黄芪中有效成分药理活性的研究进展_张蔷

黄芪中有效成分药理活性的研究进展

1,21*1

张蔷,高文远,满淑丽

(1. 天津大学药物科学与技术学院,天津300072;2. 天津医科大学总医院老年病研究所,天津300072)

[“补药之长”摘要]黄芪药用历史悠久,古有之称,为历代中医最常用的中药之一。近年来,国内外学者对黄芪的化学药理活性进行了较为广泛的研究。成分分析表明,黄芪以多糖、三萜、黄酮等成分为主;药理实验及临床报道表明,黄芪组成、

在免疫调节、抗肿瘤、抗病毒、糖尿病、延缓衰老等方面具有重要作用。因此,对黄芪的各个有效成分的活性总结具有临床指总结了黄芪不同活性成分的药理活性及作用机制,为该药临床研究提供理论依据,进而为其示性意义。该文通过文献综述,开发利用提供依据。

[关键词]黄芪;多糖;三萜;黄酮

黄芪作为传统中药材,具有扶正补气之功效。现代药学研究表明,黄芪含有多种活性成分,包括黄芪多糖、黄芪皂苷、黄芪黄酮类成分等。近几年,国内外围绕这些成分报道本文以黄芪的活性成分、药理作用为研了大量的实验数据,

究对象,对近年来试验结果进行汇总,以期为临床应用及产品开发提供依据。1

黄芪多糖

其结构与活性研究黄芪多糖作为一类生物大分子成分,

较为广泛。目前认为黄芪多糖的单糖种类主要包括L -鼠李L -D -L -D -L -D -糖、阿拉伯糖、木糖、木糖、核糖、核糖、半乳糖、D -葡萄糖和D -甘露糖等

[1]

的产生,因此对肠炎患者有一定的治疗作用

[12]

另一方面,黄芪多糖也可应用于抗肿瘤方面,如黄芪多糖与云芝糖肽组方后可明显降低阿霉素在抗肿瘤过程中引发的免疫耐受现象

[13]

;此外,黄芪多糖与长春瑞滨、顺铂等联合静脉注

[14]

射可改善晚期非小细胞肺癌患者的生存质量和生存期。

黄芪多糖的免疫调节作用,促使其另一主要药理活性为降血糖作用,有报道称,黄芪多糖可通过增加肌细胞内半乳1的表达凝素-病

[17]

[15]

[16]

,增加胰腺β-细胞总质量,治疗I 型糖尿

。此外,富含糖类或多糖丰富的黄芪可缓解II 型糖尿

[18]

病大鼠的胰岛素耐受及脂肪肝等症状。黄芪多糖的降糖

[2]

[3][4]

、降血糖、抗病毒、治

机制多数还是与其对骨骼肌的影响有关,它降低蛋白酪氨酸

[19]

磷酸酶1B 的表达,调节骨骼肌内PKB /GLUT4信号通

多糖发挥着极其重要的生物功能,目前报道,其具有免疫调节、抗肿瘤、抗动脉粥样硬化疗代谢性紊乱

[5]

[6]

、迟发性神经退行性疾病及抗衰老等,同

[7]

[20]

,进而增加机体对胰岛素的敏感性。这种降血糖作用

I κB 的的同时,黄芪多糖还可以通过影响肾皮质内NF-κB ,

[21]

mRNA 表达,改善早期糖尿病肾病变症状。另外,它可以

提高动物的抗病能力时已广泛应用于兽医临床,。

其中黄芪多糖的免疫调节作用报道最多,被认为与黄芪的免疫调节作用直接相关,是其最重要的作用之一。起初认对T 细胞无明显作为它只可激活B 细胞和巨噬细胞的增生,用

[8]

减少肝内质网应激并维持糖稳态发挥降血糖作用22. 1

黄芪皂苷黄芪总皂苷

[22]

