JP3792745B2 - Tyrosinase inhibitor - Google Patents

Tyrosinase inhibitor Download PDF

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Publication number
JP3792745B2
JP3792745B2 JP06716995A JP6716995A JP3792745B2 JP 3792745 B2 JP3792745 B2 JP 3792745B2 JP 06716995 A JP06716995 A JP 06716995A JP 6716995 A JP6716995 A JP 6716995A JP 3792745 B2 JP3792745 B2 JP 3792745B2
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JP
Japan
Prior art keywords
chestnut
tyrosinase
tyrosinase inhibitor
ethanol
extract
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
JP06716995A
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Japanese (ja)
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JPH08217687A (en
Inventor
肇 下村
ゆり 三田
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Mikimoto Pharmaceutical Co Ltd
Original Assignee
Mikimoto Pharmaceutical Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Mikimoto Pharmaceutical Co Ltd filed Critical Mikimoto Pharmaceutical Co Ltd
Priority to JP06716995A priority Critical patent/JP3792745B2/en
Publication of JPH08217687A publication Critical patent/JPH08217687A/en
Application granted granted Critical
Publication of JP3792745B2 publication Critical patent/JP3792745B2/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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  • Cosmetics (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Medicinal Preparation (AREA)

Description

【0001】
【産業上の利用分野】
本発明は他の目的の医薬品等として多年内用され、安全性が保証された植物の抽出物を用いて、チロシナーゼの活性を抑制して、皮膚の美白に有効なチロシナーゼ阻害剤に関する。
【0002】
【従来の技術】
栗は北海道西南部から九州及び朝鮮半島に分布する落葉高木で堅実は広く食用とされ、その葉は栗葉と、またそのいがは栗毛毬と呼ばれ、うるしかぶれ、あせも、やけどなどに外用される。
【0003】
【発明が解決しようとする課題】
本発明の目的は、皮膚に適用して安全であると共に、チロシナーゼ阻害作用が強い原料を提供することである。
チロシナーゼは、皮膚に存在する酵素で、その働きはチロシンからメラニンを生成し、皮膚の色を黒色化する。古くより色の白いのは七難隠すといわれ、多くの女性の願望であった。
【0004】
【課題を解決する手段】
本発明者らは、前記の課題を解決するため、すでに多年にわたって食用に供され、人体に対する安全性が確認されている植物をスクリーニングして調べ、チロシナーゼ阻害剤として利用価値のあるものを検討した。
その結果、栗の葉、栗のいがが非常にチロシナーゼ阻害作用が強い原料であることを見出した。
【0005】
すなわち、本発明は、栗の葉、栗のいがの溶媒抽出物を含むチロシナーゼ阻害剤である。
【0006】
栗の葉、栗のいがの利用方法としては、水或いは親水性有機溶媒例えば、エタノール、メタノール、アセトン等で抽出する。しかしながら、化粧品原料の抽出であるから、水或いはエタノール或いはこれの混合溶媒での抽出が好ましいのは当然である。また、場合によっては、グリセリン、1,3ブチレングリコール、プロピレングリコール等の多価アルコール又は多価アルコールと水の混液も抽出に利用できる。またさらに凍結乾燥して粉体として利用することも利用方法によっては有効である。
【0007】
この物質を他の化粧品原料例えばスクワラン、ホホバ油等の液状油、ミツロウ、セチルアルコール等の固体油、各種の活性剤、グリセリン、1,3ブチレングリコール等の保湿剤や各種薬剤等を添加してさまざまな剤形の化粧料を調整することができる。例えばローション、クリーム、乳液、パック等で目的に応じて利用形態を考えればよい。
【0008】
【実施例】
以下に実際の利用方法である実施例を記載するが、本発明はこの実施例によって何ら限定されるものではない。
本発明で使用した栗の葉、栗のいがの抽出物の実施例を次に示す。
【0009】
実施例1
栗の葉10gに精製水300mlを加えて3時間加熱する。これを濾過後凍結乾燥した。
【0010】
実施例2
栗いが10gに精製水300mlを加えて3時間加熱する。これを濾過後凍結乾燥した。
【0011】
実施例3
栗いが30gにエタノール300mlを加えて時々撹拌しつつ5日間放置した。これをエバポレート濾過後凍結乾燥した。
【0012】
実施例4
栗いが(乾燥品)を10gに精製水300mlを加えて3時間加熱する。これを濾過後凍結乾燥した。
【0013】
実施例5 ローション
オリーブ油 0.5
実施例1による溶媒抽出物 0.5
ホリオキシエチレン(20E.0)ソルヒタンモノステアレート 2.0
ホリオキシエチレン(60E.0)硬化ヒマシ油 2.0
エタノール 10.0
1.0%ヒアルロン酸ナトリウム水溶液 5.0
精製水 80.0
【0014】
実施例6 クリーム
A スクワラン 20.0
オリーブ油 2.0
ミンク油 1.0
ホホバ油 5.0
ミツロウ 5.0
セトステアリルアルコール 2.0
グリセリンモノステアレート 1.0
ソルビタンモノステアレート 2.0
実施例2による溶媒抽出物 1.0
B 精製水 47.9
ホリオキシエチレン(20E.0)ソルヒタンモノステアレート 2.0
ホリオキシエチレン(60E.0)硬化ヒマシ油 1.0
グリセリン 5.0
1.0%ヒアルロン酸ナトリウム水溶液 5.0
パラオキシ安息香酸メチル 0.1
AとBをそれぞれ計量し、70℃まで加温し、BにAを撹拌しつつ徐々に加えたのち、ゆっくり撹拌しつつ30℃まで冷却した。
【0015】
実施例−7は実施例−5の実施例1の抽出物を実施例3の抽出物に変え作成したもの
【0016】
実施例−8は実施例−6の実施例2の抽出物を実施例4の抽出物に変え作成したもの
【0017】
チロシナーゼ活性阻害試験
(試験方法)
30mMリン酸緩衝液(pH6.8)0.9ml、1.66mMチロシン(Tyrosine)溶液1.0ml、前記実施例(凍結乾燥品)の0.1wt/v%水溶液(溶解しにくい場合はエタノールを加えて溶解したのち精製水を加えて、エバポレートし、エタノールを除去したのち、0.1wt/v%になるように調製した)1.0mlをスクリューバイアルにとり、37℃恒温水槽中で5分以上加温した。
チロシナーゼ溶液(Sigma社製、マッシユルーム由来、914ユニット/ml)0.1mlを加え、37℃恒温水槽中で保温し、10分後に475nmで吸光度を測定した。
対照として、上記試料液のかわりに純水を加え同様に測定した。
この試験では試料の終濃度は0.033%となる。
(計算式)

