JP2813695B2 - Anti-aging agent for skin and skin cosmetic containing the same - Google Patents
Anti-aging agent for skin and skin cosmetic containing the sameInfo
- Publication number
- JP2813695B2 JP2813695B2 JP18676390A JP18676390A JP2813695B2 JP 2813695 B2 JP2813695 B2 JP 2813695B2 JP 18676390 A JP18676390 A JP 18676390A JP 18676390 A JP18676390 A JP 18676390A JP 2813695 B2 JP2813695 B2 JP 2813695B2
- Authority
- JP
- Japan
- Prior art keywords
- skin
- compound
- aging
- present
- aging agent
- 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 - Lifetime
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Description
【発明の詳細な説明】 〔産業上の利用分野〕 本発明は、皮膚の柔軟性を向上させ、皮膚の老化防止
効果（血流促進効果，皮膚柔軟化効果，皮膚の弾力性及
び平滑性の改善効果，しわの改善効果）に優れた皮膚化
粧料に関する。DETAILED DESCRIPTION OF THE INVENTION [Industrial Application Field] The present invention improves skin softness and prevents skin aging (blood flow promoting effect, skin softening effect, skin elasticity and smoothness). Skin cosmetics excellent in the effect of improving skin and wrinkles).
〔従来の技術〕 老化した皮膚は、皮膚表面が乾燥し、荒れ肌様の状態
になるが、これは角質層の水分保持機能の低下やバリヤ
ー機能の低下、更に皮脂分泌量の低下等に起因すると考
えられている。また、表皮，真皮ともに細胞数の減少を
伴い、代謝機能の低下が生じる。更に、表皮の酸化還元
関連の酵素活性や皮膚の酸素分圧が低下し、角質層のタ
ーンオーバ速度が低下することが知られている。[Prior art] Aged skin, the skin surface becomes dry and rough skin-like, but this is caused by a decrease in the moisture retention function and barrier function of the stratum corneum, a decrease in sebum secretion, etc. It is considered. In addition, the number of cells in both the epidermis and the dermis is reduced, and the metabolic function is reduced. Furthermore, it is known that the activity of redox-related enzymes in the epidermis and the oxygen partial pressure of the skin decrease, and the turnover speed of the stratum corneum decreases.
一方、皮膚の大部分の構造を形成する成分として、コ
ラーゲンとエラスチンがあり、皮膚の弾力性と柔軟性を
左右していると言われている。加齢によりこれらの成分
の可溶性分画が減少し、架橋結合が形成され弾力性と柔
軟性が低下すると考えられている。更に、加齢によりコ
ラーゲンの代謝が低下すると共に、皮膚の細胞間物質で
あるヒアルロン酸が顕著に減少し、皮膚の水分量の低下
を招く。その結果、老化皮膚は全体的に萎縮して菲薄化
した状態になり、柔軟性，弾力性や滑かさを失い、荒れ
た肌となる。On the other hand, collagen and elastin are components that form most of the structure of the skin, and are said to affect the elasticity and flexibility of the skin. It is believed that the aging decreases the soluble fraction of these components, forming cross-links and reducing elasticity and flexibility. Furthermore, the metabolism of collagen decreases with aging, and hyaluronic acid, which is an intercellular substance of the skin, is remarkably reduced, leading to a decrease in the water content of the skin. As a result, the aging skin becomes atrophied and thinned as a whole, loses flexibility, elasticity and lubricity, and becomes rough skin.
このような老化した皮膚の改善剤として、コラーゲン
やヒアルロン酸を配合した化粧料が数多く提案されてい
るが、表面の保湿効果が改善されるだけであり、本質的
に老化肌を改善するものではない。その他、皮膚細胞賦
活剤としてビタミン類や生薬類が使用されているが、や
はり老化肌の治療にまでは至っていないのが現状であ
る。Numerous cosmetics containing collagen or hyaluronic acid have been proposed as an agent for improving such aged skin, but only those that improve the moisturizing effect on the surface and do not essentially improve aging skin. Absent. In addition, vitamins and herbal medicines are used as skin cell activators, but at present the treatment of aging skin has not yet been achieved.
