JP2002212048A - Skin bleaching cosmetic containing natural black component extracted from muscovado - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a skin bleaching cosmetic containing a natural black component extracted from muscovado, having antiinflammatory action and effective for preventing various troubles on the skin or ameliorating the symptom of the skin trouble. SOLUTION: The skin bleaching cosmetic containing a natural black component extracted from muscovado contains 3,4,6-trimethoxyphenyl-4'-O-D-glucose and 2,5-dimethoxyphenyl-4'-O-D-glucose.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a cosmetic for beautiful skin containing a natural black component extracted from brown sugar, which has an anti-inflammatory effect and prevents various troubles occurring on the skin. Another object of the present invention is to provide a cosmetic for beautiful skin containing a natural black component extracted from brown sugar, which can ameliorate the onset symptoms.

[0002]

2. Description of the Related Art Acne, a kind of seborrheic skin disease,
About 80% of male and female adolescents are affected to varying degrees. It is said that acne is caused by active sebum secretion due to increased secretion of testosterone, a type of male hormone. In other words, when sebum secretion increases due to the action of testosterone, there is no problem if sebum can flow out of the skin, but if the pores are narrowed for some reason, sebum cannot flow out. Agglomeration of sebum (comedone) occurs in the skin. Inflammation occurs due to the action of acne bacilli present in the sebum, and suppuration occurs due to the action of Staphylococcus aureus, which worsens the symptoms.

[0003] Prevention of acne requires careful face washing in order to remove sebum and dirt which may be the cause. External preparations for acne are also commercially available. These external preparations include keratolysis and keratolysis for removing keratin with narrow pores.
A peeling agent, a bactericide for acne bacilli, Staphylococcus aureus, and the like are compounded. Kummenfeld's solution and the like are used as the exfoliating agent. As the keratolytic agent, sulfur, thioxolone, resorcin, salicylic acid, and the like are used. As a bactericide, hexachlorophen, chlorhexidine, trichlorocarbanilide, trichlorohydroxydiphenyl ether and the like are used.

[0004] In recent years, the number of patients who develop atopic dermatitis has increased rapidly. Atopic dermatitis is a type of allergic reaction and is accompanied by marked itching. Although various factors can be considered as the cause, it is said that one of the causes is a food additive compounded in a food to be taken on a daily basis, or a large amount of a chemical substance that is ingested casually. In the treatment of atopic dermatitis, oral administration of an antihistamine or application of a corticosteroid ointment to the skin, etc. are performed, but all of them have side effects and may not show a sufficient effect.

[0005]

It is known that the natural black component of brown sugar is effective in resolving various skin problems as described above or in alleviating the symptoms thereof. This includes 3,4-dimethoxyphenyl-4′-OD-glucose, 2,5-dimethoxyphenyl-4′-OD-glucose, 3,4 contained in the natural black component of brown sugar.
This is due to the action of a phenylglucose compound such as 6-trimethoxyphenyl-4′-OD-glucose. When each of these phenylglucose compounds is used alone, it is effective for rough skin such as spots, acne and rash, and in particular, 2,5-dimethoxyphenyl-4'-O-
D-glucose can exert an excellent effect.
On the other hand, 3,4,6-trimethoxyphenyl-4′-O—
D-glucose is less effective than the other two phenylglucose compounds. (JP-A-7-33057
No. 4)

The present inventors have conducted intensive studies on the natural black component extracted from brown sugar, and found that among the natural black components extracted from brown sugar, 3,4,6-trimethoxyphenyl-4'-O When -D-glucose and 2,5-dimethoxyphenyl-4'-OD-glucose were mixed together,
When 6-trimethoxyphenyl-4′-OD-glucose and 3,4-dimethoxyphenyl-4′-OD-glucose are mixed together, 3,4-dimethoxyphenyl-4′-OD-glucose When glucose and 2,5-dimethoxyphenyl-4′-OD-glucose are mixed together,
And 3,4,6-trimethoxyphenyl-4'-O-
D-glucose and 3,4-dimethoxyphenyl-4'-
O-D-glucose and 2,5-dimethoxyphenyl-
Compared with the case where 4′-OD-glucose is added together, the present inventors have found that the effect of preventing the onset of atopic dermatitis and the like is greatly increased and that inflammation that occurs on the skin and the like can be suppressed. The invention has been completed.