。近年来,我国学者利用微波提取、膜过滤、阴离子交换目前,从膜荚黄芪和蒙古黄芪及其同属近缘植物中分离出40多种三萜皂苷类化合物,主要有黄芪皂苷、异黄芪皂苷、乙酰基黄芪皂苷、大豆皂苷四大类(图1,表1)

5,树脂及凝胶色谱等分离鉴定了一多糖成分MAPS-药理实验表明,其仅具有诱导T 细胞增生,而对B 细胞无明显作用

[9]

。在对巨噬细胞的活性试验中,黄芪多糖可以显著提高

[10-11]

CSF ,TNF-NO 等细胞因子,巨噬细胞产生GM-α,增加NF-κB 蛋白水平

。由此可见,黄芪多糖作为生物大分子成分,

发挥着不同的免疫调节活性,这些免疫调节作用使之一方面8可以用于炎症治疗,如它可抑制脂多糖引发的TNF-α和IL-

[稿件编号][1**********]

[基金项目]天津市自然科学基金项目(10JCYBJC25800);天津医科大学基金资助项目(2009KY17);[通信作者]

*

图1Fig. 1

黄芪皂苷的母核Structure of astragaloside

E-mail :pharmgao@tju. edu. cn 高文远,

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表1黄芪皂苷部分列举List of astragalosides

化合物

R1H H H H H H H

CH 3CO H

CH 3CO H H

R2CH 3CO H H H H H H H

CH 3CO H H H

R3CH 3CO CH 3CO Glc H Glc Glc H

CH 3CO H H H Ara

R4Glc Glc H Glc H Glc Glc Glc Glc Glc H Glc

R5H H H H H H H H H H

CH 3CO H

R6H H H H Glc H Glc H H H H H

Table 1

黄芪皂苷I 黄芪皂苷II 黄芪皂苷III 黄芪皂苷IV 黄芪皂苷V 黄芪皂苷VI 黄芪皂苷VII 异黄芪皂苷I 异黄芪皂苷II cyclocephaloside II trojanoside A trojanoside H

黄芪皂苷具有多种药理活性,主要包括免疫调节、抗肿降血糖、抗病毒、多脏器保护等作用。在对多脏器保护作瘤、

用研究中,发现黄芪总苷可保护冲击波诱发的肾氧化损伤

[23]

[42]

[44]

;对代谢综合症及内皮功能障碍[43]、衰退型疾病等

发现黄芪甲苷对促血管都有保护作用。从基因水平上分析,

生成、心肌发育、增强心肌功能等基因有上调作用2. 2. 2

抗病毒方面

有抗乙型肝炎病毒的活性柯萨奇B3病毒的作用路

[49]

[48]

[46]

[45]

;通过清除氧自由基、抑制Kupffer 肝细胞内TNF-α和

[25]

在抗病毒方面,有报道称黄芪甲苷具

,在人肺腺癌细胞中可抑制腺。通过上调干扰素-γ发挥抗

[47]

[24]

TGF-β的产生,缓解肝纤维化进程;通过减少心肌细胞钙

增强自由基的迁移,降低脂质过氧化物的产生离子外流,缓衰老等作用

[26]

病毒的复制和诱导细胞凋亡

等途径防治心肌的损伤。以上抗氧化机制使之同样具有延

[27]

。同时可通过抑制TGF-β1信号通

[50]

,诱发心肌细胞的凋亡,缓解由该病毒引发的心肌炎

在对脑海马神经元保护作用研究中发现,黄芪总苷具有抑制胸腺细胞、海马神经元内钙离子浓度的升高和凋亡作用

同时抑制脑内APP 及其mRNA 、β-分泌酶mRNA 的表达,促进

[28]

α-分泌酶mRNA 的表达,最终发挥对记忆损伤保护的作用。

患者心肌细胞成纤维化进程。2. 2. 3

降糖方面

[51]

L1脂肪细胞研究中,降糖方面,在对3T3-

黄芪皂苷IV 可通过诱导TNF-α分泌,降低脂解作用,改善胰岛的耐受作用降糖作用2. 2. 4

[52]

