CN106822198A - 一种痰火草提取物及其在制备治疗肺癌药物中的应用 - Google Patents
一种痰火草提取物及其在制备治疗肺癌药物中的应用 Download PDFInfo
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Abstract
本发明属于中药领域,具体涉及一种痰火草提取物的制备方法,及其在治疗肺癌药物中的应用。本发明提供的具有治疗肺癌作用的痰火草提取物制备方法,包括前处理、粗提、过滤、浓缩、萃取以及获得提取物步骤。所述痰火草提取物为石油醚部位提取物、氯仿部位提取物、乙酸乙酯部位提取物、正丁醇部位提取物和水层部位提取物。本发明提供的痰火草提取物,对人肺腺癌细胞A549有显著的抑制作用,并具有明显的量效关系。本发明以痰火草为原料,制得有效部位提取物,加药用辅料可制备成颗粒剂、胶囊、片剂、丸剂、溶液剂等制剂,可应用于治疗肺癌的药物或者辅助治疗肺癌的功能性食品。本发明的制备方法工艺简单、稳定,易于批量生产,具有良好的药用及功能食品开发前景。
Description
技术领域:
本发明属于中药领域,涉及一种痰火草提取物的制备,可用于肺癌的治疗,具体地说是一种痰火草提取物及其在制备治疗肺癌药物中的应用。
背景技术:
肺癌是发病率和死亡率增长最快,对人群健康和生命威胁最大的恶性肿瘤之一。近50年来许多国家都报道肺癌的发病率和死亡率均明显增高,男性肺癌发病率和死亡率均占所有恶性肿瘤的第一位,女性发病率占第二位,死亡率占第二位。非小细胞型肺癌(non-small cell lungcancer,NSCLC)是最常见的一类肺癌,包括鳞状细胞癌(鳞癌)、腺癌、大细胞癌,与小细胞癌相比其癌细胞生长分裂较慢,扩散转移相对较晚。
临床上,肺癌的治疗采用以手术为主、化疗或放疗为辅的综合疗法。非小细胞肺癌占肺癌发病率的80%-85%,5年内生存率不到15%,目前最有效的化疗方案对其晚期的缓解率也仅为30%左右。因此,寻求新的有效的肺癌治疗药物,仍是肺癌化疗迫切需要解决的课题之一。
痰火草,别名:癌草、围夹草、青竹壳菜、青鸭跖草,为鸭跖草科水竹草属植物大苞水竹叶Murdannia bracteata(C.B.Clarke)O.Kuntze ex J.K.Morton[Aneilema nudiflorum R.Br.var.bracteatum C.B.Clarke;A.bracteatum(Clarke)O.Kuntze]的全草,具有化痰散结、清热通淋等功效。痰火草主要分布于广东、海南、广西、云南等地,可人工种植,民间用于治疗肺痨咳嗽、淋巴结结核、痔疮等症。但迄今为止,痰火草应用疾病治疗,仅流行于民间百姓使用,尚未见有关痰火草提取物治疗肺癌的研究报道和专利。
痰火草生长于海拔500-850m的水沟边及密林下,不仅有大量的野生资源,且已有成熟的人工栽培技术,应用于屋顶及天台地被绿化。目前,痰火草的药用只在民间,如何发掘痰火草这一民间特色植物的药用价值,对于寻找肺癌防治的药物,具有广阔的开发潜力。
发明内容:
本发明的目的是提供痰火草提取物的一种新用途,该新用途是痰火草提取物在制备抗癌药物中的应用,尤其是在制备治疗非小细胞肺癌药物中的应用,可应用于治疗肺癌的药物或者在制备辅助治疗肺癌的功能性食品。
本发明所述痰火草提取物为油醚部位提取物、氯仿部位提取物、乙酸乙酯部位提取物、正丁醇部位提取物和水层部位提取物。
