JP3667376B2 - Hyaluronidase inhibitor - Google Patents

Description

【００２３】
【表２】

【００２４】
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６、７よりそれぞれ実施例１、２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。

【００２５】
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。
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
【００２６】

【００２７】
【効果】
本発明の抽出物としての効果は、ヒアルロニダーゼの活性抑制作用である。ヒアルロニダーゼは、生体中に広く分布し、皮膚にも存在する酵素で、その名の通りヒアルロン酸を分解する。ヒアルロン酸はβ−Ｄ−Ｎ−アセチルグルコサミンとβ−Ｄ−グルクロン酸が交互に結合した直鎖状の高分子多糖で、コンドロイチン硫酸などとともに噛乳動物の結合組織に広く存在するグリコサミノグルカンの一種である。
結合組織内でのヒアルロン酸の機能として、細胞間隙に水を保持し、また組織内にジェリー状のマトリックスを形成して細胞を保持したり、皮膚の潤滑性と柔軟性を保ち、外力（機械的障害）および細菌感染を防止していると考えられている。皮膚のヒアルロン酸は齢をとるにつれて減少し、その結果小ジワやかさつきなどの老化をもたらすといわれている。
従って、これを分解するヒアルロニダーゼの活性を抑制することは、製剤に使用されているヒアルロン酸の安定性や、皮膚に塗布した後の製剤のヒアルロン酸及び皮膚に存在していたヒアルロン酸の安定に寄与すると考えられる。また、ヒアルロニダーゼは炎症酵素としても知られ、活性抑制することは炎症を抑え、また、アレルギーにも抑制的に働くことが知られている。[0001]
[Industrial application fields]
The present invention is a hyaluronidase activity that degrades hyaluronic acid that keeps the lubricity and flexibility of the skin and prevents aging, using a plant extract that has been used for many years as a medicinal product for other purposes and whose safety is guaranteed. The present invention relates to a hyaluronidase inhibitor that suppresses skin wrinkles and roughness.
[0002]
[Prior art]
Chestnut is a deciduous tree that is distributed from southwestern Hokkaido to Kyushu and the Korean peninsula. Is done.
Sputum is said to be native to central and southern China, and widely distributed in the west of Kanto in Japan.
Japanese Patent Application Laid-Open No. 62-67028 discloses cell activation and damage healing.
[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 hyaluronidase inhibitory action.
[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 hyaluronidase inhibitors. .
As a result, it was found that chestnut leaves, chestnuts and persimmon leaves are raw materials with a very strong hyaluronidase inhibitory action.
[0005]
That is, the present invention is a hyaluronidase inhibitor containing a solvent extract of chestnut leaves, chestnuts, and bamboo leaves.
[0006]
As a method of using chestnut leaves, chestnuts, and bamboo leaves, 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]
Hyaluronidase is an enzyme that is widely distributed in the living body and is also present in the skin. As its name suggests, it degrades hyaluronic acid. Hyaluronic acid is a linear macromolecular polysaccharide in which β-D-N-acetylglucosamine and β-D-glucuronic acid are alternately bound, and is a glycosaminoglucan widely present in connective tissues of mammals together with chondroitin sulfate. It is a kind.
As a function of hyaluronic acid in connective tissue, water is retained in the cell gap, and cells are retained by forming a jelly-like matrix in the tissue, and the lubricity and flexibility of the skin are maintained. ) And bacterial infections. It is said that hyaluronic acid in the skin decreases with age, resulting in aging such as fine wrinkles and bulkiness.
[0009]
Therefore, suppressing the activity of the hyaluronidase that degrades the hyaluronic acid used in the formulation and the stability of the hyaluronic acid in the formulation after application to the skin and the hyaluronic acid present in the skin. It is thought to contribute.
Hyaluronidase is also known as an inflammatory enzyme. It is known that suppressing the activity suppresses inflammation and suppresses allergies.
[0010]
【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.
[0011]
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.
[0012]
Example 2
Add 300 ml of purified water to 10 g of chestnuts and heat for 3 hours. This was filtered and freeze-dried.
[0013]
Example 3
Chestnuts were added to 300 g of ethanol and left for 5 days with occasional stirring. This was evaporated, filtered and lyophilized.
[0014]
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.
[0015]
Example 5
300 g of distilled liquor (alcohol 35%) was added to 10 g of koji leaves and allowed to stand for 5 days with occasional stirring. This was evaporated, filtered and lyophilized.
[0016]
Example 6 Lotion Olive Oil 0.5
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
[0017]
Example 7 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
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.
[0018]
Example-8 was prepared by replacing the extract of Example 1 of Example-6 with the extract of Example 3.
Example-9 was prepared by replacing the extract of Example 2 of Example-7 with the extract of Example 4.
Example-10 was prepared by replacing the extract of Example 1 of Example-6 with the extract of Example 5.
(Hyaluronidase activity inhibition test)
(Test method)
6 g of 0.4% sodium hyaluronate 0.1 M (pH 6.0) phosphate buffer solution is weighed and left in a constant temperature water bath at 37 ° C. for 5 minutes, and then 0.1 wt / v% of the above-mentioned example (lyophilized product). Add 1.0 ml of an aqueous solution (if it is difficult to dissolve, add ethanol to dissolve, then add purified water, evaporate, remove ethanol, and adjust to 0.1 wt / v%) and stir. 1. Ostwald viscometer in which 1 ml of 0.1% hyaluronidase (manufactured by Sigma Co., Ltd., Ushizukumaru, type IS) 0.1M (pH 6.0) phosphate buffer solution was added and stirred immediately, and 6 was placed in a constant temperature bath at 37 ° C. Put in.
The viscosity was measured after 1 minute, 5 minutes, 10 minutes, 20 minutes and 40 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 0.0125%.
The results are shown in Tables 1 to 7 as indices, with the viscosity after 1 minute as 100.
[0022]
[Table 1]

[0023]
[Table 2]

[0024]
Use test 6 females were divided into left and right faces, and one was used as an example and the other was used as a comparative example. In the comparative example, Examples 1 and 2 were replaced with water from Examples 6 and 7, respectively. (Comparative Examples 1 and 2) Twelve persons were divided into two groups, and experiments were performed using the following samples.

[0025]
The criteria are as follows, and the results of the questionnaire are summarized in the following table.
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
[0026]

[0027]
【effect】
The effect as the extract of the present invention is the activity suppression action of hyaluronidase. Hyaluronidase is an enzyme that is widely distributed in the living body and is also present in the skin. As its name suggests, it degrades hyaluronic acid. Hyaluronic acid is a linear macromolecular polysaccharide in which β-D-N-acetylglucosamine and β-D-glucuronic acid are alternately bound, and is a glycosaminoglucan widely present in connective tissues of mammals together with chondroitin sulfate and the like It is a kind of.
As a function of hyaluronic acid in connective tissue, water is retained in the cell gap, and cells are retained by forming a jelly-like matrix in the tissue, and the lubricity and flexibility of the skin are maintained. ) And bacterial infections. It is said that hyaluronic acid in the skin decreases with age, resulting in aging such as fine wrinkles and bulkiness.
Therefore, suppressing the activity of the hyaluronidase that degrades the hyaluronic acid used in the formulation and the stability of the hyaluronic acid in the formulation after application to the skin and the hyaluronic acid present in the skin. It is thought to contribute. Hyaluronidase is also known as an inflammatory enzyme. It is known that suppressing its activity suppresses inflammation and suppresses allergies.

Claims (1)

  Hyaluronidase inhibitor containing a chestnut leaf and chestnut garlic solvent extract