牛蒡子的研究进展

综述了国内外近年来对牛蒡子化学成分、药理作用、提取方法以及检测方法的研究状况。     

牛蒡子口腔崩解片的处方研究

目的确定牛蒡子口腔崩解片的处方。方法采用正交设计法选择牛蒡子口腔崩解片的处方。结果确定牛蒡子口腔崩解片处方中主要的成分配比为:交联聚乙烯吡咯烷酮8%,微晶纤维素25%,α-乳糖25%。结论确定了牛蒡子口腔崩解片的处方,但是此片剂口感一般,须进一步研究。     

转化牛蒡子苷牛蒡内生菌的分离及L2菌株的鉴定

从牛蒡(Arctium lappa L.)的根、茎、叶、总苞、种子中分离纯化了57株内生菌。以牛蒡子粉为底物,采用高效液相色谱法定量测定转化培养液中牛蒡子苷和牛蒡子苷元的含量,筛选得到6株转化牛蒡子苷的内生菌。其中L2的转化率最高,可达76.9%。利用LC-MS方法对其转化产物牛蒡子苷元进行了验证。L2经过形态观察、生理生化特征分析及16S rDNA序列分析,鉴定为氧化微杆菌(Microbacterium oxydans)。本试验结果为探索牛蒡内生菌转化牛蒡子苷成主要药效成分牛蒡子苷元技术提供了科学依据。     

Arctigenin isolated from the seeds of Arctium lappa ameliorates memory deficits in mice

The seeds of Arctium lappa L. (AL, family Asteraceae), the main constituents of which are arctiin and arctigenin, have been used as an herbal medicine or functional food to treat inflammatory diseases. These main constituents were shown to inhibit acetylcholinesterase (AChE) activity. Arctigenin more potently inhibited AChE activity than arctiin. Arctigenin at doses of 30 and 60?mg/kg (p.?o.) potently reversed scopolamine-induced memory deficits by 62?% and 73?%, respectively, in a passive avoidance test. This finding is comparable with that of tacrine (10?mg/kg p.?o.). Arctigenin also significantly reversed scopolamine-induced memory deficits in the Y-maze and Morris water maze tests. On the basis of these findings, arctigenin may ameliorate memory deficits by inhibiting AChE.     

Gastroprotective activity of the chloroform extract of the roots from Arctium lappa L

Arctium lappa L. is used in folk medicine as a diuretic, depurative and digestive stimulant and in dermatological conditions. The objective of this study was to evaluate the effect and the possible mechanisms involved in the gastroprotective effects of a chloroform extract (CE) of the roots from A. lappa and its fractions. Oral pretreatment with CE (10, 30 and 100 mg kg(-1)) significantly reduced gastric lesions induced by ethanol by 61%, 70% and 76%, respectively. Oral administration of CE (100 mg kg(-1) per day for 7 days) reduced the chronic gastric ulceration induced by acetic acid by 52%. Intraduodenal CE (100, 300 and 600 mg kg(-1)) reduced the total acidity of gastric secretion by 22%, 22% and 33%, respectively, while i.p. administration (10, 30 and 100 mg kg(-1)) inhibited total acidity by 50%, 60% and 67%, respectively. In-vitro, CE inhibited H+, K+ -ATPase activity with an EC50 of 53 microgmL(-1) and fraction A (30 and 100 microgmL(-1)) reduced this by 48% and 89%, respectively. CE had no effect on gastrointestinal motility. CE (250 microgmL(-1)) and fraction B (100 and 250 microgmL(-1)) had free-radical scavenging ability, inhibiting 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical activity by 50%, 20% and 55%, respectively. Collectively, the results show that the CE protects animals from gastric lesions by reducing gastric acid secretion via inhibition of gastric H+, K+ -ATPase.     

A new lignan from the seeds of Arctium lappa

A new compound, neoarctin A (1), together with nine known compounds (2-10), were obtained from the ethanolic extract of the seeds of Arctium lappa. The structure of 1 was elucidated on the basis of spectral and chemical evidence.     

