CN103687585B - 美白剂及黑素生成抑制剂 - Google Patents
美白剂及黑素生成抑制剂 Download PDFInfo
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- CN103687585B CN103687585B CN201280017155.5A CN201280017155A CN103687585B CN 103687585 B CN103687585 B CN 103687585B CN 201280017155 A CN201280017155 A CN 201280017155A CN 103687585 B CN103687585 B CN 103687585B
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- Prior art keywords
- chafurosideb
- whitening agent
- agent
- melanogenesis
- whitening
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Abstract
本发明提供一种具有优异的美白作用及黑素生成抑制作用、且作为美白剂及黑素生成抑制剂有用的化合物。本发明的美白剂及黑素生成抑制剂的特征在于其包含Chafuroside？B。
Description
相关申请
本申请主张2011年4月12日申请的日本国专利申请2011-88317号的优先权，将其包含在内。
技术领域
本发明涉及一种美白剂及黑素生成抑制剂，特别是涉及其有效成分。
背景技术
一般认为皮肤的斑点、雀斑等色素沉积是以激素异常或紫外线、皮肤局部炎症为原因而导致过量形成黑素、并使该黑素沉积在皮肤内而产生的。成为皮肤色素沉积的原因的该黑素在位于表皮基底层的色素细胞(黑素细胞)内的被称为黑素体的细胞器内生成，生成的黑素被摄入至周围角化细胞(角化细胞)。
作为预防、改善如上所述的色素沉积的方法，主要使用具有美白作用的物质、即抑制黑素生成的物质。作为色素沉积的预防、改善方法，公知有例如：大量口服维他命C的方法、注射谷胱甘肽等的方法、或者以软膏、霜膏、洗液等的形式在皮肤上局部涂布曲酸、维他命C及其衍生物、半胱氨酸等的方法等。
另一方面，Chafuroside(チャフロサィド)为一种可以通过由乌龙茶等的茶萃取而分离的化合物。该Chafuroside对过敏性疾病有效，已知有得到以高比例包含该Chafuroside的茶叶的方法(专利文献1)。但是，没有关于ChafurosideB的美白效果、黑素生成抑制效果的报告。
现有技术文献
专利文献
专利文献1：日本特开2009-131161号公报
发明内容
发明所要解决的课题
本发明是鉴于所述现有技术而进行的，其想要解决的课题在于提供一种具有优异的美白作用、黑素生成抑制作用，且作为美白剂及黑素生成抑制剂有用的化合物。
用于解决课题的手段
本发明人等为了解决所述课题而潜心研究，结果发现ChafurosideB具有优异的美白作用及黑素生成抑制作用，从而完成了本发明。
即，本发明的美白剂，其特征在于，包含ChafurosideB。
本发明的黑素生成抑制剂，其特征在于，包含ChafurosideB。
本发明的黑素生成抑制方法，其特征在于，将包含有效量的ChafurosideB的组合物经口服施与。
另外，本发明的黑素生成抑制方法，其特征在于，将包含有效量的ChafurosideB的组合物涂布在皮肤上。
在所述黑素生成抑制方法中，优选ChafurosideB作为美白剂发挥功能。
ChafurosideB的使用，其中，ChafurosideB在以包含ChafurosideB为特征的本发明的美白剂的制造中作为有效成分而使用。
在所述使用中，优选所述ChafurosideB抑制黑素的生成。
发明的效果
本发明的美白剂及黑素生成抑制剂可以提供一种包含ChafurosideB且美白作用及黑素生成抑制作用优异的制剂。
附图的说明
图1为验证牡荆素、异牡荆黄素和ChafurosideB对于UVB表皮黑素细胞活化的效果的图。
图2为表示ChafurosideA及ChafurosideB对于UVB表皮黑素细胞活化的效果的图。
具体实施方式
本发明的美白剂及黑素生成抑制剂包含ChafurosideB。ChafurosideB为由下式(I)所示的黄酮C糖苷。
[化学式1]