[0007]

According to the first aspect of the present invention,
3,4,6-trimethoxyphenyl-4'-OD-glucose and 2,5-dimethoxyphenyl-4'-O-
The present invention relates to a cosmetic for beautiful skin containing a natural black component extracted from brown sugar, characterized by containing D-glucose.

[0008]

BEST MODE FOR CARRYING OUT THE INVENTION The cosmetics for beautiful skin containing a natural black component extracted from brown sugar according to the present invention will be described below in detail. The cosmetic for beautiful skin containing a natural black component extracted from brown sugar according to the present invention is represented by the following formula 3 as an active ingredient:
3,4,6-trimethoxyphenyl-4′-OD-glucose represented by the following formula (3) and 2,5-dimethoxyphenyl-4′-OD-glucose represented by the following formula (4): Glucose is blended. The reason why 3,4,6-trimethoxyphenyl-4′-OD-glucose and 2,5-dimethoxyphenyl-4′-OD-glucose are blended as essential components is that when each is blended alone. This is because, as compared with the above, the effect of preventing the onset of atopic dermatitis and the like is excellent, and the inflammation occurring in the skin and the like can be suppressed.

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The active ingredients 3,4,6-trimethoxyphenyl-4'-OD-glucose and 2,5-dimethoxyphenyl-4'-OD-glucose are all natural black sugars. It is a kind of component and can be obtained by extracting and purifying from brown sugar. The method for obtaining these natural black components from brown sugar is not particularly limited, but the following methods can be exemplified. First,
Extract only natural black components from brown sugar. That is, after dissolving brown sugar in an appropriate amount of water and bringing it into contact with an adsorbent to adsorb the natural black component, the adsorbent is washed with water to sufficiently remove the sugar, and finally the adsorbed natural black component Is eluted with the solvent. Usually, this operation is performed using a column packed with an adsorbent. As the adsorbent to be used, a non-polar polystyrene-based adsorption resin, for example, Amberlite X
AD-1, Amberlite XAD-2 (trade name, manufactured by Rohm and Haas) and Selvachrome XAD-2
(Trade name, manufactured by Selva) and the like, and it is preferable to use Selvachrome XAD-2 from the viewpoint of yield. Although the amount of the adsorbent used is not particularly limited, it is 30 to 300 times by weight, more preferably 50 to 300 times the amount of the natural black component contained.
It is assumed to be 200 weight times.

Before eluting the adsorbed natural black component, it is preferable to sufficiently flow down water so as to sufficiently remove sugars until the washing liquid has no sweetness. The solvent used for eluting the natural black component is not particularly limited,
A lower alcohol having a concentration of 20% or more is preferably used,
Examples include methanol, ethanol, and isopropanol. Particularly in the present invention, first, 20 to 3
Elution is performed with 0% lower alcohol, and after little coloration of the flowing solution is recognized, it is preferable to further elute with 95-99% high-concentration lower alcohol. The reason for this is that elution with only low-concentration lower alcohols is not preferable because the yield of natural black components decreases. If the removal of sugar is incomplete and sweetness remains in the eluate, the evaporation residue is mixed with pure lower alcohol such as pure ethanol, and the insoluble sugar is removed by filtration. Preferably, the black component is obtained by recrystallization. This is because a highly pure natural black component can be obtained.

As a method for obtaining a natural black component of brown sugar, in addition to the above-mentioned method, brown sugar is directly cold-immersed or digested in a pure lower alcohol such as methanol or pure ethanol.
After removing insoluble sugars by a method such as filtration, a method of evaporating the remaining liquid to dryness to obtain a natural black component can be exemplified.

[0012] Such a natural black component of brown sugar can be obtained from raw brown sugar in a yield of about 0.05 to 0.3% by weight. The natural black component of brown sugar is a light brown, hygroscopic powder with a slightly burning odor and a slightly bitter taste.

Next, the obtained natural black component is isolated and purified by silica gel column chromatography to obtain 3,4,6-trimethoxyphenyl-4'-OD.
-Glucose and 2,5-dimethoxyphenyl-4'-
O-D-glucose can be obtained.

