KR101904920B1 - Composition for skin whitening containg voglibose - Google Patents

Abstract

The present invention relates to a skin whitening composition for inhibiting or inhibiting melanin production, and more particularly, to a skin whitening composition comprising a valiolamine derivative.

Description

TECHNICAL FIELD The present invention relates to a composition for skin whitening comprising voglibose,

The present invention relates to a skin whitening composition for inhibiting or inhibiting melanin production, and more particularly, to a skin whitening composition comprising a valiolamine derivative.

Melanin, which determines the color of a person's skin, is made in skin cells called melanocytes and then transferred to epidermal cells called keratinocytes. Here, melanin forms a hat-like structure around the nucleus, protecting genes from ultraviolet rays, and removing free radicals to protect intracellular proteins. These melanin-degrading enzymes are not present in the body, but are removed as they leave the skin when keratinocytes fall off the epidermis. However, when melanin is produced more than necessary, it induces hyperpigmentation such as spots, freckles, and dots, resulting in poor cosmetic results. In addition, as the number of people enjoying outdoor activities increased due to the increase in the leisure population, the demand for preventing melanin pigmentation caused by ultraviolet rays was further increased. This has led to the development of whitening agents that prevent excessive melanin production, and many efforts have been made in the meantime.

The development of whitening agents has consisted primarily of finding substances that reduce the amount of melanin by inhibiting the enzymatic activity of tyrosinase, an essential and essential enzyme in melanin biosynthesis. There are kojisan, arbutin, glutathione, vitamin A and vitamin C, but these products have no satisfactory whitening effect and there is limited use due to side effects. Therefore, it is urgent to develop a more effective whitening agent that is more effective than the whitening agent so far.

Meanwhile, tyrosinase, an enzyme that biosynthesizes melanin, is a sugar-bound glycoprotein that is produced through a glycosylation process, which is a glycoprotein synthesis process in vivo. There are many enzymes involved in this glycosylation process, the major enzymes being mannosidase and glucosidase. When glycosylation of tyrosinase is inhibited, the stability of tyrosinase is degraded and the degradation accelerates, and melanin production is inhibited due to loss of enzyme activity and migration into the intracellular organelle that produces melanin.

The inventors of the present invention have confirmed that the valiolamine derivative weakens the stability of thyrosinase and thereby accelerates the degradation, thereby inhibiting melanogenesis, thus completing the present invention.

Korean Patent Publication No. 10-2005-0097537

It is an object of the present invention to provide a novel whitening composition which inhibits the production of melanin fundamentally and has no side effects.

In order to achieve the above object, the present invention provides a skin whitening composition comprising, as an active ingredient, a valiolamine derivative of the formula (1) or a pharmaceutically acceptable salt thereof.

[Chemical Formula 1]

The composition for skin whitening, which is one aspect of the present invention, destabilizes tyrosinase, which is a source material that causes melanin production, and promotes decomposition. Accordingly, it is useful to provide a composition which effectively inhibits melanin production and exhibits excellent whitening effect and which has no adverse effects on the skin. Specifically, the composition for skin whitening, which is one aspect of the present invention, contains a valiolamine derivative, specifically, voglibose as an active ingredient, to inhibit the expression of melanin-producing enzyme tyrosinase, By inhibiting the formation, a whitening effect can be exhibited. In addition, the composition for skin whitening, which is one aspect of the present invention, can reduce the overall amount of tyrosinase protein.

1 shows the cytotoxicity test result of voglibose using human melanoma cells.
2 shows the effect of inhibiting melanin production of voglibose using human melanoma cells.
FIG. 3 shows the effect of voglibose on tyrosinase glycosylation and tyrosinase protein expression using human normal melanin-producing cells.

In one aspect, the present invention relates to a skin whitening composition comprising, as an active ingredient, a valiolamine derivative represented by the general formula (1) or a pharmaceutically acceptable salt thereof.

