WO2015194875A1 - Composition containing danpung bean leaf extract - Google Patents

Abstract

The present specification relates to a composition for a skin preparation for external use, containing an extract of bean leaves (danpung bean leaves) of a specific stage among the growth stages of beans as an active ingredient. The composition according to the present invention has an excellent antioxidant property, an excellent antiaging property and no skin irritation since natural-derived ingredients are contained in the composition, and thus is useful. The composition of the present specification can be widely used, by such characteristics, as an antioxidant or antiaging composition of an individual in the pharmaceutical or cosmetic field.

Description

Composition comprising maple bean extract

The present specification relates to a composition comprising an extract for a soybean leaf at a particular stage in the growth stage of soybean.

Human skin is changed by a number of internal and external factors as it ages. That is, internally, the secretion of various hormones that regulate metabolism decreases, and the function of immune cells and the activity of cells decreases, thereby reducing the biosynthesis of immune proteins and constituent proteins necessary for living organisms. Due to the increase in the amount of ultraviolet rays that reach the surface of the sun's rays and further increase environmental pollution, free radicals and free radicals, such as free radicals, skin thickness is reduced, wrinkles are increased, elasticity is reduced only In addition, the color of the skin becomes dull, skin problems frequently occur, and various changes such as blemishes, freckles, and black mushrooms also increase.

As aging progresses, symptoms such as changes and decreases in the content and arrangement of collagen, elastin, hyaluronic acid, and glycoproteins, which are constituting skin, appear, and are subjected to oxidative stress caused by free radicals and active harmful oxygen. In addition, by aging or ultraviolet light, cyclooxygenase-2 (Cox-2, cyclooxygenase), an enzyme that produces proinflammatory cytokine, which is known to cause inflammation in most cells that make up the skin Increased biosynthesis, increased biosynthesis of matrix metalloproteinase (MMP), an enzyme that degrades skin tissue by these inflammatory factors, and increased nitric oxide (NO) production by inducible nitric oxide synthase (iNOS) It is known. In other words, the biosynthesis of the substrate material is reduced by the reduction of cellular activity and micro-inflammation due to naturally occurring endogenous aging, and by external factors such as the increase of stress caused by various harmful environments and the increase of free radical species caused by sunlight. As a result, decomposition and degeneration are accelerated, and the skin matrix is destroyed and thinned, resulting in various symptoms of skin aging. Therefore, a lot of research is being conducted on the active ingredient that can prevent and improve the phenomenon of aging.

On the other hand, free radicals generated by various physical, chemical and environmental factors such as enzymes, reducing metabolism, chemicals, pollutants and photochemical reactions in the body are non-selective and irreversible to cell components such as lipids, proteins, sugars and DNA. It has been known to cause various diseases including cell aging or cancer by performing a destructive action. In addition, various peroxides in the body, including lipid peroxides produced as a result of lipid peroxidation by these free radicals, also cause oxidative destruction of cells and cause various functional disorders. Accordingly, antioxidants such as free radical scavengers or peroxide production inhibitors are expected as agents for inhibiting or treating aging and various diseases caused by these oxides.

Accordingly, the present inventors have confirmed that when the soybean leaf extract is applied to the skin, it is possible to enhance not only the antioxidant and anti-aging functions of the skin but also the whitening and moisturizing functions, thereby completing the present invention.

An object of the present specification is to provide a composition of natural origin to promote skin health.

In order to achieve the above object, the present specification provides a composition comprising maple leaf extract as an active ingredient.

The composition according to the present disclosure is excellent in anti-oxidation ability, excellent in anti-aging ability, and contains components derived from nature, thereby showing an advantage of no skin irritation. Due to these properties, the composition of the present disclosure can be widely used in the pharmaceutical or cosmetic field as a composition for antioxidant or anti-aging of an individual.

1 is a graph showing the HPLC results of the maple leaf extract and soybean extract according to an aspect of the present invention.

Korean Patent Application No. 10-2014-0074820, filed June 19, 2014 and Korean Patent Application No. 10-2015-0085091, filed June 16, 2015 are hereby incorporated by reference in their entirety for all purposes. Included. In addition, this application claims the benefit of Korean Patent Application Nos. 10-2014-0074820 and 10-2015-0085091, which are hereby incorporated by reference in their entirety.

In one aspect, the present invention may be directed to a composition comprising maple leaf extract as an active ingredient. Specifically, in one aspect of the present invention, the composition may be a composition comprising as an active ingredient the extract of maple bean leaves of which the color of the bean leaf is changed to yellow. More specifically, in one aspect of the present invention, the maple bean leaf may be a bean leaf of R7 to R8 step of the growth stage of the bean.

In one aspect of the invention, the composition may be a topical skin composition.

In one aspect of the invention, the composition may be an antioxidant or anti-aging composition.

In one aspect of the invention, the composition may be a pharmaceutical, cosmetic, or food composition.

In one aspect, the present invention may be directed to an antioxidant method comprising administering a maple leaf extract or a composition comprising the same as an active ingredient to an individual in need thereof. Specifically, the administration may be by the method of administration described herein.

In one aspect, the present invention may be directed to the antioxidant use of maple leaf extract.

In one aspect, the present invention may be directed to a maple leaf extract for use in antioxidants.

In one aspect, the present invention may be directed to an anti-aging method comprising administering a maple bean extract or a composition comprising the same as an active ingredient to an individual in need of anti-aging. Specifically, the administration may be by the method of administration described herein.

The present invention in one aspect, may be directed to the anti-aging use of maple leaf extract.

