responses.

On the other hand, in order to eliminate inflammation, an anti-inflammatory agent that acts to remove an inflammatory source, reduce biological reactions and symptoms. Substances used for anti-inflammatory purposes so far include flufenamic acid, ibuprofen, benzydamine, indomethacin, etc. as a non-steroidal type, and prednisolone as a steroid type. , and dexamethasone. In addition, allantoin, azene, hydrocortisone, etc. are known to be effective in anti-inflammatory, but these substances have limitations in usage due to safety issues for the skin, or have insignificant effects, so that no inflammatory relief effect can be expected. There is this.

Also, to have fair and fair skin is everyone's unchanging desire. Skin color is genetically determined according to the concentration and distribution of melanin in human skin, but it is also affected by environmental or physiological conditions such as ultraviolet rays from the sun, fatigue, and stress. Melanin is produced through a non-enzymatic oxidation reaction after the enzyme tyrosinase acts on tyrosine, a kind of amino acid, to convert it into DOPA and dopaquinone. Although the pathway by which melanin is made is known, the mechanism of inducing melanin synthesis, which is the previous step in which tyrosinase acts, is still unclear.

On the other hand, as a general whitening component, a substance that inhibits tyrosinase enzyme activity such as kojic acid, arbutin, etc., hydroquinone, vitamin C (L-Ascorbic acid) and derivatives thereof are known. By inhibiting the synthesis of melanin pigment, it is possible to brighten the skin tone and provide a skin whitening effect, as well as to improve skin hyperpigmentation such as spots or freckles caused by ultraviolet rays, hormones, or heredity. However, when applied to the skin, there is a problem in that there is a limitation in the amount of use due to safety issues such as irritation and redness, so that a practical effect cannot be expected.

In order to overcome this limitation, natural products, including herbal medicines, have been attracting attention as new raw materials to replace existing raw materials, and recently, research and development of cosmetic compositions containing these natural substances have been variously attempted.

On the other hand, stems of melons or cucumbers, that is, vines are removed and thrown away after harvesting the fruit, and usually the vines removed are crushed and used as compost. Therefore, it is necessary to develop a method for creating high added value by using the discarded stems of melons and cucumbers.

Under this background, the present inventors have conducted research on substances that are non-toxic and have excellent skin condition improvement effects from natural resources, and thus melon stem extract, cucumber stem extract, and melon stem extract and cucumber stem extract To determine that the mixture exhibits anti-inflammatory or skin trouble improvement effects by suppressing NO production, and skin whitening or complexion improvement effects by inhibiting melanin synthesis, using this to complete a composition for anti-inflammatory, trouble improvement, whitening or complexion improvement reached

[Patent Literature]

Japanese Patent Application Laid-Open No. 8-231370

Japanese Patent Application Laid-Open No. 8-208424

[Non-patent literature]

Cardinale G. et al, Adv. Enzymol., 1974, 41, p. 425

It is an object of the present invention to provide a composition for anti-inflammatory, trouble improvement, whitening or complexion improvement, characterized in that it contains a natural extract as an active ingredient.

Another object of the present invention is to provide a composition for preventing or treating at least one selected from the group consisting of skin inflammatory diseases, skin troubles, and skin hyperpigmentation, characterized in that it contains a natural extract as an active ingredient.

In order to solve the above problems, the present invention is an embodiment, as a cosmetic composition for improving skin condition comprising one or more extracts or fractions thereof selected from the group consisting of melon stems and cucumber stems as an active ingredient, the skin condition The improvement of anti-inflammatory, trouble improvement, whitening and complexion improvement is at least one selected from the group consisting of, it provides a cosmetic composition.

In another embodiment of the present invention, the composition may include a mixed extract of melon stem and cucumber stem or a fraction thereof.

The melon stem (oriental melon stem) of the present invention is a melon ( Cucumis) which is an annual creeper plant of the Cucurbitaceae family. melo var. makuwa ) means the stem part. The melon is taxonomically called melon ( Cucumis). melo ) is a variant of The main stem of the melon stretches out to the side and winds up other objects with tendrils. In the present invention, the melon stem is meant to include both the original stem and tendrils. In the present invention, as the melon stem, the original stem, tendril, or a mixture thereof may be used. Other names for melon stems include Cheomgwagyeong, Cheomgwaman, Cheomgwadeung or Hyanggwadung. Melon stems are known to be effective in menstrual pain and hypertension.

Cucumber stem (cucumber stem) is an annual plant of the vine and cucumber foil of the present invention (Cucumis sativus ) refers to the stem region. The main stem of cucumber has thick hair along with ridges and grows long by attaching to other objects while winding it with tendrils. In the present invention, cucumber stems include both original stems and tendrils. In the present invention, as the cucumber stem, a raw stem, tendril, or a mixture thereof may be used. Other names for cucumber stems include Hwanggwaeung. Cucumber stems are collected in June and dried in the shade or fresh. The taste is sweet and bitter, and the nature is cool and non-toxic. Cucumber stems are effective in urinating and detoxifying. It is also used to treat dysentery, jaundice, etc.

As used herein, the term "extract" refers to an extract obtained by extracting the melon stem, cucumber stem, or a mixture thereof, a diluted or concentrated liquid of the extract, a dried product obtained by drying the extract, a prepared product of the extract, or It includes extracts of all formulations that can be formed using the extract itself and the extract, such as purified products or mixtures thereof.