ChafurosideB的制造方法没有特别限定，可以使用通过公知的方法所合成的合成品，也可以通过公知的纯化方法由绿茶、焙茶、红茶、乌龙茶等的茶叶进行分离。
在口服包含美白剂及黑素生成抑制剂的有效成分、即ChafurosideB的组合物的情况下，优选服用有效量的ChafurosideB。ChafurosideB优选每一天服用0.001mg／kgb.w.以上。另外，特别优选每一天服用1mg／kgb.w.以上。
本发明的美白剂及黑素生成抑制剂也可以配混在美白用饮料或者美白用食品中。美白用饮料或美白用食品中，除作为有效成分的ChafurosideB之外，还可以根据需要任意选择添加剂并配混。作为添加剂，可以举出：赋形剂、呈味剂、着色剂、保存剂、增稠剂、稳定剂、凝胶化剂、抗氧化剂、功能性材料等。
作为功能性材料，可以举出：各种维他命类、泛酸、叶酸、生物素、锌、钙、镁、氨基酸、寡糖、蜂胶、蜂王浆、EPA、DHA、辅酶Ｑ10、软骨素、乳酸菌、乳铁蛋白、异黄酮、梅干、甲壳质、壳聚糖、氨基葡萄糖等。
作为赋形剂，只要为制作所需剂型时通常所使用的物质则没有限定，例如，可以举出：如二氧化硅微粒之类的粉末类、蔗糖脂肪酸酯、结晶纤维素／羧甲基纤维素钠、磷酸氢钙、小麦淀粉、大米淀粉、玉米淀粉、马铃薯淀粉、糊精、环糊精等淀粉类、结晶纤维素类、乳糖、葡萄糖、砂糖、还原麦芽糖、糖浆、果寡糖、乳化寡糖等糖类、山梨糖醇、赤藓糖醇、木糖醇、乳糖醇、甘露醇等糖醇类等。
作为呈味剂，可以举出：作为果汁提取物的文旦提取物、荔枝提取物、苹果果汁、橘子汁、柚子萃取物、桃子香精、梅子香精、作为甜味剂的安赛蜜K、赤藓糖醇、寡糖类、甘露糖、木糖醇、异构化糖类、作为茶成分的绿茶、乌龙茶、巴拿巴茶、杜仲茶、铁观音茶、薏仁茶、绞股蓝茶、茭白茶、昆布茶、酸奶香精等。
着色剂、保存剂、增稠剂、稳定剂、凝胶化剂、抗氧化剂可以适当选择用于食物和饮料的公知的物质。
作为本发明的美白剂及黑素生成抑制剂的形态，可以制成安瓿剂、胶囊、丸剂、片剂、粉末、颗粒、固形、液体、凝胶或气泡、霜膏等任意形态。
具体而言，例如，可以举出：美容·健康饮料或食品、医药品、西点类、和糕点类、口香糖、糖果、焦糖等一般糕点类、果汁等一般清凉饮料水、鱼糕、圆筒状鱼糕等加工水产糊状产品、香肠、火腿等畜产产品、鲜面条、煮面、荞麦面等面类、调味汁、酱油、调味酱、砂糖、蜂蜜、糖粉、糖浆等调料、咖喱粉、芥末粉、胡椒粉等的香辣佐料、果酱、橘子酱、巧克力酱、奶酪、黄油、酸奶等乳制品等。为了可高效地摄取，可以优选举出：口服的美容／健康饮料、美容／健康食品等。
另外，它们可以通过现有公知的方法来制造。
应予说明，本发明的美白剂及黑素生成抑制剂期待透皮吸收的效果，也可以配混在皮肤外用剂等的组合物中。作为皮肤外用剂的形式，可以举出：化妆品、贴剂、医药品等。
在皮肤外用剂中，除作为有效成分的ChafurosideB以外，也可以根据需要适当配混通常用于化妆品或医药品等皮肤外用剂中的成分，例如：保湿剂、抗氧化剂、油性成分、紫外线吸收剂、表面活性剂、增稠剂、醇类、粉末成分、色剂、水性成分、水、各种皮肤营养剂等。
在包含本发明的美白剂的皮肤外用剂中，优选配混有效量的ChafurosideB。就ChafurosideB的配混量而言，在皮肤外用剂总量中，特别优选为0.001～5.0质量％。如配混量过少，则不能充分发挥美白效果，即使配混量过多，也并没有大的效果的提高，故不优选。
实施例
下面列举实施例对本发明进而进行详细说明，但本发明不受其限定。
作为下面的试验中所使用的动物，使用雄性DBA／2小鼠(日本CharlesRiver公司)。购买5周龄的小鼠，驯化饲养一周后使用。
另外，让小鼠自由摄取灭菌蒸馏水及饲料AIN-93G(日本农产工业公司)。
牡荆素、异牡荆黄素使用市售品(SIGMA-ALDRICH公司)，ChafurosideB通过公知的方法(J.Agric.FoodChem.2009，57，6779-6786)由茶分离。然后，使用上述动物，通过下述试验方法进行黑素细胞活化抑制试验。
应予说明，牡荆素、异牡荆黄素分别与ChafurosideB一样为在茶中包含的黄酮类。
·黑素细胞活化抑制试验方法
使用包含牡荆素或异牡荆黄素或ChafurosideB(1mg／kgb.w.)的介质对小鼠经口进行灌胃9天，施与后照射照射量为120mJ的中波长紫外线（UVB)。对照(UV非照射组）及对照(UV照射组)同样施与介质。应予说明，各组各以8只小鼠进行试验。
