JP3647296B2 - Inhibition of tyrosinase activity and compositions containing the same - Google Patents

Description

【００２７】
［実施例１］（クリーム）
下記記載の配合量においてＡ成分を加熱混合し、７０℃に保つ。次いでＢ成分を加熱混合し、７０℃に保つ。Ｂ成分をＡ成分に均一に混合し、次いでＣ成分を注入撹拌混合した後、撹拌しながら３０℃まで冷却しクリームを得た。

【００２８】
［比較例１］（クリーム）
実施例１において成分（Ｂ）キク科植物学名:Gnaphalium semiamplexicaule抽出物を除いた以外はすべて実施例１と同様にして調製し、試験に使用した。
【００２９】
［実施例２］（美白乳液）
下記記載の配合量においてＡ成分を加熱混合し、７０℃に保つ。次いでＢ成分を加熱混合し、７０℃に保つ。Ｂ成分をＡ成分に均一に混合し、次いでＣ成分を注入撹拌混合した後、撹拌しながら３０℃まで冷却し美白乳液を得た。
（組成）
配合成分 配合量（wt%）
（A） １，３−ブチレングリコール 5.0
エチルアルコール 5.0
キク科植物学名:Gnaphalium semiamplexicaule抽出物（抽出例１） 2.0
精製水 残量
（B） スクワラン 5.0
ワセリン 2.0
ミツロウ 0.5
ソルビタンセスキオレイン酸エステル 0.8
ポリオキシエチレンオレイルエーテル（２０E.O.） 1.2
防腐剤 適量
香料 適量
(C) カルボキシビニルポリマー（1.0%水溶液） 20.0
水酸化カリウム 0.1
【００３０】
［比較例２］（美白乳液）
実施例２において成分（Ｂ）キク科植物学名:Gnaphalium semiamplexicaule抽出物を除いた以外はすべて実施例２と同様にして調製し、試験に使用した。
【００３１】
［試験例２］（使用効果試験）
実施例１、２、比較例１、２において調製されたクリームおよび美白乳液の美白効果について、使用テストによる試験を行った。使用テストは各々２５〜４０才の２０名の女性をパネルとし、毎日、朝夜の２回、洗顔後に試験クリームまたは美白乳液を適量顔面に２週間にわたって塗布することにより行った。美白効果の評価基準は、シミ ソバカスがほとんど目立たなくなったものを「有効」、シミ ソバカスがあまり目立たなくなったものを「やや有効」、変わらないものを「無効」として、比較例と比較して評価を行った。
第２表（表２）に示すごとく、比較例１、２に比べ実施例１、２では良好な結果が得られた。
【００３２】
【表２】