The extract of the present invention may be extracted from a natural, hybrid or mutated plant of each of the corresponding plants, and may also be extracted from a plant tissue culture.

In the extraction of the melon stem, cucumber stem, or a mixture thereof of the present invention, the extraction method is not particularly limited, and may be extracted according to a method commonly used in the art. Non-limiting examples of the extraction method include hot water extraction, ultrasonic extraction, filtration, and reflux extraction, which may be performed alone or in combination of two or more methods.

In the present invention, the type of extraction solvent used to extract the melon stem, cucumber stem, or a mixture thereof is not particularly limited, and any solvent known in the art may be used. Non-limiting examples of the extraction solvent include water; _{C 1} to C ₄ lower alcohols such as methanol, ethanol, propyl alcohol, and butyl alcohol; polyhydric alcohols such as glycerin, butylene glycol and propylene glycol; and hydrocarbon solvents such as methyl acetate, ethyl acetate, acetone, benzene, hexane, diethyl ether, and dichloromethane; Alternatively, a mixture thereof may be used, and preferably, water, lower alcohol, 1,3-butylene glycol, and ethyl acetate may be used alone or in a mixture of two or more. As a solvent for extracting melon stems, cucumber stems, or mixtures thereof in the present invention, methanol, water (or distilled water), or a mixed solvent thereof may be used, and even more preferably methanol and water 5 to 10: A mixture in a weight ratio of 1 to 5 may be used. A solvent extract may be prepared by extracting the melon stem, cucumber stem, or a mixture thereof one or more times using the solvent, and the solvent extract is filtered to remove suspended solid particles, for example, particles using nylon or the like. After filtering or filtering using freeze filtration, etc., it can be used as it is, or after distillation under reduced pressure, a dried extract obtained by freeze-drying, hot air drying or spray drying can be prepared. For example, finely pulverize each of the melon stem and cucumber stem of the present invention, add a solvent 5 to 20 times the volume of the dry weight of the pulverized product, and in an extractor equipped with a cooler at 40 to 100° C. for 1 to 5 hours After heating, the solvent extract can be obtained by filtration with a filter cloth. By repeating the above process for the solvent extract, a solvent extract extracted twice or more can be prepared. In a specific embodiment of the present invention, a melon stem extract and a cucumber stem extract were respectively prepared using an extraction solvent (methanol: distilled water = 7:3), and a mixed extract was obtained by mixing them (Example 1).

As used herein, the term "fraction" refers to a result obtained by performing fractionation in order to separate a specific component or a specific component group from a mixture containing various various components.

The fractionation method for obtaining the fraction in the present invention is not particularly limited, and may be performed according to a method commonly used in the art. Non-limiting examples of the fractionation method include a method of obtaining a fraction from the extract by treating an extract obtained by extracting a melon stem, a cucumber stem, or a mixture thereof with a predetermined solvent.

The kind of solvent used to obtain the fraction in the present invention is not particularly limited, and any solvent known in the art may be used. Non-limiting examples of the fractionation solvent include polar solvents such as water and alcohol; and non-polar solvents such as hexane, ethyl acetate, chloroform, and dichloromethane. These may be used alone or in combination of two or more. In the case of using alcohol in the fractionation solvent, preferably C ₁ to C ₄ alcohol may be used.

The mixed extract of the melon stem and the cucumber stem of the present invention may be prepared by extracting the melon stem and the cucumber stem and then mixing the respective extracts, or may be prepared by extracting the melon stem and the cucumber stem together.

As described above, the mixed extract of the melon stem and cucumber stem of the present invention has a superior synergistic effect in anti-inflammatory, trouble improvement, whitening or complexion improvement efficacy than when each extract of the melon stem or cucumber stem is used alone. indicates. In particular, the mixed extract of the melon stem and cucumber stem suppresses nitric oxide (NO) production and reduces the total amount of melanin in melanoma cells, thereby exhibiting an excellent synergistic effect to exhibit anti-inflammatory, trouble improvement, whitening or complexion improvement effects, Each of these exhibits a significantly superior skin condition improvement or prevention, improvement or treatment effect of a skin disease compared to the case of using each alone.

The mixing ratio of the melon stem extract and cucumber stem extract contained in the composition of the present invention is not particularly limited, but preferably 1 to 10: 10 to 1 by weight, more preferably 1 to 5 by weight : 5 to 1, most preferably 1:1 by weight. When contained in the above range, there is an advantage that can effectively improve the skin condition and effectively prevent, improve or treat skin diseases.

As used herein, the term "improving skin condition" may refer to one or more selected from the group consisting of anti-inflammatory, trouble improvement, whitening, and complexion improvement.

As used herein, the term “improvement” refers to any action that at least reduces a parameter related to alleviation or treatment of a condition, for example, the severity of a symptom.

Specifically, the melon stem extract, cucumber stem extract, or a mixture extract thereof of the present invention effectively inhibits the production of nitric oxide (N0) to show anti-inflammatory or trouble improvement efficacy, and also has the effect of effectively inhibiting the production of melanin, resulting in It shows the effect of reducing the total amount of melanin synthesized, thereby showing the effect of skin whitening or complexion improvement. In addition, since the composition of the present invention is a material derived from a natural product, it is non-toxic and does not cause side effects even when applied to the human body, so it can be used as a cosmetic composition.

