CN105902585A - 白刺属植物或其提取物在制备抑制脂肪酸合酶的药物、保健品、食品或日化用品中的用途 - Google Patents
白刺属植物或其提取物在制备抑制脂肪酸合酶的药物、保健品、食品或日化用品中的用途 Download PDFInfo
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Abstract
本发明公开了白刺属植物或其提取物在制备抑制脂肪酸合酶的药物、保健品、食品或日化用品中的用途。酶活性实验结果表明，本发明白刺果粉及提取物对脂肪酸合酶活性均有显著的抑制作用；其中，白刺果提取物抑制肪酸合酶活性的能力较已知的脂肪酸合酶抑制剂槲皮素更强。
Description
技术领域
本发明涉及白刺属植物或其提取物在制备抑制脂肪酸合酶的药物、保健品、食品或日化用品中的用途，属于医药及生物领域。
背景技术
脂肪酸合酶(FAS)是生物细胞内合成脂肪过程中最重要的酶。田维熙等研究提出“抑制FAS活性是控制动物体脂水平的有效方法”(田维熙,1994.动物的体脂水平和脂肪酸合酶活性的调控.生命的化学,14,(1):184；田维熙等,1996.不同生长期蛋鸡的体脂水平和肝脏脂肪酸合酶活性的关系.生物化学杂志，12(2):234-236；Mei Li et al.,1999.Factors influencing the levels of fattyacid synthase complex activity in fowl.Biochemistry and Molecular BiologyInternational,47(1):63-69)。2000年，《SCIENCE》报道了美国科学家霍普金斯大学Loftus等人的研究结果，证明抑制FAS可造成丙二酸单酰辅酶A的积累，而后者抑制与进食相关的下丘脑神经肽Y的表达，在不影响小鼠活动能力的情况下使小鼠食欲下降、体重降低；T.Loftus等指出，FAS可以作为控制体重的潜在治疗靶位(Loftus.T.M.et al.,2000.Science,288(5475):2379-2381)。另有研究证实，FAS的抑制剂cerulenin能够杀死癌细胞和阻碍异种移植瘤的生长，其他FAS抑制剂如cerulenin的衍生物C75、β-内酯orlistat、EGCG、luteolin、quercetin、kaempferol等也已被确认可以通过诱导细胞凋亡抑制肿瘤细胞的生长。
以上结果表明，FAS是潜在的抑脂减肥和抑制肿瘤的双重靶点。因此，研制和开发FAS抑制剂将具有重大的现实意义及开发潜力。
白刺是蒺藜科(Zygophyllceae)白刺属(Nitraria)的落叶灌木，主要生长在荒漠或半荒漠地区，是耐干旱、耐盐碱、耐严寒、抗沙埋的抗逆性先锋植物，同时也是我国沙漠地区特有的传统药用植物，在西北少数民族地区入药历史悠久。如见《中国沙漠地区药用植物》中记载：白刺“果实多用于民间，具有健脾胃、滋补强壮、调经活血的功能，主治身体瘦弱、气血两亏、脾胃不和、消化不良、月经不调、虚寒腰痛等症”。现代研究表明，白刺属植物中除氨基酸、矿物质等营养成分含量丰富外，从其果实、叶片、幼枝、种子等部位提取得到的主要次生代谢物质之一为黄酮类化合物(1、刘金荣等.西伯利亚白刺果实微量元素及总黄酮含量测定[J].中国现代应用药学杂志，2002,19(5):385-386；2、贾忠建等.唐古特白刺黄酮类化合物的研究[J].植物学报，1989,31(3):241-243；3、段金廒等.唐古特白刺叶黄酮类及酚酸类成分的分离鉴定[J].植物资源与环境，1999,8(1):6-9)，并且认为该类化合物与白刺属植物抗氧化、降血压等功效密切相关。
然而，迄今尚未见关于白刺抑制脂肪酸合酶活性作用的相关报道。
发明内容
本发明的目的在于提供白刺属植物或其提取物在制备抑制脂肪酸合酶的药物、保健品、食品或日化用品中的用途。
本发明提供了白刺属Nitraria植物或其提取物在制备抑制脂肪酸合酶的药物、保健品、食品或日化用品中的用途。
进一步的，所述的药物、保健品、食品或日化用品具有抑脂减肥功效。
进一步的，所述的药物、保健品、食品或日化用品是以白刺属植物全果、果汁、果实任意部位或其提取物为活性成分制备而成。
本发明所述白刺果实任意部位包括果皮、果肉、种籽或其任意组合。
优选的，所述的白刺属植物为唐古特白刺Nitraria tangutorum Bobr.、西伯利亚白刺Nitraria sibirica Pall.或大果白刺Nitraria roborowskii Kom.中的一种或几种。
