JP4959103B2 - Whitening agent and external preparation for skin - Google Patents
Whitening agent and external preparation for skin Download PDFInfo
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- JP4959103B2 JP4959103B2 JP2003191709A JP2003191709A JP4959103B2 JP 4959103 B2 JP4959103 B2 JP 4959103B2 JP 2003191709 A JP2003191709 A JP 2003191709A JP 2003191709 A JP2003191709 A JP 2003191709A JP 4959103 B2 JP4959103 B2 JP 4959103B2
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- 229910052725 zinc Inorganic materials 0.000 description 1
Description
【0001】
【発明の属する技術分野】
本発明は美白剤及び皮膚外用剤に関し、さらに詳細には、メラノサイトにおけるチロシナ−ゼの働きを阻害してメラニン産生を抑制し、紫外線照射後の皮膚に対する美白効果に優れ、また、日焼けなどによるシミ・ソバカス等を予防又は治療することが出来る美白剤及び皮膚外用剤に関する。
【0002】
【従来の技術、及び発明が解決しようとする課題】
シミ・ソバカスや日焼け後の皮膚色素沈着等は、皮膚内に存在する色素細胞の活性化によりメラニン産生が著しく亢進して生じるものであり、そのメカニズムについては必ずしも明確ではないが、チロシナ−ゼの働きによりチロシンからド−パ、ド−パからド−パキノンに変化したのち種々の中間体を経ることにより産生されるものと推測されている。このため、皮膚の黒色化を予防又は治療するためには、チロシナ−ゼの活性を阻害せしめ、また、メラニンを産生する過程の一部又は全部を阻害せしめる必要があるものである。
【0003】
ところで、従来より皮膚の黒色化を予防又は治療せしめるチロシナ−ゼ活性阻害剤やメラニン産生抑制剤としては、特開平6−256150号公報(特許文献1)、特開2002−128646号公報(特許文献2)等に開示されているように、アスコルビン酸、コウジ酸、アルブチン、あるいはハイドロキノン等が知られている。
しかしながら、上記アスコルビン酸は安定性に難があると共に、外用では効果が殆んど認められないものである。また、ハイドロキノンも物質自体の安定性(刺激性、アレルギ−性)に問題があるのみならず、白斑を生じさせるケ−スもある等の点から薬剤として配合することは問題があり、コウジ酸等についても安定性、安全性の面から必ずしも満足し得ないものである。
【0004】
【特許文献1】
特開平6−256150号公報
【特許文献2】
特開2002−128646号公報
【0005】
本発明は従来の問題点を解決し、優れた美白効果を有するのみならず、安定性・安全性に優れた美白剤及び皮膚外用剤を提供しようとするものである。
【0006】
【課題を解決するための手段】
本発明者は、皮膚の黒色化を予防・治療せしめるべく鋭意研究を行った結果、ピテセロビウムテニュクライブの抽出物が皮膚の黒色化を予防・治療する優れた効果を有するのみならず、安定性・安全性の面においても優れていることを知見し、本発明を完成するに至ったものである。
【0007】
即ち、本発明はピテセロビウムテニュクライブの抽出物を含有する美白剤及び皮膚外用剤を要旨とするものである。
【0008】
【発明の実施の形態】
本発明のピテセロビウムテニュクライブ(Pithecellobium tenue craib)は、マメ科(FABACEAE)に属する植物で、タイなど高温多湿で適度な降雨が認められる東南アジアで栽培されている。そして、かかるピテセロビウムテニュクライブの抽出物調製方法は特に限定されないが、生又は乾燥した樹皮を種々の溶媒を用い、低温から加温下において抽出する方法が挙げられる。具体的抽出媒体としては、水、メタノ−ル、エタノ−ル等の低級一価アルコ−ル、グリセリン、プロピレングリコ−ル、ジプロピレングリコ−ル、1,3−ブチレングリコ−ル等の液状多価アルコ−ル、酢酸エチル等の低級アルキルエステルを挙げることができ、これらの一種又は二種以上の混合溶媒を用いることが出来る。ピテセロビウムテニュクライブの抽出物は、そのまま用いてもよいが、必要に応じて濾過、濃縮してもよい。また、抽出物をカラムクロマト法、向流分配法等により、分画、精製して用いることも出来る。更に、上記の抽出物を減圧乾燥又は凍結乾燥した後、粉末又はペ−スト状に調製し、適宜製剤化して用いることも出来る。
