CN117946218A - 一种蝎毒多肽及其用于美白抗皱的化妆品或药物中的用途 - Google Patents
一种蝎毒多肽及其用于美白抗皱的化妆品或药物中的用途 Download PDFInfo
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- CN117946218A CN117946218A CN202410322953.3A CN202410322953A CN117946218A CN 117946218 A CN117946218 A CN 117946218A CN 202410322953 A CN202410322953 A CN 202410322953A CN 117946218 A CN117946218 A CN 117946218A
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- scorpion venom
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Abstract
本发明涉及一种蝎毒多肽及其用于美白抗皱的化妆品或药物中的用途。本发明通过从蝎子中提取得到蝎毒,将蝎毒酶解、超滤分离、柱分离等方法筛选获得了具有较好抗氧化特性的蝎毒抗氧化多肽7‑C3‑5。该多肽除了具有较好的抗氧化特性之外,还能增强皮肤保湿以及弹性的效果,从而能够较好的实现皮肤抗皱效果。所述多肽能够制备成为相应的美白、抗氧化、抗皱的化妆品或者药物。
Description
技术领域
本申请涉及化妆品以及药物领域,具体的涉及一种蝎毒多肽及其用于美白抗皱的化妆品或药物中的用途。
背景技术
蝎子的主要功效在于蝎毒,蝎毒的功效是全蝎煎剂的18倍。研究表明,蝎毒主要由非蛋白质部分和蛋白质部分组成。而蝎毒中的主要成份,是具有药理学活性的蛋白质。蛋白质部分中主要含50-70种氨基酸,其中含有人体必需的氨基酸有27种。非蛋白质部分主要包括一些脂类、如一些活性蛋白质、活性酶等,在临床上可以治疗脑血管类、神经类、血栓类和一些肿瘤疾病。蝎毒中的主要成分为具有药理活性的蛋白质,其中包括一些具有特异功能细胞因子、神经因子、细胞毒蛋白和一些工具酶。
蝎毒中的细胞毒蛋白能够快速破坏一些病毒细胞和亚病毒细胞的表面结构,对一些与此相关的疾病具有一定的效果:如破伤风、急性扁桃体炎、肺结核、顽固性湿疹、淋病、尖锐湿疣、肝炎、肝硬化和一些癌症。如:食道癌、结肠癌、肝癌、肺癌、乳腺癌、胃癌、脑良恶性黑色素瘤、癌性胸膜炎等。体外细胞培养的实验证明:蝎毒蛋白有抑制肿瘤细胞功能。本身有抑制杀灭肿瘤细胞作用。蝎毒蛋白可双向调节人体免疫系统,维护人体免疫系统平衡。一方面蝎毒具有抗疲劳,明显提高免疫力的作用,另一方面蝎毒蛋白还能调节人体反应,因而对自身免疫性疾病(如类风湿)有很好效果。蝎毒蛋白经长期毒性试验和急性毒性试验均表明:蝎毒蛋白无毒副作用,适合人体长期应用。经常服用蝎毒可以提高人体免疫力、防衰老、促长寿、恢复肝功能。
随着经济的快速发展和生活水平的不断提高,现代社会对化妆品的关注度越来越高。人体皮肤细胞完全更新一次需要历时三个月,在新更新的细胞还未到达皮肤表层时就已经被各种自由基氧化;此外,随着人体的衰老、基因、环境等的影响,胶原蛋白、弹性蛋白减少,最终导致皱纹产生。皱纹是皮肤老化的典型症状,由弹性丧失引起,弹性丧失与皮肤真皮组织弹性相关的胶原蛋白和弹性蛋白减少有关。胶原蛋白约占人类真皮细胞外基质(ECM)的90%,I型胶原蛋白是皮肤和结缔组织中最丰富的结构蛋白,占总胶原蛋白的80%,其结构变化被认为是皮肤老化和皱纹形成的主要原因。