従って本発明の目的は、コラーゲンの代謝を促進し、
皮膚の線維化を解消することにより、本質的に老化肌を
改善する皮膚老化防止剤，及びそれを含有する皮膚化粧
料を提供することにある。Therefore, an object of the present invention is to promote collagen metabolism,
An object of the present invention is to provide a skin aging inhibitor which essentially improves aging skin by eliminating fibrosis of the skin, and a skin cosmetic containing the same.
本発明は、 （１） 下記一般式（Ｉ）： で表される化合物から成る皮膚老化防止剤。The present invention provides: (1) the following general formula (I): A skin aging inhibitor comprising a compound represented by the formula:
（２） 化合物（Ｉ）がＮ−メチル−Ｌ−セリンである
請求項（１）記載の皮膚老化防止剤 （３） 化合物（Ｉ）を含有することを特徴とする皮膚
化粧料 （４） 化合物（Ｉ）がＮ−メチル−Ｌ−セリンである
請求項（３）記載の皮膚化粧料 である。(2) The skin aging inhibitor according to (1), wherein the compound (I) is N-methyl-L-serine. (3) A skin cosmetic comprising the compound (I). The skin cosmetic according to claim 3, wherein (I) is N-methyl-L-serine.
一般式（Ｉ）で表される本発明の皮膚老化防止剤は、
例えばＮ−メチル−Ｌ−セリンおよびＮ−メチル−DL−
セリンを挙げることができる。The skin anti-aging agent of the present invention represented by the general formula (I)
For example, N-methyl-L-serine and N-methyl-DL-
Serine can be mentioned.
本発明に用いられる化合物（Ｉ）の含有量は、本発明
の皮膚化粧料の全重量に対して好ましくは0.001〜10.0
重量％（以下wt％と略記する）、等に好ましくは0.01〜
5.0wt％である。0.001wt％より少ないと効果は十分でな
く、10.0wt％を越えてもの増量分に見合った効果は期待
できない。The content of the compound (I) used in the present invention is preferably 0.001 to 10.0 with respect to the total weight of the skin cosmetic of the present invention.
Wt% (hereinafter abbreviated as wt%), preferably 0.01 to
5.0 wt%. If the amount is less than 0.001% by weight, the effect is not sufficient, and if it exceeds 10.0% by weight, the effect corresponding to the increased amount cannot be expected.
本発明の皮膚老化防止剤は、皮膚化粧料等に適用する
ことが可能である。The anti-aging agent for skin of the present invention can be applied to skin cosmetics and the like.
本発明の皮膚化粧料は、常法に従って、ローション
類，乳液類，クリーム類，軟膏類，パック類等の剤型に
することが可能である。The skin cosmetic of the present invention can be made into dosage forms such as lotions, emulsions, creams, ointments, packs and the like according to a conventional method.
また、本発明の皮膚化粧料には、界面活性剤，殺菌
剤，防腐剤，角質溶解剤，抗酸化剤，香料，色素等を本
発明の目的を達成する範囲内で適宜配合することができ
る。Further, the skin cosmetic of the present invention may appropriately contain a surfactant, a bactericide, a preservative, a keratolytic agent, an antioxidant, a fragrance, a pigment and the like within a range that achieves the object of the present invention. .
〔作用〕 本発明者らは既に、化合物（Ｉ）が皮膚中のプロコラ
ゲナーゼの産生を促進することを見出している（特願平
２−99579）。[Action] The present inventors have already found that compound (I) promotes the production of procollagenase in skin (Japanese Patent Application No. 2-99579).
プロコラゲナーゼは生体内においてプラスミンやスト
ロメライシン等の蛋白分解酵素によってコラゲナーゼに
活性化される（The Biochemioal Journal 166巻21〜31
頁 1977年，及びProceedings of the National Academ
y of Sciences of the U.S.A. 86巻2632頁,1989年参
照）。そしてこのコラーゲナーゼが異常蓄積したオラー
ゲンを分解し、皮膚の線維化を防止する。Procollagenase is activated into collagenase in vivo by proteolytic enzymes such as plasmin and stromelysin (The Biochemioal Journal 166, 21-31).