In one aspect, the present invention may be directed to a maple leaf extract for use in anti-aging.

In one aspect of the invention, the maple leaf extract or a composition comprising the same as an active ingredient may have one or more of the following characteristics:

(1) the characteristic that IC ₅₀ is 70 ppm or less in the antioxidant activity experiment by DPPH reduction;

(2) collagenase expression is 55% or less in the collagenase production inhibition experiment.

In one aspect, the present invention may be directed to a maple leaf extract having one or more of the following characteristics or a composition comprising the same as an active ingredient:

(1) the characteristic that IC ₅₀ is 70 ppm or less in the antioxidant activity experiment by DPPH reduction;

(2) collagenase expression is 60% or less in the collagenase production inhibition experiment.

In one aspect of the invention, the characteristics as

(1) In the antioxidant activity test by DPPH reduction, IC ₅₀ is 70ppm or less, 65ppm or less, 60ppm or less, 55ppm or less, 50ppm or less, 48ppm or less, 46ppm or less, 44ppm or less, 42ppm or less, 41ppm or less, 40ppm or less, 38ppm or less, 36 ppm or less, 34 ppm or less, 30 ppm or less, 25 ppm or less, 20 ppm or less, 15 ppm or less, 10 ppm or less, 5 ppm or less, or 1 ppm or less;

(2) The degree of collagenase expression in the inhibition of collagenase production was 60% or less, 58% or less, 56% or less, 55% or less, 54% or less, 53% or less, 52% or less, 51% or less, 50% Up to 48%, up to 46%, up to 44%, up to 42%, up to 40%, up to 35%, up to 30%, up to 20%, up to 10%, up to 5%, or up to 1%.

In the present specification, the "foliage bean leaf" may mean a soybean leaf in which the color of the soybean leaf is changed yellow during the growth process of the soybean leaf, and the soybean leaf is in the growth stage of the soybean 1) soybean pods and soybean turns yellow (time R7 below) ); From 2) with the leaves falling soybean pods and beans completely yellow (time R8); It means a bean leaf in. Specifically, the “foliage bean leaf” may refer to a bean leaf in which a green or green bean leaf is in a yellow state or a bean leaf in a completely yellow color, and includes a case in which the bean leaf is partially changed to yellow. This is the broadest concept.

As used herein, the term "antioxidant" refers to an effect that can slow down, prevent, or prevent the oxidation process known in the art, and is not limited thereto.

As used herein, 'anti-aging' refers to an effect that can slow down, prevent or prevent the aging process known in the art, and specifically, by effectively inhibiting the expression of collagenase in the skin, it reduces collagen breakdown in the skin, thereby making skin elasticity. It may mean, but is not limited to, the effect of improving the appearance and improving wrinkles.

In one aspect of the invention, the composition may exhibit an activity that inhibits DPPH oxidation, and may exhibit an effect of inhibiting the expression of collagenase or the activity of collagenase. Specifically, in one aspect of the present invention, the composition may be a composition for inhibiting DPPH oxidation, or a composition for inhibiting collagenase expression or activity.

In one aspect of the invention, the composition is the maple leaf extract at least 0.1 μg / ml, 1 μg / ml, 5 μg / ml, 10 μg / ml, 20 μg / ml, 30 μg / ml or more, 50 μg / ml or more, 70 μg / ml or more, 80 μg / ml or more, 90 μg / ml or more, 100 μg / ml or more, 110 μg / ml or more, 120 μg / ml or more, 130 μg / at least 150 μg / ml, at least 170 μg / ml, at least 200 μg / ml, at least 500 μg / ml, or at least 1000 μg / ml, at least 2000 μg / ml, at most 1000 μg / ml, at 500 μg / ml or less, 300 μg / ml or less, 200 μg / ml or less, 170 μg / ml or less, 150 μg / ml or less, 130 μg / ml or less, 120 μg / ml or less, 110 μg / ml or less, 100 μg / ml 90 μg / ml or less, 80 μg / ml or less, 70 μg / ml or less, 50 μg / ml or less, 30 μg / ml or less, 20 μg / ml or less, 10 μg / ml or less, 5 μg / ml or less, 1 μg / ml or less, or 0.1 μg / ml or less.

In one aspect of the invention, the composition is the maple leaf extract 0.001% by weight, 0.01% by weight, 0.1% by weight, 0.5% by weight, 1% by weight, 2% by weight or more, based on the total weight of the composition At least 4%, at least 4%, at least 5%, at least 6%, at least 7%, at least 8%, at least 9%, at least 10%, at least 15%, or at least 20% 20% by weight, 15% by weight, 10% by weight, 9% by weight, 8% by weight, 7% by weight, 6% by weight, 5% by weight, 4% by weight, 3% by weight 2 wt% or less, 1 wt% or less, or 0.1 wt% or less.

In the extraction process of the maple bean leaf extract of the present specification, for example, washed and dried finely divided maple leaf powder in water or an organic solvent, extracted and deposited, and then separating the residue and the filtrate through filtration and centrifugation of filter cloth. , The concentrated filtrate is concentrated under reduced pressure to obtain a maple leaf extract. In one aspect of the invention, the organic solvent that can be used for extraction may be selected from ethanol, methanol, butanol, ether, ethyl acetate, chloroform or a mixed solvent of these organic solvents and water, preferably considering the safety of the raw material Use water or ethanol at 30-70% concentration. After obtaining the extract using a solvent in the above can be obtained by cooling, heating and filtration at room temperature in a conventional manner known in the art to obtain a liquid, or may further evaporate the solvent, spray drying or freeze drying, but The present invention is not limited thereto, and any method generally used in the art may be used without limitation.