【0009】
本発明の美白剤及び皮膚外用剤におけるピテセロビウムテニュクライブ抽出物の配合量は、特に限定はないが、効力、配合性、感触等の観点から乾燥固形物に換算して0.0001〜10.0重量%、好ましくは0.001〜5.0重量%,特に好ましくは0.01〜3.0重量%である。配合量が0.0001重量%未満では美白効果が乏しくなる傾向にあり、逆に10.0重量%を越えて配合しても効果の増加は実質上望めないし、皮膚外用剤への配合も難しくなる傾向にある。
【0010】
本発明の美白剤及び皮膚外用剤には、ピテセロビウムテニュクライブの抽出物の他、必要により本発明の効果を損なわない範囲内で通常化粧品、医薬部外品、医薬品等の皮膚外用剤に用いられる成分、例えば界面活性剤、油分、保湿剤、増粘剤、酸化防止剤、紫外線防御剤、アルコ−ル類、粉末成分、色剤、香料、水性成分、水、各種皮膚栄養剤等を必要に応じて適宜配合することが出来る。
さらに、金属イオン封鎖剤、防腐抗菌剤、細胞賦活剤、皮脂分泌調整剤、消炎剤、収斂剤、活性酸素抑制剤、抗アレルギ−剤、老化防止剤等、さらに生理活性作用を有する植物抽出物及びこれらの抽出分画、精製物等も適宜配合することが出来る。
【0011】
本発明における美白剤及び皮膚外用剤は、常法により製造することが出来る。また、本発明における美白剤及び皮膚外用剤は、一般皮膚化粧料に限定されるものではなく、医薬品、医療部外品、薬用化粧料等を包含するものである。本発明の美白剤及び皮膚外用剤の剤型は、可溶化系、乳化系、粉末分散系等何れでもよく、用途も化粧水、乳液、クリ−ム、パック等の基礎化粧料、ファンデ−ション等のメ−クアップ化粧料、シャンプ−、リンス、石けん、ボディ−シャンプ−等のトイレタリ−製品、浴用剤等を問わないものである。
【0012】
【実施例】
次に本発明の実施例を具体的に説明するが、本発明はこれらの実施例に限定されるものではない。なお、以下の実施例において重量%は単に%とする。
【0013】
製造例1 ピテセロビウムテニュクライブ抽出物
ピテセロビウムテニュクライブの樹皮粉砕物100gに50vol%エタノ−ル溶液1kgを加え、50℃にて8時間抽出した。これを濾過し、濾液を減圧下、濃縮乾固せしめた。乾固物を50%エタノ−ルに溶解した後、濾過してピテセロビウムテニュクライブ抽出物を得た。蒸発残留物は、0.48%であった。
【0014】
試験例1 チロシナ−ゼ活性阻害試験
上記により得られたピテセロビウムテニュクライブ抽出物を用い、精製水にて希釈し、1mg/mL、0.1mg/mL、0.05mg/mLの各濃度とした。10%FBS(牛胎児血清;日冷社製)及びテオフィリン(0.09mg/mL)含有MEM(ギブコ社商品名)を用い、マウス由来B16メラノ−マ培養細胞を96穴プレ−トに3×103cells/wellの密度で播種し、37℃、5%CO2にて24時間培養した後、試験試料の各濃度を添加し、37℃、5%CO2にてさらに3日間培養した。チロシナ−ゼ活性の測定前にウエル中の培地は除去し、PBS100μLで2回洗浄した。各ウエル中に45μLkl%トラインX(ロ−ム・アンド・ハウス社商品名)を含むPBSを加え、1分間プレ−トを振動させて細胞膜を破壊し、マイクロプレ−トリ−ダ−で波長475nmの吸光度を測定し、これを0分時の吸光度とした。その後、すばやく5μLの10mMのL−DOPA溶液を加えて、37℃にて60分間インキュベ−トした。1分間プレ−トを振動させた後、同様に吸光度を測定し、60分時の吸光度とした。そして、試験試料を添加していない(コントロ−ル)場合の0分時と60分時の吸光度差に対する試験試料の吸光度差の割合をチロシナ−ゼ活性阻害率とした。その結果を表1に示す。
【0015】
【表1】
【0016】
表1から明らかな通り、ピテセロビウムテニュクライブ抽出物は顕著なチロシナ−ゼ活性阻害作用を有することが理解出来る。
【0017】
試験例2 メラニン産生抑制試験
マウス由来B16メラノ−マ細胞を5%FBSを含むDMEM培地を用い、35mmのシャ−レに5×104cellずつ播種し、5%CO2にて37℃24時間培養した。24時間後、シャ−レの培地を除去し、5%FBSを含むDMEM培地2mLと各濃度に溶解した試験試料(ピテセロビウムテニュクライブ抽出物のエキス末をDMSOに10%溶解し、さらにPBS(−)に希釈して濃度調整)20μLを加え、さらに37℃にて3日間培養した。次いで培地を除去し、PBS(−)で2回洗浄後、トリプシン−EDTAを用いて細胞を剥離し、1.5mLチュ−ブに入れ、25℃、12000回転、10分間遠心操作し、細胞ペレットを生成した。コントロ−ルには、20μLのPBS(−)を用いた。ピテセロビウムテニュクライブ抽出物の固形分は1%として添加実験を行った。評価は、下記の評価基準にて行い、その結果を表2に示す。