The inflammatory response is a mechanism to regenerate damage caused by physical action, harmful substances, chemical stimuli, bacterial infection, etc. as part of the body's defense response to external stimuli. The persistent inflammatory response rather causes damage to the mucous membrane and promotes damage to skin tissue, inflammation, and skin troubles.

Macrophages play a very important role in the immune response and regulate various mediators of inflammation, including nitric oxide, prostaglandins, and inflammatory cytokines, which are immune proteins. Among them, nitric oxide plays an important role, such as killing bacteria or removing tumors, but excessive nitric oxide production by etiology causes inflammation, and such inflammation causes skin troubles.

That is, when nitric oxide production of macrophages is suppressed, skin inflammation can be prevented, alleviated, improved and treated, and skin troubles caused by an inflammatory reaction can be prevented, alleviated, improved, and treated.

Specifically, in one embodiment of the present invention, when melon stem extract, cucumber stem extract, or a mixed extract thereof was used, respectively, it was confirmed that nitric oxide production was inhibited in macrophages compared to the untreated negative control (Example 4).

In particular, the extract or fraction thereof of a mixture containing both the melon stem extract and the cucumber stem extract of the present invention is a single extract of each plant by a synergistic or cooperative action between the extracts and/or active ingredients in the extract. Compared to L-NMMA (L-NG-Monomethylarginine), which is a known nitrogen monoxide production inhibitor, it has a superior ability to inhibit the production of nitrogen monoxide, and given that it is not purified at all, it produces a very strong nitrogen monoxide equal to or greater than that in macrophages. It was confirmed that there is an inhibitory ability, which was first identified in the present invention.

On the other hand, melanin is a black-brown pigment produced by melanocytes, which determines the skin color of a person, and can be expected to have the effect of brightening the skin by inhibiting melanin pigment.

According to a specific embodiment of the present invention in relation to the above efficacy, when the melanoma stem extract, cucumber stem extract, or a mixture extract thereof is treated by concentration in mouse melanoma cells (B-16 mouse melanoma cells), melanin of melanoma cells It was confirmed that the total amount of was decreased (Example 3).

In particular, the extract or fraction thereof of a mixture containing both the melon stem extract and the cucumber stem extract of the present invention is a single extract of each plant by a synergistic or cooperative action between the extracts and/or active ingredients in the extract. It may exhibit a more excellent skin whitening or complexion improvement effect compared to that, which was identified for the first time in the present invention.

As used herein, the term “anti-inflammatory” refers to any action in which an immune response is alleviated and NO production is suppressed.

As used in the present invention, the term "trouble" refers to skin rashes, acne, pimples, injections (red nose, rosacea), etc. that harm the appearance of the skin, which may be caused by inflammation caused by excessive nitric oxide production in macrophages. skin condition.

As used herein, the term "trouble improvement" refers to inhibiting or inhibiting the generation of troubles on the skin, or alleviating the troubles already generated.

As used herein, the term "whitening" refers to any action that inhibits or prevents the deposition of melanin on the skin by inhibiting the synthesis of melanin.

As used herein, the term "improving complexion" means that skin blemishes such as facial blemishes, freckles, and age spots are removed or the production is suppressed, and the skin tone is brightened, so that the overall color of the face is aesthetically improved.

The cosmetic composition of the present invention is a solution, external ointment, cream, foam, nourishing lotion, softening lotion, pack, soft water, emulsion, makeup base, essence, soap, liquid detergent, bath agent, sunscreen cream, sun oil, suspension, emulsion , paste, gel, lotion, powder, soap, surfactant-containing cleansing, oil, powder foundation, emulsion foundation, wax foundation, patch and spray, but is not limited thereto. .

The cosmetic composition of the present invention may further include one or more cosmetically acceptable carriers to be formulated in general skin cosmetics, and common ingredients include, for example, oil, water, surfactant, humectant, lower alcohol, and thickener. , a chelating agent, a pigment, a preservative, a fragrance, etc. may be appropriately mixed, but is not limited thereto.

The cosmetically acceptable carrier included in the cosmetic composition of the present invention varies depending on the formulation of the cosmetic composition.

When the dosage form of the present invention is an ointment, paste, cream or gel, as a carrier component, animal oil, vegetable oil, wax, paraffin, starch, tracanth, cellulose derivative, polyethylene glycol, silicone, bentonite, silica, talc, zinc oxide, etc. may be used, but is not limited thereto. These may be used alone or in combination of two or more.

When the formulation of the present invention is a powder or a spray, lactose, talc, silica, aluminum hydroxide, calcium silicate, polyamide powder, etc. may be used as a carrier component, and in particular, in the case of a spray, additional chlorofluorohard propellants such as, but not limited to, locarbon, propane/butane or dimethyl ether. These may be used alone or in combination of two or more.

When the formulation of the present invention is a solution or emulsion, a solvent, solubilizer, or emulsifier may be used as a carrier component, for example, water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, Propylene glycol, 1,3-butylglycol oil and the like can be used, and in particular, cottonseed oil, peanut oil, corn germ oil, olive oil, castor oil and sesame oil, glycerol aliphatic esters, fatty acid esters of polyethylene glycol or sorbitan may be used, but is not limited thereto. These may be used alone or in combination of two or more.

