KR20200077750A - Composition for skin whitening comprising Cacalia firma extract produced by enzyme treatment as effective component - Google Patents

Abstract

The present invention relates to a composition for skin whitening comprising a Cacalia firma extract produced by enzyme treatment as an effective ingredient. According to the present invention, the Cacalia firma extract obtained through with viscozyme or pectinex enzyme treatment has a remarkably excellent effect of inhibiting the melanin biosynthesis of melanoma cells increased by α-MSH compared to an ethanol extract of Cacalia firma. Accordingly, the composition of the present invention, which contains the Cacalia firma extract produced from enzyme treatment as an effective component, may be used in a functional cosmetic product for skin whitening, a health functional food, or a therapeutic agent for skin pigmentation diseases, which may prevent or ameliorate skin pigmentation diseases.

Description

Composition for skin whitening comprising Cacalia firma extract produced by enzyme treatment as effective component}

The present invention relates to a composition for skin whitening containing an extract obtained by enzymatic treatment as an active ingredient.

Since ancient times, white and bright skin has been recognized as a symbol of health and fame as well as beauty. Melanocytes in the basement layer at the bottom of the epidermis make melanin by various stimulating factors of the skin and send it to the upper layer. When this melanin reaches the stratum corneum, the skin looks black. Factors involved in melanin formation include follicle hormones, progesterone, pigment cell stimulating hormone, UV rays of sunlight, stress, and heredity.

It is called skin whitening to quickly release unnecessary melanin pigment and restore the transparency of the person's original skin. A mulberry extract, arbutin, ethyl ascorbyl ether, oil-soluble licorice extract, ascorbyl glucoside, niacinamide, alpha-bisabolol, and ascorbyltetraisopalmitate are registered as whitening ingredients by the Food and Drug Administration, and using such substances, lotions Whitening cosmetics are made with ina liquids, creams, and mask packs.

The mulberry extract, arbutin, alpha-bisabolol and oil-soluble licorice extract inhibit the activation of tyrosinase, an enzyme involved in making melanin, and ascorbyl glucoside, ethyl ascorbyl ether and ascorbyltetraisopalmitate are tyrosinase enzymes Inhibits the oxidation of the stimulated tyrosine, and niacinamide inhibits the step in which melanin, which has already been produced, passes from melanocytes to keratinocytes, thereby preventing the last step of melanin from actually entering the skin cells.

The representative material used for medical purposes other than beauty is hydroquinone, which is prescribed as a medicine. Hydroquinone is mainly used as a skin ointment. To purchase an ointment containing 4% or more of this substance in Korea, you must have a doctor's prescription, and a 2% ointment can be purchased at a pharmacy without a prescription. Hydroquinone ointment used for medical purposes, unlike whitening cosmetics, directly destroys skin cells with melanin to help new skin cells grow.

However, the above substances have a problem in that the application range of the product is narrow, such as the effect of inhibiting tyrosinase activity only at a relatively high concentration, or the stability is low for a long time, and hydroquinone is due to skin irritation and stability problems. Use in cosmetics is limited.

On the other hand, Cacalia firma ( Cacalia firma) is also known as a large screen and a screen, and is a perennial herbaceous plant belonging to the Chrysanthemum family, and is distributed in forests of deep mountains in northeastern Korea and China. The height is 1~2m, and the root leaf has long and round petioles, the shape of the heart bottom is 27~32cm in diameter, the edges are divided into 11~15 pieces, and the forked pieces are triangular egg-shaped and irregular serrated. . Flowers bloom in June-August in yellowish-white colors, and shoots on the branches of the cone-shaped inflorescence, and the fruit has a light grayish-white feather. The plant has a unique scent, and young plants are eaten as herbs. Currently, there have been few known cases of domestic and foreign research on Byungpung Ssam, and studies on the efficacy of Byungpung Ssam have been incomplete.

On the other hand, prior art related to whitening discloses a composition for skin whitening using an extract of an enzyme treatment of wild ginseng seeds in Korean Registered Patent No. 18673501, and Korean Registered Patent No. 1546339 uses a tangerine peel enzyme treatment or an extract thereof. Although a composition for skin whitening has been disclosed, it has not been disclosed about a composition for skin whitening containing the Byeongpungsam extract obtained through the enzyme treatment of the present invention as an active ingredient.