Figure 0003792745
【0018】
【表1】
Figure 0003792745
【0019】
使用テスト
女性6名づつの顔面を左右に分け、一方を実施例、もう一方を比較例として毎日、1回以上使用してもらって、3月後、アンケートした。なお、比較例は実施例5、6よりそれぞれ実施例1、2による溶媒抽出物を水にかえたものである。(比較例1,2)
なお、12名を2班にわけ、下記の試料を使って実験した。
Figure 0003792745
【0020】
判定基準は以下のようでアンケートの結果をまとめたのが以下の表である。
(なお、数値は判定結果の合計点で示した)
実施例の方が非常によい 3
実施例の方がかなりよい 2
実施例の方がややよい 1
差がない 0
比較例の方がややよい −1
比較例の方がかなりよい −2
比較例の方が非常によい −3
【0021】
Figure 0003792745
【0022】
【効果】
本発明の栗の葉、栗のいがの溶媒抽出物、或いはそれを配合したクリーム、ローション等のチロシナーゼ活性阻害剤は優れたチロシナーゼ活性阻害を示し、美白効果を有する。また、これらは長年にわたって利用されてきており、その安全性については保証されている。[0001]
[Industrial application fields]
The present invention relates to a tyrosinase inhibitor that is effective for whitening the skin by suppressing the activity of tyrosinase using a plant extract that has been used for many years as a medicinal product for other purposes and whose safety is guaranteed.
[0002]
[Prior art]
Chestnut is a deciduous tree that is distributed from southwestern Hokkaido to Kyushu and the Korean peninsula. Is done.
[0003]
[Problems to be solved by the invention]
An object of the present invention is to provide a raw material that is safe to apply to the skin and has a strong tyrosinase inhibitory action.
Tyrosinase is an enzyme present in the skin, and its function is to produce melanin from tyrosine and blacken the color of the skin. The older white color is said to conceal the seven difficulties and was the desire of many women.
[0004]
[Means for solving the problems]
In order to solve the above problems, the present inventors screened and examined plants that have been used for food for many years and have been confirmed to be safe for the human body, and examined those that are useful as tyrosinase inhibitors. .
As a result, it was found that chestnut leaves and chestnut potatoes are raw materials with a very strong tyrosinase inhibitory action.
[0005]
That is, the present invention is a tyrosinase inhibitor containing a solvent extract of chestnut leaves and chestnut ginger.
[0006]
As a method of using chestnut leaves and chestnut ginger, extraction is performed with water or a hydrophilic organic solvent such as ethanol, methanol, acetone or the like. However, since it is extraction of cosmetic raw materials, it is natural that extraction with water, ethanol, or a mixed solvent thereof is preferable. In some cases, polyhydric alcohols such as glycerin, 1,3 butylene glycol, propylene glycol, or a mixture of polyhydric alcohol and water can also be used for extraction. Furthermore, it is also effective to freeze-dry and use as powder depending on the method of use.
[0007]
This substance is added to other cosmetic raw materials such as liquid oils such as squalane and jojoba oil, solid oils such as beeswax and cetyl alcohol, various active agents, humectants such as glycerin and 1,3 butylene glycol, and various drugs. Various dosage forms of cosmetics can be adjusted. For example, the use form may be considered according to the purpose, such as lotion, cream, milky lotion, pack and the like.
[0008]
【Example】
Examples which are actual utilization methods will be described below, but the present invention is not limited to these examples.
Examples of chestnut leaves and chestnut garlic extracts used in the present invention are shown below.
[0009]
Example 1
Add 300 ml of purified water to 10 g of chestnut leaves and heat for 3 hours. This was filtered and freeze-dried.
[0010]
Example 2
Add 300 ml of purified water to 10 g of chestnuts and heat for 3 hours. This was filtered and freeze-dried.
[0011]
Example 3
