CN1255357A - 具有强力的抵抗酪氨酸酶活性的葡萄种子提取物及其应用 - Google Patents
具有强力的抵抗酪氨酸酶活性的葡萄种子提取物及其应用 Download PDFInfo
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- CN1255357A CN1255357A CN99103166A CN99103166A CN1255357A CN 1255357 A CN1255357 A CN 1255357A CN 99103166 A CN99103166 A CN 99103166A CN 99103166 A CN99103166 A CN 99103166A CN 1255357 A CN1255357 A CN 1255357A
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- grape seed
- seed extract
- extract
- organic solvent
- melanin
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Abstract
本发明公开了一种葡萄种子提取物和它的应用。利用水,乙醇,甲醇或丙酮作为提取溶剂在热水条件或加热条件下制备葡萄种子提取物。葡萄种子提取物具有对酪氨酸酶的强力的抑制活性而没有副作用。所以,葡萄种子提取物可以用作化妆品,该化妆品具有抑制黑色素生物合成,预防皮肤老化,保护皮肤和皮肤美白的功能。
Description
本发明涉及葡萄种子提取物和它作为抵抗酪氨酸酶的强力抑制活性的用途。更具体地说,本发明涉及葡萄种子提取物的用途,该提取物是用水,乙醇,甲醇或丙酮萃取葡萄种子制备的,该提取物可以作为美白化妆品,治疗色素和预防食物变黑。
现有技术的说明
黑色素是苯酚类型的大分子,由黑色色素和蛋白质的复合物组成。这一多聚体色素可以在动物的皮肤,眼睛,毛发,鸟的皮毛和当苹果,土豆和香蕉的切面与空气接触产生的棕色表面中看到。在身体中的过量黑色素可以导致面部变色,在皮肤上形成雀斑,促进皮肤老化,甚至可能是皮肤癌的起因。另外,对于食物,如蔬菜,水果和鱼,如果合成了较多的黑色素,它们的质量就下降了。
据报道,黑色素是通过酪氨酸酶的作用生物合成的。酪氨酸酶,一种与铜结合的单加氧酶,广泛存在于动物,植物,微生物和人,催化酚化合物如单羟基苯丙氨酸和二羟基苯丙氨酸(DOPA)的需氧氧化。当皮肤在紫外线下过度暴露时,酪氨酸酶的作用是在暴露的区域储存melanintorth,损坏或老化皮肤。另外,在蔬菜和水果中的变黑现象是由多酚氧化酶如酪氨酸酶引起的。
动物黑色素,是由酪氨酸酶催化合成的,可以分为黄色-微红棕色pheomelanin和棕黑色真黑色素。
黑色素的生物合成取决于酪氨酸酶的活性。将L-酪氨酸羟化成L-3,4-二羟基苯丙氨酸(DOPA),后者氧化成多巴醌,进一步成为隐色素,最后成为多巴色素。将多巴色素转换成为5,6-二羟基吲哚(DHI),然后,氧化聚合化,最后与蛋白质结合。除了将多巴色素转换成DHI,已报道的一个可替代的途径是其中的多巴色素是5,6-二羟基吲哚羧酸(DHICA),作用的酶是多巴色素互变异构酶。
最近对与皮肤癌相关的黑色素的生物合成代谢进行了广泛的研究。结果是,开发了各种黑色素合成抑制剂,并用于医学作为皮肤病的治疗剂,用于化妆品工业作为皮肤美白剂,以预防和治疗面部的变黑和雀斑和在食品工业中用作变色防护剂。最近,在与环境问题的关联中,对这些黑色素合成抑制剂的需求已经大大提高。
所以,迄今为止对黑色素合成抑制剂的主要研究集中在酪氨酸酶抑制剂的开发上。代表性的酪氨酸酶抑制剂是用于形成酪氨酸酶的协同因子的螯合物的物质,即铜离子,还原剂,如抗坏血酸,用于将醌还原成酚,和重硫酸盐用于变性酪氨酸酶本身。
