COMPOSITION COMPRISING ALLULOSE AS ACTIVE INGREDIENT FOR SKIN WHITENING

Abstract

The present invention relates to a cosmetic composition for skin whitening.

Claims

1. A composition for skin whitening comprising allulose as an active ingredient.

2. The composition for skin whitening of claim 1, wherein the allulose is contained in an amount of 0.2-60 wt % with respect to 100 wt % of the composition.

3. The composition for skin whitening of claim 1, wherein the skin whitening is performed by inhibiting pigmentation caused by melanogenesis or inhibiting tyrosinase activity.

4. The composition for skin whitening of claim 1, wherein the composition is a cosmetic, food, or pharmaceutical composition.

5. A composition for preventing, inhibiting or treating a pigmentation disease comprising allulose as an active ingredient.

6. A composition for inhibiting tyrosinase activity comprising allulose.

7. A method for whitening skin, the method comprising administering to a subject an effective amount of allulose.

8. A method for preventing or treating a pigmentation disease, the method comprising administering to a subject an effective amount of allulose.

9-10. (canceled)

Description

BRIEF DESCRIPTION OF THE DRAWINGS

[0081] FIG. 1 is a graph showing the result of quantifying the amount of melanin released from murine melanocytes.

[0082] FIG. 2 is a graph showing the inhibitory effect of allulose on tyrosinase activity.

MODE FOR CARRYING OUT THE INVENTION

[0083] Hereinafter, the present invention will be described in detail with reference to Preparation Examples and Experimental Examples.

[0084] However, Preparation Examples and Experimental Examples below may be exemplified merely as illustrative purpose, and thus the contents of the present application are not limited thereto.

Experimental Example 1. Confirmation of Inhibitory Effect of Allulose on Melanogenesis

[0085] Murine melanocytes were seeded on each 6-well plate at 1×10.sup.4 cells/well. In a sample treatment group 24 hours after the seeding, cells were treated with allulose (CJ CheilJedang, 98% or higher purity) at a concentration of 0.01 wt %, 0.1 wt %, and 1 wt %. In a positive control group, cells were treated with arbutin at 0.02 wt %. A comparative group was treated with 1 wt % of glucose (Sigma Aldrich) or 1 wt % of fructose (Sigma Aldrich). An untreated group (control) was not treated with a sample, or a-MSH inducing melanin production. The sample treatment group, the positive control group, the comparative group, and the negative control group were treated with 50 μM of a-MSH. After 72 hours of treatment, cells were recovered and lysed with NaOH to detect intracellular melanin. The absorbances (OD.sub.405) of the untreated group, the negative control group (treated with only a-MSH), the sample treatment group (treated with a-MSH and each sample by concentration), and the positive control group (treated with a-MSH and arbutin) were measured.

[0086] As a result, as shown in FIG. 1, it was confirmed that melanogenesis was suppressed in the allulose-treated group, resulting in a whitening effect. In particular, it was confirmed that melanogenesis was significantly inhibited when allulose was 1 wt %.

[0087] On the other hand, in the case of glucose and fructose which are the same saccharides as allulose and are known to have antioxidant activity, it was confirmed that melanogenesis was not inhibited at all even when the comparative group was treated at a concentration of 1 wt % of each of glucose and fructose. In addition, from the above results, it can be seen that not all substances exhibiting antioxidant activity exhibit melanogenesis inhibitory effect or whitening effect, and from this, the whitening effect through the melanogenesis inhibitory effect of allulose is not naturally derived from antioxidant activity.

Experimental Example 2. Confirmation of Inhibitory Effect of Allulose on Tyrosinase

[0088] The following experiment was performed to confirm the tyrosinase inhibitory effect, which is one of the mechanisms of the whitening effect.

Experimental Example 2-1. Measurement of Polyphenol Oxidase (Tyrosinase from Mushroom) Activity

[0089] An enzyme solution was prepared by dissolving 0.2 mg/ml of tyrosinase from mushroom (25KU, 2687 units/mg solid) in 50 mM sodium phosphate buffer (pH 6.5). Allulose (Example), sucrose (Comparative Example 1), and fructose (Comparative Example 2) were each prepared at 50 mM. As a substrate, 30 mM catechol, an enzyme solution, and 100 mM sodium phosphate buffer (pH 6.5) were mixed so that the mixing ratio of catechol:enzyme solution:sodium phosphate buffer was 5:1:4. The allulose, sucrose, and fructose were each added to the mixture at 50 mM. As a co-sample solution, DW was added instead of the enzyme solution. After mixing, absorbance was measured at 420 nm.

[0090] As a result, tyrosinase activity was inhibited in Example as shown in FIG. 2. On the other hand, it was confirmed that the tyrosinase activity was not inhibited at all in the case of Comparative Examples 1 and 2 known as saccharides having antioxidant activity.