【００３３】
【発明の効果】
本発明のチロシナーゼ活性阻害剤およびこれを含有する化粧品、医薬品、医薬部外品、食品等の組成物は、生体内におけるメラニンの生成を抑制する効果がある。従って、健康上、美容上の障害についての治療に有効である。[0001]
BACKGROUND OF THE INVENTION
The present invention relates to a tyrosinase activity inhibitor having a tyrosinase activity inhibitory effect effective for prevention and improvement of pigmentation, stains and freckles after sunburn, and a composition containing these. Furthermore, the present invention relates to a skin external preparation that can be used in the fields of pharmaceuticals, quasi-drugs, cosmetics and the like containing the inhibitor.
[0002]
[Prior art]
Melanin pigments are deeply involved in the development of skin pigmentation and spots. Melanin pigments are produced in granules called melanosomes present in melanocytes, but the mechanism of their production is dopaquinone produced by the action of the enzyme tyrosinase from tyrosine, an essential amino acid, which is oxidized enzymatically or non-enzymatically. This is the process leading to the formation of black melanin pigment. Therefore, it is considered that the production of melanin pigment is suppressed by inhibiting the activity of the enzyme tyrosinase. Conventionally, ascorbic acid, glutathione, and the like are blended in whitening cosmetics and the like as substances that inhibit tyrosinase activity. However, since ascorbic acid has the property of being easily oxidized, cosmetics containing ascorbic acid cause quality deterioration such as discoloration and odor change. Moreover, since glutathione has a peculiar odor, it is unsuitable for blending it into cosmetics.
[0003]
Further, natural extracts have been studied for the purpose of whitening effect, but the effect was still insufficient (Japanese Patent Laid-Open Nos. 8-12566, 9-227333, and No. 4-342519). However, natural product extracts are expected to be useful because of their high safety, and therefore, the development of cosmetics containing natural product extract components that are excellent in whitening effects and have no problems with safety, color, smell, etc. Is desired.
[0004]
[Problems to be solved by the invention]
Provided are a plant extract having high tyrosinase activity inhibitory activity (tyrosinase inhibitory activity) and suppressing melanin production caused by tyrosinase, and a composition containing the same.
[0005]
[Means for Solving the Problems]
In light of this situation, the present inventors have conducted extensive research to improve the problems of the prior art, and as a result, surprisingly, the extract of the asteraceae plant name: Gnaphalium semiamplexicaule has a strong tyrosinase activity. It was found to have an inhibitory effect.
[0006]
That is, the present invention includes an extract of a tyrosinase activity containing an extract of the asteraceae plant, scientific name: Gnaphalium semiamplexicaule), and a composition such as a cosmetic, pharmaceutical, or quasi-drug containing the same. Is to provide.
[0007]
DETAILED DESCRIPTION OF THE INVENTION
Hereinafter, embodiments of the present invention will be described in detail. Scientific name used in the invention: Gnaphalium semiamplexicaule is a plant belonging to the family Asteraceae, native to Mexico.
[0008]
The extract of Gordobo used in the present invention is obtained by extracting from a part or all of a plant body such as leaves, stems, flowers, seeds, fruits, rhizomes and roots of the plant. Preferably, it is obtained by extraction from one of leaves or stems or a mixture of both. Generally, dry or live plants are used as they are or after cutting.
[0009]
As the extraction solvent to be used, 100 parts of the following extraction solvent is used for 5 to 50 parts per dry matter or dry matter equivalent of the live plant.
[0010]
The extraction solvent is generally water, lower monohydric alcohols (methanol, ethanol, 1-propanol, 2-propanol, 1-butanol, 2-butanol, etc.), liquid polyhydric alcohol (1,3-butylene glycol). , Propylene glycol, etc.), lower alkyl esters (ethyl acetate, etc.), hydrocarbons (benzene, hexane, pentane, etc.), ketones (acetone, methyl ethyl ketone, etc.), ethers (diethyl ether, tetrahydrofuran, dipropyl ether), acetonitrile, etc. Is mentioned. These solvents may be used alone or in combination of two or more. Preferably, one or two or more solvents among water or a water-soluble solvent (solvents that can be mixed with water in an arbitrary ratio. For example, ethanol, methanol, propylene glycol, etc.) may be used.
[0011]
The extraction method is not particularly limited, and the extraction is performed at room temperature or under heating. Examples of the method include normal extraction and Soxhlet extraction. Although there is no restriction | limiting in extraction time, Generally 1 hour-1 week are preferable.
[0012]
As described above, the extract according to the present invention is usually obtained as a liquid extract. Although the said extract may be used as it is, a processed material can also be used after performing various processes. Such processed products are also included in the extract according to the present invention. As such, for example, a concentrate obtained by concentrating them under normal pressure or reduced pressure, or a solid obtained by evaporating the solvent in the concentrate to dryness, or crystallization of an active ingredient from the concentrate, followed by filtration and drying. Or a solid obtained by freeze-drying the concentrated liquid.
[0013]
The use amount (blending amount) per dry matter as the tyrosinase activity inhibitor of the extract of the gold lobo according to the present invention is not particularly limited, but is 0.001 to 20.0 wt% (hereinafter referred to as wt%) based on the total amount. ), Particularly 0.01 to 10 wt% is desirable.
[0014]
The composition containing the tyrosinase activity inhibitor of the present invention is characterized by containing the above tyrosinase activity inhibitor, and its use is optional, but it is widely used in cosmetics, pharmaceuticals, quasi drugs, toiletries, foods, etc. be able to.