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 esters and polyoxyethylene sorbitan esters; Crystalline cellulose, aluminum metahydroxide, bentonite, agar or tracanth may be used, but is not limited thereto. These may be used alone or in combination of two or more.

When the formulation of the present invention is a soap, alkali metal salts of fatty acids, fatty acid hemiester salts, fatty acid protein hydrolysates, isethionate, lanolin derivatives, aliphatic alcohols, vegetable oils, glycerol, sugar, etc. are used as carrier components. may be, but is not limited thereto. These may be used alone or in combination of two or more.

According to another embodiment of the present invention, there is provided a quasi-drug composition for improving skin condition comprising one or more extracts or fractions thereof selected from the group consisting of melon stems and cucumber stems as an active ingredient, wherein the improvement of the skin condition is anti-inflammatory, It provides a quasi-drug composition that is at least one selected from the group consisting of trouble improvement, whitening and complexion improvement.

The term "quasi-drug" as used in the present invention refers to items with a milder action than pharmaceuticals among items used for the purpose of diagnosing, treating, improving, alleviating, treating or preventing diseases of humans or animals, for example, in the Pharmaceutical Affairs Act. According to the report, quasi-drugs exclude products used for pharmaceutical purposes, and include products used for the treatment or prevention of diseases in humans and animals, and products with minor or no direct action on the human body.

The quasi-drug composition of the present invention may be prepared in a formulation selected from the group consisting of body cleanser, foam, soap, mask, ointment, cream, lotion, essence and spray, but is not limited thereto.

In the quasi-drug composition of the present invention, the description of one or more extracts or fractions thereof selected from the group consisting of melon stem and cucumber stem, and the description of skin condition improvement are the same as those described above with respect to the cosmetic composition.

According to another embodiment of the present invention, there is provided a food composition for improving skin condition comprising one or more extracts or fractions thereof selected from the group consisting of melon stems and cucumber stems as an active ingredient, wherein the improvement of the skin condition is anti-inflammatory, It provides a food composition that is at least one selected from the group consisting of trouble improvement, whitening and complexion improvement.

The food composition of the present invention is not particularly limited, and includes a health functional food composition.

When the health functional food composition of the present invention is used as a food additive, the composition may be added as it is or used together with other foods or food ingredients, and may be appropriately used according to a conventional method.

The type of the food is not particularly limited, and includes all foods in the ordinary sense. Non-limiting examples of foods to which the above substances can be added include meat, sausage, bread, chocolate, candy, snacks, confectionery, pizza, ramen, other noodles, gum, dairy products including ice cream, various soups, beverages, tea , drinks, alcoholic beverages, and vitamin complexes.

When the health functional food composition of the present invention is a beverage composition, it may contain various flavoring agents or natural carbohydrates as an additional component like a conventional beverage. Non-limiting examples of the natural carbohydrate include monosaccharides such as glucose and fructose; disaccharides such as maltose and sucrose; natural sweeteners such as dextrin and cyclodextrin; and synthetic sweeteners such as saccharin and aspartame. The proportion of the additional components to be added may be appropriately determined by the selection of those skilled in the art.

In addition to the above, the health functional food composition of the present invention includes various nutrients, vitamins, electrolytes, flavoring agents, colorants, pectic acid and salts thereof, alginic acid and salts thereof, organic acids, protective colloidal thickeners, pH adjusters, stabilizers, preservatives, glycerin , alcohol, carbonation agents used in carbonated beverages, and the like. In addition, the health functional food composition of the present invention may contain the pulp for the production of natural fruit juice, fruit drink or vegetable drink. These components may be used independently or in combination of two or more. The proportion of these additives may also be appropriately selected by those skilled in the art.

In the food composition of the present invention, the description of one or more extracts or fractions thereof selected from the group consisting of melon stems and cucumber stems, and the description of skin condition improvement are the same as those described above with respect to the cosmetic composition.

In the cosmetic composition, quasi-drug composition or food composition of the present invention, one or more extracts or fractions thereof selected from the group consisting of melon stems and cucumber stems may be included in an amount of 0.0001 to 50% by weight of the total composition, preferably by dry weight. and more preferably 0.0005 to 10% by weight. There is an advantage of exhibiting excellent anti-inflammatory, skin trouble improvement, whitening or complexion improvement efficacy within the above range, and there is an advantage in that the formulation of the composition is stabilized.

According to another embodiment of the present invention, there is provided a pharmaceutical composition for preventing or treating skin diseases comprising one or more extracts or fractions thereof selected from the group consisting of melon stems and cucumber stems as an active ingredient.

The skin disease includes at least one selected from the group consisting of skin inflammatory diseases, skin troubles, and skin hyperpigmentation.

In the pharmaceutical composition of the present invention, the description of one or more extracts or fractions thereof selected from the group consisting of melon stems and cucumber stems is the same as described above with respect to the cosmetic composition.

The skin inflammatory disease of the present invention means any disease caused by immune stimulation. Non-limiting examples of the skin inflammatory disease include atopic dermatitis, eczema, seborrheic dermatitis, psoriasis, acne, and the like.

