药理学本科教学与国家题库考试初探

介绍了药理学本科教学与国家题库考试的几种作法 ,并对药理学成绩考核方法的改进作了一些尝试 ,结果表明 :使用国家题库考试平均成绩逐年提高 ,χ2 检验 ,均在正态分布范围 .     

Pharmacodynamic profile of CQP 201-403, a novel 8α-amino-ergoline

Summary The profile of action in animals of CQP 201-403, a novel 8-amino-ergoline, is in most aspects that of a very potent dopaminomimetic, both as a prolactin secretion inhibitor, and at the levels of the CNS and the cardiovascular system. Qualitatively CQP 201-403 differs slightly from bromocriptine and apomorphine in its effects on the CNS (no influence on serotonin metabolism in the rat cortex; induction of masculine mounting behavior in rats) and the cardiovascular system of the dog (reflex tachycardia in response to a blood-pressure fall). In man the new compound proved to be highly active in lowering prolactin serum levels and to be more potent than bromocriptine (Parlodel^®).In memory of Dr Annemarie Closse, who died 14 June 1987.     

Suitability of urethane anesthesia for physiopharmacological investigations in various systems Part 1: General considerations

Summary The suitability of urethane anesthesia for physiopharmacological investigations is reviewed. Total dose administered and route of administration are recognized as factors having a great influence on both resting parameters and biological responses to drugs. A peculiar characteristic of urethane is represented by its ability to induce a surgical plane of anesthesia without affecting neurotransmission in various subcortical areas and the peripheral nervous system. This makes urethane a suitable general anesthetic for studying neural function in both central and peripheral nervous systems and accounts for the preservation of a number of reflex responses in urethane-anesthetized animals.     

基于网络药理学和分子对接探讨智脑胶囊改善阿尔茨海默病的作用机制

借助网络药理学和分子对接技术,探讨智脑胶囊改善阿尔茨海默病的干预机制。通过TCMSP、TCMID等多个数据库寻找与智脑胶囊相关的化学成分及其作用靶点;利用GeneCard等数据库获取阿尔茨海默病的作用靶点;运用Venny2.1网站筛选出药物与疾病的交集靶点;使用STRING平台和Cytoscape软件进行拓扑分析得到智脑胶囊治疗阿尔茨海默病的核心作用靶点;采用Metaspace数据库对潜在核心作用靶点进行GO(gene ontology)及KEGG(Kyoto encyclopedia of genes and genomes)通路富集分析;利用AutoDock软件使用分子对接验证活性化合物与核心靶点的结合能力。结果表明：在智脑胶囊中共筛选出44个活性成分和292个有效靶点,智脑胶囊与阿尔茨海默病共同靶点58个;蛋白质-蛋白质相互作用得出关键靶点包括AKT1、IL-6、TNF等;GO分析共包含1 419条,KEGG得到175条代谢通路,主要包括脂质与动脉硬化、TNF信号通路;分子对接显示关键成分与靶点具有良好的结合能力。研究表示智脑胶囊可能通过脂质与动脉硬化和TNF信号通路等途径来减轻...     

新疆雪莲的化学成分、药理作用及其临床应用

综述新疆雪莲在化学成分、药理学及临床方面的研究．通过对其多糖、黄酮、生物碱以及黄酮苷，愈创内酯、挥发油、微量元素、氨基酸等主要成分对应的药理作用的综述，介绍其在临床上作为民族药在抗炎镇痛、抗旱孕、抗衰老及抑制癌细胞增生等方面的应用前景．     

