CN1200922A - 用橙提取液清除自由基的方法 - Google Patents
用橙提取液清除自由基的方法 Download PDFInfo
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Abstract
本发明涉及橙提取液用于制备具有抗自由基活性的药物、化妆品、食品和农用组合物的应用。所述的橙提取液基本上不含有抗坏血酸。
Description
本发明涉及通过将橙提取液掺入一种组合物中来清除自由基的方法。
自由基的有害作用在许多情况下是已知的并且在不断地被研究。例如,据信皮肤变坏的原因之一就是形成皮肤的各要素如纤维、细胞和酶中形成自由基。自由基的形成可以部分地由阳光的外部辐射作用引起。这样形成的自由基可以通过链反应攻击皮肤的各要素,只要自由基存在,例如只要自由基不与产生稳定分子的物质(一般被称为清除剂或抑制剂)结合,所述的链反应就会继续。这些自由基在皮肤体被水平的不利作用可以引起细胞DNA的破坏和结缔组织(胶原和弹性硬蛋白)的侵蚀。这样,皮肤显得更老。
因此,不断地在寻找可以在自由基链反应期间阻断或抑制自由基形成的物质。目前,熟知的清除剂(也称作抑制剂或抗氧剂,如在下述说明书和所附的权利要求书中所用的都应该被认为是与清除剂是同义的)包括酚类、芳香胺类、硫化合物类、生籽油(raw seed oils)、麦胚油、生育酚类和树胶类。也据信磷酸、柠檬酸和抗坏血酸各自具有清除活性或增强上面提到的已知清除剂的活性。
这样,法国申请2,597,337-A2描述了一种化妆品,它通过袭击自由基而减慢老化过程。该化妆品包括第一水溶性活性成分,它可以包括维生素C源如巴巴多斯樱桃提取液,和第二脂溶性成分,它包括自由基清除剂如维生素E。
虽然上面的法国申请描述了巴巴多斯樱桃提取液的应用,但它具体是关于维生素C的存在,已知与其它天然源的维生素C源比较时它的维生素C的含量较高。同样,日本公开申请2-200610和70-61915描述了从艾西罗拉的果实中得到的提取液可以掺入化妆品中。这些申请教导了巴巴多斯樱桃含有维生素C或抗坏血酸,并且申请号为2-200610的申请描述了含有至少1%L-抗坏血酸的提取液,正是L-抗坏血酸的存在提供了所需的增白作用。这并不使人惊奇,因为人们熟知L-抗坏血酸可以提供增白作用。
然而,没有人认识到基本上不含维生素C的橙提取液具有自由基清除活性。本发明人现已发现,橙提取液显示出自由基清除活性,因此可以发现在制备药物、食品和农用组合物中及更特别是在供皮肤外用的化妆品中的特殊的用途。因此,在本发明中用于清除自由基的橙提取液的能力是令人惊奇的和出人意料的。
本发明的目的是提供抑制自由基形成或清除自由基存在的组合物。本发明还注视到含有已知自由基清除剂的组合物可以通过掺入橙提取液来增强。这样,本发明包括含有自由基清除剂的类型的组合物,其改进是加入了橙提取液。优选地,所述组合物是适于人皮肤使用的化妆品组合物。例如,橙提取液可以单独起作用或与皮肤增白剂一起用作皮肤增白剂。
本发明还包括一种在组合物中提供自由基清除活性的方法,包括将有效量的橙提取液混入组合物中以增强组合物的自由基清除活性。
已知在由分子氧引起的氧化反应期间产生的过氧化物离子是非常活泼的并且具体攻击蛋白质和核酸。因此,本发明基于橙提取液对过氧化物基团的抗自由基活性。本发明的掺入了橙提取液的组合物特别适用于保护皮肤,这特别是由于其对抗光线损害反应和UV攻击的保护。
本发明还包括一种在人皮肤中清除自由基的方法,包括局部施用于皮肤一种包含橙提取液的组合物。优选地,该组合物还包含可药用的载体。
用于本发明的橙提取液基本上不含有抗坏血酸,并且仅含有少量的有机酸,特别是羧酸。
本说明书和所附的权利要求书中所用的术语“基本上不含有抗坏血酸”是指存在于橙提取液中的任何抗坏血酸的量不超过橙提取液的大约1%重量,优选地不超过大约0.1%,更优选地不超过大约0.01%。最优选地,如果存在的话,抗坏血酸的量不超过橙提取液的大约0.005%。
本说明书和所附的权利要求书中所用的术语“少量的有机酸”和“少量的羧酸”是指任何有机酸和任何羧酸,包括饱和的和不饱和的羧酸和二羧酸、羟基单羧酸、羟基二羧酸和羟基三羧酸,其存在的量不超过橙提取液的大约5%重量,优选地不超过大约3%,更优选地不超过大约2%。
在本发明的组合物中,所用的橙提取液的量不可以绝对化,因为它随制备物的形式而变。然而,一般的用量基于组合物的总重量为大约0.01%至大约50%、优选大约0.01%至大约5%、理想的是大约0.05%至大约2%、更优选的是大约0.1%至大约1%。
请注意,除非另有说明,在本说明书和所附的权利要求书中给出的所有百分数均指重量百分数。
按照本发明,提供了一种包含橙提取液作为活性成分的自由基清除剂组合物。
然而,在本发明中,所述的橙提取液基本上不含有任何实质量的维生素C(抗坏血酸或其衍生物)。换句话说,橙提取液中不含有超过大约1%重量、优选地不超过大约0.1%、更优选地不超过大约0.01%。最优选地,如果存在的话,所述抗坏血酸的量不超过橙提取液的大约0.005%。