但是目前,针对蝎毒研究主要停留在抗癌、提高免疫力等方面,相应的美白抗皱、抗衰老功效的研究还没有报道。
发明内容
本发明从蝎毒中分离筛选鉴定得到具有较好抗氧化特性的多肽,其命名为7-C3-5,其氨基酸序列如SEQ ID NO:1所示。
本发明的多肽具有较好的抗氧化特性以及增强皮肤保湿以及弹性的效果,从而能够较好的实现皮肤抗皱效果。
抗氧化特性一般与美白特性紧密相关,多肽具有抗氧化特性一般对应也就有较好的美白效果。
进一步的,本发明的抗氧化肽具有良好的皮肤渗透性,含有的多种疏水性氨基酸可以修复和增强皮肤的屏障功能,防止皮肤脱水。
进一步的,本发明的多肽还可以被修饰,如保守性取代,但是仍然保持生物学活性。
保守取代的实例是在下列氨基酸组内发生的取代:碱性氨基酸(如精氨酸、赖氨酸和组氨酸)、酸性氨基酸(如谷氨酸和天冬氨酸)、极性氨基酸(如谷氨酰胺、天冬酰胺)、疏水性氨基酸(如亮氨酸、异亮氨酸和缬氨酸)、芳香氨基酸(如苯丙氨酸、色氨酸和酪氨酸),以及小分子氨基酸(如甘氨酸、丙氨酸、丝氨酸、苏氨酸和甲硫氨酸)。
本发明中氨基酸序列的取代、缺失或添加是本领域的常规技术,优选这种氨基酸变化为:小的特性改变。
进一步的,本发明提供7-C3-5多肽在制备用于皮肤抗氧化、保湿以及提高皮肤弹性抗皱的化妆品中的用途。
按照本发明的化妆品制剂可以在例如太阳霜,太阳胶,晒后产品,日霜,晚霜,面膜,爽身水,清洁乳剂,化妆品,唇膏,爽身粉,眼部化妆品,发罩(hairmask)护发素,洗发剂,淋浴凝胶,淋浴油,浴油中使用。这些产品可以用本领域技术人员已知的方式生产。
本发明使用的油可以是常用的化妆品油,如矿物油;水合聚异丁烯;合成的角鲨烷或来自天然产物的角鲨烷;支化或未支化的,饱和或不饱和的化妆品用酯或醚;植物油;或它们两个或几个的混合物。
特别适合的油是例如氢化了的聚异丁烯,聚异戊二烯,角鲨烷类,酸十三烷基酯,三甲基丙烷-三异硬脂酸酯,柠檬酸异癸酯,酸新戊二醇酯,PPG-15-硬脂酰醚和植物油,如金盏草油,霍霍巴油,鳄梨油,澳洲坚果油,蓖麻油,小麦胚芽油,葡萄籽油,烛果油,蓟油,月见草油,红花油或它们的几个的混合物。
按照本发明的化妆品组合物还可以作为凝胶提供。合适的形成凝胶的试剂包括卡波姆(Carbomer),汉生胶(XanthaneGum),角叉菜胶,Arabine,瓜耳豆胶,琼脂,藻酸盐类和纤基乙酸钠类,羧甲基纤维素,羟乙基纤维素,季铵化的纤维素,季铵化的瓜耳豆,某些聚丙烯酸酯类,聚乙烯醇,聚乙烯吡咯烷酮,蒙脱石。
按照本发明的制剂可添加颜料,颜料混合物或有颜料类似作用的粉末。这类颜料也包括有上釉作用的颜料或颜料如氧化铁,天然硅酸铝,如赭石,氧化钛,云母,高岭土,含镁粘土,如本影或代赭石,碳酸钙,滑石,云母-钛氧化物,云母-钛铁氧化物,氯氧化铋,尼龙珍珠,陶瓷珍珠,膨胀型和非膨胀型合成的聚合物粉末,研磨成粉的天然有机化合物,如海底(ground)固体藻,海底植物部分,密封的和未密封的谷类淀粉以及云母-钛氧化物-有机染料。