这种酪氨酸抑制剂现在被开发为各种美白剂,但存在着各种问题。例如,4-羟基苯甲醚和羟基醌,它们现在用于局部治疗色素疾病如变色,雀斑,斑点和怀孕期间的色素沉着,这两种物质具有强力的抵抗黑色素形成的抑制活性,但具有的副作用是引起色素细胞的变性或死亡,和损坏细胞的内部功能。特别是,羟基醌化合物被开发为黑色素生物合成的美白乳液抑制剂,但羟基醌化合物的用途现在只在几个国家允许使用,因为据报道由于它们的细胞毒性,它们能引起皮肤刺激或皮肤疾病。所以,已经进行了更多的努力选择对身体安全的天然物质,如酪氨酸酶抑制剂。
本发明人通过对酪氨酸酶深入和完全的研究,发现浓缩的鞣酸或原花色素,一种多酚化合物,具有强力的抵抗酪氨酸酶的活性,以致能抑制黑色素的生物合成并且以相当大的量包含在葡萄种子中。
本发明的概要
本发明的目的是为克服现有技术中遇到的上述问题,提供一种葡萄种子提取物,该提取物具有对酪氨酸酶的强力的抑制剂活性,所以能预防黑色素的生物合成。
本发明的另一目的是提供一种葡萄种子提取物,它被用作需要抑制黑色素合成的产物的有效成分。
根据本发明,通过提供一种葡萄种子提取物可以达到上面的目的,该葡萄种子提取物具有对酪氨酸酶的抑制活性。通过利用水或60-90%有机溶剂如乙醇,甲醇或丙酮在热水条件或加热条件下萃取可以制备葡萄种子提取物。
根据本发明的另一方面,提供了一种化妆品物质,其中含有作为有效成分的葡萄种子提取物,该提取物具有抑制黑色素生物合成,预防皮肤老化,保护皮肤和美白皮肤的功能。
根据本发明的另一方面,提供了一种抑制黑色素生物合成的药物组合物,该药物组合物含有葡萄种子提取物作为药物有效成分。该药物组合物是变色,雀斑,斑点和怀孕过程中的色素沉着的治疗剂。
根据本发明的另一方面,提供了一种食物添加剂,其中含有作为预防变黑的有效成分的葡萄种子提取物,如在水果,蔬菜和鱼中。
附图的简要说明
图1显示了相对与葡萄种子提取物和羟基醌的样品浓度划出的酪氨酸酶的抑制百分数,其中符合◆表示利用70%的乙醇(30℃)获得的葡萄种子提取物,符号■表示利用70%的丙酮获得的葡萄种子提取物,符号Δ是羟基醌,符号●是利用热水获得的葡萄种子提取物,符号□是利用70%乙醇(90℃)获得的葡萄种子提取物,符合0是利用70%甲醇(90℃)获得的葡萄种子提取物。
图2显示了葡萄种子提取物在Streptomyces bikiniensis中抵抗黑色素生物合成的作用形成的抑制区。
本发明的详细说明
本发明涉及葡萄种子提取物对酪氨酸酶的活性的抑制。为了制备葡萄种子提取物,利用水和有机溶剂在各种温度提取脱脂葡萄种子粉末。在这点上,首先考虑溶剂和温度,因为它们在干燥后影响多酚,即本发明的有效成分,的产量和含量。优选利用60-90%的丙酮在热水条件下和60-90%乙醇或60-90%甲醇在加热条件下进行提取,更优选地是利用70-80%在热水条件下或70-80%或70-80%甲醇在加热条件下进行。
从蘑菇酪氨酸酶与L-二羟基苯丙氨酸(L-DOPA)的反应获得的葡萄种子提取物对酪氨酸酶的抑制活性的吸收资料证明在酪氨酸酶的抑制活性上,葡萄种子提取物比常规化学物质如曲酸,羟基醌,熊果苷,4-羟基茴香醚,抗坏血酸,松香油和氢化可的松优越。特别是,利用70-80%的丙酮在热水条件下或利用70-80%乙醇或甲醇在加热条件下制备的葡萄种子提取物显示优选的抑制活性。
利用生物合成黑色素的微生物,如Streptomyces bikiniensis测量葡萄种子提取物对黑色素生物合成的抑制活性。葡萄种子的提取物形成的抑制区相对于曲酸,羟基醌,熊果苷和4-羟基茴香醚形成的那些更大和更清晰。
所以,本发明的葡萄种子提取物,酪氨酸酶活性的抑制剂,可以用于预防和治疗变色,雀斑,斑点和怀孕过程中的色素沉着。另外,葡萄种子提取物可以用作化妆品物质,该物质可以加入柔润的皮肤洗液,营养皮肤洗液,营养乳液,按摩乳液,精华乳液和化妆品包装中,以便发挥抑制黑色素生物合成,预防皮肤老化,保护皮肤和美白皮肤的功能。另外,葡萄种子提取物可以用作预防变黑的食物添加剂,如在水果,蔬菜和鱼中,并能维持食物的新鲜。
因为葡萄种子提取物是来自水果的提取物,已经证明是无害的,它可以用作医学治疗剂。对于用它制备药物,可以使用本领域已知的方法。例如,单独或与药物可接受载体,构成试剂,稀释剂和诸如此类组合,可以将葡萄种子提取物配制进各种制剂,包括软膏,粉末,颗粒,片剂,锭剂,胶囊,用于注射的液体和诸如此类。它们可以口服或肠胃外或包衣在皮肤上给药。
