JP5583346B2 - c−Kit活性阻害剤、及び、肌美白剤 - Google Patents
c−Kit活性阻害剤、及び、肌美白剤 Download PDFInfo
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- JP5583346B2 JP5583346B2 JP2008551174A JP2008551174A JP5583346B2 JP 5583346 B2 JP5583346 B2 JP 5583346B2 JP 2008551174 A JP2008551174 A JP 2008551174A JP 2008551174 A JP2008551174 A JP 2008551174A JP 5583346 B2 JP5583346 B2 JP 5583346B2
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- skin
- kit
- diosmethine
- skin whitening
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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
- A61Q19/02—Preparations for care of the skin for chemically bleaching or whitening the 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
-
- 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
- A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
- A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
- A61K8/9783—Angiosperms [Magnoliophyta]
- A61K8/9789—Magnoliopsida [dicotyledons]
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Birds (AREA)
- Dermatology (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Biotechnology (AREA)
- Botany (AREA)
- Microbiology (AREA)
- Mycology (AREA)
- Cosmetics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Plant Substances (AREA)
- Pyrane Compounds (AREA)
Description
市販されている化学式1ないし9のフラボン誘導体化合物を購入して使用した。各フラボン誘導体化合物を最終濃度が1μMになるようにして384ウェルプレートの各ウェルに入れ、c−Kit RTK及びATPも384ウェルプレートの各ウェルに添加して常温で1次反応させた。その後、基質としてビオチン化ポリ[グルタミン:チロシン](4:1)を添加して2次酵素反応を行った。
阻害率(%)=(試料の平均値−陰性対照群の平均値)/(陽性対照群の平均値−陰性対照群の平均値)×100
健康な男女20人を選定して両腕の下膊部に直径7mmの穴が6個ずつ2列あるアルミホイルを貼り、腕から10cm離れた距離からORIELソーラーシミュレーター1000W(ORIEL solar simulator 1000W)を使って60mJ/cm2の光量を照射した。照射の前に70%エタノール水溶液で照射部位をきれいに洗浄した。照射の3日前から調査後3週目まで、1日2回製造例1ないし3及び比較例1によって製造された基剤を一対の同じ行に塗布した。
しみのある健康な女性10人を選定して顔面部のしみ部位に1日2回製造例1によって製造された基剤を3週間塗布した。
[実施例1]
生薬材として市販されている乾燥した甘菊を購入して細かく粉砕し、粉砕物10kgに対してメタノール150Lで、還流冷却器が設けられた抽出器にて70℃で3時間加熱して抽出した。抽出物をろ布でろ過した後、残渣を同じ方法で1回以上さらに抽出した。抽出液を合わせて減圧濃縮し、乾燥抽出物1.2kgを得た。
実施例1で製造された甘菊メタノール抽出物1kgを10Lの水に懸濁させた後、ヘキサンを10Lずつ加え、3回溶媒分画してヘキサン分画を除去した。その後、残った水層に対してブタノールを10Lずつ加え、3回溶媒分画してブタノール分画を得て、これを減圧濃縮して乾燥物125gを得た。
実施例1で製造された甘菊メタノール抽出物1kgを10Lの水に懸濁させた後、エチルアセテートを10Lずつ加え、3回溶媒分画してエチルアセテート分画を得た。これを減圧濃縮して乾燥物230gを得た。
実施例2で製造された甘菊ブタノール可溶分画100gを溶離液としてクロロホルム、メタノール混合溶媒を用いてシリカゲルカラムクロマトグラフィーで有効分画を得た。この分画から分取用HPLCを使って有効成分1.2gを得た。分離した有効成分は核磁気共鳴スペクトル(NMR)及び質量分析(Mass)を通じて(図1ないし3参照)、次のように、前記化学式10で表したジオスメチンであると確認した。
分子式:C16H12O6
分子量:300.27
融点:260ないし264℃
UV(λax、nm)(MeOH):272、342
1H−NMR(DMSO−d6)σ:3H(6.69、s)、6H(6.13、s)、8H(6.39、s)、2’H(7.41、s)、5’H(7.06、d、8.6Hz)、6’H(7.51、d、8.6Hz)、5−OH(12.89、br)、7−OH(10.0、br)、4’−OMe(3.85、s)
前記実施例1(メタノール抽出物)及び実施例2(ブタノール可溶分画)の濃度がそれぞれ20μg/mlになるように、実施例4(ジオスメチン)は最終濃度が0.3μMになるようにして、前述した化学式1ないし9のフラボン誘導体化合物の評価方法と同様に評価した。その結果を下記表5に示した。
しみのある健康な女性10人を選定して顔面部のしみ部位に1日2回製造例4によって製造された基剤を3週間塗布した。
Claims (3)
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
KR1020060005369A KR100798252B1 (ko) | 2006-01-18 | 2006-01-18 | c-Kit 활성 저해제, 피부미백제 및 이를 함유하는피부미백용 조성물 |
KR10-2006-0005369 | 2006-01-18 | ||
KR1020060026683A KR100817662B1 (ko) | 2006-03-23 | 2006-03-23 | c-Kit 활성 저해제, 피부미백제 및 이를 함유하는피부미백용 조성물 |
KR10-2006-0026683 | 2006-03-23 | ||