Page 1977, and Proceedings of the National Academ
y of Sciences of the USA 86: 2632, 1989). Then, the collagenase degrades the abnormally accumulated oragen to prevent skin fibrosis.
本発明の皮膚老化防止剤及び皮膚化粧料は、上述した
作用に基づき、皮膚の線維化を防止し、皮膚の柔軟化を
促進し、老化肌を本質的に改善するものと考えられる。The anti-aging agent and skin cosmetic of the present invention are considered to prevent skin fibrosis, promote skin softening, and essentially improve aging skin, based on the above-mentioned effects.
以下、実施例及び比較例に基づいて本発明を詳説す
る。尚、実施例に記載の皮膚血流量試験法，皮膚粘弾性
試験法，美肌効果試験法を下記に示す。Hereinafter, the present invention will be described in detail based on Examples and Comparative Examples. The skin blood flow test, skin viscoelasticity test and skin effect test described in the examples are shown below.
（１） 皮膚血流量試験法 ニュージーランドホワイト系家兎３羽の腹部を刈毛
し、18時間絶食させた後、ペンタバリビトールのナトリ
ウム塩を35mg/kgの割合で静脈注射し麻酔処置する。家
兎の背部を固定し、腹部試験部位中、３×2cm2の部分２
ケ所に、化合物（Ｉ）配合試料及び無配合試料を各々0.
1g均一に塗布し、プレートタイプトランスジューサーを
腹部の試料塗布部位上にセロファンテープでとめ、交叉
熱電堆式皮膚血流計（シンエイ社製シンコーダー,201
型）を用いて試料塗布一定時間後（0.5,1.0,2.0時間
後）の皮膚血流量（μＶ）を測定する。(1) Skin blood flow test method The abdomen of three New Zealand white rabbits was shaved, fasted for 18 hours, and then anesthetized by intravenous injection of sodium pentavaribitol at a rate of 35 mg / kg. Fix the back of the rabbit, 3 x 2 cm 2 part 2 in the abdominal test site
In each of the places, the compound (I) -containing sample and the non-compound
Apply 1 g uniformly, place the plate-type transducer on the abdominal sample application site with cellophane tape, and use a cross thermoelectric type skin blood flow meter (Shinei Co., 201
), The skin blood flow (μV) is measured after a certain time (0.5, 1.0, 2.0 hours) after application of the sample.
化合物（Ｉ）配合試料を塗布した場合の血流量をＣA,
無配合試料の場合の血流量をCBとし、CA/CBを算出し
た。１羽については、３回（0.5,1.0,2.0時間）の値を
平均し、更に３羽の平均を求め、皮膚血流量増加率とし
た。The blood flow rate when the compound (I) -containing sample was applied was C A,
The blood flow in the case of non-blended sample and C B, was calculated C A / C B. For one bird, the values of three times (0.5, 1.0, 2.0 hours) were averaged, and the average of the three birds was determined to obtain the skin blood flow increase rate.
（２） 皮膚粘弾性試験法 局方記載の吸水軟膏に実施例及び比較例で示される各
種試料を５重量％の濃度で配合し、試料クリームを作製
した。（尚、無配合のものをコントロールとして用い
た。）。(2) Skin viscoelasticity test method Various samples shown in Examples and Comparative Examples were mixed at a concentration of 5% by weight with a water-absorbing ointment described in the Pharmacopoeia to prepare a sample cream. (Note that a non-blended one was used as a control.)
次に、ウィスター系ヘアレスラット（６週齢，オス,1
群５匹）の背部を毛刈りし、右肩の２×2cmの部位に、
連日試料クリームを0.1g塗布した。Next, Wistar hairless rats (6 weeks old, male, 1
Shaving the back of a group of 5), on the 2 × 2 cm site on the right shoulder,
Every day, 0.1 g of the sample cream was applied.
試験開始後45日目に、特開昭59−120130号公報記載の
振動式の皮膚弾性率測定器を用いて皮膚粘弾性値を測定
した。On the 45th day after the start of the test, the skin viscoelasticity value was measured using a vibration-type skin elastic modulus meter described in JP-A-59-120130.