【0018】
〈評価基準〉
細胞ペレットの色調
0:コントロ−ルと同様な黒色
1:コントロ−ルに比べてわずかに薄い黒色
2:コントロ−ルに比べ明瞭に薄い黒色
3:灰色に近い黒色
4:灰色
5:白色
細胞ペレットの量
1:コントロ−ルに比べ明瞭に少ない
2:コントロ−ルに比べわずかに少ない
3:コントロ−ルと同量
【0019】
【表2】
【0020】
表2から明らかな通り、ピテセロビウムテニュクライブ抽出物には顕著なメラニン産生抑制効果が見られ、細胞毒性も少ないことが理解出来る。
【0021】
常法により実施例1〜11に示す美白剤及び皮膚外用剤を調製した。
【0022】
実施例1 クリ−ム
下記成分A、別に下記成分Bを75℃に加温溶解し、それぞれA液及びB液とする。A液にB液を加えて乳化し、攪拌しながら50℃まで冷却し、成分Cを加え、クリ−ムを調製した。
成分A
ホホバ油 3.0重量%
スクワラン 2.0重量%
メチルポリシロキサン 0.5重量%
ステアリルアルコ−ル 0.5重量%
セチルアルコ−ル 0.5重量%
トリ(カプリル・カプリン酸)グリセリル 12.5重量%
モノステアリン酸グリセリル 5.0重量%
モノステアリン酸ジグリセリル 1.5重量%
モノステアリン酸デカグリセリル 3.0重量%
パラオキシ安息香酸プロピル 0.1重量%
成分B
キサンタンガム 0.1重量%
ピテセロビウムテニュクライブ抽出物 3.0重量%
グリセリン 1.0重量%
1,3−ブチレングリコ−ル 5.0重量%
パラオキシ安息香酸メチル 0.2重量%
精製水 62.0重量%
成分C
香料 0.1重量%
【0023】
実施例2 化粧水
下記成分Aを混合溶解させA液とし、これとは別に下記成分Bを混合溶解させてB液とし、A液とB液を均等に混合し、化粧水を調製した。
成分A
ポリオキシエチレンソルビタンラウリン酸エステル 1.2重量%
エチルアルコ−ル 5.0重量%
パラオキシ安息香酸メチル 0.2重量%
香料 0.1重量%
成分B
クインスシ−ドエキス 8.0重量%
グリセリン 3.0重量%
1,3ブチレングリコ−ル 5.0重量%
ピテセロビウムテニュクライブ抽出物 2.0重量%
精製水 75.5重量%
【0024】
実施例3 乳液
下記成分A、別に成分Bを75℃で加熱溶解させてそれぞれA液及びB液とし、A液にB液を加えて乳化し、攪拌しながら50℃まで冷却し、成分Cを加え、乳液を調製した。
成分A
ホホバ油 1.0重量%
スクワラン 2.0重量%
ベヘニルルコ−ル 1.0重量%
トリ(カプリル・カプリン酸)グリセリル 2.0重量%
テトラグリセリン縮合シリノレイン酸 0.1重量%
モノオレイン酸プロピレングリコ−ル 0.5重量%
モノステアリン酸グリセリル 1.0重量%
モノミレスチン酸ヘキサグリセリン 1.0重量%
モノミリスチン酸デカグリセリン 0.5重量%
パラオキシ安息香酸プロピル 0.1重量%
成分B
クインスシ−ドエキス 5.0重量%
ホホバ葉エキス 2.0重量%
ピテセロビウムテニュクライブ抽出物 2.0重量%
1,3ブチレングリコ−ル 3.0重量%
精製水 78.7重量%
成分C
香料 0.1重量%
【0025】
実施例4 石けん
石けん製造の常法により下記成分を混合して石けんを生成した。
成分
石けん素地 53.2重量%
スクロ−ル 19.4重量%
ホホバ油 0.25重量%
ピテセロビウムテニュクライブ抽出物 2.5重量%
濃グリセリン 6.5重量%
ヒドロキシエタンジホスホン酸 0.15重量%
常水 18.0重量%
【0026】
実施例5 クレンジングジェル
下記成分A、別に成分Bを70℃で加熱溶解させてそれぞれA液及びB液とし、A液にB液を加えて均一になるまで攪拌する。攪拌しながら50℃まで冷却し、成分Cを加え、クレンジングジェルを調製した。
成分A
モノミリスチン酸ヘキサグリセリル 20.0重量%
流動パラフィン 58.8重量%
パラオキシ安息香酸エステル 0.3重量%
成分B
ピテセロビウムテニュクライブ抽出物 0.5重量%
濃グリセリン 5.9重量%
ソルビト−ル 5.0重量%
精製水 9.4重量%
成分C
香料 0.1重量%
【0027】
実施例6 パック剤
A相、B相、C相をそれぞれ均一に溶解し、A相にB相を加えて可溶化し、ついでC相を加えて均一に溶解し、パック剤を調製した。
A相
ジプロピレングリコ−ル 5.0重量%
ポリオキシエチレン硬化ヒマシ油 5.0重量%
B相
オリ−ブ油 5.0重量%
酢酸トコフェノ−ル 0.2重量%
パラオキシ安息香酸エステル 0.2重量%