The chestnut was added to 30 g of ethanol and 300 ml of ethanol, and allowed to stand for 5 days with occasional stirring. This was evaporated and then lyophilized.
[0012]
Example 4
Add 10 ml of chestnut ginger (dried product) to 300 g of purified water and heat for 3 hours. This was filtered and freeze-dried.
[0013]
Example 5 Lotion Olive Oil 0.5
Solvent extract according to Example 1 0.5
Polyoxyethylene (20E.0) sorbitan monostearate 2.0
Polyoxyethylene (60E.0) hydrogenated castor oil 2.0
Ethanol 10.0
1.0% sodium hyaluronate aqueous solution 5.0
Purified water 80.0
[0014]
Example 6 Cream A Squalane 20.0
Olive oil 2.0
Mink oil 1.0
Jojoba oil 5.0
Beeswax 5.0
Cetostearyl alcohol 2.0
Glycerol monostearate 1.0
Sorbitan monostearate 2.0
Solvent extract according to Example 2 1.0
B Purified water 47.9
Polyoxyethylene (20E.0) sorbitan monostearate 2.0
Polyoxyethylene (60E.0) hydrogenated castor oil 1.0
Glycerin 5.0
1.0% sodium hyaluronate aqueous solution 5.0
Methyl paraoxybenzoate 0.1
A and B were weighed and heated to 70 ° C., A was gradually added to B while stirring, and then cooled to 30 ° C. with slow stirring.
[0015]
Example-7 was prepared by replacing the extract of Example 1 of Example-5 with the extract of Example 3.
Example-8 was prepared by replacing the extract of Example 2 of Example-6 with the extract of Example 4.
Tyrosinase activity inhibition test (test method)
0.9 ml of 30 mM phosphate buffer (pH 6.8), 1.0 ml of 1.66 mM tyrosine solution, and 0.1 wt / v% aqueous solution of the above-mentioned example (lyophilized product) (if it is difficult to dissolve, ethanol is used. After adding and dissolving, purified water was added, evaporated, ethanol was removed, and adjusted to 0.1 wt / v%) 1.0 ml was taken in a screw vial and kept in a 37 ° C constant temperature bath for 5 minutes or longer Warmed up.
0.1 ml of tyrosinase solution (manufactured by Sigma, derived from Massy Room, 914 units / ml) was added, and the mixture was kept warm in a constant temperature water bath at 37 ° C., and the absorbance was measured at 475 nm after 10 minutes.
As a control, pure water was added instead of the sample solution, and the same measurement was performed.
In this test, the final concentration of the sample is 0.033%.
(a formula)
Figure 0003792745
[0018]
[Table 1]
Figure 0003792745
[0019]
Use test 6 female faces were divided into left and right sides, and one was used as an example and the other was used as a comparative example. In the comparative example, the solvent extracts according to Examples 1 and 2 were replaced with water from Examples 5 and 6, respectively. (Comparative Examples 1 and 2)
In addition, 12 people were divided into 2 groups, and the following samples were used for experiments.
Figure 0003792745
[0020]
The criteria are as follows, and the results of the questionnaire are summarized in the following table.
(The numerical value is indicated by the total score of the judgment results)
The example is much better 3
The example is much better 2
Example is slightly better 1
No difference 0
Comparative example is slightly better -1
The comparative example is much better -2
The comparative example is much better -3
[0021]
Figure 0003792745
[0022]
【effect】
The tyrosinase activity inhibitors such as chestnut leaf, chestnut garlic solvent extract of the present invention, or creams and lotions containing the same exhibit excellent tyrosinase activity inhibition and have a whitening effect. In addition, they have been used for many years and their safety is guaranteed.