The skin trouble of the present invention refers to a skin condition that impairs the appearance of the skin, which may be caused by inflammation caused by excessive nitric oxide production in macrophages. Non-limiting examples of the skin troubles include skin rash, acne, pimples, injections (red nose, rosacea), and the like.

Skin hyperpigmentation of the present invention means any disease caused by skin hyperpigmentation by melanin synthesis. Non-limiting examples of the skin hyperpigmentation may include spots, freckles, and age spots.

In the pharmaceutical composition of the present invention, the effective content of one or more extracts or fractions thereof selected from the group consisting of melon stems and cucumber stems is not particularly limited, and is 0.00001% to 50% by weight based on the total weight of the pharmaceutical composition. may be included.

The pharmaceutical composition of the present invention, in addition to containing one or more extracts or fractions thereof selected from the group consisting of melon stems and cucumber stems as an active ingredient, may further include a pharmaceutically acceptable carrier.

In the present invention, the "pharmaceutically acceptable" means that when administered, it does not stimulate an organism and does not inhibit the biological activity and properties of the administered compound, and can be commonly used in the pharmaceutical field.

The pharmaceutical composition of the present invention, formulated together with the carrier, can be utilized as food, medicine, feed additive, drinking water additive, and the like.

In the present invention, the type of the carrier is not particularly limited, and any carrier commonly used in the art may be used. Non-limiting examples of the carrier include saline, sterile water, Ringer's solution, buffered saline, albumin injection solution, lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, maltodextrin, glycerol, ethanol, and the like. can These may be used alone or in mixture of two or more.

In addition, the pharmaceutical composition of the present invention can be used by adding other pharmaceutically acceptable additives such as excipients, diluents, antioxidants, buffers or bacteriostats, if necessary, and fillers, extenders, wetting agents, disintegrants, dispersants, surfactants, etc. , a binder or lubricant may be additionally added.

The pharmaceutical composition of the present invention may be formulated and used in various formulations suitable for oral or parenteral administration.

Non-limiting examples of the formulation for oral administration include troches, lozenges, tablets, aqueous suspensions, oily suspensions, prepared powders, granules, emulsions, hard capsules, soft capsules, syrups or elixirs, and the like. can be heard

In order to formulate the pharmaceutical composition of the present invention for oral administration, a binder such as lactose, saccharose, sorbitol, mannitol, starch, amylopectin, cellulose (Cellulose) or gelatin (Gelatin); excipients such as dicalcium phosphate; disintegrating agents such as corn starch or sweet potato starch; Lubricating oils such as magnesium stearate, calcium stearate, sodium stearyl fumarate or polyethylene glycol wax can be used, and sweeteners, fragrances, syrups, etc. can also be used. can

Furthermore, in the case of capsules, in addition to the above-mentioned substances, a liquid carrier such as fatty oil may be additionally used.

Non-limiting examples of the parenteral formulation include injections, suppositories, powders for respiratory inhalation, aerosols for spraying, oral sprays, mouthwashes, toothpastes, ointments, powders for application, oils, creams, etc. have.

In order to formulate the pharmaceutical composition of the present invention for parenteral administration, sterile aqueous solutions, non-aqueous solvents, suspensions, emulsions, freeze-dried preparations, external preparations, etc. may be used, and the non-aqueous solvents and suspensions include propylene glycol, polyethylene Glycol, vegetable oils such as olive oil, injectable esters such as ethyl oleate, and the like can be used.

In addition, more specifically, when the pharmaceutical composition of the present invention is formulated as an injection solution, the composition of the present invention is mixed in water with a stabilizer or buffer to prepare a solution or suspension, and this is an ampoule or vial. It may be formulated for unit dosage. In addition, when the pharmaceutical composition of the present invention is formulated as an aerosol, a propellant or the like may be blended with an additive so that the water-dispersed concentrate or wet powder is dispersed.

In addition, when the pharmaceutical composition of the present invention is formulated into an ointment, cream, etc., animal oil, vegetable oil, wax, paraffin, starch, tracanth, cellulose derivative, polyethylene glycol, silicone, bentonite, silica, talc, zinc oxide It can be formulated using the like as a carrier.

The pharmaceutical composition of the present invention may be preferably formulated as a dosage form for parenteral administration, and more preferably composed of a gel, a patch, a spray, an ointment, a warning agent, a lotion, a liniment agent, a pasta agent, and a cataplasma agent. It may have a formulation selected from the group.

The pharmaceutically effective amount and effective dosage of the pharmaceutical composition of the present invention may vary depending on the formulation method, administration method, administration time and/or administration route of the pharmaceutical composition, and the reaction to be achieved by administration of the pharmaceutical composition the type and extent of the drug, the type of subject to be administered, age, weight, general health condition, symptoms or degree of disease, sex, diet, excretion, drug and other composition components used at the same time or at the same time for the subject It may vary depending on several factors, including those well known in the pharmaceutical field, and those skilled in the art can easily determine and prescribe an effective dosage for the desired treatment. Administration of the pharmaceutical composition of the present invention may be administered once a day, may be administered divided into several times. Therefore, the above dosage does not limit the scope of the present invention in any way.

A preferred dosage of the pharmaceutical composition of the present invention may be 1 mg/kg to 1,OOO mg/kg per day.

