CN118055768A - 包含聚半乳糖苷作为有效成分的用于预防或治疗癌症的组合物 - Google Patents
包含聚半乳糖苷作为有效成分的用于预防或治疗癌症的组合物 Download PDFInfo
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- CN118055768A CN118055768A CN202280066256.5A CN202280066256A CN118055768A CN 118055768 A CN118055768 A CN 118055768A CN 202280066256 A CN202280066256 A CN 202280066256A CN 118055768 A CN118055768 A CN 118055768A
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Abstract
本发明涉及包含聚半乳糖苷、其旋光异构体或其药学上可接受的盐作为有效成分的示出优秀的预防或治疗癌症的效果的组合物。本发明的聚半乳糖苷具有活性氧抑制效果、还原型辅酶II氧化酶2(NOX2)蛋白活性抑制效果,具有癌细胞杀灭效果、癌细胞增殖抑制效果,发挥预防、改善或治疗癌症的效果,从而可以用作药物组合物、改善用食品组合物。并且,本发明还可以根据活性氧抑制效果来用作发挥抗老化或抗氧化效果的改善用食品组合物、改善用化妆品组合物。
Description
技术领域
本发明涉及包含聚半乳糖苷(polygalatenoside)作为有效成分的用于预防或治疗癌症的组合物。
背景技术
根据联合国(UN,United Nations)刊发的“2017年世界人口老龄化(WorldPopulation Ageing 2017)”,全世界60岁以上的老龄人口为9亿6200万(2017年),与1980年相比,37年间增加了2倍。而且,预计到37年后的2050年,老龄人口的增速将得到加速使这一数字再翻一番达21亿人。预计从现在(2021年)到9年后的2030年,全世界老龄人口的人数将超过未满10岁的儿童数量。而且,因老龄化引起的老年性疾病患者增加并增加由此带来的医疗成本,因此,预防老化的重要性日渐抬头。
众所周知,老化的主要原因为氧化胁迫,氧化胁迫在癌症、痴呆、神经退行性疾病、心血管疾病、关节炎等老化相关疾病的发病中起作用(Ilaria Liguori et al.,Oxidativestress,aging,and diseases,Clinical interventions in aging,2018;13:757-772)。还原型辅酶II氧化酶(NOX,NADPH oxidase)为膜结合酶,为以氧为催化剂来生成活性氧的氧化胁迫的主要原因,与多种疾病有关。还原型辅酶II氧化酶的活性与老化一同增加,诱发心血管系统严重的氧化应激。还原型辅酶II氧化酶可以在前列腺癌、胰腺癌、黑色素瘤、神经胶质瘤、乳腺癌、膀胱癌、大肠癌、卵巢癌等癌细胞中调节生长和凋亡。因此,还原型辅酶II氧化酶抑制在抗氧化、老化预防、老化相关疾病的治疗中用作重要策略。
并且,老化为癌症(cancer)发病的最为重要的风险因素。根据美国国家癌症研究所(National Cancer Institute)的报告,在过去五年(2013~2017年),癌症发病率激增至每10万人中,小于20岁为25人,45~49岁为350人,60岁以上为1000人。虽然随着癌症治疗技术的发展,一部分癌症的10年以上存活率可达99%,但胰腺癌等癌症的10年存活率仍不足1%。并且,与癌症治疗技术相比,预防癌症的技术开发相对不足,而现在使用的抗癌剂大部分都具有伴随强烈的副作用的问题。
现有的抗癌剂在通过直接向细胞施加胁迫来杀死细胞的同时引起作为氧化胁迫的原因的活性氧的生成。抗癌剂因上述原因而可能发生脱发、呕吐、恶寒、免疫力降低等多种副作用,因此,对抑制活性氧生成的技术的需要日益增加。大部分癌细胞的活性氧水平增加,活性氧起到诱导细胞增殖的信号传导因子的作用。
另一方面,聚半乳糖苷最初从在中国用作抗精神病药剂的药用植物远志(Polygala tenuifolia)中分离,据报告,具有抑郁症治疗效果和对神经疾病的治疗效果。本发明确认到聚半乳糖苷对癌症的预防或治疗效果,这可以用作药物组合物或保健功能食品组合物。并且,本发明可以用作发挥随活性氧抑制效果的抗老化或抗氧化效果的保健功能食品组合物、化妆品组合物。