C相
亜硫酸水素ナトリウム 0.03重量%
ポリビニルアルコ−ル 13.0重量%
ピテセロビウムテニュクライブ抽出物 1.0重量%
ホホバ葉エキス 1.0重量%
エタノ−ル 7.0重量%
精製水 62.77重量%
【0028】
実施例7 乳化型ファンデ−ション
下記成分Aを充分に混合粉砕した粉末部Aとし、成分BをB液、成分CをC液とする。C液を加熱攪拌後、Aを添加しホモミキサ−処理し、さらに加熱混合したB液を加えてホモミキサ−処理する。攪拌しながら50℃まで冷却し、成分Dを加え、さらに室温まで冷却して乳化型ファンデ−ションを調製した。
成分A
二酸化チタン 10.3重量%
セリサイト 5.4重量%
カオリン 3.0重量%
黄色酸化鉄 0.7重量%
ベンガラ 0.4重量%
黒色酸化鉄 0.2重量%
成分B
デカメチルシクロペンタシロキサン 11.5重量%
流動パラフィン 8.5重量%
成分C
セスキオレイン酸ソルビタン 3.0重量%
ピテセロビウムテニュクライブ抽出物 1.5重量%
1,3−ブチレングリコ−ル 5.0重量%
パラオキシ安息香酸エステル 0.2重量%
精製水 50.1重量%
成分D
香料 0.2重量%
【0029】
実施例8 固形ファンデ−ション
下記成分Aをブレンダ−で均一に混合し、これに成分Bを加え、よく混練して固形ファンデ−ションを調製した。
成分A
タルク 42.4重量%
カオリン 15.5重量%
セリサイト 10.0重量%
亜鉛華 7.0重量%
二酸化チタン 3.8重量%
黄色酸化鉄 2.9重量%
黒色酸化鉄 0.2重量%
成分B
スクワラン 8.0重量%
イソステアリン酸 4.0重量%
モノオレイン酸ポリオキシエチレンソルビタン 3.0重量%
オクタン酸イソセチル 2.0重量%
ピテセロビウムテニュクライブ抽出物 1.0重量%
パラオキシ安息香酸エステル 0.1重量%
香料 0.1重量%
【0030】
実施例9 ヘア−トニック
下記成分Aに成分Bを加え、攪拌溶解した後、成分Cを加えてさらに攪拌してヘア−トニックを調製した。
成分A
エタノ−ル 50.0重量%
成分B
グリセリン 3.0重量%
L−メント−ル 0.1重量%
センブリエキス 2.0重量%
ピテセロビウムテニュクライブ抽出物 5.0重量%
香料 0.2重量%
成分C
オタネニンジンエキス 3.0重量%
精製水 36.7重量%
【0031】
実施例10 シャンプ−
下記成分を加温均一に混合してシャンプ−を調製した。
成分
N−ヤシ油脂肪酸グルタミン酸トリエタノ−ルアミン 25.0重量%
ラウリン酸ジエタノ−ルアミド 5.0重量%
ミリスチン酸カリウム 5.0重量%
ジステアリン酸エチレングリコ−ル 2.0重量%
ポリエチレングリコ−ル400 15.0重量%
ホホバ油 1.0重量%
ピテセロビウムテニュクライブ抽出物 3.0重量%
クロルキシレノ−ル 0.1重量%
ビタミンE 0.1重量%
パラオキシ安息香酸エステル 0.2重量%
香料 0.3重量%
精製水 43.3重量%
【0032】
実施例11 浴用剤
下記成分により常法でもって浴用剤を調製した。
成分
乾燥硫酸ナトリウム 40.0重量%
炭酸水素ナトリウム 57.5重量%
オリ−ブ油 0.2重量%
ピテセロビウムテニュクライブ抽出物 0.1重量%
軽質無水ケイ酸 0.3重量%
香料 1.7重量%
黄色202号の(1) 0.2重量%
【0033】
【発明の効果】
本発明によれば以上の次第で、ピテセロビウムテニュクライブの抽出物は優れたチロシナ−ゼ活性阻害およびメラニン産生抑制作用を有するものであって、シミ・ソバカス、日焼け後の皮膚色素沈殿による黒化の予防及び治療のみならず
、安全性・安定性においても優れているものである。[0001]
BACKGROUND OF THE INVENTION
The present invention relates to a whitening agent and an external preparation for skin, and more specifically, inhibits the action of tyrosinase in melanocytes, suppresses melanin production, has an excellent whitening effect on the skin after ultraviolet irradiation, and causes spots due to sunburn. -It is related with the whitening agent and skin external preparation which can prevent or treat buckwheat etc.