。此外,它可以作用于肝糖调节酶,从而发挥。

B 淋巴细免疫方面,黄芪甲苷对T ,

[54]

2. 2黄芪甲苷

黄芪皂苷中活性研究较系统的为黄芪甲苷(黄芪皂苷

。对肝星胶质细胞以及猪血诱导的肝纤维化等

[53]

都有保护作用

IV ),其在黄芪中含量最高,对缺血造成的心、脑损伤具有保同时具有抗病毒、降血糖、免疫调节等活性,很多护性作用,

活性已被应用于临床。2. 2. 1伤

[29]

免疫调节方面

胞增殖、腹腔巨噬细胞功能等都有影响2. 3

其他皂苷单体

。通过抑制

[55]

NF-κB 活性以及黏附分子的表达发挥抗炎作用。

缺血保护性作用目前明确黄芪甲苷在心肌损

[30]

、低氧-复氧造心肌损伤、31]缺血大鼠[等模型中,可

[32]

其余齐墩果烷型和除黄芪甲苷具有较好的药理活性外,环菠萝烷型皂苷多具有调节淋巴细胞增殖的作用

[56-57]

ATP 酶,缓解肌浆网,并影响肌浆网内Ca-从而调节钙的转运1的水平过程,影响心脏功能。通过上调超氧歧化酶-累

[33]

,其中

、干预Macrophyllosaponin B 和黄芪皂苷VII ,两种黄芪皂苷类成分可通过体液免疫、细胞免疫等发挥免疫调节活性

[58]

PI3-K/Akt通路,刺激血管生成和提高缺氧诱导因子α1的积

,最终对心肌缺血

[34]

。黄芪

、脑缺血模型

[36]

[35]

,甚至是原位肝移植

[37]

II ,III 对不同癌细胞显示了不同的细胞毒作用[59]。皂苷I ,

在对结肠癌实验中,黄芪总皂苷可通过抑制p21,抑制细胞周G2/M期阻滞,期依赖性激酶活性等,增加细胞周期S 期、抑制癌细胞的增殖,也可通过诱导细胞凋亡的抑制作用

[62]

[60]

模型造成的缺血再灌注损伤等都具有保护作用。同时对脑

[38]

缺血再灌注导致的血脑屏障渗透性增加病变也有改善作用在对脑损伤引发的神经损伤也有一定的保护作用

。有报道,,转录激活

川芎嗪与黄芪甲苷联合应用在大鼠缺血/再灌注脑损伤模型中,

[39]

1β和caspase-3基因的表达,可通过降低IL-保护脑神经。

NSAID 活化基因[61]等,发挥抗肿瘤作用,对骨髓瘤也有很好

。在抗肿瘤、免疫调节方面,黄芪皂苷可活化

2细胞因子,2主要由活特别是黄芪皂苷VII ,而IL-诱生IL-具有免疫、抗肿瘤作用,因此推测这一机制化的T 细胞产生,

可能也是三萜类皂苷具有免疫、抗肿瘤活性的原因之一

[63]

除对缺血模型有保护作用外,黄芪甲苷心肌有保护性作如缓解大鼠的心衰用,

[40]

。对抗抑制压力过载型心肌肥厚

[41]

大鼠的肾素-血管紧张素过度激活,逆转左室肥厚。另外,。

黄芪甲苷可调节高半胱氨酸诱导的急性期内皮功能异除以上活性外,黄芪皂苷类成分特别是黄芪皂苷V 可阻

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碍(羧甲基)赖氨酸、戊糖苷等的形成,抑制糖尿病患者视网膜病变、神经病变等的发展进程,最终对糖尿病并发症有预防作用3

[64]

