CN115227702A - 重楼皂苷ⅶ在制备抗色素沉着的产品中的用途 - Google Patents
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Abstract
本发明涉及化妆品或药品技术领域，具体涉及重楼皂苷Ⅶ在制备抗色素沉着的产品中的用途。
Description
技术领域
本发明涉及化妆品或药品技术领域，具体涉及重楼皂苷Ⅶ在制备抗色素沉着的产品中的用途。
背景技术
炎症是一种基本病理过程，其主要表现为具有血管系统的活体组织对各种损伤因子的刺激所发生的一种防御反应。炎症反应又叫发炎，是指生物组织受到外伤、出血、或者病原体感染等刺激引发的生理反应的统称，又称为炎性反应。
炎症反应主要表现为患病部位红、肿、热、痛和机体功能障碍，伴随着机体局部组织发生变质、增生、液体渗出等症状。炎症反应并非像后天免疫系统一样针对特定的病原体，它是机体的免疫系统为对抗有害刺激以及促进机体修复的一种先天保护措施。
导致炎症的因素繁多，我们把能够造成机体组织损伤而引起炎症反应的因素都统称为致炎因子。致炎因子可以大致分为几类，包括生物性致炎因子、物理性致炎因子、化学性致炎因子、异物致炎因子。炎症反应囊括全身，其中皮肤是极其重要的反映部位，皮肤炎症会导致皮肤炎症后色素沉着，出现皮肤暗沉、色斑、黧黑等等皮肤问题。如何改善因炎症导致的皮肤色素沉着问题，是改善肤色问题的一个新切入点。
炎症后色素沉着(Post-inflammatory hyperpigmentation，PIH)作为炎症性皮肤病结局，是皮肤抵御各种损伤因子刺激后所发生的病理过程。能引起皮肤组织细胞损伤的内外源性因素均可导致PIH，这些因素包括物理因素、化学因素、生物因素、变态反应、组织坏死和异物等。
PIH具体发病机制尚不完全清楚，研究表明，黑素细胞与相邻皮肤细胞对PIH产生发挥重要作用。黑素细胞的迁移与增殖分化、酪氨酸酶合成和激活、黑素体转移至角质形成细胞等多环节影响PIH发生，影响细胞再生与分化的炎症调节因子如炎性介质、炎性细胞因子、促黑素及一氧化氮(NO)对上述环节起到不同程度调节作用。
当皮肤发生炎症时，角质形成细胞、黑素细胞、成纤维细胞、肥大细胞与内皮细胞的细胞膜代谢活跃，细胞膜磷脂经过不同途径合成多种炎性介质如：白三烯、前列腺素、血栓素和组胺。其中前列腺素E2作为一种重要炎性介质，通过多种途径介导PIH发生。
前列腺素是重要的花生四烯酸代谢产物，前列腺素E2通过4个G蛋白偶联受体(EP1-EP4)产生生物活性。PGE-2通过激活EP1和EP3受体刺激黑素细胞树突形成，使黑素细胞树突增多。PGE-2通过激活EP4受体信号可以刺激黑素细胞中cAMP的产生，cAMP是调控黑色素细胞增殖和黑素生成的关键信号通路，通过上调相关基因小眼畸形转录因子(MITF)、酪氨酸酶(TYR)、酪氨酸相关蛋白-1(TRP-1)、酪氨酸相关蛋白-2(TRP-2)的表达影响黑素合成。但是PGE-2刺激EP3受体降低了基础cAMP水平。所以，PGE-2是通过EP受体的相对水平或活性影响黑素细胞cAMP的表达量，cAMP的表达量升高，从而导致色素沉着，即炎症后色素沉着。
