JP2007169203A - Whitening cosmetics and skin external preparations containing Kusunohakebomo extract - Google Patents

Abstract

A whitening agent that suppresses the production of melanin, has a tyrosinase activity inhibitory effect effective in preventing and improving pigmentation, stains, freckles, liver spots, etc. after sunburn, and has an excellent effect on skin whitening, and Anti-oxidant effective in preventing skin aging and preventing acne, atopic dermatitis, allergic dermatitis and dandruff etc It was an issue to provide a skin external preparation excellent in skin resistance.
The present invention has found that an extract of the genus Coccinaceae (scientific name: Vaccinium dunalianum var. Urophyllum) has excellent tyrosinase activity inhibitory activity and antioxidant activity.
[Selection figure] None

Description

  The present invention contains a specific plant extract to suppress the production of melanin, and has a tyrosinase activity inhibitory effect effective in preventing and improving pigmentation, stains, freckles, liver spots, etc. after sunburn. In addition to the agent and whitening cosmetics that have an excellent effect on skin whitening, it has an excellent antioxidant effect to prevent skin aging and is effective in preventing acne, atopic dermatitis, allergic dermatitis and dandruff The present invention relates to an antioxidant and an external preparation for skin excellent in these effects.

  Pigmentation such as skin spots and freckles is a result of excessive synthesis of melanin pigments caused by ultraviolet rays and other stimuli, and is a major cosmetic problem.

  This melanin pigment is produced in melanin-producing granules (melanosomes) in melanocytes (melanocytes) existing in the basal layer at the bottom of the epidermis, and the produced melanin diffuses to adjacent cells by osmotic action. The biochemical reaction in this melanocyte is considered as follows.

That is, tyrosine, an essential amino acid, is converted to dopaquinone by the action of the enzyme tyrosinase, and this process changes from red and colorless pigments to black melanin pigments by enzymatic or non-enzymatic oxidation. is there. Therefore, suppressing the action of tyrosinase, which is the first stage of the reaction, is important for suppressing melanin production. (See Patent Documents 1 and 2)
Conventionally, substances that suppress the production of melanin have been used to prevent stains and freckles. For example, L-ascorbic acid, L-ascorbic acid-2-magnesium phosphate, L-ascorbic acid glucoside, cysteine, arbutin, glutathione A method of applying a whitening agent such as ointment, cream, lotion and the like to a topical application is common. In addition, a method of locally injecting a reducing amino acid such as glutathione is also performed. However, these whitening cosmetics and the like cannot always be said to be sufficiently effective, and there has been a demand for enhancing the whitening effect and further the skin beautifying effect. In addition, since these substances have a strong action on the skin, there are some problems in terms of safety, and mild whitening agents for the skin have been demanded.

In recent years, the generation of active oxygen in the living body and various effects caused by it have been reported. Since the skin is an organ that is in direct contact with the outside world, it is easily affected by environmental factors such as ultraviolet rays and radiation. When the active oxygen becomes excessive in the skin, it reacts with unsaturated fatty acids of biological membrane phospholipids to produce lipid peroxide. This lipid peroxide may cause protein denaturation, membrane destruction, aging, carcinogenesis, etc., which causes rough skin and skin aging. Against this background, vitamin E, vitamin C and oryzanol as antioxidants, and various plant extracts (Hamelis, Clove, Rosemary, Ages, Keihi, Licorice) have been used to eliminate excess active oxygen. However, its antioxidant action was weak and the effect was insufficient. The current situation is that there is a strong demand for the development of new antioxidants that are effective in preventing oxidation of lipid components of skin, oxidative damage of skin, and skin aging by blending into cosmetics. (See Patent Documents 3, 4, and 5)
JP-A-5-105620 JP 2001-105620 A JP-A-5-238925 JP-A-5-70333 JP 11-279069 A

  The present invention has been made in view of the above circumstances, and the purpose thereof is skin aging by having an excellent tyrosinase activity inhibitory action and a whitening effect excellent in a whitening effect, and further having an excellent antioxidant effect. It is to provide an antioxidant effective for preventing acne, preventing acne, atopic dermatitis, allergic dermatitis and dandruff, and a skin external preparation excellent in these effects.

