感冒一小时胶囊中总香豆素、总黄酮、总生物碱三类成分的指纹图谱研究

目的:建立感冒一小时胶囊(羌活、独活、粉葛、黄芩、黄连等)中总香豆素、总黄酮和总生物碱的特征指纹图谱。方法:运用HPLC-DAD方法,色谱柱为Hypersil C18(4.6 mm×150 mm,5μm),流动相A为乙腈,分离香豆素类成分时流动相B为水,分离黄酮类成分时流动相B为0.1%磷酸水溶液,分离生物碱类成分时流动相B为0.05 mol/L磷酸二氢钾缓冲液(含0.3%三乙胺,磷酸调pH 3.0),梯度洗脱;检测波长分别为318 nm、277 nm和347 nm。结果:香豆素类成分特征指纹图谱中含有38个共有峰,主要成分为蛇床子素和异欧前胡素,约占总峰面积的30%,其中蛇床子素为18%,异欧前胡素为12%;黄酮类成分特征指纹图谱中含有17个共有峰,主要成分为黄芩苷,约占总峰面积的37%;生物碱类成分特征指纹图谱中含有26个共有峰,主要成分为盐酸小檗碱,约占总峰面积的46%。结论:建立的三类成分色谱指纹图谱特征性和专属性较强,可用于感冒一小时胶囊的质量控制。     

黄连总生物碱对实验性糖尿病肾病大鼠肾功能保护作用的研究

目的 观察黄连总生物碱对实验性糖尿病肾病大鼠肾功能的保护作用.方法 雄性SD大鼠30只,随机分为5组,每组6只.一组作为正常对照组,其余4组分别以高糖高脂饮食加单肾切除、腹腔内注射链脲佐菌素建立糖尿病肾病模型.造模后其中3组分别给予高中低剂量黄连总生物碱,另一组为模型对照组.各模型组及对照组每4周,测1次血糖及尿微量白蛋白.造模后12周,心脏取血,测肌酐、尿素、糖化血红蛋白等.结果 模型组血糖、血尿素氮、血肌酐均显著高于正常对照组,P＜0.05,尿肌酐、肾小球滤过率均低于正常对照组,P＜0.05.尿微量白蛋白值升高.黄连总生物碱干预组大鼠血糖显著降低,肾功能显著改善,其中中剂量组降糖及肾功能改善效果最为显著.结论 黄连总生物碱对糖尿病肾病大鼠有保护其肾功能,并延缓肾功衰竭过程的作用.     

闽产代代果中化学成分的分离分析

采用薄层色谱法对闽产代代果中主要化学成分进行初步的分离、分析、鉴定,结果:代代果中生物碱类成分以正丁醇-冰醋酸-水(4∶1∶5上层)为展开剂,黄酮类以A醋酸乙酯-甲醇-水(100∶17∶13)和B二甲苯-醋酸乙酯-甲酸-水(20∶10∶1∶1)为展开剂,挥发油类以石油醚-醋酸乙酯(10∶1)为展开剂,各类主要化学成分均获得良好的分离,说明薄层色谱鉴别方法可作为闽产代代的质量控制方法之一.     

氮、磷、钾对益母草生长及水苏碱和总生物碱影响的研究

目的研究氮、磷、钾肥对益母草生长发育及次生代谢物的影响。方法采用大田试验与室内分析相结合的方法。结果益母草各项生长、产量及水苏碱和总生物碱的量基本均为复肥型高于单肥型，复肥型中又以营养平衡型大于营养失调型，但单施氮肥对以上各项指标均有很大促进作用。在复肥型中，足量磷元素与氮元素的合理配施可以提高氮的肥效。结论以益母草株高、叶片数、分蘖数、产量及水苏碱和总生物碱的量为评价标准，根据氮、磷、钾二次肥料数学模型的计算结果，确定最佳施肥量为：N：37．5～44．0g／m^2，P：37．4～54．3g／m^2，K：31．6～34．4g／m^2，氮、磷、钾的最佳配比为4：4．5：3．3。     

In vitro antimalarial activity,chloroquine potentiating effect and cytotoxicity of alkaloids of Hernandia voyronii Jum. (Hernandiaceae)

Hernandia voyronii is traditionally used as adjuvant to chloroquine in Madagascar. Neutral and basic alkaloidal extracts of this plant were evaluated for their intrinsic in vitro antimalarial activity, cytotoxicity and chloroquine potentiating action against the chloroquine resistant Plasmodium falciparum strain FCM29. Bioassay directed fractionation clearly demonstrated that both the intrinsic antimalarial activity and the chloroquine potentiating action was localized in the polar alkaloidal extract. Moreover, this extract had low cytotoxicity to HeLa cells and L929 fibroblasts. These results support the traditional use of H. voyronii as an antimalarial and adjuvant to chloroquine.     