In an aspect of the present invention, maple bean leaf extract may be extracted from the soybean leaves of R7 to R8 step of the growth of the following beans. In this specification, the growth stage of the beans is as follows.

VE time: 1 to 2 weeks after planting seeds, cotyledons from soil

VC season: Cotyledon blooms wide, a word grows over it, and leaves are formed.

Period V1: A word is formed from the first outer leaf, resulting in three leaves.

V2 phase: One more word from V1 Stage, resulting in 3 leaves

V3 phase: Three more leaves are created in the V2 Stage.

V4 season: 3 more leaves are created in V3 Stage.

R2 season: Beanstalk in full bloom

R4 season: Soybean pod creation complete

R5 season: Soybeans are produced in the pods

R6 season: Green beans in the pods

R7 season: Soybean pods and beans turning yellow

R8 season: Soybean pods and soybeans completely yellow as leaves fall

In one aspect of the present invention, the 'bean' is not limited in kind, for example, Seoritae (Seoritae, Glycin max MERR), Seomoktae (Seomoktae, Rhynchosia Nolubilis ), Black soybean, Glycine max (L.) Merr.), cheongtae (blue bean, Glycime max MERR) , hwangtae (yellow bean, Glycime max MERR) , fence bean (field bean, Vicia faba), kidney bean (kidney bean, Phaseolus vulgaris), stains kidney bean (pinto bean, Phaseolus vulgaris L.), red beans (small red bean, Vigna angularis ), soybeans (small black bean, Phaseolus angularis WF WIGHT.), bean sprouts (sprouting bean, Glycine max (L.) Merr.) and soybeans (soybean, Glycine max It may be any one or more selected from the group consisting of, but is not limited thereto.

In one aspect of the invention, 'bean leaf' means the leaf portion of the bean tree.

In one aspect of the invention, an "extract" includes all materials obtained by extracting the components of the natural product, regardless of the extraction method, extraction solvent, extracted component or form of the extract and obtained by extracting the components of the natural product The present invention is a broad concept that includes all materials that can be obtained by extraction or processing or processing by other methods, and specifically, the processing or processing may be further fermentation or enzymatic treatment of the extract. It is a broad concept including fractions, fermentations, concentrates, dry matters, and specifically, the extract herein may be a fermentation product.

In one aspect of the invention, the "foliage leaf extract" includes all materials obtained by extracting the components of the maple leaf, regardless of the extraction method, extraction solvent, extracted component or form of the extract and extracts the components It includes the material obtained by the extraction method including the process of treatment with heat, acid, base, enzyme, etc. in the process, and extracts the material obtained by extracting the components of the maple leaf and then processed by another method or It is a broad concept that includes all of the materials that can be obtained by treatment. Specifically, the processing or treatment may be to perform fermentation or enzyme treatment, such as maple leaf extract. Thus, in one aspect of the invention, the maple bean leaf extract may be a fermentation product.

In one aspect of the present invention, the "foliage bean leaf" may be in the form of an extract, or raw (bean) raw maple leaves, the pulverized product of the herbal medicine, dried product of the herbal medicine, dry ground product of the herbal medicine, fermented product of the maple bean leaves, It is not limited to this. In addition, the maple bean leaf used in the present specification is not limited to the acquisition method, may be grown and used or purchased commercially available, may use part or all of the ground or root portion of the herbal. More specifically, one or more selected from the group consisting of leaves, stems, roots, and flowers of maple leaf herb may be used, and more specifically, flowers, leaves, and stems may be used. In one aspect of the present invention, the maple bean leaf is not necessarily produced through drying and is not limited as long as it is a raw material of a form suitable for extracting the active ingredient of the maple bean leaf.

In one aspect of the invention, the maple leaf extract may be one or more extracts selected from the group consisting of water, organic solvents and mixtures thereof.

In one aspect of the invention, the water comprises distilled or purified water, the organic solvent is selected from the group consisting of C ₁ ~ C ₆ Lower alcohol, acetone, ether, ethyl acetate, diethyl ether, ethyl methyl ketone and chloroform Including but not limited to one or more. Specifically, the alcohol may be methanol or ethanol.

In one aspect of the invention, maple leaf extract may be an extract sequentially extracted with ethanol and ethyl acetate.

In one aspect of the invention, the maple leaf extract may comprise an ethyl acetate extract of maple beans.

In one aspect of the invention, the maple leaf extract or a composition comprising the same as an active ingredient may be obtained by a manufacturing method comprising the step of extracting the maple bean leaves with water, an organic solvent, or a mixture thereof. Specifically, in one aspect of the present invention, the manufacturing method may include the steps of: extracting the maple bean leaf with water, an organic solvent, or a mixture thereof; Thereafter adding an organic solvent to the primary extract and performing secondary extraction; It may be a method comprising the step of concentrating and drying the secondary extract under reduced pressure.

In one aspect of the present invention, maple bean leaf extract or a composition comprising the same as an active ingredient may be prepared by a manufacturing method according to an aspect of the present invention.

In one aspect, the present invention may relate to a method of preparing a maple leaf extract or a composition comprising the same, including extracting maple leaf with water, an organic solvent, or a mixture thereof.

In one aspect of the invention, the method may further comprise the step of washing and then drying the soybean leaves with purified water before the extraction step and then semalization.

