CN104473992B - 一种桔梗提取物及在制备医药和保健品中的新用途 - Google Patents
一种桔梗提取物及在制备医药和保健品中的新用途 Download PDFInfo
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- A61K36/18—Magnoliophyta (angiosperms)
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- A—HUMAN NECESSITIES
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- A61K2236/33—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones
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- A—HUMAN NECESSITIES
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- A61K2236/331—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones using water, e.g. cold water, infusion, tea, steam distillation, decoction
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- A—HUMAN NECESSITIES
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- A61K2236/33—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones
- A61K2236/333—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones using mixed solvents, e.g. 70% EtOH
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Abstract
本发明属于医药技术领域，主要公开了一种桔梗提取物的制备方法及其在医药和保健品中的新用途。经实验研究表明：该桔梗提取物加工工艺简单，易于操作，活性成分丰富。药效学实验研究证明，该提取物对化学物质诱导肝损伤小鼠具有明显的保护作用。因此，可以使用该有效成分制备护肝的药物、保健品、食品添加剂或复方制剂等。其药物或保健品可以是现有的任何剂型，如片剂，胶囊剂，粉针剂，注射剂，丸剂，软胶囊，颗粒剂和贴剂等。
Description
技术领域
本发明涉及桔梗提取物其组合物在医药和保健品中的新用途。
背景技术
化学性肝损伤是一种常见的肝疾病，主要由氧化应激造成的系列损伤所致，如重视不够，容易演变成肝炎，肝纤维化，肝坏死，甚至肝硬化和肝癌，当前医学界对于化学性肝损伤没有较好的治疗策略。然而，从中药中发现的多种活性成分具有明显的预防和治疗肝损伤的作用。
桔梗为桔梗科桔梗（Platycodon grandiflorum）的干燥根。始载于《神农本草经》，列为下品。为历版《中国药典》収载品种，是我国40种常用大宗药材之一，为卫生部公布的“既是食品又是药品”的物品。药理学研究表明：桔梗对酒精，四氯化碳和高脂饮食诱导的肝损伤动物均具有明显的保护作用（参见：Noh JR, et, al. Hepatoprotective effect ofPlatycodon grandiflorum against chronic ethanol-induced oxidative stress inC57BL/6 mice. Ann Nutr Metab. 2011; Ahn YM, et, al. Platycodon grandiflorummodifies adipokines and the glucose uptake in high-fat diet in mice and L6muscle cells. J Pharm Pharmacol. 2012; Khanal T, et, al. Protective effectsof saponins from the root of Platycodon grandiflorum against fatty liver inchronic ethanol feeding via the activation of AMP-dependent protein kinase.Food Chem Toxicol. 2009）。