[Chemical Formula 1]

In the above formula (1), A may be substituted with the following compounds, but is not limited thereto. Specifically, A is hydroxyl, phenoxy, thienyl, furyl, pyridyl, cyclohexyl, alkyl alcohol, the alkyl alcohol or a di-C _{1 -10} acyclic which may be substituted with an optionally substituted phenyl hydrocarbon group; A C _{5 -6} cyclic hydrocarbon group which may be substituted with hydroxyl, hydroxymethyl, methyl or amino; Or sugar residue.

In Formula 1, A also includes a C _{1 -10} straight chain or branched aliphatic hydrocarbon group which may be saturated or unsaturated, and which may be substituted by hydroxy, phenoxy, thienyl, furyl, pyridyl, cyclohexyl, Phenyl. ≪ / RTI > Substituent of the optionally substituted phenyl is lower alkyl (e.g. C _{1 -6),} lower alkoxy (e.g. C _{1 -6),} lower dialkoxy (e.g. C _{1 -6),} a halogen (e.g. Fluorine, chlorine, bromine, iodine), phenyl, and the like.

In addition, A denotes a C _{5 -6} cyclic hydrocarbon group or a sugar moiety. These groups may be substituted with hydroxy, hydroxymethyl, methyl or amino. As used herein, the term " sugar residue " refers to the group upon removal of one hydrogen atom from a polysaccharide molecule, and thus may refer to a residue derived, for example, from a monosaccharide or oligosaccharide.

The derivative can be used in the form of a salt with an inorganic acid (e.g., hydrochloric acid) or an organic acid (e.g., citric acid).

As used herein, the term " pharmaceutically acceptable "refers to the approval of a government or equivalent regulatory agency that can be used on animals, and more specifically on humans, by avoiding significant toxic effects when used in conventional medicinal dosage Received, approved, or listed in pharmacopoeia or other general pharmacopoeia.

As used herein, "pharmaceutically acceptable salt" means a salt according to one aspect of the present invention which is pharmaceutically acceptable and has the desired pharmacological activity of the parent compound. The salt may be (1) formed with inorganic acids such as hydrochloric acid, hydrobromic acid, sulfuric acid, nitric acid, phosphoric acid and the like; (3-hydroxybenzoyl) benzoic acid, or an acetic acid, propionic acid, hexanoic acid, cyclopentenepropionic acid, glycolic acid, pyruvic acid, lactic acid, malonic acid, succinic acid, malic acid, maleic acid, fumaric acid, Benzoic acid, cinnamic acid, mandelic acid, methanesulfonic acid, ethanesulfonic acid, 1,2-ethane-disulfonic acid, 2-hydroxyethanesulfonic acid, benzenesulfonic acid, 4- chlorobenzenesulfonic acid, 2- 4-methylbicyclo [2,2,2] -oct-2-en-1-carboxylic acid, glucoheptonic acid, 3-phenylpropionic acid, trimethylacetic acid, tert Acid addition salts formed with organic acids such as butylacetic acid, laurylsulfuric acid, gluconic acid, glutamic acid, hydroxynaphthoic acid, salicylic acid, stearic acid, muconic acid; Or (2) salts formed when the acidic proton present in the parent compound is substituted.

As used herein, the term " active ingredient "alone refers to an ingredient that exhibits the desired activity or that can exhibit activity with a carrier that is not itself active.

In the present specification, "skin whitening" is understood as a result of inhibition of the production of melanin, specifically, prevention of symptoms caused by the production of melanin, such as spots, freckles, skin aging, .

In one aspect of the present invention, the valioamine derivative is selected from the group consisting of voglibose (1S, 2S, 3R, 4S, 5S) -5- (1,3- dihydroxypropan-2-ylamino) -1- hydroxymethyl) cyclohexane-1,2,3,4-tetraol, derivatives thereof or pharmaceutically acceptable salts thereof. The chemical structure of voglibose is shown in Figure 2 below.

