超声-表面活性剂法提取黄柏生物碱工艺研究

目的:研究超声-表面活性刺法在黄柏生物碱提取工艺中的应用.方法:采用单因素实验和正交实验考察不同因素对超声-表面活性剂法提取生物碱的影响,优化最佳工艺参数.结果:最佳提取工艺为提取温度60℃,乙醇浓度80%,活性荆TW60,料液比为30:1,超声30 min,提取率达到7.24%,高于文献值6.37%.结论:超声-表面活性剂对黄柏生物碱的提取,具有提取率高、快速、有效等优点.     

黄连总生物碱对糖尿病模型大鼠血管内皮功能的保护作用

目的观察黄连总生物碱对糖尿病模型大鼠血管内皮功能的保护作用。方法链脲佐菌素一次性腹腔注射复制糖尿病大鼠模型。黄连总生物碱高、中、低剂量及格列齐特分别灌胃,正常组和模型组给予等量生理盐水,每日1次,连续8周。实验结束后,分光光度法测定血清中一氧化氮（NO）、丙二醛（MDA）、超氧化物歧化酶（SOD）含量;放射免疫法测定血浆中内皮素（ET）-1、细胞间黏附分子（ICAM）-1的含量;HE染色法观察主动脉病理学改变。结果黄连总生物碱各剂量组不仅能显著降低糖尿病大鼠MDA、ET-1、ICAM-1水平,减轻主动脉病理损伤程度,还能升高NO、SOD水平。结论黄连总生物碱对糖尿病大鼠血管内皮功能具有一定的保护作用。     

莲子心总生物碱的毒性试验研究

摘要 目的： 探讨莲子心总生物碱的毒副作用,以对莲子心总生物碱作出安全性评价。方法 ：小鼠急性毒性试验中一次性给予最大灌胃量5000mg/kg莲子心总生物碱,观察小鼠中毒症状。长期口服毒性实验,Sprague-Dawley(SD)大鼠随机分为四组,分别按照400mg/kg?d、200 mg/kg?d、100 mg/kg?d的剂量给予SD大鼠灌胃实验室自制莲子心总生物碱,对照组给予等量体积0.3%羧甲基纤维素钠,连续服用30天。结果 ：在急性毒性试验中给予5000mg/kg莲子心总生物碱对小鼠不产生毒性作用。在长期毒性试验中,除不同剂量给药组SD大鼠血清尿素氮与对照组具有显著性差异(P<0.05),高、中剂量组SD大鼠血糖含量与对照组有明显差异(P<0.05)外余下指标与对照组相比均无明显差异。高、中、低剂量组大鼠肝组织病理切片与对照组相比均明显异常,表现为肝小叶结构正常。结论 ： 莲子心总生物碱对小鼠最大耐受剂量为5000mg/kg,同时灌胃给药400mg/kg/天莲子心总生物碱对大鼠无毒副作用。     

Ergot Alkaloids Produced by Endophytic Fungi of the Genus Epichlo?

The development of fungal endophytes of the genus Epichloë in grasses results in the production of different groups of alkaloids, whose mechanism and biological spectrum of toxicity can differ considerably. Ergot alkaloids, when present in endophyte-infected tall fescue, are responsible for “fescue toxicosis” in livestock, whereas indole-diterpene alkaloids, when present in endophyte-infected ryegrass, are responsible for “ryegrass staggers”. In contrast, peramine and loline alkaloids are deterrent and/or toxic to insects. Other toxic effects in livestock associated with the consumption of endophyte-infected grass that contain ergot alkaloids include the “sleepy grass” and “drunken horse grass” diseases. Although ergovaline is the main ergopeptine alkaloid produced in endophyte-infected tall fescue and is recognized as responsible for fescue toxicosis, a number of questions still exist concerning the profile of alkaloid production in tall fescue and the worldwide distribution of tall fescue toxicosis. The purpose of this review is to present ergot alkaloids produced in endophyte-infected grass, the factors of variation of their level in plants, and the diseases observed in the mammalian species as relate to the profiles of alkaloid production. In the final section, interactions between ergot alkaloids and drug-metabolizing enzymes are presented as mechanisms that could contribute to toxicity.     