发明内容
技术问题
本发明的目的在于,提供包含聚半乳糖苷作为有效成分的用于预防或治疗癌症的药物组合物。
本发明的目的在于,提供包含聚半乳糖苷作为有效成分的用于预防或改善癌症的食品组合物。
本发明的目的在于,提供包含聚半乳糖苷作为有效成分的示出抗老化或抗氧化效果的改善用食品组合物。
本发明的目的在于,提供包含聚半乳糖苷作为有效成分的示出抗老化或抗氧化效果的改善用化妆品组合物。
最后,本发明的另一目的在于,提供治疗癌症的方法,包括向个体给药上述药物组合物的步骤。
技术方案
本发明提供包含由下述化学式1表示的化合物或其药学上可接受的盐作为有效成分的用于预防或治疗癌症的药物组合物。
化学式1
在上述化学式1中,R1、R2及R3独立地为氢原子或RBz,上述R1、R2及R3中的至少一个为RBz,上述RBz为下述化学式2。
化学式2
在上述化学式2中,R2为氢原子、卤素、氰基、硝基、叠氮基、苯基、包含选自由N、O及S组成的组中的一种以上杂原子的5-6元杂环基、C1-6烷基、C1-6烷氧基、C1-6烷硫基、C2-6烯基、C2-6炔基或药剂学上可接受的盐。
在本发明的一实施例中,上述药物组合物的特征在于,上述化合物可以为由下述化学式3表示的化合物,但不限定于此。
化学式3
在本发明的一实施例中,上述药物组合物的特征在于,上述化合物可以为由下述化学式4表示的化合物,但不限定于此。
化学式4
在本发明的一实施例中,上述药物组合物的特征在于,上述化合物可以为由下述化学式5表示的化合物,但不限定于此。
化学式5
在本发明的一实施例中,上述药物组合物的特征在于,上述化合物可以具有抗氧化效果,但不限定于此。
在本发明的一实施例中,上述药物组合物的特征在于,上述化合物可以具有还原型辅酶II氧化酶2蛋白活性抑制效果,但不限定于此。
在本发明的一实施例中,上述药物组合物的特征在于,上述癌症可以为前列腺癌、胰腺癌、黑色素瘤、神经胶质瘤、乳腺癌、膀胱癌、大肠癌及卵巢癌中的一种以上,但不限定于此。
并且,本发明提供包含由下述化学式1表示的化合物、其旋光异构体或其药学上可接受的盐作为有效成分的用于预防或改善癌症的食品组合物。
化学式1
在上述化学式1中,R1、R2及R3独立地为氢原子或RBz,上述R1、R2及R3中的至少一个为RBz,上述RBz为下述化学式2。
化学式2
在上述化学式2中,R2为氢原子、卤素、氰基、硝基、叠氮基、苯基、包含选自由N、O及S组成的组中的一种以上杂原子的5-6元杂环基、C1-6烷基、C1-6烷氧基、C1-6烷硫基、C2-6烯基、C2-6炔基或药剂学上可接受的盐。
并且,本发明提供包含由下述化学式1表示的化合物、其旋光异构体或其药学上可接受的盐作为有效成分的示出抗老化或抗氧化效果的改善用食品组合物。
化学式1
在上述化学式1中,R1、R2及R3独立地为氢原子或RBz,上述R1、R2及R3中的至少一个为RBz,上述RBz为下述化学式2。
化学式2
在上述化学式2中,R2为氢原子、卤素、氰基、硝基、叠氮基、苯基、包含选自由N、O及S组成的组中的一种以上杂原子的5-6元杂环基、C1-6烷基、C1-6烷氧基、C1-6烷硫基、C2-6烯基、C2-6炔基或药剂学上可接受的盐。
并且,本发明提供包含由下述化学式1表示的化合物、其旋光异构体或其药学上可接受的盐作为有效成分的示出抗老化或抗氧化效果的改善用化妆品组合物。
最后,本发明提供预防或治疗癌症的方法,包括向个体给药上述药物组合物的步骤。
化学式1
在上述化学式1中,R1、R2及R3独立地为氢原子或RBz,上述R1、R2及R3中的至少一个为RBz,上述RBz为下述化学式2。
化学式2
在上述化学式2中,R2为氢原子、卤素、氰基、硝基、叠氮基、苯基、包含选自由N、O及S组成的组中的一种以上杂原子的5-6元杂环基、C1-6烷基、C1-6烷氧基、C1-6烷硫基、C2-6烯基、C2-6炔基或药剂学上可接受的盐。
发明的效果
本发明提供包含聚半乳糖苷、其旋光异构体或其药学上可接受的盐作为有效成分的在癌症的预防和治疗中示出优秀效果的组合物。本发明的聚半乳糖苷具有活性氧抑制效果、还原型辅酶II氧化酶2蛋白活性抑制效果,具有癌细胞杀灭效果、癌细胞增殖抑制效果,从而发挥预防、改善或治疗癌症的效果。