The administration route and administration method of the pharmaceutical composition of the present invention may be each independent, and the method is not particularly limited, and may be applied to any administration route and administration method as long as the pharmaceutical composition can reach the desired site. can follow The pharmaceutical composition may be administered by oral administration or parenteral administration.

As the method of parenteral administration, for example, intravenous administration, intraperitoneal administration, intramuscular administration, transdermal administration, or subcutaneous administration may be used, and a method of applying, spraying, or inhaling the composition to a diseased site may also be used. can, but is not limited to these.

The pharmaceutical composition of the present invention may preferably be administered parenterally, and more preferably, it may be administered in a manner that is applied topically to areas in need of improvement of skin condition or prevention, improvement or treatment of skin diseases. have.

As used herein, the term "prevention" refers to the onset of skin diseases including at least one selected from the group consisting of skin inflammatory diseases, skin troubles, and skin hyperpigmentation by administering the pharmaceutical composition of the present invention to an individual. Any action that inhibits or delays

As used in the present invention, the term "treatment" means that one or more symptoms selected from the group consisting of skin inflammatory diseases, skin troubles, and skin hyperpigmentation are improved or beneficial by administering the pharmaceutical composition of the present invention to an individual. means all actions

According to another embodiment of the present invention, a cosmetic composition, quasi-drug composition or food composition containing one or more extracts or fractions thereof selected from the group consisting of melon stems and cucumber stems as an active ingredient, comprising administering to an individual , to provide a method for improving skin condition.

As used herein, the term “individual” refers to all animals, including mammals, including mice, livestock, and humans.

In the present invention, the cosmetic composition, quasi-drug composition or food composition containing one or more extracts or fractions thereof selected from the group consisting of melon stems and cucumber stems as an active ingredient is the same as described above, and the meaning of skin condition improvement is also It is the same as described above.

In the present invention, the description of the dosage, administration route, administration method, etc. of the composition is replaced with the description in relation to the pharmaceutical composition of the present invention.

According to another embodiment of the present invention, it comprises administering to an individual a pharmaceutical composition containing one or more extracts or fractions thereof selected from the group consisting of melon stems and cucumber stems as an active ingredient, prevention of skin diseases or treatment methods are provided.

In the present invention, the pharmaceutical composition containing one or more extracts or fractions thereof selected from the group consisting of melon stems and cucumber stems as an active ingredient is the same as described above, and the meaning of individual, skin disease, prevention, and treatment is also described above. same as described in

In the present invention, the description of the dosage, administration route, administration method, etc. of the pharmaceutical composition is the same as described in relation to the pharmaceutical composition of the present invention.

The composition containing the extract or fraction thereof of melon stem, cucumber stem, or a mixture thereof of the present invention is excellent in anti-inflammatory, trouble improvement, whitening and complexion improvement effects. Specifically, the composition of the present invention is excellent in the efficacy of inhibiting nitric oxide production in macrophages, and excellent in inhibiting the increase in the total amount of melanin.

In addition, since the composition of the present invention is a material derived from a natural product, it is non-toxic, and does not cause side effects even when applied to the human body, so that it is highly useful as a cosmetic composition.

Hereinafter, the configuration and effects of the present invention will be described in more detail through examples. These examples are only for illustrating the present invention, and the scope of the present invention is not limited by these examples.

Example 1: Preparation of melon stem extract, cucumber stem extract and mixtures thereof

After each melon stem and cucumber stem were dried and chopped, 200 g each of the dry weight was placed in a flask, and extracted by cooling with 1000 g of an extraction solvent (methanol:distilled water = 7:3) for 3 days. The chilled extract was filtered through a filter having a pore size of 0.2 μm to prepare a melon stem extract and a cucumber stem extract, respectively. The melon stem and cucumber stem extract mixture was prepared by mixing each extract in a ratio of 1:1 by weight.

Example 2: Cytotoxicity test

Cytotoxicity was evaluated for each substance listed in Table 1 below.

MTT assay by culturing V79-4 cells (Chinese hamster, a continuous cell line of lung tissue fibroblasts) [Reference: Mossman T. (1983). Rapid colorimetric assay for cellular growth & survival: application to proliferation & cytotoxicity assays. Journal of Immunological Methods 65, 55-63] was performed. Briefly, first, V79-4 cells are cultured for 24 hours, and the sample is diluted (100000ppm, 10000ppm, 1000ppm, 100ppm, 10ppm, 1ppm, and 0.1ppm) to an appropriate concentration in the medium (3% FBS) and cultured for 24 hours. Cell viability was determined by measuring absorbance at 570 nanometers (nm) using Alamarblue. The results are shown in Table 1 below. At this time, sodium lauryl sulfate (SLS) was used as a control. The following IC ₅₀ (Inhibitory Concentration 50) is a concentration that kills 50% of cells, and the experiment was repeated 3 times.

sample IC ₅₀ (%, w/v) melon stem extract 0.5 Cucumber Stem Extract 1.1 Mixture of melon stem extract and cucumber stem extract 0.7 squalane 0.05 Sodium Lauryl Sulfate (SLS) 0.006

As can be seen from the results of Table 1, the melon stem extract, cucumber stem extract, and mixtures thereof showed excellent safety by showing 10 times or more lower cytotoxicity than squalane, a raw material with excellent safety.