In one aspect of the invention, the method may further include a second extraction step of extracting once more by adding an organic solvent to the extract after the extraction step, specifically, the secondary extraction step is the solution is separated into two layers It may be to take the upper portion (organic solvent layer). In this case, the first extraction step is called a primary extraction step.

In one aspect of the invention, the secondary extraction step may be repeated one or more times, two or more times, or three or more times with respect to the same solution, specifically taking the upper layer (organic solvent layer) separated by an organic solution Thereafter, the organic layer may be added to the lower layer (water layer) again and may be repeated as if the upper layer was taken in the same manner. Specifically, the organic solvent may be ethyl acetate.

In one aspect of the invention, the method may further comprise the step of concentration and drying the extract under reduced pressure after the second extraction step.

In one aspect of the invention, the maple leaf extract may be a crude extract of water, an organic solvent, and a solvent selected from the group consisting of a combination thereof. The organic solvent may be a C ₁ -C ₆ alcohol, and specifically, the C ₁ -C ₆ alcohol may be methanol or ethanol. In one aspect of the present invention, when the maple leaf is extracted with a solvent, it is preferable to extract by adding a solvent corresponding to about 5 to 15 times the maple leaf, specifically to extract by adding a solvent of about 10 times However, the present invention is not limited thereto.

In one aspect of the present invention, the extraction may be used, such as hot water extraction, ethanol extraction, heat extraction, cold extraction, reflux extraction, reflux cooling extraction, or ultrasonic extraction, there is no limitation if the extraction is obvious to those skilled in the art, Extraction may be hot water extraction or ethanol extraction.

In one aspect of the invention, the extraction may be carried out at room temperature, but for more efficient extraction may be carried out under warm conditions, preferably at a temperature of about 40 to 100 ℃, more preferably about 80 ℃ It may be, but is not limited thereto. Extraction time may be performed for about 2 to about 14 hours, specifically 8 hours to 14 hours, more specifically 11 hours to 13 hours, most specifically 12 hours, but is not limited thereto. It may vary depending on conditions such as temperature. The extraction may be extracted one or more times several times in order to obtain a larger amount of the active ingredient, preferably one to five times, more preferably three times the continuous extraction can be used combined extract.

In one aspect of the present invention, the maple leaf extract may include crude extracts of maple beans as described above, may be included as a soluble fraction of the organic solvent obtained by further extracting the crude extract with a low polar organic solvent. . In an aspect of the present invention, an organic solvent may be hexane, methylene chloride, ethyl acetate, n-butanol, and the like, but is not limited thereto. The extract extracted by the above method or a soluble fraction of the extract may be used as it is, but may be used in the form of an extract by concentrating after filtration, may be used as a form of dried by drying after concentration.

In one aspect of the present invention, the drying may be evaporation drying, spray drying, freeze drying, and specifically, freeze drying may be performed at -50 to -70 ° C. for 3 to 4 days.

In one aspect of the present invention, the cosmetic composition is not particularly limited in formulation, and may be appropriately selected as desired. For example, skin lotion, skin softener, skin toner, astringent, lotion, milk lotion, moisturizing lotion, nutrition lotion, massage cream, nutrition cream, moisturizing cream, hand cream, foundation, essence, nutrition essence, pack, soap, cleansing It may be prepared in any one or more formulations selected from the group consisting of foam, cleansing lotion, cleansing cream, body lotion and body cleanser, but is not limited thereto.

When the formulation of the cosmetic composition according to an aspect of the present invention is a paste, cream or gel, the carrier component is animal fiber, vegetable fiber, wax, paraffin, starch, tracant, cellulose derivative, polyethylene glycol, silicone, bentonite, silica, talc Or zinc oxide may be used.

When the formulation of the cosmetic composition according to an aspect of the present invention is a powder or a spray, lactose, talc, silica, aluminum hydroxide, calcium silicate or polyamide powder may be used as the carrier component, and particularly in the case of a spray Propellants such as chlorofluorohydrocarbons, propane / butane or dimethyl ether.

When the formulation of the cosmetic composition according to an aspect of the present invention is a solution or an emulsion, a solvent, a solvating agent or an emulsifying agent is used as a carrier component, for example, water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl Fatty acid esters of benzoate, propylene glycol, 1,3-butylglycol oil, glycerol aliphatic ester, polyethylene glycol or sorbitan.

When the formulation of the cosmetic composition according to an aspect of the present invention is a suspension, a liquid diluent such as water, ethanol or propylene glycol, ethoxylated isostearyl alcohol, polyoxyethylene sorbitol ester and polyoxyethylene sorbitan ester may be used as a carrier component. The same suspending agent, microcrystalline cellulose, aluminum metahydroxy, bentonite, agar or tracant and the like can be used.

In the case of surfactant-containing cleansing of the cosmetic composition according to an aspect of the present invention, as a carrier component, an aliphatic alcohol sulfate, an aliphatic alcohol ether sulfate, a sulfosuccinic acid monoester, an isethionate, an imidazolinium derivative, a methyltaurate, a sarco Cinates, fatty acid amide ether sulfates, alkylamidobetaines, aliphatic alcohols, fatty acid glycerides, fatty acid diethanolamides, vegetable oils, linolin derivatives or ethoxylated glycerol fatty acid esters and the like can be used.

The cosmetic composition according to an aspect of the present invention may further include functional additives and components included in the general cosmetic composition in addition to the maple bean leaf extract. The functional additive may include a component selected from the group consisting of water-soluble vitamins, oil-soluble vitamins, polymer peptides, polymer polysaccharides, sphingolipids and seaweed extract.