The total amount of the active ingredients 3,4,6-trimethoxyphenyl-4'-OD-glucose and 2,5-dimethoxyphenyl-4'-OD-glucose is not particularly limited. But 0.001 in the cosmetic composition
% By weight or more, preferably 0.005 to 50% by weight. Further, 3,4,6-trimethoxyphenyl-4′-
O-D-glucose and 2,5-dimethoxyphenyl-
The mixing ratio of 4'-OD-glucose is not particularly limited, but 1 part by weight of 3,4,6-trimethoxyphenyl-
2,5-dimethoxyphenyl-4′-OD-glucose is added to 4′-OD-glucose in an amount of 0.01 to 10%.
0 parts by weight, preferably 0.1 to 10 parts by weight.

The active ingredients of the present invention, 3,4,6-trimethoxyphenyl-4'-OD-glucose and 2,2
When 5-dimethoxyphenyl-4′-OD-glucose was added together, as is clear from the results of the test examples described later, acne and atopic dermatitis were compared with the case of using each alone. It is possible to prevent or troubleshoot various troubles occurring on the skin such as beforehand. In addition, by selectively inhibiting the activity of cyclooxygenase among the enzymes contained in platelets, it suppresses the production of arachidonic acid metabolites TXB ₂ and HHT, which are considered to be closely related to inflammation. Can be reduced. Moreover, it does not inhibit the activity of lipoxygenase, an enzyme contained in platelets that can metabolize arachidonic acid to 12-HETE.

In the present invention, a Maillard reaction product can be blended. The Maillard reaction is a browning phenomenon that occurs when a mixed aqueous solution of an amino acid and a reducing sugar is heated, and as a reaction product, an amalide transfer product, a dicarbonyl compound, a furan compound,
It contains reaction products such as pyrrole compounds and melanoidins. The reason for incorporating the Maillard reaction product is that generation of spots, freckles, and the like can be suppressed. The Maillard reaction product used in the present invention is not particularly limited, but a Maillard reaction product obtained by removing phenylglucose compounds from a natural black component of brown sugar can be suitably used.

In order to obtain a Maillard reaction product from the natural black component of brown sugar, first, only the natural black component of brown sugar is obtained by the above-described method. Next, a Maillard reaction product can be obtained by removing phenylglucose compounds by silica gel column chromatography. The amount of the Maillard reaction product is not particularly limited, but is preferably 0.001 to 10 based on 1 part by weight of 3,4,6-trimethoxyphenyl-4′-OD-glucose.
Parts by weight, preferably 0.01 to 5 parts by weight. That is, 3,4,6-trimethoxyphenyl-4 ′ by weight ratio.
-OD-glucose: 2,5-dimethoxyphenyl-
4'-OD-glucose: Maillard reaction product =
1: 0.01 to 100: 0.001 to 10, preferably 1: 0.1 to 10: 0.01 to 5.

The above-mentioned essential components can be used as they are in the cosmetic composition, but they can be mixed with known excipients, diluents or other optional ingredients to form granules,
It can also be prepared and used in the form of solutions, suspensions and the like. Furthermore, in the cosmetic composition containing a natural black component extracted from brown sugar according to the present invention, in addition to the above essential components, a humectant such as vitamins and sodium hyaluronate as long as the effects of the present invention are not impaired. , Thickeners, surfactants, wetting agents, fragrances, dyes, preservatives, UV absorbers,
Antioxidants, amino acids, various animal and plant extracts, placenta extracts, and the like can be appropriately combined and combined.

The cosmetics for beautiful skin containing natural black components extracted from brown sugar according to the present invention include lotions, emulsions,
It can be used as creams such as cleansing creams, massage creams, emollient creams, basic cosmetics such as packs, and makeup cosmetics such as foundations, lipsticks, blushers, eye shadows, and towels. It can also be prepared as a soap, face wash cream, body lotion, bath salt and the like.