并且,本发明提供包含聚半乳糖苷、其旋光异构体或其药学上可接受的盐作为有效成分的示出抗老化或抗氧化效果的改善用食品组合物。并且,本发明提供包含聚半乳糖苷、其旋光异构体或其药学上可接受的盐作为有效成分的示出抗老化或抗氧化效果的改善用化妆品组合物。
附图说明
图1为示出随着处理本发明的聚半乳糖苷的活性氧抑制效果的图。
图2为示出随着处理本发明的聚半乳糖苷的还原型辅酶II氧化酶2蛋白活性抑制效果的图。
图3为示出随着处理本发明的聚半乳糖苷的癌细胞杀灭效果的图。
图4为示出随着处理本发明的聚半乳糖苷的癌细胞增殖抑制效果的图。
最佳实施方式
本发明提供包含作为由下述化学式1表示的化合物的聚半乳糖苷、其旋光异构体或其药学上可接受的盐作为有效成分的用于预防或治疗癌症的药物组合物。
化学式1
在上述化学式1中,R1、R2及R3独立地为氢原子或RBz,上述R1、R2及R3中的至少一个为RBz,上述RBz为下述化学式2。
化学式2
在上述化学式2中,R2为H(氢原子)、卤素(halogen)、氰基(cyano group)、硝基(nitro group)、叠氮基(azide group)、苯基(phenyl group)、包含选自由N、O及S组成的组中的一种以上杂原子的5-6元杂环基(heterocyclic group)、C1-6烷基(alkyl group)、C1-6烷氧基(alkoxy group)、C1-6烷硫基(alkylthio group)、C2-6烯基(alkenyl group)、C2-6炔基(alkynyl group)或药剂学上可接受的盐。
在本发明中,在上述化学式1的R1=RBz,R2=R3=H,化学式2的R2=H的情况下,上述化合物为由下述化学式3表示的聚半乳糖A(polygalatenoside A)。
化学式3
在本发明中,在上述化学式1的R1=R2=H,R3=RBz,化学式2的R2=H的情况下,上述化合物为由下述化学式4表示的聚半乳糖苷B(polygalatenoside B)。
化学式4
在本发明中,在上述化学式1的R1=R3=H,R2=RBz,化学式2的R2=H的情况下,上述化合物为由下述化学式5表示的聚半乳糖苷C(polygalatenoside C)。
化学式5
本发明的聚半乳糖苷通过抑制活性氧来具有抗氧化效果(antioxidant),可以从由氧化胁迫引起的老化中保护细胞并预防老化相关疾病。上述老化相关疾病可以为选自糖尿病(diabetes)、心肌梗塞(myoxardial infraction)、心绞痛(angina pectoris)、动脉硬化(atheroscleosis)、心衰(heart failure)中的任一种。并且,本发明的聚半乳糖苷可以应用为通过活性氧抑制效果来在抗老化或抗氧化中示出效果的改善用食品组合物、改善用化妆品组合物。
本发明的聚半乳糖苷可以通过抑制还原型辅酶II氧化酶2蛋白活性来诱导前列腺癌、胰腺癌、黑色素瘤、神经胶质瘤、乳腺癌、膀胱癌、大肠癌、卵巢癌等癌细胞的凋亡。
并且,确认到本发明的聚半乳糖苷通过示出癌细胞杀灭效果和癌细胞增殖抑制效果来具有抗癌效果。
在本发明中,单独进行3次以上实验,以平均值±标准差(mean±standarddeviation(SD))的方式表示3个实验数据。使用GraphPad PRISM软件(GraphPad PRISMsoftware)和微软Excel软件(Microsoft Excel software)进行数据分析。利用基于tukey多重比较检验的方差分析(ANOVA with Tukey’s multiple comparisons test)计算统计显著性(p值)。当p值小于0.05时,视为统计学上具有显著性,在附图中,p值小于0.05表示为*,小于0.01表示为**,小于0.001表示为***,小于0.0001表示为****。
在本说明书全文中,若无单独说明,则表示特定物质的浓度的为“%”,固体/固体为(w/w)%,固体/液体为(w/v)%,液体/液体为(v/v)%。
在本发明中,除有效成分以外,上述药物组合物还可以包含佐剂(adjuvant)。上述佐剂只要是本发明所属技术领域中通常使用的就可以不受限制地使用。
本发明的药物组合物可以制备为在药学上可接受的载体中混合有效成分的形态。其中,药学上可接受的载体包括治疗领域中通常使用的载体、赋形剂及稀释剂。本发明的药物组合物中可以使用的药学上可接受的载体可以为乳糖、葡萄糖、蔗糖、山梨醇、甘露醇、木糖醇、赤藓糖醇、麦芽糖醇、淀粉、阿拉伯胶、海藻酸盐、明胶、磷酸钙、硅酸钙、纤维素、甲基纤维素、聚乙烯吡咯烷酮、水、羟基苯甲酸甲酯、羟基苯甲酸丙酯、滑石粉、硬脂酸镁及矿物油,但不限定于此。