The present invention was derived by the above-mentioned needs, and provides a composition for skin whitening containing Byeongpungsam extract obtained through enzymatic treatment as an active ingredient, and Byungpungsam extract obtained through the enzyme treatment does not process enzymes. The present invention was completed by confirming that the effect of reducing melanin biosynthesis is superior to that of Byeongpungsam extract.

In order to solve the above problems, the present invention

1) Drying and pulverizing Byeongpung Ssam to prepare Byeongpung Ssam powder;

2) adding water and a hydrolase to the Byeongpungsam powder of step 1), followed by hydrolysis; And

3) a hydrolyzate of the above step 2) water, C ₁ ~ C ₄ lower alcohol or extracting process the mixtures thereof; the folding rolls (Cacalia manufacture, including firma ) It provides a cosmetic composition for skin whitening containing the extract as an active ingredient.

In addition, the present invention

1) Drying and pulverizing Byeongpung Ssam to prepare Byeongpung Ssam powder;

2) adding water and a hydrolase to the Byeongpungsam powder of step 1), followed by hydrolysis; And

3) a hydrolyzate of the above step 2) water, C ₁ ~ C ₄ lower alcohol or extracting process the mixtures thereof; the folding rolls (Cacalia manufacture, including firma ) It provides a pharmaceutical composition for the prevention or treatment of melanin hyperpigmentation disease containing the extract as an active ingredient.

In addition, the present invention

1) Drying and pulverizing Byeongpung Ssam to prepare Byeongpung Ssam powder;

2) adding water and a hydrolase to the Byeongpungsam powder of step 1), followed by hydrolysis; And

3) a hydrolyzate of the above step 2) water, C ₁ ~ C ₄ lower alcohol or extracting process the mixtures thereof; the folding rolls (Cacalia manufacture, including firma ) Provides a health functional food composition for preventing or improving melanin pigmentation excessive deposition disease containing an extract as an active ingredient.

The present invention relates to a composition for skin whitening containing the Byeongpung Ssam extract obtained through enzymatic treatment as an active ingredient, and the Byungpung Ssam extract obtained through the enzyme treatment of the present invention is excellent in inhibiting melanin biosynthesis, thus The composition of the present invention containing the obtained Byeongpungsam extract as an active ingredient may be used as a functional material for skin whitening.

1 is a result confirming the melanin biosynthesis inhibitory effect of the Byeongpungsam extract prepared by each manufacturing method. α-MSH is a melanin biosynthesis inducer, and arbutin is a positive control. **, *** means that the melanin biosynthesis was statistically significantly reduced compared to the Byeongpungsam ethanol extract treated group, ** is p<0.01, *** is p<0.001.

The present invention

1) Drying and pulverizing Byeongpung Ssam to prepare Byeongpung Ssam powder;

2) adding water and a hydrolase to the Byeongpungsam powder of step 1), followed by hydrolysis; And

3) a hydrolyzate of the above step 2) water, C ₁ ~ C ₄ lower alcohol or extracting process the mixtures thereof; the folding rolls (Cacalia manufacture, including firma ) relates to a cosmetic composition for skin whitening containing an extract as an active ingredient.

The hydrolase of step 2) may be pectinase, carbohydrase, or a mixture thereof, preferably pectin hydrolase or carbohydrate hydrolase, more preferably Is Pectinex or Viscozyme, but is not limited thereto.

The pectin hydrolase pectinex is a commercial enzyme, an enzyme having the activity of pectinase and hemicellulase, and the carbohydrate hydrolase biscozyme is a commercial enzyme, aspergillus aculea It is a complex enzyme containing arabinase, cellulase, beta-glucanase, hemicellulase and xylanase derived from Aspergillus aculeatus .

In one embodiment of the present invention, after the step 3), the step of ultra-high pressure homogenization; may further include; preferably after step 3), the step of ultra-high pressure homogenization under a pressure of 100 ~ 130MPa; It includes, but is not limited to.

