CN115209868A - 用于治疗面部血管分布提高的植物提取物 - Google Patents
用于治疗面部血管分布提高的植物提取物 Download PDFInfo
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- CN115209868A CN115209868A CN202080079455.0A CN202080079455A CN115209868A CN 115209868 A CN115209868 A CN 115209868A CN 202080079455 A CN202080079455 A CN 202080079455A CN 115209868 A CN115209868 A CN 115209868A
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- galangal
- myricetin
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Abstract
本发明涉及高良姜(Alpinia officinarum)提取物用于治疗面部血管分布提高的用途。本发明还涉及包含选自以下的至少两种不同活性组分的组合的化妆品或药物制剂及其用于治疗面部血管分布提高的用途:高良姜提取物、杨梅素、肺衣酸和头花蓼(Persicaria capitata)提取物。本发明还涉及用于产生包含选自以下的至少两种不同活性组分的组合的化妆品或药物制剂的方法:高良姜提取物、杨梅素、肺衣酸和头花蓼提取物。
Description
本发明提供了用于治疗面部血管分布提高的高良姜(Alpinia officinarum)提取物。本发明还提供了用于治疗面部血管分布提高的化妆品或药物制剂,以及用于产生该制剂的方法。
背景技术
酒渣鼻(rosacea)是常见但知之甚少的长期慢性皮肤病症,其主要发生在面部,通常发生在鼻、脸颊和前额。酒渣鼻的成因尚不清楚,并且目前无法治愈。
酒渣鼻的症状通常始于患者遭受潮红发作,其中皮肤在短时间内变红。随着病症的发展,患者可出现其他症状,包括例如:灼热和刺痛感、永久性发红、斑点和/或皮肤中的小血管变得可见。酒渣鼻是复发性病症,这意味着患者可经历症状减轻或完全消失的一段时间,然后症状又复发。
酒渣鼻有四种亚型,包括:与面部发红、潮红和可见的血管相关的红斑毛细血管扩张性酒渣鼻(erythematotelangiectactic rosacea,ETR);与痤疮样爆发相关的丘疹脓疱性酒渣鼻(papulopustular rosacea);与鼻上皮肤增厚相关的肥大性酒渣鼻;以及与眼区上症状相关的眼酒渣鼻。
酒渣鼻可以通过使用常规药物的长期治疗在一定程度上得到控制。然而,由酒渣鼻引起的外观变化对患者有重大心理影响,例如导致失去信心。
已发现人激肽释放酶相关肽酶(KLK)在许多组织中的表达不同,并作为15种丝氨酸蛋白酶的亚组存在。在表皮中,激肽释放酶5(KLK5)和激肽释放酶7(KLK7)发挥主要功能。KLK5的活性通过复杂机制调节,其涉及多种因素例如其他蛋白酶、内源性抑制剂和生理环境。
在病变酒渣鼻皮肤中,激肽释放酶5(KLK5)水平提高,导致LL-37及其蛋白水解片段二者的水平提高。除了KLK5水平和LL-37及其蛋白水解片段的丰度提高之外,这些肽也不同于在正常个体中发现的那些。与正常的LL-37肽片段不同,这些异常肽控制功能例如白细胞趋化性、血管生成和胞外基质组分的表达。LL-37和其他肽水平的提高诱导见于酒渣鼻的临床表现,其包括炎症和面部血管分布提高。
因此,需要用于治疗酒渣鼻的化妆品或药物制剂,其与常规药物相比具有改善的效力。特别是需要能够阻断激肽释放酶5(KLK5)的活性或抑制其产生的化妆品或药物制剂。通过阻止激肽释放酶5的产生或阻断其活性,该制剂还应降低和/或阻止LL-37和异常肽片段的形成,从而抑制已发现与酒渣鼻中的主要临床发现相关的主要炎症级联反应。
发明内容
根据本发明的第一方面,提供了高良姜提取物用于治疗面部血管分布提高的用途。
高良姜,又称小高良姜,原产于中国东南部(广东、广西、海南)和印度支那。高良姜属于姜科(Zingiberaceae)家族,并为多年生草本植物,具有粗而匍匐的红褐色根状茎、线状渐尖的观赏叶以及在总状花序中的艳丽的白色花朵。