本发明的药物组合物可以分别根据通常的方法配制为散剂、颗粒剂、片剂、胶囊剂、悬混剂、乳剂、糖浆、气雾剂等口服剂型以及外用剂、栓剂或灭菌注射溶液等形态来使用。
在配制时,可以使用通常使用的填充剂、增量剂、结合剂、湿润剂、崩解剂、表面活性剂等稀释剂或赋形剂来制备。用于口服给药的固体制剂包括片剂、丸剂、散剂、颗粒剂、胶囊剂等,上述固体制剂可以在有效成分中混合一种以上赋形剂,例如,淀粉、碳酸钙、蔗糖、乳糖、明胶等来制备。并且,除单纯的赋形剂以外,还可以使用硬脂酸镁、滑石粉等润滑剂。用于口服给药的液体制剂有悬混剂、内溶液剂、乳剂、糖浆剂等,除通常用作稀释剂的水、液体石蜡以外,还可以包含多种赋形剂,例如湿润剂、甜味剂、芳香剂、保存剂等。用于胃肠外给药的制剂包括灭菌的水溶液、非水溶性溶剂、悬混剂、乳剂、冷冻干燥机及栓剂。非水溶性溶剂、悬混剂可以使用丙二醇、聚乙二醇、橄榄油等植物油、油酸乙酯等可注射的酯类等。栓剂的基剂可以使用witepsol、吐温(tween)61、可可脂、肉实树脂、甘油明胶等。
本发明的药物组合物可以通过多种途径向个体给药。可以考虑给药的所有方式,例如,可以通过口服、静脉、肌肉、皮下、腹腔内注射来给药。
上述药物组合物可以配制为多种口服或胃肠外给药形态。
例如,口服给药用剂型有片剂、丸剂、硬质胶囊剂、软质胶囊剂、溶剂、悬混剂、乳化剂、糖浆剂、颗粒剂等,除有效成分以外,这些剂型还可以包含稀释剂(例如,乳糖、葡萄糖、蔗糖、甘露醇、山梨醇、纤维素和/或甘氨酸)、滑泽剂(例如,二氧化硅、滑石粉、硬脂酸及其镁盐或钙盐和/或聚乙二醇)。并且,上述片剂可以含有硅酸镁铝、淀粉糊、明胶、黄芪胶、甲基纤维素、羧甲基纤维素钠和/或聚乙烯吡咯烷酮等结合剂,还可以根据情况含有淀粉、琼脂、海藻酸或其钠盐等崩解剂或沸腾混合物和/或吸收剂、着色剂、香味剂及甜味剂。上述剂型可以通过通常的混合、颗粒化或包衣方法来制备。
并且,胃肠外给药用剂型的代表剂型为注射用制剂,注射用制剂的溶剂可以为水、林格氏液、等渗性生理盐水或助悬液。上述注射用制剂的灭菌固定油可以使用溶剂或助悬介质,包括甘油单酯、甘油二酯在内的任何无极性固定油都能够以这样的目的来使用。
并且,上述注射用制剂可以使用油酸等脂肪酸。
并且,除包含作为有效成分的聚半乳糖苷、其旋光异构体或其药学上可接受的盐以外,本发明的改善用食品组合物像通常的食品组合物一样包含多种香味剂或天然碳水化合物作为追加成分。
上述天然碳水化合物的例为:单糖,例如葡萄糖、果糖等;二糖,例如麦芽糖、蔗糖等;多糖,例如,糊精、环糊精等通常的糖;以及木糖醇、山梨糖醇、赤藓糖醇等糖醇。上述香味剂可以有利地使用天然香味剂(索马甜)、甜叶菊提取物(例如莱鲍迪苷A、甘草甜素等)以及合成香味剂(糖精、阿斯巴甜等)。本发明的食品组合物能够以与下述药物组合物相同的方式配制来用作功能性食品,或者添加到各种食品中。可以添加本发明的组合物的食品有例如饮料类、肉类、巧克力、饼干类、披萨、拉面、其他面类、口香糖类、糖果类、冰淇淋类、酒精饮料类、维生素复合物及健康辅助食品类等。
并且,除作为有效成分的聚半乳糖苷、其旋光异构体或其药学上可接受的盐以外,上述食品组合物还可以含有多种营养剂、维生素、矿物质(电解质)、合成风味剂及天然风味剂等风味剂、着色剂及填充剂(奶酪、巧克力等)、果胶酸及其盐、海藻酸及其盐、有机酸、保护性胶体增粘剂、pH调节剂、稳定剂、防腐剂、甘油、酒精、碳酸饮料中使用的碳酸化剂等。此外,本发明的食品组合物还可以含有天然果汁以及用于制备果汁饮料及蔬菜饮料的果肉。
本发明的改善用食品组合物可以制备及加工为片剂、胶囊、粉末、颗粒、液体、丸等形态。在本发明中,“保健功能食品组合物”是指使用有关保健功能食品的法律第6727号指出的对人体有用的功能性的原料或成分来制备及加工的食品,是指对于人体的结构及功能在调节营养素或生理学作用等保健用途方面以获得有用的效果为目的来摄取的食品。本发明的食品组合物可以包含通常的食品添加物,食品添加物的适合与否没有另行规定,根据韩国食品药品安全厅认证的食品添加物法典的总则及通常试验法等通过相关品目有关的规则及标准来判定。例如,上述“食品添加物法典”中收录的品目可以为:酮类、甘氨酸、柠檬酸钙、烟酸、肉桂酸等化学合成物;柿色素、甘草提取物、结晶纤维素、高粱色素、瓜尔胶等天然添加物;L-谷氨酸钠制剂、面类碱性添加剂、防腐制剂、焦油色素制剂等混合制剂等。