CN107184573B - 环淫羊藿素在制备抗皮肤损伤药物中的应用 - Google Patents

环淫羊藿素在制备抗皮肤损伤药物中的应用 Download PDF

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CN107184573B
CN107184573B CN201710434792.7A CN201710434792A CN107184573B CN 107184573 B CN107184573 B CN 107184573B CN 201710434792 A CN201710434792 A CN 201710434792A CN 107184573 B CN107184573 B CN 107184573B
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左付国
吴金峰
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Shanghai Hi Tech Industrial Co Ltd
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Abstract

本发明涉及医药技术领域，提出了环淫羊藿素在制备抗皮肤损伤药物中的应用。本发明研究显示，淫羊藿素对双氧水致皮肤损伤无明显保护作用，而其同分异构体环淫羊藿素则对氧化应激致皮肤损伤有较强的保护作用。本发明发现了环淫羊藿素可以抗皮肤损伤这一新的医药用途。

Description

环淫羊藿素在制备抗皮肤损伤药物中的应用
技术领域
本发明涉及医药技术领域，特别涉及一种环淫羊藿素的新应用，具体为环淫羊藿素在制备抗皮肤损伤药物中的应用。
背景技术
淫羊藿素及环淫羊藿素为小檗科植物淫羊藿Epimedium brevicornum Maxim.、箭叶淫羊藿Epimedium sagittatum(Sieb.et Zucc.)Maxim.、柔毛淫羊藿Epimediumpubescens Maxim.、巫山淫羊藿Epimedium wushanense T.S.Ying、或朝鲜淫羊藿Epimedium koreanum Nakai的干燥地上部分经过提取得到淫羊藿苷，然后经过不同的水解方法得到。淫羊藿素和环淫羊藿素的结构如下，其中A为环淫羊藿素化学结构图，B为淫羊藿素化学结构图。
目前关于淫羊藿素用途有很多。专利CN101836976A公开了淫羊藿素具有抗肿瘤血管生成的作用；专利CN101428015A公开了淫羊藿素具有抗内毒素血症的作用；专利CN101284000A公开了淫羊藿素具有防治肥胖症或脂肪肝的作用；专利CN1194701C公开了淫羊藿素或去甲基淫羊藿素具有在制备雌激素受体调节剂中的应用。目前关于环淫羊藿素的药理活性报道不多。有关环淫羊藿素的用途，专利CN103271903A公开了淫羊藿素、环淫羊藿素在制备α-葡萄糖苷酶抑制剂药物中的应用。
发明内容
环淫羊藿素(cytoicaritin)是淫羊藿素(icaritin)的同分异构体。理论上讲，淫羊藿素和环淫羊藿素化学结构相似，其药理作用也应相似。比如，淫羊藿素有抗氧化作用，环淫羊藿素也应有类似药理作用。理论上讲，两者均可以保护氧化应激引起的皮肤损伤。然而本发明显示，淫羊藿素对双氧水(氧化应激)致皮肤损伤无明显保护作用，而环淫羊藿素则对氧化应激致皮肤损伤有较强的保护作用。本发明发现了环淫羊藿素可以抗皮肤损伤这一新的药理作用。
因此，本发明的目的是提出了环淫羊藿素的一种新用途，具体为环淫羊藿素在制备抗皮肤损伤药物中的应用。
本发明的环淫羊藿素(可市购)属黄酮醇类化合物，少量存在于淫羊藿药材中，其化学结构式如下：
本发明将上述环淫羊藿素进行了对抗H2O2引起的皮肤角质损伤及细胞凋亡实验。结果表明，环淫羊藿素可保护双氧水(H2O2)引起的皮肤角质形成细胞损伤，并可逆转H2O2诱导的皮肤角质形成细胞凋亡。
所述的环淫羊藿素可以作为药物有效成分，加以药物学上可接受的载体，制备抗皮肤损伤的药物组合物。尤其用于制备抗外界环境因素如紫外线、吸烟、雾霾等通过氧化应激引起皮肤损伤的药物。
附图说明
图1：双氧水对皮肤角质形成细胞的损伤及淫羊藿素的干预对保护该细胞损伤的结果；