根据它的吸收效率,失活深度,和挥发速度,病人的年龄,性别和症状,和疾病的严重性,来确定药物有效成分的剂量。通常,以5-300毫克一天,优选地25-200毫克一天给药葡萄种子提取物。至于这些配制的制剂的给药途径,如果需要,可以按照专家的建议。该制剂可以施用或以一定规律的间隔包覆在皮肤上。
通过下面的实施例可以更好地理解本发明,这些实施例只是为了说明,不是对本发明的限制。实施例1制备葡萄种子提取物
用水洗涤葡萄种子,利用碾磨机粉碎,利用己烷脱脂并干燥。将这样得到的葡萄种子的粉末的等分试样100克在不同的温度下加入各0.5-3升水,乙醇,甲醇和丙酮,根据温度,利用振摇温育器(30℃)或装备温度控制器的回流提取器(60-95℃)12小时内提取。在减压下,利用旋转蒸发器在50℃浓缩得到的粗提取物,然后,在真空中干燥得到粉末状葡萄种子提取物。根据提取溶剂和温度,从葡萄种子和粉末葡萄种子提取物的重量的测量计算葡萄种子提取物的干产量。对于葡萄种子的多酚含量,利用了FollinDennis方法。考虑到根据提取溶剂和温度的干产量和多酚含量,发现最有效的提取是利用70-80%丙酮在热水条件下和利用70-80%乙醇或甲醇在加热条件下获得的。
表1
实施例II葡萄种子提取物对酪氨酸酶的抑制活性
提取溶剂 提取温度(℃) %干产量 %GSE中的多酚含量 |
水 80-95 7.7 14.510%已醇 30 2.1 5.140%已醇 30 2.9 10.170,80%已醇 30 2.8 19.210%已醇 60-80 3.5 15.040%已醇 60-80 7.4 27.470,80%4已醇 60-80 7.7 38.299%已醇 60-75 1.5 50.010%丙酮 30 2.3 4.040%丙酮 30 4.1 19.070.80%丙酮 30 3.7 40.310%甲醇 60-80 3.0 14.140%甲醇 60-80 7.1 25.270,80%甲醇 60-80 7.5 35.4 |
将蘑菇酪氨酸酶(Sigma,E.C.1.14.18.1)用于研究实施例I制备的粉末葡萄种子提取物的抑制活性。将酪氨酸酶溶解于1/15摩尔的磷酸缓冲液(pH6.8),使给出的酶溶液的浓度为1560单位/毫升,将酶溶液储存在冰箱中。在冰上融化酶溶液以便使用。作为底物,在1/15摩尔磷酸缓冲液中,在稍微屏蔽的瓶中溶解L-3,4-二羟基苯丙氨酸(L-DOPA)。在使用前即时制备这一溶液。
在25℃,与1.4615毫升1/15摩尔磷酸缓冲液一起,预温育0.0625毫升(78单位)的酪氨酸酶溶液5分钟,然后加入0.476毫升L-DOPA溶液。在475纳米测量吸光值10分钟。这一实验进行了对照组(A)(酪氨酸酶+1/15摩尔磷酸缓冲液),空白组(B)(1/15摩尔只有磷酸缓冲液),样品组(C)(酪氨酸酶+葡萄种子提取物)和酶对照组(D)(1/15摩尔磷酸缓冲液)。每组制备三份进行实验。从吸光值的测量,根据下面的方程计算酶抑制%。作为对照,使用的是曲酸,羟基醌,熊果苷,4-羟基茴香醚,抗坏血酸,松香油和羟基可的松。
资料显示利用70-80%丙酮在热水条件下和利用70-80%乙醇或甲醇在加热条件下获得的含有最高含量多酚的葡萄种子提取物与任何对照相比具有强力的抑制活性。方程I其中,A:没有GSE的对照在475纳米处的吸光值B:既没有GSE也没有酶的对照在475纳米处的吸光值C:含有GSE和酶的测试样品在475纳米处的吸光值D:没有酶的对照在475纳米处的吸光值。
表2
GSE对酪氨酸酶活性的抑制
提取的溶剂 提取的温度(℃) 含量(微克/毫升) %抑制 |
水 80-95 50 30.010%已醇 30 50 7.040%已醇 30 50 28.370,80%已醇 30 50 29.410%已醇 60-80 50 15.140%已醇 60-80 50 30.870,80%已醇 60-80 50 58.199%已醇 60-80 50 61.110%丙酮 30 50 7.140%丙酮 30 50 31.870,80%丙酮 30 50 5210%甲醇 60-80 50 15.140%甲醇 60-80 50 25.270,80%甲醇 60-80 50 56.2 |
