CN108096381A - 一种具有降脂功能的中药复方制剂 - Google Patents
一种具有降脂功能的中药复方制剂 Download PDFInfo
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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Abstract
本发明提供一种具有降脂功能的中药复方制剂,含有绿茶提取物、大花紫薇提取物、棠梨果提取物和苦瓜子提取物。其中,绿茶提取物、大花紫薇提取物、棠梨果提取物和苦瓜子提取物的质量比为5‑85:5‑85:5‑45:5‑45。采用荧光实时定量PCR技术(RT‑qPCR)检测所述中药复方制剂对脂代谢相关基因的影响,实验结果显示,该复方制剂可以上调LDLR基因,具有降血脂的功能。
Description
技术领域
本发明属于中药制剂领域,具体涉及一种具有降脂功能的中药复方制剂。
背景技术
高血脂是指血中胆固醇(TC、LDL-c)和/或甘油三酯(TG)过高或高密度脂蛋白胆固醇(HDL-c)过低。全世界每年3000万人死于高血脂引起的相关疾病,最为严重的为心血管疾病。随着生活水平的提高,我国冠心病的发病率、死亡率也明显上升,高血压患者10年内增加了25%,目前已达2亿人左右。据卫生部统计,我国心脑血管疾病患者首次发病年龄1/3在60岁以下,发病率高达13.6%,65岁以上的老人心脑血管疾病发病率达95%,都不同程度的存在心慌、胸闷、头晕、血压高、血脂高、疲倦、偏瘫、心绞痛等症状,发病率高。每天以2万人的速度递增,占总死亡人数的40.72%。据世界卫生组织(WHO)统计:2012年全球死于心脑血管疾病人数达1750万人。心脑血管疾病已成为人类健康的“第一杀手”。因此,降血脂是减少心血管疾病发病率的关键。
目前临床上应用最广泛的一类降脂药,即3-羟基3-甲基戊二酰辅酶A还原酶(HMG-CoA)抑制剂,即他汀类药物。临床常用的他汀类药物有洛伐他汀(Lovastatin)、辛伐他汀(Simvastatin)、普伐他汀(Pravastatin)、氟伐他汀(Fluvastatin)、阿托伐他汀(Atorastatin)。该类药物能抑制肝脏细胞内的胆固醇合成早期阶段的限速酶,造成肝脏细胞内游离胆固醇减少,并通过反馈性上调肝细胞表面低密度脂蛋白受体(LDLR)的表达,加速循环血液中低密度脂蛋白的清除。苯氧芳酸类(贝特类)是一类人工合成的过氧化酶体增殖激活受体α(PPAR-α)的配体,是目前降甘油三酯的最有效的首选药物,能有效地延缓动脉粥样硬化的发展进程。烟酸类药物主要通过抑制脂肪水解,降低血浆低密度脂蛋白水平。胆酸结合树脂(又称胆酸螯合剂),通过阻止胆酸或胆固醇从肠道吸收,促使其随粪便排出,促进胆固醇降解。
目前用于临床治疗高血脂的药物很多,但仍存在很多问题,包括疗效的局限性、副作用强、价格高。如他汀类药物调脂疗效的特点是每种他汀的起始剂量均有较好的调脂疗效,而当剂量加倍时,低密度脂蛋白胆固醇进一步降低幅度仅为约6%(他汀疗效6%效应),而药费成比例增加,不良反应发生概率大幅增加,他汀的不良反应包括肌痛、肌炎和横纹肌溶解,且长期服用他汀有增加新发糖尿病的风险,发生率约为10%~12%。相比西药,中药的优点在于副作用小。