进一步的,本发明的药物可包括一种或多种已知或换句话讲可有效用于药物组合物的任选组分,前提条件是该任选组分与本发明上文所述药物活性物质在物理和化学上相容,或换句话讲不会不适当地损害产品的稳定性、美观性或性能。可以包括在粉末药物组合物中的任选组分的浓度按所述组合物的重量计在约0.001%至约89.8%,优选约0.01%至约80%的范围内变化。这些任选组分包括例如调味剂、甜味剂、染料、抗氧化剂(包括柠檬酸、抗坏血酸)、防腐剂,等等的物质。合适的任选调味剂的非限制性实施例包括例如茴芹、胡椒薄荷油、丁香油、桉树油、柠檬、酸橙、蜂蜜、蜜柠檬、红果、薄荷、柚子、橙、葡萄、樱桃、樱桃可乐、浆果,以及它们的混合物的物质。合适的任选甜味剂的非限制性实施例包括例如天冬甜素、糖精及其盐(包括糖精钙和糖精钠)、天然糖,以及它们的混合物的物质。
上文所述的药物还含有药学上可接受的载体。药学上可接受的载体是指药学领域常规的药物载体,例如:稀释剂、赋形剂如水等,填充剂如淀粉、蔗糖等;黏合剂如纤维素衍生物、藻酸盐、明胶和聚乙烯吡咯烷酮;湿润剂如甘油;崩解剂如琼脂、碳酸钙和碳酸氢钠;吸收促进剂如季铵化合物;表面活性剂如十六烷醇;吸附载体如高岭土和皂黏土;润滑剂如滑石粉、硬脂酸钙和镁、以及和聚乙二醇等。另外还可以在组合物中加入其它辅剂如香味剂、甜味剂等。
用于片剂制剂的适宜的可药用赋形剂包括例如,惰性稀释剂例如乳糖、碳酸钠、磷酸钙或碳酸钙;制粒和崩解剂例如玉米淀粉和藻酸;粘合剂例如淀粉;润滑剂例如硬脂酸镁、硬脂酸或滑石粉;防腐剂例如对羟基苯甲酸乙酯或丙酯,和抗氧剂,例如抗坏血酸。片剂制剂可以是未包衣的,也可以采用包衣以改变其崩解作用以及活性成分在胃肠道内的后续吸收作用,或改进其稳定性和/或外观,在任意情况中,均可使用该领域熟知的常规包衣剂和方法。
口服使用的组合物可以是硬明胶胶囊的形式,其中活性成分与惰性固体稀释剂例如碳酸钙、磷酸钙或高岭土混合,或是软明胶胶囊形式,其中活性成分与水或油例如花生油、液体石蜡或橄榄油混合。
水性混悬剂一般含有微粉形式的活性成分和一种或多种助悬剂,所述助悬剂例如为羧甲基纤维素钠、甲基纤维素、羟丙基甲基纤维素、藻酸钠、聚乙烯-吡咯烷酮、西黄蓍胶和阿拉伯胶;分散或湿润剂,例如卵磷脂或烯基氧化物与脂肪酸的缩合物(例如聚氧乙烯硬脂酸酯),或环氧乙烷与长链脂肪醇的缩合产物,例如十七氧化亚乙基鲸蜡醇,或环氧乙烷与衍生自脂肪酸与己糖醇的偏酯的缩合产物,例如聚氧化乙烯山梨糖醇一油酸酯,或环氧乙烷与衍生自脂肪酸和己糖醇酐的偏酯的缩合产物,例如聚乙烯脱水山梨糖醇一油酸酯。水性混悬剂还可含有一种或多种防腐剂(例如对羟基苯甲酸乙酯或丙酯)、抗氧剂(例如抗坏血酸)、着色剂、矫味剂、和/或甜味剂(例如蔗糖,糖精和天冬酰苯丙氨酸甲酯)。
本发明多肽可以组合物的形式通过口服、鼻吸入、直肠或肠胃外给药的方式施用于需要这种治疗的患者。用于口服时,可将其制成常规的固体制剂如片剂、粉剂、粒剂、胶囊等,制成液体制剂如水或油悬浮剂或其他液体制剂如糖浆、酏剂等;用于肠胃外给药时,可将其制成注射用的溶液、水或油性悬浮剂等。优选的形式是片剂、胶囊和注射剂。本发明药物组合物的各种剂型可以按照药学领域的常规生产方法制备。例如使活性成分与一种或多种载体混合,然后将其制成所需的剂型。本发明的多肽可以用于口服美容类产品中。
本发明的药物组合物优选含有重量比为0.1%~10%的多肽作为活性成分。
