莲子心中酚性生物碱3种主要成分定量分析及其特征图谱研究

目的:建立同时测定莲子心中酚性生物碱:莲心碱、异莲心碱、甲基莲心碱含量的RP-HPLC法以及酚性生物碱的特征图谱.方法:采用RP-HPLC法,流动相为乙腈-水-三乙胺(25∶75∶0.1,用磷酸调pH3.3),紫外检测波长282 nm,流速0.8 mL·min-1,进样量20 μL.结果:莲心碱、异莲心碱、甲基莲心碱线性方程显示线性关系良好.特征图谱研究确定了酚性生物碱16个共有峰.结论:本方法简便、准确,重现性好,专属性强,可为莲子心中生物碱类物质标准提取物质量控制提供参考.     

杂交贝母生物碱成分的研究

目的 :对杂交贝母进行化学成分研究。方法 :采用IR ,¹H NMR ,¹³ C-NMR ,2D-NMR ,MS及与对照品和文献对照等方法鉴定结构。结果 :分离并鉴定了 7个化合物 :湖贝乙素 (hupehenirine ,ZF1) ;湖贝嗪 (hupehenizine ,ZF2 ) ;浙贝乙素 (peiminine ,verticinone ,ZF3) ;湖贝甲素 (hupehenine ,ZF4 )、异浙贝甲素 (isoverticinone ,ZF5 )、浙贝甲素(peimine ,verticine ,ZF6 )、湖贝甲素苷 (hupeheninoside,ZF7) ;结论 :化合物 1～ 7均为首次从杂交贝母中得到。     

蝙蝠葛酚性碱对实验性心肌缺血血流动力学的影响

目的: 观察蝙蝠葛酚性碱对实验性心肌缺血血流动力学的影响.方法: 结扎大鼠左冠状动脉前降支制备急性心肌缺血模型. 结果: 蝙蝠葛酚性碱可显著抑制心肌缺血所致LVEDP的升高和MBP、 dp/dtmax、-dp/dtmax、CO的降低.结论: 蝙蝠葛酚性碱能改善心肌缺血时血流动力学的紊乱,提示蝙蝠葛酚性碱对心肌缺血具有保护作用.     

Four new C19-diterpenoid alkaloids from Aconitum hemsleyanum var. circinatum

Four new C19-diterpenoid alkaloids, hemaconitines A–D (1–4), were isolated from the roots of Aconitum hemsleyanum var. circinatum. Their structures were elucidated as 19R-hydroxyl-secoyunnaconitine (1), (3R)-hydroxyl-liwaconitine (2), 14-anisoyl-leucanthumsine E (3), and 19R -acetonyl-8-O-methyltalatisamine (4) by extensive spectroscopic analysis (IR, UV, HR-ESI-MS, 1D, and 2D NMR).     

基于UHPLC-QE-MS分析结合网络药理学探讨小叶黄杨生物碱治疗阿尔茨海默病的作用机制

目的 鉴定小叶黄杨中生物碱类化学成分，探讨治疗阿尔茨海默病的物质基础和作用机制。方法 表征小叶黄杨生物碱成分，并利用PubChem、SwissADME、Swiss Target Prediction、Genecards和OMIM等数据库获取小叶黄杨生物碱的活性成分和对应靶点，以及阿尔茨海默病的相关靶点；运用Cytoscape3.9.0软件绘制“成分-靶点”网络图；运用String平台构建蛋白互作网络图；运用微生信在线绘图工具进行通路富集分析可视化；用AutodockTools-1.5.6软件对筛选出的核心成分做分子对接。结果 鉴定小叶黄杨生物碱成分23个，筛选有效成分19个，对应靶点216个；筛选阿尔茨海默病靶点880个，药物-疾病交集靶点49个；GO富集分析主要相关的生物过程有化学性突触传递，顺行跨突触信号，跨突触信号等；KEGG通路富集分析中神经活性配体-受体相互作用，5-羟色胺能突触，cAMP信号等为主要信号通路。分子对接显示筛选的核心靶点和核心成分均有较强结合力。结论 本研究初步证明了小叶黄杨生物碱成分可以多成分、多靶点、多通路共同作用治疗阿尔茨海默病，为进一步深入研究小叶黄杨生物碱对阿尔茨海默病作用的物质基础以及作用机制提供参考。     

Drug target interaction of tubulin-binding drugs in cancer therapy

Microtubules and their component protein, tubulin, constitute a popular target for the treatment of cancer. Many drugs that are presently used in clinics or in clinical trials and drugs that show promise as anticancer drugs bind to tubulin and microtubules. There are three conventional binding sites on β-tubulin where many of these drugs bind. The binding properties, conformational changes upon binding, association constants and thermodynamic parameters for the drug–tubulin interaction on these three sites are discussed. The antiproliferative activities of these drugs and the possible correlation with the binding properties are also described.     