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黄芪黄酮

黄芪总黄酮是黄芪的又一活性部位,主要包括毛蕊异黄

芒柄花素(图2)及其糖苷等成分,具有免疫调节、抗损酮、

伤、抗突变、抗肿瘤、抑制动脉粥样硬化等活性。如,有学者发现甘肃黄芪黄酮类化合物可剂量依赖性抑制AngII 诱导的其机制可能与降低Fas 相关内皮细胞凋亡,

[65]

。在抗肿瘤方

面,黄芪总黄酮及毛蕊异黄酮等都具有抑制人红白血病K562细胞增殖的作用,可将细胞停滞在G 0/G1期,同时降低

[66]

细胞内Cyclin D1mRNA 水平。

图2Fig. 24

黄芪黄酮类典型成分

Typical structures of Astragalus flavonoids

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effects of polysaccharopeptide and Astragalus polysaccharides on tumor-bearing mice [J ].

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[15]X Zhou ,Y Xu ,G Yang ,et al. Increased galectin-1expression in

muscle of Astragalus polysaccharide-treated type 1diabetic mice [J ]. J Nat Med ,2011,65(3/4):500.

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[17]R J Li ,S D Qiu ,H X Chen ,et al. The immunotherapeutic

effects of Astragalus polysaccharide in type 1diabetic mice [J ]. Biol Pharm Bull ,2007,30(3):470.

[18]Y C Juan ,Y H Kuo ,C C Chang ,et al. Administration of a de-coction of sucrose-and polysaccharide-rich Radix Astragali (huang qi )ameliorated insulin resistance and fatty liver but af-fected beta-cell function in type 2diabetic rats [J ]. Evid Based Complement Alternat Med ,2011,2011:349807.

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结语

“补药之长”总之,黄芪药用历史悠久,古有之称,为历代

中医最常用的中药之一。近年来,国内外学者对黄芪的化学组成、药理活性进行了较为广泛的研究。经过大量的药理实黄芪呈现出极具开发价值的药用资源,在免疫调验及临床报道,

节、抗肿瘤、抗病毒、糖尿病、延缓衰老等方面具有重要地位。

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·3206·

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. 中国药理学通报,2006,22(12):细胞凋亡的保护作用[J ]1505.

[66]张冬青,汪德清,于勇. 黄芪总黄酮和毛蕊异黄酮对K562

J ]. 中国中药杂志,2011,36细胞的抑制作用及其机制研究[(24):3502.

Chemical composition and pharmacological activities of Astragali Radix

2

ZHANG Qiang 1,,GAO Wen-yuan 1*,MAN Shu-li 1

(1.School of Pharmaceutical Science and Technology ,Tianjin University ,Tianjin 300072,China ;2.Tianjin Medical University General Hospital Institute of Geriatrics ,Tianjin 300072,China )

[Abstract ]Astragali Radix ,as a tonic with a long history ,is one of the most common traditional Chinese medicines.Recently ,chemical composition and pharmacological activities of Astragali Radix have been widely reported.Polysaccharide ,triterpenes and fla-vonoids are regarded to its effective components.Pharmacological experiments and clinical reports show that Astragali Radix has good anti-tumor ,anti-virus ,diabetes ,anti-aging and so on.Therefore ,it shows a good prospect to make good effects on immune-regulation ,use of its effective components.

[Key words ]Astragali Radix ;active ingredient ;pharmacological activities ;polysaccharides ;triterpenes

doi :10.4268/cjcmm20122109

[责任编辑

马超一]

·3207·

黄芪中有效成分药理活性的研究进展

1,21*1

张蔷,高文远,满淑丽

(1. 天津大学药物科学与技术学院,天津300072;2. 天津医科大学总医院老年病研究所,天津300072)

[“补药之长”摘要]黄芪药用历史悠久,古有之称,为历代中医最常用的中药之一。近年来,国内外学者对黄芪的化学药理活性进行了较为广泛的研究。成分分析表明,黄芪以多糖、三萜、黄酮等成分为主;药理实验及临床报道表明,黄芪组成、