正交设计法优选草乌炮制工艺

用正交设计,以草乌炮制前后总生物碱和酯型碱含量变化为指标,研究草乌炮制工艺。试验数据经用多指标试验公式评分法处理,选择出草乌的最佳炮制工艺为水浸润透,切厚片,加压(127℃,0.15MPa)蒸3h。     

Tetrandrine and related bis—benzylisoquinoline alkaloids from medicinal herbs：cardiovascular effects and mechanisms of action

Tetrandrine(TET),a bis-benzylisoquinoline alkaloid purified and identified an active ingredient in a Chinese medicinal herb,Radix Stephanae tetrandrae,has been used traditionally for the treatment of congestive circulatory disorder and inflammatory diseases.TET,together with a few of its structural analogues,has long been demonstrated to have antihypertensive action in clinical as well as animal studies.Presumably,the primary anti-hypertensive action of TET is due to its vasodilatory properties.TET prevents or inhibits vascular contraction induced by membrane depolarization with KCl or α-adrenoceptor activation with phenylephrine (PE).TET(30μmol/L) also inhibits the release of endothelium-derived nitric oxide(NO) as well as NO production by inducible NO synthase.TET apparently inhibits multiple Ca^2 entry pathways as demonstrated in cell types lacking the L-type Ca^2 channels.In cardiac muscle cells,TET inhibits both L-and T-type Ca^2 channels.In addition to its actions on cardiovascular tissues,TET may also exert its anti-hypertensive action via a Ca^2 -dependent manner on other tissues intimately involved in the modulation of blood pressure control,such as adrenal grands.In adrenal glomerulosa cells,KCl-or angiotensin II-induced aldosterone synthesis is highly dependent on extracellular Ca^2 .Steroidogenesis and Ca^2 -influx in bovine adrenal glomerulosa cells have been shown to be potently inhibited by TET.In bovine adrenal chromaffin cells,TET inhibits Ca^2 currents via L-and N-type channels as well as other unidentified channels with IC50 of 10μmol/L.Other than the Ca^2 antagonistic effects.TET also interacts with the α-adrenergic receptors and muscarinic receptors based on functional as well as radioligand binding studies.Apart from its functional effects,TET and related compounds also exert effects on tissue structures,such as remodelling of hypertrophied heart and inhibition of angiogenesis,probably by causing apoptotic responses.TET is also known for its anti-inflammatory and anti-fibrogenic actions,which make TET and related compound potentially useful in the treatment of lung silicosis,liver cirrhosis,and rheumatoid arthritis.     

Immunomodulatory effects and mechanisms of plant alkaloid tetrandrine in autoimmune diseases

Autoimmune diseases characterized by activation of immune effector cells and damage of target organs are currently treated with a combination of several disease-modifying antirheumatic drugs (DMARDs) that preserve different immunomodulatory mechanisms. Such a combination treatment strategy not only provides synergistic effects but also reduces side effects from individual drug. Tetrandrine (Tet), purified from a creeper Stephania tetrandra S Moore, is a bis-benzylisoquinoline alkaloid and has been used to treat patients with silicosis, autoim-mune disorders, and hypertension in Mainland China for decades. The accumulated studies both in vitro and in vivo reveal that Tet preserves a wide variety of immunosuppressive effects. Importantly, the Tet-mediated immu-nosuppressive mechanisms are evidently different from some known DMARDs. The synergistic effects have also been demonstrated between Tet and other DMARDs like FK506 and cyclosporin. These results highlight Tet a very potential candidate to be consid     

风湿定胶囊的质量标准研究

目的建立风湿定胶囊的质量标准。方法用中和法检测了总生物碱的限量;HPLC测定了欧前胡素的含量,色谱柱:A lltech ODS(4.0mm×250mm),流动相:甲醇-水(70∶30),检测波长248nm,结果加样回收97.74%,RSD=2.92%。线性范围为0.01564mg/mL~0.1564mg/mL,r=0.999 7,重复性RSD=1.83%(n=5),精密度RSD=0.77%(n=5)。结论方法稳定、可靠,可作为该药的质量控制方法。     

Physicochemical quality evaluation of natural compounds isolated from crude drugs

Aconite root has high toxicity caused by diester alkaloids, thus it was necessary to define the limiting value of diester alkaloids used in medicine formulation. To give the quality of “Processed Aconite Root” and “Powdered Processed Aconite Root” in the Japanese Pharmacopoeia (14th edn, supplement II), we established the official specification and evaluation methods of standard substances. High qualitative grade diester alkaloids, aconitine, hypaconitine, jesaconitine and mesaconitine, which were useful to evaluate the purity of processed aconite root and powdered processed aconite root, were prepared and evaluated for their stability. We studied the physicochemical specification and evaluation methods of these alkaloids. In addition, an “Aconitum diester alkaloids standard solution for purity”, which was used for the purity test, was prepared, and we also studied its physicochemical specification and evaluation methods. In addition, to evaluate the quality of processed aconite root and powdered processed aconite root, a TLC identification test was established. A monoester alkaloid of benzoylmesaconine hydrochloride was used as the reference standard in the latter test, and we also investigated its physicochemical specification and evaluation methods.