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黄连花薹化学成分和药理作用的研究进展



全 文 :现代生物医学进展 www.shengwuyixue.com Progress inModern Biomedicine Vol.14 NO.27 SEP.2014
*基金项目:国家自然科学基金项目(11175222)
作者简介:魏华波(1985-),男,硕士,研究方向:医院临床药学和肿瘤分子药理学相关方面的研究
△通讯作者:王振华(1973-),电话:023-70723441,E-mail: zhenhuawang@tom.com
(收稿日期:2013-07-14 接受日期:2013-08-12)
·药学·
doi: 10.13241/j.cnki.pmb.2014.27.039
黄连花薹化学成分和药理作用的研究进展 *
魏华波 1 董 洋 1 谭 兵 1 王振华 2△
(1重庆市丰都县人民医院 重庆 408200;2烟台大学生命科学学院 山东烟台 264005)
摘要:传统中药材黄连因其含有黄连素、黄连碱、黄藤素、药根碱等生物碱类,黄酮类和酚类活性物质,而具有清热解毒、抗炎抗病
毒、降血糖血脂血压、保护胃肠道、抗肿瘤等作用。近些年体内和体外研究发现,黄连花薹与黄连具有相似的化学活性物质,在体
内外具有广泛的药理作用。本文就近几年黄连花薹的化学成分和药理作用做一综述,为黄连花薹的综合开发和合理应用提供思
路。
关键词:黄连;黄连花薹;化学成分;药理作用;研究进展
中图分类号:R284.2,R285 文献标识码:A 文章编号:1673-6273(2014)27-5342-03
Advances in the Study of Chemical Composition and Pharmacologic Action
of Coptis Chinensis Inflorescence*
WEI Hua-bo1, DONG Yang1, TAN Bing1, WANG Zhen-hua2△
(1 The Fengdu People’s Hospital of Chongqing, Chongqing, 408200, China;
2 School of Life Science, Yantai University, Yantai, Shandong, 264005, China)
ABSTRACT: Coptis chinensis franch of traditional Chinese medicine contains alkaloids (including the berberine, coptisine,
palmatine, and jatrorrhizine, et al.), flavonoids, and phenolic active substances. It can heat-clearing and detoxicating, anti-viral and
anti-inflammatory, lowering blood sugar/fat/pressure, protecting the gastrointestinal tract, and anti-tumor. In recent years, studies have
found that Coptis chinensis inflorescence has similar chemical active substances with Coptis chinensis Franch, and has a wide range of
pharmacological effects in vitro and in vivo. This review is to summarize the current research of chemical composition and pharma-
cological action of coptis chinensis inflorescence, to provide potential candidates for synthetic exploitation and its reasonable application.
Key words: Coptis chinensis franch; Coptis chinensis inflorescence; Chemical composition; pharmacologic action;
Chinese Library Classification: R284.2; R285 Document code: A
Article ID: 1673-6273(2014)27-5342-03
黄连花薹是毛茛科(Ranunculaceae)传统中药黄连(Coptis
chinensis Franch.)的花序,春季开花,摘除能增产黄连根茎,在
黄连生产基地除留种外皆摘除丢弃,造成了大量的资源浪费。
现已将黄连花薹开发成黄连花茶饮品供应于市,取得了一定的
经济效益。近年大量研究发现,黄连花薹含有大量的生物碱、黄
酮和酚类活性物质,具有降血脂血糖血压、抗氧化、促进小肠蠕
动、促进排便和保护心肌缺血再灌损伤等作用,为黄连花薹资
源的综合开发和合理应用提供了新的发展方向。
1 黄连花薹的化学成分
近年研究发现,黄连花薹含有大量的生物碱,如黄连素、黄
连碱、黄藤素、药根碱等;黄酮类和酚类活性物质;以及大量的
氨基酸和矿物质;对黄连花薹的深入研究和综合开发具有重要
意义。众所周知,黄连着为一种非常重要的传统中药,常用于治
疗各种炎症、出血、高血糖和高血压等疾病,这些药理作用与其
含有黄连素、黄连碱、黄藤素、药根碱等生物碱类活性物质有关
[1]。黄连花薹着为黄连的副产品也含类似的生物碱类活性物质
[2-4]。研究证明[2],黄连花薹和叶与黄连根茎一样,含有大量的黄
连素、总生物碱和氨基酸,黄连花、叶和根茎中三者的含量分别
为 1.16%、1.76%和 5.42%,2.02%、2.94%和 10.12%,20.63%、
12.18%和 5.82%。Yuan LJ等[3]也报道,黄连花薹水提取物干浸
膏中含有大量的生物碱类物质,并且黄连素占到了总生物碱的
40%,即 100g干浸膏中含 8.11g总生物碱、3.34g黄连素、1.08g
大黄藤碱和 0.66g药根碱,以及大量的氨基酸和矿物质。进一
步研究研究发现[4],黄连花薹富含多种人体必需氨基酸,并且所
含的 7种必须氨基酸占总氨基酸的 39.42%,而所含氨基酸占花
薹的 17.44%;黄连花薹富含的矿物质有 K、Ca、Fe、Mg、Cu、Zn、
Mn、Ni 等,含量分别是 2893、870.33、572.5、1137、16.33、208.