表3
对照对酪氨酸酶活性的抑制
实施例IIIGSE对黑色素生物合成的抑制活性
对照 含量(微克/毫升) %抑制 |
曲酸 50 51.0羟基醌 50 5.0熊果苷 50 7.04-羟基茴香醚 50 3.0抗坏血酸 50 20.0松香油 50 4.9羟基可的松 50 3.7 |
为了研究实施例1得到的粉末葡萄种子提取物对黑色素生物合成的抑制活性,利用了Streptomyces bikiniensis。在papavizas’s VDYA(15)斜面培养基中接种这一菌株,该培养基含有200毫升V-8汁(Cambell Soup公司,美国),2克葡萄糖,2克酵母提取物,1克CaCO3,2克细菌培养琼脂,和800毫升蒸馏水。在28℃温育2星期后,在斜面培养基中加入2毫升蒸馏水,用金属针刮下气生的菌丝形成的孢子,得到孢子悬浮液,然后在冷冻温度储存在无菌试管中。
将含有葡萄糖1.5%,L-酪氨酸0.05%,L-精氨酸0.1%,K2HPO4 0.05%,MgSO4,7H2O 0.05%,NaCl 0.05%,FeSO4.7H2O 0.001%,细菌酵母提取物0.2%和细菌琼脂2%的酪氨酸琼脂(ISP号7)高压灭菌,在每盘(90毫米i.d.)注入40毫升的量,并固化。在这样制备的各个琼脂平板上,加入0.4毫升S.bikiniensis孢子悬浮液,利用玻璃弯曲棒均一地涂布。干燥固体培养基的表面。在浸泡在测试组后,将直径8毫米的纸片(Toyo Roshi Kasha有限公司,日本)放在培养基上。在28℃温育48小时导致出现抑制区。在平板的背面测量黑色素合成的抑制区的大小。作为对照,使用的是曲酸,羟基醌,熊果苷和4-羟基茴香醚。
利用热水,70-80%丙酮,70-80%乙醇和70-80%甲醇获得的葡萄种子提取物形成相对大而清楚的抑制区,如图2所示。
表4
在S.bikiniesis中GSE对黑色素生物合成的抑制
提取溶剂 提取温度(℃) 浓度(%) 抑制区(毫米) |
水 95 1 20.010%已醇 30 1 13.040%已醇 30 1 14.070,80%已醇 30 1 16.010%已醇 80 1 13.040%已醇 80 1 18.070,80%已醇 80 1 30.099%已醇 75 1 16.010%丙酮 30 1 12.040%丙酮 30 1 19.070,80%丙酮 30 1 23.010%甲醇 80 1 12.040%甲醇 80 1 17.079,80%甲醇 80 1 22.0 |
表5在S.bikiniensis中对照对黑色素生物合成的抑制百分数
制备实施例I
对照 含量(%) 抑制区(毫米) |
曲酸 1 11羟基醌 1 74熊果苷 1 164-羟基茴香醚 1 72 |
如下给出含有葡萄种子提取物的柔润洗液的配方。利用75%乙醇在实施例I的加热条件下获得用于这一目的的葡萄种子提取物。重量份葡萄种子提取物 0.01
甘油 3.0
丁二醇 12.0
丙二醇 12.0羧基乙烯基聚合物 0.1
乙醇 10.0
三乙醇胺 0.1
防腐剂 痕量
色素 痕量
香料 痕量蒸馏水加到100重量份制备实施例II
如下给出含有葡萄种子提取物的柔润洗液的配方。用于这一目的的葡萄种子提取物与制备实施例I的相同。重量份葡萄种子提取物 0.01
石蜡 4.0聚溶剂合物60 1.5Sorbi tance squiolate 0.5液体石蜡 5.0角鲨烯 5.0辛基/葵基甘油三酯 5.0
甘油 3.0
丁二醇 13.0
丙二醇 13.0羧基乙烯基聚合物 0.1三乙醇胺 0.2防腐剂 痕量色素 痕量香料 痕量蒸馏水加到100重量份制备实施例III
如下给出了含有葡萄种子提取物的营养乳液的配方。用于这一目的的葡萄种子提取物与制备实施例I的相同。重量份
葡萄种子提取物 0.005
蜡 10.0
聚溶剂合物 60 1.5
Sorbitance squiolate 0.5
液体石蜡 10.0
角鲨烯 5.0辛基/葵基甘油三酯 5.0
甘油 5.0
丁二醇 13.0
丙二醇 13.0
三乙醇胺 0.2
防腐剂 痕量
色素 痕量
香料 痕量蒸馏水加到100重量份制备实施例IV
