CN1829496A - 精胺和/或亚精胺在食用、药用或美容用组合物中对抗皮肤老化的用途 - Google Patents
精胺和/或亚精胺在食用、药用或美容用组合物中对抗皮肤老化的用途 Download PDFInfo
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- CN1829496A CN1829496A CNA200480021680XA CN200480021680A CN1829496A CN 1829496 A CN1829496 A CN 1829496A CN A200480021680X A CNA200480021680X A CN A200480021680XA CN 200480021680 A CN200480021680 A CN 200480021680A CN 1829496 A CN1829496 A CN 1829496A
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- spermidine
- compositions
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- amino
- vitamin
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- ATHGHQPFGPMSJY-UHFFFAOYSA-N spermidine Chemical compound NCCCCNCCCN ATHGHQPFGPMSJY-UHFFFAOYSA-N 0.000 title claims abstract description 52
- PFNFFQXMRSDOHW-UHFFFAOYSA-N spermine Chemical compound NCCCNCCCCNCCCN PFNFFQXMRSDOHW-UHFFFAOYSA-N 0.000 title claims abstract description 34
- 239000000203 mixture Substances 0.000 title claims abstract description 27
- 229940063673 spermidine Drugs 0.000 title claims abstract description 26
- 229940063675 spermine Drugs 0.000 title claims abstract description 17
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- 235000005911 diet Nutrition 0.000 title abstract 3
- 230000000378 dietary effect Effects 0.000 title abstract 3
- 238000002360 preparation method Methods 0.000 claims abstract description 5
- GVJHHUAWPYXKBD-UHFFFAOYSA-N (±)-α-Tocopherol Chemical compound OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 claims description 12
- 239000013522 chelant Substances 0.000 claims description 12
- LXNHXLLTXMVWPM-UHFFFAOYSA-N pyridoxine Chemical compound CC1=NC=C(CO)C(CO)=C1O LXNHXLLTXMVWPM-UHFFFAOYSA-N 0.000 claims description 11
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 claims description 8
- 150000001413 amino acids Chemical class 0.000 claims description 8
- YBJHBAHKTGYVGT-ZKWXMUAHSA-N (+)-Biotin Chemical compound N1C(=O)N[C@@H]2[C@H](CCCCC(=O)O)SC[C@@H]21 YBJHBAHKTGYVGT-ZKWXMUAHSA-N 0.000 claims description 7
- 150000003839 salts Chemical group 0.000 claims description 7
- 229940011671 vitamin b6 Drugs 0.000 claims description 7
- WRROLJSGZKCWGR-UHFFFAOYSA-N 3-(4-aminobutylamino)propylazanium;chloride Chemical compound Cl.NCCCCNCCCN WRROLJSGZKCWGR-UHFFFAOYSA-N 0.000 claims description 5
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- FAPWYRCQGJNNSJ-UBKPKTQASA-L calcium D-pantothenic acid Chemical compound [Ca+2].OCC(C)(C)[C@@H](O)C(=O)NCCC([O-])=O.OCC(C)(C)[C@@H](O)C(=O)NCCC([O-])=O FAPWYRCQGJNNSJ-UBKPKTQASA-L 0.000 claims description 5
- 230000036571 hydration Effects 0.000 claims description 5