例如,片剂形态的保健功能食品可以在将混合本发明的有效成分与赋形剂、结合剂及其他添加剂的混合物通过通常的方法颗粒化后,放入滑泽剂等来压出成型或者直接将上述混合物压出成型。并且,上述片剂形态的食品组合物还可以根据需要含有矫味剂等。胶囊形态的食品组合物中,硬质胶囊剂可以通过将混合本发明的有效成分与赋形剂等添加剂的混合物填充到硬质胶囊中来制备,软质胶囊剂可以通过将混合本发明的有效成分与赋形剂等添加剂的混合物填充到明胶等胶囊基剂中来制备。上述软质胶囊剂可以根据需要包含甘油或山梨糖醇等增塑剂、着色剂、保存剂等。丸形态的保健功能食品可以将混合本发明的有效成分与赋形剂、结合剂、崩解剂等的混合物通过现有公知的方法成型来制备,可以根据需要使用白糖或其他包衣剂来包衣,或者使用淀粉、滑石粉等物质使表面包衣。颗粒形态的食品组合物可以将混合本发明的有效成分与赋形剂、结合剂、崩解剂等的混合物通过现有公知的方法来制备为颗粒状,可以根据需要包含发香剂、矫味剂等。
并且,本发明的改善用化妆品组合物可以包含化妆品学上有效量(cosmeticallyeffective amount)的本发明的聚半乳糖苷、其旋光异构体或其药学上可接受的盐以及化妆品学上可接受的载体来制备。
在本说明书中,化妆品学有效量用来实现上述本发明组合物的抗老化或抗氧化效果的充分的量。
化妆品组合物的外形包含化妆品学或皮肤科学可接受的介质或基剂。这是适于局部应用的所有剂型,例如,能够以溶液、凝胶、固体、糊状无水生成物、水包油的乳液、悬混液、微乳液、微胶囊、微颗粒或离子型(脂质体)及非离子型的囊泡分散剂的形态,或者以霜剂、护肤霜、护肤乳、粉剂、软膏、喷剂或遮瑕棒的形态来提供。这些组合物可以根据本发明所属技术领域的通常的方法来制备。并且,本发明的组合物还能够以泡沫(foam)的形态或含有压缩气体的喷雾剂组合物的形态来使用。
本发明一实施例的上述化妆品组合物的剂型不受特别限制,例如,可以配制为柔肤化妆水、收敛化妆水、营养化妆水、营养霜、按摩霜、精华素、眼霜、眼部精华素、洁面霜、洁面泡沫、洁面水、面膜、粉剂、身体乳液、身体霜、身体油及身体精华素等化妆品。
在本发明的化妆品组合物的剂型为贴剂、霜剂或凝胶的情况下,载体成分可以使用动物纤维、植物纤维、蜡、石蜡、淀粉、黄芪胶、纤维素衍生物、聚乙二醇、硅油、膨润土、二氧化硅、滑石粉或氧化锌等。
在本发明的化妆品组合物的剂型为粉剂或喷剂的情况下,载体成分可以使用乳糖、滑石粉、二氧化硅、氢氧化铝、硅酸钙或聚酰胺粉末,尤其在喷剂的情况下,还可以包含氯氟烃、丙烷/丁烷或二甲醚等填充剂。
在本发明的化妆品组合物的剂型为溶液或乳浊液的情况下,载体成分使用溶剂、溶剂化剂或乳浊化剂,例如,水、乙醇、异丙醇、碳酸乙酯、乙酸乙酯、苯甲醇、苯甲酸苄酯、丙二醇、1,3-丁二醇油、甘油脂肪族酯、聚乙二醇或山梨醇酐的脂肪酸酯。
在本发明的化妆品组合物的剂型为悬混液的情况下,载体成分可以利用水、乙醇或丙二醇等液体稀释剂、乙氧基化异硬脂醇、山梨醇聚氧乙烯酯及脱水山梨糖醇聚氧乙烯酯等助悬剂、微晶纤维素、氢氧化铝氧化物、膨润土、淀粉或黄芪胶等。
在本发明的化妆品组合物的剂型为含有表面活性剂的洗剂的情况下,载体成分可以使用脂肪族醇硫酸盐、脂肪族醇醚硫酸盐、黄基琥珀酸单酯、羟乙基磺酸盐、咪唑啉鎓衍生物、牛磺酸甲酯、肌氨酸盐、脂肪酸酰胺醚硫酸盐、烷基氨基甜菜碱、脂肪醇、脂肪酸甘油酯、脂肪酸二乙醇酰胺、植物油、羊毛脂衍生物或乙氧基化甘油脂肪酸酯等。
本发明的化妆品组合物可以适用于护肤水、乳液、霜剂、精华素、面膜、粉底、彩妆化妆品、防晒霜、两用粉饼、敷面粉、粉饼、隔离霜、遮瑕霜、眼影膏、唇膏、唇彩、眉笔、化妆水等化妆品及洗发水、香皂等洗剂。
除聚半乳糖苷、其旋光异构体或其药学上可接受的盐以外,本发明一实施例的化妆品组合物中还可以包含功能性添加物及普通化妆品中包含的成分。上述功能性添加物可以包含选自由水溶性维生素、油溶性维生素、高分子肽、高分子多糖、鞘脂及海藻提取物组成的组中的成分。
并且,本发明的化妆品组合物还可以根据需要与上述功能性添加物一同配合普通化妆品组合物中包含的成分。此外包含的配合成分有油脂成分、保湿剂、润肤剂、表面活性剂、有机及无机颜料、有机粉末、紫外线吸收剂、防腐剂、杀菌剂、抗氧化剂、植物提取物、pH调节剂、酒精、色素、香料、血液循环促进剂、凉感剂、制汗剂、纯水等。
具体实施方式