(2)

As used herein, the term " derivatives of voglibose " refers to all compounds that are changed to other substituents at substitutable positions of voglibose, and there is no limitation on the kinds of such substituents. In one embodiment, the voglibose derivative may be represented by Formula (3), but is not limited thereto. Specifically, in the general formula (2), n or m may independently be an integer of 2 to 10.

(3)

In one aspect of the present invention, the composition may contain valiolamine derivatives or pharmaceutically acceptable salts thereof in an amount of 0.001 to 20% by weight based on the total weight of the composition.

When the amount of the valiolamine derivative or pharmaceutically acceptable salt thereof is less than 0.001% by weight, it is not sufficient to inhibit the expression of tyrosinase for whitening of the skin. When the amount of the valiolamine derivative is more than 20% by weight, It is not suitable for the content and formulation. In view of the above, the composition for skin whitening, which is one aspect of the present invention, comprises 0.001 to 19.8% by weight, 0.004 to 19.6% by weight, based on the total weight of the composition, of a valiolamine derivative or a pharmaceutically acceptable salt thereof, 0.006 to 19.4% by weight, 0.008 to 19.2% by weight, 0.01 to 19% by weight, 0.012 to 18.8% by weight, 0.014 to 18.6% by weight, 0.016 to 18.4% by weight, 0.018 to 18.2% by weight, 0.02 to 18% by weight, 17.8% by weight or 0.024 to 17.6% by weight.

In one aspect of the present invention, the active ingredient may inhibit the expression of tyrosinase.

In the present specification, the term " inhibiting the expression of tyrosinase "means an application capable of promoting degradation by making the structure of tyrosinase unstable. Specifically, by accelerating the decomposition of tyrosinase, it is possible to inhibit or inhibit the conversion of tyrosine to dopa (DOPA), to inhibit or inhibit the activity of dopaoxidase, (Dopa-quinone), thereby inhibiting or inhibiting the production of melanin.

In the composition according to one aspect of the present invention, the active ingredient may inhibit the generation of DOPA (3,4-dihydroxyphenylalanine).

The term " inhibiting the production of 3,4-dihydroxyphenylalanine (DOPA) "in the present specification means an application capable of inhibiting or inhibiting the production of DOPA. Specifically, by inhibiting DOPA, it can inhibit or inhibit the function of dopaoxidase and inhibit or inhibit the conversion of dopa into Dopa-quinone, thereby inhibiting the production of melanin Or inhibit.

In the composition according to one aspect of the present invention, the active ingredient may inhibit the production of dopaoxidase.

The term " inhibiting the production of dopaoxidase "in the present specification means inhibiting or inhibiting the production of DOPA and lowering the concentration of the dopaoxidase-acting substance. Thus, dopa-quinone Dopa-quinone), thereby inhibiting or inhibiting the production of melanin.

In an embodiment of the present invention, the active ingredient may inhibit the production of Dopa-quinone.

The term " inhibiting the production of Dopa-quinone "in the present specification means the use of inhibiting or inhibiting the production of Dopa-quinone, thereby inhibiting or inhibiting the production of melanin.

In the composition according to one aspect of the present invention, the active ingredient may inhibit the production of melanin.

As used herein, the term " inhibiting the production of melanin "means inhibiting or inhibiting the activity of proteins or enzymes involved in the up-stream of the body's mechanism of producing melanin, thereby inhibiting or inhibiting the production of melanin .

In one aspect of the invention, the composition comprises a cosmetic composition.

The formulation of the cosmetic composition is not particularly limited and may be appropriately selected according to the purpose. For example, it can be applied to softeners (skin lotion and milk lotion), nutrition lotion, essence, nutrition cream, massage cream, pack, gel, essence, eye cream, eye essence, cleansing cream, cleansing foam, cleansing water, A body lotion, a body cream, a body oil, and a body essence, but the present invention is not limited thereto. In addition, the cosmetic composition may be used in the form of an external preparation for skin in the form of ointment, patch, or the like.