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- ZZZCUOFIHGPKAK-UHFFFAOYSA-N D-erythro-ascorbic acid Natural products OCC1OC(=O)C(O)=C1O ZZZCUOFIHGPKAK-UHFFFAOYSA-N 0.000 claims description 4
- BUGBHKTXTAQXES-UHFFFAOYSA-N Selenium Chemical compound [Se] BUGBHKTXTAQXES-UHFFFAOYSA-N 0.000 claims description 4
- 229930003268 Vitamin C Natural products 0.000 claims description 4
- 229930003427 Vitamin E Natural products 0.000 claims description 4
- 229910052802 copper Inorganic materials 0.000 claims description 4
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- WIGCFUFOHFEKBI-UHFFFAOYSA-N gamma-tocopherol Natural products CC(C)CCCC(C)CCCC(C)CCCC1CCC2C(C)C(O)C(C)C(C)C2O1 WIGCFUFOHFEKBI-UHFFFAOYSA-N 0.000 claims description 4
- 239000011572 manganese Substances 0.000 claims description 4
- 229910052748 manganese Inorganic materials 0.000 claims description 4
- RADKZDMFGJYCBB-UHFFFAOYSA-N pyridoxal hydrochloride Natural products CC1=NC=C(CO)C(C=O)=C1O RADKZDMFGJYCBB-UHFFFAOYSA-N 0.000 claims description 4
- 239000011669 selenium Substances 0.000 claims description 4
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- 235000019158 vitamin B6 Nutrition 0.000 claims description 4
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- RYGMFSIKBFXOCR-UHFFFAOYSA-N Copper Chemical compound [Cu] RYGMFSIKBFXOCR-UHFFFAOYSA-N 0.000 claims 2
- PWHULOQIROXLJO-UHFFFAOYSA-N Manganese Chemical compound [Mn] PWHULOQIROXLJO-UHFFFAOYSA-N 0.000 claims 2
- FFEARJCKVFRZRR-BYPYZUCNSA-N L-methionine Chemical compound CSCC[C@H](N)C(O)=O FFEARJCKVFRZRR-BYPYZUCNSA-N 0.000 claims 1
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- 229930182817 methionine Natural products 0.000 claims 1
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- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 4
- 235000013336 milk Nutrition 0.000 description 4
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- KIDHWZJUCRJVML-UHFFFAOYSA-N putrescine Chemical compound NCCCCN KIDHWZJUCRJVML-UHFFFAOYSA-N 0.000 description 4
- 238000012360 testing method Methods 0.000 description 4
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 3
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- NKJOXAZJBOMXID-UHFFFAOYSA-N 1,1'-Oxybisoctane Chemical compound CCCCCCCCOCCCCCCCC NKJOXAZJBOMXID-UHFFFAOYSA-N 0.000 description 2
- FLPJVCMIKUWSDR-UHFFFAOYSA-N 2-(4-formylphenoxy)acetamide Chemical compound NC(=O)COC1=CC=C(C=O)C=C1 FLPJVCMIKUWSDR-UHFFFAOYSA-N 0.000 description 2
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- 125000001295 dansyl group Chemical group [H]C1=C([H])C(N(C([H])([H])[H])C([H])([H])[H])=C2C([H])=C([H])C([H])=C(C2=C1[H])S(*)(=O)=O 0.000 description 2
