CN102247418A - 竹节参总皂苷、竹节参多糖的保肝作用 - Google Patents
竹节参总皂苷、竹节参多糖的保肝作用 Download PDFInfo
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Abstract
竹节参总皂苷、竹节参多糖及竹节参总皂苷和竹节参多糖组合物的保肝用途,可与药学上可接受载体混合。
Description
技术领域
本发明的涉及竹节参总皂苷、竹节参多糖的保肝用途。
背景技术
肝损伤主要包括暴力性肝损伤、病理性肝损伤、化学性肝损伤等。其中暴力性肝损伤多表现明显快速,且严重。而病理性肝损伤和化学性肝损伤最为常见。在化学性肝损伤中,酒精和药物造成的肝损伤最为普遍,已经成为严重威胁人民生命安全和生活质量的重要因素。现在化学药物对肝损伤的治疗多采用干扰素疗法,但存在用药剂量大,费用高,毒副作用大,停药后易复发等缺点。而中药对肝损伤的治疗多采取复方汤药,或脱胎于复方的中成药,其药味众多,导致质量难以控制。因此,急切需要开发出来源于单一植物,成分简单,疗效明确的有效部位或有效成分,用于急慢性肝损伤的治疗。
竹节参为五加科人参属多年生草本植物Panax japonicus C1 A1 Mey1的干燥根。原是一种名贵的民间中草药,现已收载于《中华人民共和国药典》,药用功能类似人参和三七。竹节参生于山坡沟边、阴湿地区或岩石沟涧旁。主要分布于贵州、湖南、云南、安徽、江西、湖北等地。每年秋季采挖,除去茎叶,分出肉质根,将根茎除去外皮,晒干或阴干即可入药。始载于《本草纲目拾遗》。竹节参甘、微苦,温。具有活血化瘀、消肿止痛、滋补强壮等多种功效。既有类似人参的滋补强壮作用,又有类似三七的散瘀止痛、止血、祛痰作用,主要用于病后虚弱,劳嗽咳血,咳嗽痰多,跌打损伤。竹节参含有多种皂苷、挥发油、糖类和多种氨基酸。
本发明要解决的技术问题是研究竹节参总皂苷、竹节参多糖的保肝用途。为解决上述问题,提供技术方案如下。
竹节参总皂苷、竹节参多糖在保肝上的应用。
所述保肝方面的运用包括对肝损伤的预防和治疗。
所述组合物包括竹节参总皂苷、竹节参多糖与药学上可接受的载体或者常规食用辅料。
本发明对四氯化碳造成的肝损伤动物模型具有的降低谷丙转氨酶和谷草转氨酶的显著性作用。本发明包括用竹节参总皂苷、竹节参多糖与药学上可接受载体混合。
药学上可接受的载体包括口服制剂辅料或胃肠外途径给药的辅料。给药途径可以是口服、注射、局部给药等。根据本发明的技术方案,该组合物可以是口服制剂或注射用制剂,其中口服制剂包括胶囊剂、软胶囊剂、颗粒剂、口服液、片剂、滴丸等。所用辅料包括:淀粉、蔗糖、乳糖、糖粉、葡萄糖、甘露醇、木糖醇、聚乙二醇、异丙醇、吐温-80、甘油、丙二醇、微晶纤维素钠、糊精、环糊精、氯化钠、维生素C、半胱氨酸、柠檬酸、硫代硫酸钠、亚硫酸钠、硬脂酸盐和明胶等常规辅料,制剂的后期制备工艺及设备均属制药领域的常规技术,本发明对此不作限定,故在此不予详述。
本发明组合物口服给药的剂量为2-3次/天,0.25~0.50g/次。
本发明竹节参总皂苷、竹节参多糖提取物是从天然的中药竹节参中提取得到的,竹节参是常用的中草药,有长期的中医用药经验,该药使用安全性高,无明显毒性作用记载。
竹节参总皂苷、竹节参多糖具有确切的降低模型动物谷丙转氨酶和谷草转氨酶的作用。因此,竹节参总皂苷、竹节参多糖有开发成保肝药物的前景。
实施例一竹节参总皂苷的提取、纯化和制备
取竹节参粗粉,加入10倍量的60%的乙醇,浸泡2小时,水浴回流提取2小时,滤过,得滤液。药渣再用10倍量的60%的乙醇回流提取2次,每次2小时,滤过。合并3次滤液,减压回收乙醇至无醇味,配制成药材∶药液(g/ml)为1∶1的溶液。上已经处理好的HPD-100大孔树脂柱,一次用水、60%的乙醇洗脱。合并60%的乙醇洗脱液,回收溶剂至近干,经65℃减压干燥,得到竹节参总皂苷。