在本试验中，就介质及其施与用量而言，以0.5w／v％甲基纤维素400溶液、5mL／kgb.w.进行。
第10天采集皮肤，进行DOPA反应。在显微镜观察下，计算单位面积的DOPA阳性黑素细胞数。
将结果示于图1。应予说明，图中的＊表示在通过学生t检验(显著性水平＊p<0.05、＊＊p<0.01)进行统计处理的情况下，相对于对照(UV照射组）确认有显著差异。
根据图1，作为与ChafurosideB具有类似结构的黄酮类的牡荆素虽然具有抑制黑素细胞数增加的倾向，但未显著抑制。另外，作为与ChafurosideA具有类似结构的黄酮类的异牡荆黄素显著抑制黑素细胞数的增加。
但是，令人惊讶的是，ChafurosideB非常显著地抑制黑素细胞数的增加。
接着，本发明人等将ChafurosideA及ChafurosideB作为样品，与上述试验方法相同地进行了黑素细胞活化抑制试验。将结果示于图2。
根据图2，确认通过UV照射，DOPA阳性黑素细胞数显著增加(UV照射组)。ChafurosideA及ChafurosideB显著抑制黑素细胞数的增加。但是，与ChafurosideA相比，可以明确ChafurosideB更为明显地抑制黑素细胞数的增加。
因此，本发明的美白剂及黑素生成抑制剂的特征在于，包含ChafurosideB。
下面，列举本发明的美白剂及黑素生成抑制剂、即ChafurosideB的配混例。但本发明不受其限定。
配混例1颗粒
配混例2乳液
Claims (4)
1.ChafurosideB的用于制造美白剂的使用，其特征在于，ChafurosideB为下式(I)所示的黄酮C糖苷，
[化学式1]
2.ChafurosideB的用于制造黑素生成抑制剂的使用，其特征在于，ChafurosideB为下式(I)所示的黄酮C糖苷、即，
[化学式1]
3.下式(I)所示的黄酮C糖苷、即ChafurosideB的使用，其中，ChafurosideB在以包含ChafurosideB为特征的美白剂的制造中作为有效成分而使用，
[化学式1]
4.根据权利要求3所述的使用，其特征在于，所述ChafurosideB抑制黑素生成。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2011088317 | 2011-04-12 | ||
| JP2011-088317 | 2011-04-12 | ||
| PCT/JP2012/060046 WO2012141255A1 (ja) | 2011-04-12 | 2012-04-12 | 美白剤およびメラニン生成抑制剤 |
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| CN (1) | CN103687585B (zh) |
| HK (1) | HK1196096A1 (zh) |
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| JP2012219076A (ja) * | 2011-04-12 | 2012-11-12 | Shizuokaken Koritsu Daigaku Hojin | 美白剤およびメラニン生成抑制剤 |
| JP7001356B2 (ja) * | 2016-03-31 | 2022-01-19 | 小林製薬株式会社 | 皮膚色素沈着抑制剤 |
| CN110464669A (zh) * | 2019-08-16 | 2019-11-19 | 香港科技大学深圳研究院 | 一种美白剂及其用途、美白用化妆品和美白用医药产品 |
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| CN1671713A (zh) * | 2002-07-03 | 2005-09-21 | 三得利株式会社 | 黄酮c糖苷的新型衍生物和含有其的组合物 |
| CN1938318A (zh) * | 2004-03-31 | 2007-03-28 | 三得利株式会社 | 黄酮c糖苷衍生物的制造方法 |
| CN101938988A (zh) * | 2008-02-08 | 2011-01-05 | 株式会社资生堂 | 美白剂和皮肤外用剂 |
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| JPH11228339A (ja) * | 1998-02-13 | 1999-08-24 | Ichimaru Pharcos Co Ltd | メラニン生成抑制剤及び皮膚外用剤 |