大量研究表明皮肤的炎症反应是由很多因素诱导的，而细菌是诱导皮肤炎症的一个重要刺激因素，可引起包括感染性病变、中毒性病变和免疫介导性病变等不同类型的皮肤病。皮肤炎症的最终结果就是炎症后色素沉着，PGE-2作为一种重要的炎性介质，可以通过多种途径刺激黑素细胞树突形成及黑素细胞增殖，最后介导炎症后色素沉着的发生。就目前研究来看，针对皮肤的炎症后色素沉着研究相对较少，对炎症后色素沉着有效果的抑制剂也较少。
七叶一枝花(Paris polyphylla Sm.)，又名七叶莲、重楼、草河车等，为百合科重楼属多年生草本植物。七叶一枝花根茎药用历史悠久，以前主要用于治疗各种疮毒、痈疽、毒蛇咬伤等。现在药理研究表明，它还具有止血、镇静镇痛、免疫调节、抗肿瘤、抗炎、抗菌抑菌、抑制精子活性等作用。研究七叶一枝花的功效成分在炎症后色素沉着方面的效果具有重要意义。
因此，开发一种能解决上述技术问题的功效成分，即重楼皂苷Ⅶ在制备抗色素沉着的产品中的用途是非常必要的。
发明内容
本发明的目的是提供重楼皂苷Ⅶ在制备抗色素沉着的产品中的用途。
本发明是通过以下技术方案予以实现的：
本发明涉及重楼皂苷Ⅶ在制备抗色素沉着的产品中的用途。
优选地，所述产品包括化妆品和/或皮肤病用组合物。
本发明还涉及重楼皂苷Ⅶ在制备抑制炎症后色素沉着的化妆品和/或皮肤病用组合物中的用途。
本发明还涉及重楼皂苷Ⅶ在制备化妆的和/或皮肤病用组合物中的用途，作为酪氨酸酶和/或黑素合成的抑制剂。
本发明还涉及重楼皂苷Ⅶ在制备化妆的和/或皮肤病用组合物中的用途，抑制炎症因子诱导的酪氨酸酶生成。
本发明还涉及重楼皂苷Ⅶ在制备化妆的和/或皮肤病用组合物中的用途，抑制促黑素细胞激素α-MSH的表达。
本发明还涉及重楼皂苷Ⅶ在制备化妆的和/或皮肤病用组合物中的用途，抑制促黑素激素的生成。
本发明的有益效果是：
重楼皂苷Ⅶ在抑制炎症后色素沉着方面功效显著。通过2条途径发挥抑制炎症后色素沉着的作用：一是通过抑制菌感染、紫外照射等因素引发的炎症，二是通过抑制炎症因子诱导的酪氨酸酶生成，抑制促黑素激素的生成，发挥其抑制炎症后色素沉着的作用。
附图说明
图1为本发明实施例1中PGE-2对B16F10细胞的安全浓度测试结果。
图2为本发明实施例1中PGE-2刺激B16F10细胞建立炎症后色素沉着模型情况。
图3为本发明实施例1中各重楼皂苷单体对B16F10的细胞安全剂量测试结果。
图4为本发明实施例1中各重楼皂苷单体物对PGE-2引起的B16F10细胞黑素含量增加的影响。
图5为本发明实施例2中重楼皂苷VII对酪氨酸酶含量的影响。
图6为本发明实施例2中重楼皂苷VII对酪氨酸酶活性的影响。
图7为本发明实施例2中重楼皂苷VII对α-MSH、MITF蛋白的影响。
图8为本发明实施例2中重楼皂苷VII对α-MSH蛋白量分析。
图9为本发明实施例2中重楼皂苷VII对MITF蛋白量分析。
具体实施方式
下面结合具体实施例来进一步描述本发明，本发明的优点和特点将会随着描述而更为清楚。但这些实施例仅是范例性的，并不对本发明的范围构成任何限制。本领域技术人员应该理解的是，在不偏离本发明的精神和范围下可以对本发明技术方案的细节和形式进行修改或替换，但这些修改和替换均落入本发明的保护范围内。
实施例1重楼皂苷Ⅶ抑制炎症后色素沉着的作用
1、PGE-2对B16F10细胞的安全浓度
收集B16F10细胞溶液接种于96孔板中，放入培养箱中孵育。待细胞贴壁后，将培养基弃掉，然后每孔加入100μL(6个浓度梯度，每个浓度3个复孔)的PGE-2溶液。以未处理组做为空白对照组。孵育24h后，每孔加入10μL CCK-8(注意避光)，继续放入培养箱中孵育1h，待培养基颜色由浅粉变橙黄，此时用酶标仪在450nm波长测OD值。结果见图1。