正交试验法综合优选附子高压炮制工艺

目的：优选附子高压蒸制的最佳工艺。方法：以其含生物碱的含量和传统外观质量为综合指标，采用L9(34)正交试验法，对高压蒸制时间、压力及软化方式三个因素进行考察。结果：附子最佳高压蒸制工艺为：A1B3C3，即附子经换水浸透法处理后，0.15Mpa压力下蒸制90min，即得。结论：该方法简便易行可控，可作为代替附子传统炮制工艺的新方法。     

Zizyphus xylopyrus (Retz.) Willd: a review of its folkloric,phytochemical and pharmacological perspectives

Zizyphus xylopyrus (Retz.) Willd (Rhamnaceae) is an ever-green shrub of tremendous medicinal importance, distributed throughout the North-Western India, Pakistan, and China. Various parts of plant are used in Ayurvedic and other folk medicine for the treatment of different ailments such as obesity, diabetes, snake bite, fever, diarrhoea, insomnia and digestive disorders. The plant also possesses antisteroidogenic, anticonvulsent, antinociceptive, antiinflammatory, antidepressant, antidiarroheal and wound healing activity. Research has been carried out using different techniques to support most of these claims. This review is an attempt to compile an up-to-date on its folkloric or traditional uses, phytochemical as well as pharmacological properties of Zizyphus xylopyrus.     

A rapid and simple method for the determination of psychoactive alkaloids by CE‐UV: application to Peganum Harmala seed infusions

The β‐carboline alkaloids of the harmala (HAlks) group are compounds widely spread in many natural sources, but found at relatively high levels in some specific plants like Peganum harmala (Syrian rue ) or Banisteriopsis caapi . HAlks are a reversible Mono Amino Oxidase type A Inhibitor (MAOI) and, as a consequence, these plants or their extracts can be used to produce psychotropic effects when are combined with psychotropic drugs based on amino groups. Since the occurrence and the levels of the HAlks in natural sources are subject to significant variability, more widespread use is not clinical but recreational or ritual, for example B . caapi is a known part of the Ayahuasca ritual mixture. The lack of simple methods to control the variable levels of these compounds in natural sources restricts the possibilities to dose in strict quantities and, as a consequence, limits its use with pharmacological or clinical purposes. In this work, we present a fast, simple, and robust method of quantifying simultaneously the six HAlks more frequently found in plants, i.e., harmine, harmaline, harmol, harmalol, harmane, and norharmane, by capillary electrophoresis instruments equipped with the more common detector UV. The method is applied to analyze these HAlks in P . Harmala seeds infusion which is a frequent intake form for these HAlks. The method is validated in three different instruments in order to evaluate the transferability and to compare the performances between them. In this case, harmaline, harmine, and harmol were found in the infusion samples. Copyright © 2016 John Wiley & Sons, Ltd.     

Simultaneous Determination of Six Quaternary Ammonium Alkaloids in Coptidis Rhizoma by UPLC

Objective To establish a new, rapid, and reliable reversed-phase ultra performance liquid chromatography (RP-UPLC) method for the simultaneous determination of six quaternary ammonium alkaloids (QAAs) in Coptidis Rhizoma. Methods The effect of different experimental parameters on the analysis of QAAs by RP-UPLC was evaluated. Results Optimal resolution was achieved with an Acquity UPLC BEH C18 column using a gradient elution profile and a mobile phase consisting of water spiked with 10 mmol/L ammonium bicarbonate (A, pH adjusted to 10.0 by ammonia water) and acetonitrile (B), at a flow rate of 0.30 mL/min and wavelength of 345 nm. The column temperature was set at 30 ℃. The proposed method was found to be reproducible, precise, and rapid according to the method validation. Conclusion The proposed method, which is compatible with MS analysis and the preparation of QAA, provides some helpful insights into the quality control of Coptidis Rhizoma.