可以以任何合适的方法制备橙提取液以得到基本上不含抗坏血酸的提取液。优选地,橙提取液从橙皮、花和/或橙树上的叶得到。据信橙提取液通过下述方法制备,即干燥所述原料,预处理之,通过交替浸渍和渗滤24-48小时以冷提取预处理后的原料、过滤、微孔过滤以及加入适当的防腐剂如parabens或苯氧基乙醇。最优选地,橙提取液是得自Centerchem,Inc.的Bitter Orange Peel Extract HB或得自Cosmetochem的Herbasol Orange Extract。据信Centerchem的原料得自橙皮,而Cosmetochem的原料得自橙花。
在本发明的组合物中,所用的橙提取液的量不可以绝对化,因为它随制备物的形式而变。然而,一般的用量基于增白剂组合物的总重量为大约0.01%至大约50%、优选大约0.01%至大约5%、理想的是大约0.05%至大约2%、更优选的是大约0.1%至大约1%。
本发明的组合物可以以各种形式制备。例如,它可以是化妆品制备物形式如乳膏、化妆洗剂、包装物或粉剂,或作为乳液、洗剂、搽剂或软膏。在各种制剂中,可以掺入各种已知的常规化妆品成分。例如,掺入化妆品成分如醇类、脂和油类、表面活性剂、脂肪酸、硅油类、湿润剂、粘度调节剂、乳化剂、稳定剂、着色剂和香料。
在本发明的组合物的另一方面,提供了改进的自由基清除组合物,其中改进包括加入橙提取液,如上面充分定义的。在该方面,将橙提取液加到如皮肤增白组合物中是理想的。在该情况下,橙提取液的自由基清除活性可以抑制多巴醌(dopaquinone)的转化,结果抑制了eumelanin的产生。因此,预期橙提取液的自由基清除活性可以增加已知的酪氨酸酶抑制剂,并因此提供增强的皮肤增白性质。
本发明也提供了一种增强已知的自由基清除剂的自由基清除活性的方法,它包括将橙提取液加到含已知的自由基清除剂的组合物中。
本发明也包括一种在组合物中提供自由基清除活性的方法,包括将有效量的橙提取液混合到所述的组合物中以增加组合物的自由基清除活性。
在本发明的另一方面,提供了一种在人皮肤中清除自由基的方法,它包括将橙提取液局部施用给皮肤。更优选地,该方法包括将包含橙提取液和可药用的载体的组合物局部施用给皮肤。术语“可药用的”是指那些药品、药物或适于与人或低等动物的组织接触使用的而无不适当的毒性、不相容性、不稳定性、刺激等的、与合理的效益/危险比相称的惰性成分。
为了说明本发明的橙提取液的自由基清除活性,进行了描述在Cosmetics & Toiletries,Vol.10,pp.51-56,Oct.1995中的试验。
量去39.43mg 2,2-二苯基-1间三硝苯基偕腙肼水合物(DPPH),一种已知的自由基源,用乙醇稀释到1000ml。对照比色杯中加入1.75ml对照物和1.75ml乙醇。空白比色杯中加入3.5ml乙醇。将各比色杯置于炉中于37℃放置30分钟。将空白比色杯置于参比槽中而将对照比色杯置于样品槽中用UV/vis分光光度计测定516nm处的吸光度。
实施例1
按照上述方法制备橙提取液。试验比色杯中装入1.75ml对照溶液和1.75ml 1%的橙提取液溶液。参比比色杯中装入1.75ml橙提取液和1.75ml乙醇。将各比色杯置于炉中于37℃放置30分钟。将试验比色杯置于样品槽中而将参比比色杯置于参比槽中以如上方式测定的吸光度。
将自由基清除活性作为对自由基产生的抑制百分数用下式计算:
百分抑制=100×[1-(DT/DR)]DT是相对于参比比色杯测得的试验比色杯的吸光度,而DR是相对于空白比色杯测得的对照比色杯的吸光度。
橙提取液显示出52%的抑制。
该试验表明,橙提取液具有抗自由基活性,因此可以预期当掺入组合物中时显示出有益的结果。
实施例2
以实施例1中所述的方法进行清除活性试验,但使用下述物质的1%溶液:(a)醋酸生育酚,(b)蔷薇果油,(c)噻克索酮,和(d)Lanachrys2B。结果示于下表1中。
表1
增白剂 | %抑制 |
醋酸生育酚 | 67 |
蔷薇果油 | 63 |
噻克索酮 | 50 |
Lanachrys 2B | 40 |
应该理解,可以对上述具体实施方案进行宽范围的变化和改进。因此,上述说明书是说明而不是限制本发明的,而且它是下述权利要求,包括所有的相等物,限定本发明。
Claims (11)
1.包含橙提取液的自由基清除组合物。
2.权利要求1的组合物,其中橙提取液含有少于约1%重量的抗坏血酸。
3.一种化妆品组合物,它为洗剂、泡沫、霜剂(creme)等形式,其改进之处是包含有效量的橙提取液以提供对过氧化物基团的抗自由基活性。
4.权利要求3的组合物,其中橙提取液含有少于约1%重量的抗坏血酸。
5.一种在组合物中提供抗自由基活性的方法,包括向组合物中混入有效量的橙提取液以增加组合物的抗自由基活性。
6.权利要求5的方法,其中橙提取液含有少于约1%重量的抗坏血酸。
7.权利要求6的方法,其中所述组合物选自药物、化妆品、食品和农用组合物。
8.一种清除人皮肤中自由基的方法,包括施用包含橙提取液的组合物。
9.权利要求8的方法,其中橙提取液含有少于约1%重量的抗坏血酸。
10.一种包含皮肤增白剂的皮肤增白组合物,其改进之处是包含有效量的橙提取液。
11.权利要求10的组合物,其中橙提取液含有少于约1%重量的抗坏血酸。
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US08/865,913 US5916576A (en) | 1997-05-30 | 1997-05-30 | Method of scavenging free radicals using orange extract |