Experimental Example 2-2. Quantitative Analysis of Substrate (Catechol) of Enzyme Reactant

[0091] A catechol standard preparation was diluted according to concentration, and then was subjected to LC analysis to obtain a standard curve of the catechol. 200 μl of each enzyme reaction solution obtained in Experimental Example 2-1 above was added into a PCR tube, and was reacted at 37° C. for 0 minutes (an enzyme reaction product in which the enzyme was inactivated by heating each enzyme reaction solution for 10 minutes), 10 minutes, 20 minutes, 30 minutes, and 60 minutes to prepare an enzyme reactant for each reaction time. The reaction was stopped using a heat block. The reaction was stopped according to the planned time and heated in a heat block at 105° C. for 10 minutes, and then put in ice and cooled for 10 minutes. The PCR tube was centrifuged twice using a centrifuge. LC analysis was carried out by a typical analytical method. The enzyme reactant was filtered with a 1-ml syringe. The filtered enzyme reactant was injected into an insert, and was subjected to LC analysis. The amount of catechol in the enzyme reactant was measured according to the standard curve, which is obtained in advance, for quantifying catechol. LC analysis conditions are shown in Table 1 below, and the analysis results are shown in Table 2.

TABLE-US-00001 TABLE 1 Column Platinum EPS C18 100 Å 3micro u Solvent 70% Acetonitrile Flow rate 1.0 mL/min Injection volume 25 μl Pump temp. 35° C. Analysis time 15 min Detector DAD 254 nm, 280 nm

TABLE-US-00002 TABLE 2 Reaction time Comparative Comparative (min) D.W. Example 1 Example Example 2  0 3292.0 3296.7 3288.7 3236.0 30 3103.0 3112.0 3126.7 3069.0 60 3022.0 3031.0 3087.0 2971.0 Reduction rate 8.2% 8.1% 6.1% 8.2% of catechol compared to initial stage of reaction

[0092] (Unit: ppm) As a result, the tyrosinase activity was inhibited in Example as shown in Table 2. On the other hand, it was confirmed that the tyrosinase activity was not inhibited at all in the case of Comparative Examples 1 and 2 known as saccharides having antioxidant activity.

Preparation Example 1. Preparation of Cosmetic Formulation

[0093] 1-1. Preparation of Essence

[0094] An essence was prepared using allulose according to the content (parts by weight) shown in Table 3 below.

TABLE-US-00003 TABLE 3 Composition Content (parts by weight) Triethanolamine 0.25 Carboxyvinyl polymer 0.22 Glycerin 4 Butylene glycol 2 Allulose 1.5 Cera 0.5 Cetostearyl alcohol 1 Glyceryl monostearate 1 Squalene 4 Purified water Suitable amount

[0095] 1-2. Preparation of Skin Softener

[0096] A skin softener containing allulose as an active ingredient was prepared as described in Table 4 below.

TABLE-US-00004 TABLE 4 Raw material Content (parts by weight) 1,3-butylene glycol 1.00 Disodium EDTA 0.05 Allantoin 0.10 Dipotassium glycyrrhizate 0.05 Citric acid 0.01 Sodium citrate 0.02 Glycereth-26 1.00 Arbutin 2.00 PEG-40 1.00 Hydrogenated castor oil Ethanol 30.00 Allulose 1.5 Colorant Trace Fragrance Trace Purified water Remainder

[0097] 1-3. Preparation of Nutrition Cream

[0098] A nutrition cream containing allulose as an active ingredient was prepared as the composition of Table 5 below.

TABLE-US-00005 TABLE 5 Raw material Content (parts by weight) 1,3-butylene glycol 7.0 Glycerin 1.0 D-panthenol 0.1 Magnesium aluminum silicate 0.3 PEG-40 stearate 1.2 Stearic acid 2.0 Polysorbate 60 1.5 Lipophilic glyceryl stearate 2.0 Sorbitan sesquioleate 1.5 Cetearyl alcohol 3.0 Mineral oil 4.0 Squalene 3.8 Allulose 1.5 Vegetable oil 1.8 Dimethicone 0.4 Dipotassium glycyrrhizate Trace Allantoin Trace Sodium hyaluronate Trace Tocopheryl acetate Suitable amount Triethanolamine Suitable amount Fragrance Suitable amount Purified water Remainder

[0099] 1-4. Preparation of Lotion

[0100] A lotion containing allulose as an active ingredient was prepared as the composition of Table 6 below.

