JP5524483B2 - 有効成分としてガロカテキンガレートを含有する保湿用皮膚外用剤組成物 - Google Patents
有効成分としてガロカテキンガレートを含有する保湿用皮膚外用剤組成物 Download PDFInfo
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- JP5524483B2 JP5524483B2 JP2008531009A JP2008531009A JP5524483B2 JP 5524483 B2 JP5524483 B2 JP 5524483B2 JP 2008531009 A JP2008531009 A JP 2008531009A JP 2008531009 A JP2008531009 A JP 2008531009A JP 5524483 B2 JP5524483 B2 JP 5524483B2
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
- A61Q19/007—Preparations for dry skin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
- A61K8/4973—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom
- A61K8/498—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom having 6-membered rings or their condensed derivatives, e.g. coumarin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
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- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Dermatology (AREA)
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- Pharmacology & Pharmacy (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Cosmetics (AREA)
Description
本発明の保湿用皮膚外用剤組成物は、有効成分としてガロカテキンガレートを含有することによって、ペルオキシソーム増殖剤活性化受容体亜型アルファ(PPAR-α)の活性を活性化させて、優秀な皮膚保湿及び皮膚乾燥防止効果を示す。
PPAR−α活性化能力測定実験は、次のように進行された。
猿の腎臓上皮細胞株であるCV−1細胞(ATCC CCL 70)をチャコール(charcoal)/デキストリン処理された10%牛胎児血清を含むDMEM培地に継代培養し、フェノールレッド(phenol red)のエストロゲンによる効果を除去するために、フェノールレッド無処理培地を使用した。プラスミドは、一般的な培養条件でも発現されるユニバーサルプローモーター(universal promoter)後方にPPAR−(遺伝子を有するものとリガンド結合型のPPAR-)が結合して活性化されるPPRE(PPARs Response Element)をプローモーターとして有し、後にレポーターとして役目をするホタル(firefly)ルシフェラーゼ遺伝子を有するもの、及び参照として使用されるレニラルシフェラーゼ(Renilla luciferase)遺伝子が結合されたプラスミドが使用された。
上記試験例1で確認された緑茶の構成成分のうちガロカテキンガレート、テオブロミン、及びケルセチンのPPAR−α活性化能力を最適化させるために、反応表面分析法(responsive surface method、RSM)を利用した。これを利用すれば、独立変数のどの値で反応値が最適化されるかを把握することができ、独立変数と従属変数間の関数関係をデータから推正し、独立変数が反応変数にどんな影響を及ぼすかを予測することができ、変数間の最適の実験条件を捜し出すことができる。本発明では、MiniTab 14を利用して反応表面分析法のうち中心合成計画法(central composite designs)を行い、その結果を表2(中心合成計画法による設計とその測定値)に示した。
その結果を図1〜図2、及び下記表4(PPAR-α活性化のための最適濃度の割合)に示した。
実験に使用した細胞株は、ドイツ癌研究センターのDr. Fuseningから分譲された HaCaT細胞株(Human kerationocyte HaCaT cell line)であって、上記細胞を60mmディッシュに1×105個に分株し、1日間培養した後、各々の試験物質を処理した後、24時間培養した。上記試験物質は、陰性対照群(lane 1, 5)、ガロカテキンガレート:テオブロミン:ケルセチンの130μM:100μM:100μMの混合物(lane 2, 6)、ガロカテキンガレート:テオブロミン:ケルセチンの65μM:50μM:50μMの混合物(lane 3, 7)である。細胞培養のために10%の牛胎児血清(fetal bovine serum, FBS)が含有されたDMEM(Dulbecos modified eagles medium, GibcoBRL, Life Technology)培地で37℃、5%CO2条件で培養した。陰性対照群は、上記と同一の培地で試験物質を添加しない状態で培養したものを利用した。
下記表5の組成で製造した参考例1、実施例2〜5及び比較例1の化粧水の皮膚保湿力改善効果を測定した。