降脂作用中药近年来研究较多,具有降血脂作用的常见的中药有山楂、何首乌、泽泻、决明子、大黄、灵芝、虎杖、参三七、蒲黄、红花、丹参、女贞子、月苋草、广地龙、虫草、荷叶、玉竹、桑寄生、麦芽、葛根、郁金、茵陈、银杏叶等等。也有很多复方制剂如山丹芍药汤(山楂、丹参和赤芍)、百草降脂灵(山楂和丹参)、降脂宁、血脂康、地奥心血康等。中药降血脂的作用相对于西药比较复杂,毒副反应较少。相比单一中药,中药复方更符合“多组分、多靶点、多效应”的优势。
然而目前还没有由绿茶提取物、大花紫薇提取物、棠梨果提取物和苦瓜子提取物组成的中药复方制剂用于降脂。
发明内容
为了解决西药类降脂作用的药物毒副作用大,治疗高血脂症的同时带来了其他的毒副作用,且毒副作用难以避免,以及单一中药效果不理想的缺陷,本发明提供了一种具有降脂功能的中药复方制剂。
本发明所提供的具有降脂功能的中药复方制剂,含有绿茶提取物、大花紫薇提取物、棠梨果提取物和苦瓜子提取物。
其中,绿茶提取物、大花紫薇提取物、棠梨果提取物和苦瓜子提取物的质量份数比可为5-85:5-85:5-45:5-45,具体可为5-25:40-85:5-25:5-25。
具体地,所述中药复方制剂,由绿茶提取物、大花紫薇提取物、棠梨果提取物、苦瓜子提取物按照下述质量份数比组成:85:5:5:5;5:85:5:5;25:25:45:5;25:25:5:45;45:45:5:5或25:25:25:25。
所述绿茶提取物通过90%乙醇对绿茶茶叶进行提取获得。
所述绿茶具体可为峨眉雪芽。
具体地,所述绿茶提取物可按照包括下述步骤的方法制备得到:
称取峨眉雪芽茶叶10g,研碎,加150mL 90%乙醇,加热到85℃,提取3h,过滤,保留滤液,浓缩,干燥,得到提取物浸膏,即可。
所述大花紫薇提取物通过90%乙醇对大花紫薇花进行提取获得。
具体地,所述大花紫薇提取物可按照包括下述步骤的方法制备得到:
称取大花紫薇(花)10g,研碎,加150mL 90%乙醇,加热到85℃,提取3h,过滤,保留滤液,浓缩,干燥,得到提取物浸膏。
所述棠梨果提取物通过90%乙醇对棠梨果进行提取获得。
具体地,所述棠梨果提取物可按照包括下述步骤的方法制备得到:
称取棠梨(果)10g,研碎加150mL 90%乙醇,加热到85℃,提取3h,过滤,保留滤液,浓缩,干燥,得到提取物浸膏。
所述苦瓜子提取物通过90%乙醇对苦瓜子进行提取获得。
具体地,所述苦瓜子提取物可按照包括下述步骤的方法制备得到:
称取苦瓜(子)10g,研碎加150mL 90%乙醇,加热到85℃,提取3h,过滤,保留滤液,浓缩,干燥,得到提取物浸膏。
上述中药复方制剂在制备下述产品中的应用也属于本发明的保护范围:
1)预防或治疗高血脂症的产品;
2)降低低密度脂蛋白的产品;
3)降低甘油三酯的产品;
4)降低血清总胆固醇的产品。
本发明还提供一种预防或治疗高血脂症的产品、降低低密度脂蛋白的产品、降低甘油三酯的产品或降低血清总胆固醇的产品,其包括上述中药复方制剂。
所述产品可为药品或保健品。
采用荧光实时定量PCR技术(RT-qPCR)检测由绿茶提取物、大花紫薇提取物、棠梨果提取物和苦瓜子提取物按照图1所示比例(复方1:85:5:5:5;复方2:5:85:5:5;复方3:25:25:45:5;复方4:25:25:5:45;复方5:45:45:5:5;复方6:25:25:25:25)组成的中药复方制剂对脂代谢相关基因的影响,实验结果显示,该复方制剂可以上调LDLR基因,具有降血脂的功能。
附图说明
图1表明本发明实施例中的中药复方制剂的各组分的配比。