In the present invention, the skin whitening effect is an effect of improving or preventing dark skin, blemishes, freckles, and dark circles caused by various factors such as exposure to ultraviolet rays, changes in hormone balance, and genetic programs, and the skin is beautiful with transparency It is intended to have the effect of maintaining a beautiful skin that is transparent or transparent, an effect of reducing the dullness of the skin, and increasing the gloss and tautness. In general, it is known that melanocytes are stimulated by dark skin, blemishes, freckles, and dark circles due to stimulation by ultraviolet rays or changes in hormone balance, and thus, biosynthesized melanin pigments are deposited on the skin. Therefore, if melanin production can be suppressed, it is possible to prevent and improve dark skin, blemishes, freckles, and dark circles.

In the cosmetic composition according to an embodiment of the present invention, the cosmetic composition for skin whitening is skin, skin softener, skin toner, lotion, milk lotion, moisture lotion, nutrition lotion, massage cream, nutrition cream, eye cream, moisturizer Cream, hand cream, essence, nutrition essence, pack, cleansing foam, cleansing water, cleansing cream, body lotion, body cleanser, soap and powder may have any one selected from the formulation, but is not limited thereto. The cosmetic composition composed of each of these formulations may contain various bases and additives necessary and appropriate for the formulation of the formulation, and the types and amounts of these components can be easily selected by those skilled in the art.

The cosmetic composition of the present invention may contain one or more skin whitening active ingredients exhibiting the same or similar function in addition to the active ingredient. Skin whitening active ingredients include kojic acid and its derivatives, arbutin, ascorbic acid and its derivatives, hydroquinone and its derivatives, resorcinol, cycloalkanone, methylenedioxyphenyl alkanol, 2,7-dinitroindazole or There are vine extracts, rice extracts, plant extracts such as licorice extract, but are not limited thereto.

When the formulation of the cosmetic composition of the present invention is a paste, cream or gel, animal fibers, plant fibers, wax, paraffin, starch, tragacanth, cellulose derivatives, polyethylene glycol, silicone, bentonite, silica, talc or zinc oxide as carrier components Etc. can be used.

When the formulation of the cosmetic composition of the present invention is a powder or a spray, lactose, talc, silica, aluminum hydroxide, calcium silicate or polyamide powder may be used as a carrier component, and in the case of a spray, additionally, chlorofluorohydro Propellants such as carbon, propane-butane or dimethyl ether.

When the formulation of the cosmetic composition of the present invention is a solution or emulsion, a solvent, solvating agent or emulsifying agent is used as a carrier component, such as water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, and propylene Glycols, 1,3-butylglycol oil, glycerol aliphatic esters, polyethylene glycol or fatty acid esters of sorbitan.

When the formulation of the cosmetic composition of the present invention is a suspension, as a carrier component, liquid diluents such as water, ethanol or propylene glycol, suspensions such as ethoxylated isostearyl alcohol, polyoxyethylene sorbitol ester and polyoxyethylene sorbitan ester, Microcrystalline cellulose, aluminum metahydroxide, bentonite, agar or trakant, etc. can be used.

When the formulation of the cosmetic composition of the present invention is a surfactant-containing cleansing agent, aliphatic alcohol sulfate, aliphatic alcohol ether sulfate, sulfosuccinic acid monoester, acethionate, imidazolinium derivative, methyltaurate, sarcosinate as a carrier component , Fatty acid amide ether sulfates, alkylamidobetaines, fatty alcohols, fatty acid glycerides, fatty acid diethanolamides, vegetable oils, linoline derivatives or ethoxylated glycerol fatty acid esters and the like.

The cosmetic composition of the present invention may further contain excipients including fluorescent materials, fungicides, oleogenic agents, moisturizers, fragrances, fragrance carriers, proteins, solubilizers, sugar derivatives, sunscreens, vitamins, plant extracts, etc. .