[0015]
The cosmetic form to which the present invention is applied is not particularly limited, and examples thereof include skin lotion, emulsion, cream, foundation, pack, lipstick, face wash, shampoo, rinse, hair tonic and the like. These cosmetics include various components generally used in cosmetics, that is, aqueous components, oily components, powder components, alcohols, esters, surfactants, moisturizers, whitening components, ultraviolet absorbers, thickeners, Components such as a colorant, a fragrance, an antioxidant, a pH adjuster, a chelating agent, and an antiseptic can be blended.
[0016]
The pharmaceutical form and quasi-drug to which the present invention is applied are not particularly limited in dosage form. For example, tablets, granules, capsules, oral preparations such as liquid medicine, ointments, poultices, creams, liquid preparations, etc. Examples include external preparations, sterile solutions, suspensions and other injections, bath preparations and the like.
[0017]
These medicaments can take the required unit dosage forms together with physiologically recognized vehicles, carriers, excipients, binders, stabilizers, flavoring agents and the like. For example, compositions for tablets and capsules include binders such as tragacanth, gum arabic, and gelatin, excipients such as microcrystalline cellulose, gelatinizing starch, swelling agents such as alginic acid, and lubricants such as magnesium stearate. An agent, a sweetener such as sucrose, lactose, and saccharin, a flavoring agent such as peppermint, red mono oil, and cherry can be mixed together and formulated by an ordinary method. In addition, sterile compositions for injection dissolve active substances in vehicles such as water for injection, naturally produced vegetable oils such as sesame oil, coconut oil, peanut oil, cottonseed oil, or synthetic fat vehicles such as ethyl oleate Or it can be formulated by the usual method of suspending. As an external preparation, vaseline, paraffin, fats and oils, lanolin, macrogol and the like are used as a base, and an ointment and a cream are prepared by a usual method.
[0018]
The topical skin preparation of the present invention means any dosage form that can be applied externally, such as lotion, milky lotion, cream, foundation, pack, essence, lipstick, face wash, gel, aerosol, ointment, poultice, Examples include those applied to the skin such as paste agents, plaster bath agents, and cleaning agents, and those applied to hair such as shampoos, rinses, treatments, and hair tonics. Moreover, the external preparation for skin of the present invention can be used for any of pharmaceutical use, pharmacy use and cosmetic use.
[0019]
The skin external preparation of the present invention includes an aqueous component, an oily component, a powder component, a wax, a fatty acid, an alcohol, an ester, a surfactant, a moisturizing agent, and a whitening component, which are components used in normal skin external preparations. UV absorbers, thickeners, colorants, fragrances, antioxidants, pH adjusters, chelating agents, preservatives and the like can be appropriately blended within the scope of achieving the object of the present invention.
[0020]
The food to which the present invention is applied is not particularly limited, and can be obtained, for example, by adding a required amount of an extract to each food raw material as a general food and processing and producing it by a normal production method.
[0021]
【Example】
Hereinafter, the present invention will be described in detail based on examples. The present invention is not limited to these.
[0022]
[Extraction Example 1] Asteraceae plant scientific name: Gnaphalium semiamplexicaule flower and stem portion 16g was immersed in 50% ethanol at room temperature for 24 hours, and then the extract was concentrated to obtain 1.3 g of extract. A 1 mg / ml solution was prepared by diluting this extract with DMSO, and the following experiment was conducted by adjusting the concentration by diluting this solution.
[0023]
[Test Example 1] Tyrosinase activity inhibition test The tyrosinase activity inhibitory effect evaluation test method used in the present invention in order to examine the tyrosinase activity inhibitory ability of the Asteraceae plant scientific name: Gnaphalium semiamplexicaule extract is as follows. 1 ml of 0.3 mg / ml tyrosine solution is added to 1 ml of 0.1 M phosphate buffer (pH 6.8), and 1.0, 0.5, 0.05, 0.01, 0.0005, 0.0001% 0.9 ml of the prepared test sample was added and incubated at 37 ° C. for 10 minutes. Thereto was added 0.1 ml of 1 mg / ml mushroom-derived tyrosinase, incubated at 37 ° C. for 15 minutes, and absorbance (A) was measured at a wavelength of 475 nm using a spectrophotometer. Absorbance (B) of a buffer added instead of tyrosinase, Absorbance (C) of a buffer added instead of a test sample, and Absorbance (D) of a buffer added instead of a test sample and tyrosinase And the inhibition rate was calculated | required according to the following formula.
[0024]
[Expression 1]
Tyrosinase activity inhibition rate (%) = {1− (A−B) / (C−D)} × 100
[0025]
The results are shown in Table 1 (Table 1). As a reference example, a similar test was also conducted on a 50% ethanol extract of Mexican Arnica (FARSA ARNICA, scientific name: Heterotheca inuloides), which is already known to have an inhibitory effect on tyrosinase activity (Japanese Patent Laid-Open No. 7-118139). Publication). The results are also shown in Table 1 (Table 1). In the table,-indicates untested.
As a result of the test, it was confirmed that the Gordobo extract applied in the present invention has a tyrosinase activity inhibitory effect comparable to Mexican Arnica, which is already known to have a tyrosinase activity inhibitory action.
[0026]
[Table 1]