[0002]
[Background Art and Problems to be Solved by the Invention]
Skin freckles, skin pigmentation after sunburn, etc. are caused by markedly increased melanin production due to the activation of pigment cells present in the skin, and the mechanism is not necessarily clear, but tyrosinase It is presumed that it is produced through various intermediates after changing from tyrosine to dopa and from dopa to dopaquinone. For this reason, in order to prevent or treat skin blackening, it is necessary to inhibit the activity of tyrosinase and to inhibit part or all of the process of producing melanin.
[0003]
By the way, as a tyrosinase activity inhibitor and a melanin production inhibitor that prevent or treat skin blackening, JP-A-6-256150 (Patent Document 1) and JP-A-2002-128646 (Patent Document). As disclosed in 2), ascorbic acid, kojic acid, arbutin, hydroquinone and the like are known.
However, the ascorbic acid has difficulty in stability and hardly shows any effect when applied externally. Hydroquinone is not only problematic in terms of the stability of the substance itself (irritability, allergenicity), but also has a problem in formulating it as a drug from the viewpoint of causing cases of vitiligo. Etc. are not always satisfactory in terms of stability and safety.
[0004]
[Patent Document 1]
JP-A-6-256150 [Patent Document 2]
Japanese Patent Laid-Open No. 2002-128646
The present invention is intended to solve the conventional problems and provide a whitening agent and an external preparation for skin that have not only excellent whitening effects but also excellent stability and safety.
[0006]
[Means for Solving the Problems]
As a result of intensive studies to prevent and treat skin blackening, the present inventor not only has an excellent effect of preventing and treating skin blackening, but the extract of Piterobium tenuclide has The present inventors have found that it is excellent in terms of stability and safety, and have completed the present invention.
[0007]
That is, the gist of the present invention is a whitening agent and a skin external preparation containing an extract of Piterobium tenuclide.
[0008]
DETAILED DESCRIPTION OF THE INVENTION
The Pithecellobium tenu crib of the present invention is a plant belonging to the legume family (FABACEAE), and is cultivated in Southeast Asia such as Thailand where high-temperature and high-humidity rainfall is recognized. The method for preparing the extract of Pitecerobium tenuclide is not particularly limited, and examples thereof include a method in which raw or dried bark is extracted from a low temperature to a warm temperature using various solvents. Specific examples of the extraction medium include water, methanol, lower monohydric alcohol such as ethanol, glycerin, propylene glycol, dipropylene glycol, and 1,3-butylene glycol. Examples thereof include lower alkyl esters such as monovalent alcohol and ethyl acetate, and one or a mixture of two or more of these can be used. The extract of Piterobium tenuclide may be used as it is, but may be filtered and concentrated as necessary. In addition, the extract can be fractionated and purified by column chromatography, countercurrent distribution, or the like. Furthermore, after the above-mentioned extract is dried under reduced pressure or freeze-dried, it can be prepared in the form of powder or paste, and can be appropriately formulated and used.
[0009]
The compounding amount of the Piterobium tenuclide extract in the whitening agent and the external preparation for skin of the present invention is not particularly limited, but is 0.0001 to a dry solid in terms of efficacy, compoundability, and feel. It is 10.0 weight%, Preferably it is 0.001-5.0 weight%, Most preferably, it is 0.01-3.0 weight%. If the blending amount is less than 0.0001% by weight, the whitening effect tends to be poor. Conversely, if the blending amount exceeds 10.0% by weight, the effect cannot be substantially increased, and blending into an external preparation for skin is difficult. Tend to be.