以下,通过实施例及实验例更为详细地说明本发明。但下述实施例及实验例仅用于例示本发明,本发明不限定于这些实施例及实验例,当判断本发明所属技术领域中主旨鲜明的技术或结构的具体说明有可能不必要地混淆本发明的要旨时,将省略其详细说明。本发明可以在随附的发明要求保护范围的记载及由其解释的同等范畴内进行多种变形及应用。
准备例1.培养黑色素瘤细胞
B16-F10黑色素瘤细胞使用添加有10%(v/v)的胎牛血清及1%(v/v)的青霉素-链霉素的杜氏改良伊戈尔培养基(Dulbecco’s modified Eagle’smedium)在36.5℃及5%CO2的条件下培养。
准备例2.准备由化学式3表示的化合物(聚半乳糖A)
将西格玛奥德里奇(Sigma-Aldrich)公司的聚半乳糖A(Cat.#SMB00542-1MG)以最终2mM的浓度溶于二甲基亚砜来在下述实验中使用。
实验例1.确认聚半乳糖苷的活性氧抑制效果
通常在正常细胞内,已知活性氧(ROS)与细胞的存活及或分化等的调节相关,高水平的活性氧与细胞的基因或蛋白质反应来导致损伤或引起突变来发生癌症。已知癌细胞保持高的活性氧水平,与正常细胞相比,抑制作为与抗氧化作用相关的基因或蛋白质的超氧化物歧化酶(SOD,superoxide dismutase)、谷胱甘肽过氧化物酶(GPx,glutathioneperoxidase)、谷胱甘肽(glutathione)、维生素C(vitamin C)等物质的表达或活性。活性氧主要在细胞内的线粒体中生成,认为随着癌细胞的活性氧水平的减少,癌细胞的线粒体代谢被抑制而妨碍癌细胞的代谢作用。并且,活性氧不仅与癌细胞的代谢、发展、转移相关,在作为癌症病因的炎症发生中也起到重要作用。
已知通过活性氧在细胞内发生的氧化胁迫起到使与癌症相关的核因-κB(NF-κB,nuclear factor-kappa B)、p53、β-连环蛋白(β-catenin)/Wnt、激活子蛋白-1(AP-1,activator protein 1)等基因表达的作用。并且,多种基因的表达与有关炎症的细胞因子(cytokines)或调节细胞的细胞因子的基因相关。并且,若核因子κB被激活,则增加在炎症反应中起到重要作用的白细胞介素(IL,interleukin)-1或白细胞介素-6的生成,这给癌细胞的转移和增殖带来影响。并且,活性氧的增加还与细胞的激动蛋白细胞骨架重组(actincytoskeleton reorganization)相关来与癌细胞的移动和转移相关。
黑色素瘤多发生在皮肤,若细胞暴露在紫外线中,则发生氧化胁迫增加活性氧的发生来抑制超氧化物歧化酶等抗氧化酶的生成。已知在B16-F10细胞中增加活性氧发生时增加转移,据报告,若通过活性氧激活Rac1并表达WAVE2,则引起肌动蛋白聚合(actinpolymerization)来给细胞的移动带来影响,在减少活性氧的情况下,通过减少Rac1活性和WASP-家族verprolin-同源蛋白2(WAVE2,WASP-family verprolin-homologous protein2)的表达来抑制由活性氧增加引起的转移(Sun joo Park et al.,Antioxidant DieckolDownregulates the Rac1/ROS Signaling Pathway and Inhibits Wiskott-AldrichSyndrome Protein(WASP)-Family Verprolin-Homologous Protein 2(WAVE2)-MediatedInvasive Migration of B16 Mouse Melanoma Cells.Mol.Cells,33(4):363-369,2012April.)。
于是,在本实验中确认聚半乳糖苷给细胞内活性氧带来的影响。
培养B16-F10黑色素瘤细胞12小时后,分别以0μM、0.1μM、0.3μM、1μM、3μM及10μM浓度处理聚半乳糖A 24小时。然后,使用1μM浓度的2',7'-二氯二氢荧光素二乙酸酯(H2DCFDA,2',7'-dichlorodihydrofluorescein diacetate)处理30分钟并使用磷酸盐缓冲溶液(PBS,phosphate buffered saline;pH 7.4)洗涤细胞。收获细胞后通过流式细胞分析测定DCF-MFI(中值荧光强度(median fluorescence intensity)),结果如图1所示。流式细胞分析使用Guava EasyCyte流式细胞仪与GuavaIncyte软件(GuavaIncyte software)及FlowJo软件(FlowJo software)进行。