进一步的，所述白刺属植物或其提取物中总黄酮含量15.1％～89.2％w/w。
进一步的，所述白刺属植物或其提取物中总黄酮含量为89.2％w/w。
进一步的，所述提取物为白刺属植物全果或果实任意部位的乙醇提取物。
进一步的，所述提取物由下述方法制备得到：
a、取白刺属植物鲜果，榨汁，过滤，分别收集滤液、滤渣，干燥滤液，即得白刺果粉；
b、用50～70％v/v乙醇水溶液提取a步骤所得滤渣，料液比1:10～1:30，提取温度为45℃～70℃，提取时间为45min～120min，提取1～3次，收集提取液，浓缩，干燥，即得；或，
a、取白刺属植物干果，粉碎，得全果粉，备用；
b、用50～70％v/v乙醇水溶液提取全果粉，料液比1:10～1:30，提取温度为45℃～70℃，提取时间为45min～120min，提取1～3次，收集提取液；
c、将提取液依次经微滤膜、超滤膜两级过滤，收集超滤膜截留液，干燥，即得。
进一步的，c步骤中过滤温度20～30℃，过滤压力1.0～6.0bar；微滤膜孔径为0.01μm～10μm，微滤膜过滤流速为20～500kg/h；超滤膜孔径为0.002～0.1μm，超滤膜过滤流速为10～500kg/h。
本发明提供了一种抑制脂肪酸合酶的组合物，它是以有效量白刺属植物的原生粉、水或有机溶剂提取物、超临界流体提取物为活性成分，加入药学上可接受的辅料或辅助性成分制备而成的制剂，或加入食品用辅料制备而成的食品。
本发明提供了白刺属植物或其提取物在制备抑制脂肪酸合酶的药物、保健品、食品或日化用品中的用途。酶活性实验结果表明，本发明白刺果粉及提取物对脂肪酸合酶活性均有显著的抑制作用；其中，白刺果提取物抑制脂肪酸合酶活性的能力较已知的脂肪酸合酶抑制剂槲皮素更强。
本发明具有以下有益效果：
1、本发明不仅丰富了天然FAS抑制剂的来源，也开拓了白刺属植物在抑制脂肪酸合酶活性的新用途，开辟了具有地域特色和资源优势植物应用开发的新价值。
2、由于抑制脂肪酸合酶的活性，一方面可以使生物细胞内合成脂肪的过程弱化，从而脂肪含量得到控制甚至减少；另一方面可以使肿瘤细胞合成脂肪酸的能力下降，从而抑制肿瘤细胞的生长。因此，以本发明提供的白刺来源的脂肪酸合酶抑制剂作为活性原料制成的针对抑脂、减肥或抑制肿瘤相关的药品、保健品、食品、功能日化用品等具有靶点明确、活性明显、作用机理清楚等特点。
3、本发明提供的白刺来源的天然FAS抑制剂，其制备工序简便、环保、稳定、工业化生产成熟、开发前景广阔。
显然，根据本发明的上述内容，按照本领域的普通技术知识和惯用手段，在不脱离本发明上述基本技术思想前提下，还可以做出其它多种形式的修改、替换或变更。
以下通过实施例形式的具体实施方式，对本发明的上述内容再作进一步的详细说明。但不应将此理解为本发明上述主题的范围仅限于以下的实例。凡基于本发明上述内容所实现的技术均属于本发明的范围。
具体实施方式
本发明具体实施方式中使用的原料、设备均为已知产品，通过购买市售产品获得。
黄酮含量的测定方法参考DB13/T 385-1998《食品总黄酮测定》中第1-2页所述方法。
实施例1本发明白刺果粉的制备
取唐古特白刺Nitraria tangutorum Bobr.鲜果35g，榨汁，过滤，收集滤液，干燥，得本发明白刺果粉I共22.05g。经测定其中总黄酮含量15.1％。
实施例2本发明白刺果提取物的制备方法
1、取唐古特白刺Nitraria tangutorum Bobr.鲜果35g，榨汁，过滤，收集滤渣，干燥，粉碎，备用；
2、用50％v/v乙醇水溶液提取经粉碎的滤渣，料液比1:10，提取温度为45℃，提取时间为45min，提取1次，收集提取液，浓缩，干燥，得本发明白刺果提取物II共3.88g。经测定其中总黄酮含量68.7％。
实施例3本发明白刺果提取物的制备方法
1、取唐古特白刺Nitraria tangutorum Bobr.干果48g，粉碎，得全果粉；
2、用70％v/v乙醇水溶液提取全果粉，料液比1:30，提取温度为70℃，提取时间为120min，提取3次，收集提取液；
3、将提取液依次经微滤膜、超滤膜两级过滤，过滤温度20～30℃，过滤压力1.0～6.0bar；微滤膜孔径为0.01μm～10μm，微滤膜过滤流速为20～500kg/h；超滤膜孔径为0.002～0.1μm，超滤膜过滤流速为10～500kg/h；收集超滤膜截留液，干燥，得本发明白刺果提取物III共6.76g。经测定其中总黄酮含量89.2％。