PCT/KR2007/000227 WO2007083904A1 (en) | 2006-01-18 | 2007-01-12 | C-kit activation inhibitor, skin whitening compound and composition for skin whitening containing the same |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2009523786A JP2009523786A (ja) | 2009-06-25 |
JP5583346B2 true JP5583346B2 (ja) | 2014-09-03 |
Family
ID=38287817
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2008551174A Expired - Fee Related JP5583346B2 (ja) | 2006-01-18 | 2007-01-12 | c−Kit活性阻害剤、及び、肌美白剤 |
Country Status (2)
Country | Link |
---|---|
JP (1) | JP5583346B2 (ja) |
WO (1) | WO2007083904A1 (ja) |
Families Citing this family (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP2112145A1 (en) * | 2008-04-24 | 2009-10-28 | AxoGlia Therapeutics S.A. | Chromenone derivatives useful for the treatment of neurodegenerative diseases |
US8267951B2 (en) | 2008-06-12 | 2012-09-18 | Ncontact Surgical, Inc. | Dissecting cannula and methods of use thereof |
US20100158829A1 (en) * | 2008-12-24 | 2010-06-24 | Conopco, Inc., D/B/A Unilever | Method and Composition for Color Modulation |
EP2263664A1 (en) * | 2009-05-18 | 2010-12-22 | Nestec S.A. | Opioid receptors stimulating compounds (thymoquinone, Nigella sativa) and food allergy |
CA2827875A1 (en) * | 2011-03-01 | 2012-10-18 | Npharmakon, Llc | Use of n-(4-methoxyphenyl)-1-phenyl-1h-pyrazol-3-amine and related compounds |
JP6009791B2 (ja) * | 2012-03-28 | 2016-10-19 | ホーユー株式会社 | Hdc活性化阻害剤、hdc活性化阻害剤組成物、鎮痒剤及び鎮痒剤組成物 |
US20150335558A1 (en) * | 2012-10-22 | 2015-11-26 | Hoyu Co., Ltd. | Nerve growth inhibitor, cutaneous-sensory-irritation inhibitor, and marker for cutaneous-sensory-irritation detection |
JP6031334B2 (ja) * | 2012-11-14 | 2016-11-24 | 日本メナード化粧品株式会社 | メラノサイト分化誘導抑制剤及びその使用方法 |
CN114129495B (zh) * | 2021-12-10 | 2022-09-23 | 北京安德普泰医疗科技有限公司 | 一种抗炎舒敏修护组合物及其制备方法和应用 |
Family Cites Families (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS55111411A (en) * | 1979-02-19 | 1980-08-28 | Sansho Seiyaku Kk | Cosmetic for making fair skin |
JPS5735506A (en) * | 1980-08-11 | 1982-02-26 | Sansho Seiyaku Kk | Bleaching cosmetic |
JP3231908B2 (ja) * | 1993-07-13 | 2001-11-26 | 同和鉱業株式会社 | 美白化粧料 |
JP3993936B2 (ja) * | 1998-05-22 | 2007-10-17 | 一丸ファルコス株式会社 | メラニン生成抑制剤及び化粧料組成物 |
JP2004535792A (ja) * | 2001-04-27 | 2004-12-02 | ザ ジェネラル ホスピタル コーポレーション | チロシナーゼアッセイ法 |
KR100665313B1 (ko) * | 2003-06-26 | 2007-01-09 | 한국과학기술연구원 | 항산화 및 항바이러스 활성을 가지는 화합물 및 이를포함하는 감국 추출물 |
ATE413395T1 (de) * | 2003-08-21 | 2008-11-15 | Osi Pharm Inc | N-substituierte pyrazolyl-amidyl-benzimidazolyl-c-kit-inhibitor n |
CA2536954C (en) * | 2003-08-29 | 2012-11-27 | Exelixis, Inc. | C-kit modulators and methods of use |
KR20050030821A (ko) * | 2003-09-26 | 2005-03-31 | 한불화장품주식회사 | 2',4'-디하이드록시플라본 또는 그 유도체를 함유하는화장료 조성물 |
FR2865132A1 (fr) * | 2004-07-06 | 2005-07-22 | Oreal | Utilisation de la diosmetine, d'un de ses derives ou d'un extrait de plante contenant l'un d'eux pour favoriser la pigmentation de la peau et/ou des cheveux |
-
2007
- 2007-01-12 JP JP2008551174A patent/JP5583346B2/ja not_active Expired - Fee Related
- 2007-01-12 WO PCT/KR2007/000227 patent/WO2007083904A1/en active Application Filing
Also Published As
Publication number | Publication date |
---|---|
WO2007083904A1 (en) | 2007-07-26 |
JP2009523786A (ja) | 2009-06-25 |
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