如图1所示,示出细胞内活性氧水平随着聚半乳糖A的处理而减少,随着聚半乳糖A的处理浓度的增加,呈现活性氧抑制效果增加的倾向。
因此,确认到本发明的聚半乳糖苷通过抑制活性氧来具有抗氧化效果。并且,具有抑制或治疗因氧化胁迫诱发的癌症的效果、癌细胞增殖抑制、转移抑制效果,可以预防或治疗由通过活性氧生成的氧化物引起的疾病。
实验例2.确认聚半乳糖苷对NOX蛋白活性的抑制效果
在本实验中,通过确认聚半乳糖苷对NOX蛋白活性的抑制效果,证实了聚半乳糖苷对黑色素瘤的抗癌效果。
NOX是一种膜结合酶,是氧气催化产生活性氧的氧化应激的主要原因,与各种疾病相关。随着老化,NOX的活性增加,引发严重的心血管氧化应激。NOX在前列腺癌、胰腺癌、聚半乳糖苷、神经胶质瘤、乳腺癌、膀胱癌、结肠癌、卵巢癌等癌细胞中可以调节生长和死亡。本实验确认了聚半乳糖苷对NOX蛋白活性的影响。
培养B16-F10黑色素瘤细胞12小时后,分别以0μM、0.1μM、0.3μM、1μM、3μM及10μM浓度处理聚半乳糖A 24小时。然后,使用磷酸盐缓冲溶液洗涤细胞2次并收获细胞,使用包含苯甲磺酰氟(PMSF,phenylmethylsulfonyl fluoride)的放射免疫沉淀法(RIPA,radioimmunoprecipitation assay)缓冲液(buffer)使细胞裂解来回收蛋白质。通过十二烷基硫酸钠-聚丙烯酰胺凝胶电泳(SDS-PAGE,sodium dodecyl sulfate poly-acrylamidegel electrophoresis)分离50μg的蛋白质后,转移(transfer)到聚偏二氟乙烯(PVDF,polyvinylidene fluoride)膜上。在25℃的温度下使用包含5%(w/v)的脱脂牛奶(skimmilk)、0.05%(v/v)的吐温-20(tween-20)及0.01%(w/v)的叠氮化钠(sodium azide)的tris缓冲生理盐水(TBS,tris-buffered saline;pH 7.6)处理膜1小时。使用TBST(包含0.05%(v/v)的吐温-20的tris缓冲生理盐水)洗涤3次并处理结合抗-还原型辅酶II氧化酶2(anti-NOX2)一抗与辣根过氧化物酶(HRP,horseradish peroxidase)的一抗。使用增强化学发光(ECL,enhanced chemiluminescence)和X射线照片(X-ray film)使蛋白质水平可视化。通过ImageJ软件(ImageJ software)的密度测定法(densitometry)分析相对于β-肌动蛋白(β-actin)的还原型辅酶II氧化酶2蛋白的表达程度,结果如图2所示。
如图2所示,与未处理对照组(0μM)相比,示出还原型辅酶II氧化酶2的表达随聚半乳糖A的处理而增加,在以3μM处理聚半乳糖A的情况下,与未处理对照组相比,示出增加约1.4倍。通过药物处理的蛋白质表达增加的结果,示出以对相关蛋白质的抑制剂来起作用的可能性,示出本发明的聚半乳糖苷具有抑制还原型辅酶II氧化酶2蛋白的效果。
即,本发明的聚半乳糖苷示出还原型辅酶II氧化酶2蛋白活性抑制效果,因此判断可以诱导前列腺癌、胰腺癌、黑色素瘤、神经胶质瘤、乳腺癌、膀胱癌、大肠癌、卵巢癌等癌细胞的凋亡。并且,具有通过还原型辅酶II氧化酶2蛋白活性抑制效果的活性氧抑制效果,从而具有预防或治疗因氧化胁迫诱发的癌症的效果、癌细胞增殖抑制、转移抑制效果,可以预防或治疗因通过活性氧生成的氧化物引起的疾病。
实验例3.确认聚半乳糖苷的抗癌效果
在本实验中,根据上述实验例2中聚半乳糖苷的还原型辅酶II氧化酶2蛋白活性抑制效果来确认聚半乳糖苷的黑色素瘤细胞杀灭效果。
在96孔培养板(96-well cell culture plate)中培养B16-F10黑色素瘤细胞12小时,分别以0μM、0.1μM、0.3μM、1μM、3μM及10μM浓度处理聚半乳糖A 48小时。向培养基中处理WST8细胞存活分析试剂(Cell Viability Assay Reagent)使浓度达到10%(v/v)并培养2小时。然后,使用酶标仪(microplate reader)在450nm波长中测定吸光度来确认细胞存活率,结果如图3所示。