基于网络药理学与GC-MS探讨竹叶花椒挥发油干预高脂血症的作用机制

目的 基于气相色谱-质谱联用结合网络药理学方法,探讨竹叶花椒挥发油干预高脂血症的活性成分及作用机制,为竹叶花椒挥发油中功能性成分研究及其干预高脂血症的作用机制提供理论基础。方法 首先通过GC-MS鉴定竹叶花椒挥发油的化学成分,再借助数据库获取化学成分对应靶点和高脂血症疾病靶点。又通过Venn图、蛋白-蛋白相互作用分析、GO分析、KEGG代谢通路富集分析和构建“靶点-通路-活性成分”网络得到竹叶花椒挥发油干预高脂血症的关键靶点。最后采用分子对接软件AutoDock对竹叶花椒挥发油主要活性化合物与关键靶点进行半柔性对接验证。结果 在竹叶花椒挥发油中鉴定出29个化学成分,得到37个干预高脂血症的核心靶点,该核心靶点涉及细胞对脂质的反应、脂质的定位调节和对脂多糖的反应等方面。KEGG富集分析与“靶点-通路-活性成分”网络进一步得到PPARA、RXRA、TNF、NR1H3、PPARG和IL-6等28个关键靶点,也得到金合欢醇、亚油酸和α-石竹烯等7个主要活性成分。分子对接结果表明关键靶点与主要活性成分有较好的结合能力,结合能均小于-7.0 kJ/mol。结论 竹叶花椒挥发油中的多种功能性成分可能...     

丁香属植物的化学成分及其药理作用的研究进展

从丁香属植物的化学成分及其药理作用2个方面,综述了近年来对丁香化学成分和其药理作用的研究成果.     

Molecular mechanisms in therapy of acid-related diseases

Inhibition of gastric acid secretion is the mainstay of the treatment of gastroesophageal reflux disease and peptic ulceration; therapies to inhibit acid are among the best-selling drugs worldwide. Highly effective agents targeting the histamine H2 receptor were first identified in the 1970s. These were followed by the development of irreversible inhibitors of the parietal cell hydrogen-potassium ATPase (the proton pump inhibitors) that inhibit acid secretion much more effectively. Reviewed here are the chemistry, biological targets and pharmacology of these drugs, with reference to their current and evolving clinical utilities. Future directions in the development of acid inhibitory drugs include modifications of current agents and the emergence of a novel class of agents, the acid pump antagonists. Received 30 May 2007; received after revision 15 August 2007; accepted 13 September 2007     

基于网络药理学研究厚朴-杏仁治疗哮喘的潜在作用机制

本研究采用网络药理学方法分析厚朴-杏仁配伍治疗哮喘的潜在作用机制。通过BATMAN-TCM数据库检索厚朴、杏仁的中药化学成分及靶标信息，PALM-IST数据库搜索疾病靶标信息，string数据库构建靶标的蛋白质相互作用网络，利用Cytoscape v3.5.1对药物靶标相互作用进行可视化分析，DAVID数据库和Cytoscape v3.5.1的ClueGO+CluePedia插件对药物关键靶标进行GO生物功能富集分析和KEGG信号通路富集分析。共检索到厚朴-杏仁化合物51个，靶标435个，哮喘疾病相关靶标415个，进而分析得到药物治疗疾病关键靶标14个，包括肿瘤坏死因子、过氧化氢酶、白介素13、β2肾上腺素能受体等；GO基因功能分析主要涉及应激反应调控、先天性免疫反应调控、防御反应、急性炎症反应、刺激反应、凝血止血调节、自我内稳定、活性氧代谢过程等生物过程；KEGG分析主要参与NF-κB、IL-17、FcεRI、Toll受体及FoxO等信号通路。厚朴-杏仁能通过多个靶点、多种途径、多条通路对哮喘的气道慢性炎症、气道重塑和气道高反应起潜在治疗作用。     

基于网络药理学研究参附注射液治疗脓毒症的作用机制

利用网络药理学和分子对接方法研究参附注射液治疗脓毒症的物质基础及其可能的作用机制.通过中药系统药理学数据库与分析平台和SwissTargetPrediction数据库得到参附注射液活性成分及其药物靶点,通过GeneCards、OMIM和Drugbank数据库筛选得到脓毒症相关靶点,STRING数据库和Cytoscape...