CN107496435B - 金线莲苷在制备抗疲劳药物中的应用 - Google Patents
金线莲苷在制备抗疲劳药物中的应用 Download PDFInfo
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Abstract
本发明涉及医药技术领域,具体是金线莲苷在制备抗疲劳药物或食品中的应用。本发明提供了金线莲苷新的医药用途,经药效学研究表明,本发明的金线莲苷可显著延长负重小鼠游泳时间,抗疲劳效果显著,可用于制备抗疲劳药物或食品。本发明为寻求新的抗疲劳药物提供了一种新的来源。
Description
技术领域
本发明涉及医药技术领域,具体地说,是以开唇兰属及其近缘属植物为原料制备的金线莲苷在抗疲劳药物或食品中的应用。
背景技术
疲劳是一种生理心理现象,是机体脑力与体力活动过度,精神刺激等因素所致。一般可以分为外周疲劳、中枢疲劳两类。随着经济的发展,生活节奏的加快,长时间的工作而得不到有效睡眠或生活不规律,导致越来越多的人感到疲惫、肌肉疼痛、注意力不集中、记忆力下降、情绪低落、睡眠障碍等。这些症状,临床上一般诊断为疲劳,涵盖外周和中枢疲劳,外周疲劳多发于体力劳动者,中枢疲劳多发于脑力劳动者。疲劳尤其是中枢疲劳长期得不到有效的治疗就会转变为慢性疲劳甚至“过劳死”,严重干扰病人的日常生活和工作。目前临床上的抗疲劳药物由于副作用、成瘾性、兴奋性等不良反应,而受到严格的限制。因此,寻求高效低毒的抗疲劳药物仍是世界医学界面临的一项艰巨任务和难题。
金线莲是闽台特色中草药,来源于兰科(Orchidaceae)开唇兰属AnoectochilusBlume植物花叶开唇兰,全草入药,具有清热凉血、祛风利湿、解毒等功效(黄有霖.福建中药材标准.福州:海风出版社,2006:154.),多用于治疗高血压、糖尿病、肝炎和肿瘤等症,疗效甚佳,因此金线莲在民间素有“药王”、“金草”等盛誉。除花叶开唇兰外,台湾银线兰、兴仁金线兰、丽蕾金线兰等多种同属和近缘属植物,由于其与金线莲药材性状及化学成分均相似,因此在民间多用作金线莲药材(张铁,万京,沐建华.文山地区金线莲种质资源初步调查.文山师范高等专科学校学报,2005,18(1):26-28;郑纯,黄以钟,季连芳.金线莲文献考证、原植物及商品调查.中草药,1996,27(3):169-171.)。金线莲类药材主要含有内酯苷类(如金线莲苷)、多糖类和黄酮类活性成分,尤其以金线莲苷和多糖含量较高。现代药理研究表明,金线莲苷是金线莲最主要活性成分之一,具有免疫调节(Xiang M,Liu T,Tan W,Ren H,LiH,Liu J,Cao H,Cheng Q,Liu X,Zhu H,Tuo Y,Wang J,Zhang Y.Effects ofkinsenoside,a potential immunosuppressive drug for autoimmune hepatitis,ondendritic cells/CD8+T cells communication in mice.Hepatology.2016,64(6):2135-2150.)、降血糖(Zhang Y,Cai J,Ruan H,Pi H,Wu J.Antihyperglycemic activity ofkinsenoside,a high yielding constituent from Anoectochilus roxburghii instreptozotocin diabetic rats.J Ethnopharmacol.2007,114(2):141-145.)、保肝(Hsieh WT,Tsai CT,Wu JB,Hsiao HB,Yang LC,Lin WC.Kinsenoside,a high yieldingconstituent from Anoectochilus formosanus,inhibits carbon tetrachlorideinduced Kupffer cells mediated liver damage.Journal ofEthnopharmacology.2011,135(2):440-449.)、降血脂(Rehman SU,Choi MS,Kim IS,LuoZ,Xue Y,Yao G,Zhang Y,Yoo HH.In Vitro Assessment of CYP-Mediated DrugInteractions for Kinsenoside,an Antihyperlipidemic Candidate.Molecules.2016,21(6).pii:E800.)