In one aspect of the present invention, the cosmetic composition may further contain, in addition to the functional additives, a component contained in a general cosmetic composition, if necessary. In addition to the other components included, oils and fats, moisturizers, emollients, surfactants, organic and inorganic pigments, organic powders, ultraviolet absorbers, preservatives, fungicides, antioxidants, plant extracts, pH adjusters, alcohols, pigments, flavorings, blood circulation And accelerators, cooling agents, limiting agents, purified water, and the like.

Furthermore, in one aspect, the present invention relates to an external preparation for skin containing maple leaf extract as an active ingredient, wherein the external preparation for skin is a generic term that may include anything applied outside the skin, and cosmetics of various formulations are included herein. May be included.

The pharmaceutical composition according to one aspect of the present invention may be various oral or parenteral formulations. When formulated, diluents or excipients such as fillers, extenders, binders, wetting agents, disintegrating agents, and surfactants are usually used. Solid form preparations for oral administration include tablets, pills, powders, granules, soft or hard capsules, and the like, which may contain at least one excipient such as starch, calcium carbonate, sucrose, or the like. Or lactose, gelatin, or the like is mixed. In addition to simple excipients, lubricants such as magnesium stearate, talc and the like are also used. Liquid preparations for oral administration include suspensions, liquid solutions, emulsions, and syrups, and various excipients such as wetting agents, sweeteners, fragrances, and preservatives, in addition to commonly used simple diluents such as water and liquid paraffin, may be included. have. Formulations for parenteral administration include sterile aqueous solutions, non-aqueous solvents, suspensions, emulsions, lyophilized preparations, suppositories. As the non-aqueous solvent and the suspension solvent, propylene glycol, polyethylene glycol, vegetable oils such as olive oil, injectable esters such as ethyl oleate, and the like can be used. As the base of the suppository, witepsol, macrogol, tween 61, cacao butter, laurin butter, glycerogelatin and the like can be used.

In one aspect of the invention, the pharmaceutical dosage forms of the compositions may be used in the form of their pharmaceutically acceptable salts, and may also be used alone or in combination with other pharmaceutically active compounds as well as in a suitable collection. The salt is not particularly limited as long as it is pharmaceutically acceptable. For example, hydrochloric acid, sulfuric acid, nitric acid, phosphoric acid, hydrofluoric acid, hydrobromic acid, formic acid acetic acid, tartaric acid, lactic acid, citric acid, fumaric acid, maleic acid, succinic acid, methanesulfonic acid , Benzene sulfonic acid, toluene sulfonic acid, naphthalene sulfonic acid and the like can be used.

In one aspect of the invention, the composition may be parenterally or orally administered as desired, and may be administered in an amount of 0.1 to 500 mg, preferably 1 to 100 mg per kg of body weight per day Can be administered in divided doses. The dosage for a particular patient may vary depending on the patient's weight, age, sex, health condition, diet, time of administration, method of administration, rate of excretion, severity of the disease, and the like.

The pharmaceutical composition according to one aspect of the present invention may be a powder, granules, tablets, soft or hard capsules, suspensions, emulsions, syrups, aerosols, oral formulations, ointments, creams, etc. It may be used in any form suitable for pharmaceutical preparations, including suppositories, injectables and sterile injectable solutions, and preferably in the form of injections or external preparations for the skin.

The composition according to an aspect of the present invention may be administered to mammals such as rats, mice, livestock, humans by various routes, such as parenteral, oral, and all modes of administration may be expected. It may be administered by oral, transdermally, rectal or intravenous, intramuscular, subcutaneous, intrauterine dural or intracerebroventricular injection.

The composition according to one aspect of the present invention may be administered by various routes that can be easily applied by those skilled in the art. In particular, the pharmaceutical composition according to an aspect of the present invention may be administered by a route applied to the skin surface as an external preparation for skin.

Hereinafter, the configuration and effects of the present invention will be described in more detail with reference to Examples and Test Examples. However, these examples and test examples are provided only for the purpose of illustration in order to help the understanding of the present invention is not limited to the scope and scope of the present invention by the following examples.

Example 1 Preparation of Soybean Leaf Extract

The soybean leaves collected at each growth period (VC / V2 / V4 / R2 / R4 / R6 / R7, 7 total) were washed with purified water, dried and then granulated. 100 g of the bean leaf powder was added to 1 liter of an aqueous 70% by weight ethanol solution, and extracted at room temperature (25 ° C.) for 12 hours, followed by filtration with a 300 mesh filter cloth. The extract was added to a 3-liter separatory funnel, and 1 liter of ethyl acetate was added. After shaking, the mixture was shaken and completely separated into two layers to obtain an upper layer (ethyl acetate layer). The lower layer (water layer) is again extracted twice with a separatory funnel. Each separated upper layer was combined and concentrated under reduced pressure at 50 ° C. using a distillation apparatus equipped with a cooling condenser and dried. Thus, 10.3 g of bean leaf extract of each step was obtained.

Experimental Example 1 Antioxidant Activity Test

In order to determine the antioxidant effect of the soybean leaf extract of each of the VC / V2 / V4 / R2 / R4 / R6 / R7 prepared in Example 1, the organic radical DPPH (1,1-diphenyl-2-picrylhydride Changes in absorbance caused by reduction of lazil; 1,1-diphenyl-2-picryl hydrazyl) were used to compare DPPH antioxidant activity.