有益效果:本发明通过从蝎子中提取得到蝎毒,将蝎毒酶解、超滤分离、柱分离等方法筛选获得了具有较好抗氧化特性的蝎毒抗氧化多肽7-C3-5。该多肽除了具有较好的抗氧化特性之外,还能增强皮肤保湿以及弹性的效果,从而能够较好的实现皮肤抗皱效果。所述多肽能够制备成为相应的美白、抗氧化、抗皱的化妆品或者药物。
附图说明
图1 各组分的自由基清除活性效果图
图2 多肽对DPPH的清除能力效果图
图3 多肽对ABTS自由基的清除能力效果图
实施方式
本领域技术人员可以借鉴本文内容,适当改进工艺参数实现。特别需要指出的是,所有类似的替换和改动对本领域技术人员来说是显而易见的,它们都被视为包括在本发明。本发明的方法及应用已经通过较佳实施例进行了描述,相关人员明显能在不脱离本发明内容、精神和范围内对本文所述的方法和应用进行改动或适当变更与组合,来实现和应用本发明技术。以下实施案例中的方法、设备、材料,如果未进行特别说明,均为本领域常规方法、设备和材料,均可由市场购得。
实施例1 蝎毒抗氧化多肽的筛选及制备
用夹子夹住健壮的蝎子的蝎尾,人工刺激其头胸部,同时用高频电流10伏刺激腺体肌肉收缩获取毒液,每隔2周提取一次。将蝎毒加入木瓜蛋白酶酶解。酶解条件是优化后的加酶量5.0%、温度 52℃、酶解时间 3.5 h。沸水浴中灭酶10min,然后迅速冷却至室温,置于离心机中,以5000r/min离心10min,取上清液备用。
首先使用分子质量截留范围为10000Da和1500Da的超滤膜对酶解产物进行超滤分离,将其分为3个分子质量范围不同的组分,调整出口压力不超过0.2MPa。分别收集不同分子质量段的分级产物,冻干后采用DPPH自由基清除法测定其抗氧化活性。具体方法为:配制浓度为1×10-5mol/L的DPPH乙醇溶液,避光保存。将2mL,0.1mmol/L的DPPH无水乙醇溶液加入到含有2mL不同酶解样品的洁净试管中,混匀。室温下放置30min后,于517nm处测定吸光度,吸光值越小,表明自由基清除能力越强。清除率(%)=〔1-(Ai-Aj)/A0〕×100%。式中,A0:2mL,0.1mmol/L的DPPH无水乙醇溶液+2mL的样品溶剂,空白对照;Ai:2mL,0.1mmol/L的DPPH无水乙醇溶液+2mL的样品;Aj:2mL的无水乙醇+2mL的样品。结果如图1所示。
结果如图1所示,分子质量小于1500Da的组分具有较强的自由基清除活性,清除率达到了(53.42±2.16)%。收集该组分,真空浓缩后冻干,于4℃下保存待用。
将具有最强抗氧化活性的分子质量小于1500Da的超滤组分用pH4.0、20mmol/L的醋酸-醋酸钠缓冲液溶解后用于SP-Sphadex C-25离子交换层析柱。离子交换层析柱先用0.02mol/L的醋酸-醋酸钠缓冲液(pH4.0)进行充分平衡。上样后,再用0.02mol/L的醋酸-醋酸钠缓冲液(pH4.0)进行平衡,洗去未吸附组分并收集,以含0~0.35mol/LNaCl的0.02mol/L,pH4.0乙酸-乙酸钠缓冲液线性梯度洗脱,收集不同的洗脱峰组分。流速为0.5mL/min,10min/每管,225nm检测吸收值。吸收值相同的合并一起,共获得组分11个,采用前述的DPPH自由基清除活性检测发现,7号组分具有最强的抗氧化特性。