在一个实施方案中,高良姜提取物用于治疗酒渣鼻。
在一个实施方案中,高良姜提取物是激肽释放酶5(KLK5)的抑制剂。
已发现高良姜提取物能够治疗血管分布提高,并且尤其是酒渣鼻的症状(包括炎症和面部血管分布提高),与常规药物相比具有改善的效力。已发现高良姜提取物能够阻断激肽释放酶5(KLK5)的活性或抑制其产生,因此降低和/或阻止LL-37和异常肽片段的形成,从而抑制已发现与酒渣鼻中的主要临床发现相关的主要炎症级联反应。
高良姜提取物优选包含以下中的一种或更多种:山柰酚(kaempferol)、高良姜素、槲皮素、松属素、二氢高良姜素、3-O-甲基高良姜素、7-O-甲基高良姜素、山柰素(kaempferide)、5-羟基-7-(4'-羟基-3'-甲氧基苯基)-1-苯基-3-庚酮、3,5-二羟基-1,7-双(3,4-二羟基苯基)庚烷、良姜素B、高良姜素7-葡糖苷或其任意组合。
高良姜提取物可以以化妆品或药物制剂的形式提供,用于治疗面部血管分布提高,例如用于治疗酒渣鼻(例如用于治疗与酒渣鼻相关的症状,其包括例如炎症和面部血管分布提高)。
所述提取物优选为高良姜的根的提取物。
根据本发明的第二方面,提供了包含选自以下的至少两种不同组分的组合的化妆品或药物制剂:高良姜提取物、杨梅素(myricetin)、肺衣酸和头花蓼(Persicariacapitata,PCA)提取物。
所述提取物优选为头花蓼和/或高良姜的根的提取物。
在一个实施方案中,化妆品或药物制剂包含高良姜提取物和杨梅素。
在一个实施方案中,化妆品或药物制剂包含高良姜提取物和肺衣酸。
在一个实施方案中,化妆品或药物制剂包含高良姜提取物和头花蓼提取物。
在一个实施方案中,化妆品或药物制剂包含杨梅素和肺衣酸。
在一个实施方案中,化妆品或药物制剂包含肺衣酸和头花蓼提取物。
在一个实施方案中,化妆品或药物制剂包含杨梅素和头花蓼提取物。
根据本发明的第三方面,提供了如本文中所述的化妆品或药物制剂在治疗皮肤炎症中的用途,优选在治疗面部血管分布提高中的用途,例如在治疗酒渣鼻中的用途。
在一个实施方案中,如本文中所述的化妆品或药物制剂被用作激肽释放酶5(KLK5)抑制剂。
根据本发明的另一方面,提供了用于产生如本文中所述的化妆品或药物制剂的方法,该方法包括:
获得选自高良姜提取物、杨梅素、肺衣酸和头花蓼提取物的至少两种不同组分的至少两种来源;以及
将至少两种组分组合以提供化妆品或药物制剂。
根据本发明的又一个方面,提供了用于产生如本文中所述的化妆品或药物制剂的试剂盒(kit),该试剂盒包含:
选自高良姜提取物、杨梅素、肺衣酸和头花蓼提取物的至少两种不同组分的至少两种来源。
将参照附图对本发明的一些实施方案进行详细描述:
附图说明
图1A至C示出了三种高良姜(ALO)提取物的UHPLC/Q-ToF-MS色谱图;
图1A示出了高良姜(ALO)甲醇提取物的UHPLC/Q-ToF-MS色谱图;
图1B示出了高良姜(ALO)水提取物的UHPLC/Q-ToF-MS色谱图;和
图1C示出了高良姜(ALO)乙醇-水提取物的UHPLC/Q-ToF-MS色谱图;
图2示出了高良姜甲醇提取物的UHPLC/Q-ToF-MS色谱图以及提取物中已鉴定的化合物;
图3是举例说明协同作用和拮抗作用的模型线的等效线图;
图4示出了纯的化合物和提取物对酶激肽释放酶5的抑制百分比;
图5是包含杨梅素/高良姜(ALO)组合的制剂的等效线图;
图6是包含高良姜(ALO)和头花蓼(PCA)组合的制剂的等效线图;
图7示出了在用10μM杨梅素处理角质形成细胞24小时之后AQP3、CASP14和CLDN1的基因表达。将处理与赋于1的经载剂处理样品进行比较。统计在PRISM 5中进行,其中对ΔCt值使用重复测量单因素方差分析(one-way ANOVA)和Dunnett事后检验(Dunnet's posthoc test),p*≤0.05、p**≤0.01和p***≤0.001;
图8示出了使用HaCaT细胞在PAR2诱导的促炎性IL-8模型中的抗炎活性;和
图9示出了在真皮微血管内皮(DMVEC)细胞中IL-1β诱导的炎症模型中的杨梅素抗炎活性。
具体实施方式
实施例1-高良姜(ALO)的提取方法