Two new compounds from the fruits of Arctium lappa

Phytochemical investigation of the extract of Arctii Fructus led to the isolation and characterization of two new compounds, named arctiisesquineolignan B (1) and arctiiphenolglycoside A (2). Their structures were elucidated by means of spectroscopic methods (UV, IR, HR-ESI-MS, 1D and 2D NMR) and chemical evidence, as well as by comparison with known analogs in the literature. Compound 2 exhibited stronger antioxidant activity than the positive control ascorbic acid at a concentration of 10 μM.     

A new lignan from the seeds of Arctium lappa

A new compound, neoarctin A (1), together with nine known compounds (2-10), were obtained from the ethanolic extract of the seeds of Arctium lappa. The structure of 1 was elucidated on the basis of spectral and chemical evidence.     

牛蒡子化学成分及药理作用研究进展

牛蒡子为中医临床常用解表药,有较高的药用价值。本文对牛蒡子的化学成分、药理作用做一综述,对牛蒡子的进一步研究提供参考。     

牛蒡子化学成分的分离与鉴定

目的:分离与鉴定牛蒡子中的化学成分。方法:采用硅胶柱色谱、SephadexLH-20等手段对牛蒡子进行分离纯化,通过理化性质鉴别与各种波谱学方法鉴定其结构。结果:从牛蒡子中分离鉴定出10个化学成分,分别为β-谷甾醇(1)、牛蒡子苷元(2)、罗汉松脂素(3)、牛蒡酚B(4)、牛蒡酚A(5)、牛蒡酚F(6)、牛蒡子苷(7)、8-hydroxypinoresino(l8)、(+)-Fraxiresino(l9)、胡萝卜苷(10)。其中,化合物8、9为首次从牛蒡子中获得。结论:本试验结果可为牛蒡子的进一步研究提供依据。     

Antiproliferative and apoptotic effects of butyrolactone lignans from Arctium lappa on leukemic cells

In the course of screening for pharmacologically active substances from extracts of crude drugs used traditionally in Sino-Japanese herbal medicines, it was found that the 70 % ethanol extract from the fruits of Arctium lappa L. (Compositae) showed potent antiproliferative activity against B cell hybridoma cell, MH60. By bioassay-guided purification, a new lignan, (+)-7,8-didehydroarctigenin, together with the known lignans (-)-arctigenin and (-)-matairesinol were isolated as the active ingredients from an aqueous ethanolic extract of the fruits of A. lappa. Of these active compounds, (-)-arctigenin showed the most potent antiproliferative activity against MH60 cells (IC (50) : 1.0 microM), and the activity was suggested to be due to apoptosis.     

牛蒡根4种提取物体外抗肿瘤活性的比较研究

目的:研究牛蒡根4种提取物体外抗肿瘤活性。方法:以系统溶剂分离法分别提取牛蒡根的石油醚、氯仿、乙酸乙酯、正丁醇部位。采用MTT法检测4种提取物对人乳腺癌细胞MCF-7、人胃腺癌细胞BGC-823、小鼠肝癌细胞HepA、肉瘤细胞S180和小鼠脾淋巴细胞生长的抑制作用。结果:牛蒡根石油醚、氯仿、乙酸乙酯3种提取物对MCF-7细胞和BGC-823细胞在体外有一定生长抑制作用;牛蒡根4种提取物对HepA细胞、S180细胞和小鼠脾淋巴细胞在体外有一定的生长抑制作用。结论:牛蒡根石油醚、氯仿、乙酸乙酯提取物体外具有一定的抗肿瘤活性,这种作用与增强细胞免疫活性无关。     

Ethanolic extract of roots from Arctium lappa L. accelerates the healing of acetic acid-induced gastric ulcer in rats: Involvement of the antioxidant system

