中药生物碱的提取及抗炎作用研究

为探讨自拟中药复方"宫炎净"总生物碱、简化复方总生物碱以及益母草生物碱对小鼠的抗炎作用,将实验小鼠分为生理盐水、地塞米松、复方"宫炎净"总生物碱、简化复方总生物碱以及益母草生物碱组,依据建立小鼠耳廓肿胀、腹腔毛细血管通透性、足趾肿胀以及肉芽肿炎症模型来评估各组药物的抗炎效果。结果表明,复方"宫炎净"总生物碱组与简化复方总生物碱能够显著抑制二甲苯所致小鼠耳廓肿胀率、降低小鼠腹腔毛细血管通透性、抑制蛋清所致小鼠足趾肿胀率、降低棉球所致小鼠肉芽组织增生,均与益母草生物碱组差异显著(P0.05),并与地塞米松组差异不显著(P0.05)。结果显示,复方"宫炎净"总生物碱组与简化复方总生物碱抗炎效果相差不大,简化复方可作为临床用药组方使用。     

On the Chemistry,Toxicology and Genetics of the Cyanobacterial Toxins,Microcystin, Nodularin,Saxitoxin and Cylindrospermopsin

The cyanobacteria or “blue-green algae”, as they are commonly termed, comprise a diverse group of oxygenic photosynthetic bacteria that inhabit a wide range of aquatic and terrestrial environments, and display incredible morphological diversity. Many aquatic, bloom-forming species of cyanobacteria are capable of producing biologically active secondary metabolites, which are highly toxic to humans and other animals. From a toxicological viewpoint, the cyanotoxins span four major classes: the neurotoxins, hepatotoxins, cytotoxins, and dermatoxins (irritant toxins). However, structurally they are quite diverse. Over the past decade, the biosynthesis pathways of the four major cyanotoxins: microcystin, nodularin, saxitoxin and cylindrospermopsin, have been genetically and biochemically elucidated. This review provides an overview of these biosynthesis pathways and additionally summarizes the chemistry and toxicology of these remarkable secondary metabolites.     

板蓝根生物碱抗猪细小病病毒的作用

摘 要:【目的】探讨板蓝根水溶性生物碱和脂溶性生物碱对猪细小病毒的体外抑制作用。【方法】采用醇提法从板蓝根中提取了水溶性生物碱和脂溶性生物碱,并测定其对PK-15细胞的最大无毒浓度（TD50）,应用先加药后接种病毒、先接种病毒后加药、病毒和药物体外作用2h后再同时加入细胞单层三种加药方式测定了生物碱的体外抗PPV效果。【结果】板蓝根水溶性生物碱的TD0为62.5μg /ml,板蓝根脂溶性生物碱的TD0为50μg /ml.板蓝根水溶性生物碱对PPV的最小阻断浓度、最小抑制浓度和直接杀灭浓度分别为7.81μg /ml、15.62μg /ml、7.81μg /ml。板蓝根脂溶性生物碱对PPV的最小阻断浓度、最小抑制浓度和直接杀灭浓度分别为0.78μg /ml、12.5μg /ml、0.78μg /ml。板蓝根混合生物碱对PPV的最小阻断浓度、最小抑制浓度和直接杀灭浓度分别为0.78μg /m、12.5μg /ml、0.78μg /ml。【结论】板蓝根脂溶性生物碱的抗病毒作用强于板蓝根水溶性生物碱,板蓝根混合生物碱的抗病毒作用比两种生物碱单独使用效果要好。     

New Antimicrobial Bromotyrosine Analogues from the Sponge Pseudoceratina purpurea and Its Predator Tylodina corticalis

Bioassay-guided fractionation of extracts from temperate Australian collections of the marine sponge Pseudoceratina purpurea resulted in the isolation and characterisation of two new and six known bromotyrosine-derived alkaloids with antibiotic activity. Surprisingly, a single specimen of the mollusc Tylodina corticalis, which was collected while feeding on P. purpurea, contained only a few of the compounds found in the sponge suggesting selective accumulation and chemical modification of sponge metabolites.     