细胞存活率＝(测定孔OD值/空白对照组OD值)×100％。
2、炎症后色素沉着模型的建立
收集B16F10细胞溶液，接种于24孔板中，放入培养箱中孵育。待细胞贴壁后，每孔加入500μL(5个浓度梯度，每个浓度3个复孔)的含血清培养基稀释的PGE-2溶液作为实验组；对照组不加PGE-2，加入等体积的含血清培养基的溶液。在5％CO2，37℃条件下孵育36h后。收集到EP管内，细胞计数。清洗细胞后，一半细胞用以测黑色素含量：加入300μL的1M的NaOH裂解液(含10％DMSO)，放入80℃水浴锅30min后取出，静置30min后在475nm波长测OD值。另一半细胞用以测总蛋白浓度，使用BCA试剂盒，根据试剂盒说明操作。根据标准曲线计算总蛋白浓度。
黑色素变化量＝(实验组OD值/蛋白浓度)/(对照组OD值/蛋白浓度)。结果见图2。
选择B16F10细胞，利用PGE-2炎症因子刺激，以黑色素含量变化率为检测指标，建立炎症后色素沉着模型。通过检测不同PGE-2剂量下B16F10细胞的存活率以及对比空白组与不同剂量PGE-2刺激下细胞的黑色素含量变化水平，筛选出合适的PGE-2剂量。结果见图1和图2，结果显示选择浓度为20μg/ml的PGE-2进行造模。
3、重楼皂苷单体对B16F10的细胞安全剂量
收集B16F10细胞溶液，接种于96孔板中(其余孔加入无菌PBS溶液)，放入培养箱中孵育。当80％～90％的B16F10细胞贴壁时，将培养基弃掉，然后用PBS缓冲液进行两次清洗，分别加入重楼皂苷I(即重楼皂苷1)、重楼皂苷II(即重楼皂苷2)、重楼皂苷VI(即重楼皂苷4)、重楼皂苷VII(即重楼皂苷7)稀释液，(剂量分别为10、5、2.5、1.25、0.625μmol)，以未处理组做为空白对照组，每组设3个复孔。培养24h，每孔加入10μL CCK-8继续孵育1h，待培养基颜色由浅粉变橙黄，此时用酶标仪在450nm波长测OD值。
细胞存活率＝(测定孔OD值/空白对照组OD值)×100％。结果见图3。
4、重楼皂苷单体对PGE-2引起的B16F10细胞黑素含量增加的影响
收集B16F10细胞溶液，接种于6孔板中，放入培养箱中孵育。待细胞贴壁后，将培养基弃掉，空白组(不做任何处理)与对照组(仅添加PGE-2，记为PEG-2组；添加100μg/ml的VC溶液为阳性对照组)每孔加2mL培养基，样品组每孔加入2mL的含血清培养基稀释的重楼皂苷稀释液。放入培养箱4h后，除空白组外，每孔加入20μL 2mg/mL的PGE-2溶液(稀释后PGE-2终浓度为20μg/mL)。孵育36h。收集细胞到EP管内，计数。清洗细胞后，一半细胞用以测黑色素含量：加入300μL的1M的NaOH裂解液(含10％DMSO)，放入80℃水浴锅30min后取出，静置30min后在475nm波长测OD值。另一半细胞用以测总蛋白浓度，使用BCA试剂盒，根据试剂盒说明操作。根据标准曲线计算总蛋白浓度。结果见图4(##表示与空白组对比，P<0.01；*表示与PGE-2组对比，P<0.05；**表示与PGE-2组对比，P<0.01)。
黑色素变化量＝(样品组OD值/蛋白浓度)/(对照组OD值/蛋白浓度)。