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JP (1) | JP3012594B2 (zh) |
KR (1) | KR100358210B1 (zh) |
CN (1) | CN1195488C (zh) |
HK (1) | HK1017259A1 (zh) |
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CA2387703A1 (en) | 1999-10-01 | 2001-04-12 | Johnson & Johnson Consumer Companies, Inc. | Method for calming human beings using personal care compositions |
JP2001114634A (ja) * | 1999-10-12 | 2001-04-24 | Pola Chem Ind Inc | カタラーゼ保護剤及びこれを含有する老化防止用化粧料。 |
JP2001122758A (ja) * | 1999-10-22 | 2001-05-08 | Pola Chem Ind Inc | AGEs分解作用を有する老化肌防御、改善化粧料 |
JP5349719B2 (ja) * | 2000-01-26 | 2013-11-20 | 株式会社コーセー | 皮膚外用剤 |
ES2233630T3 (es) * | 2000-04-12 | 2005-06-16 | Bitop Aktiengesellschaft Fur Biotechnische Optimierung | Uso de solutos compatibles como sustancias con propiedades barredoras de radicales. |
EP1147764A3 (en) * | 2000-04-19 | 2002-03-20 | Nof Corporation | Cosmetic composition |
EP1311238B1 (de) * | 2000-08-18 | 2009-10-21 | Bitop Gesellschaft für Biotechnische Optimierung mbH | Verwendung von di-zuckeralkoholphosphaten zum schutz menschlicher hautzellen vor uv- und/oder ir-strahlung |
US20020151527A1 (en) * | 2000-12-20 | 2002-10-17 | Benjamin Wiegand | Method for reducing acne or improving skin tone |
US20020146469A1 (en) * | 2000-12-20 | 2002-10-10 | Benjamin Wiegand | Methods for reducing chronic stress in mammals |
GB2384563A (en) * | 2002-01-29 | 2003-07-30 | Johnson & Johnson Consumer | Method of measuring the stress or relaxation level of a mammal |
GB0203045D0 (en) * | 2002-02-08 | 2002-03-27 | Johnson & Johnson Consumer | Method of afefecting sleep and sleep-related behaviours |
KR20020040719A (ko) * | 2002-04-18 | 2002-05-30 | 김대도 | 오랜지 팩 |
FR2844451A1 (fr) * | 2002-09-12 | 2004-03-19 | Jean Morelle | Application locale cutanee, d'emulsions caracterisees par leurs proprietes antiprostanoidiques |
FR2844450A1 (fr) * | 2002-09-12 | 2004-03-19 | Jean Morelle | Application locale cutanee d'emulsions, caracterisees par leurs proprietes antiprostanoidiques |
US20040175438A1 (en) * | 2003-03-03 | 2004-09-09 | Benjamin Wiegand | Methods for alleviating symptoms associated with menopause using sensory regimen |