将7号组分按照5:1进行浓缩,随后凝胶色谱柱SephadexG-50(Φ1.6cm×100cm)先用去离子水平衡。上样完后再用去离子水进行洗脱,直至所有肽被洗脱出来。流速为0.4mL/min,25min每管,225nm检测。分别收集洗脱峰,并测定其DPPH自由基清除活性,其中7-C3组分具有最强的抗氧化特性。将7-C3组分进一步的采用反相高效液相色谱(RP-HPLC)进行分离,获得了抗氧化特性最强的7-C3-5组分,将该组分进行质谱鉴定,获得了其氨基酸序列如SEQ ID NO:1所示。
实施例2 蝎毒多肽7-C3-5抗氧化能力鉴定
多肽对ABTS自由基的清除能力:将0.4mL不同浓度的多肽,加入3.6mLABTS工作液(OD734nm为0.700),混合均匀后,室温下静置10min,在734nm处测定吸光值。空白样采用双蒸水。抑制率=[(A1-A0)/A0]×100%,其中A0(加0.4mL双蒸水和3.6mL ABTS工作液)为加入样品前的吸光值,A1为加入样品后的吸光值。
多肽对DPPH的清除能力:配制浓度为1×10-5mol/L的DPPH乙醇溶液,避光保存。将2mL,0.1mmol/L的DPPH无水乙醇溶液加入到含有2mL不同浓度多肽的洁净试管中,混匀。室温下放置30min后,于517nm处测定吸光度,吸光值越小,表明自由基清除能力越强。清除率(%)=〔1-(Ai-Aj)/A0〕×100%。式中,A0:2mL,0.1mmol/L的DPPH无水乙醇溶液+2mL的样品溶剂,空白对照;Ai:2mL,0.1mmol/L的DPPH无水乙醇溶液+2mL的样品;Aj:2mL的无水乙醇+2mL的样品。二个实验均以GSH作为对照。
图2和图3的结果表明,DPPH、ABTS自由基清除实验表明,随着多肽浓度的增加,其抗氧化能力越强。并且通过分析发现,本发明的多肽对DPPH和ABTS的IC50为:0.42、0.03mg/mL,具有较好的抗氧化特性。
实施例3 蝎毒多肽7-C3-5安全性鉴定
取小鼠10只,体重(28±2)g,雌雄各半,适应性喂养3d。于试验前24h背部脊柱两侧进行脱毛,面积每侧约2cm×2cm,分笼饲养。取5只小鼠,涂抹本发明的多肽5mg/mL, 早晚各一次,连续涂抹7d。另外5只小鼠,涂抹生理盐水作为对照,也是连续涂抹7d。7d后,检测多肽涂抹区发现,均未出现局部红斑及水肿,与空白对照组无差异。表明本发明的多肽具有较好的安全性。
实施例4 蝎毒多肽7-C3-5的功效验证
蝎毒多肽抗皱乳液的制备:将1%的十八醇、3%的聚二甲基硅氧烷、1%辛酸、2%山梨坦橄榄油酸酯加热至80~90℃并搅拌均匀;并缓慢倒入混合均匀的0.03%透明质酸钠、0.2%黄原胶、3% 1,3-丁二醇、0.1% EDTA-2Na、1%卡波940中,5000r/min均质5min,冷却至45℃,加入香精、防腐剂和1%蝎毒多肽7-C3-5,使用0.1mol/L的NaOH溶液调节pH至6.5,搅拌冷却至25℃,即可出料灌装。
对照乳液为上述乳液中不加多肽。
受试对象主要来自志愿者,共50例。其中男30例,女20例,年龄40-60岁。将50例符合纳入标准的受试对象随机分为试验组和对照组,各25例。两组性别、年龄、皱纹程度经统计学检验差异无统计学意义(P>0.05)。
测试前,受试者统一用清水清洗前臂内侧,并做好测量标记。试验区域间隔1cm,每处试验区域为3cm×3cm,按2mg/cm2的用量称取护肤品,使用乳胶指套将护肤品均匀涂抹于试验区内,每天早晚涂抹一次,连续涂抹30天。