通过重楼皂苷单体对B16F10细胞的细胞毒性情况及这几种皂苷单体抑制炎症后色素沉着的作用效果，分析重楼皂苷Ⅶ具有抑制炎症后色素沉着的作用(P<0.05)。判断重楼皂苷Ⅶ是发挥抑制炎症后色素沉着功效的主要成分。
5、统计学分析
所有实验均重复3次，结果以均值±标准偏差(Mean±SD)表示，采用SPSS25.0对各组数据进行分析，采用单因素方差分析。p<0.05(*)，表示差异显著；p<0.01(**)，则表示差异极显著。
实施例2重楼皂苷Ⅶ抑制炎症后色素沉着作用的机制
1、重楼皂苷Ⅶ对酪氨酸酶含量及活性的影响
收集B16细胞溶液，接种于24孔板中，放入培养箱中孵育。待细胞贴壁后，将培养基弃掉，然后每孔加入500μL(3个浓度梯度，每个浓度3个复孔)的含血清培养基稀释的重楼皂苷Ⅶ溶液，阳性对照组每孔加入500μL的100μg/ml的VC溶液，空白组(不做任何处理)与PEG-2组(仅添加PGE-2)每孔加500μL培养基。孵育36h后，收集细胞到EP管内，计数。清洗细胞后，1/3的细胞用BCA试剂盒测总蛋白浓度，1/3的细胞使用小鼠酪氨酸酶ELISA试剂盒测酪氨酸酶含量，1/3的细胞测酪氨酸酶活性。结果见图5和图6(##表示与空白组对比，P<0.01；#表示与空白组对比，P<0.05；*表示与PGE-2组对比，P<0.05)。
酪氨酸酶含量变化率＝(酪氨酸酶含量/总蛋白浓度)/(空白对照酪氨酸酶含量/空白对照总蛋白浓度)；
酪氨酸酶活性变化率＝(酪氨酸酶活性OD值/酪氨酸酶量)/(空白对照酪氨酸酶活性OD值/空白对照酪氨酸酶量)。
2、重楼皂苷Ⅶ对α-MSH、MITF蛋白的影响
细胞培养、刺激后(方法同实施例2-1)，PBS缓冲液清洗两次，使用细胞刮刀将细胞取出，用移液枪把混合物转移到离心管中(以上操作均在冰上进行)。
将装有细胞的离心管在4℃1000rcf的条件下离心5min，弃上清。然后加入200μL预冷的配置好的蛋白裂解缓冲液。用移液枪吹打把细胞吹散，旋涡震荡5min以充分裂解细胞，以没有明显的沉淀作为充分裂解的标志。然后在4℃1000rcf的条件下，离心10min，取上清，便收获蛋白样品。利用western blot法检测重楼皂苷对α-MSH、MITF蛋白的影响。用凝胶显色仪曝光拍照，之后用Image J分析膜上条带浓度，以计算相对目标蛋白表达量。结果见图7、图8和图9(##表示与空白组对比，P<0.01；**表示与PGE-2组对比，P<0.01)。
上述详细说明是针对本发明其中之一可行实施例的具体说明，该实施例并非用以限制本发明的专利范围，凡未脱离本发明所为的等效实施或变更，均应包含于本发明技术方案的范围内。
Claims (7)
1.重楼皂苷Ⅶ在制备抗色素沉着的产品中的用途。
2.根据权利要求1所述的用途，其特征在于，所述产品包括化妆品和/或皮肤病用组合物。
3.重楼皂苷Ⅶ在制备抑制炎症后色素沉着的化妆品和/或皮肤病用组合物中的用途。
4.重楼皂苷Ⅶ在制备化妆的和/或皮肤病用组合物中的用途，作为酪氨酸酶和/或黑素合成的抑制剂。
5.重楼皂苷Ⅶ在制备化妆的和/或皮肤病用组合物中的用途，抑制炎症因子诱导的酪氨酸酶生成。
6.重楼皂苷Ⅶ在制备化妆的和/或皮肤病用组合物中的用途，抑制促黑素细胞激素α-MSH的表达。
7.重楼皂苷Ⅶ在制备化妆的和/或皮肤病用组合物中的用途，抑制促黑素激素的生成。
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