如下给出含有葡萄种子提取物的按摩乳液的配方。用于这一目的的葡萄种子提取物与制备实施例I相同。重量份
葡萄种子提取物 0.005
蜡 10.0
聚溶剂合物60 0.8
Sorbi tance squiolate 0.5
液体石蜡 40.0
角鲨烯 5.0辛基/葵基甘油三酯 4.0
甘油 5.0
丁二醇 13.0
丙二醇 13.0
三乙醇胺 0.2
防腐剂 痕量
色素 痕量
香料 痕量蒸馏水加到100重量份。制备实施例V
如下给出含有葡萄种子提取物的包装的配方。用于这一目的的葡萄种子提取物与制备实施例I的相同。重量份
葡萄种子提取物 0.005
聚乙烯基乙醇 13.0
羧甲基纤维素钠 0.2
尿囊素 0.1
壬基苯醚 0.3
防腐剂 痕量
色素 痕量
香料 痕量蒸馏水加到100重量份实验实施例I抑制皮肤上的色素
将所有20个健康男人和妇女测试者的手臂包裹起来,除了前臂上2×2厘米2的预定面积,接着在每块暴露的皮肤离两个光源10厘米的距离辐射紫外光,光源如Toshiba,Japan销售的“FL20S BLB”和“FL20S E-30”,能量为0.8×107erg/厘米2。辐射每天进行一次,总共3天。在辐射之前,暴露的皮肤用70%异丙基乙醇溶液清洁。在辐射后,将制备实施例I-V的制剂用于紫外辐射的皮肤3次一天,总共3星期。然后,肉眼观察确定色素的变化,并与那些对照比较(不用制剂的)。本发明的制剂对色素的抑制效果分成良好,有效和无效级别。下面的表6给出了结果。
表6
制剂 良好(人) 有效(人) 无效(人) |
制剂I 2 11 7制剂II 2 12 6制剂III 3 13 4制剂IV 2 13 5制剂V 1 13 6 |
在表6的数据中可以看到本发明的制剂显示了对色素的良好的抑制活性,因为至少65%的测试者的结果是“有效”或“良好”。
正如本文前面所述,从天然物质制备的本发明的葡萄种子提取物具有对酪氨酸酶的强力的抑制活性而没有副作用,以致在葡萄种子提取物的影响下,可以良好的效果抑制黑色素的生物合成。所以,葡萄种子提取物可用作化妆品,具有抑制黑色素生物合成,预防皮肤老化,保护皮肤和美白皮肤的功能,可用作药物试剂用于预防和治疗变色,雀斑,斑点和怀孕期间的色素沉着,和用作防止食物变黑的食物添加剂。
本发明已经通过说明的方式进行了叙述,所使用的术语应被理解为用于叙述而不用于限制。
基于上面的陈述,可以对本发明进行许多的修改和变化。所以在权利要求的范围内,可以通过具体描述的方式以外的方式实施本发明。
Claims (6)
1.一种具有针对酪氨酸酶的抑制活性的葡萄种子提取物,它是通过用水或有机溶剂萃取葡萄种子制备的。
2.如权利要求1所述的葡萄种子提取物,其中所述的有机溶剂是60-90%乙醇,甲醇或丙酮,并在热水条件下或加热条件下用于提取。
3.如权利要求1所述的葡萄种子提取物,其中它被用作化妆品的有效成分用于抑制黑色素生物合成,预防皮肤老化,保护皮肤或美白皮肤。
4.如权利要求1所述的葡萄种子提取物,其中它被用作抑制黑色素生物合成的药物组合物的有效成分。
5.如权利要求4所述的葡萄种子提取物,其中它是变色,雀斑,斑点或怀孕期间的色素沉着的治疗剂。
6.一种食品添加剂,含有作为有效成分的权利要求1所述的葡萄种子提取物,以预防食物包括水果,蔬菜和鱼的变色。
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WO2002011744A1 (fr) * | 2000-07-27 | 2002-02-14 | Shanghai Beijing Medical University Biology Science And Technology Co., Ltd. | Capsule renfermant des antioxydants de type opc (oligomeres procyanidoliques ) a base d'extrait de pepins de raisin et son procede de preparation |
CN102958500A (zh) * | 2010-06-30 | 2013-03-06 | 雀巢产品技术援助有限公司 | 咖啡酰酒石酸及衍生物在食品或饮料中用于调节皮肤色素沉着的用途 |