在免疫调节、抗肿瘤、抗病毒、糖尿病、延缓衰老等方面具有重要作用。因此,对黄芪的各个有效成分的活性总结具有临床指总结了黄芪不同活性成分的药理活性及作用机制,为该药临床研究提供理论依据,进而为其示性意义。该文通过文献综述,开发利用提供依据。

[关键词]黄芪;多糖;三萜;黄酮

黄芪作为传统中药材,具有扶正补气之功效。现代药学研究表明,黄芪含有多种活性成分,包括黄芪多糖、黄芪皂苷、黄芪黄酮类成分等。近几年,国内外围绕这些成分报道本文以黄芪的活性成分、药理作用为研了大量的实验数据,

究对象,对近年来试验结果进行汇总,以期为临床应用及产品开发提供依据。1

黄芪多糖

其结构与活性研究黄芪多糖作为一类生物大分子成分,

较为广泛。目前认为黄芪多糖的单糖种类主要包括L -鼠李L -D -L -D -L -D -糖、阿拉伯糖、木糖、木糖、核糖、核糖、半乳糖、D -葡萄糖和D -甘露糖等

[1]

的产生,因此对肠炎患者有一定的治疗作用

[12]

另一方面,黄芪多糖也可应用于抗肿瘤方面,如黄芪多糖与云芝糖肽组方后可明显降低阿霉素在抗肿瘤过程中引发的免疫耐受现象

[13]

;此外,黄芪多糖与长春瑞滨、顺铂等联合静脉注

[14]

射可改善晚期非小细胞肺癌患者的生存质量和生存期。

黄芪多糖的免疫调节作用,促使其另一主要药理活性为降血糖作用,有报道称,黄芪多糖可通过增加肌细胞内半乳1的表达凝素-病

[17]

[15]

[16]

,增加胰腺β-细胞总质量,治疗I 型糖尿

。此外,富含糖类或多糖丰富的黄芪可缓解II 型糖尿

[18]

病大鼠的胰岛素耐受及脂肪肝等症状。黄芪多糖的降糖

[2]

[3][4]

、降血糖、抗病毒、治

机制多数还是与其对骨骼肌的影响有关,它降低蛋白酪氨酸

[19]

磷酸酶1B 的表达,调节骨骼肌内PKB /GLUT4信号通

多糖发挥着极其重要的生物功能,目前报道,其具有免疫调节、抗肿瘤、抗动脉粥样硬化疗代谢性紊乱

[5]

[6]

、迟发性神经退行性疾病及抗衰老等,同

[7]

[20]

,进而增加机体对胰岛素的敏感性。这种降血糖作用

I κB 的的同时,黄芪多糖还可以通过影响肾皮质内NF-κB ,

[21]

mRNA 表达,改善早期糖尿病肾病变症状。另外,它可以

提高动物的抗病能力时已广泛应用于兽医临床,。

其中黄芪多糖的免疫调节作用报道最多,被认为与黄芪的免疫调节作用直接相关,是其最重要的作用之一。起初认对T 细胞无明显作为它只可激活B 细胞和巨噬细胞的增生,用

[8]

减少肝内质网应激并维持糖稳态发挥降血糖作用22. 1

黄芪皂苷黄芪总皂苷

[22]

。近年来,我国学者利用微波提取、膜过滤、阴离子交换目前,从膜荚黄芪和蒙古黄芪及其同属近缘植物中分离出40多种三萜皂苷类化合物,主要有黄芪皂苷、异黄芪皂苷、乙酰基黄芪皂苷、大豆皂苷四大类(图1,表1)

5,树脂及凝胶色谱等分离鉴定了一多糖成分MAPS-药理实验表明,其仅具有诱导T 细胞增生,而对B 细胞无明显作用

[9]

。在对巨噬细胞的活性试验中,黄芪多糖可以显著提高

[10-11]