  As a result of investigating the tyrosinase activity inhibitory action and antioxidant action of a wide variety of substances, the present inventor has found that an extract of the genus Ezoaceae genus Echinacea (scientific name Vaccinium dunalianum var. Urophyllum) has an excellent tyrosinase activity inhibitory action and It has been found that it has an antioxidant action, and has led to the completion of the present invention. There has been no report on the tyrosinase activity inhibitory action of an extract of the genus Azalea, Vaccinium dunalianum var. Urophyllum, and it has not been used as a whitening agent, an antioxidant, or an application to an external skin preparation. Is also not known.

  That is, this invention relates to the skin external preparation characterized by mix | blending the extract of the genus Coccinaceae genus Cusnohaco biloba (scientific name Vaccinium dunalianum var. Urophyllum). In addition, it is a whitening agent and an antioxidant containing as an active ingredient an extract of the genus Ezocephalum genus Cusnohaco biloba (scientific name: Vaccinium dunalianum var. Urophyllum).

  According to the present invention, a whitening agent having an inhibitory effect on tyrosinase activity and having an excellent whitening effect can be obtained, and a whitening cosmetic preparation having excellent prevention and improvement of pigmentation, sunburn, freckles, liver spots and the like after sunburn can be obtained. Antioxidant with antibacterial and deodorizing effects, which is effective in preventing skin aging by having an excellent antioxidative effect, and is effective in preventing acne, atopic dermatitis, allergic dermatitis and dandruff And a skin external preparation excellent in these effects can be obtained.

  Hereinafter, the configuration of the present invention will be described in more detail.

  The azalea family genus Coccinella genus used in the present invention (scientific name: Vaccinium dunalianum var. Urophyllum) grows in forests or broad-leaved forests of 2000-2700 m above sea level in Yunnan, Guangxi, southern Mongolia, China. In its name, it is Tsubaki Koshiba Tachibana. The extract of the genus Coxnochacoceae used in the present invention is the leaves, stems, buds, flowers, seeds, or whole plant plants of the genus Coxnocochidae soaked or heated under reflux together with the extraction solvent, filtered and concentrated. Obtained.

  In more detail, kusunochakebomo is a solvent, for example, a polar solvent such as water, lower alcohol, hydrous lower alcohol, propylene glycol, 1,3-butylene glycol, butanol, or an organic solvent such as chloroform, ethyl acetate, ether, or a mixture thereof. The extract obtained by extraction in (1) is used as it is or a concentrated extract, or the extract is adsorbed, for example, after removing impurities using an ion exchange resin, or after being adsorbed on a porous polymer column, methanol or Extracts eluted and concentrated with ethanol can also be used. Also, a partitioning method, for example, an extract extracted with butanol can be used.

  To give a specific example of the production method, the leaves of Cusnus palmatum are extracted with 50-100% ethanol aqueous solution when heated, the insoluble matter is filtered after cooling, and the filtrate is concentrated under reduced pressure to precipitate. The filtrate is further concentrated and allowed to stand after concentration, and the precipitated crystals are collected and recrystallized repeatedly with water to obtain a concentrated extract of Cinnospider.

  In the present invention, the amount of the extract of the genus Coccinaceae (Vaccinium dunalianum var. Urophyllum) in the azalea family is 0.005 to 20.0%, preferably in a solid content concentration in the total amount of the whitening cosmetic or skin external preparation. Is 0.01 to 10.0%.

  The whitening cosmetic or skin external preparation of the present invention includes L-ascorbic acid, L-ascorbic acid-2-sodium phosphate, L-ascorbic acid-2-phosphoric acid, which are existing whitening agents, together with an extract of Kusunochakebomo. Magnesium, L-ascorbic acid glucoside, ascorbyl tetrahexyldecanoate, cysteine, arbutin, tranexamic acid, glutathione and the like may be blended.

  The skin external preparation of the present invention includes antioxidants such as vitamin E, vitamin C, vitamin B2, carotenoid, flavonoid, saponin, tannin, coenzyme Q10 and oryzanol and their derivatives, various plant extracts (hamamelis, clove) , Rosemary, age, keihi, licorice) and the like.