实施例二竹节参多糖的提取、纯化和制备
取竹节参粗粉,加入10倍量的水,浸泡2小时,直火煎煮提取1.5小时,滤过,得滤液。药渣再用10倍量的水直火煎煮提取2次,每次1.5小时,滤过。合并3次滤液,减压浓缩至体积适量。加乙醇至浓度为70%进行醇沉,室温下放置12小时以上,滤过,收集沉淀物,反复醇沉2次,合并沉淀物,经65℃减压干燥,得到竹节参多糖。
实施例三竹节参总皂苷和竹节参多糖的保肝实验研究
1.实验材料
1.1药品试剂
联苯双酯片(江苏鹏鹞药业有限公司,批号0811161);辛伐他汀片(上海信谊万象药业股份有限公司,批号:080201);血脂康胶襄(北京北大维信生物科技有限公司,批号:20080708);四氯化碳(北京市新光化学试剂厂生产);花生油(食用油,山东玉皇粮油食品有限公司生产);谷丙转氨酶(ALT)临床诊断试剂盒(上海科欣生物技术研究所,批号20090401);谷草转氨酶(AST)临床诊断试剂盒(上海科欣生物技术研究所,批号20090301)。竹节参多糖(D1)、竹节参总皂苷(Z1)为本实验室自制。
1.2实验仪器
721分光光度计(上海菁华仪器厂),LXJ-II离心机(上海医用分析仪器厂),Satrious电子天平(德国);恒温水浴锅(上海亚荣生化仪器厂);移液枪;,低温高速离心机(天美Z323K)。
1.3实验动物
昆明种雄性小白鼠,体重18~22g,由中国药科大学动物中心提供。
2.实验样品的制备
实施例一、二中制备的竹节参总皂苷和竹节参多糖。
3.试验样品液的配制
3.1.CMC-Na溶液的配制:精密称取5gCMC-Na,1000mL蒸馏水,配制成浓度为0.5%的CMC-Na溶液。
3.2.阳性对照药取联苯双酯液制备:取联苯双酯片16片(25mg/片),置于研钵中碾成细粉,溶解于40ml水中,得10mg/ml的联苯双酯混悬液,为阳性对照药液。
3.3.阳性对照药血脂康药液的配制:精密称取5g内容物,以0.5%CMC-Na混悬,定容至100ml,配制成浓度为0.05g/ml的药液样品。
3.4.阳性对照药辛伐他汀药液的配制:精密称取14g辛伐他汀片(含辛伐他汀70mg),100ml0.5%CMC-Na混悬,配成浓度为0.0007g/ml的药液样品。
3.5.高剂量竹节参多糖药液的配制:精密称取1.5g竹节参多糖。100ml 0.5%CMC-Na混悬,配制成浓度为0.015g/ml的药液样品。
3.6.低剂量竹节参多糖药液的配制:精密称取0.75g竹节参多糖,100ml0.5%CMC-Na混悬,配制成浓度为0.0075g/ml的药液样品。
3.7.高剂量竹节参总皂苷药液的配制:精密称取1.5g竹节参总皂苷。100ml 0.5%CMC-Na混悬,配制成浓度为0.015g/ml的药液样品。
3.8.低剂量竹节参总皂苷药液的配制:精密称取0.75g竹节参总皂苷,100ml0.5%CMC-Na混悬,配制成浓度为0.00715g/ml的药液样品。
3.9.高剂量竹节参总皂苷和多糖药液的配制:精密分别称取0.75g竹节参总皂苷和0.75g竹节参多糖。100ml 0.5%CMC-Na混悬,配制成浓度为0.015g/ml的药液样品。
3.10.低剂量竹节参总皂苷药液的配制:精密分别称取0.375g竹节参总皂苷和0.375g竹节参多糖。100ml0.5%CMC-Na混悬,配制成浓度为0.0075g/ml的药液样品。
4.实验方法