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- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
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- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline
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Abstract
本发明涉及精胺和亚精胺作为活性成分在制备食用、药用或美容用组合物中的用途,所述组合物在人中用于皮肤和皮肤附属物的健康和美观,还涉及相关的施用于人的药用或食用或美容用组合物。
Description
本发明涉及称为精胺(N,N′-二(3-氨基丙基)四亚甲基二胺)和亚精胺(N-(3-氨基丙基)四亚甲基二胺)的聚胺的新用途。
在文献中已知,属于脂肪族聚胺类的化合物在控制细胞生长、分裂、分化和动物组织增殖的生物学机制中起决定性的作用。
所述聚胺主要包括腐胺、精胺和亚精胺等化合物。后两种化合物的名字是源于它们最初是在人的精子中被发现的这一事实。实际上,亚精胺几乎存在于所有体液(血液、唾液、泪液、乳汁)中。后来还在很多动物来源的食物(肉、鱼、蛋、奶、乳酪)和植物来源的食物(水果和蔬菜)中发现了亚精胺。它在人乳中的浓度特别高(在24小时期间中在乳汁中平均有约600微克亚精胺),它对婴儿具有非常重要的作用。事实上,在婴儿体内,消化道的粘膜尚未完全形成,乳汁中所含有的亚精胺可促进胃肠粘膜上皮的生长。
通过特定的氨基-丙基供体酶的作用可从亚精胺生物合成得到精胺,该酶将共同的前体腐胺首先转变成N-单氨基丙基衍生物(亚精胺),然后转变成N,N′-二氨基丙基对称衍生物(精胺)。因此,亚精胺是生物合成精胺的前体。
因此,亚精胺和精胺是重要的细胞生长和增殖因子。
根据本发明,现已令人惊讶地发现含有精胺或亚精胺的制剂无论是口服施用还是应用于皮肤均可刺激皮肤和皮肤附属物如体毛、毛发和指/趾甲的细胞,从而促进细胞的生长和再生。该结果的效果是既可改善皮肤及皮肤附属物的外观和功能特性,又可对抗老化。
因此,本发明的主题是原形或成盐形式的聚胺、即精胺和亚精胺作为活性成分在制备人食用、药用或美容用组合物中的用途,所述组合物用于保持皮肤和皮肤附属物的健康和美观以及对抗老化。
本发明的主题还有药用、食用或美容用组合物,所述组合物用于在人中保持皮肤和皮肤附属物的健康和美观以及对抗老化,其特征在于其包含精胺、亚精胺或它们的盐作为活性成分。
所述组合物可以包含游离或成盐形式的精胺或亚精胺或二者作为活性成分。
为了更好地理解本发明的特点和优势,现在描述产生所述发明的实验性研究的详细情况。
临床研究
该研究测定了皮肤和皮肤附属物的健康和功能的一些基本指标。为了验证被研究物质的效果,确定了下列被认为非常重要的参数并对其进行了评价:
水合作用
弹性
细胞更新
水合作用和弹性的评价
通过在20名知情同意的成年志愿者(年龄从18到55岁)中进行使用测试对产品的在体效果进行了评价。
在每名志愿者的前臂上选3个区域:
-一个区域应用被研究的含有亚精胺的产品;
-一个区域应用被研究的不含亚精胺的产品;
-一个区域作为对照区域。
将本发明的局部用组合物(含有亚精胺的组合物)和不含亚精胺的产品(安慰剂)给予受试者,受试者根据上述方法使用它们,每天2次,使用1个月。
在测试开始和结束时,对有效性进行以下仪器评价:
-用角质层测量仪(corneometer)评价皮肤水合作用
-用肤质测量仪(cutometer)评价皮肤弹性。
通过适当的统计学处理,将每个区域(产品、安慰剂、对照)在测试开始时记录的值与在测试结束时获得的数据进行比较。进一步将在用产品处理的区域获得的变化与在应用安慰剂的区域所记录的变化进行比较。
结果显示,在处理后所观察到的平均值与应用安慰剂后所观察到的相应值之间,皮肤水合作用的增加具有统计学显著性差异。通过用角质层测量仪所测量的电容来测定的水合作用程度增加超过10%,具有高度统计学显著性(p<0.001)。
在处理前和处理后的弹性值之间,用肤质测量仪记录的值也显示该参数具有统计学显著性差异(+20%;p<0.001),同时也考虑了安慰剂的效果。
细胞更新的评价
在每名志愿者的前臂上选3个区域,在每个区域上应用5%的丹磺酰氯的凡士林混悬液(闭合包扎20±4小时)。第二天,除去贴片,在石英UV灯下检查3个皮肤区域以评价由丹磺酰氯产生的荧光度。使用数值参比刻度对每个斑点的强度打分。
然后,将本发明的组合物和安慰剂给予受试者,建议如下进行应用:
-在第一个区域应用含有亚精胺的产品;
-在第二个区域应用不含亚精胺的产品;
-在第三个区域不应用任何产品,将其作为对照区域。
志愿者每天应用两次样品,并定时召回实验室直到荧光斑点完全消失。在测试开始和结束时,相应于所选的两个区域,用D-Squame(透明的粘性圆片)测量表面角质细胞的量。
将细胞更新的有效性表示为相对于对照区域的被处理区域(用产品或用安慰剂处理)中荧光消失所需要的天数。统计学分析显示细胞更新周期以20%的数量级缩短(p<0.01)。
实施例
现在对本发明组合物的一些非限制性实例进行描述。
实施例1
用于皮肤和指/趾甲健康和美观的口服食用组合物片剂
每片含有:
甲磺酰基甲烷(methyl sulfonyl methane) 200mg
三盐酸亚精胺 0.25mg
维生素C 61.86mg
维生素E(dl-α生育酚) 32.89mg
维生素B6(吡哆素) 3.65mg
d-泛酸钙(calcium d-Panthotenate) 4mg
d-生物素 0.23mg
锌氨基酸螯合物 37.5mg
铜氨基酸螯合物 12mg
锰氨基酸螯合物 22.5mg
硒酵母2000μg/g 13.75mg
微晶纤维素 120mg
磷酸氢钙二水合物 98.89mg
羟丙基甲基纤维素 52.5mg
硬脂酸镁 8mg
二氧化硅 3.5mg
实施例2
用于暴露于辐射的皮肤的健康和美观的口服食用组合物片剂
每片含有:
三盐酸亚精胺 0.25mg
泛酸钙 4mg
泛癸利酮 10mg
维生素C 62mg
维生素E(dl-α生育酚) 33mg
β-胡萝卜素 36mg
维生素B6(吡哆素) 3.65mg
d-生物素 0.225mg