本发明提供了所述的痰火草提取物制备方法,具体包括以下步骤:
(1)前处理:将痰火草进行干燥并粉碎成粗粉;
(2)粗提:体积浓度60%~90%的乙醇溶液回流提取2~3次,每次1~3个小时;
(3)过滤;
(4)浓缩:将滤液进行减压浓缩,浓缩至相对密度为1.05~1.35;
(5)获得提取物:将浓缩液进行溶剂回收后冷冻干燥或真空干燥。
进一步,步骤(4)与步骤(5)之间还包括萃取步骤:用浓缩液3倍体积的有机溶剂进行萃取,将萃取液减压浓缩。
优选的,所述有机溶剂为石油醚、氯仿、乙酸乙酯和正丁醇。
可选的,萃取步骤为用石油醚、氯仿、乙酸乙酯和正丁醇依次进行萃取,或者为用石油醚、氯仿、乙酸乙酯和正丁醇之中的两种依次进行萃取;或者为用石油醚、氯仿、乙酸乙酯和正丁醇之中的一种进行萃取;优选地,萃取步骤为用石油醚、氯仿、乙酸乙酯和正丁醇依次进行萃取。
可选的,步骤(1)中痰火草干燥粗粉的重量与步骤(2)中所述乙醇的体积比为1∶5~1∶20。
本发明提供了一种具有治疗肺癌作用的痰火草提取物,该提取物由所述制备方法所制得。
进一步,所述痰火草提取物为石油醚部位提取物、氯仿部位提取物、乙酸乙酯部位提取物、正丁醇部位提取物和水层部位提取物。
本发明还提供了一种具有治疗肺癌作用的痰火草提取物在治疗肺癌的药物方面的应用或者在制备辅助治疗肺癌的功能性食品方面的应用,所述药物,优选药物剂型为片剂、颗粒剂、丸剂、胶囊或者溶液剂。
优选的,所述丸剂为滴丸,所述胶囊为硬胶囊或软胶囊,所述溶液剂为糖浆剂或合剂,所述的药物包括痰火草提取物以及药学可接受的载体。
根据本发明提供的一种痰火草提取物及其在制备治疗肺癌药物中的应用,能够带来以下有益效果:根据本发明提供的具有治疗肺癌作用的痰火草提取物因具有明显的抑制人肺腺癌A549细胞增殖、细胞凋亡的作用,能够应用于治疗肺癌的药物和制备辅助治疗肺癌的功能性食品,可用于肺癌的治疗或辅助治疗,从而扩大了痰火草的药用范围,提高了痰火草的药用价值。此外,本发明提供的具有治疗肺癌作用的痰火草提取物制备方法简单、易操作,为痰火草提取物在治疗肺癌的药物和制备辅助治疗肺癌的功能性食品的开发利用奠定了基础。
附图说明:
图1本发明实施例提供的痰火草提取物制备方法的流程示意图
图2痰火草各部位提取物对人肺腺癌细胞A549增殖抑制的剂量-效应曲线
图3痰火草乙酸乙酯提取物对肺腺癌细胞A549细胞形态的影响
图4痰火草乙酸乙酯提取物对肺腺癌细胞A549细胞凋亡的影响
具体实施方式
下面结合具体实施例进一步阐述本发明,使本领域技术人员能更全面的理解本发明,附图和具体实施例不旨在对本发明进行限定,本发明的范围由所附权利要求限定。
图1为本发明实施例提供的具有治疗肺癌作用的痰火草提取物的制备方法的流程示意图,包括以下步骤:
(1)前处理:将痰火草进行干燥并粉碎成粗粉;
(2)粗提:体积浓度60%~90%的乙醇溶液回流提取2~3次,每次1~3个小时;
(3)过滤;
(4)浓缩:将滤液进行减压浓缩,浓缩至相对密度为1.05~1.35;
(5)获得提取物:将浓缩液进行溶剂回收后冷冻干燥或真空干燥。
其中,步骤(1)中痰火草干燥粗粉的重量与步骤(2)中所述乙醇的体积比为1∶5~1∶20。
步骤(2)中用60%~90%的乙醇溶液回流提取2~3次,每次1~3个小时。乙醇浓度优选80%;第一次回流提取的时间可为2~3个小时,第二次回流提取的时间可为1~2个小时,第三次回流提取的时间可为1~2个小时。