图2为本发明实施例中对照DMSO、绿茶提取物、大花紫薇提取物、棠梨果提取物、苦瓜子提取物和复方制剂处理细胞24小时后上调LDLR基因的效果图。
具体实施方式
下面通过具体实施例对本发明进行说明,但本发明并不局限于此。
下述实施例中所使用的实验方法如无特殊说明,均为常规方法;下述实施例中所用的试剂、生物材料等,如无特殊说明,均可从商业途径得到。
实施例1、中药复方制剂的制备
将绿茶提取物、大花紫薇提取物、棠梨果提取物、苦瓜子提取物按照图1所示的比例制成6种中药复方制剂。
实施例2、药效实验
利用荧光实时定量PCR技术(RT-qPCR)检测由绿茶提取物、大花紫薇提取物、棠梨果提取物和苦瓜子提取物按照一定配比(如图1所示,复方1:85:5:5:5;复方2:5:85:5:5;复方3:25:25:45:5;复方4:25:25:5:45;复方5:45:45:5:5;复方6:25:25:25:25)组成的中药复方对脂代谢相关基因的影响,确定了该中药复方具有降脂作用。其中,重点关注的基因是LDLR。基因LDLR,低密度脂蛋白受体,定位于肝细胞膜上,通过内吞作用介导血液中LDL的清除,血液中75%以上的LDL通过LDLR清除,上调LDLR对降血脂有利。
本发明发现绿茶提取物、大花紫薇提取物、棠梨果提取物、苦瓜子提取物按上述6种比例组成的复合物可以上调LDLR。
本发明利用RT-qPCR方法验证上述基因的表达,其过程为:
1、对照DMSO、绿茶提取物(75μg/ml)、大花紫薇提取物(75μg/ml)、棠梨果提取物(75μg/ml)、苦瓜子提取物(75μg/ml)4种提取物按照图1所示比例组成的复方处理人源肝细胞系24小时。
2、利用试剂盒提取RNA并反转为cDNA。
3、RT-qPCR反应,程序:95℃,3min,(95℃,3s,60℃,30s)40个循环。
引物序列为:
LDLR:上游引物ACCAACGAATGCTTGGACAAC,
下游引物ACAGGCACTCGTAGCCGAT;
qPCR结果如图2所示,图2显示该复方可以上调LDLR基因,具有降血脂的功能。
Claims (7)
1.一种中药复方制剂,含有绿茶提取物、大花紫薇提取物、棠梨果提取物和苦瓜子提取物。
2.根据权利要求1所述的中药复方制剂,其特征在于:所述中药复方制剂中,绿茶提取物、大花紫薇提取物、棠梨果提取物和苦瓜子提取物的质量份数比为:5-85:5-85:5-45:5-45。
3.根据权利要求1或2所述的中药复方制剂,其特征在于:所述中药复方制剂,由绿茶提取物、大花紫薇提取物、棠梨果提取物、苦瓜子提取物按照下述质量份数比组成:85:5:5:5;5:85:5:5;25:25:45:5;25:25:5:45;45:45:5:5或25:25:25:25。
4.权利要求1-3中任一项所述的中药复方制剂在制备下述产品中的应用:
1)预防或治疗高血脂症的产品;
2)降低低密度脂蛋白的产品;
3)降低甘油三酯的产品;
4)降低血清总胆固醇的产品。
5.一种预防或治疗高血脂症的产品、降低低密度脂蛋白的产品、降低甘油三酯的产品或降低血清总胆固醇的产品,包括权利要求1-3中任一项所述的中药复方制剂。
6.根据权利要求5所述的产品,其特征在于:所述产品为药品或保健品。
7.权利要求1-3中任一项所述的中药复方制剂在上调LDLR基因的转录中的应用。
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