如图3所示,确认到在处理3μM的聚半乳糖A的情况下,示出细胞杀灭效果。
接着,为了测定细胞数量的变化,培养B16-F10细胞12小时后分别以0μM、0.1μM、0.3μM、1μM、3μM及10μM浓度处理聚半乳糖A 72小时。每24小时收获细胞来使用台盼蓝(trypan blue)染色并使用血细胞计数器(hemocytometer)测定存活细胞的数量,结果如图4所示。
如图4所示,示出随着聚半乳糖A的处理抑制黑色素瘤细胞的增殖,尤其在以3μM的浓度处理聚半乳糖A的情况下,增殖抑制效果最为显著。
因此,本发明的聚半乳糖苷示出对黑色素瘤的癌细胞杀灭效果和癌细胞增殖抑制效果,从而确认具有抗癌效果。
Claims (11)
1.一种用于预防或治疗癌症的药物组合物,其特征在于,
包含由下述化学式1表示的化合物、其旋光异构体或其药学上可接受的盐作为有效成分,
化学式1:
在上述化学式1中,
R1、R2及R3独立地为氢原子或RBz,上述R1、R2及R3中的至少一个为RBz,上述RBz为下述化学式2,
化学式2:
在上述化学式2中,
R2为氢原子、卤素、氰基、硝基、叠氮基、苯基、包含选自由N、O及S组成的组中的一种以上杂原子的5-6元杂环基、C1-6烷基、C1-6烷氧基、C1-6烷硫基、C2-6烯基、C2-6炔基或药剂学上可接受的盐。
2.根据权利要求1所述的用于预防或治疗癌症的药物组合物,其特征在于,上述化合物为由下述化学式3表示的化合物,
化学式3:
3.根据权利要求1所述的用于预防或治疗癌症的药物组合物,其特征在于,上述化合物为由下述化学式4表示的化合物,
化学式4:
4.根据权利要求1所述的用于预防或治疗癌症的药物组合物,其特征在于,上述化合物为由下述化学式5表示的化合物,
化学式5:
5.根据权利要求1所述的用于预防或治疗癌症的药物组合物,其特征在于,上述化合物具有抗氧化效果。
6.根据权利要求1所述的用于预防或治疗癌症的药物组合物,其特征在于,上述化合物具有还原型辅酶II氧化酶2蛋白活性抑制效果。
7.根据权利要求1所述的用于预防或治疗癌症的药物组合物,其特征在于,上述癌症为前列腺癌、胰腺癌、黑色素瘤、神经胶质瘤、乳腺癌、膀胱癌、大肠癌及卵巢癌中的一种以上。
8.一种用于预防或改善癌症的食品组合物,其特征在于,
包含由下述化学式1表示的化合物、其旋光异构体或其药学上可接受的盐作为有效成分,
化学式1:
在上述化学式1中,R1、R2及R3独立地为氢原子或RBz,上述R1、R2及R3中的至少一个为RBz,上述RBz为下述化学式2,
化学式2:
在上述化学式2中,
R2为氢原子、卤素、氰基、硝基、叠氮基、苯基、包含选自由N、O及S组成的组中的一种以上杂原子的5-6元杂环基、C1-6烷基、C1-6烷氧基、C1-6烷硫基、C2-6烯基、C2-6炔基或药剂学上可接受的盐。
9.一种示出抗老化或抗氧化效果的改善用食品组合物,其特征在于,
包含由下述化学式1表示的化合物、其旋光异构体或其药学上可接受的盐作为有效成分,
化学式1:
在上述化学式1中,R1、R2及R3独立地为氢原子或RBz,上述R1、R2及R3中的至少一个为RBz,上述RBz为下述化学式2,
化学式2:
在上述化学式2中,
R2为氢原子、卤素、氰基、硝基、叠氮基、苯基、包含选自由N、O及S组成的组中的一种以上杂原子的5-6元杂环基、C1-6烷基、C1-6烷氧基、C1-6烷硫基、C2-6烯基、C2-6炔基或药剂学上可接受的盐。
10.一种示出抗老化或抗氧化效果的改善用化妆品组合物,其特征在于,
包含由下述化学式1表示的化合物、其旋光异构体或其药学上可接受的盐作为有效成分,
化学式1:
在上述化学式1中,R1、R2及R3独立地为氢原子或RBz,上述R1、R2及R3中的至少一个为RBz,上述RBz为下述化学式2,
化学式2:
在上述化学式2中,
R2为氢原子、卤素、氰基、硝基、叠氮基、苯基、包含选自由N、O及S组成的组中的一种以上杂原子的5-6元杂环基、C1-6烷基、C1-6烷氧基、C1-6烷硫基、C2-6烯基、C2-6炔基或药剂学上可接受的盐。
11.一种预防或治疗癌症的方法,其特征在于,包括向个体给药权利要求1所述的用于预防或治疗癌症的药物组合物的步骤。
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