190 μl of 100 μM (in ethanol) DPPH solution and the leaf extract of Example VC / V2 / V4 / R2 / R4 / R6 / R7 obtained above and Trolox (positive control), a synthetic antioxidant, were prepared at a concentration of 10,000 ppm. After the preparation, the final reaction concentration was diluted to be 500ppm, 250ppm, 125ppm, 62.5ppm, 31.25ppm, 15.63ppm, and then 10µl each of them was added to make a reaction solution and reacted at 37 ° C for 30 minutes, and the absorbance was measured at 540nm. The analysis results are shown in Table 1 below, and IC ₅₀ means the sample concentration when the absorbance was reduced by 50% by the added sample.

Table 1 Test substance IC ₅₀ (ppm) Concentration ratio to show similar efficacy with R7 season soybean leaf extract Trolox (positive control) 38 VC Season Bean Leaf Extract no effect X V2 Season Bean Leaf Extract no effect X V4 Season Bean Leaf Extract 251 6.1x R2 Season Bean Leaf Extract 168 4.1x R4 Season Bean Leaf Extract 124 3.1x R6 Season Bean Leaf Extract 79 1.9x R7 Season Bean Leaf Extract 41 1x

As can be seen in Table 1, it can be seen that the soybean leaf extract of the R7 step shows the best antioxidant activity among the soybean leaf extracts obtained in each of VC / V2 / V4 / R2 / R4 / R6 / R7. there was. In addition, it was confirmed that the soybean leaf (autumn soybean leaf) extract of the R7 step shows a similar effect effect as trolox.

Experimental Example 2 Anti-Aging Performance Test

Tocopherol (Comparative Example 1) and EGCG (Comparative Example 2) to inhibit the collagenase (collagenase) production of the soybean leaf extract obtained in the respective steps of VC / V2 / V4 / R2 / R4 / R6 / R7 prepared in Example 1 Measured in comparison with. Tocopherols and EGCG are known substances that have the function of regenerating the epidermal cells of the skin to prevent aging of the skin.

Human fibroblasts (Cascade Biologics) (Portland, OR, USA) in 96-well microtiter plates containing DMEM (Dulbecco's Modified Eagle's Media) medium containing 2.5% fetal calf serum. 5,000 cells / well were added and incubated until 90% growth. After culturing for 24 hours in serum-free DMEM medium, 100 ㎍ / ml concentration of soybean leaf extract obtained in each of the steps of VC / V2 / V4 / R2 / R4 / R6 / R7 of Example 1 dissolved in serum-free DMEM medium After treatment with tocopherol and EGCG (Sigma Aldrich) for 10 hours at 10 ^-4 molarity, the cell culture was collected.

The degree of collagenase production of the cell cultures collected using a collagenase measuring instrument (Amersham Pharmacia, USA) was measured. First, the collected cell culture solution was placed in a 96-well plate uniformly coated with primary collagenase antibody, and the antigen-antibody reaction was performed in a thermostat (36 ° C.) for 3 hours.

After 3 hours, the chromophore-conjugated secondary collagen antibody was placed in a 96-well plate and reacted again for 15 minutes. After 15 minutes, add the coloring inducing substance and color it for 15 minutes at room temperature. Then, add 1M sulfuric acid to stop the reaction (color development). The color of the reaction solution becomes yellow, and the degree of yellow varies depending on the progress of the reaction. It was confirmed.

The absorbance of the yellowish 96-well plate (96-well plate) was measured at 405 nm using an absorbance meter, and the degree of synthesis of collagenase was calculated by the following equation (1). At this time, the reaction absorbance of the collected cell culture medium of the group not treated with the composition was used as a control. That is, the expression level of collagenase in the non-treated group was set to 100, and the collagenase expression level in the group treated with the test substance was calculated. The results are shown in Table 2 below.

[Equation 1]

TABLE 2 Test substance Collagenase expression level (%) Untreated group 100 Tocopherol (Comparative Example 1) 74 EGCG (Comparative Example 2) 61 VC Season Bean Leaf Extract 98 V2 Season Bean Leaf Extract 95 V4 Season Bean Leaf Extract 92 R2 Season Bean Leaf Extract 86 R4 Season Bean Leaf Extract 81 R6 Season Bean Leaf Extract 69 R7 Season Bean Leaf Extract 53

As can be seen in Table 2, among the soybean leaf extracts obtained in each of the steps VC / V2 / V4 / R2 / R4 / R6 / R7, the soybean leaf (foliage leaf) extract of R7 stage is the most cola in vitro . It was found that the expression of the genease was effectively suppressed, and the expression of collagenase was superior to that of tocopherol and EGCG, which are known as anti-aging substances. Through this, it can be seen that the extract or the composition comprising the same according to an aspect of the present invention exhibits a significant anti-aging effect.

Experimental Example 3 Irritation Test

In order to compare the usability of a known anti-aging retinol and maple leaf extract (R7 season extract) used as an active ingredient in the present invention, stinging, burning on 15 panels sensitive to irritation such as stinging, burning The degree of back irritation was tested.

Retinol (Retinol, purchased through Sigma) and maple leaf extract obtained in Example 1 solution to the subject at a concentration of 1mg / ml, each 0.5ml randomly applied to the left and right rub between 0 ~ 3.0 by 0.1 point unit To score. The results are shown in Table 3 below.

<Evaluation Criteria>

0 to 0.4: no stimulation

0.5 to 1.0: slightly irritating

1.1 to 2.0: moderate stimulation

2.1 to 3.0: severe irritation

TABLE 3 division Retinol Maple Bean Leaf Extract Stinging 0.87 0.19 Burning 0.42 0.23 Average 0.65 0.21

As can be seen in Table 3, in the case of retinol it was found that there is a feeling of irritation that is usually slightly felt because there is some tingling, burning. On the other hand, the maple leaf extract used in the present invention was almost irritable because it can hardly feel both hot and stinging.