Example 3: Investigation of whitening effect by confirming the effect of reducing the total amount of melanin

The whitening effect at the cellular level was tested by adding the substances in Table 2 below to the culture medium of B-16 mouse melanoma cells.

Before the experiment, toxicity was evaluated for melanoma cells in mice, and a non-toxic concentration was selected to evaluate whitening. Arbutin, a positive control, was treated in the medium at a concentration of 200 μg/ml, and each extract and extract mixture was treated in B-16 melanoma cells at the concentrations described in Table 2. It was cultured for 3 days after the above treatment.

Thereafter, the cells were treated with trypsin, removed from the culture vessel, centrifuged, and then melanin was extracted. To the detached cells, 1 ml of sodium hydroxide solution (1N concentration) was added and boiled for 10 minutes to dissolve melanin. Using a spectrophotometer, absorbance was measured at 400 nm to measure the amount of melanin produced.

The amount of melanin was measured by a method expressed as absorbance per unit cell number (10 ⁶ cells), calculated as the inhibition rate (%) with respect to the total amount of melanin relative to the negative control (untreated group), and the results are summarized in Table 2. In addition, the experiment was repeated 3 times.

sample Total amount of melanin (Abs) Inhibition rate (%) Melon stem extract (100 μg/ml) 0.063 23.17 Cucumber stem extract (100 μg/ml) 0.069 15.85 Mixture of melon stem extract and cucumber stem extract (200 μg/ml) 0.040 51.22 negative control (no treatment) 0.082 - Positive control (arbutin) (200 μg/ml) 0.042 48.78

As can be seen from the results of Table 2, it can be seen that the melon stem extract and the cucumber stem extract have an effect of reducing the total amount of melanin like arbutin, which is a known whitening material. In addition, these mixtures showed superior efficacy than when each extract was treated alone, and it was confirmed that the effect of reducing the total amount of melanin similar to arbutin as a simple extract of a plant appeared.

Example 4: NO Investigation of anti-inflammatory effect by checking the production inhibitory effect

Nitric oxide (NO) formation inhibition test using RAW264.7 cell line (ATCC number: CRL-2278) using the RAW264.7 cell line (ATCC number: CRL-2278) to confirm the anti-inflammatory and skin trouble relief effects of melon stem extract, cucumber stem extract and mixtures thereof. was carried out.

Specifically, RAW264.7 cells, which are macrophages of mice, were subcultured several times, ^{and placed in a 24-well plate so that 3×10 5} cells were put into each well, and then cultured for 24 hours. Then, each extract was diluted to the concentration shown in Table 3 and replaced with the cell medium containing it. At this time, the NO production inhibitor, L-NMMA (L-NG-Monomethylarginine) was treated as a positive control and cultured for 30 minutes, and LPS (Lipopolysaccharide) was treated as a stimulant by 1 μg and cultured for 24 hours. 100 μl of the supernatant was taken and transferred to a 96-well plate, 100 μl of GRIESS solution was added, reacted at room temperature for 10 minutes, and absorbance at 540 nm was measured to inhibit NO inhibitory effect of melon stem extract, cucumber stem extract and mixtures thereof was measured and calculated as a relative NO inhibition rate (%) with respect to the negative control group (untreated group), and the results are shown in Table 3 below. In addition, the experiment was repeated 3 times.

sample NO production inhibition rate (%) Melon stem extract (100 μg/ml) 21.28 Cucumber stem extract (100 μg/ml) 18.29 Mixture of melon stem extract and cucumber stem extract (200 μg/ml) 48.27 negative control (no treatment) - Positive control (L-NMMA) (10 μg/ml) 39.54

As shown in Table 3, it was found that the melon stem extract, cucumber stem extract, and mixtures thereof used in the cosmetic composition of the present invention inhibited NO production, like L-NMMA, which is known as an NO production inhibitor. Although lower than the positive control L-NMMA, it was confirmed that an excellent NO production inhibition rate was shown as a plant extract, and in particular, a mixture of the two extracts exhibited superior NO production inhibition efficacy than when each extract was treated alone. .

manufacturing example : Manufacturing of cosmetics

manufacturing example 1: Manufacture of softening lotion (skin lotion)

As in the following composition, a softening lotion was prepared according to a conventional method.

0.1% by weight of melon stem extract, cucumber stem extract, or a mixture of these extracts

Beta-1,3-glucan 1.0 wt%

Butylene glycol 2.0 wt%

Propylene glycol 2.0 wt%

0.1 wt% of carboxyvinyl polymer

PEG-12 nonylphenyl ether 0.2 wt%

Polysorbate 80 0.4 wt%

Ethanol 10.0 wt%

Triethanolamine 0.1 wt%

Preservative 0.05 wt%

dye 0.05% by weight

Flavor 0.05% by weight

Purified water remaining

manufacturing example 2: Nutrient lotion ( milk lotion ) manufacturing

As in the following composition, nutrient lotion was prepared according to a conventional method.

0.1% by weight of melon stem extract, cucumber stem extract, or a mixture of these extracts

Beta-1,3-glucan 1.0 wt%

Beeswax 4.0 wt%

Polysorbate 60 1.5 wt%

1.5 wt% of sorbitan sesquioleate

Liquid paraffin 0.5 wt%

5.0 wt% caprylic/capric triglyceride

Glycerin 3.0 wt%

Butylene glycol 3.0 wt%

Propylene glycol 3.0 wt%

0.1 wt% of carboxyvinyl polymer

Triethanolamine 0.2 wt%

Preservative 0.05 wt%

dye 0.05% by weight

Flavor 0.05% by weight

Purified water remaining

manufacturing example 3: Preparation of nourishing cream

As in the following composition, a nourishing cream was prepared according to a conventional method.