In addition, the present invention

1) Drying and pulverizing Byeongpung Ssam to prepare Byeongpung Ssam powder;

2) adding water and a hydrolase to the Byeongpungsam powder of step 1), followed by hydrolysis; And

3) a hydrolyzate of the above step 2) water, C ₁ ~ C ₄ lower alcohol or extracting process the mixtures thereof; the folding rolls (Cacalia manufacture, including firma ) It relates to a pharmaceutical composition for the prevention or treatment of melanin hyperpigmentation disease containing the extract as an active ingredient.

As used herein, the term "hyperpigmentation of melanin" means to become darker or darker than other sites due to excessive increase in melanin in certain areas of the skin or nails. The melanin hyperpigmentation disease is hyperpigmentation after inflammation due to freckles, senile plaques, liver spots, blemishes, brown or black spots, daylight pigment spots, cyanic melasma, hyperpigmentation after drug use, scratches, burns or dermatitis Calming or gestational gravoids (gravidic chloasma), and the like.

The pharmaceutical composition of the present invention may include a pharmaceutically acceptable carrier in addition to the active ingredient, and such a carrier is commonly used in preparation, such as lactose, dextrose, sucrose, sorbitol, mannitol, starch, acacia rubber, Calcium phosphate, alginate, gelatin, calcium silicate, microcrystalline cellulose, polyvinylpyrrolidone, cellulose, water, syrup, methyl cellulose, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate and minerals Oil, and the like, but is not limited thereto. The pharmaceutical composition of the present invention may further include a lubricant, a wetting agent, a sweetener, a flavoring agent, an emulsifying agent, a suspending agent, a preservative, etc. in addition to the above components.

Suitable dosages of pharmaceutical compositions according to the invention are variously prescribed by factors such as formulation method, mode of administration, patient's age, weight, sex, morbidity, food, time of administration, route of administration, rate of excretion and response sensitivity. Can be.

The pharmaceutical composition of the present invention may be administered orally or parenterally, and in the case of parenteral administration, topically applied to the skin, intravenous injection, subcutaneous injection, intramuscular injection, intraperitoneal injection, transdermal administration, and the like. Considering that the pharmaceutical composition of the present invention is applied for the treatment or prevention of melanin hyperpigmentation disease, it is preferable to be applied topically to the skin.

The concentration of the active ingredient contained in the composition of the present invention can be determined in consideration of the purpose of treatment, the patient's condition, and the required period, and is not limited to a specific range of concentration.

The pharmaceutical composition of the present invention is prepared in a unit dose form by formulating using a pharmaceutically acceptable carrier or excipient according to a method that can be easily carried out by those skilled in the art to which the present invention pertains, or It can be prepared by incorporating into a dose container. At this time, the formulation may be prepared as any one of a formulation selected from injections, creams, patches, sprays, ointments, warning agents, lotions, linen agents, pasta agents, and cataplasmas, and may additionally include dispersants or stabilizers. have.

In addition, the present invention

1) Drying and pulverizing Byeongpung Ssam to prepare Byeongpung Ssam powder;

2) adding water and a hydrolase to the Byeongpungsam powder of step 1), followed by hydrolysis; And

3) a hydrolyzate of the above step 2) water, C ₁ ~ C ₄ lower alcohol or extracting process the mixtures thereof; the folding rolls (Cacalia manufacture, including firma ) It relates to a health functional food composition for preventing or improving melanin hyperpigmentation disease containing an extract as an active ingredient.

When the health functional food composition of the present invention is used as a food additive, the health functional food composition may be added as it is or used with other foods or food ingredients, and may be suitably used according to a conventional method. The amount of the active ingredient may be appropriately used depending on the purpose of use (prevention or improvement). In general, the health functional food composition of the present invention in the manufacture of a food or beverage is added in an amount of 15 parts by weight or less, preferably 10 parts by weight or less with respect to the total raw material. However, when ingested for a long period of time for health purposes, the amount may be below the above range, and since there is no problem in terms of safety, the active ingredient may be used in an amount above the above range.

There are no particular restrictions on the type of the health functional food. Examples of foods to which the health functional food composition can be added are meat, sausage, bread, chocolate, candy, snacks, confectionery, pizza, ramen, other noodles, gum products, dairy products including ice cream, various soups, beverages, tea Drinks, alcoholic beverages, and vitamin complexes are included, and all health foods in the ordinary sense are included.