US20050249720A1 (en) * | 2004-05-05 | 2005-11-10 | Perez Mary R | Cosmetic skin formulation |
JP4669670B2 (ja) * | 2004-06-04 | 2011-04-13 | 株式会社ロッテ | 抗インフルエンザウイルス剤及びこれを吸着、含浸、添加させてなるインフルエンザ感染抑制用品 |
JP5748996B2 (ja) * | 2010-12-24 | 2015-07-15 | 日本メナード化粧品株式会社 | 皮膚外用剤 |
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US1990676A (en) * | 1931-11-21 | 1935-02-12 | Louis J Stern | Cosmetic cream |
US2255341A (en) * | 1939-04-13 | 1941-09-09 | Fruit Growers Exchange Ca | Composition of citrus fruit constituents and boric acid and method for making the same |
FR2472934A1 (fr) * | 1980-01-04 | 1981-07-10 | Oreal | Compositions cosmetiques a base d'une poudre d'origine vegetale |
JPS6479103A (en) * | 1987-06-09 | 1989-03-24 | Lion Corp | External preparation |
IT1219884B (it) * | 1988-03-28 | 1990-05-24 | Helga Frey | Composizione di lozione per capelli procedimento per la sua produzione e suo impiego |
JPH03227911A (ja) * | 1990-01-31 | 1991-10-08 | Yutaka Miyauchi | 育毛剤 |
ATE117665T1 (de) * | 1990-11-14 | 1995-02-15 | Oreal | Amphiphile, nichtionische derivate des glycerins sowie die entsprechenden zwischenprodukte, verfahren zu ihrer herstellung und diese enthaltende zusammensetzungen. |
EP0561305B1 (en) * | 1992-03-17 | 1999-08-11 | Eisai Co., Ltd. | Skin whitening composition containing teprenone |
JP3415197B2 (ja) * | 1993-06-30 | 2003-06-09 | 三省製薬株式会社 | 皮膚外用剤 |
JP3605420B2 (ja) * | 1993-07-14 | 2004-12-22 | 三省製薬株式会社 | 皮膚外用剤 |
US5482710A (en) * | 1993-07-30 | 1996-01-09 | Chesebrough-Pond'usa Co., Division Of Conopco, Inc. | Cosmetic composition for treatment of pimples and redness |
JPH0797311A (ja) * | 1993-09-29 | 1995-04-11 | Ken Suzawa | 化粧水 |
US5445747A (en) * | 1994-08-05 | 1995-08-29 | The Procter & Gamble Company | Cellulase fabric-conditioning compositions |
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WO1996016956A1 (fr) * | 1994-12-02 | 1996-06-06 | Kao Corporation | Derives de flavanonol et composition contenant ces derives propre a nourrir les cheveux et a stimuler leur croissance |
JP3638338B2 (ja) * | 1995-06-15 | 2005-04-13 | 株式会社アドバンストスキンリサーチ研究所 | メラニン生成抑制剤 |
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JPH1017485A (ja) * | 1996-07-02 | 1998-01-20 | Hino Seiyaku Kk | 抗酸化剤 |
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