Experimental Example 4 Comparison of Components of Maple Bean Leaf Extract and Bean Extract

Maple bean leaf extract according to an aspect of the present invention to the bean extract obtained as described in Comparative Example 1 of the maple bean leaf extract (R7 time) and Comparative Example 1 in order to confirm that the components are different from the general bean extract HLPC assay experiments were performed.

Comparative Example 1 Preparation of Soybean Extract

Soy beans (paju jangdan bean, purchased from Paju Nonghyup) were washed with purified water, dried and then semalized. 100 g of the soy flour was added to 1 liter of an aqueous 70% by weight ethanol solution and extracted at room temperature (25 ° C.) for 12 hours, followed by filtration with a 300 mesh filter cloth. The extract was added to a 3-liter separatory funnel, and 1 liter of ethyl acetate was added. After shaking, the mixture was shaken and completely separated into two layers to obtain an upper layer (ethyl acetate layer). The lower layer (water layer) is again extracted twice with a separatory funnel. Each separated upper layer was combined and concentrated under reduced pressure at 50 ° C. using a distillation apparatus equipped with a cooling condenser and dried. Thus, 13.4 g of soybean extract was obtained.

In the experiment, the soybean extract and the maple bean leaf extract were dissolved in 70 vol% ethanol, respectively, and made into a 10,000 ppm solution, followed by component analysis (waters, 2996 PDA detector) using HPLC (Waters, 2695 model). The stationary phase used a Mightysil RP-18 GP 250-4.6 (5 μm) column of Kanto Chemical, and the mobile phase used a composition ratio as shown in Table 4 below. These results are shown graphically in FIG. 1.

Table 4 Minutes Water (0.1% Acetic acid) Acetonitrile (0.1% Acetic acid) 0 95 5 65 62 38 70 38 62 75 95 5 80 95 5

According to Figure 1, it can be seen that the maple leaf extract and the bean extract of the comparative example according to an aspect of the present invention shows a completely different appearance in the HPLC results. In particular, it can be seen that the difference in the number and intensity of the peaks appearing in the HPLC results. Therefore, according to these results, it can be seen that the maple leaf extract and the soybean extract have different properties and correspond to different configurations, and accordingly, they will show a difference even in the case of the antioxidant and anti-aging effects to be achieved in the present invention. Can be inferred

Hereinafter, the formulation example of the composition according to an aspect of the present invention, but not intended to limit the present invention is intended to be described in detail only.

Formulation Example 1 Milk Lotion (Nutrition Lotion)

To the nutritional lotion was prepared in a conventional manner according to the composition shown in Table 5.

Table 5 Ingredient weight% Maple Bean Leaf Extract of Example 1 3.00 L-ascorbic acid-2-magnesium phosphate 1.00 Water Soluble Collagen (1% Aqueous Solution) 1.00 Sodium citrate 0.10 Citric acid 0.05 Baekgulchae Extract 0.20 1,3-butylene glycol 3.00 Purified water to 100

Formulation Example 2 Nutrition Cream

Nutritional cream was prepared in a conventional manner according to the composition shown in Table 6.

Table 6 Ingredient weight% Maple Bean Leaf Extract of Example 1 1.00 Polyethylene Glycol Monostearate 2.00 Self-emulsifying glycerin monostearate 5.00 Cetyl alcohol 4.00 Squalene 6.00 Tri2-ethylhexaneglyceryl 6.00 Sphingolipid 1.00 1,3-butylene glycol 7.00 Purified water to 100

[Formulation Example 3] Pack

To prepare a pack in a conventional manner according to the composition described in Table 7.

TABLE 7 Ingredient weight% Maple Bean Leaf Extract of Example 1 5.00 Polyvinyl alcohol 13.00 L-ascorbic acid-2-magnesium phosphate 1.00 Lauroylhydroxyproline 1.00 Water Soluble Collagen (1% Aqueous Solution) 2.00 1,3-butylene glycol 3.00 ethanol 5.00 Purified water to 100

Formulation Example 4 Serum

To prepare a cosmetic liquid in a conventional manner according to the composition shown in Table 8.

Table 8 Ingredient weight% Maple Bean Leaf Extract of Example 1 2.00 Hydroxyethylene cellulose (2% aqueous solution) 12.00 Xanthan gum (2% aqueous solution) 2.00 1,3-butylene glycol 6.00 Dark glycerin 4.00 Sodium Hyaluronate (1% aqueous solution) 5.00 Purified water to 100

Formulation Example 5 Ointment

The ointment was described in a conventional manner according to the composition described in Table 9 below.

Table 9 Compounding ingredient Content (% by weight) Maple Bean Leaf Extract of Example 1 0.1 glycerin 8.0 Butylene glycol 4.0 Liquid paraffin 15.0 Beta Glucan 7.0 Carbomer 0.1 Caprylic / Capric Triglycerides 3.0 Squalane 1.0 Cetearyl Glucoside 1.5 Sorbitan stearate 0.4 Cetearyl Alcohol 1.0 Beeswax 4.0 Preservative, coloring, flavoring Quantity Purified water Remaining amount

Formulation Example 6 Soft Capsule

8 mg of maple leaf extract of Example 1, vitamin E 9 mg, vitamin C 9 mg, palm oil 2 mg, vegetable hardened oil 8 mg, lead 4 mg and lecithin 9 mg were mixed and mixed according to a conventional method to prepare a soft capsule fill solution. 400 mg per capsule is filled to prepare a soft capsule. In addition, a soft capsule sheet was prepared at a ratio of 66 parts by weight of gelatin, 24 parts by weight of glycerine, and 10 parts by weight of sorbitol solution and filled with the filler to prepare a soft capsule containing 400 mg of the composition according to an aspect of the present invention. do.