、抗炎(Hsiao HB1,Hsieh CC,Wu JB,Lin H1,Lin WC.Kinsenosideinhibits the inflammatory mediator release in a type-II collagen inducedarthritis mouse model by regulating the T cells responses.BMC ComplementAltern Med.2016,16:80)和抗骨质疏松(Hsiao HB,Lin H,Wu JB,Lin WC.Kinsenosideprevents ovariectomy-induced bone loss and suppresses osteoclastogenesis byregulating classical NF-κB pathways.Osteoporos Int.2013,24(5):1663-1676.)等生物活性,但至今未见有关金线莲及其单体化合物金线莲苷用于抗疲劳方面的报道。
发明内容
本发明的目的在于提供金线莲苷新的医药用途。
本发明的第一方面,提供金线莲苷在制备抗疲劳药物或食品中的应用。
所述的金线莲苷的化学结构如下所示:
本发明的第二方面,提供一种抗疲劳药物或食品,所述的抗疲劳药物或食品中的活性成分为金线莲苷。
优选的,所述的抗疲劳药物或食品中还包括药学上可接受的辅料。
所述的金线莲苷,其制备方法包括以下步骤:
(A)制备提取液:将开唇兰属及其近缘属植物药材粉碎后,投入提取罐,用40~90%的乙醇热提2~3次,每次溶媒用量约为生药量的8~10倍,每次提取时间为1~2小时,合并提取液;
(B)精制浓缩干燥:将步骤A得到的提取液进行浓缩,浓缩液经乙酸乙酯萃取除杂后,将水层浓缩干燥得粗提物;
(C)分离纯化:将步骤B得到的粗提物溶于水后上样大孔吸附树脂,收集0~10%乙醇洗脱部分,浓缩干燥得金线莲苷粗品,上样正向硅胶柱,采用二氯甲烷-甲醇***洗脱,收集6:1洗脱部分,得金线莲苷(纯度>90%)。
优选的,步骤A中所述的开唇兰属及其近缘属植物选自花叶开唇兰、台湾银线兰、浙江金线兰、兴仁金线兰、滇南金线兰、长片金线兰、南丹金线兰、丽蕾金线兰、高金线兰、短唇金线兰、斑叶兰、大花斑叶兰、小小斑叶兰、毛梗斑叶兰、天全斑叶兰和血叶兰中的一种或两种以上。
优选的,步骤B中所述的浓缩是减压回收溶剂。
优选的,步骤C中所述的大孔树脂选自HP-20、AB-8、D-101、ZTC-1、HPD-100或DA201中的一种。
本发明采用负重小鼠强迫游泳模型(Liu Y,Li L,An S,Zhang Y,Feng S,Zhao L,Teng L,Wang D.Antifatigue Effects of Antrodia cinnamomea Cultured Myceliumvia Modulation of Oxidative Stress Signaling in a Mouse Model.Biomed ResInt.2017:9374026.),观察本发明提供的金线莲苷灌胃给药的抗疲劳作用。此动物模型是广泛认可的抗疲劳动物模型,实验主要针对运动性疲劳,包括中枢性疲劳和外周性疲劳(王丛笑,周军.对中药抗运动性疲劳研究中动物模型的一些思考.中国实验方剂学杂志,2009,15(3):83-85;郑澜,陆爱云.运动性疲劳动物模型的研究.中国体育科技,2003,39(2):20-23;田峰.对中枢与外周运动性疲劳的再认识.中国组织工程研究,2015,19(42):6849-6854)。
实验结果显示,金线莲苷100mg/kg连续灌胃给药18天后,对小鼠正常生理情况和体重变化无显著影响;空白组小鼠负重游泳时间为1577.7±303.1秒,金线莲苷给药组小鼠负重游泳时间为2775.2±770.3秒,与空白组存在显著性差异(p<0.01);且金线莲苷还能显著降低负重游泳小鼠血清中BLD(乳酸)的含量和提高小鼠血清中LDH(乳酸脱氢酶)的活性,说明金线莲苷具有很好的抗疲劳效果。
本发明所述的抗疲劳,是指预防或治疗外周疲劳或中枢疲劳,提高机体作业能力,降低血清中乳酸的含量和提高血清中乳酸脱氢酶的活性等,改善肌肉疼痛、注意力不集中、记忆力下降等症状。
本发明寻找到了理想的抗疲劳药物。本发明提供了金线莲苷新的医药用途,经药效学研究表明,本发明的金线莲苷可显著延长负重小鼠游泳时间,抗疲劳效果显著,可用于制备抗疲劳药物或食品。本发明为寻求新的抗疲劳药物提供了一种新的来源。
附图说明
图1是动物体重随时间变化图;
图2是金线莲苷对负重小鼠游泳时间的影响(mean±SD,n=10),其中**vs空白对照组,p<0.01;