CN113234049A (zh) * | 2021-04-16 | 2021-08-10 | 广州纳丽生物科技有限公司 | 一种基于葡萄籽提取的酪氨酸酶抑制剂及其提取方法和应用 |
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FR2808190B1 (fr) * | 2000-04-28 | 2002-06-21 | Oreal | Extrait de vegetal de l'espece vitis vinifera comme inhibiteur de no-synthase et utilisations |
ES2172475B1 (es) * | 2001-03-02 | 2003-12-16 | Raoul J Hermitte | Composiciones cosmeticas obtenidas a partir de plantas del genero vitis y de alfahidroxiacidos. |
KR100409041B1 (ko) * | 2001-03-09 | 2003-12-18 | 학교법인 청강학원 | 지방이 제거된 포도씨 추출물로 코팅된 쌀 |
KR20030023172A (ko) * | 2001-09-12 | 2003-03-19 | 주식회사 퓨쳐바이오테크 | 과일활성성분 추출물 및 그 제조방법 |
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US20150272863A1 (en) * | 2014-03-25 | 2015-10-01 | Active Concepts, LLC | H3 antagonist by-product, its manufacture, and method of using by-product to reduce pigmentation in skin |
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-
1998
- 1998-11-27 KR KR1019980051189A patent/KR20000034037A/ko not_active Application Discontinuation
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Publication number | Priority date | Publication date | Assignee | Title |
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WO2002011744A1 (fr) * | 2000-07-27 | 2002-02-14 | Shanghai Beijing Medical University Biology Science And Technology Co., Ltd. | Capsule renfermant des antioxydants de type opc (oligomeres procyanidoliques ) a base d'extrait de pepins de raisin et son procede de preparation |
CN102958500A (zh) * | 2010-06-30 | 2013-03-06 | 雀巢产品技术援助有限公司 | 咖啡酰酒石酸及衍生物在食品或饮料中用于调节皮肤色素沉着的用途 |
CN103025308A (zh) * | 2010-06-30 | 2013-04-03 | 雀巢产品技术援助有限公司 | 咖啡酰酒石酸及衍生物在食品补充剂中用于调节皮肤色素沉着的用途 |
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