The cosmetic composition according to the present invention may contain, in addition to the above-mentioned substances, other ingredients which can give a synergistic effect to the main effect, so long as they do not impair the main effect. The cosmetic composition according to the present invention may further comprise a moisturizing agent, an emollient agent, an ultraviolet absorber, an antiseptic, a bactericide, an antioxidant, a pH adjuster, an organic and inorganic pigment, a fragrance, a cold agent or a limiting agent. The compounding amount of the above components can be easily selected by those skilled in the art within a range not to impair the objects and effects of the present invention. The amount thereof may be 0.01 to 5% by weight, specifically 0.01 to 3% by weight, have.

In one aspect of the invention, the composition comprises a pharmaceutical composition.

The formulation of the pharmaceutical composition according to the present invention may be a solution, a suspension, a milk, a gel, a drip, a suppository, a patch or a spray, but is not limited thereto. The formulations can be readily prepared according to conventional methods in the art and can be prepared by conventional means such as excipients, wetting agents, emulsifying accelerators, suspending agents, salts or buffers for controlling osmotic pressure, coloring agents, spices, stabilizers, preservatives, Adjuvants may be used as appropriate.

The effective ingredients of the pharmaceutical composition of the present invention will vary depending on the age, sex, weight, pathological condition and severity of the subject to be treated, administration route or judgment of the prescriber. Determination of the amount of application based on these factors is within the level of ordinary skill in the art and its daily dose is, for example, 0.000025 mg / g / day to 0.025 mg / g / day, more specifically 0.00025 mg / g / day. < / RTI >

The pharmaceutical composition of the present invention may be administered orally or transdermally, but is not limited thereto.

In one aspect of the invention, the composition comprises a health food composition.

The health food composition of the present invention provides various forms of food additives or functional foods. The composition may be processed into an extruded tea, a liquid tea, a beverage, a fermented milk, a cheese, a yogurt, a juice, a probiotic agent, a health supplement, and the like, and various other food additives.

In one embodiment, the composition may contain other ingredients or the like that can give synergistic effects to the main effect within a range that does not impair the intended main effect of the present invention. For example, additives such as perfume, coloring agent, bactericide, antioxidant, preservative, moisturizing agent, thickening agent, inorganic salt, emulsifier and synthetic polymer substance may be further added for improvement of physical properties. In addition, it may further contain auxiliary components such as water-soluble vitamins, oil-soluble vitamins, polymer peptides, polymeric polysaccharides and seaweed extract. The above components may be mixed and selected without difficulty by those skilled in the art depending on the purpose of formulation or use, and the amount thereof may be selected within a range that does not impair the objects and effects of the present invention. For example, the addition amount of the above components may be in the range of 0.01 to 5% by weight, more specifically 0.01 to 3% by weight, based on the total weight of the composition.

The composition according to the present invention may be in various forms such as a solution, an emulsion, a viscous mixture, a tablet, a powder, etc., and may be administered by various methods such as simple drinking, injection administration, spraying or squeezing.

Hereinafter, the present invention will be described in more detail with reference to Examples. It is to be understood by those skilled in the art that these embodiments are only for illustrating the present invention and that the scope of the present invention is not construed as being limited by these embodiments.

Cytotoxicity experiments using human melanoma cells

Human melanoma cells MNT1 cells (Proc. Natl. Acad. Sci. USA 2001 98: 10698-10703., Proc Natl Acad Sci USA 2004, 101: 14865-70) (MEM) medium and cultured at 37 ° C under 5% CO ₂ . The cultured cells were treated with 0.5, 1, and 2 mM of voglibose, cultured for 0, 2, 4, and 6 days, respectively, and then subjected to cytotoxicity tests using a thiazolyl blue (MTT) assay.

As a result (FIG. 1), cell proliferation similar to that of the control group was observed when compared with the control group (NC) not treated with voglibose at a high concentration of 0.5, 1 or 2 mM for 6 days or longer . Therefore, it was confirmed that voglibose is a substance capable of exhibiting a whitening effect without side effects such as cytotoxicity.