使用三种不同的溶剂甲醇、水和50:50乙醇:水混合物来提取植物材料(高良姜)的根。如下所讨论的植物的提取方法对于所用的每种溶剂都是相同的。
称取约1g植物材料并置于50ml管中。向其添加20ml合适的溶剂(如上)。然后将管内的植物材料/溶剂混合物在室温下在超声波浴中声处理2×60分钟。然后将植物材料/溶剂混合物以2000rcf离心5分钟。然后将植物材料/溶剂混合物使用两个过滤器(在底部的1级(11μm)过滤器和在顶部的4级(20至25μm)过滤器)在Büchner上过滤,以获得高良姜提取物。首先使用旋转蒸发仪(温度=37℃,压力=50mbar)蒸发含有甲醇或乙醇的提取物的挥发性溶剂部分,然后冷冻干燥约4天。
表1示出了使用三种不同溶剂得到的高良姜的提取产率:
表1
提取物 | 提取溶剂 | 提取产率% |
高良姜-001 | MeOH | 10.7 |
高良姜-002 | H<sub>2</sub>O | 16.3 |
高良姜-003 | 50:50EtOH:H<sub>2</sub>O | 22.2 |
使用包含50:50乙醇和水EtOH:H2O混合物的溶剂制备的高良姜提取物得到22.2%的最高提取产率
实施例2-使用UHPLC/Q-ToF-MS进行的高良姜提取物的表征
制备三种溶液(对于根据实施例1高良姜的提取方法制备的每种提取物一种溶液)以通过LC/MS进行分析。所述三种溶液如下:
溶液1(高良姜-001):8.8mg/1mL 95:5H2O:ACN
溶液2(高良姜-002):7.4mg/1mL 95:5H2O:ACN
溶液3(高良姜-003):7.8mg/1mL 95:5H2O:ACN
每种溶液在分析之前使用0.22μm注射器过滤器过滤。
UHPLC分析如下进行:
UHPLC:1290Infinity
Q-ToF LC/MS:6520
方法:文库法
柱:Zorbax extend C18 2.1×150mm,1.8μm
柱温:35℃
流量:0.25mL/分钟
进样体积:20μL
UHPLC梯度结果在表2中示出:
表2
时间(分钟) | A%(H<sub>2</sub>O+0.1%FA) | B%(ACN+0.1%FA) |
0 | 98 | 2 |
10 | 98 | 2 |
70 | 40 | 60 |
90 | 2 | 98 |
95 | 2 | 98 |
96 | 98 | 2 |
Q-ToF离子源:-ESI
气体温度:350℃
干燥气体:8L/分钟
雾化器:40psig
Vcap:3500V
采集速率:8谱/秒
采集时间:125毫秒/谱
图1A至C中示出了三种提取物中每一种的谱。可以看出,三种提取物(使用实施例1中描述的三种不同溶剂系统)的谱非常相似。
使用甲醇制备的提取物(高良姜-001)来鉴定每种提取物中存在的化合物。这些化合物示于表3和图2中:
表3–使用甲醇作为溶剂的高良姜提取物(高良姜-001)中存在的化合物
实施例3-激肽释放酶5酶抑制测定
人组织激肽释放酶5(KLK5或hK5,也称为角质层胰蛋白酶)是在表皮中表达的丝氨酸蛋白酶。KLK5与KLK7和KLK14联合调节细胞脱落(脱屑),因为其能够降解形成角质层中细胞连接的胞外组分的蛋白质。
酶KLK5的活性通过其切割荧光肽底物Boc-VPR-AMC的能力来测量。该测定测量作为高荧光基团的AMC的形成(λexc=380nm;λem=460nm)
初步筛选测定根据经验证的标准方案进行,即用于KLK5酶抑制测定的SP-SR-201-v3。制剂中活性组分的组合根据经验证的标准方案进行,即用于等效线图分析的SP-SR-234。
使用等效线图分析,已使用两种方法来确定本发明制剂中两种活性组分的组合是否提供协同作用:
-筛选产生50%抑制的浓度
第一步是确定本发明制剂中每种单独活性组分(即活性组分A和活性组分B)的IC50。然后在Graph Pad Prism上追踪对于50%抑制的相加等效线(additive isobole),如图3所示。
将产生50%抑制的活性组分B的浓度与活性组分A的选定浓度进行插值。然后需要筛选在这些浓度下两种活性组分A和B的组合。
·如果结果显示50%的抑制,则意味着在那些浓度下,制剂的两种活性组分之间存在相加作用;或者
·如果结果显示<50%的抑制,则意味着制剂需要存在更浓缩的活性组分才能实现50%的抑制,即活性组分的组合具有拮抗作用;或者