烟草生物碱对菜青虫的生物活性研究

用醇萃取法提取烟草中的杀虫物质烟草生物碱,对菜青虫进行拒食、毒杀和生长抑制试验。结果表明:烟草生物碱对菜青虫3龄幼虫具有强烈的拒食作用和生长抑制作用,     

烤烟叶片性状与生物碱含量及感官质量的关系研究

2009年以烤烟主栽品种‘NC89’为试验材料,研究中上部叶片性状间的相关性、叶长、单叶重的感官评吸质量及其与生物碱含量的关系。研究结果表明,除中部叶质重与叶长呈负相关外其他中上部叶片性状均与叶长呈正相关。中上部叶长适宜范围分别为56~68 cm、53~65 cm,且叶长每增加3 cm烟碱含量分别增加2.80 mg/g、1.67 mg/g;中部叶单叶重在8~16 g范围内平均每增加2 g烟碱含量增加2.2 mg/g;上部叶单叶重在9~21 g范围内平均每增加3 g烟碱含量增加1.60 mg/g。降烟碱、假木贼碱、新烟草碱与烟碱的变化趋势一致且中上部烟叶的生物碱含量随叶片长度、单叶重的变化趋势一致。中、上部叶片长度分别在53.01~68.99 cm、59.01~65.99 cm,单叶重分别在14.001~16.999 g、15.001~18.999 g范围内感官质量较好。     

Isoquinoline Alkaloids as Protein Tyrosine Phosphatase Inhibitors from a Deep-Sea-Derived Fungus Aspergillus puniceus

Puniceusines A–N (1–14), 14 new isoquinoline alkaloids, were isolated from the extracts of a deep-sea-derived fungus, Aspergillus puniceus SCSIO z021. Their structures were elucidated by spectroscopic analyses. The absolute configuration of 9 was determined by ECD calculations, and the structures of 6 and 12 were further confirmed by a single-crystal X-ray diffraction analysis. Compounds 3–5 and 8–13 unprecedentedly contained an isoquinolinyl, a polysubstituted benzyl or a pyronyl at position C-7 of isoquinoline nucleus. Compounds 3 and 4 showed selective inhibitory activity against protein tyrosine phosphatase CD45 with IC₅₀ values of 8.4 and 5.6 µM, respectively, 4 also had a moderate cytotoxicity towards human lung adenocarcinoma cell line H1975 with an IC₅₀ value of 11.0 µM, and 14, which contained an active center, -C=N⁺, exhibited antibacterial activity. An analysis of the relationship between the structures, enzyme inhibitory activity and cytotoxicity of 1–14 revealed that the substituents at C-7 of the isoquinoline nucleus could greatly affect their bioactivity.     

美丽蛇根草正丁醇部生物碱成分研究

采用柱色谱技术进行分离纯化,利用薄层色谱法及波谱方法分别鉴定药用植物美丽蛇根草Ophiorrhiza rosea Hook全草甲醇提取物正丁醇萃取部分化合物结构,研究美丽蛇根草的生物碱成分。结果表明：从美丽蛇根草中共得到4个吲哚生物碱化合物,分别鉴定为Harman(1)、Strictosidinic acid(2)、5-Carbomethoxylyaloside(3)、Lyalosidic acid(4);化合物2～4为首次从该种植物中分离得到。     

披针叶黄华的研究进展

披针叶黄华(Thermopsis lanceolate)别名“牧马豆”,是豆科野决明属植物,广泛分布于内蒙古、甘肃、宁夏、青海等省区.牧马豆是有毒植物,可引起牲畜中毒,但也是药用植物,具有兴奋呼吸、抗辐射及祛痰止咳等功效.采用醇类溶剂提取法和硅胶柱层析技术从披针叶黄华总生物碱中提取、分离,得到了3个单体和6段生物碱混合物.单体经红外光谱鉴定为金雀花碱、黄华碱和臭豆碱等.该类生物碱多具有抗癌、抗心率失调、抗微生物等作用.     

植物ABC转运蛋白与次生代谢产物的跨膜转运

ABC（ATP-Binding Cassette）转运蛋白是目前已知最大、功能最广泛的蛋白家族，参与生物体内多种物质的转运，因其在生物体内与肿瘤细胞耐药性等一些重要的生理过程密切相关而引起了人们的广泛关注。研究发现，在已完成全基因组测序的生物中，ABC转运蛋白在拟南芥和水稻中数量最多，推测与植物次生代谢产物的跨膜转运相关。植物产生生物碱、萜类化合物、酚类等大量次生代谢产物，保护植物体免受环境中生物和非生物胁迫的损伤。这些化合物的累积和排泌被高度调节，ABC转运蛋白在其中起着重要的作用。本综述介绍了植物ABC转运蛋白及其在植物次生代谢产物累积和跨膜转运中的研究进展。