CN114920801B - 一种多肽及其多肽组合物和应用、制得的除皱乳液 - Google Patents
一种多肽及其多肽组合物和应用、制得的除皱乳液 Download PDFInfo
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Abstract
本发明提出了一种多肽及其多肽组合物和应用、制得的除皱乳液,属于生物技术领域。包括多肽1或多肽2。本发明两种多肽均具有较好的促进胶原蛋白分泌的功能,同时由于分子量较小,可以自由透过角质层,增加真皮层细胞的活力,加快细胞增殖,补充和修复皮肤表面流失的胶原蛋白,使皮下组织坚强,损伤(例如来自紫外线或氧化)迅速愈合,进而达到除皱抗衰老的目的,同时多肽1和多肽2的组合具有协同增效的作用。
Description
技术领域
本发明涉及生物技术领域,具体涉及一种多肽及其多肽组合物和应用、制得的除皱乳液。
背景技术
除皱抗衰老已经是医学科学研究的热点之一,更是化妆品行业的重中之重,据美国化妆品市场调查,市售的化妆品中保湿除皱的份额已经占到一半以上。随着国内老龄化比例的增大,国内对保湿除皱的护肤品需求越来越大。
皱纹的出现就是皮肤衰老的标志,皮肤衰老是机体老化的一部分,机体的老化在皮肤上表现的最为明显。衰老虽然是自然规律,但也受其他因素影响,如生活习惯、紫外线、经常性夸张的表情、缺乏运动、皮肤缺水干燥或环境和心理因素等。
目前化妆品市场保湿除皱的产品种类非常多,但持久缓慢释放效果与预期的相差甚远,而且经常性的使用该类产品会对皮肤造成负担以及活性成分的浪费。因此,对保湿除皱活性成分的长时间释放的探究成为攻克现有保湿除皱产品不足的关键。
发明内容
本发明的目的在于提出一种多肽及其多肽组合物和应用、制得的除皱乳液,具有较好的促进胶原蛋白分泌的功能,同时由于分子量较小,可以自由透过角质层,增加真皮层细胞的活力,加快细胞增殖,补充和修复皮肤表面流失的胶原蛋白,使皮下组织坚强,损伤(例如来自紫外线或氧化)迅速愈合,进而达到除皱抗衰老的目的,多肽1和多肽2的组合具有协同增效的作用。
本发明的技术方案是这样实现的:
本发明提供一种多肽,包括多肽1或多肽2,所述多肽1具有以下序列:Ala-Glu-Lys-Glu-Met-Asp-Glu-Arg-Tyr(SEQ ID No.1);所述多肽2具有以下序列:Trp-Thr-Ile-Val-Glu-His-Ile-Glu-Arg-Leu-Asn(SEQ ID No.2)。
本发明进一步保护一种多肽组合物,包括上述的多肽1和多肽2。
作为本发明的进一步改进,所述多肽1和多肽2的质量比为(3-5):1。
本发明进一步保护一种多肽衍生物,所述多肽衍生物为上述的多肽1或多肽2的修饰产品。
本发明进一步保护一种多肽衍生物组合物,所述多肽衍生物组合物包括上述的多肽1和多肽2的修饰产品,质量比为(2-7):1。
本发明进一步保护一种组合物,包括上述的多肽1、多肽2中的至少一种和上述的多肽1、多肽2的修饰产品中的至少一种的组合物,以及分散载体。
作为本发明的进一步改进,所述分散载体包括水、缓冲盐溶液、脂肪醇、固体蜡、乙二醇、甘油或有机酯中的一种或多种。
本发明进一步保护一种组合物,包括上述的组合物及至少一种治疗某疾病的有效剂量的药物活性成分。
本发明进一步保护一种上述的多肽或上述多肽组合物或上述多肽衍生物或上述多肽衍生物组合物在制备外用护肤品中的应用。