图3是金线莲苷对负重游泳小鼠血清中BLD(乳酸)水平的影响(mean±SD,n=10),其中**vs空白对照组,p<0.01;
图4是金线莲苷对负重游泳小鼠血清中LDH(乳酸脱氢酶)水平的影响(mean±SD,n=10),其中*vs空白对照组,p<0.05。
具体实施方式
下面结合实施例和附图对本发明提供的具体实施方式作详细说明。
实施例1:金线莲苷的制备
(1)制备提取液:将开唇兰属及其近缘属植物药材粉碎后,投入提取罐,用40~90%的乙醇热提2~3次,每次溶媒用量约为生药量的8~10倍,每次提取时间为1~2小时,合并提取液;
(2)精制浓缩干燥:将上述提取液进行浓缩,浓缩液经乙酸乙酯萃取除杂后,将水层浓缩干燥得粗提物;
(3)分离纯化:将上述粗提物溶于水后上样大孔吸附树脂,收集0~10%乙醇洗脱部分,浓缩干燥得金线莲苷粗品,上样正向硅胶柱,采用二氯甲烷-甲醇***洗脱,收集6:1洗脱部分,得金线莲苷(纯度>90%)。
实施例2:金线莲苷的抗疲劳药效学实验
2.1实验材料
18~22g ICR小鼠(第二军医大学实验动物中心提供)20只,小鼠LDH(乳酸脱氢酶)和BLA(血乳酸)试剂盒(南京建成生物工程研究所)。主要仪器:5L烧杯(上海禾汽玻璃仪器有限公司)、酶标仪(BIO-RAD 550)、离心机(Labofuge 400R,Heraeus公司)、电子天平(FA110A型,上海精密科学仪器有限公司)。
2.2动物分组及实验处理
实验前将20只小鼠称重,按体质量随机分为2组,每组10只,自由饮食、进水。分为空白组和金线莲苷组。空白组:给予与给药组相同体积生理盐水;金线莲苷组:灌胃给药,每日一次,剂量为100mg/kg,连续给药18d。
2.3观察指标
(1)记录各组小鼠体质量变化情况,每9天称重一次。
(2)最后一天灌胃30min后,在小鼠尾根处负重6%(铅块)让其在5L烧杯中开始游泳至7s内头不能浮出水面计时停止,计为力竭时间。
(3)取出老鼠,拨眼球取血。血液4℃、3500r/min离心10分钟,取上清保存-80℃。根据试剂盒说明书进行操作测定BLA、LDH。
2.4实验结果
采用SPSS13.0对两组数据进行两样本t检验统计学分析,P<0.05时认为差异有统计学意义。
(1)小鼠体重变化
空白组小鼠体重逐渐升高,金线莲苷给药处理后小鼠体重基本平稳,和空白组比较无显著性差异,说明金线莲苷对小鼠正常生理情况基本没影响,如图1所示。
(2)小鼠负重游泳时间
如图2所示,空白组小鼠负重力竭游泳时间为1577.7±303.1秒,金线莲苷给药组小鼠力竭负重游泳时间为2775.2±770.3秒,与空白组存在显著性差异(p<0.01),表明金线莲苷可显著增加小鼠负重游泳时间。
(3)血清指标
如图3、图4所示,金线莲苷组与空白组相比p<0.05,金线莲苷能显著降低小鼠血清中乳酸BLA的含量和提高小鼠血清中乳酸脱氢酶LDH的活性,说明金线莲苷100m g/kg灌胃给药能显著改善负重小鼠动物模型血清中的疲劳相关因子水平。
鉴于上述药效实验结果,本发明的金线莲苷具有显著抗疲劳活性,因此可用于制备抗疲劳药物或食品。
以上已对本发明创造的较佳实施例进行了具体说明,但本发明创造并不限于所述实施例,熟悉本领域的技术人员在不违背本发明创造精神的前提下还可做出种种的等同的变型或替换,这些等同的变型或替换均包含在本申请权利要求所限定的范围内。
Claims (2)
1.金线莲苷在制备抗疲劳药物或食品中的应用。
2.金线莲苷的制备方法,其特征在于,包括以下步骤:
(A)制备提取液:将开唇兰属及其近缘属植物药材粉碎后,投入提取罐,用40~90%的乙醇热提2~3次,每次溶媒用量约为生药量的8~10倍,每次提取时间为1~2小时,合并提取液;所述的开唇兰属及其近缘属植物选自花叶开唇兰、台湾银线兰、浙江金线兰、兴仁金线兰、滇南金线兰、长片金线兰、南丹金线兰、丽蕾金线兰、高金线兰、短唇金线兰、斑叶兰、大花斑叶兰、小小斑叶兰、毛梗斑叶兰、天全斑叶兰和血叶兰中的一种或两种以上;
(B)精制浓缩干燥:将步骤A得到的提取液进行浓缩,浓缩液经乙酸乙酯萃取除杂后,将水层浓缩干燥得粗提物;所述的浓缩是减压回收溶剂;
(C)分离纯化:将步骤B得到的粗提物溶于水后上样大孔吸附树脂,收集0~10%乙醇洗脱部分,浓缩干燥得金线莲苷粗品,上样正向硅胶柱,采用二氯甲烷-甲醇***洗脱,收集6:1洗脱部分,得金线莲苷;所述的大孔树脂选自HP-20、AB-8、D-101、ZTC-1、HPD-100或DA201中的一种。
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