| EP1513848A4 (en) * | 2002-06-12 | 2005-11-09 | Biogen Idec Inc | METHOD FOR TREATING ISCHEMIA REPERFUSION INJURIES WITH ADENOSINE RECEPTOR ANTAGONISTS |
| JP2006008626A (ja) * | 2004-06-28 | 2006-01-12 | Daiichi Asubio Pharma Co Ltd | フラボン誘導体の製造法ならびにフラボン誘導体およびそれを含む医薬組成物 |
| JP2006342103A (ja) * | 2005-06-09 | 2006-12-21 | National Cancer Center-Japan | ウーロン茶葉抽出物ｏｔａｃを有効成分とする発癌抑制剤 |
| WO2008045272A2 (en) * | 2006-10-06 | 2008-04-17 | Dynamis Therapeutics, Inc. | Compositions and methods for skin lightening |
| JP5226982B2 (ja) * | 2007-08-06 | 2013-07-03 | 全薬工業株式会社 | ソバガラの抽出物を含む皮膚外用剤 |
| EP2385049A4 (en) * | 2009-01-03 | 2012-08-08 | Shizuoka Prefecture Public University Corp | SULFATED C-GLYCOSIDE, METHOD FOR THE ISOLATION THEREOF AND METHOD FOR THE SYNTHESIS THEREOF |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1671713A (zh) * | 2002-07-03 | 2005-09-21 | 三得利株式会社 | 黄酮c糖苷的新型衍生物和含有其的组合物 |
| CN1938318A (zh) * | 2004-03-31 | 2007-03-28 | 三得利株式会社 | 黄酮c糖苷衍生物的制造方法 |
| CN101938988A (zh) * | 2008-02-08 | 2011-01-05 | 株式会社资生堂 | 美白剂和皮肤外用剂 |
Non-Patent Citations (2)
| Title |
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| Concise Synthesis of Chafurosides A and B;Takumi Furuta，等;《ORGANIC LETTERS》;20090427;第11卷(第11期);第2233-2236页 * |
| Quantitation of Chafurosides A and B in Tea Leaves and Isolation of Prechafurosides A and B from Oolong Tea Leaves;HITOSHI ISHIDA，等;《JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY》;20091231;第57卷(第15期);第6779-6786页 * |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2012141255A1 (ja) | 2012-10-18 |
| HK1196096A1 (zh) | 2014-12-05 |
| JP5162727B2 (ja) | 2013-03-13 |
| TW201247197A (en) | 2012-12-01 |
| TWI566772B (zh) | 2017-01-21 |
| CN103687585A (zh) | 2014-03-26 |
| JPWO2012141255A1 (ja) | 2014-07-28 |
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