67、0.013 mg/100g。屠大伟等[5]通过对黄连同花期的花薹进行总
生物碱和盐酸黄连素含量的比较发现,初花期的花薹中的总生
物碱和盐酸黄连素含量最高,分别为 3.95%和 0.52%。Ban XQ
等[6]研究报道,黄连花薹 70%乙醇、正丁醇、乙酸乙酯、环已烷和
氯仿五种溶剂的提取物的提取率分别是 38%、8.78%、7.46%、
2.59%和 10.76%;前三种溶剂提取物中含有大量的酚类化合
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现代生物医学进展 www.shengwuyixue.com Progress inModern Biomedicine Vol.14 NO.27 SEP.2014
物,后三种溶剂提取物中含有黄酮类物质,其中 70%乙醇提取
物酚类物质占到了 87.66,乙酸乙酯提取物黄酮类物质占到了1.48。
2 黄连花薹的药理作用
黄连单味或组方治疗咯血、呕血、炎症、脑和消化道出血、
高血压、高血糖等疾病。近年研究表明,黄连花薹因含有大量的
生物碱类、黄酮类和酚类活性物质而在体内外具有降血脂血糖
血压、抗氧化、促进小肠蠕动、促进排便和保护心肌缺血再灌损
伤等作用。
2.1 降血脂血糖血压作用
有资料表明,血浆中的 TC的增加,特别是低密度脂蛋白
胆固醇(LDL-C)及其氧化衍生物,是冠状动脉粥样硬化的一种
严重病理学改变,并且在动脉粥样硬化过程中扮演着重要的作
用;而通过饮食疗法或药物疗法降低血浆中的胆固醇可减少冠
状动脉疾病的发病率和死亡率[7-12]。研究发现[13],黄连花薹提取
液能显著降低高脂血症大鼠血清中总胆固醇(TC)、甘油三酯
(TG)、LDL-C,升高高密度脂蛋白胆固醇(HDL-C),抑制腹腔
和肝脏脂肪的富集,从而发挥其降血脂的作用,对预防和治疗
脂肪肝和动脉粥样硬化具有一定的作用。Yuan LJ等[3]报道,给
用含 18%酪蛋白、1%胆固醇和 0.5%胆酸饮食诱导的高胆固醇
血症老鼠黄连花薹水提物灌胃,可显著的降低 TC和 LDL-C的
水平,并且成剂量依赖关系;给用四氧嘧啶诱导的高血糖症老
鼠黄连花薹水提物灌胃三周,可显著降低血糖。黄连着为一种
传统中药,单用或组方降血糖作用可能与黄连多糖保护胰腺的
胰岛和β细胞,从而增加胰岛素的分泌有关。有研究发现,黄连
素可通过刺激胰岛素分泌、调节脂质代谢、抑制肠粘膜对葡萄
糖的吸收和增加胰岛素的利用率来降低血糖作用[14,15]。
2.2 抗氧化
活性氧(Reactive Oxygen Species, ROS)是指化学性质活跃
的含氧原子或原子团,如超氧自由基(·O2-)、过氧化氢(H2O2)、羟
自由基(·OH)等。当细菌或异物进入机体,ROS可以杀灭细菌
和清除异物,而过多的 ROS可以氧化不饱和脂肪酸、蛋白质和
DNA等而造成损伤,使机体发生病变。正常情况下机体内的超
氧化物歧化酶、过氧化氢酶等可以清除 ROS,使机体在清除细