[0010]
The whitening agent and skin external preparation of the present invention include, in addition to the extract of Piterobium tenuclide, an external skin preparation for cosmetics, quasi-drugs, pharmaceuticals, etc. as long as the effects of the present invention are not impaired as necessary. Ingredients used in the above, such as surfactants, oils, moisturizers, thickeners, antioxidants, UV protection agents, alcohols, powder ingredients, colorants, fragrances, aqueous ingredients, water, various skin nutrients, etc. Can be appropriately blended as necessary.
Furthermore, sequestering agents, antibacterial agents, cell activators, sebum secretion regulators, anti-inflammatory agents, astringents, active oxygen inhibitors, anti-allergic agents, anti-aging agents, and other plant extracts having further physiological activity These extracted fractions, purified products, and the like can also be appropriately blended.
[0011]
The whitening agent and external preparation for skin in the present invention can be produced by conventional methods. Further, the whitening agent and the external preparation for skin in the present invention are not limited to general skin cosmetics, but include pharmaceuticals, quasi-drugs, medicinal cosmetics, and the like. The dosage form of the whitening agent and the external preparation for skin of the present invention may be any of solubilization system, emulsification system, powder dispersion system, etc., and is used for basic cosmetics such as lotions, emulsions, creams, packs, etc. Makeup cosmetics such as shampoos, rinses, soaps, body shampoos and other toiletries, bath preparations and the like.
[0012]
【Example】
Next, examples of the present invention will be specifically described, but the present invention is not limited to these examples. In the following examples,% by weight is simply%.
[0013]
Production Example 1 Pitherobium tenuclide extract 1 kg of 50 vol% ethanol solution was added to 100 g of bark pulverized product of pitecerobium tenuclide and extracted at 50 ° C. for 8 hours. This was filtered, and the filtrate was concentrated to dryness under reduced pressure. The dried product was dissolved in 50% ethanol and filtered to obtain a Piterobium tenuclide extract. The evaporation residue was 0.48%.
[0014]
Test Example 1 Tyrosinase Activity Inhibition Test Using the extract of Piterobium tenuclide obtained as described above, diluted with purified water, and each concentration of 1 mg / mL, 0.1 mg / mL, 0.05 mg / mL It was. Using 10% FBS (fetal bovine serum; manufactured by Nissho) and theophylline (0.09 mg / mL) -containing MEM (Gibco product name), mouse-derived B16 melanoma cultured cells were 3 × in a 96-well plate. After seeding at a density of 10 3 cells / well and culturing at 37 ° C. and 5% CO 2 for 24 hours, each concentration of the test sample was added, followed by further culturing at 37 ° C. and 5% CO 2 for 3 days. Prior to measurement of tyrosinase activity, the medium in the wells was removed and washed twice with 100 μL of PBS. PBS containing 45 μL kl% Triin X (Rome and House trade name) was added to each well, the plate was shaken for 1 minute to disrupt the cell membrane, and the wavelength was 475 nm with a microplate reader. The absorbance was measured and this was taken as the absorbance at 0 minutes. Thereafter, 5 μL of a 10 mM L-DOPA solution was quickly added and incubated at 37 ° C. for 60 minutes. After shaking the plate for 1 minute, the absorbance was measured in the same manner as the absorbance at 60 minutes. The ratio of the difference in absorbance of the test sample with respect to the difference in absorbance at 0 minutes and 60 minutes when no test sample was added (control) was defined as the tyrosinase activity inhibition rate. The results are shown in Table 1.
[0015]
[Table 1]
[0016]
As is apparent from Table 1, it can be understood that the extract of Piterobium tenuclide has a remarkable inhibitory action on tyrosinase activity.
[0017]
Test Example 2 Melanin Production Inhibition Test Mouse-derived B16 melanoma cells were seeded in 5 mm 10 4 cells in a 35 mm dish using a DMEM medium containing 5% FBS, and cultured at 37 ° C. for 24 hours at 5% CO 2. After 24 hours, the dish medium was removed, 2 mL of DMEM medium containing 5% FBS and a test sample dissolved in each concentration (10% of the extract powder of Piterobium tenuclide extract was dissolved in DMSO, 20 μL of the solution was diluted with PBS (−) to adjust the concentration, and further cultured at 37 ° C. for 3 days. Next, the medium is removed, and after washing twice with PBS (−), the cells are detached using trypsin-EDTA, placed in a 1.5 mL tube, centrifuged at 25 ° C., 12,000 rpm for 10 minutes, and cell pellet. Was generated. For the control, 20 μL of PBS (−) was used. The addition experiment was conducted with the solid content of Piterobium tenuclide extract being 1%. Evaluation is performed according to the following evaluation criteria, and the results are shown in Table 2.