本发明进一步保护一种除皱乳液,由以下原料按重量份制备而成:上述多肽组合物0.5-1份、霍霍巴油2-5份、肉豆蔻酸异丙酯3-4份、PEG-7甘油椰油酸酯2-4份、卵磷脂10-15份、卡波姆5-7份、甘油5-7份、丙二醇3-5份、PEG-400 1-2份、透明质酸钠0.5-1份、神经酰胺0.5-1份、柠檬酸0.05-1份,去离子水30-60份。
本发明具有如下有益效果:本发明提供了一种新的多肽序列以及多肽组合物,包括多肽1和多肽2,这两种多肽具有较好的促进胶原蛋白分泌的功能,同时由于分子量较小,可以自由透过角质层,增加真皮层细胞的活力,加快细胞增殖,补充和修复皮肤表面流失的胶原蛋白,使皮下组织坚强,损伤(例如来自紫外线或氧化)迅速愈合,进而达到除皱抗衰老的目的,多肽1和多肽2的组合具有协同增效的作用。
本发明制得的除皱乳液包含有润肤剂成分,包括甘油、丙二醇、PEG-400,在皮肤上有很好的铺展性,在表面形成一层膜,起到滋润和保湿的作用,同时透明质酸钠、神经酰胺和多肽组合物渗透到皮肤内部,缓慢释放,进一步起到长效保湿和除皱的作用。本发明产品稳定,保质期长,制备方法简单,生产成本低。
具体实施方式
下面将对本发明实施例中的技术方案进行清楚、完整地描述,显然,所描述的实施例仅仅是本发明一部分实施例,而不是全部的实施例。基于本发明中的实施例,本领域普通技术人员在没有做出创造性劳动前提下所获得的所有其他实施例,都属于本发明保护的范围。
本发明的发明人从具有美容功效的植物中提取了活性蛋白,并通过多步骤酶解和筛选,获得了数十种功能性多肽。
本发明一实施例提供了一种多肽,包括多肽1或多肽2;
所述多肽1具有以下序列:Ala-Glu-Lys-Glu-Met-Asp-Glu-Arg-Tyr(SEQ IDNo.1);
所述多肽2具有以下序列:Trp-Thr-Ile-Val-Glu-His-Ile-Glu-Arg-Leu-Asn(SEQID No.2)。
所述多肽为短肽,能够被较好的吸收,具有较好的促进胶原蛋白分泌的功能,同时由于分子量较小,可以自由透过角质层,增加真皮层细胞的活力,加快细胞增殖,补充和修复皮肤表面流失的胶原蛋白,使皮下组织坚强,损伤(例如来自紫外线或氧化)迅速愈合,进而达到除皱抗衰老的目的。
如本领域技术人员所公知的,上述多肽中,各氨基酸缩写所代表的氨基酸如表1所示:
表1:各氨基酸缩写所代表的氨基酸
本发明另一实施例,提供了一种多肽组合物,其特征在于,包括多肽1和多肽2,质量比为(3-5):1。
本发明另一实施例提供了一种多肽衍生物,所述多肽衍生物为如上所述的多肽1或多肽2的修饰产物。
如本文所用的术语“衍生物”是指母体分子如多肽的一种变型。例如多肽的衍生物,可以包括相对于多肽而言一个或多个氨基酸被取代的一种变型,优选为保守型变异序列。还可以包括对于多肽的修饰,包含但不限于非天然存在的氨基酸、D型氨基酸、氨基和/或羧基末端(N-或C-末端)修饰的氨基酸,特别是对于在N-末端的氨基和/或C-末端的羧基的修饰、脂肪酸修饰、肽模拟物和伪肽等诸如此类的修饰物。
如本文所述,本发明的多肽可以通过改造修饰,形成多肽衍生物。如本文所述,本发明的多肽可以通过改造修饰,形成多肽衍生物。本发明的多肽或其衍生物可以使用本领域技术人员所熟知的方法制备,包括众所周知的化学合成的方法。
具体地,本发明所述保守型变异序列是指通过一个或两个氨基酸保守性替换获得的序列,其中所述保守性替换是指性质相似的另一个氨基酸取代指定的氨基酸。例如,可以被认为是保守型替换(性质相似)的例子包括但不限于:
a)丙氨酸、丝氨酸和苏氨酸;
b)谷氨酸和天冬氨酸;
c)天冬酰胺和谷氨酰胺;
d)精氨酸和赖氨酸;
e)异亮氨酸、亮氨酸、蛋氨酸和;
f)苯丙氨酸,酪氨酸和色氨酸。
本发明另一实施例,提供了一种多肽衍生物组合物,包括上述的多肽1和多肽2的修饰产品,质量比为(2-7):1。
本发明另一实施例,提供了一种组合物,包括上述的多肽1、多肽2中的至少一种和上述的多肽1、多肽2的修饰产品中的至少一种的组合物,以及分散载体。所述分散载体包括水、缓冲盐溶液、脂肪醇、固体蜡、乙二醇、甘油或有机酯中的一种或多种。将多肽通过分散载体进行分散液化,尤其适用于化妆品或护肤品领域,能够提高其与皮肤的接触附着和渗透效率。
本发明另一实施例,提供了一种组合物,包括上述的组合物及至少一种治疗某疾病的有效剂量的药物活性成分。
由于所述多肽本身链段较短,具有较好的可吸收特性,通过将组合物与治疗皮肤损伤的药物活性成分联合使用,促进其药效的发挥,明显提高药效。
本发明的另一实施例提供了如上所述的多肽、多肽组合物、多肽衍生物、多肽衍生物组合物在制备外用护肤品中的应用。
实施例1
一种除皱乳液,由以下原料按重量份制备而成:多肽组合物0.5份、霍霍巴油2份、肉豆蔻酸异丙酯3份、PEG-7甘油椰油酸酯2份、卵磷脂10份、卡波姆5份、甘油5份、丙二醇3份、PEG-400 1份、透明质酸钠0.5份、神经酰胺0.5份、柠檬酸0.05份,去离子水30份。所述多肽组合物包括多肽1和多肽2,所述多肽1和多肽2的质量比为3:1。
制备方法:
(1)将卵磷脂、卡波姆、甘油、丙二醇、PEG-400搅拌混合,300W超声10min后形成乳化剂;
(2)将多肽组合物、霍霍巴油、肉豆蔻酸异丙酯、PEG-7甘油椰油酸酯混合均匀后,加热至35℃,形成油相;
(3)将透明质酸钠、神经酰胺和1/3的去离子水混合均匀,形成水相;
(4)将柠檬酸加入剩余的去离子水中,得到pH调剂剂;
(5)将步骤(2)中的油相和步骤(1)中的乳化剂搅拌混合,逐滴加入步骤(3)的水相中,1000r/min搅拌状态下加入步骤(4)得到的pH调节剂,继续搅拌15h,制得除皱乳液。
实施例2
一种除皱乳液,由以下原料按重量份制备而成:多肽组合物1份、霍霍巴油5份、肉豆蔻酸异丙酯4份、PEG-7甘油椰油酸酯4份、卵磷脂15份、卡波姆7份、甘油7份、丙二醇5份、PEG-400 2份、透明质酸钠1份、神经酰胺1份、柠檬酸1份,去离子水60份。所述多肽组合物包括多肽1和多肽2,所述多肽1和多肽2的质量比为5:1。
制备方法与实施例1相同。
实施例3
一种除皱乳液,由以下原料按重量份制备而成:多肽组合物0.7份、霍霍巴油3.5份、肉豆蔻酸异丙酯3.5份、PEG-7甘油椰油酸酯3份、卵磷脂12份、卡波姆6份、甘油6份、丙二醇4份、PEG-400 1.5份、透明质酸钠0.7份、神经酰胺0.7份、柠檬酸0.2份,去离子水45份。所述多肽组合物包括多肽1和多肽2,所述多肽1和多肽2的质量比为4:1。
制备方法与实施例1相同。
对比例1
与实施例3相比,多肽组合物由多肽1替代,其他条件均不改变。
对比例2
与实施例3相比,多肽组合物由多肽2替代,其他条件均不改变。
对比例3
与实施例3相比,多肽组合物由除皱活性成分辅酶Q10替代,其他条件均不改变。
测试例1稳定性试验
将实施例1-3和对比例1-3制得的除皱乳液取30mL,分成3份,每份10ml放于密封的玻璃瓶内,分别置于4℃、25℃和35℃下放置半年,分别在1月、3月和6月时,取样观察,均保持稳定状态,未见分层或沉淀出现。