  The whitening cosmetic or skin external preparation of the present invention can be blended with what is usually used in cosmetics, quasi-drugs and the like as long as the effects of the present invention are not impaired. Hydrocarbons, vegetable oils and fats, waxes, synthetic ester oils, silicone oil phase components, fluorine oil phase components, higher alcohols, fatty acids, thickeners, UV absorbers, powders, pigments, colors Material, anionic surfactant, cationic surfactant, nonionic surfactant, amphoteric surfactant, polyhydric alcohol, sugar, polymer compound, physiologically active ingredient, transdermal absorption enhancer, solvent, Antioxidants, fragrances, preservatives and the like can be blended.

  In addition, metal sequestering agents such as edetate disodium, edetate trisodium, sodium citrate, sodium polyphosphate, sodium metaphosphate, and gluconic acid can be blended.

  The whitening cosmetic and skin external preparation according to the present invention can be applied not only to skin care cosmetics, but also to makeup cosmetics such as foundations and lipsticks, and hair cosmetics such as hair creams and hair tonics. , Lotions, lotions, emulsions, creams, packs, ointments, dispersions, solids, mousses, and the like.

EXAMPLES The present invention will be specifically described below with reference to examples, but the technical scope of the present invention is not limited to these examples.
(1) Tyrosinase activity inhibitory effect The following test was done about the tyrosinase activity inhibitory effect and the whitening effect of the compound which concerns on this invention.
<Preparation of sample>
(1) Kusunohokoberry extract 1
After immersing 100 g of camphor leaf leaves in 50% ethanol aqueous solution for 1 day, the extract was concentrated to obtain 5.3 g of solid content.
(2) Kusunohokoberry extract 2
100 g of blackberry leaves are extracted with a 60% aqueous ethanol solution when heated, the insoluble matter is filtered after cooling, the filtrate is concentrated under reduced pressure, and the first deposited precipitate is removed by filtration. The filtrate was further concentrated and allowed to stand, and the deposited precipitate was collected and recrystallized three times with water to obtain 2.3 g of a solid content.
<Experiment method>
Normal melanocytes were dissolved in a phosphate buffer solution (100 mM, pH 6.8) containing 0.1% Torton X-100 to a concentration of 3.0 × 10 ⁵ cells / mL, and this was used as a tyrosinase crude enzyme solution. . The effect of the crude enzyme solution on the tyrosinase activity of the sample was evaluated by measuring the dopa oxidase activity of the crude enzyme solution. The dopa oxidase activity was obtained by dispensing 50 μL of the crude enzyme solution into a 96-well microplate and adding L-DOPA (0.25 mg / mL phosphate buffer (50 mM, pH 6.8)) and a sample with a predetermined concentration. Started. The absorbance at 405 nm was measured with a microplate reader immediately after the start and after incubation at 37 ° C. for 2 hours. The amount of melanin produced was calculated using a calibration curve created with commercially available synthetic melanin. Tyrosinase activity was calculated as the amount of melanin produced per unit time and the amount of protein in the enzyme solution.

As a reference example, arbutin, which is already known to have a tyrosinase activity inhibitory effect, was also tested in the same manner as described above.
<Result>
The results are shown in Table 1.

From the results shown in Table 1, it can be seen that the cinnamon bilberry extract of the present invention exhibits an excellent tyrosinase activity inhibitory action and has a tyrosinase activity inhibitory action superior to arbutin.
(2) Whitening effect test <Test method>
1. Preparation of pigmentation by ultraviolet irradiation The test site is the inner left upper arm that is not easily exposed to sunlight in daily life. Irradiation with ultraviolet rays corresponding to 5 MED was performed to produce pigmentation with a diameter of 1 cm. As a light source, a multiport solar UV simulator model 601 (Solar Light Co. Inc.) is used with a wavelength range of 300 to 400 nm and a peak wavelength of 356 nm, and the irradiation intensity is measured using a multi-function measurement system model PMA2100 (Solar Light Co. Inc.). It was measured.
2. Test preparation A test preparation having the following formulation is used. A test preparation was obtained according to a conventional method for preparing an oil-in-water emulsion composition.

1. Application Method and Application Period About 20 mg of the test preparation was applied twice a day in the morning and evening for 3 weeks to 2 × 2 cm ² including each ultraviolet irradiation site.
2. Skin color measurement and evaluation On the day of observation, the test site was measured using a spectrocolorimeter CR-13 (Minolta). L * was used as a colorimetric parameter, and pigmentation was evaluated using a ΔL * value (= L * value before ultraviolet irradiation−L * value after ultraviolet irradiation).