[0018]
<Evaluation criteria>
Color of cell pellet 0: Black similar to control 1: Black slightly lighter than control 2: Clearly light black compared to control 3: Black close to gray 4: Gray 5: White cell pellet 1: Clearly less than control 2: Slightly less than control 3: Same amount as control
[Table 2]
[0020]
As is apparent from Table 2, it can be understood that the pithecerobium tenuclide extract has a remarkable melanin production inhibitory effect and has little cytotoxicity.
[0021]
The whitening agent and the external preparation for skin shown in Examples 1 to 11 were prepared by a conventional method.
[0022]
Example 1 Cream The following component A and separately the following component B are heated and dissolved at 75 ° C. to obtain A solution and B solution, respectively. Liquid B was added to liquid A, emulsified, cooled to 50 ° C. with stirring, component C was added, and a cream was prepared.
Component A
Jojoba oil 3.0% by weight
Squalane 2.0% by weight
Methyl polysiloxane 0.5% by weight
Stearyl alcohol 0.5% by weight
Cetyl alcohol 0.5% by weight
Tri (capryl / capric acid) glyceryl 12.5% by weight
Glyceryl monostearate 5.0% by weight
Diglyceryl monostearate 1.5% by weight
Decaglyceryl monostearate 3.0% by weight
Propyl paraoxybenzoate 0.1% by weight
Component B
Xanthan gum 0.1% by weight
Piterobium tenuclide extract 3.0% by weight
Glycerin 1.0% by weight
1,3-butylene glycol 5.0% by weight
Methyl paraoxybenzoate 0.2% by weight
Purified water 62.0% by weight
Component C
Fragrance 0.1% by weight
[0023]
Example 2 Toner lotion The following component A was mixed and dissolved to prepare A solution. Separately, the following component B was mixed and dissolved to prepare solution B, and A and B solutions were mixed evenly to prepare a lotion.
Component A
Polyoxyethylene sorbitan laurate 1.2% by weight
Ethyl alcohol 5.0% by weight
Methyl paraoxybenzoate 0.2% by weight
Fragrance 0.1% by weight
Component B
Quinceaide extract 8.0 wt%
Glycerin 3.0% by weight
1,3-butylene glycol 5.0% by weight
Pitecerobium tenuclide extract 2.0% by weight
75.5% by weight of purified water
[0024]
Example 3 Emulsion The following component A and separately component B were heated and dissolved at 75 ° C. to give A and B solutions, respectively. The B solution was added to the A solution to emulsify, and the mixture was cooled to 50 ° C. with stirring. In addition, an emulsion was prepared.
Component A
Jojoba oil 1.0% by weight
Squalane 2.0% by weight
Behenyl alcohol 1.0% by weight
Tri (capryl / capric acid) glyceryl 2.0% by weight
Tetraglycerin condensed silinoleic acid 0.1% by weight
Propylene glycol monooleate 0.5% by weight
1.0% by weight of glyceryl monostearate
Monoglycerin hexaglycerin 1.0% by weight
Monomyristic acid decaglycerin 0.5% by weight
Propyl paraoxybenzoate 0.1% by weight
Component B
Quince essence extract 5.0% by weight
Jojoba leaf extract 2.0% by weight
Pitecerobium tenuclide extract 2.0% by weight
1,3-butylene glycol 3.0% by weight
78.7% by weight of purified water
Component C
Fragrance 0.1% by weight
[0025]
Example 4 The soap was produced by mixing the following components according to a conventional method for producing soap.
Ingredients soap base 53.2% by weight
Scroll 19.4% by weight
Jojoba oil 0.25% by weight
Pitecerobium tenuclide extract 2.5% by weight
Concentrated glycerin 6.5% by weight
Hydroxyethanediphosphonic acid 0.15% by weight
Normal water 18.0% by weight
[0026]
Example 5 Cleansing Gel The following component A and component B were dissolved by heating at 70 ° C. to prepare A solution and B solution, respectively, and B solution was added to A solution and stirred until uniform. Cooling to 50 ° C. with stirring, component C was added to prepare a cleansing gel.