角质层含水量的测定:采用Corneometer CM825水分测试探头测定受试者前臂内侧标记处使用样品前及连续使用样品30 d后皮肤含水量的变化,来评价化妆品的保湿效果。每个测试点平行测5次取平均值,结果用电容值表示,无单位。结果如表1所示。
表1 不同实验组对角质层含水量的影响
分组 | 含水量 |
蝎毒多肽抗皱乳液 | 59.63±2.30* |
对照乳液 | 42.18±1.95 |
测试前含水量 | 36.51±0.34 |
*表示与对照乳液相比,差异显著(P<0.05)。
从表1的结果可以看出,蝎毒多肽抗皱乳液连续涂抹30d后,角质层含水量得到显著的提示,使得皮肤更加水嫩光滑。
皮肤弹性测试:采用MPA580弹性纤维组织测试探头测定受试者前臂内侧标记处使用样品前及连续使用样品30 d后皮肤弹性的变化,来评价化妆品对皮肤弹性的影响。恒定负压作用时,皮肤最大拉升量用Uf表示,取消测试负压到下次施加负压时的皮肤恢复值用Ua表示,皮肤弹性参数R2=Ua/Uf,R2数值越大,表明皮肤弹性越好。结果如表2所示。
表2 不同实验组对皮肤弹性的影响
分组 | 皮肤弹性(R2) |
蝎毒多肽抗皱乳液 | 0.78±0.09* |
对照乳液 | 0.56±0.06 |
测试前皮肤弹性 | 0.41±0.03 |
*表示与对照乳液相比,差异显著(P<0.05)。
由表2可知,受试者未使用护肤品时弹性参数平均值为0.41,而使用蝎毒多肽抗皱乳液处理后,皮肤弹性显著提升到0.78,与对照乳液的0.56相比,抗氧化肽具有很好的使皮肤弹性增大效果,从而起到较好的抗皱效果。
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。
最后应说明的是:以上各实施例仅用以说明本发明的技术方案,而非对其限制;尽管参照前述各实施例对本发明进行了详细的说明,但本领域的普通技术人员应当理解:其依然可以对前述各实施例所记载的技术方案进行修改,或者对其中部分或者全部技术特征进行等同替换;而这些修改或者替换,并不使相应技术方案的本质脱离本发明各实施例技术方案的范围。
Claims (7)
1.一种蝎毒抗氧化多肽,其命名为7-C3-5,其氨基酸序列如SEQ ID NO:1所示。
2.如权利要求1所述的蝎毒抗氧化多肽在制备用于增强皮肤含水量、抗氧化以及通过增加皮肤弹性而实现抗皱的化妆品中的用途。
3.如权利要求2所述的用途,其特征在于所述的化妆品是乳液。
4.如权利要求3所述的用途,其特征在于所述的乳液通过如下方法制备:将1%的十八醇、3%的聚二甲基硅氧烷、1%辛酸、2%山梨坦橄榄油酸酯加热至80~90℃并搅拌均匀;并缓慢倒入混合均匀的0.03%透明质酸钠、0.2%黄原胶、3% 1,3-丁二醇、0.1% EDTA-2Na、1%卡波940中,5000r/min均质5min,冷却至45℃,加入香精、防腐剂和1%蝎毒多肽7-C3-5,以上物质的百分比均为质量百分比,使用0.1mol/L的NaOH溶液调节pH至6.5,搅拌冷却至25℃,即可出料灌装获得相应的乳液。
5.如权利要求1所述的蝎毒抗氧化多肽在制备抗氧化药物中的用途。
6.如权利要求5所述的用途,其特征在于所述的药物中还含有药学上可接受的载体。
7.如权利要求6所述的用途,其特征在于所述的载体包括赋形剂以及pH调节剂。
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