[0020]

Hereinafter, the present invention will be described based on examples.
The present invention is not limited by these examples. In addition, the compounding amount is weight%. (Preparation of Sample; Preparation of Sample Extracted from Brown Sugar) 5 kg of brown sugar produced in Okinawa was dissolved in 25 liters of water, and this was filled with polystyrene resin (Amberlite XAD, 2500 g) dispersed in 1 liter of water. The mixture was injected into a column having an inner diameter of 8 cm, and allowed to flow at a rate of 20 ml / min to adsorb the natural black component of brown sugar. Next, the mixture was washed with water until the sweetness was completely eliminated, and then 20% methanol was allowed to flow at a rate of 10 ml / min to elute the dye from the adsorbent. The developing solution was continued to flow until the flowing solution was no longer colored, and the developing solution was mixed and evaporated to dryness under reduced pressure at 60 ° C. or lower to obtain about 16 g of a brown residue having no sweetness.
This was dissolved in 2 liters of pure ethanol by heating, and after cooling, the deposited precipitate was separated by filtration. A brown powder consisting of a natural black component of no brown sugar was obtained. The resulting brown powder was further purified and separated by silica gel column chromatography to separate 2,5-dimethoxyphenyl-4'-OD-glucose, 3,4,6-trimethoxyphenyl-4'-OD-. Glucose, 3, 4
-Dimethoxyphenyl-4'-OD-glucose was obtained. 2,5-dimethoxyphenyl-4′-OD-glucose was used as sample 1, 3,4,6-trimethoxyphenyl-4′-OD-glucose was used as sample 2, and 3,4-
Sample 3 was dimethoxyphenyl-4′-OD-glucose. Samples 1 to 3 and Comparative Examples 1 to 6 were prepared by mixing Samples 1 to 3 at the ratios shown in Table 1.

[Table 1]

(Test Example 1: Anti-inflammatory action confirmation test)
Blood was collected from -King rats (250 to 350 g), and EDTA (5.8 mM) was added as an anticoagulant. The blood was centrifuged at 220 × g for 10 minutes, and the supernatant was further centrifuged at 1500 × g for 10 minutes. The precipitated platelets were washed twice with HEPES-saline buffer containing 2 mM EGTA (HEPES-25 mM, NaCl-135 mM, pH 7.4). Each of the samples of Examples 1 to 3 and Comparative Examples 1 to 6 was subjected to the concentrations (μg /
ml) was preincubated for 5 minutes at 37 ° C. Thereafter, ^{1-C 14} - 5 by addition of arachidonic acid
Incubated for minutes. The reaction was stopped with formic acid, and arachidonic acid metabolite was extracted with ethyl acetate. The extract was dried with nitrogen gas. A small amount of ethyl acetate was added thereto, and the mixture was separated and quantified by silica gel thin layer chromatography.
(Developing solution: chloroform: methanol: acetic acid: water = 9)
0: 8: 1: 0.8) The radioactive substance was detected by autoradiography, the spot was cut out, and the radioactivity was quantified with a liquid scintillation counter. Using the samples of Examples 1 to 3 and Comparative Examples 1 to 6 as no control, the ratios (%) of products when the samples of Examples and Comparative Examples were added to the control were calculated. The results are shown in Tables 2 to 5.

[0022]

[Table 2]

[0023]

[Table 3]

[0024]

[Table 4]

[0025]

[Table 5]

Test Example 2 Sensory Test Preparation of Samples According to the following composition, lotions 1 to 3 containing the respective samples of Examples 1 to 3 as active ingredients were prepared. Further, lotions 4 to 6 containing the samples of Comparative Examples 1 to 3 as active ingredients were prepared according to the following compositions. Lotion lotion Active ingredient 0.1 Calcium hydroxide 0.03 Glycerin 20.0 Ethanol 15.0 Purified water Remaining Total 100.0% by weight

2. Test Method The condition of a subject with atopic dermatitis was determined according to the following evaluation criteria, and the above-mentioned prepared lotion 1 was applied to the affected area every day before going to bed, to 20 subjects having an evaluation of 3 or 4. Next, the state of atopy of the subject after eight weeks was determined again according to the following evaluation criteria. Significantly effective when symptoms improved by 3 or more stages, Effective when improved by 2 stages,
The case where the improvement was one stage was slightly valid, and the others were invalid.
In addition, the ratio of the significant effect to the overall effect was defined as the improvement rate.
In addition, evaluation was similarly performed for lotions 2 to 5. Table 6 shows the results. <Evaluation Criteria> The skin turns darker and often has strong itching.
・ ・ ・ 4 Skin turns dark and sometimes with strong itching ・ ・ ・ ・ ・ ・
... 3 Skin discoloration, sometimes accompanied by strong itching ...
・ ・ ・ 2 The skin is slightly discolored with slight itching ・ ・ ・ ・ ・ ・ ・ ・ ・
... 1 No discoloration of the skin is seen, and almost no itching is felt ...
... 0