[0027]
[Example 1] (Cream)
In the blending amount described below, the component A is heated and mixed and kept at 70 ° C. Next, the component B is heated and mixed and maintained at 70 ° C. The B component was uniformly mixed with the A component, and then the C component was injected, mixed with stirring, and then cooled to 30 ° C. with stirring to obtain a cream.

[0028]
[Comparative Example 1] (Cream)
In Example 1, except that the component (B) Asteraceae plant scientific name: Gnaphalium semiamplexicaule extract was removed, it was prepared in the same manner as in Example 1 and used in the test.
[0029]
[Example 2] (Whitening emulsion)
In the blending amount described below, the component A is heated and mixed and kept at 70 ° C. Next, the component B is heated and mixed and maintained at 70 ° C. The B component was uniformly mixed with the A component, and then the C component was injected, mixed with stirring, and then cooled to 30 ° C. with stirring to obtain a whitening emulsion.
(composition)
Compounding ingredients Compounding amount (wt%)
(A) 1,3-butylene glycol 5.0
Ethyl alcohol 5.0
Asteraceae plant scientific name: Gnaphalium semiamplexicaule extract (Extraction Example 1) 2.0
Purified water remaining (B) Squalane 5.0
Vaseline 2.0
Beeswax 0.5
Sorbitan sesquioleate ester 0.8
Polyoxyethylene oleyl ether (20E.O.) 1.2
Preservative appropriate amount Fragrance proper amount
(C) Carboxyvinyl polymer (1.0% aqueous solution) 20.0
Potassium hydroxide 0.1
[0030]
[Comparative Example 2] (Whitening emulsion)
In Example 2, except that the component (B) Asteraceae plant scientific name: Gnaphalium semiamplexicaule extract was removed, it was prepared in the same manner as in Example 2 and used in the test.
[0031]
[Test Example 2] (Use effect test)
The test by use test was done about the whitening effect of the cream and the whitening emulsion prepared in Examples 1 and 2 and Comparative Examples 1 and 2. The use test was carried out by using 20 women each 25 to 40 years old as a panel, and applying test cream or whitening milk on the face for 2 weeks after washing the face twice daily in the morning and night. The evaluation criteria for the whitening effect are as follows: “Effective” when the freckles are almost inconspicuous, “Slightly effective” when the freckles are less noticeable, and “Invalid” when the freckles are not noticeable. Went.
As shown in Table 2 (Table 2), better results were obtained in Examples 1 and 2 than in Comparative Examples 1 and 2.
[0032]
[Table 2]

[0033]
【The invention's effect】
The tyrosinase activity inhibitor of the present invention and cosmetics, pharmaceuticals, quasi drugs, foods and other compositions containing the same have an effect of suppressing the production of melanin in vivo. Therefore, it is effective for treating health and cosmetic disorders.

Claims (1)

 A tyrosinase activity inhibitor characterized by containing an extract of the scientific name Gnaphalium semiamplexicaule which is a plant native to Mexico.