锌氨基酸螯合物 37.5mg
铜氨基酸螯合物 12mg
锰氨基酸螯合物 17.5mg
磷酸氢钙二水合物 120mg
微晶纤维素 259.38mg
羟丙基甲基纤维素 56mg
硬脂酸镁 7mg
二氧化硅 1.75mg
实施例3
用于局部皮肤处理的美容用组合物
乳剂
100ml乳剂含有:
三盐酸亚精胺 0.02g
Emulgade SE(硬脂酸甘油酯,十六/十八醇聚氧乙烯(20)醚(Ceteareth-20),十六/十八醇聚氧乙烯(12)醚(Ceteareth-12),十六/十八醇(Cetearyl alcohol),
鲸蜡醇十六酸酯) 4.5g
十六/十八醇聚氧乙烯(20)醚 1g
椰油醇辛酸/癸酸酯 5g
二辛基醚(dicaprylyl ether) 5g
水 适量至100ml
实施例4
含遮光剂(sun filter)的用于局部皮肤处理的美容用组合物也可以以喷雾剂形式应用的洗剂
100ml洗剂含有:
三盐酸亚精胺 0.01g
Emulgade SE(硬脂酸甘油酯,十六/十八醇聚氧乙烯(20)醚,十六/十八醇聚氧乙烯(12)醚,十六/十八醇,鲸蜡醇十六酸酯) 3.9g
十六/十八醇聚氧乙烯(20)醚 3.1g
椰油醇辛酸/癸酸酯 7g
甲氧肉桂酸辛酯 4g
甲氧基肉桂酸异戊酯 6g
二苯酮-3 2g
生育酚 0.5g
甘油 5g
防腐剂,芳香剂 适量
水 64.5g
Claims (8)
1.游离或成盐形式的精胺和/或亚精胺作为活性成分在制备食用、药用或美容用组合物中的用途,所述组合物在人中用于皮肤和皮肤附属物的健康和美观、对抗其老化。
2.游离或成盐形式的精胺和/或亚精胺作为活性成分在制备食用、药用或美容用组合物中的用途,所述组合物在人中使用以便改善人皮肤下列性质中的至少一种:水合作用、弹性、细胞更新。
3.在人中施用用于皮肤和皮肤附属物健康和美观的药用或食用或美容用组合物,其特征在于其包含游离或成盐形式的精胺或亚精胺或二者作为活性成分。
4.药用或食用或美容用组合物,其在人中施用以便改善人皮肤下列性质中的至少一种:水合作用、弹性、细胞更新,其特征在于其包含游离或成盐形式的精胺或亚精胺或二者作为活性成分。
5.权利要求3和4的组合物,其特征在于其还包含甲磺酰基甲烷或甲硫氨酸、维生素C、维生素E、维生素B6、d-泛酸钙、d-生物素、锌(为氨基酸螯合物形式),铜(为氨基酸螯合物形式)、锰(为氨基酸螯合物形式)和有机硒源。
6.权利要求3和4的组合物,其特征在于其包含:
甲磺酰基甲烷 200mg
三盐酸亚精胺 0.25-0.5mg
维生素C 60-90mg
维生素E(dl-α生育酚) 33mg
维生素B6(吡哆素) 3.7mg
d-泛酸钙 4mg
d-生物素 0.23mg
锌(氨基酸螯合物形式) 7.5mg
铜(氨基酸螯合物形式) 1.25mg
锰(氨基酸螯合物形式) 2.25mg
硒(硒酵母形式) 0.03mg
7.权利要求3和4的组合物,其特征在于其适合于口服施用。
8.权利要求3和4的组合物,其特征在于其适合于局部施用,例如洗剂或乳膏剂。
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IT001570A ITMI20031570A1 (it) | 2003-07-31 | 2003-07-31 | Composizione per uso dietetico, farmaceutico o cosmetico |
PCT/EP2004/008572 WO2005013932A1 (en) | 2003-07-31 | 2004-07-30 | Use of spermine and/or spermidine against skin ageting in dietary, pharmaceutical or cosmetic compositions |
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EP (1) | EP1651175A1 (zh) |
JP (1) | JP2007500678A (zh) |
CN (1) | CN1829496B (zh) |
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CA (1) | CA2534102A1 (zh) |
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CN108684668A (zh) * | 2018-05-04 | 2018-10-23 | 华南农业大学 | 亚精胺盐在防治松材线虫病中的应用 |
CN108684668B (zh) * | 2018-05-04 | 2020-10-23 | 华南农业大学 | 亚精胺盐在防治松材线虫病中的应用 |
CN114786502A (zh) * | 2020-04-03 | 2022-07-22 | 三菱瓦斯化学株式会社 | 肌肉增强剂 |
CN113785975A (zh) * | 2021-09-09 | 2021-12-14 | 天津医科大学 | 精胺、亚精胺脂质体在抗氧化、抗衰老中的应用 |
CN113785975B (zh) * | 2021-09-09 | 2023-08-29 | 天津医科大学 | 精胺、亚精胺脂质体在抗氧化、抗衰老中的应用 |
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ITMI20031570A1 (it) | 2005-02-01 |
US20060252838A1 (en) | 2006-11-09 |
WO2005013932A1 (en) | 2005-02-17 |
EP1651175A1 (en) | 2006-05-03 |
CN1829496B (zh) | 2011-02-09 |
JP2007500678A (ja) | 2007-01-18 |
AU2004262499A1 (en) | 2005-02-17 |
CA2534102A1 (en) | 2005-02-17 |
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