Component A
Hexaglyceryl monomyristate 20.0% by weight
Liquid paraffin 58.8% by weight
P-Hydroxybenzoate 0.3% by weight
Component B
Piterobium tenuclide extract 0.5% by weight
Concentrated glycerin 5.9% by weight
Sorbitol 5.0% by weight
Purified water 9.4% by weight
Component C
Fragrance 0.1% by weight
[0027]
Example 6 Packing agent A phase, B phase, and C phase were each uniformly dissolved, B phase was added to A phase to solubilize, and then C phase was added and uniformly dissolved to prepare a packing agent.
Phase A dipropylene glycol 5.0% by weight
Polyoxyethylene hydrogenated castor oil 5.0% by weight
Phase B olive oil 5.0% by weight
Tocophenol acetate 0.2% by weight
P-Hydroxybenzoate 0.2% by weight
Phase C sodium bisulfite 0.03% by weight
Polyvinyl alcohol 13.0% by weight
Pitecerobium tenuclide extract 1.0% by weight
Jojoba leaf extract 1.0% by weight
Ethanol 7.0% by weight
Purified water 62.77% by weight
[0028]
Example 7 Emulsion type foundation A powder part A in which the following component A is sufficiently mixed and ground is used, component B is liquid B, and component C is liquid C. After the liquid C is heated and stirred, A is added and subjected to a homomixer treatment, and the liquid B which has been heated and mixed is further added to perform the homomixer treatment. While stirring, the mixture was cooled to 50 ° C., component D was added, and the mixture was further cooled to room temperature to prepare an emulsified foundation.
Component A
Titanium dioxide 10.3% by weight
Sericite 5.4 wt%
Kaolin 3.0% by weight
Yellow iron oxide 0.7% by weight
Bengala 0.4% by weight
Black iron oxide 0.2% by weight
Component B
Decamethylcyclopentasiloxane 11.5% by weight
Liquid paraffin 8.5% by weight
Component C
Sorbitan sesquioleate 3.0% by weight
Piterobium tenuclide extract 1.5% by weight
1,3-butylene glycol 5.0% by weight
P-Hydroxybenzoate 0.2% by weight
Purified water 50.1% by weight
Component D
Fragrance 0.2% by weight
[0029]
Example 8 Solid Foundation The following component A was uniformly mixed with a blender, component B was added thereto, and kneaded well to prepare a solid foundation.
Component A
Talc 42.4% by weight
Kaolin 15.5% by weight
Sericite 10.0% by weight
Zinc flower 7.0% by weight
Titanium dioxide 3.8% by weight
2.9% by weight of yellow iron oxide
Black iron oxide 0.2% by weight
Component B
Squalane 8.0 wt%
Isostearic acid 4.0% by weight
Polyoxyethylene sorbitan monooleate 3.0% by weight
Isocetyl octoate 2.0% by weight
Pitecerobium tenuclide extract 1.0% by weight
Paraoxybenzoate 0.1% by weight
Fragrance 0.1% by weight
[0030]
Example 9 Hair-Tonic After component B was added to component A below and dissolved by stirring, component C was added and further stirred to prepare a hair-tonic.
Component A
Ethanol 50.0% by weight
Component B
Glycerin 3.0% by weight
L-menthol 0.1% by weight
Assembly extract 2.0% by weight
Piterobium tenuclide extract 5.0% by weight
Fragrance 0.2% by weight
Component C
Ginseng extract 3.0% by weight
Purified water 36.7% by weight
[0031]
Example 10 Shampoo
The following components were heated and mixed uniformly to prepare a shampoo.
Component N-coconut oil fatty acid glutamic acid triethanolamine 25.0% by weight
Lauric acid diethylethanolamide 5.0% by weight
Potassium myristate 5.0% by weight
2.0% by weight of ethylene glycol distearate
Polyethylene glycol 400 15.0% by weight
Jojoba oil 1.0% by weight
Piterobium tenuclide extract 3.0% by weight
Chloroxylenol 0.1% by weight
Vitamin E 0.1% by weight
P-Hydroxybenzoate 0.2% by weight
Fragrance 0.3% by weight
Purified water 43.3% by weight
[0032]
Example 11 Bath Agent A bath agent was prepared in the usual manner using the following components.
Ingredient dry sodium sulfate 40.0% by weight
Sodium bicarbonate 57.5% by weight
Olive oil 0.2% by weight
Piterobium tenuclide extract 0.1% by weight
Light anhydrous silicic acid 0.3% by weight
Fragrance 1.7% by weight
Yellow No. 202 (1) 0.2% by weight
[0033]
【Effect of the invention】
According to the present invention, according to the above, the extract of Piterobium tenuclide has excellent tyrosinase activity inhibition and melanin production suppression action, and it is caused by skin freckles and skin pigment precipitation after sunburn. Not only prevention and treatment of blackening but also safety and stability are excellent.
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