对于痰火草提取物的提取方法并不局限于乙醇回流提取法,还可以采用水煎法、超声协同回流法、微波协同回流法、表面活性剂协同超声法、表面活性剂协同微波法等。
本发明中提供的痰火草提取物的提取方法中的乙醇回流提取法并不局限于:步骤(1)中痰火草干燥粗粉的重量与步骤(2)中所述乙醇的体积比为1∶5~1∶20,用体积浓度60%~90%的乙醇溶液回流提取2~3次,每次1~3个小时。因为提取时间、乙醇溶剂的用量倍数和浓度对痰火草提取物的提取率都是有影响的,所以上述提取条件可依药材质量、提取方法来确定。
步骤(3)中过滤后,将滤液合并,然后再进行下一步骤。
参照图1,步骤(4)与步骤(5)之间还包括萃取步骤:用浓缩液3倍体积的有机溶剂进行萃取,将萃取液减压浓缩。上述有机溶剂为石油醚、氯仿、乙酸乙酯和正丁醇。
萃取步骤为用石油醚、氯仿、乙酸乙酯和正丁醇依次进行萃取,或者为用石油醚、氯仿、乙酸乙酯和正丁醇之中的两种依次进行萃取;或者为用石油醚、氯仿、乙酸乙酯和正丁醇之中的一种进行萃取;优选地,萃取步骤为用石油醚、氯仿、乙酸乙酯和正丁醇依次进行萃取。
经大量的药理实验可知,痰火草提取物在体外具有一定抗肺癌的作用,其中,乙酸乙酯部位提取物是最主要的活性部位。
本发明提供了一种具有治疗肺癌作用的痰火草提取物,该提取物由所述制备方法所制得。所述痰火草提取物为石油醚部位提取物、氯仿部位提取物、乙酸乙酯部位提取物、正丁醇部位提取物和水层部位提取物。
本发明还提供了一种具有治疗肺癌作用的痰火草提取物在治疗肺癌的药物方面的应用或者在制备辅助治疗肺癌的功能性食品方面的应用,所述药物,优选药物剂型为片剂、颗粒剂、丸剂、胶囊或者溶液剂。所述丸剂为滴丸,所述胶囊为硬胶囊或软胶囊,所述溶液剂为糖浆剂或合剂等。
将上述痰火草提取物进行:干燥,粉碎,加入辅料适量,制成片剂、颗粒剂;与聚乙二醇加热熔融混匀后,滴入不相混溶的冷凝液中,收缩冷凝制成球形或类球形的制剂,分装即得滴丸;加入炼蜜收膏,加入适量辅料,分装即得煎膏剂;80℃减压干燥,粉碎,加入辅料适量,混匀,分装在空心胶囊或密封于软质囊材中,分装即得硬胶囊产品或软胶囊产品;加入辅料适量,制成合剂或糖浆剂。
实施例1:一种采用表面活性剂协同回流提取法,制备痰火草提取物的方法,其步骤如下:
取痰火草1kg,粉碎成粗粉,加入12倍量的70%乙醇,加入1.0%的十二烷基硫酸钠,加热回流提取3次,分别提取3h、2h和1h,过滤,合并3次滤液,减压回收乙醇,得痰火草流浸膏;依次用石油醚、氯仿、乙酸乙酯和正丁醇进行萃取,减压回收有机溶剂,浓缩至比重1.15,得各部位浸膏;各部位浸膏真空干燥,粉碎,得痰火草石油醚部位提取物、氯仿部位提取物、乙酸乙酯部位提取物、正丁醇部位提取物和水层部位提取物。
实施例2:一种采用超声波-回流协同提取法,制备痰火草提取物的方法,其步骤如下:
取痰火草1kg,粉碎成粗粉,加入10倍量的80%乙醇,超声波加热回流提取45min,超声功率200W,加热回流提取3次,分别提取2h、2h和1h,过滤,合并3次滤液,减压回收乙醇,得痰火草流浸膏;依次用石油醚、氯仿、乙酸乙酯和正丁醇进行萃取,减压回收有机溶剂,浓缩至比重1.25,得各部位浸膏;各部位浸膏真空干燥,粉碎,得痰火草石油醚部位提取物、氯仿部位提取物、乙酸乙酯部位提取物、正丁醇部位提取物和水层部位提取物。
实施例3:一种采用水煎法,制备痰火草提取物的方法,其步骤如下:
取痰火草1kg,粉碎成粗粉,加入15倍量的水,加热煎煮提取3次,分别提取3h、2h和2h,过滤,合并3次滤液,减压浓缩,得痰火草流浸膏;依次用石油醚、氯仿、乙酸乙酯和正丁醇进行萃取,减压回收有机溶剂,浓缩至比重1.15,得各部位浸膏;各部位浸膏真空干燥,粉碎,得痰火草石油醚部位提取物、氯仿部位提取物、乙酸乙酯部位提取物、正丁醇部位提取物和水层部位提取物。
实施例4:一种采用湿法制粒法,制备痰火草提取物的片剂,其步骤如下:
实施例2制备的痰火草乙酸乙酯提取物20g,与淀粉20g、糊精30g和乳糖30g于混合机中混合15min;在混合粉末中,分次加入2%羧甲基纤维素钠溶液,混合均匀制成软材;将软材过20目筛制湿颗粒,置烘箱50℃干燥4小时,干颗粒过16目筛整粒,筛除过60目的细粉。将1.0%硬脂酸镁加入到干颗粒中,混合5分钟;调节片重100mg,硬度6~10千克,脆碎度0.6%以下,将总混物进行压制成片。压片过程中,对片重、硬度、脆碎度等跟踪测量,保证片剂要求的相应指标在可控范围内,制得的痰火草提取物片剂。
实施例5:一种采用滴制法,制备痰火草提取物的滴丸,其步骤如下:
实施例2制备的痰火草乙酸乙酯提取物6g,与聚乙二醇-400016g、聚乙二醇-60008g水浴加热至熔融,冷却剂为药用二甲基硅油,料液温度为80℃,冷却温度为6℃,滴距为4cm,滴头直径3mm,滴制成丸,干燥,制成痰火草提取物滴丸剂。
实施例6:一种采用热溶法法,制备痰火草提取物的糖浆剂,其步骤如下:
实施例3制备的痰火草乙酸乙酯提取物10g,加注射用水100mL,80℃加热成混悬液;加入蔗糖834g,搅拌使溶化,再加入用水溶化后的阿胶溶液及防腐剂适量,搅匀,加入上述油状物,煮沸30分钟,滤过,加水调整总量,制成痰火草提取物糖浆剂。
为考察本发明提供的痰火草提取物的治疗肺癌作用,按照实施例2制备痰火草提取物。采用人肺腺癌细胞A549实验,考察痰火草各部位提取物抗肺癌的药理作用。
药理实验1:痰火草不同部位提取物对肺腺癌细胞A549的增殖抑制作用
实验方法:采用MTT法测定。收集对数生长期人肺癌细胞A549,以0.25%胰蛋白酶消化制成单细胞悬液,调整细胞悬液浓度,按每孔5×103个接种于96孔细胞培养板,在CO2培养箱培养过夜。贴壁12h后,弃原培养基,加入含不同浓度的提取物部位溶液,每组设6个复孔,并设对照组,继续培养72h。吸除每孔培养基,PBS洗3次,加入100μl含MTT(1mg/ml)的完全培养基,培养4h后,弃去上清液,每孔加入100μl DMSO,避光振荡5min,置酶标仪上在492nm处测定各孔的吸光度(A)。计算各给药浓度的抑制率,公式:细胞增殖抑制率(%)=(1-A加药/A对照)×100%。
实验结果:MTT实验结果显示(见图2),在5-200μg/ml范围内,痰火草石油醚、氯仿、乙酸乙酯部位对A549细胞的增殖有较强的抑制作用,而正丁醇、水层部位则作用较弱。乙酸乙酯部位对A549细胞增殖的抑制最强,并呈现剂量依赖性,IC50为30.80μg/ml。
药理实验2:痰火草乙酸乙酯提取物对肺腺癌细胞A549细胞形态的影响
实验方法:取浓度为5×104个/ml的A549细胞株接种于6孔板中培养,待细胞完全贴壁后,弃原培养基,加有效部位的含药培养基,培养24h后,在倒置相差显微镜下观察细胞形态的变化。
实验结果:倒置显微镜下观察结果显示(见图3),对照组细胞贴壁生长良好,形态大小均匀,胞质透亮,增殖旺盛;痰火草乙酸乙酯部位可显著改变A549细胞形态,抑制细胞生长,并呈现剂量依赖性。