The whitening effect was evaluated according to the following criteria. X: ΔL * value is the same as control value Δ: ΔL * value is (control value −1.0) or more ○: ΔL * value is (control value−1) .0) <Result>

From the results shown in Table 3, it can be seen that the cinnamon leaf extract of the present invention has a whitening effect superior to that of arbutin.
(3) Antioxidant effect test <Test method>
Dissolve 1.0 mg methyl linolenate in 1.0 mL of acetone, add 0.001 mg or 0.01 mg solid extract of Cunnochakeboko extract 1 and Cunnochakeboko extract 2 to a threaded test tube. After pouring and drying, the oxidized group was treated at 50 ° C. for 4 hours, and the non-oxidized group was stored at 4 ° C. After the treatment, 3.0 mL of a non-aqueous TBA reagent (0.12% 2-thiobarbituric acid / 0.50% triethylamine / acetic acid) was added and reacted at 95% for 1 hour. Immediately after the reaction, the mixture was cooled with water, the absorbance at 532 nm was measured, and the oxidation inhibition rate was calculated.

Oxidation inhibition rate (%) = [1- (As50−As4) / (Ac50−Ac4)] × 100
Ac50: control Absorbance at 50 ° C heating Ac4: control Absorbance at 4 ° C storage As50: Sample Absorbance at 50 ° C heating As4: Absorbance at 4 ° C storage Note that the target is vitamin C instead of 50% ethanol aqueous extract Table 4 shows the results of the same operation with E (DL-α-tocopherol, manufactured by Tokyo Chemical Industry Co., Ltd.) and BHT (manufactured by Wako Pure Chemical Industries, Ltd.).

  As shown in Table 4, the Kusonochaboko extract has an antioxidant effect superior to that of Vitamin E, and exhibits an antioxidant effect equivalent to that of BHT when the concentration is increased.

  Examples of whitening cosmetics and external preparations for skin containing the compounds according to the present invention will be given below. A compounding quantity represents the mass%.

Example 1
Cream 1
(Prescription) Mass%
Oil phase Cetyl alcohol 7.0
Stearyl alcohol 3.0
Squalane 4.0
Vaseline 3.0
Liquid paraffin 15.0
Aqueous phase POE (20) sorbitan monostearate
3.0
1,3-butylene glycol 3.0
Kusunohokoberry extract 1 0.5
Preservative appropriate amount Fragrance 0.2
Purified water balance (preparation method)
The oil-in-water emulsion composition was prepared according to a conventional method.

Example 2
Essence (Prescription) Mass%
Stearic acid 2.5
Cetyl alcohol 1.5
Vaseline 3.0
Liquid paraffin 15.0
Decaglyceryl monolaurate 1.0
Monostearic acid POE (20) sorbitan
3.0
Xanthan gum 0.5
1,3-butylene glycol 10.0
Triethanolamine 1.0
Kusunohokoberry extract 2 0.3
Preservative appropriate amount Fragrance 0.2
Purified water balance (preparation method)
The oil-in-water emulsion composition was prepared according to a conventional method.

Example 3
Lotion (Prescription) Mass%
Oleyl alcohol 0.1
POE (20) sorbitan monolaurate
0.5
POE (15) lauryl ether 0.5
Glycerin 4.0
1,3-butylene glycol 6.0
Ethyl alcohol 10.0
Kusunoha peach ethyl acetate extract 0.01
Preservative appropriate amount Fragrance 0.2
Purified water balance (preparation method)
All ingredients were mixed and prepared at 50 ° C. until uniform.

Example 4
Cream 2 (emollient type)
(Prescription) Mass%
Oil phase Stearyl alcohol 6.0
Stearic acid 2.0
Isocetyl myristate 6.0
Glyceryl tri-2-ethylhexanoate 3.0
Macadamia nut oil 1.0
Dimethylpolysiloxane (6cs) 0.2
POE (20) cetyl ether 3.0
Glyceryl monostearate 2.0
Aqueous phase Hydrogenated soybean lecithin 0.2
1,3-butylene glycol 5.0
Kusunohokoberry extract 1 10.0
Xanthan gum 0.1
Sodium hyaluronate 0.01
Citric acid 0.1
Sodium citrate 0.4
Preservative Appropriate amount Purified water The remainder (preparation method)
It was prepared according to a conventional method for producing an oil-in-water emulsion composition.