CSF ,TNF-NO 等细胞因子,巨噬细胞产生GM-α,增加NF-κB 蛋白水平

。由此可见,黄芪多糖作为生物大分子成分,

发挥着不同的免疫调节活性,这些免疫调节作用使之一方面8可以用于炎症治疗,如它可抑制脂多糖引发的TNF-α和IL-

[稿件编号][1**********]

[基金项目]天津市自然科学基金项目(10JCYBJC25800);天津医科大学基金资助项目(2009KY17);[通信作者]

*

图1Fig. 1

黄芪皂苷的母核Structure of astragaloside

E-mail :pharmgao@tju. edu. cn 高文远,

·3203·

表1黄芪皂苷部分列举List of astragalosides

化合物

R1H H H H H H H

CH 3CO H

CH 3CO H H

R2CH 3CO H H H H H H H

CH 3CO H H H

R3CH 3CO CH 3CO Glc H Glc Glc H

CH 3CO H H H Ara

R4Glc Glc H Glc H Glc Glc Glc Glc Glc H Glc

R5H H H H H H H H H H

CH 3CO H

R6H H H H Glc H Glc H H H H H

Table 1

黄芪皂苷I 黄芪皂苷II 黄芪皂苷III 黄芪皂苷IV 黄芪皂苷V 黄芪皂苷VI 黄芪皂苷VII 异黄芪皂苷I 异黄芪皂苷II cyclocephaloside II trojanoside A trojanoside H

黄芪皂苷具有多种药理活性,主要包括免疫调节、抗肿降血糖、抗病毒、多脏器保护等作用。在对多脏器保护作瘤、

用研究中,发现黄芪总苷可保护冲击波诱发的肾氧化损伤

[23]

[42]

[44]

;对代谢综合症及内皮功能障碍[43]、衰退型疾病等

发现黄芪甲苷对促血管都有保护作用。从基因水平上分析,

生成、心肌发育、增强心肌功能等基因有上调作用2. 2. 2

抗病毒方面

有抗乙型肝炎病毒的活性柯萨奇B3病毒的作用路

[49]

[48]

[46]

[45]

;通过清除氧自由基、抑制Kupffer 肝细胞内TNF-α和

[25]

在抗病毒方面,有报道称黄芪甲苷具

,在人肺腺癌细胞中可抑制腺。通过上调干扰素-γ发挥抗

[47]

[24]

TGF-β的产生,缓解肝纤维化进程;通过减少心肌细胞钙

增强自由基的迁移,降低脂质过氧化物的产生离子外流,缓衰老等作用

[26]

病毒的复制和诱导细胞凋亡

等途径防治心肌的损伤。以上抗氧化机制使之同样具有延

[27]

。同时可通过抑制TGF-β1信号通

[50]

,诱发心肌细胞的凋亡,缓解由该病毒引发的心肌炎

在对脑海马神经元保护作用研究中发现,黄芪总苷具有抑制胸腺细胞、海马神经元内钙离子浓度的升高和凋亡作用

同时抑制脑内APP 及其mRNA 、β-分泌酶mRNA 的表达,促进

[28]

α-分泌酶mRNA 的表达,最终发挥对记忆损伤保护的作用。

患者心肌细胞成纤维化进程。2. 2. 3

降糖方面

[51]

L1脂肪细胞研究中,降糖方面,在对3T3-

黄芪皂苷IV 可通过诱导TNF-α分泌,降低脂解作用,改善胰岛的耐受作用降糖作用2. 2. 4

[52]

。此外,它可以作用于肝糖调节酶,从而发挥。

B 淋巴细免疫方面,黄芪甲苷对T ,

[54]

2. 2黄芪甲苷

黄芪皂苷中活性研究较系统的为黄芪甲苷(黄芪皂苷

。对肝星胶质细胞以及猪血诱导的肝纤维化等

[53]

都有保护作用

IV ),其在黄芪中含量最高,对缺血造成的心、脑损伤具有保同时具有抗病毒、降血糖、免疫调节等活性,很多护性作用,

活性已被应用于临床。2. 2. 1伤

[29]