尚、同測定器により表示される皮膚粘弾性値（任意単
位）は、皮膚が柔らかい程高い値を示す。In addition, the skin viscoelasticity value (arbitrary unit) displayed by the measuring device indicates a higher value as the skin is softer.
化合物（Ｉ）配合クリーム塗布群の皮膚粘弾性の平均
値を（Ｓ），化合物（Ｉ）無配合クリーム塗布群の皮膚
粘弾性の平均値（Ｃ）を求め、（Ｓ）／（Ｃ）を算出し
て、皮膚粘弾性を評価した。The average value of the skin viscoelasticity of the group coated with the compound (I) -containing cream was determined as (S), and the average value of the skin viscoelasticity of the group coated with the compound (I) -free cream (C) was determined. Calculated to evaluate skin viscoelasticity.
（３） 美肌効果試験（実用テスト） 荒れ肌，小皺，乾燥肌等を訴える女子被験者（35〜55
才）20人に試料を１日２回（朝・夕）連続３ケ月使用さ
せた後、皮膚の柔軟性，弾力性，しわの改善について評
価させた。結果は、各項目に対して、「皮膚の柔軟性が
向上した」「皮膚の弾力性が向上した」「皮膚のしわが
改善した」と回答した人数で示した。(3) Beautiful skin effect test (practical test) Female subjects complaining of rough skin, fine wrinkles, dry skin, etc. (35-55
20 years old) The sample was used twice daily (morning / evening) for three consecutive months, and then evaluated for improvement in skin softness, elasticity, and wrinkles. The results were shown by the number of respondents who answered, "Improved skin flexibility", "Improved skin elasticity", and "Improved skin wrinkles" for each item.
実施例１〜３比較例１〜４ ［スキンミルク］ （１） 組成 （２） 調製法 （Ａ）成分を撹拌下に均一に混合した後、75℃で５分
間、加熱撹拌して均一に溶解した。次に（Ｂ）成分を
（Ｃ）成分中に均一に溶解せしめた後、（Ａ）成分中に
添加し、均一に混合撹拌分散し、30℃まで冷却する、使
用時には内容物を均一に振盪分散して使用する。Examples 1-3 Comparative Examples 1-4 [Skin Milk] (1) Composition (2) Preparation method After uniformly mixing the component (A) with stirring, the mixture was heated and stirred at 75 ° C for 5 minutes to be uniformly dissolved. Next, after the component (B) is uniformly dissolved in the component (C), the mixture is added to the component (A), and the mixture is uniformly mixed, stirred and dispersed, and cooled to 30 ° C. Use distributed.
（３） 特性 各スキンミルクの諸試験を実施した結果を第１表に記
載した。(3) Characteristics Table 1 shows the results of various tests performed on each skin milk.
この表からわかる通り、比較例１〜２のスキンミルク
と比較して、化合物（Ｉ）を含有した実施例１〜３の本
発明の皮膚化粧料は、諸試験の全てに亘って良好なる結
果を示した。 As can be seen from this table, the skin cosmetics of the present invention of Examples 1 to 3 containing the compound (I) showed better results over all the tests than the skin milks of Comparative Examples 1 and 2. showed that.
実施例４〜6,比較例５〜８ ［スキンクリーム］ 実施例１〜３と同様に、下記の組成に於いて各々のス
キンクリームを調製して諸試験を実施し、その結果を第
２表に示した。Examples 4 to 6, Comparative Examples 5 to 8 [Skin cream] In the same manner as in Examples 1 to 3, each skin cream was prepared with the following composition, and various tests were carried out. It was shown to.
（１） 組成 （２） 調製法 （Ｂ）成分を（Ｃ）成分中に均一に溶解してから、80
℃に加熱する。一方（Ａ）成分を80℃に加熱溶解してか
ら、（Ａ）成分中に（Ｃ）成分を注入撹拌混合する。次
いで、撹拌しながら温度30℃迄冷却する。(1) Composition (2) Preparation method After the component (B) is uniformly dissolved in the component (C),
Heat to ° C. On the other hand, the component (A) is heated and dissolved at 80 ° C., and then the component (C) is poured into the component (A), followed by stirring and mixing. Then cool to a temperature of 30 ° C. with stirring.