桔梗中的桔梗皂苷含量丰富，被认为是其主要的活性成分，亦是桔梗的刺激性成分，其为典型的双糖链皂苷，水溶性强。近年来，对生桔梗的研究较多，对热处理后的桔梗研究较少。桔梗在《神农本草经》中列为下品，具有小毒，其热处理后的桔梗经过梅拉德反应，产生芳香的小分子物质，皂苷结构进一步水解，刺激性有所减少。有研究报道：经化学或生物转化后的桔梗次级皂苷具有更好的生物活性，和较小的毒性，且相对摩尔量增加（参见：许小琴，等. 转化型桔梗皂甙抗IBDV、AIV和NDV的研究, 《扬州大学学报》, 2006; 刘墨祥,等. 桔梗总皂苷与其总次皂苷溶血效应的比较研究, 《扬州大学学报》, 2006）.研究表明：热处理可以减少中药的毒性，且易生成部分次级皂苷，多种活性成分容易提取，生物活性好。鲜人参加工成红参就是热处理的典型例证，与鲜人参比较，红参含有丰富的人参次级皂苷（Rg3, Rh2, Rh1等）,且生物活性强。本发明主要基于中药传统的热处理的理论，对桔梗进行热处理，得到桔梗提取物后，发现具有明显的肝损伤保护作用。。
发明内容
本发明提供了一种桔梗提取物的制备方法及在预防和治疗化学性肝损伤方面的药物或保健品及食品添加剂的应用。
前述桔梗提取物，主要是通过热处理得到桔梗原料后，再经提取制备，这里所述的热处理主要包括清蒸和液体辅料蒸制，再晒干或烘干即可熟桔梗原料；桔梗提取物的制备，包括用水，低级醇，低级酮或乙酸乙酯做溶剂，或者这些溶剂中任选额混合溶剂，进行提取得到的提取物；提取用溶剂中所用低级醇可以使甲醇、乙醇或正丁醇，低级酮为丙酮；提取方法选自浸泡提取、回流提取、超声提取、逆流提取以及超临界萃取。例如：用乙醇：水（按体积比90-10:10-90）的混合溶剂进行提取，优选可以用乙醇：水（按体积比70:30）的混合溶剂进行提取。
前述的桔梗提取物，主要包含桔梗皂苷，党参炔苷，酚酸及黄酮类化合物。
前述的桔梗提取物，主要对化学性肝损伤具有预防和治疗作用，能够在日常生活中使用，以缓解和或改善化学物质引起的各种肝损伤。
当本发明用于上述用途时，其口服或胃肠外给药，均是安全的，在口服情况下，其可以以任何常规的形式给药，如片剂，胶囊剂，粉针剂，注射剂，丸剂，软胶囊，颗粒剂和贴剂等。
本发明制备预防和制备化学性肝损伤的桔梗提取物可以与药用载体或食品载体混合，这里使用的固体或液体的赋形剂在本领域是总所周知的，下面举几个例子，散剂是内服的粉末剂，它的赋形剂有乳糖，淀粉，糊精，碳酸钙，合成或天然硫酸铝，氧化镁，硬脂酸镁，碳酸氢钠，干燥酵母等；溶液剂的赋形剂有水，甘油，1，2-丙二醇，单糖浆，乙醇，乙二醇，聚乙二醇，山梨糖醇等；软膏剂的赋形剂可以使用脂油，含水羊毛脂、凡士林、甘油、蜂蜡、木蜡、液体石蜡等组合成的疏水剂或亲水剂。
本发明可以通过下面的实验例进一步说明。
实施例1. 桔梗提取物的制备方法
制备方法1：新鲜的桔梗，2-3年生，洗净，去皮，用纱布包好放入普通常压蒸锅中，蒸锅中放的蒸馏水作为蒸汽源，预热30min，蒸制6h，然后取出放入烘箱中45℃烘干24h，即为蒸制桔梗。
将上述所得蒸制桔梗，粉碎，过40目筛，用70%乙醇超声提取3次，合并提取物，减压浓缩，得桔梗提取物。
制备方法2：新鲜的桔梗，2-3年生，洗净，去皮，用纱布包好放入立式压力蒸汽灭菌器中，灭菌器中放的蒸馏水作为蒸汽源，预热30min，于105℃高压蒸制1h，然后取出放入烘箱中45℃烘干24h，即为蒸制桔梗。
将上述所得蒸制桔梗，粉碎，过40目筛，用70%乙醇超声提取3次，合并提取物，减压浓缩，得桔梗提取物。
制备方法3：新鲜的桔梗，2-3年生，洗净，去皮，用纱布包好放入立式压力蒸汽灭菌器中，灭菌器中放的陈醋作为蒸汽源，预热30min，于105℃高压蒸制1h，然后取出放入烘箱中45℃烘干24h，即为蒸制桔梗。
将上述所得蒸制桔梗，粉碎，过40目筛，用70%乙醇超声提取3次，合并提取物，减压浓缩，得桔梗提取物。
实验例2. 桔梗提取物中有效成分的分析
应用UV和HPLC法测定了蒸制桔梗中不同有效成分含量，结果表明：经蒸制处理后，党参炔苷，桔梗总皂苷含量明显增加。此外，蒸制后桔梗香味增加，口服口感好，刺激性减弱。通过LC/MS分析，其有效成分含量丰富，见附图1。
表1 蒸制前后有效成分对比(清蒸)
| 有效成分 | 蒸制前 | 蒸制后 | 测定方法 |
| 总皂苷 | 4.15% | 5.21% | UV |
| 党参炔苷 | 0.47 mg/g | 0.61mg/g | HPLC |
实验例3. 桔梗提取物对酒精诱导的急性肝损伤小鼠的保护作用
适应性喂养1周后的雄性ICR小鼠，随机分为6组，即空白对照组、模型组、水飞蓟素阳性对照组（50 mg·kg-1）、桔梗提取物低剂量组（100mg·kg-1）、中剂量组（200mg·kg-1）和高剂量组（400mg·kg-1）。阳性对照组和给药组采用灌胃给药，连续15天，空白对照组和模型组给予等体积的生理盐水，末次给药1 h后，除空白组外，其余各组一次性给予体积分数为50%的酒精，按4.8g·kg-1(12mL/kg·bw)诱导急性酒精性肝损伤，禁食不禁水。6小时后眼眶静脉丛采血，分离血清，12h后，颈椎脱臼处死小鼠，快速取出各组肝和脾，称重，计算肝指数和脾指数(脏器重/体重×100%)。
从表1可以看出，给药15天后，各组动物体重均有所增加，但各给药组与空白对照组相比体重无显著差异( P＞0.05)，表明蒸制桔梗对小鼠体重没有影响。研究表明：一次性大剂量酒精冲击可以造成小鼠脏器指数的明显升高，主要包括肝指数和脾指数。本实验结果表明：与空白组相比，模型组小鼠肝指数和脾指数显著增加( P＜0.05)，而桔梗各给药组和阳性对照组均能不能程度的降低肝指数和脾指数 ( P＜0.05)。