Formulation Example 7 Tablets

8 mg of maple leaf extract of Example 1, 9 mg of vitamin E, 9 mg of vitamin C, 200 mg of galactooligosaccharide, 60 mg of lactose and 140 mg of maltose were granulated using a fluidized bed drier, and then 6 mg of sugar ester was added. Add. Tablets are prepared by tableting 500 mg of these compositions in a conventional manner.

Formulation Example 8 Drinks

After mixing 8 mg of maple leaf extract of Example 1, 9 mg of vitamin E, 9 mg of vitamin C, 10 g of glucose, 0.6 g of citric acid, and 25 g of liquid oligosaccharide, 300 ml of purified water was added to each bottle to fill 200 ml. After filling the bottle sterilized for 4 to 5 seconds at 130 ℃ to prepare a drink.

Formulation Example 9 Granules

8 mg of maple leaf extract of Example 1, 9 mg of vitamin E, 9 mg of vitamin C, 250 mg of anhydrous glucose, and 550 mg of starch were mixed, molded into granules using a fluidized bed granulator, and then filled into fabrics to prepare granules.

Formulation Example 10 Injection

Injectables were prepared by conventional methods according to the compositions set forth in Table 10 below.

Table 10 Compounding ingredient content Maple Bean Leaf Extract of Example 1 10-50 mg Sterile Distilled Water for Injection Quantity pH regulator Quantity

Formulation Example 11 Health Functional Food

To prepare a health functional food in a conventional manner according to the composition shown in Table 11.

Table 11 Compounding ingredient content Maple Bean Leaf Extract of Example 1 20mg Vitamin A Acetate 70 μg Vitamin E 1.0mg Vitamin B1 0.13mg Vitamin B2 0.15mg Vitamin B6 0.5mg Vitamin B12 0.2 μg Vitamin c 10mg Biotin 10 μg Nicotinic acid amide 1.7mg Folic acid 50 μg Calcium Pantothenate 0.5mg Ferrous sulfate 1.75mg Zinc oxide 0.82 mg Magnesium carbonate 25.3 mg Potassium phosphate monobasic 15 mg Dicalcium Phosphate 55 mg Potassium citrate 90 mg Calcium carbonate 100mg Magnesium chloride 24.8 mg

Although the composition ratio of the said vitamin and mineral mixture was mixed and consisted with the component suitable for a health functional food in a preferable Example, you may change arbitrarily the compounding ratio.

Formulation Example 12 Healthy Drink

To prepare a health drink in a conventional manner according to the composition shown in Table 12.

Table 12 Compounding ingredient content Maple Bean Leaf Extract of Example 1 1000 mg Citric acid 1000 mg oligosaccharide 100 g Taurine 1 g Purified water Remaining amount

The above ingredients are mixed according to a conventional method for preparing a health beverage, then stirred and heated at 85 ° C. for about 1 hour, and then the resulting solution is filtered and sterilized.

As described above in detail the specific parts of the present invention, it is apparent to those skilled in the art that such specific description is merely a preferred embodiment, thereby not limiting the scope of the present invention. something to do. Thus, the substantial scope of the present invention will be defined by the appended claims and their equivalents.

Claims (13)

Skin external composition comprising maple leaf extract as an active ingredient. Antioxidant or anti-aging composition comprising maple bean extract as an active ingredient. The composition of claim 1 or 2, wherein the maple bean leaves are soybean leaves of R7 to R8 during the growing stage of the beans. The composition of claim 1 or 2, wherein the composition comprises 0.001 to 20% by weight maple leaf extract, based on the total weight of the composition. The composition of claim 1 or 2, wherein the maple leaf extract is at least one extract selected from the group consisting of water, organic solvents and mixtures thereof. The composition of claim 5, wherein the organic solvent is at least one selected from the group consisting of C ₁ to C ₆ lower alcohols, acetone, ether, ethyl acetate, diethyl ether, ethyl methyl ketone, and chloroform. The composition of claim 6, wherein the maple leaf extract is an extract sequentially extracted with ethanol and ethyl acetate. The composition of claim 1 or 2, wherein the composition inhibits oxidation of DPPH (1,1-diphenyl-2-picryl hydrazyl). The composition of claim 1 or 2, wherein the composition inhibits the expression of collagenase. The composition of claim 1 or 2, wherein the composition is a pharmaceutical or cosmetic composition. The composition of claim 2, wherein the composition is a food composition. The method of claim 1 or 2, wherein the maple leaf extract comprises the steps of first extracting the maple bean leaves with water, an organic solvent, or a mixture thereof; Thereafter adding an organic solvent to the primary extract and performing secondary extraction; A composition obtained by the method comprising the step of concentrating and drying the secondary extract under reduced pressure. The composition according to claim 1 or 2, wherein the composition is a composition in which the Maple Bean Leaf extract has one or more of the following properties: (1) In the antioxidant activity test by DPPH reduction, the IC ₅₀ is 70 ppm or less; (2) Collagena Collagenase expression is less than 55% in the production inhibition experiment.

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