Example 5
Skin lotion (prescription)
Oil phase Stearyl alcohol 0.3
Tri (caprylic acid / capric acid) glyceryl
0.1
POP (4) POE (20) cetyl ether 0.6
Aqueous phase Propylene glycol 10.0
Sodium hyaluronate 0.1
Kusunoha peach acetone extract 5.0
Preservative Appropriate amount Purified water The remainder (preparation method)
It was prepared according to a conventional method for producing an oil-in-water emulsion composition.

Example 6
Emulsion (prescription) mass%
Oil phase Batyl alcohol 1.0
d-δ-tocopherol 0.1
Squalane 5.0
Cetyl 2-ethylhexanoate 5.0
Dimethylpolysiloxane 0.5
Cetyl palmitate 0.5
Behenyl alcohol 1.5
Stearic acid 0.5
Lipophilic glyceryl monostearate 1.0
Monostearic acid POE (20) sorbitan
1.0
Tetraoleic acid POE (40) sorbitan
1.5
Aqueous phase Propylene glycol 7.0
Xanthan gum 0.1
Kusunoha peach 50% 1,3-butylene glycol aqueous solution extract
1.0
Preservative Appropriate amount Purified water The remainder (preparation method)
It was prepared according to a conventional method for producing an oil-in-water emulsion composition.

Example 7
Cream 3 (water-in-oil emollient type)
(Prescription) Mass%
Oil phase Dimethylpolysiloxane 4.0
Dimethicone copolyol 0.5
Decamethylcyclopentasiloxane 5.0
Tri (Capryl / Capric Acid) Glyceryl
15.0
Beeswax 2.0
Decaglyceryl pentahydroxy acid 2.0
Isostearic acid 1.0
Aqueous phase Glycerin 4.5
Sodium hyaluronate 0.01
Kusunohabokomomo extract 2
3.0
Preservative Appropriate amount Purified water The remainder (preparation method)
An emulsified composition was prepared according to a conventional method for emulsifying water-in-oil emulsified compositions.

Example 8
Sunscreen cream (prescription)
Oil phase Dimethylpolysiloxane 2.5
Liquid paraffin 7.0
Decamethylcyclopentasiloxane 3.0
Cetyl alcohol 4.0
Octyl paramethoxycinnamate 7.0
Condensed ricinoleic acid hexaglyceryl 0.5
POE (20) cetyl ether 1.0
Powder phase Titanium oxide 3.0
Aqueous phase Sodium cetyl sulfate 1.0
Stearoyl methyl taurine sodium 0.3
1,3-butylene glycol 5.0
Kusunohokoberry extract 1 0.8
Xanthan gum 0.3
Preservative appropriate amount Purified water balance

(Preparation method)
After the powder phase was added to the oil phase, an emulsion composition was prepared according to a conventional method for emulsifying water-in-oil emulsion compositions.

(Evaluation of effect)
As a result of evaluating the whitening effect and the antioxidant effect of the cosmetics of Examples 1 to 8 according to the whitening effect test method and the antioxidant effect test method described above, the whitening effect and the antioxidant effect were recognized in all the cosmetics. .

  The whitening agent of the present invention has an excellent inhibitory effect on tyrosinase activity, has an effect of fainting pigmentation, stains, freckles, liver spots and the like after sunburn, and has an excellent effect on whitening, and can be applied to whitening cosmetics. Furthermore, it has an excellent anti-oxidant effect to prevent skin aging, and to obtain an anti-oxidant effective for acne, atopic dermatitis, allergic dermatitis and dandruff, and a skin external preparation excellent in these effects. I can do it.

Claims (4)

A whitening agent comprising an extract of the genus Ezoaceae of the genus Ezoaceae (scientific name: Vaccinium dunalianum var. Urophyllum) as an active ingredient. A whitening cosmetic comprising the whitening agent according to claim 1. An antioxidant comprising an extract of the genus Ezoaceae of the genus Azalea (scientific name: Vaccinium dunalianum var. Urophyllum) as an active ingredient. An external preparation for skin, comprising an extract of the genus Ezoaceae of the genus Ezoaceae (scientific name: Vaccinium dunalianum var. Urophyllum).