图2：双氧水对皮肤角质形成细胞的损伤及环淫羊藿素的干预对保护该细胞损伤的结果；
图3：双氧水和环淫羊藿素干预下，皮肤角质形成细胞的流式图；
图4：双氧水和环淫羊藿素干预下，皮肤角质形成细胞的流式统计图；
图5：双氧水和环淫羊藿素干预下，抗凋亡蛋白Bcl2表达的western blot图；
图6：双氧水和环淫羊藿素干预下，抗凋亡蛋白Bcl2表达的统计图；
图7：双氧水和环淫羊藿素干预下，促凋亡蛋白BIM表达的western blot图；
图8：双氧水和环淫羊藿素干预下，促凋亡蛋白BIM表达的统计图。
具体实施方式
为使本发明的目的、技术方案和优点更加清楚明白，下面结合实施例对本发明进行详细的说明，但是不能把它们理解为对本发明保护范围的限定。
本发明具体实施例中，如无特殊说明，均采用本领域中的常规实际及方法。
本发明具体实施例中所用的细胞株HacaT来源于ATCC(美国标准生物品收藏中心)，也可采用本领域中的其他皮肤角质细胞株。
本发明具体实施例中，淫羊藿素和环淫羊藿素为市购商品，购自上海融禾医药科技有限公司。
实施例1
环淫羊藿素对保护双氧水引起的皮肤角质形成细胞损伤实验
材料与方法：
皮肤角质形成细胞株(HacaT)采用DMEM高糖培养基+10％胎牛血清进行培养。在96孔板中，每孔铺4000个细胞，过夜培养后吸除旧培养基，每孔加200uL新鲜含培养基，采用不同浓度的淫羊藿素或环淫羊藿素(0，10，100uM)预处理1小时，再给予不同浓度的H2O2(0，500，1000uM)刺激6或24小时，每孔加20uL MTT(5mg/mL)，孵育2小时后，吸除培养基，每孔加100uL DMSO，震荡混匀后，用酶标仪570/630双波长检测吸光度值(OD)。
细胞活性(cell viability)＝100*处理组OD值/对照组OD值。
结果见图1和图2。结果表明，H2O2可引起皮肤角质形成细胞活性下降，随着双氧水处理浓度的增加，皮肤角质形成细胞活性逐渐下降。
淫羊藿素干预未能显示保护作用，在添加了淫羊藿素0、10和100uM的浓度下，皮肤角质形成细胞活性依然低于未处理的细胞活性。
环淫羊藿素则显示了较好的保护作用。在用不同浓度环淫羊藿素处理后，双氧水造成的皮肤角质细胞损伤都有不同程度的减轻，且随着环淫羊藿素浓度的增加，对双氧水造成的皮肤角质细胞损伤保护作用逐渐增加。
实施例2
环淫羊藿素对逆转H2O2引起的皮肤角质形成细胞凋亡的实验
材料与方法：
6孔板，皮肤角质形成细胞株(HacaT)每孔铺2×105个细胞，过夜培养后吸除旧培养基，每孔加1ML新鲜含培养基，采用不同浓度的环淫羊藿素(IT0，40，100uM)预处理1小时，再给予H2O2(500uM)刺激24小时，收集细胞，无水乙醇固定过夜，采用PI单染，流式细胞术检测，并用flowjo软件分析subG1峰(凋亡峰)比例。其中，PI单染和流式细胞术检测均采用本领域技术人员所熟知的方法。
结果见图3和图4。结果表明，H2O2可引起皮肤角质形成细胞凋亡，而环淫羊藿素则显示了较好的保护作用。
实施例3
环淫羊藿素可对抗H2O2引起的角质形成细胞抗凋亡及促凋亡蛋白表达的改变
材料与方法：
6孔板，皮肤角质形成细胞株(HacaT)每孔铺2×105个细胞，过夜培养后吸除旧培养基，每孔加1ML新鲜含培养基，采用不同浓度的环淫羊藿素(IT0，40，100uM)预处理1小时，再给予H2O2(500uM)刺激24小时，收集细胞，抽提总蛋白，western blot检测抗凋亡蛋白BCL2和促凋亡蛋白BIM的表达。
结果见图5～8，其中图5～6为BCL2的变化图，图7～8为BIM变化图。结果表明，H2O2可减少皮肤角质形成细胞抗凋亡蛋白BCL2表达，增加促凋亡蛋白BIM表达，而环淫羊藿素则显示了逆转作用。
以上所述仅是本发明的优选实施方式，应当指出，对于本技术领域的普通技术人员来说，在不脱离本发明原理的前提下，还可以做出若干改进和润饰，这些改进和润饰也应视为本发明的保护范围。

Claims (2)

1.环淫羊藿素在制备抗皮肤损伤药物中的应用，其特征在于，所述皮肤损伤为双氧水所致的皮肤损伤，所述的环淫羊藿素具有如下化学结构：
2.根据权利要求1所述的应用，其特征在于，所述抗皮肤损伤的药物包括活性成分环淫羊藿素以及药物学上可接受的载体。
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