In addition, the health functional food composition of the present invention may be prepared as a food, particularly a functional food. The functional food of the present invention includes ingredients that are conventionally added during food production, and includes, for example, proteins, carbohydrates, fats, nutrients, and seasonings. For example, when manufactured as a drink agent, natural carbohydrates or flavoring agents may be included as additional ingredients in addition to the active ingredient. The natural carbohydrates include monosaccharides (eg, glucose, fructose, etc.), disaccharides (eg, maltose, sucrose, etc.), oligosaccharides, polysaccharides (eg, dextrins, cyclodextrins, etc.) or sugar alcohols (eg. , Xylitol, sorbitol, erythritol, and the like). The flavoring agent may be a natural flavoring agent (for example, taumatin, stevia extract, etc.) and a synthetic flavoring agent (for example, saccharin, aspartame, etc.).

Various nutritional supplements, vitamins, electrolytes, flavors, colorants, pectic acid and salts thereof, alginic acid and salts thereof, organic acids, protective colloidal thickeners, pH adjusting agents, stabilizers, preservatives, glycerin, alcohol, carbonic acid, in addition to the above-mentioned health functional food composition It may further contain a carbonizing agent used in beverages. The proportion of the components to be added is not particularly important, but it is generally selected from 0.01 to 0.1 parts by weight based on 100 parts by weight of the health functional food composition of the present invention.

Hereinafter, the present invention will be described in more detail by using manufacturing examples and examples. It is apparent to those skilled in the art that these manufacturing examples and examples are only intended to illustrate the present invention more specifically and that the scope of the present invention is not limited by them.

Manufacturing example One. Byeongpung Ssam Preparation of extract

(1) Preparation of ethanol extract from Byeongpungsam

100 g of 70% (v/v) ethanol prepared using distilled water adjusted to pH 4.5 is added to 2.5 g of Byeongpungsam pulverized by hot air drying at 40° C. and crushed at room temperature (18 to 25° C.) 2 It was extracted with stirring for an hour. Thereafter, the extract was centrifuged at 12,000 rpm for 15 minutes, and then the supernatant was filtered to prepare an ethanol extract of Byeongpungsam.

(2) Preparation of enzyme-treated Byeongpungsam extract

To 2.5 g of Byeongpungsam pulverized by hot air drying at 40° C., add 30 ml of distilled water adjusted to pH 4.5 and 50 units/ml of Viscozyme or 500 unit/ml of Pectinex, respectively. The mixture was stirred at 50°C for 10 hours and at 37°C for 2 hours at 180 rpm. Thereafter, 70 ml of 100% (v/v) ethanol was added to extract at 180 rpm for 2 hours at room temperature, centrifuged at 12,000 rpm for 15 minutes, and then filtered to prepare an enzyme-treated Byeongpungsam extract.

(3) Preparation of ultra-high pressure homogenization treatment of Byeongpungsam extract

After adding 100 ml of 70% (v/v) ethanol prepared using distilled water adjusted to pH 4.5 to 2.5 g of Byeongpungsam crushed by hot air drying at 40° C., stirring at 180 rpm for 3 hours at room temperature. And extracted. The extracted extract was centrifuged at 12,000 rpm for 15 minutes, filtered to prepare a filtrate, and then passed through an orifice tube twice at a pressure of 110 MPa to produce an ultra-high pressure homogenization-treated bottled wrap extract.

(4) Preparation of Byeongpungsam extract with enzyme treatment and ultra-high pressure homogenization treatment

To 2.5 g of Byeongpungsam pulverized by hot air drying at 40° C., add 30 ml of distilled water adjusted to pH 4.5 and 50 units/ml of Viscozyme or 500 unit/ml of Pectinex, respectively. The mixture was stirred at 50°C for 10 hours and at 37°C for 2 hours at 180 rpm. Thereafter, 70 ml of 100% (v/v) ethanol was added, extracted at 180 rpm for 2 hours at room temperature, centrifuged at 12,000 rpm for 15 minutes, and then filtered to prepare a filtrate, followed by twice at 110 MPa pressure. The ultra-high pressure homogenization was performed by passing through an orifice tube to prepare an enzyme-treated and ultra-high pressure homogenization-treated Byeongpungsam extract.