·如果结果>50%的抑制,则意味着制剂中需要存在较少浓缩的活性组分以能实现50%的抑制,即活性组分的组合具有协同作用。
图4示出了许多活性组分和植物提取物包括肺衣酸、杨梅素、高良姜(ALO)和头花蓼(PCA)的激肽释放酶5的%抑制。
发现肺衣酸、杨梅素、高良姜(ALO)和头花蓼(PCA)显示出非常好的KLK5抑制百分比,并且确定了这些活性组分和提取物中的每一种的IC50,并且结果显示在表4中。
表4
化合物/提取物 | IC50(μM) |
肺衣酸 | 51.1 |
杨梅素 | 18.6 |
ALO | 8.8 |
PCA | 227.6 |
实施例4-包含两种活性组分杨梅素和高良姜提取物的制剂
图5的等效线图示出了本发明的包含杨梅素和高良姜提取物的许多不同制剂的抑制激肽释放酶5的IC50值。从等效线图可以看出,本发明制剂的IC50值低于相加等效线,因此可以看出,本发明的包含杨梅素和高良姜提取物的组合的制剂提供了对KLK5抑制活性的协同作用。
实施例5-包含两种活性组分高良姜提取物和PCA的制剂
图6的等效线图示出了本发明的包含高良姜提取物和PCA的许多不同制剂的抑制激肽释放酶5的IC50值。从等效线图可以看出,本发明制剂的IC50值低于相加等效线,因此可以看出,本发明的包含高良姜提取物和PCA组合的制剂提供了对KLK5抑制活性的协同作用。
实施例6-包含选自肺衣酸与高良姜提取物、头花蓼提取物或杨梅素一起的两种活性组分的制剂
发现了本发明的包含肺衣酸与高良姜提取物(ALO)、头花蓼提取物(PCA)或杨梅素的组合的制剂提供了高于50%的激肽释放酶5抑制的结果。因此,发现本发明的包含肺衣酸与高良姜(ALO)提取物、头花蓼提取物或杨梅素的组合的制剂对于制剂抑制KLK5的产生的能力具有协同作用,如表5和表6中所示。
表5
表6
已发现实施例3至6的提取物和制剂产生改善的激肽释放酶5抑制,并且对激肽释放酶5的抑制具有协同作用。因此,已显示本发明的提取物和制剂对治疗与酒渣鼻相关的症状例如炎症和面部血管分布提高具有改善的效力。
实施例7-杨梅素对屏障基因(barrier gene)的基因表达的作用
所分析的屏障基因是OCLN、AQP3 CLDN1、IVL、CASP14、KRT1、KRT10、FLG、PNPLA和TJP1。
使用qPCR来分析屏障基因的基因表达。将人表皮角质形成细胞(KC)在48孔板中培养并用活性物质处理24小时,然后提取RNA,随后合成cDNA,然后对所需基因进行qPCR。使用GAPDH作为管家基因。
评价杨梅素的作用。结果在图7中示出。图7示出了与经载剂处理样品相比,用杨梅素(10μm)进行处理在24小时之后上调了三种屏障基因(AQP3、CASP14和CLDN1),具有统计学显著性。基因表达的提高指示皮肤中皮肤屏障的改善。
实施例8-肺衣酸作为抗炎剂的作用
TRPV1是重要的离子通道,并且已表明其在敏感皮肤中过度表达。TRPV1可直接或通过PAR2间接地被激活。通过PAR2靶向TRPV1可以在体外通过使用导致炎性IL-8分泌的PAR2特异性激动肽(SLIGKV-NH2)完成。
该研究的目的是通过靶向HaCaT角质形成细胞细胞系中的PAR2来诱导炎性应答,并测试肺衣酸(Lobaric acid,L.A)抑制PAR2驱动的IL-8的抗炎潜力。
-将HaCaT细胞用在T75中培养的80%汇合细胞的相应培养基平板接种到48孔格式中。(稀释系数:1:8)
-24小时之后或当细胞达到50%汇合时,在无FBS的DMEM培养基中开始饥饿
-饥饿之后24小时,在完全培养基(DMEM中5%FBS)中用肺衣酸(3uM)预处理细胞,并且对照孔用对照拮抗肽(ENMD-1068,100μM)以阻断PAR 2。
-预处理之后30分钟添加PAR2激动肽(SLIGKV-NH2,100uM)
-处理之后24小时收集上清液以用于ELISA。
图8提供了(以下组:UT(未经处理)、PAR2 Ago(用激动肽进行PAR2刺激)、PAR2+Antago(对照,用拮抗肽预处理降低PAR2表达)、PAR2+肺衣酸(在PAR2刺激之前进行L.A预处理)的)IL-8ELISA结果,其示出了两个相同的独立实验的代表性数据。
如图8中所示,PAR 2在HaCaT细胞中诱导IL-8上调,而阳性对照PAR2拮抗肽显著下调IL-8。肺衣酸显著抑制PAR2诱导的IL-8,并因此被认为可用于治疗与炎症相关的敏感皮肤。