Using human melanoma cells Boglibos  Melanin inhibition experiment

After MNT1 cells were cultured in the same manner as in Example 1, the cells were placed in a 60-well dish such that the number of cells was 1 × 10 ⁵ per dish. After waiting for the cells to attach to the wall of the dish overnight, I changed it to a badge. Voglibose was used at 1 mM. The new medium containing the samples was changed once every two days and cultured until the cells reached the dish.

After the cells were grown, the cells were treated with voglibose Photographs were taken for color comparison with the control group.

Also, the relative amount of melanin obtained by measuring the absorbance at 490 nm after completely growing the cells in 1N NaOH is shown in a graph.

As a result (Fig. 2), melanin production of human melanoma cells was decreased in a concentration-dependent manner by voglibose, thereby confirming the whitening effect of voglibose.

Using human normal melanin-producing cells Boglibose Tairosineiz Glyco Shale inhibition efficacy and whitening mechanism

(HMGs, human melanocyte growth supplement) containing 10 ng / ml of povol 12-myristate 13-acetate (PMA) in medium 254 (Medium 254, Cascade Biologics) , And human normal melanocytes (Cascade Biologics) were cultured in a 5% CO ₂ incubator at 37 ^° C using the medium as a medium.

Cells were collected and lysed in a lysis buffer (2% CHAPS in 50 mM Hepes and 200 mM NaCl, pH 7.5). The cells were treated with 1 mM each of voglibose or DNJ (deoxynojirimycin) , protease inhibitors) were added and ultrasonicated. The cell lysate was centrifuged at 12,000 rpm at 4 ° C for 30 minutes to remove unbroken cells and melanin, and only the supernatant was removed. The cells in which the cells cultured in Fig. 3 were intact were labeled with D, DNJ (deoxynojirimycin) -treated group and V with voglibose-treated group.

Endoglycosidase H (125 units) or PNase was treated with the supernatant (protein amount: 10 mg), and the reaction was carried out overnight at 37 ° C. After electrophoresis, the proteins in the supernatant were separated by size Respectively. The protein isolated by electrophoresis was confirmed by Western blotting using thiocyanate as an antibody.

Thyrosinase, which normally has a sugar residue, is a glycoprotein having a size of about 62 kD due to the enzyme digestion of the endo-glycoside H by the endo-glycosidase H. On the other hand, tyrosinase, which does not form a normal sugar residue by voglibose The endogenous hydrolysis of the residues by the endoglucosidase H causes the protein to appear at a size of about 50 kD. PNase hydrolyzes both normal sugar residues and abnormal sugar residues to show a sugar-free protein.

3, in the endoH, tyrosinase of the control group (N) not treated with voglibose had a large size (about 62 kD) due to the fact that the endo-glycosidase H did not decompose the sugars, The tyrosinase of the melanin-producing cell treated with 1 mM of voglibose showed that the sugar moiety was degraded by endoglycosidase H and appeared to be small (about 50 kD).

In addition, Ctrl showed that boglibose reduced the overall protein content of thyroxinase.

From the above results, it can be confirmed that the voglibose has a whitening effect that reduces the expression amount of tyrosinase and thereby inhibits melanin production.

Hereinafter, a formulation example of the composition according to the present invention will be described. However, the pharmaceutical composition, the cosmetic composition or the health food composition can be applied to various formulations, and the present invention is not limited thereto but is specifically described.

[Formulation Example 1] Softening lotion (skin lotion)

Compounding ingredient Content (% by weight) Boglibos 0.0025 glycerin 3.0 Butylene glycol 2.0 Propylene glycol 2.0 Carboxyvinyl polymer 0.1 Phage-12 nonylphenyl ether 0.2 Polysorbate 80 0.4 ethanol 10.0 Triethanolamine 0.1 Preservative, coloring, fragrance Suitable amount Purified water Balance

[Formulation Example 2] Nutritional lotion (Milk lotion)

