甘草新木脂素的分离与化学结构

从陕北产甘草Clycyrrhiza uralensis Fisch)的根中分离出五种结晶,分别鉴定为β-谷甾醇(β-sitosterol),芒柄花黄素(Formononetin)甘草西定(Licoricidin)及甘草利酮(Licoricone)。晶V为一新成分,命名为甘草新木脂素(Liconeolignan)其化学结构用化学降解和光谱分析定为[Ⅳa]。     

蒙古黄芪中芒柄花素含量的测定及黄酮类成分提取工艺的优化

目的建立芒柄花素的含量测定方法,优选黄芪中黄酮类成分的提取工艺。方法采用高效液相色谱-紫外检测法,建立芒柄花素的含量测定方法,以芒柄花素含量为指标,用正交设计法对影响超声提取的因素如乙醇浓度、乙醇用量、提取次数和超声时间进行考察,优化提取工艺。结果芒柄花素在1～40μg/ml范围内线性关系良好,以峰面积(A)对浓度(C)进行线性回归,方程为A=212096C+3958.7,r2=0.9999。日内、日间相对标准差(RSD)均<5%;平均回收率均在98.0%～102.0%;优化提取条件为加15倍量75%乙醇,连续提取3次,每次20min。结论所建立的含量测定方法可用于蒙古黄芪中芒柄花素的含量测定,优化的提取工艺具有效率高和操作简便等优点。     

黄芪活性成分研究

本实验是利用溶媒提取和层析方法相结合,分离出两种化合物,它们分别是芒柄花素和毛蕊异黄酮。     

Preparation and in vivo/in vitro evaluation of formononetin phospholipid/vitamin E TPGS micelles

To enhance the formononetin (FN) antitumor effect, we developed a passive targeting FN-contained formulation. FN-contained Vitamin E d-α-tocopheryl polyethylene glycol 1000 succinate (vitamin E TPGS or TPGS)/phospholipid micelles were prepared by the solvent injection method. Particle size, polydispersity, zeta potential, encapsulation efficiency, drug release profile, and micelles morphology were evaluated and characterized by various methods including high-performance liquid chromatography, dynamic light scattering, and transmission electron microscopy. Cellular uptake of micelles was evaluated with fluorescence imaging coupled with HPLC method. Cytotoxicity of FN micelles and free FN was compared using MTT method. In vivo imaging was employed to assess the accumulation of DiR micelles and free DiR at tumor site. The antitumor effect of FN micelles was examined in tumor-bearing mice. The results showed that prepared FN micelles had an average particle diameter of 111.91?±?5.82?nm with good stability. FN micelles enhanced the cellular uptake and improved cell cytotoxicity than free FN. Furthermore, DiR micelles quickly accumulated at the tumor site than free DiR. FN micelles significantly improved tumor inhibition rate compared to that observed with free FN in tumor-bearing mice with great biosafety. Thus, FN micelles demonstrated a clear treatment advantage and provided an ideal drug administration system to improve the antitumor effect of FN.     

HPLC法测定补中益气丸中芒柄花黄素的含量

目的:建立测定补中益气丸中芒柄花黄素含量的方法。方法:采用高效液相色谱法。色谱柱为Eclipse PlusC18柱,流动相为甲醇-水(含0.2%磷酸)梯度洗脱,流速为1.0mL·min-1,检测波长为250nm,柱温为室温,进样量为20μL。结果:芒柄花黄素检测浓度在9.8×10-7～0.025g·L-1范围内与峰面积积分值呈良好的线性关系(r=0.9998);平均加样回收率为96.0%,RSD=2.2%(n=6)。结论:该方法灵敏度高、重复性好,可用于补中益气丸中芒柄花黄素含量的测定。     

刺芒柄花素对凝血酶诱导大鼠血管平滑肌细胞增殖的影响及作用机制

目的:探讨刺芒柄花素(7-羟-4'-甲氧异黄酮,FN)对凝血酶诱导血管平滑肌细胞(VSMCs)增殖的影响及其可能机制。方法:通过不同浓度FN(5、25、50μmol/L)预处理后凝血酶(1U/ml)刺激培养3～5代大鼠胸主动脉SMCs;用活细胞计数试剂盒(CCK-8)检测细胞的增殖能力;用Transwell小室法检测其迁移能力;用流式细胞仪检测其细胞周期变化;用Western blotting法检测其细胞磷酸化-细胞外信号调节激酶蛋白1/2(p-ERK1/2)的表达。结果:50μmol/LFN可明显抑制凝血酶诱导的胸主动脉SMCs增殖、迁移,促进细胞停滞于G0-G1期;下调p-ERK1/2蛋白的表达。结论:FN能有效抑制凝血酶诱导的VSMCs增殖、迁移及由G1期进入S期,其分子机制与FN抑制ERK1/2通路的活化有关。