牛蒡子苷元现代药理作用研究进展

ARC-G（牛蒡子苷元）为中药牛蒡子中常见的主要活性物质,通过众多学者的潜心钻研,使得ARC-G在药用方面的作用逐渐凸显出来。目前对其药理作用的研究比较深入,有抗炎及增强免疫力、抵御病毒、抗白血病、抑制肿瘤细胞活性和调节血糖等作用。已进行初步研究的药理活性包括抗菌、抵御血小板活化因子（PAF）受体、调节血压稳定以及对于心脏病的调节。本文综述了近几年关于牛蒡子苷元药理作用的文献,以期为更深入地研究ARC-G药理作用以及扩大其临床应用提供参考。     

牛蒡子水解后牛蒡苷元的含量测定

目的：建立牛蒡子药材水解后药材中牛蒡苷元的含量测定方法。方法：采用HPLC,以牛蒡苷元的含量测定为指标,测定牛蒡子药材水解后药材中牛蒡苷元的含量。Agilentll00液相色谱系统四元泵,色谱柱：Phenomsil PC-8025,（4．6mm×250mm,5μm）,流动相：甲醇-水（50：55）;检测波长：280nm。结果：牛蒡苷元的线性方程Y=905．74X-90．113,r=0．9993,线性范围0．81～4．86μg;平均回收率为100．09％,RSD=2．244％。结论：采用HPLC含量测定的方法,精密度、重现性及稳定性皆良好,方法简便、易行,可作为牛蒡苷元含量的测定方法。     

不同产地牛蒡子药材质量评价

目的：对不同产地牛蒡子药材进行质量评价。方法：用HPLC法测定了不同产地牛蒡子药材中牛蒡子苷和牛蒡子苷元的含量。结果：苷含量为2．85％～7.82％，以天水最低，建德最高，苷元含量为0．03％～1．37％，以会川最低，金陵最高。结论：该方法快速准确，可同时测定牛蒡子药材中牛蒡子苷和牛蒡子苷元的含量，可作为牛蒡子药材的质量评价方法。     

牛蒡子苷元对人食管癌细胞增殖细胞核抗原表达及细胞周期影响的研究

目的 观察牛蒡子苷元(arctigenin ARG)对体外培养的人食管癌细胞(esophageal cancer-1 cells,EC-1)增殖和增殖细胞核抗原(Proliferating Cell Nuclear Antigen,PCNA)表达及细胞周期的影响.方法 将不同浓度的ARG作用于EC-1,噻唑蓝(methyl thiazolyl tetrazolium M1Tr)实验检测细胞增殖抑制率、流式细胞术测定细胞周期变化,免疫组织化学法测定PCNA表达水平.结果 与对照组比较,ARG对EC-1细胞生长有抑制作用,随着时间/浓度的增加抑制作用逐渐增强(P<0.05);牛蒡子苷元可抑制EC-1由G0/G1向S期转换,G0/G1期细胞百分率较对照组显著增加,S期细胞百分率显著降低;随ARG浓度增加EC-1内PCNA表达水平逐渐降低.结论 ARG有抑制EC-1增殖,下调EC-1内PCNA表达水平,阻滞细胞周期的作用.     

牛蒡子提取物中牛蒡苷和牛蒡苷元的含量测定研究

目的建立牛蒡子提取物中牛蒡苷及其苷元的含量测定方法.方法采用HPLC,以牛蒡甘、牛蒡苷元为含量测定指标,测定了牛蒡了提取物中牛蒡苷和牛蒡苷元的含量.色谱柱为Kromasil C18 100A(150mm×4.6mm,51μm).流动相甲醇-水(采川梯度洗脱的方式0～7min,35%～45%甲醇;7～9[Bin,45%～48%甲醇;9～15min,48%～53%甲醇;15～24min,53%～80%甲醇;24～30min,80%～100%甲醇);检测波长为280nm.结果牛蒡苷及牛蒡苷元的平均回收率分别为97.7%,96.9%.RSD分别为1.3%,0.9%(n=5);线性方程分别为Y=782.6X-64.11(r=0.999 8).y=1 220.217X-35.26(r=0.999 8).结论该方法快速准确,可同时测定牛蒡提取物中牛蒡苷和牛蒡苷元的含量,可用作牛蒡子提取物的质量控制方法.     