Compounding ingredient Content (% by weight) Boglibos 0.0025 glycerin 3.0 Butylene glycol 3.0 Propylene glycol 3.0 Carboxyvinyl polymer 0.1 Wax 4.0 Polysorbate 60 1.5 Caprylic / capric triglyceride 5.0 Squalane 5.0 Sorbitacecequioleate 1.5 Liquid paraffin 0.5 Cetearyl alcohol 1.0 Triethanolamine 0.2 Preservative, coloring, fragrance Suitable amount Purified water Balance

[Formulation Example 3] Nourishing cream

Compounding ingredient Content (% by weight) Boglibos 0.0025 glycerin 3.0 Butylene glycol 3.0 Liquid paraffin 7.0 Beta Glucan 7.0 Carbomer 0.1 Caprylic / capric triglyceride 3.0 Squalane 5.0 Cetearyl glucoside 1.5 Sorbitan stearate 0.4 Polysorbate 60 1.2 Triethanolamine 0.1 Preservative, coloring, fragrance Suitable amount Purified water Balance

[Formulation Example 4] Massage cream

Compounding ingredient Content (% by weight) Boglibos 0.0025 glycerin 8.0 Butylene glycol 4.0 Liquid paraffin 45.0 Beta Glucan 7.0 Carbomer 0.1 Caprylic / capric triglyceride 3.0 Wax 4.0 Cetearyl glucoside 1.5 Sesquioleic acid sorbitan 0.9 Vaseline 3.0 paraffin 1.5 Preservative, coloring, fragrance Suitable amount Purified water Balance

[Formulation Example 5] Pack

Compounding ingredient Content (% by weight) Boglibos 0.0025 glycerin 4.0 Polyvinyl alcohol 15.0 Hyaluronic acid extract 5.0 Beta Glucan 7.0 Allantoin 0.1 Nonyl phenyl ether 0.4 Polysorbate 60 1.2 Ethanol preservative 6.0 Good Preservative, coloring, fragrance Suitable amount Purified water Balance

[Formulation Example 6] ointment

Compounding ingredient Content (% by weight) Boglibos 0.0025 glycerin 8.0 Butylene glycol 4.0 Liquid paraffin 15.0 Beta Glucan 7.0 Carbomer 0.1 Caprylic / capric triglyceride 3.0 Squalane 1.0 Cetearyl glucoside 1.5 Sorbitan stearate 0.4 Cetearyl alcohol 1.0 Wax 4.0 Preservative, coloring, fragrance Suitable amount Purified water Balance

[Formulation Example 1] Soft capsule

A soft capsule was prepared by mixing 0.0025 g of voglibose, 50 mg of red ginseng extract, 2 mg of palm oil, 8 mg of palm kernel oil, 4 mg of yellow radish, and 6 mg of lecithin and filling them with 400 mg per capsule according to a conventional method.

[Formulation Example 2] Tablets

The granules were formed by mixing 0.0025 g of voglibose, 100 mg of glucose, 50 mg of red ginseng, 96 mg of starch and 4 mg of magnesium stearate and 40 mg of 30% ethanol, followed by drying at 60 ° C., Respectively.

[Formulation Example 3] Granules

150 mg of active ingredient, 100 mg of glucose, 50 mg of red ginseng extract and 600 mg of starch were mixed with 100 mg of 30% ethanol and 100 mg of the active ingredient containing at least one selected from the group consisting of voglibose, its derivatives and pharmaceutically acceptable salts thereof To form granules, followed by drying at 60 DEG C to form granules, which were then filled in a capsule. The final weight of the contents was 1 g.

[Formulation Example 4] Drinking agent

0.0025 g of voglibose, 10 g of glucose, 50 mg of red ginseng extract, 2 g of citric acid and 187.8 g of purified water were mixed and filled in a bottle. The final volume of the contents was adjusted to 200 ml.