实施例4本发明白刺果提取物的制备方法
1、取西伯利亚白刺Nitraria sibirica Pall.鲜果35g，榨汁，过滤，收集滤渣，干燥，粉碎，备用；
2、用50％v/v乙醇水溶液提取经粉碎的滤渣，料液比1:10，提取温度为45℃，提取时间为45min，提取1次，收集提取液，浓缩，干燥，得本发明白刺果提取物IV共4.21g。经测定其中总黄酮含量70.3％。
实施例5本发明白刺果提取物的制备方法
1、取大白刺Nitraria roborowskii Kom.鲜果35g，榨汁，过滤，收集滤渣，干燥，粉碎，备用；
2、用50％v/v乙醇水溶液提取经粉碎的滤渣，料液比1:10，提取温度为45℃，提取时间为45min，提取1次，收集提取液，浓缩，干燥，得本发明白刺果提取物V共3.95g。经测定其中总黄酮含量65.8％。
以下通过酶活性实验证明本发明的有益效果。
实验例1本发明白刺果粉及白刺果提取物对脂肪酸合酶的抑制作用
采用专利CN2012102513440的方法(参见[0044]～[0061]段)，分别检测根据实施例1～5制备的白刺果粉、白刺果提取物以及已知的脂肪酸合酶抑制剂槲皮素对脂肪酸合酶(FAS)的抑制作用，结果见表1。
表1抑制FAS全反应IC50(单位：μg/ml)
以上结果表明，本发明白刺果粉I、白刺果提取物II～V对脂肪酸合酶活性均有显著的抑制作用；其中，白刺果提取物II～V的IC50值明显低于已知的脂肪酸合酶抑制剂槲皮素，表明其抑制脂肪酸合酶活性的能力更强；白刺果提取物III的抑制能力最强。
Claims (10)
1.白刺属Nitraria植物或其提取物在制备抑制脂肪酸合酶的药物、保健品、食品或日化用品中的用途。
2.如权利要求1所述的用途，其特征是：所述的药物、保健品、食品或日化用品具有抑脂减肥功效。
3.如权利要求1或2所述的用途，其特征是：所述的药物、保健品、食品或日化用品是以白刺属植物全果、果实任意部位、果汁或其提取物为活性成分制备而成。
4.如权利要求1～3任意一项所述的用途，其特征是：所述的白刺属植物为唐古特白刺Nitraria tangutorum Bobr.、西伯利亚白刺Nitraria sibirica Pall.或大果白刺Nitraria roborowskii Kom.中的一种或几种。
5.如权利要求1～4任意一项所述的用途，其特征是：所述白刺属植物或其提取物中总黄酮含量为15.1％～89.2％w/w。
6.如权利要求5所述的用途，其特征是：所述白刺属植物或其提取物中总黄酮含量为89.2％w/w。
7.如权利要求1～6任意一项所述的用途，其特征是：所述提取物为白刺属植物全果或果实任意部位的乙醇提取物。
8.如权利要求7所述的用途，其特征是：所述提取物由下述方法制备得到：
a、取白刺属植物鲜果，榨汁，过滤，分别收集滤液、滤渣，干燥滤液，即得白刺果粉；
b、用50～70％v/v乙醇水溶液提取a步骤所得滤渣，料液比1:10～1:30，提取温度为45℃～70℃，提取时间为45min～120min，提取1～3次，收集提取液，浓缩，干燥，即得；或，
a、取白刺属植物干果，粉碎，得全果粉，备用；
b、用50～70％v/v乙醇水溶液提取全果粉，料液比1:10～1:30，提取温度为45℃～70℃，提取时间为45min～120min，提取1～3次，收集提取液；
c、将提取液依次经微滤膜、超滤膜两级过滤，收集超滤膜截留液，干燥，即得。
9.如权利要求8所述的用途，其特征是：c步骤中过滤温度20～30℃，过滤压力1.0～6.0bar；微滤膜孔径为0.01μm～10μm，微滤膜过滤流速为20～500kg/h；超滤膜孔径为0.002～0.1μm，超滤膜过滤流速为10～500kg/h。
10.一种抑制脂肪酸合酶的组合物，其特征是：它是以有效量白刺属植物的原生粉、水或有机溶剂提取物、超临界流体提取物为活性成分，加入药学上可接受的辅料或辅助性成分制备而成的制剂，或加入食品用辅料制备而成的食品。
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| CN108553489A (zh) * | 2018-03-23 | 2018-09-21 | 青海大学 | 一种改善血脂异常的泡腾片及其用途 |
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