菌和异物的同时免遭氧化损伤。
众多研究发现,黄连花薹及提取物和黄连单药或方剂具有
相似的化学活性物质,在体内外能够清除 ROS发挥其抗氧化
作用。谢云峰等[16]和王利津等[17]报道,黄连解毒汤中黄连、黄芩、
黄柏和栀子四味中药均具有直接清除活性氧的作用,其汤体不
但能明显抑制红细胞自氧化或 H2O2的所致红细胞溶血,并能
抑制小鼠肝匀浆自发笥或 Fe2+-Vit C诱发的脂质过氧化反应,
对 H2O2所产生的羟自由基亦有直接的清除作用。黄连提取物
不但对小鼠红细胞溶血和脂质过氧化具有明显的抑制作用,还
具有极强的清除超氧化和羟自由基清除活性[19,20],而黄连的止
泻解毒作用也可能与其抗氧化和自由基清除活性有关[21]。黄连
甲醇提取物含有落叶松脂素和反式阿魏酸,二者对羟基苯乙酯
具有清除作用,且表现出超氧化物歧化酶样作用,前者清除自
由基清除活性比抗体坏血酸更强[22-24]。Ban XQ等[6]研究发现,黄
连花薹 70%乙醇提取物含有大量酚类物质,在体内外具有强烈
的抗氧化活性,进一步研究发现其发挥抗氧化活性与其增加超
氧化物歧化酶(SOD)、过氧化氢酶(CAT)和]还原型谷胱甘肽
(GSH)的表达,使机体清除自由基的能力增加,从而减少机体
蛋白质和脂质等的氧化,进而减少机体的氧化损伤。屠大伟等
[26]用水杨酸法测定黄连花薹的抗氧化能力时发现,黄连花薹水
浸出物具有清除羟自由基(·OH)、超氧自由基(·O2-)和过氧化
氢(H2O2)的能力。
2.3 其它
黄连花薹或提取物除了具有降血脂血糖血压和抗氧化作
用外,还具有其它作用。如黄连花薹复配物在地芬诺酯引起小
鼠便秘模型中表现出促进小肠蠕动和促进排便的功效[25];在酵
母致大鼠发热模型的解热实验中表现出解热的功效[26]。付晓春
等[27]报道,黄连解毒汤能通过抑制心肌核因子 IkB诱导激酶和
IkB激酶 β水平的表达,减少 IkBα蛋白的磷酸化降解,进而抑
制NF-kB的过度活化途径来保护心肌缺血再灌注的损伤作用。
3 小结与展望
在我国黄连作为传统名贵中药药,已有悠久的栽培、炮制
和应用历史,如今我国年产量 170~220万公斤。黄连移载后第
二年开始,每年春季开花,为使黄连丰产,除留种外常将花薹摘
除弃去,在各生产基地大量的黄连花薹抛弃田间地头。近年的
大量的研究发现,黄连花薹具有降血脂血糖血压、抗氧化、促进
小肠蠕动、促进排便和保护心肌缺血再灌损伤等作用,为黄连
的综合开发提供思路;石柱黄连生产基地和科研单位合作,在
黄连花薹综合开发利用这方面已作出了尝试,现已将黄连花薹
开发成黄连花茶饮品供应于市,取得了一定的经济效益。但在
黄连资源的综合开发和合理利用上还不够理想,仍需各大生产
基地和广大学者不断去努力,如尝试将黄连花薹开始发成抗衰
老和预防相关疾病的保健食品或作为抗氧化剂加以使用,将具
有重要的经济价值和社会价值。
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