柚木的植物化学与药理学研究进展

柚木Tectona grandis 树干通直,木材纹理优美,是世界著名的速生珍贵用材树种。树体含有 甲基蒽醌、拉帕醌和脱氧拉帕醌等活性成分,可抵抗白蚁和真菌侵害。柚木树皮、叶片、心材等部位富 含萘醌、蒽醌和类异戊二烯醌等次级代谢产物,以及三萜类、类固醇、木酚素、脂肪酯和酚类等植物化 学物质。药理上,柚木被证实具有抗氧化、消炎、解热、细胞毒性、镇痛、降血糖、伤口愈合等多重功 效。文章着重介绍柚木的植物化学和药理研究方面的最新进展,以及其后续开发利用潜力。     

Molecular cloning and pharmacological characterisation of a tyramine receptor from the rice stem borer,Chilo suppressalis (Walker)

BACKGROUND: Tyramine (TA) and octopamine (OA) are considered to be the invertebrate counterparts of the vertebrate adrenergic transmitters. Because these two phenolamines are the only biogenic amines whose physiological significance is presumably restricted to invertebrates, the attention of pharmacologists has been focused on the corresponding receptors, which are believed to represent promising targets for novel insecticides. For example, the formamidine pesticides, such as chlordimeform and amitraz, have been shown to activate OA receptors. RESULTS: A full‐length cDNA (designated CsTyR1) from the rice stem borer, Chilo suppressalis (Walker), has been obtained through homology cloning in combination with rapid amplification of cDNA ends/polymerase chain reaction (RACE‐PCR). The mRNA of CsTyR1 is present in various tissues, including hemocytes, fat body, midgut, Malpighian tubules, nerve cord and epidermis, and it is found predominantly in the larval nerve cord with 16–80‐fold enrichment compared with other tissues. The authors generated a HEK 293 cell line stably expressing CsTyR1 in order to examine functional and pharmacological properties of this receptor. Both TA and OA at 0.01–100 µM can reduce forskolin‐stimulated intracellular cAMP levels in a dose‐dependent manner (TA, EC₅₀ = 369 nM ; OA, EC₅₀ = 978 nM ). In agonist assays, activation of CsTyR1 by clonidine and amitraz but not by naphazoline and chlordimeform can also significantly inhibit forskolin‐stimulated cAMP production. The inhibitory effect of TA at 10 µM is eliminated by coincubation with yohimbine, phentolamine or chlorpromazine (each 10 µM ). CONCLUSION: This study represents a comprehensive molecular and pharmacological characterisation of a tyramine receptor in the rice stem borer. Copyright © 2012 Society of Chemical Industry     

抗植物病毒剂研究进展和面临的挑战与机遇

 就抗植物病毒剂研究进展进行综述，并简要介绍病毒的危害、防治现状，文中回顾抗植物病毒剂的研究历史、抑制物种类、研究与开发的进展、现状与动向；指出抗植物病毒剂的实用化研发面临的困境与挑战，其中牵扯到多学科的相关发展与相互协作，强调药理研究在抗植物病毒剂研发中的意义，并连同其它学科和相关技术的进展给抗植物病毒剂研究所带来的机遇，最后对抗植物病毒剂的前景进行了展望。     

网络药理学方法研究石菖蒲治疗神经退行性疾病的作用机制

目的 从系统水平研究石菖蒲治疗神经退行性疾病的有效成分和作用机制。方法 采用计算机网络药理学方法,从中药系统药理学数据库中筛选石菖蒲治疗神经退行性疾病的活性成分,并构建药物-靶标-疾病网络。结果 通过网络药理学方法筛选出石菖蒲活性成分20种,显示该中药化学成分和作用靶点与阿尔茨海默病、抑郁症和帕金森综合征等神经退行性疾病之间存在一定的联系。结论 通过网络药理学方法构建的石菖蒲网络可以将该中药化学成分的聚类、差异以及有效成分与相关靶标及疾病的复杂分子作用机制可视化。     

高职农业院校《动物药理学》课程的建设与教学实践

从课程建设、教学内容和方法改革、实验教学模式创新、教师队伍培养等方面介绍了《动物药理学》课程的教学改革实践。以期为《动物药理学》课程的改革与建设提供参考。     

基于网络药理学黄精抗炎活性成分及作用机制研究

黄精属百合科黄精属，性味甘甜，食用爽口，具有重要的药用和食用价值。为探讨黄精抗炎可能活性成分及作用机制，借助TCMSP数据库筛选黄精活性成分，利用Pharmmapper和Uniprot数据库查找黄精活性成分靶点基因，借助GeneCards和MalaCards数据库筛选人体炎症相关基因，取交集获取黄精抗炎潜在靶点；在Metascape数据库进行GO富集和KEGG通路注释；使用Cytoscape3.6.1软件构建黄精抗炎潜在靶点的“成分-靶点-通路”网络图，STRING数据库构建PPI网络图。共筛选出(+)-丁香树脂醇-O-β-D-葡萄糖苷、中华在线1、甲基原纤细薯蓣皂苷、西伯利亚蓼苷A、3’-甲氧基大豆苷元、β-谷甾醇等12个潜在活性成分和ALB、EGFR、MAPK1、CASP3、ESR1等65个黄精抗炎潜在靶标，生物信息学富集分析中筛选出46个GO条目和13条KEGG通路，主要涉及Pathways in cancer（癌症的途径）、Prostate cancer（前列腺癌）、IL-17 signaling pathway（IL-17信号通路）、Hepatitis B（乙型肝炎）通路。该研究揭示了黄精抗炎多成分、多靶点、多通路的作用机制，为黄精抗炎机制研究和后续试验研究提供依据。