香附中mesocyperusphenol A的含量测定研究

目的：建立香附中 mesocyperusphenol A 的超高效液相色谱（UHPLC）含量测定方法,为香附的合理质量控制提供依据。方法采用 Poroshell 120 EC - C18色谱柱（3.0 mm ×150 mm,1.8μm）,流动相乙腈-水（28∶72,V∶V）,检测波长：325 nm。结果 Mesocyperusphenol A 在0.784~7.84μg·mL -1范围内线性关系良好,r ＝0.9997（n＝6）,加样回收率为101.6%,RSD ＝1.39%（ n ＝9）;6批香附药材中 mesocyperusphenol A 的含量为3.72~10.00μg·g -1。结论 Mesocyperusphenol A 为香附子药材中的特征活性成分,所建立的测定方法操作简便可靠,可为香附药材的质量控制提供依据。     

(+)-Nootkatone and (+)-valencene from rhizomes of Cyperus rotundus increase survival rates in septic mice due to heme oxygenase-1 induction

Ethnopharmacological relevance

The rhizomes of Cyperus rotundus have been used as traditional folk medicine for the treatment of inflammatory diseases. However, the mechanism by which extract of rhizomes of Cyperus rotundus (ECR) elicits anti-inflammation has not been extensively investigated so far. The aim of the present study was to test whether heme oxygenase (HO)-1 induction is involved in the anti-inflammatory action of ECR.

Materials and methods

Induction of HO-1 and inhibition of inducible nitric oxide synthase (iNOS)/NO production by ECR and its 12 constituents (3 monoterpenes, 5 sesquiterpenes, and 4 aromatic compounds) were investigated using RAW264.7 cells in vitro. In addition, anti-inflammatory action of ECR and its two active ingredients (nookkatone, valencene) were confirmed in sepsis animal model in vivo.

Results

ECR increased HO-1 expression in a concentration-dependent manner, which was correlated with significant inhibition of iNOS/NO production in LPS-activated RAW264.7 cells. Among 12 compounds isolated from ECR, mostly sesquiterpenes induced stronger HO-1 expression than monoterpenes in macrophage cells. Nootkatone and valencene (sesquiterpenes) significantly inhibited iNOS expression and NO production in LPS-simulated RAW264.7 cells. Inhibition of iNOS expression by nootkatone, valencene, and ECR were significantly reduced in siHO-1 RNA transfected cells. Furthermore, all three showed marked inhibition of high mobility group box-1 (HMGB1) in LPS-activated macrophages and increased survival rates in cecal ligation and puncture (CLP)-induced sepsis in mice.

Conclusions

Taken together, we concluded that possible anti-inflammatory mechanism of ECR is, at least, due to HO-1 induction, in which sesquiterpenes such as nootkatone and valencene play a crucial role.     

正交试验法优化香附总黄酮提取工艺

目的优选香附总黄酮的提取工艺。方法以乙醇体积分数、料液比、提取时间、提取次数为考察因素,以总黄酮含量为测定指标,采用正交试验优化香附总黄酮的最佳提取工艺。结果香附总黄酮的最佳提取工艺为乙醇体积分数70%、料液比1∶15、提取时间45 min、提取次数为2次。结论该提取工艺稳定,适合香附总黄酮的提取。     

四制香附与生品香附挥发油成分的比较

目的:研究建昌帮四制香附与生品香附挥发油成分的差异,探讨建昌帮四制法对挥发性成分的影响。方法:采用HPLC与GC-MS对香附炮制前后的挥发油成分进行比较分析。结果:HPLC法表明:四制香附与生品香附在主成分(相对峰面积>10%)种类上无明显差异(含3种),主成分相对峰面积略有不同。GC-MS气质联用检测结果表明,四制香附与生品香附所含化合物种类数量有所不同,从香附生品挥发油提取物中鉴别出33种化合物,四制香附挥发油提取物中鉴别出41种化合物。但主成分种类比较无明显差异,四制法主成分挥发油相对峰面积总体呈下降趋势。结论:四制香附挥发油提取物比生品香附挥发油提取物中成分种类增加20种,但对主成分相对峰面积进行比较含量略有差异,HPLC与GC-MS分析所得结果一致。     

Hypotensive and spasmolytic activities of crude extract ofCyperus scariosus

Intravenous administration of hydro-methanolic extract ofCyperus scarious (3–10 mg/kg) produced hypotensive and bradycardiac effects. These effects remained unaltered in atropinized animals indicating that cardiovascular effects of the plant extract are not mediated through activation of muscarinic receptors. In thein vitro studies, it suppressed the spontaneous contractions of guinea-pig paired atria, rat uterus and rabbit jejunum in a concentration-dependent (0.1–1 mg/ml) manner. It also inhibited histamine or acetylcholine-induced contractions of guinea-pig ileum indicating non-specific spasmolytic action. In rabbit aorta, it inhibited norepinephrine (10 μM) as well as K⁺ (80 mM)-induced contractions at similar concentrations (0.1–1mg/ml). These data indicate thatCyperus scariosus contains Ca²⁺ channel blocker-like constituent(s) which may explain hypotensive effect observedin vivo and the general spasmolytic activity of plant may explain its folkloric use in diarrhoea.     

香附总黄酮的超声波提取工艺研究

目的 探讨香附总黄酮的提取及鉴别方法,以充分利用香附植物资源,避免资源的浪费.方法 采用超声波乙醇浸提法从香附中提取黄酮类物质,对所提取的黄酮类物质进行验证,并用分光光度法测定含量.结果 测得样品中总黄酮的含量C=0.186 4 mg/ml,回收率为102.7%,其纯度和产率均较高.结论 该方法采用全物理过程,无任何污染,是提取香附黄酮类物质的有效途径.     

不同产地香附中总黄酮含量比较研究

摘 要 目的： 建立香附总黄酮含量检测方法,并考察不同产地香附中总黄酮的含量。 方法: 以芦丁作为标准品,紫外分光光度法检测不同产地香附中总黄酮含量。结果:芦丁对照品浓度在0.064 3～0.642 6 mg·ml^-1范围内与吸光度呈良好的线性关系（r=0.999 1）,加样回收率为99.74%,RSD为2.16%(n=6)。不同产地香附总黄酮含量依次是河南>四川>广东>安徽>海南>山东。结论: 该方法简便、准确,可用于香附的质量控制。香附总黄酮含量以河南产地最高。     

香附化学成分研究进展

香附是中医常用的一种妇科良药,具有疏肝理气,调经止痛之功效。现代药理研究也证明其具有抗抑郁、抗肿瘤、抑制乙酰胆碱酯酶活性、抗糖尿病等作用。迄今为止从香附中已分离得到100多个化合物,其中倍半萜类化合物就近70个,且骨架类型多样,有桉烷型、广藿香烷型、胡椒烷型、Rotundane型等,此外,还有黄酮类和三萜类化合物等。本文对其化学成分进行系统、全面的综述,为其进一步的开发利用提供参考。