免疫调节方面

胞增殖、腹腔巨噬细胞功能等都有影响2. 3

其他皂苷单体

。通过抑制

[55]

NF-κB 活性以及黏附分子的表达发挥抗炎作用。

缺血保护性作用目前明确黄芪甲苷在心肌损

[30]

、低氧-复氧造心肌损伤、31]缺血大鼠[等模型中,可

[32]

其余齐墩果烷型和除黄芪甲苷具有较好的药理活性外,环菠萝烷型皂苷多具有调节淋巴细胞增殖的作用

[56-57]

ATP 酶,缓解肌浆网,并影响肌浆网内Ca-从而调节钙的转运1的水平过程,影响心脏功能。通过上调超氧歧化酶-累

[33]

,其中

、干预Macrophyllosaponin B 和黄芪皂苷VII ,两种黄芪皂苷类成分可通过体液免疫、细胞免疫等发挥免疫调节活性

[58]

PI3-K/Akt通路,刺激血管生成和提高缺氧诱导因子α1的积

,最终对心肌缺血

[34]

。黄芪

、脑缺血模型

[36]

[35]

,甚至是原位肝移植

[37]

II ,III 对不同癌细胞显示了不同的细胞毒作用[59]。皂苷I ,

在对结肠癌实验中,黄芪总皂苷可通过抑制p21,抑制细胞周G2/M期阻滞,期依赖性激酶活性等,增加细胞周期S 期、抑制癌细胞的增殖,也可通过诱导细胞凋亡的抑制作用

[62]

[60]

模型造成的缺血再灌注损伤等都具有保护作用。同时对脑

[38]

缺血再灌注导致的血脑屏障渗透性增加病变也有改善作用在对脑损伤引发的神经损伤也有一定的保护作用

。有报道,,转录激活

川芎嗪与黄芪甲苷联合应用在大鼠缺血/再灌注脑损伤模型中,

[39]

1β和caspase-3基因的表达,可通过降低IL-保护脑神经。

NSAID 活化基因[61]等,发挥抗肿瘤作用,对骨髓瘤也有很好

。在抗肿瘤、免疫调节方面,黄芪皂苷可活化

2细胞因子,2主要由活特别是黄芪皂苷VII ,而IL-诱生IL-具有免疫、抗肿瘤作用,因此推测这一机制化的T 细胞产生,

可能也是三萜类皂苷具有免疫、抗肿瘤活性的原因之一

[63]

除对缺血模型有保护作用外,黄芪甲苷心肌有保护性作如缓解大鼠的心衰用,

[40]

。对抗抑制压力过载型心肌肥厚

[41]

大鼠的肾素-血管紧张素过度激活,逆转左室肥厚。另外,。

黄芪甲苷可调节高半胱氨酸诱导的急性期内皮功能异除以上活性外,黄芪皂苷类成分特别是黄芪皂苷V 可阻

·3204·

碍(羧甲基)赖氨酸、戊糖苷等的形成,抑制糖尿病患者视网膜病变、神经病变等的发展进程,最终对糖尿病并发症有预防作用3

[64]

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[6]H Zhang ,N Pan ,S Xiong ,et al. Inhibition of polyglutamine-me-diated proteotoxicity by Astragalus membranaceus polysaccharide through the DAF-16/FOXOtranscription factor in caenorhabditis elegans [J ]. Biochem J ,2012,441(1):417.

[7]郇志利,黄云,毛小伟,等. 黄芪及黄芪多糖在养殖上的应

. 当代水产,2011(11):59. 用[J ]

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[9]林梦感,杨义芳,许海燕. 黄芪多糖MAPS-5的化学结构及

其体外淋巴细胞增殖活性[J ]. 中草药,2009,40(12):1865.