[0028]

[Table 6]

As is evident from the above test results, the cosmetic for beautiful skin containing a natural black component extracted from brown sugar according to the present invention contains 3,4,6-trimethoxyphenyl-4 'as an active ingredient. -OD-glucose and 2,5-
Since it contains dimethoxyphenyl-4′-OD-glucose, it prevents or prevents various troubles occurring on the skin, such as atopic dermatitis, as compared with when used alone. It can be seen that an excellent effect can be obtained, which is improved, and that it has an anti-inflammatory effect.

The following is an example of the formulation of a cosmetic for beautiful skin containing a natural black component extracted from brown sugar according to the present invention.
In addition, the compounding amount is weight%. (Formulation Example 1) Emulsion Self-emulsifying glycerol monostearate 1.11 Polyoxyethylene cetyl ether 1.89 MC stearic acid 2.00 Cetanol 1.00 Isopropyl myristate 2.00 Paraoxybenzoic acid methyl ester 0.20 Sample of Example 1 0.01 Mulberry extract 0.01 Appropriate amount of flavoring agent Appropriate amount of preservative Purified water balance 100.00

(Formulation Example 2) Nutrition cream squalane 4.00 cetyl isooctanolate 2.50 cetyl alcohol 1.00 stearic acid 1.00 sorbitan monooleate 0.50 polyoxyethylene stearate 2.50 propylene glycol 8 0.000 Sorbinol 2.00 Potassium hydroxide 0.10 Sample of Example 2 0.02 Appropriate amount of fragrance Preservatives Appropriate amount Purified water balance 100.00

Formulation Example 3 Emulsifiable pack Liquid paraffin 5.00 Sorbitan monooleate 1.00 Polyoxyethylene monooleate 1.50 Cetanol 1.00 Ethanol 1.00 Polyvinyl alcohol 14.00 Pyrrolidone carboxylic acid sodium salt 5.00 Sample of Example 3 0.01 Perfume Appropriate amount Preservative Appropriate amount Purified water balance 100.00

Formulation Example 4 Body Shampoo Sodium Lauryl Sulfate 10.00 Sodium Lauryl Sulfosuccinate 20.00 Lauryl Diethanolamide 4.00 Hydrolyzed Collagen 1.00 Ethylene Glycol Distearate 1.00 Tetrasodium Edetate Tetrahydrate 0 .10 Allantoin 0.01 Lysozyme chloride 0.01 Sample of Example 0.02 Perfume Appropriate amount Purified water Balance 100.00

Formulation Example 5 Medicated Cleansing Cream Light Liquid Paraffin 35.00 Beeswax 8.00 Cetyl Palmitate 3.00 Lanolin 1.00 Sorbitan Sesquioleate 2.00 Polyoxyethylene (20) Sorbit Beeswax 4.50 Preservative Agent / antioxidant qs 70% sorbitol 4.00 Sample of Example 2 0.008 perfume qs Purified water balance 100.00

[0035]

Industrial Applicability The cosmetics for beautiful skin containing a natural black component extracted from brown sugar according to the present invention prevent or prevent various troubles occurring on the skin such as atopic dermatitis. And inflammation of the skin and the like can be prevented.

──────────────────────────────────────────────────続 き Continued on the front page (51) Int.Cl. ⁷ Identification code FI Theme coat ゛ (Reference) A61K 7/50 A61K 7/50 F term (Reference) 4C083 AA082 AA112 AB032 AC022 AC072 AC122 AC132 AC182 AC242 AC352 AC392 AC402 AC422 AC442 AC482 AC532 AC642 AC682 AC782 AC792 AC852 AD112 AD391 AD392 AD432 AD472 AD512 CC05 CC07 CC11 CC23 DD31 EE12 EE13

Claims (1)

[Claims] 1. A 3,4,6-formula represented by the following formula 1
A brown sugar comprising trimethoxyphenyl-4'-OD-glucose and 2,5-dimethoxyphenyl-4'-OD-glucose represented by the following formula (2): A cosmetic for beautiful skin containing natural black components extracted from. Embedded image Embedded image