TABLE-US-00006 TABLE 6 Raw material Content (parts by weight) Cetostearyl alcohol 1.6 Stearic acid 1.4 Lipophilic glyceryl monostearate 1.8 PEG-100 stearate 2.6 Sorbitan sesquioleate 0.6 Squalene 4.8 Macadamia nut oil 2 Jojoba oil 2 Tocopherol acetate 0.4 Methylpolysiloxane 0.2 Tocopherol acetate 0.4 1,3-butylene glycol 4 Xanthan gum 0.1 Glycerin 4 D-panthenol 0.15 Allulose 1.0 Allantoin 0.1 Carbomer (2% aq. Sol) 4 Triethanolamine 0.15 Ethanol 3 Purified water Suitable amount

Preparation Example 2. Preparation of Food

[0101] 2-1. Preparation of Wheat Flour Foods

[0102] 0.5-5.0 parts by weight of allulose of the present invention was added to wheat flour, and this mixture was used to prepare bread, cake, cookies, crackers, and noodles.

[0103] 2-2. Preparation of Soups and Gravies

[0104] 0.2-5.0 parts by weight of allulose of the present invention was added to soups and gravies to prepare soups and gravies for meat products and noodles for enhancing health.

[0105] 2-3. Preparation of Ground Beef

[0106] 10 parts by weight of allulose of the present invention was added to ground beef to prepare ground beef for enhancing health.

[0107] 2-4. Preparation of Dairy Products

[0108] 5 to 10 parts by weight of allulose of the present invention was added to milk, and the milk was used to prepare various dairy products such as butter and ice cream.

[0109] 2-5. Preparation of Cereal Flour Foods

[0110] Brown rice, barley, glutinous rice, and adlay were gelatinized and dried by a known method, and the resulting product was roasted and then prepared into a powder having a particle size of 60 mesh with a pulverizer.

[0111] Black beans, black sesame seeds, and perilla seeds were also steamed and dried by a known method, and the resulting product was roasted and then prepared into a powder having a particle size of 60 mesh with a pulverizer.

[0112] The dried product obtained by concentrating the allulose of the present invention under reduced pressure in a vacuum concentrator, and drying the concentrated allulose with a spray hot air dryer was pulverized into a particle size of 60 mesh with a pulverizer to obtain a dry powder.

[0113] The above-prepared cereals, seeds and allulose of the present invention were blended in the following ratio to prepare cereal flour foods:

[0114] Cereals (30 parts by weight of brown rice, 15 parts by weight of adlay, and 20 parts by weight of barley), seeds (7 parts by weight of perilla seeds, 8 parts by weight of black beans, and 7 parts by weight of black sesame), allulose of the present invention (3 parts by weight), Ganoderma lucidum (0.5 parts by weight), and Rehmannia glutinosa (0.5 parts by weight)

[0115] 2-6. Preparation of Health Drinks

[0116] Minor ingredients such as high-fructose corn syrup (0.5%), oligosaccharide (2%), sugar (2%), salt (0.5%), and water (75%), and 5 g of allulose of the present invention were uniformly blended and flash pasteurized, and then the mixture was packaged in a small container such as a glass bottle or a plastic bottle to prepare health drinks.

[0117] 2-7. Preparation of Vegetable Juices

[0118] 5 g of allulose of the present invention was added to 1,000 mL of a tomato or carrot juice to prepare vegetable juices.

[0119] 2-8. Preparation of Fruit Juices

[0120] 5 g of allulose of the present invention was added to 1,000 mL of an apple or grape juice to prepare fruit juices.

Preparation Example 3. Preparation of Pharmaceutical Composition

[0121] 3-1. Preparation of Powder

[0122] 2 g of allulose of the present invention

[0123] 1 g of lactose

[0124] The ingredients above were mixed and filled into an airtight packet to prepare a powder.

[0125] 3-2. Preparation of Tablets

[0126] 100 mg of allulose of the present invention

[0127] 100 mg of corn starch

[0128] 100 mg of lactose

[0129] 2 mg of magnesium stearate

[0130] The ingredients above were mixed, and then tableted according to a typical tablet preparation method to prepare a tablet.

[0131] 3-3. Preparation of Capsules

[0132] 100 mg of allulose of the present invention

[0133] 100 mg of corn starch

[0134] 100 mg of lactose

[0135] 2 mg of magnesium stearate

[0136] The ingredients above were mixed, and then filled into a gelatin capsule according to a typical capsule preparation method to prepare a capsule.

[0137] 3-4. Preparation of Pills

[0138] 1 g of allulose of the present invention

[0139] 1.5 g of lactose

[0140] 1 g of glycerin

[0141] 0.5 g of xylitol

[0142] After the ingredients above were mixed, pills were prepared to be 4 g per one pill according to a typical method.

[0143] 3-5. Preparation of Granules

[0144] 150 mg of allulose of the present invention

[0145] 50 mg of soybean extract

[0146] 200 mg of glucose

[0147] 600 mg of starch

[0148] After the ingredients above were mixed, 100 mg of 30% ethanol was added thereto and dried at 60° C. to form granules, and then the granules were filled into packets.