药理实验3:痰火草乙酸乙酯提取物对肺腺癌细胞A549细胞凋亡的影响
实验方法:待A549细胞完全贴壁后,弃去培养基,加入提取部位的含药培养基,培养24h后,吸除每孔培养基,PBS漂洗3次,加入甲醇配置的Hoechst 33258染液(5μmol/l)50μl,孵育20min,弃染液,甲醇轻轻洗2次,立即置荧光微镜下观察细胞核形态。
实验结果:Hoechst33258荧光染色结果显示(见图4),对照组细胞核形态完整,呈正常微弱的蓝色荧光;痰火草乙酸乙酯提取物作用24h后,细胞核碎裂呈圆状、固缩状或团块状结构,形成凋亡小体,蓝色荧光增强。表明随着痰火草乙酸乙酯提取物浓度的增大,细胞核碎裂程度更加明显呈碎块状,提示痰火草乙酸乙酯提取物诱导A549细胞凋亡有浓度依赖性。
综合上述实验结果,本发明以痰火草药材为原料,经过前处理、粗提、过滤、浓缩、萃取以及获得提取物步骤,制得痰火草提取物。细胞药理实验证实,痰火草乙酸乙酯提取物,对人肺腺癌A549细胞增殖有显著的抑制作用,对细胞形态、细胞凋亡有显著的影响,并具有明显的量效关系。以上所述实施例仅表达本发明的几种实施方式,但并不能由此理解为对本发明专利范围的限制。在不脱离本发明构思的前提下,还可以产生若干变形和改进,这些均属于本发明的保护范围,应以本发明权利要求书保护的范围为准。
Claims (9)
1.一种具有治疗肺癌作用的痰火草提取物的制备方法,包括以下步骤:
(1)前处理:将痰火草进行干燥并粉碎成粗粉;
(2)粗提:体积浓度60%~90%的乙醇溶液回流提取2~3次,每次1~3个小时;
(3)过滤;
(4)浓缩:将滤液进行减压浓缩,浓缩至相对密度为1.05~1.35;
(5)获得提取物:将浓缩液进行溶剂回收后,冷冻干燥或真空干燥。
2.根据权利要求1所述的制备方法,其中,步骤(4)与步骤(5)之间还包括萃取步骤:用浓缩液3倍体积的有机溶剂进行萃取,将萃取液减压浓缩。
3.根据权利要求2所述的制备方法,其中,所述有机溶剂为石油醚、氯仿、乙酸乙酯和正丁醇。
4.根据权利要求3所述的制备方法,其中,萃取步骤为用石油醚、氯仿、乙酸乙酯和正丁醇依次进行萃取,或者为用石油醚、氯仿、乙酸乙酯和正丁醇之中的两种依次进行萃取;或者为用石油醚、氯仿、乙酸乙酯和正丁醇之中的一种进行萃取;优选地,萃取步骤为用石油醚、氯仿、乙酸乙酯和正丁醇依次进行萃取。
5.根据权利要求1所述的制备方法,其中,步骤(1)中痰火草干燥粗粉的重量与步骤(2)中所述乙醇的体积比为1∶5~1∶20。
6.一种具有治疗肺癌作用的痰火草提取物,该提取物由权利要求1至5中任一项所述的制备方法所制得。
7.根据权利要求6所述的具有治疗肺癌作用的痰火草提取物,其特征在于,所述痰火草提取物为石油醚部位提取物、氯仿部位提取物、乙酸乙酯部位提取物、正丁醇部位提取物和剩余部位提取物。
8.根据权利要求6或7所述的具有治疗肺癌作用的痰火草提取物在治疗肺癌的药物方面的应用或者在制备辅助治疗肺癌的功能性食品方面的应用,所述药物,优选药物剂型为片剂、颗粒剂、丸剂、胶囊或者溶液剂。
9.根据权利要求8所述的应用,所述丸剂为滴丸,所述胶囊为硬胶囊或软胶囊,所述溶液剂为糖浆剂或合剂,包含根据权利要求6或7所述的痰火草提取物以及药学可接受的载体。
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