皮膚乾燥症を示す50〜80代の成人男女50名を5個グループに分け、各グループに下記比較例1、参考例1及び実施例2〜5の化粧水を毎日2回ずつ4週間顔面に塗布した。塗布開始前と塗布後1週、2週、4週経過した時点、そして塗布を中止してから2週経過(全体6週経過)後に恒温、恒湿条件(24℃、相対湿度40%)でコニオメータを用いて皮膚水分量を測定した。
本発明者らは、上記組成物が長期間の皮膚損傷による皮膚障壁(skin barrier)の回復に及ぶ効果を評価するための試験を実施した。生後8乃至10週が経過した若い無毛マウスの背中にアセトンを1日2回ずつ5日間周期的に塗布し、実験動物の背中皮膚の障壁機能を損傷させた後、蒸発計(evaporimeter)で経皮水分損失量(TEWL;transepidermal waterloss)を測定し、40g/m2/hr以上の経皮水分損失を示す皮膚を有する実験動物だけを対象にしてビヒクル(vehicle)(プロピレングリコール:エタノール=7:3)と下記表8の参考例6、実施例7及び比較例2〜3を含有する試験物質を皮膚面積5cm2当たり200μlの用量で1日2回ずつ3日間連続塗布しながら、一定時間毎にTEWLを測定し、下記数学式1によって障壁回復率を求め、その結果を表8(障壁回復率(%))に示した。
障壁回復率(%)=(TEWL0−TEWLX)/(TEWL0−TEWLbasal)×100
TEWL0:皮膚損傷直後のTEWL測定値
TEWLX:皮膚障壁損傷後、一定時間経過後のTEWL測定値
TEWLbasal:初期TEWL測定値
Claims (5)
- 有効成分としてガロカテキンガレート(gallocatechin gallate: GCG)、テオブロミン(theobromine)及びケルセチン(quercetin)を含有した保湿用皮膚外用剤組成物であって、
前記ガロカテキンガレートは組成物の全体重量に対して0.001〜30.0重量%の量で含有され、
前記有効成分は、各々モル濃度として、(i)ガロカテキンガレートが0.7モル以下である時、テオブロミンが少なくとも0.4モルであって、ケルセチンが少なくとも0.4モルであり、(ii)ガロカテキンガレートが0.7〜1.4モルである時、テオブロミンが少なくとも0.3モルであって、ケルセチンが少なくとも0.3モルであり、(iii)ガロカテキンガレートが1.4モル以上である時、テオブロミンが少なくとも0.2モルであって、ケルセチンが少なくとも0.2モルであることを特徴とする皮膚外用剤組成物。 - 前記有効成分は、組成物の全体重量に対して各々0.001〜30.0重量%の量で含有されることを特徴とする請求項1に記載の皮膚外用剤組成物。
- 前記組成物は、PPAR−αの活性化用であることを特徴とする請求項1に記載の皮膚外用剤組成物。
- 前記組成物は、皮膚のフィラグリン(filaggrin)の発現促進用であることを特徴とする請求項1に記載の皮膚外用剤組成物。
- 前記組成物は、皮膚のインボルクリン(involucrin)の発現促進用であることを特徴とする請求項1に記載の皮膚外用剤組成物。
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KR10-2005-0086821 | 2005-09-16 | ||
PCT/KR2006/003579 WO2007032624A1 (en) | 2005-09-16 | 2006-09-08 | Composition for skin external application containing gallocatechin gallate for moisturizing effect on the skin |
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JP5761888B2 (ja) * | 2008-09-30 | 2015-08-12 | 丸善製薬株式会社 | 抗老化剤及び皮膚化粧料 |
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DK2504357T3 (en) | 2009-11-23 | 2017-10-23 | Res Dev Foundation | RECOMBINANT FILAGGRIN POLYPEPTIDES FOR CELL IMPORT |
KR101326932B1 (ko) | 2009-11-26 | 2013-11-11 | (주)아모레퍼시픽 | 퍼옥시좀 증식체 활성화 수용체 델타의 활성촉진 조성물 |
US9132294B2 (en) | 2010-06-30 | 2015-09-15 | Avon Products, Inc. | Compositions and methods for stimulation MAGP-1 to improve the appearance of skin |
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KR101914157B1 (ko) | 2011-08-24 | 2018-12-31 | (주)아모레퍼시픽 | 녹차 성분을 함유하는 화장료 조성물 |
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CN103585040B (zh) * | 2013-10-31 | 2015-07-22 | 天津郁美净集团有限公司 | 抗水性液晶化妆品用乳剂组合物及其应用 |
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WO2019066031A1 (ja) * | 2017-09-29 | 2019-04-04 | サントリーホールディングス株式会社 | アクアポリン3発現促進用組成物及びその使用 |
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