[Formulation Example 5] Preparation of health food

Voglibose ..................................... 0.0025g

Vitamin mixture

Vitamin A Acetate ....................... 70 ㎍

Vitamin E ............................................ 1.0 mg

Vitamin B1 ........................................... 0.13 mg

Vitamin B2 .......................................... 0.15 mg

Vitamin B6 ........................................... 0.5 mg

Vitamin B12 .............................. 0.2 g

Vitamin C ............................................. 10 mg

Biotin ................................................. 10 [mu] g

Nicotinic acid amide .................................. 1.7 mg

Folic acid ................................................. ..... 50 μg

Calcium pantothenate .................................... 0.5 mg

Mineral mixture

Ferrous sulfate .......................................... 1.75 mg

Zinc oxide ............................................ 0.82 mg

Magnesium carbonate ...................................... 25.3 mg

Potassium Phosphate ......................................... 15 mg

Secondary calcium phosphate ...................................... 55 mg

Potassium citrate ............................................ 90 mg

Calcium carbonate .............................................. 100 mg

Magnesium chloride ..................................... 24.8 mg

Although the composition ratio of the above-mentioned vitamin and mineral mixture is comparatively mixed with a composition suitable for health food as a preferred embodiment, the compounding ratio may be arbitrarily modified, and the above ingredients are mixed according to a conventional method for producing healthy foods , Granules can be prepared and used in the manufacture of health food compositions according to conventional methods.

[Formulation Example 6] Preparation of health drink

Boglibose .......................... 0.0025g

Citric acid ................................................. ... 1000 mg

oligosaccharide................................................. .... 100 g

Plum concentrate ................................................ ..... 2 g

Taurine ................................................. ........... 1 g

Purified water was added to the mixture to complete 900 ml

The above components were mixed according to a conventional health drink manufacturing method, and the mixture was heated for about 1 hour at 85 DEG C with stirring, and the solution thus prepared was filtered to obtain a sterilized 2-liter container, which was sealed and sterilized, ≪ / RTI >

Although the composition ratio is relatively mixed with a component suitable for a favorite drink, it is also possible to arbitrarily modify the blending ratio according to the regional or national preference such as the demand level, the demanding country, the use purpose, and the like. It will be understood by those skilled in the art that various changes in form and details may be made therein without departing from the spirit and scope of the invention as defined by the appended claims.

While the present invention has been particularly shown and described with reference to specific embodiments thereof, those skilled in the art will readily appreciate that many modifications are possible in the exemplary embodiments without materially departing from the novel teachings and advantages of this invention. something to do. Accordingly, the actual scope of the present invention will be defined by the appended claims and their equivalents.

Claims (11)

A composition for skin whitening comprising, as an active ingredient, a valiolamine derivative of the formula (1) or a pharmaceutically acceptable salt thereof.
[Chemical Formula 1]

The method according to claim 1, wherein the valiolamine derivative is selected from the group consisting of voglibose (1S, 2S, 3R, 4S, 5S) -5- (1,3- dihydroxypropan- 2- ylamino) -1- (hydroxymethyl) cyclohexane- 1,2,3,4-tetraol), derivatives thereof, or pharmaceutically acceptable salts thereof. The composition for skin whitening according to claim 1, wherein the composition contains valiolamine derivatives or pharmaceutically acceptable salts thereof in an amount of 0.001 to 20% by weight based on the total weight of the composition. The skin whitening composition according to claim 1, wherein the active ingredient inhibits the expression of tyrosinase. The skin whitening composition according to claim 1, wherein the active ingredient inhibits the production of 3,4-dihydroxyphenylalanine (DOPA). The skin whitening composition according to claim 1, wherein the active ingredient inhibits the production of dopaoxidase. The skin whitening composition according to claim 1, wherein the active ingredient inhibits the production of Dopa-quinone. The skin whitening composition according to claim 1, wherein the active ingredient inhibits the production of melanin. 9. The composition according to any one of claims 1 to 8, wherein the composition is a cosmetic composition. 9. The composition according to any one of claims 1 to 8, wherein the composition is a pharmaceutical composition. 9. The composition according to any one of claims 1 to 8, wherein the composition is a health food composition.

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