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inhibits lipopolysaccharide-induced production of TNF-alpha and J ]. World J Gastroenterol ,2009,15(29):3676. interleukin-8[

黄芪黄酮

黄芪总黄酮是黄芪的又一活性部位,主要包括毛蕊异黄

芒柄花素(图2)及其糖苷等成分,具有免疫调节、抗损酮、

伤、抗突变、抗肿瘤、抑制动脉粥样硬化等活性。如,有学者发现甘肃黄芪黄酮类化合物可剂量依赖性抑制AngII 诱导的其机制可能与降低Fas 相关内皮细胞凋亡,

[65]

。在抗肿瘤方

面,黄芪总黄酮及毛蕊异黄酮等都具有抑制人红白血病K562细胞增殖的作用,可将细胞停滞在G 0/G1期,同时降低

[66]

细胞内Cyclin D1mRNA 水平。

图2Fig. 24

黄芪黄酮类典型成分

Typical structures of Astragalus flavonoids

[13]J Li ,Y Bao ,W Lam ,et al. Immunoregulatory and anti-tumor

effects of polysaccharopeptide and Astragalus polysaccharides on tumor-bearing mice [J ].

Immunopharmacol Immunotoxicol ,

2008,30(4):771.

[14]L Guo ,S P Bai ,L Zhao ,et al. Astragalus polysaccharide injec-tion integrated with vinorelbine and cisplatin for patients with ad-vanced non-small cell lung cancer :effects on quality of life and survival [J ]. Med Oncol ,2012,29(3):1656.

[15]X Zhou ,Y Xu ,G Yang ,et al. Increased galectin-1expression in

muscle of Astragalus polysaccharide-treated type 1diabetic mice [J ]. J Nat Med ,2011,65(3/4):500.

[16]李如江,邱曙东,陈红霞,等. 黄芪多糖对1型糖尿病小鼠

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[17]R J Li ,S D Qiu ,H X Chen ,et al. The immunotherapeutic

effects of Astragalus polysaccharide in type 1diabetic mice [J ]. Biol Pharm Bull ,2007,30(3):470.

[18]Y C Juan ,Y H Kuo ,C C Chang ,et al. Administration of a de-coction of sucrose-and polysaccharide-rich Radix Astragali (huang qi )ameliorated insulin resistance and fatty liver but af-fected beta-cell function in type 2diabetic rats [J ]. Evid Based Complement Alternat Med ,2011,2011:349807.

[19]Y Wu ,J P Ou-Yang ,K Wu ,et al. Hypoglycemic effect of As-. Acta Phar-tragalus polysaccharide and its effect on PTP1B [J ]macol Sin ,2005,26(3):345.

结语

“补药之长”总之,黄芪药用历史悠久,古有之称,为历代

中医最常用的中药之一。近年来,国内外学者对黄芪的化学组成、药理活性进行了较为广泛的研究。经过大量的药理实黄芪呈现出极具开发价值的药用资源,在免疫调验及临床报道,

节、抗肿瘤、抗病毒、糖尿病、延缓衰老等方面具有重要地位。

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Chemical composition and pharmacological activities of Astragali Radix

2

ZHANG Qiang 1,,GAO Wen-yuan 1*,MAN Shu-li 1

(1.School of Pharmaceutical Science and Technology ,Tianjin University ,Tianjin 300072,China ;2.Tianjin Medical University General Hospital Institute of Geriatrics ,Tianjin 300072,China )

[Abstract ]Astragali Radix ,as a tonic with a long history ,is one of the most common traditional Chinese medicines.Recently ,chemical composition and pharmacological activities of Astragali Radix have been widely reported.Polysaccharide ,triterpenes and fla-vonoids are regarded to its effective components.Pharmacological experiments and clinical reports show that Astragali Radix has good anti-tumor ,anti-virus ,diabetes ,anti-aging and so on.Therefore ,it shows a good prospect to make good effects on immune-regulation ,use of its effective components.

[Key words ]Astragali Radix ;active ingredient ;pharmacological activities ;polysaccharides ;triterpenes

doi :10.4268/cjcmm20122109

[责任编辑

马超一]

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