昆明种小鼠132只,18-22g,雌雄各半,随机分成11组,每组12只。分为正常空白对照组、高脂模型组、取联苯双酯阳性对照组、辛伐他汀阳性对照组、血脂康阳性对照组、竹节参总皂苷高剂量组、竹节参总皂苷低剂量组、竹节参多糖高剂量组、竹节参多糖低剂量组、竹节参多糖和竹节参总皂苷低剂量组、竹节参多糖和竹节参总皂苷高剂量组。灌胃给药。正常对照组和高脂模型组每日按0.2ml/10g灌胃0.5%CMCNa,给药组每日灌胃给予0.2ml/10g体积的相应药物,给药剂量分别为:取联苯双酯对照组0.2g/kg、血脂康对照组为1g/kg、辛伐他汀对照组为0.014g/kg、竹节参多糖高剂量组为0.3g/kg、竹节参多糖低剂量组为0.15g/kg、竹节参总皂苷高剂量组为0.3g/kg、竹节参总皂苷低剂量组为0.15g/kg、竹节参多糖和竹节参总皂苷高剂量组为0.15g多糖/kg和0.15g皂苷/kg、竹节参多糖和竹节参总皂苷低剂量组为0.075g多糖/kg和0.075g皂苷/kg。共给药6天。最后1次给药2小时后,除空白组外,其余8组均腹腔注射0.1%的四氯化碳花生油溶液0.1mL/10g。禁食16个小时后,于小鼠眼底静脉丛采血约0.5ml,分离血清(4000rp/min,10min,4℃),利用试剂盒测定ALT、AST活力。
5.结果与讨论
注:▲表示模型与空白相比有显著性差异P<0.05,▲▲表示模型与空白相比有极显著性差异P<0.01。*表示各给药组与模型组相比有显著性差异P<0.05,**表示各给药组与模型组相比有极显著性差异P<0.01。下同。
表2.竹节参多糖(D1)、总皂苷(Z1)对小鼠血清谷草转氨酶(AST)的影响(n=10,)
由表1和表2可知,竹节参多糖(D1)、总皂苷(Z1)及二者组合物(Z1D1)给药组与模型组相比,对CCl4致急性肝损伤模型小鼠的ALT、AST升高有极其显著性的降低作用,分别是P<0.01和P<0.05。实验显示竹节参多糖(D1)、总皂苷(Z1)及二者组合物(Z1D1)具有良好的保肝降酶作用。
Claims (4)
1.竹节参总皂苷、竹节参多糖及竹节参总皂苷和竹节参多糖组合物的保肝用途。
2.权利要求1中所述的保肝用途主要是通过对降低降低谷丙转氨酶和谷草转氨酶达到的。
3.权利要求1中所述的保肝用途可以被用在对肝损伤的预防和治疗。
4.权利要求1中所述的保肝用途,其最终实施形式包括竹节参总皂苷、竹节参多糖及竹节参总皂苷和竹节参多糖组合物与药学上可接受的载体或者常规食用辅料。
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CN105998118A (zh) * | 2016-07-05 | 2016-10-12 | 三峡大学 | 竹节参总皂苷在制备预防及治疗肝脏衰老的药物上的应用 |
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19961231 李翔,等 竹节参对四氯化碳诱发大鼠肝损伤模型保护作用的初步观察 8 第13卷, 第2期 * |
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CN104490965B (zh) * | 2014-12-03 | 2017-08-18 | 中南民族大学 | 竹节参多糖、竹节参总皂苷及竹节参皂苷v的应用 |
CN105998118A (zh) * | 2016-07-05 | 2016-10-12 | 三峡大学 | 竹节参总皂苷在制备预防及治疗肝脏衰老的药物上的应用 |
CN105998118B (zh) * | 2016-07-05 | 2019-12-03 | 三峡大学 | 竹节参总皂苷在制备预防及治疗肝脏衰老的药物上的应用 |
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