Example 1. According to the extraction method Byeongpung Ssam Melanin in extract ( melanin ) Biosynthesis inhibitory effect

B16-F10 mouse melanoma cells were inoculated to a 12-well plate to be 1×10 ⁵ cells/ml, incubated for 24 hours, and then treated with α-MSH (melanocyte-stimulating hormone) to induce melanin biosynthesis. Then, arbutin (100 μg/ml) or 100 μg/ml of Byeongpungsam extract extracted for each condition of Preparation Example 1 was treated for 48 hours. After 48 hours, the medium was removed, washed twice with phosphate buffer saline (PBS), and the attached cells were centrifuged to obtain pellets. To the precipitated melanoma cells, 200 μl of a solution made of 10% (v/v) DMSO was added to 1N NaOH, dissolved at 60° C. for 1 hour, and absorbance was measured at 405 nm.

As a result, as shown in Figure 1, when treated with a bottle pungssam extract of 100㎍ / ㎖ concentration that does not show cytotoxicity, increased by α-MSH in all of the bottle pungssam extract treatment group except the ultra-high pressure homogenization treatment bottle pungssam extract The reduced biosynthesis of melanin was reduced, and especially, the effect of reducing the biosynthesis of melanin was significantly higher in the biscozyme enzyme-treated Byeongpungsam extract and Pectinex enzyme-treated Byeongpungsam extract compared to Byeongpungsam ethanol extract. In the case, it was confirmed that the increase in melanin biosynthesis was significantly reduced compared to ethanol extract of Byeongpungsam when the ultra-high pressure homogenization process was added after enzyme treatment.

Claims (8)

1) Drying and pulverizing Byeongpung Ssam to prepare Byeongpung Ssam powder;
2) adding water and a hydrolase to the Byeongpungsam powder of step 1), followed by hydrolysis; And
3) Water, C in the hydrolyzate of step 2)_One~C₄The process of extracting by treating the lower alcohol or a mixture thereof;Cacalia firma) Cosmetic composition for skin whitening containing the extract as an active ingredient. The cosmetic composition for skin whitening according to claim 1, wherein the hydrolase of step 2) is pectinase or carbohydrase or a mixture thereof. The cosmetic composition for skin whitening according to claim 2, wherein the pectin hydrolase is Pectinex, and the carbohydrate hydrolase is biscozyme. According to claim 1, After the step 3), ultra-high pressure homogenizing step; skin whitening cosmetic composition further comprises a. The cosmetic composition for skin whitening according to claim 4, wherein the ultra-high pressure homogenization is performed under a pressure of 100 to 130 MPa. 1) Drying and pulverizing Byeongpungsam to prepare Byeongpungsam powder;
2) adding water and a hydrolase to the Byeongpungsam powder of step 1), followed by hydrolysis; And
3) a hydrolyzate of the above step 2) water, C ₁ ~ C ₄ lower alcohol or extracting process the mixtures thereof; the folding rolls (Cacalia manufacture, including firma ) A pharmaceutical composition for preventing or treating melanin hyperpigmentation disease containing an extract as an active ingredient. The method of claim 6, wherein the melanin hyperpigmentation disease is freckle, senile plaque, liver spots, blemishes, brown or black spots, daylight pigment spots, cyanic melasma, hyperpigmentation after drug use, scratches, burns or dermatitis. A pharmaceutical composition for the prevention or treatment of melanin hyperpigmentation disease, characterized in that it is hyperpigmentation or gestational chloasma after inflammation. 1) Drying and pulverizing Byeongpungsam to prepare Byeongpungsam powder;
2) adding water and a hydrolase to the Byeongpungsam powder of step 1), followed by hydrolysis; And
3) the step of extracting by treating the hydrolyzate of step 2) with water, a lower alcohol of C ₁ to C ₄ or a mixture thereof; and containing bottled ssam ( Cacalia firma ) extract prepared as an active ingredient Health functional food composition for preventing or improving hyperpigmentation disease.

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