表1 桔梗提取物对小鼠体质量及免疫器官指数的影响（ ，n =8）
Table 1 Effect of steamed Radix Platycodi on body weight and index ofimmune organs in mice
“*”模型组与空白对照组相比较，“#”给药组与模型组相比较，差异显著（P<0.05）。
从表2可以看出，与空白对照组相比，模型组的ALT、AST和TG的水平均明显增高，说明急性酒精诱导肝损伤模型创建成功（P<0.05）；与模型组相比，给予不同剂量桔梗提取物的各组小鼠血清中ALT、AST和TG含量均明显降低，尤其是中、高剂量组具有显著差异（P<0.05），并且在高剂量组中ALT和AST水平接近阳性对照组的水平，与文献[16]所报道的一致。说明桔梗提取物能够不同程度的抑制急性酒精肝损伤小鼠ALT、AST和TG水平的升高。
表2 桔梗提取物对小鼠血清ALT、AST和TG含量的影响（，n =8）
Table 2 Effect of steamed Radix Platycodi on plasma ALT, AST and TGlevel in mice
“*”模型组与空白对照组相比较，“#”给药组与模型组相比较，差异显著（P<0.05）。
从表3可以看出，与空白对照组相比，模型组的MDA水平均明显升高，而GSH含量显著下降，说明急性酒精诱导肝损伤模型成功建立（P<0.05）；与模型组相比，桔梗提取物各剂量组小鼠的MDA含量随着给药剂量的增加而逐渐降低，并有显著性差异（P<0.05）；而GSH的含量随着给予桔梗提取物剂量的增加均有所提升并呈一定的剂量关系，并且桔梗提取物中、高剂量组与模型组相比有显著性差异（P<0.05）。研究表明桔梗提取物能够有效改善小鼠肝脏的氧化应激损伤。
表3 桔梗提取物对小鼠肝脏MDA和GSH的影响（，n =8）
Table 3 Effect of steamed Radix Platycodi on liver MDA and GSH levelin mice
肝脏组织病理学观察如图所示，正常小鼠肝脏组织细胞排列整齐，细胞核结构和细胞边界清晰，细胞索排列有序，无脂肪变性坏死，无炎症细胞浸润等现象（图2a）；模型组可见肝细胞间界限模糊，中央静脉扩大，细胞内出现炎症细胞浸润和大量变性空泡，部分肝细胞核萎缩或消失（图2b）等现象；与模型组相比，阳性对照组（图2c）肝损伤有显著的减轻，肝细胞结构及肝索排列基本接近正常，无炎性细胞浸润和脂质空泡；在给予高剂量蒸制桔梗的小鼠肝细胞中，可以明显看到肿胀和裂解程度减轻，炎症细胞浸润以及变性空泡减少，但仍可见部分凋亡细胞和变性空泡（图2d）。
制备药剂的实施例一
桔梗提取物20.00g，药用淀粉适量，两者充分混匀，装胶囊，制成100粒胶囊，每粒重0.25g，含桔梗提取物200mg。
制备药剂的实施例二
桔梗提取物20.00g，以1,2-丙二醇1000ml溶解，过滤后分装于1000只安瓶中，每瓶1.0ml，含桔梗提取物20mg。
附图说明
附图1 桔梗提取物的HPLC色谱图
附图2. 肝组织HE病理切片图观察，a，正常对照组；b，模型组；c，阳性药组；d，高剂量桔梗提取物组。
Claims (4)
1.一种应用于治疗和预防肝损伤药物、保健品及食品添加剂的桔梗提取物的提取方法，其特征在于，新鲜采挖2-3年生桔梗，洗净泥土，进行液体辅料蒸制，液体辅料是陈醋或蒸馏水，蒸制时间一般为30min～24h，蒸制温度为90～120℃，之后取出晾晒至干，粉碎，即得桔梗原料，然后70％乙醇超声提取。
2.一种应用于治疗和预防肝损伤药物、保健品及食品添加剂的桔梗提取物的提取方法，其特征在于，新鲜的桔梗，2-3年生，洗净，去皮，用纱布包好放入普通常压蒸锅中，蒸锅中放的蒸馏水作为蒸汽源，预热30min，蒸制6h，然后取出放入烘箱中45℃烘干24h，即为蒸制桔梗；将上述所得蒸制桔梗，粉碎，过40目筛，用70％乙醇超声提取3次，合并提取物，减压浓缩，得桔梗提取物。
3.一种应用于治疗和预防肝损伤药物、保健品及食品添加剂的桔梗提取物的提取方法，其特征在于，新鲜的桔梗，2-3年生，洗净，去皮，用纱布包好放入立式压力蒸汽灭菌器中，灭菌器中放的蒸馏水作为蒸汽源，预热30min，于105℃高压蒸制1h，然后取出放入烘箱中45℃烘干24h，即为蒸制桔梗；将上述所得蒸制桔梗，粉碎，过40目筛，用70％乙醇超声提取3次，合并提取物，减压浓缩，得桔梗提取物。
4.一种应用于治疗和预防肝损伤药物、保健品及食品添加剂的桔梗提取物的提取方法，其特征在于，新鲜的桔梗，2-3年生，洗净，去皮，用纱布包好放入立式压力蒸汽灭菌器中，灭菌器中放的陈醋作为蒸汽源，预热30min，于105℃高压蒸制1h，然后取出放入烘箱中45℃烘干24h，即为蒸制桔梗；将上述所得蒸制桔梗，粉碎，过40目筛，用70％乙醇超声提取3次，合并提取物，减压浓缩，得桔梗提取物。
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