实施例9-杨梅素作为抗炎剂的作用
-在6孔格式中的CADMEC培养基(现成的)中培养人微血管内皮细胞(Humanmicrovascular endothelial cell,HMVEC)。
-当达到80%汇合时,将细胞接种到48孔格式中以用于实验(从6孔格式板的1个孔分板接种(split)到48孔培养板格式的8个孔中)。
-用杨梅素(25μM)预处理细胞。
-预处理之后2.5小时,添加重组细胞因子IL/1b(50pg/ml)。
-处理之后24小时,收集上清液以用于ELISA测定。
图9示出了以下组的IL-8ELISA结果:UT(未经处理)、IL-1b(重组IL-1b刺激)、IL-1b+M(IL-1b+杨梅素)(用IL-1b诱导)。
如图9中所示,IL-1b在HMVEC和杨梅素预处理中诱导IL-8上调,显著抑制细胞因子诱导。因此,已表明杨梅素可用于治疗与促炎细胞因子相关的敏感皮肤发红。
Claims (17)
1.高良姜(Alpinia officinarum)提取物用于治疗面部血管分布提高的用途。
2.如权利要求1所述的提取物用于治疗酒渣鼻的用途。
3.如权利要求1和2中任一项所述的提取物的用途,其中所述提取物是激肽释放酶5(KLK5)的抑制剂。
4.如权利要求1至3中任一项所述的提取物的用途,其中所述提取物包含以下中的一种或更多种:山柰酚、高良姜素、槲皮素、松属素、二氢高良姜素、3-O-甲基高良姜素、7-O-甲基高良姜素、山柰素、5-羟基-7-(4'-羟基-3'-甲氧基苯基)-1-苯基-3-庚酮、3,5-二羟基-1,7-双(3,4-二羟基苯基)庚烷、良姜素B、高良姜素7-葡糖苷或其任意组合。
5.化妆品或药物制剂,其包含选自以下的至少两种不同活性组分的组合:高良姜提取物、杨梅素、肺衣酸和头花蓼(Persicaria capitata)提取物。
6.如权利要求5所述的化妆品或药物制剂,其中所述制剂包含高良姜提取物和杨梅素。
7.如权利要求5所述的化妆品或药物制剂,其中所述制剂包含高良姜提取物和肺衣酸。
8.如权利要求5所述的化妆品或药物制剂,其中所述制剂包含高良姜提取物和头花蓼提取物。
9.如权利要求5所述的化妆品或药物制剂,其中所述制剂包含杨梅素和肺衣酸。
10.如权利要求5所述的化妆品或药物制剂,其中所述制剂包含肺衣酸和头花蓼提取物。
11.如权利要求5所述的化妆品或药物制剂,其中所述制剂包含杨梅素和头花蓼提取物。
12.如权利要求5至11中任一项所述的化妆品或药物制剂在治疗皮肤炎症中的用途。
13.如权利要求5至11中任一项所述的化妆品或药物制剂在治疗面部血管分布提高中的用途。
14.如权利要求5至11中任一项所述的化妆品或药物制剂在治疗酒渣鼻中的用途。
15.如权利要求5至11中任一项所述的化妆品或药物制剂的用途,其中所述制剂是激肽释放酶5(KLK5)抑制剂。
16.用于产生如权利要求5至11中任一项所述的化妆品或药物制剂的方法,其包括:
获得选自高良姜提取物、杨梅素、肺衣酸和头花蓼提取物的至少两种不同组分的至少两种来源;以及
将所述至少两种组分组合以提供化妆品或药物制剂。
17.用于产生如权利要求5至11中任一项所述的化妆品或药物制剂的试剂盒,所述试剂盒包含:
选自高良姜提取物、杨梅素、肺衣酸和头花蓼提取物的至少两种不同组分的至少两种来源。
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SE1930415A SE544843C2 (en) | 2019-12-23 | 2019-12-23 | Plant extracts for treatment of rosacea |
PCT/EP2020/082154 WO2021129977A1 (en) | 2019-12-23 | 2020-11-13 | Plant extracts for treatment of increased facial vascularity |
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WO2021129977A1 (en) | 2021-07-01 |
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