Claims (1)

栗の葉及び/又は栗のいがの溶媒抽出物を有効成分として含有してなるチロシナーゼ阻害剤  Tyrosinase inhibitor comprising a chestnut leaf and / or chestnut ginger solvent extract as an active ingredient
JP06716995A 1995-02-15 1995-02-15 Tyrosinase inhibitor Expired - Fee Related JP3792745B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP06716995A JP3792745B2 (en) 1995-02-15 1995-02-15 Tyrosinase inhibitor

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP06716995A JP3792745B2 (en) 1995-02-15 1995-02-15 Tyrosinase inhibitor

Publications (2)

Publication Number Publication Date
JPH08217687A JPH08217687A (en) 1996-08-27
JP3792745B2 true JP3792745B2 (en) 2006-07-05

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Country Status (1)

Country Link
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Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20130008081A (en) 2004-02-13 2013-01-21 바스프 뷰티 케어 솔루션즈 프랑스 에스에이에스 Cosmetic composition comprising an extract of the leaves of castanea sativa
JP3747223B2 (en) * 2004-06-14 2006-02-22 三栄製薬株式会社 Active oxygen scavenger
WO2010147441A2 (en) * 2009-06-18 2010-12-23 (주)아모레퍼시픽 Cosmetic composition comprising chestnut shell extract
KR101304677B1 (en) * 2012-05-08 2013-09-06 신유현 A chestnut bur extracts and a cosmetic composition containing the chestnut bur extracts as an active ingredient

Also Published As

Publication number Publication date
JPH08217687A (en) 1996-08-27

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