0.2% by weight of melon stem extract, cucumber stem extract, or a mixture of these extracts

Beta-1,3-glucan 5.0 wt%

Beeswax 10.0 wt%

Polysorbate 60 1.5 wt%

Sebum 60 hydrogenated castor oil 2.0 wt%

Sorbitan sesquioleate 0.5 wt%

Liquid paraffin 10.0 wt%

5.0 wt% squalane

5.0 wt% caprylic/capric triglyceride

glycerin 5.0 wt%

Butylene glycol 3.0 wt%

Propylene glycol 3.0 wt%

Triethanolamine 0.2 wt%

Preservative 0.05 wt%

dye 0.05% by weight

Flavor 0.05% by weight

Purified water remaining

manufacturing example 4: Preparation of massage cream

As in the following composition, a massage cream was prepared according to a conventional method.

0.1% by weight of melon stem extract, cucumber stem extract, or a mixture of these extracts

Beta-1,3-glucan 3.0 wt%

Beeswax 10.0 wt%

Polysorbate 60 1.5 wt%

Sebum 60 hydrogenated castor oil 2.0 wt%

Sorbitan sesquioleate 0.8 wt%

Liquid paraffin 40.0 wt%

5.0 wt% squalane

4.0 wt% caprylic/capric triglyceride

glycerin 5.0 wt%

Butylene glycol 3.0 wt%

Propylene glycol 3.0 wt%

Triethanolamine 0.2 wt%

Preservative 0.05 wt%

dye 0.05% by weight

Flavor 0.05% by weight

Purified water remaining

manufacturing example 5: Preparation of the pack

As with the following composition, the pack was prepared according to a conventional method.

0.2% by weight of melon stem extract, cucumber stem extract, or a mixture of these extracts

Beta-1,3-glucan 1.0 wt%

13.0 wt% of polyvinyl alcohol

0.2 wt% of sodium carboxymethylcellulose

glycerin 5.0 wt%

Allantoin 0.1 wt%

ethanol 6.0 wt%

PEG-12 nonylphenyl ether 0.3 wt%

Polysorbate 60 0.3 wt%

Preservative 0.05 wt%

dye 0.05% by weight

Flavor 0.05% by weight

Purified water remaining

Claims (12)

A cosmetic composition for improving skin condition comprising a melon stem extract or a fraction thereof as an active ingredient, wherein the improvement of the skin condition is at least one selected from the group consisting of anti-inflammatory and whitening.
The cosmetic composition of claim 1, wherein the composition further comprises a cucumber stem extract or a fraction thereof.
The cosmetic composition according to claim 2, wherein the mixing ratio of the melon stem extract and the cucumber stem extract is 1 to 10: 10 to 1 by weight.
The method according to claim 2, wherein the mixed extract of the melon stem and the cucumber stem is prepared by extracting the melon stem and the cucumber stem, respectively, and then mixing the respective extracts, or it is characterized in that it is prepared by extracting the melon stem and the cucumber stem together. A cosmetic composition comprising
According to claim 1, wherein the extract is melon stem water, C ₁ to C ₄ lower alcohol, glycerin, butylene glycol, propylene glycol, methyl acetate, ethyl acetate, acetone, benzene, hexane, diethyl ether and dichloromethane A cosmetic composition, characterized in that it is obtained by extraction with one or more solvents selected from the group consisting of.
The cosmetic composition according to claim 5, wherein the solvent is a mixture of methanol and water in a weight ratio of 5 to 10: 1 to 5.
According to claim 1, wherein the cosmetic composition is a solution, external ointment, cream, foam, nourishing lotion, softening lotion, pack, softening water, emulsion, makeup base, essence, soap, liquid detergent, bath agent, sunscreen cream, sun oil, A cosmetic, characterized in that it has a formulation selected from the group consisting of suspensions, emulsions, pastes, gels, lotions, powders, soaps, surfactant-containing cleansing, oils, powder foundations, emulsion foundations, wax foundations, patches and sprays. composition.
A quasi-drug composition for improving skin condition comprising a melon stem extract or a fraction thereof as an active ingredient, wherein the improvement of the skin condition is at least one selected from the group consisting of anti-inflammatory and whitening, quasi-drug composition.
The quasi-drug composition of claim 8, wherein the composition further comprises a cucumber stem extract or a fraction thereof.
A pharmaceutical composition for preventing or treating a skin disease comprising a melon stem extract or a fraction thereof as an active ingredient, wherein the skin disease is at least one selected from the group consisting of skin inflammatory diseases and skin hyperpigmentation.
The pharmaceutical composition according to claim 10, wherein the composition further comprises a cucumber stem extract or a fraction thereof.
The pharmaceutical composition according to claim 10, wherein the skin disease is at least one selected from the group consisting of atopic dermatitis, eczema, seborrheic dermatitis, acne, skin rash, pimples, rosacea, melasma, freckles and age spots.