（３） 特性 各スキンクリームの諸試験を実施した結果を第２表に
記載した。(3) Characteristics Table 2 shows the results of various tests performed on each skin cream.
この表からかる通り、比較例５〜６のスキンクリーム
と比較して、化合物（Ｉ）を含有した実施例４〜６の本
発明の皮膚化粧料は諸試験の全てに亘って良好なる結果
を示した。 As can be seen from this table, compared with the skin creams of Comparative Examples 5 and 6, the skin cosmetics of the present invention of Examples 4 and 6 containing the compound (I) showed good results over all of the tests. Indicated.
以上記載の如く、本発明の皮膚老化防止剤及び皮膚化
粧料が、皮膚の柔軟性及び弾力性を向上させ、皮膚の老
化を防止することは明らかである。As described above, it is clear that the skin anti-aging agent and the skin cosmetic composition of the present invention improve skin softness and elasticity and prevent skin aging.
───────────────────────────────────────────────────── フロントページの続き (56)参考文献 特公 平５−79645（ＪＰ，Ｂ２) フレグランスジャーナル Ｎｏ．22 （Ｖｏｌ．５，Ｎｏ．１） （1977） Ｐ．６〜Ｐ．14 (58)調査した分野(Int.Cl.6，ＤＢ名) A61K 7/00 - 7/50──────────────────────────────────────────────────続 き Continuation of the front page (56) References JP-B 5-79645 (JP, B2) Fragrance Journal No. 22 (Vol. 5, No. 1) (1977) 6-P. 14 (58) Field surveyed (Int. Cl. 6 , DB name) A61K 7/00-7/50
Claims (4)
ある請求項１記載の皮膚老化防止剤。2. The antiaging agent according to claim 1, wherein the compound (I) is N-methyl-L-serine.
とを特徴とする皮膚化粧料。3. A skin cosmetic comprising the compound (I) according to claim 1.
ある請求項３記載の皮膚化粧料。4. The skin cosmetic according to claim 3, wherein the compound (I) is N-methyl-L-serine.
Priority Applications (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP18676390A JP2813695B2 (en) | 1990-07-13 | 1990-07-13 | Anti-aging agent for skin and skin cosmetic containing the same |
| PCT/JP1991/000937 WO1992000733A1 (en) | 1990-07-13 | 1991-07-12 | Collagen metabolism ameliorant and its use |
| DE69110861T DE69110861T2 (en) | 1990-07-13 | 1991-07-12 | AGENTS FOR IMPROVING AND USING COLLAGEN METABOLISM. |
| EP91912371A EP0506965B1 (en) | 1990-07-13 | 1991-07-12 | Collagen metabolism ameliorant and its use |
| US08/004,107 US5332758A (en) | 1990-07-13 | 1993-01-13 | Collagen metabolism ameliorant and its use |
| US08/229,724 US5565493A (en) | 1990-07-13 | 1994-04-19 | Collagen metabolism ameliorant and its use in the stimulation of hair growth |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP18676390A JP2813695B2 (en) | 1990-07-13 | 1990-07-13 | Anti-aging agent for skin and skin cosmetic containing the same |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPH0474106A JPH0474106A (en) | 1992-03-09 |
| JP2813695B2 true JP2813695B2 (en) | 1998-10-22 |
Family
ID=16194210
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP18676390A Expired - Lifetime JP2813695B2 (en) | 1990-07-13 | 1990-07-13 | Anti-aging agent for skin and skin cosmetic containing the same |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JP2813695B2 (en) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2000095641A (en) * | 1998-09-25 | 2000-04-04 | Kanebo Ltd | Bleaching preparation |
-
1990
- 1990-07-13 JP JP18676390A patent/JP2813695B2/en not_active Expired - Lifetime
Non-Patent Citations (1)
| Title |
|---|
| フレグランスジャーナル Ｎｏ．２２ （Ｖｏｌ．５，Ｎｏ．１） （１９７７） Ｐ．６〜Ｐ．１４ |
Also Published As
| Publication number | Publication date |
|---|---|
| JPH0474106A (en) | 1992-03-09 |
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