We evaluate the curative efficacy of the ethanolic extract (EET) of roots from Arctium lappa (bardana) in healing of chronic gastric ulcers induced by 80% acetic acid in rats and additionally studies the possible mechanisms underlying this action.Oral administration of EET (1, 3, 10 and 30 mg/kg) reduced the gastric lesion area in 29.2%, 41.4%, 59.3% and 38.5%, respectively, and at 10 mg/kg promoted significant regeneration of the gastric mucosa, which was confirmed by proliferating cell nuclear antigen immunohistochemistry. EET (10 mg/kg) treatment did not increase the gastric mucus content but restored the superoxide dismutase activity, prevented the reduction of glutathione levels, reduced lipid hydroperoxides levels, inhibited the myeloperoxidase activity and reduced the microvascular permeability. In addition, EET reduced the free radical generation and increased scavenging of 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radicals in vitro. Furthermore, intraduodenal EET (10 and 30 mg/kg) decreased volume and acidity of gastric secretion. Total phenolic compounds were high in EET (Folin–Ciocalteau assay) and the analysis by liquid chromatography-mass spectrometry revealed that the main compounds present in EET were a serie of hydroxycinnamoylquinic acid isomers. In conclusion, these data reveal that EET promotes regeneration of damaged gastric mucosa, probably through its antisecretory and antioxidative mechanisms.     

牛蒡子的临床研究述要

对牛蒡子近几年的现代临床应用资料进行检索和归纳,以期更好地综合开发利用牛蒡子。     

In vitro and in vivo antimutagenic effects of DIG,a herbal preparation of Berberis vulgaris,Taraxacum officinale and Arctium lappa,against mitomycin C

DIG, a liquid herbal preparation made from a mixture of diluted mother tinctures of Berberis vulgaris, Taraxacum officinale and Arctium lappa, was assessed for its antimutagenic properties against mitomycin C. The micronucleus assay on Chinese hamster ovary (CHO)-K1 cells was used to evaluate the in vitro anticlastogenic activity of DIG compared to those of separately diluted mother tinctures. The micronucleus assay was performed on mouse erythrocytes and the comet assay was performed on mouse liver, kidney, lung, brain and testicles to assess the protective effects of DIG (0.2 and 2 % at libitum) against an intraperitoneal injection of mitomycin C (1 mg Kg^?1) in mice. DIG exerted a powerful anticlastogenic activity, under both pretreatment and simultaneous treatment conditions as assessed by the micronucleus assay in CHO-K1 cells. Its protective activity was greater than that observed for each mother tincture. DIG reduced micronuclei levels in mouse erythrocytes and suppressed >80 % of DNA strand breaks in the liver, kidney, lung, brain and testicles of mice exposed to mitomycin C.

     

牛蒡子浸膏的稳定性研究

目的确定牛蒡子浸膏的干燥条件。方法在不同的干燥温度和时间下,测定牛蒡子浸膏中有效成分牛蒡苷的含量。结果在80℃干燥48h后,牛蒡子浸膏有效成分牛蒡苷的损失较小,而在100℃烘48h后牛蒡苷的含量约下降了20．00％。结论牛蒡子浸膏的干燥温度应控制在80℃以下。     

Polyamide柱层析／RP—HPLC／LC—ESI—MS分离纯化鉴定牛蒡叶中的绿原酸

目的：建立分离纯化鉴定牛蒡（Arctium lappa L.)叶中绿原酸（chlorogenic acid)的PolyamideSC6柱层析／RP－HPLC／LC－ESI－MS方法，方法：牛蒡叶经80％甲醇抽提，减压浓缩后，用氯仿去色素，得粗提物。粗提物经PolyamideSC6柱层析，依次用水，30％甲醇、60％甲醇及甲醇洗脱，甲醇洗脱组分进行RP－HPLC和LC－ESI－MS分析。结果：牛蒡叶的80％甲醇粗提物经PolyamideSC6柱层析，甲醇洗脱组分经RP－HPLC分析为单一成分，tR=20.0min,λmax(nm)为216．6／240 sh/300sh/325.6，与对照品绿原酸共注射进行RP－HPLC实验，表明两者有叠加效应，tR与λmax均一致。LC－ESI－MS测定结果表明，该洗脱组分与对照品绿原酸的分子量相同，均为354。由此可鉴定该甲醇洗脱组分为绿原酸。结论：牛蒡叶的80％甲醇粗提物经PolyamideSC6柱层析，甲醇洗脱组分为单一成分－－绿原酸。