Arctigenin induces cell cycle arrest by blocking the phosphorylation of Rb via the modulation of cell cycle regulatory proteins in human gastric cancer cells

Gastric cancer is a leading cause of cancer-related deaths, worldwide being second only to lung cancer as a cause of death. Arctigenin, a representative dibenzylbutyrolactone lignan, occurs in a variety of plants. However, the molecular mechanisms of arctigenin for anti-tumor effect on gastric cancer have not been examined. This study examined the biological effects of arctigenin on the human gastric cancer cell line SNU-1 and AGS. Cell proliferation was determined by MTT assay. In MTT assay, the proliferation of SNU-1 and AGS cells was significantly inhibited by arctigenin in a time and dose dependent manner, as compared with SNU-1 and AGS cells cultured in the absence of arctigenin. Inhibition of cell proliferation by arctigenin was in part associated with apoptotic cell death, as shown by changes in the expression ratio of Bcl-2 to Bax by arctigenin. Also, arctigenin blocked cell cycle arrest from G₁ to S phase by regulating the expression of cell cycle regulatory proteins such as Rb, cyclin D1, cyclin E, CDK4, CDK2, p21Waf1/Cip1 and p15 INK4b. The antiproliferative effect of arctigenin on SNU-1 and AGS gastric cancer cells revealed in this study suggests that arctigenin has intriguing potential as a chemopreventive or chemotherapeutic agent.     

Survivin基因在牛蒡子苷元增强人肺癌H460细胞化疗敏感性中的作用

目的 研究Survivin基因在牛蒡子苷元促进肺癌细胞化疗敏感性中的作用.方法 应用RT-PCR技术从H460细胞中扩增全长人Survivin cDNA,并将其克隆至pcDNA3.1(+)表达载体,构建人Survivin基因真核表达质粒.将pcDNA3.1-Survivin重组质粒或空载体分别转染H460细胞,孵育24 h后,应用Western blot法检测Survivin过表达情况;转染细胞与牛蒡子苷元单独或联合顺铂处理,应用Annexin-Ⅴ/PI染色法检测细胞凋亡情况.结果 与未转染和转染空载体质粒的H460细胞相比,转染pcDNA3.1-Survivin重组质粒H460细胞Survivin水平显著增加,提高大约10倍.低剂量顺铂对H460细胞Survivin蛋白表达影响不显著,而牛蒡子苷元可显著抑制Survivin蛋白表达水平.当牛蒡子苷元与顺铂联合作用时,Survivin蛋白表达抑制程度更大.与转染空载体质粒相比,转染Survivin表达重组质粒的细胞对牛蒡子苷元单独或联合顺铂诱导的凋亡具有抗性,细胞凋亡比率显著下降.结论 牛蒡子苷元抑制人肺癌细胞中Survivin基因表达.牛蒡子苷元促人肺癌细胞顺铂敏感性与抑制Survivin通路有关.     

不同产地牛蒡子药材质量评价

目的建立不同产地牛蒡子药材综合质量评价方法。方法用HPLC法测定了市售不同产地牛蒡子药材10个样品中牛蒡子苷及牛蒡子苷元的含量。结果苷含量为5.07%～8.25%,以西安市售药材含量最高;牛蒡子苷元的含量为0.145%～1.39%,以广西市售药材含量最高。结论以牛蒡子苷和牛蒡子苷元的总和作为质量评价指标,得出西安市售药材的质量较好。本方法简便、易行。     

In vitro anti-inflammatory effects of arctigenin,a lignan from Arctium lappa L., through inhibition on iNOS pathway

Ethnopharmacological relevance

Arctigenin, a bioactive constituent from dried seeds of Arctium lappa L. (Compositae) which has been widely used as a Traditional Chinese Medicine for dispelling wind and heat included in Chinese Pharmacophere, was found to exhibit anti-inflammatory activities but its molecular mechanism remains unknown yet.

Aim of the study

To investigate the anti-inflammatory mechanism of arctigenin.

Materials and methods

Cultured macrophage RAW 264.7 cells and THP-1 cells were used for the experiments. Griess assay was used to evaluate the inhibitory effect of arctigenin on the overproduction of nitric oxide (NO). ELISA was used to determine the level of pro-inflammatory cytokines including tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6). The inhibitory effect on the enzymatic activity of cyclooxygenase-2 (COX-2) was tested by colorimetric method. Western blot was used to detect the expression of inducible nitric oxide synthase (iNOS) and COX-2.

Results

Arctigenin suppressed lipopolysaccharide (LPS)-stimulated NO production and pro-inflammatory cytokines secretion, including TNF-α and IL-6 in a dose-dependent manner. Arctigenin also strongly inhibited the expression of iNOS and iNOS enzymatic activity, whereas the expression of COX-2 and COX-2 enzymatic activity were not affected by arctigenin.

Conclusions

These results indicated that potent inhibition on NO, TNF-α and IL-6, but not COX-2 expression and COX-2 activity, might constitute the anti-inflammatory mechanism of arctigenin. Arctigenin suppressed the overproduction of NO through down-regulation of iNOS expression and iNOS enzymatic activity in LPS-stimulated macrophage.     

牛蒡子苷元对肝癌侵袭转移的影响

目的:研究牛蒡子苷元(arctigenin,ARG)对肿瘤黏附、侵袭、转移的影响.方法:体外实验分别采用MTT法、Transwell 法检测ARG对SMMC-7721细胞黏附、侵袭和转移的影响;体内实验采用裸鼠肺转移瘤模型,检测ARG对SMMC-7721细胞肺转移的影响.结果:与空白对照组相比,ARG作用后SMMC-7...