测定实施例1-3和对比例1-3制得的除皱乳液的物理性能,包括折射率、pH值、粘度、电导率和表面张力,折射率用阿贝折光仪测定;pH计测量pH值;粘度用布氏粘度仪测定;电导率用电导仪测定;表面张力用表面张力仪测定;所有样品测定时都在25℃,湿度为65%条件下测定。结果如表2所示。
表2:稳定性试验结果
由表2可知,本发明的除皱乳液具有良好的物理性能,pH值为弱酸性,接近人的皮肤的pH值,粘度低、表面张力小,表明该除皱乳液易于在皮肤上铺展。
测试例2效果试验
选择36-52岁的60名女士,分为6组,每组10人,连续试用30天,对比分析评价实施例1-3和对比例1-3制得的除皱乳液的除皱效果。其中,所述的除皱效果为面部皱纹、眼部皱纹、抬头纹、细纹、皮肤弹性等的改善情况,结果见表3。
表3:除皱效果
由上表可知,本发明制得的除皱乳液具有明显的除皱效果,能明显改善面部皱纹、眼部皱纹、抬头纹、细纹,提高皮肤弹性,这两种多肽具有较好的促进胶原蛋白分泌的功能,同时由于分子量较小,可以自由透过角质层,增加真皮层细胞的活力,加快细胞增殖,补充和修复皮肤表面流失的胶原蛋白,使皮下组织坚强,损伤(例如来自紫外线或氧化)迅速愈合,进而达到除皱抗衰老的目的,多肽1和多肽2的组合具有协同增效的作用。
以上所述仅为本发明的较佳实施例而已,并不用以限制本发明,凡在本发明的精神和原则之内,所作的任何修改、等同替换、改进等,均应包含在本发明的保护范围之内。
序列表
<110> 澳大利亚健康产业有限公司
<120> 一种多肽及其多肽组合物和应用、制得的除皱乳液
<130> 22SG1F1889
<160> 2
<170> PatentIn version 3.5
<210> 1
<211> 9
<212> PRT
<213> 人工序列
<220>
<223> 肽1
<400> 1
Ala Glu Lys Glu Met Asp Glu Arg Tyr
1 5
<210> 2
<211> 11
<212> PRT
<213> 人工序列
<220>
<223> 肽2
<400> 2
Trp Thr Ile Val Glu His Ile Glu Arg Leu Asn
1 5 10
Claims (5)
1.一种多肽,其特征在于,其为多肽1或多肽2,所述多肽1的序列如下:Ala-Glu-Lys-Glu-Met-Asp-Glu-Arg-Tyr(SEQ ID No.1);所述多肽2的序列如下:Trp-Thr-Ile-Val-Glu-His-Ile-Glu-Arg-Leu-Asn(SEQ IDNo.2)。
2.一种多肽组合物,其特征在于,包括如权利要求1中所述的多肽1和多肽2。
3.根据权利要求2所述多肽组合物,其特征在于,所述多肽1和多肽2的质量比为(3-5):1。
4.如权利要求1所述的多肽或权利要求2所述多肽组合物在制备外用护肤品中的应用。
5.一种除皱乳液,其特征在于,由以下原料按重量份制备而成:权利要求3所述多肽组合物0.5-1份、霍霍巴油2-5份、肉豆蔻酸异丙酯3-4份、PEG-7甘油椰油酸酯2-4份、卵磷脂10-15份、卡波姆5-7份、甘油5-7份、丙二醇3-5份、PEG-400 1-2份、透明质酸钠0.5-1份、神经酰胺0.5-1份、柠檬酸0.05-1份,去离子水30-60份。
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