Diversification of Ergot Alkaloids in Natural and Modified Fungi

Several fungi in two different families––the Clavicipitaceae and the Trichocomaceae––produce different profiles of ergot alkaloids, many of which are important in agriculture and medicine. All ergot alkaloid producers share early steps before their pathways diverge to produce different end products. EasA, an oxidoreductase of the old yellow enzyme class, has alternate activities in different fungi resulting in branching of the pathway. Enzymes beyond the branch point differ among lineages. In the Clavicipitaceae, diversity is generated by the presence or absence and activities of lysergyl peptide synthetases, which interact to make lysergic acid amides and ergopeptines. The range of ergopeptines in a fungus may be controlled by the presence of multiple peptide synthetases as well as by the specificity of individual peptide synthetase domains. In the Trichocomaceae, diversity is generated by the presence or absence of the prenyl transferase encoded by easL (also called fgaPT1). Moreover, relaxed specificity of EasL appears to contribute to ergot alkaloid diversification. The profile of ergot alkaloids observed within a fungus also is affected by a delayed flux of intermediates through the pathway, which results in an accumulation of intermediates or early pathway byproducts to concentrations comparable to that of the pathway end product.     

阳离子交换树脂酸水洗脱法纯化苦参总碱的工艺优选

目的优选阳离子交换树脂不同浓度盐酸溶液洗脱纯化苦参总碱的最佳工艺条件。方法以苦参碱、氧化苦参碱和总生物碱的洗脱率为考察指标,以盐酸溶液作为洗脱剂,优选阳离子交换树脂纯化苦参总碱的最佳工艺和参数条件。结果苦参总碱阳离子交换树脂纯化洗脱条件为:以5%盐酸溶液作为洗脱剂,以6 BV.h-1的流速洗脱,苦参碱和氧化苦参碱、苦参总碱洗脱率均可达85%。结论采用阳离子交换树脂酸水洗脱法纯化苦参总碱效率高,工艺简便,可用于苦参总碱的提取纯化。     

植物来源的生物碱类乙酰胆碱酯酶抑制剂研究进展

乙酰胆碱酯酶抑制剂是阿尔茨海默病治疗药物的研究热点。根据类胆碱学说,乙酰胆碱酯酶抑制剂可提高脑部神经递质乙酰胆碱的水平从而改善阿尔茨海默病患者的胆碱功能,并缓解神经性紊乱的症状。植物天然产物是乙酰胆碱酯酶抑制剂先导化合物的重要来源,其中生物碱为此类天然产物的重要组成部分。综述植物来源且具有抗乙酰胆碱酯酶活性生物碱的结构类型、作用机制及其构效关系。     

苦豆子种子生物碱类化学成分及细胞毒活性

目的:研究苦豆子种子的化学成分并对其抗肿瘤活性进行测试。方法:采用常规的硅胶柱层析(CC),葡聚糖(Sephadex LH-20)柱层析,和重结晶等实验手段对其进行了分离纯化,利用波谱技术(1H-NMR,13C-NMR)及与文献数据对照,对分离的化合物进行了结构鉴定;并采用MTT测定部分生物碱单体化合物体外对C6肿瘤细胞的细胞毒活性。结果:共分离出7个生物碱类化合物,分别鉴定为:苦参碱(1),氧化苦参碱(2),槐果碱(3),9α-羟基槐果碱(4),氧化槐果碱(5),9α-羟基槐胺碱(6),(-)-13,14-去氢槐定碱(7),1个非生物碱化合物3-吲哚甲醛(8)。结论:化合物8为首次从该属植物中分离得到。细胞毒活性测试结果表明,化合物1~3和5对鼠脑胶质瘤C6细胞显示了较强的生长抑制活性。     

黄连上清丸(片)中小檗型生物碱的含量测定

目的:分离并测定黄连上清丸(片)(黄连,栀子,连翘,黄柏等)中的小檗碱型生物碱的含量.方法:采用反向高效液相法,以乙腈-3.4 g·L-1KH3PO4溶液(磷酸调pH为3.0)(40:60),内含SDS1.7 g·L-1为流动相,345 nm检测.结果:在上述条件下,测定了10个厂家黄连上清丸(片)中小檗型生物碱(小檗碱、巴马汀、黄连碱、表小檗碱、药根碱)的含量.结论:本方法操作简便、结果准确、回收率高、重现性好,可用于该制剂的质量控制.     

延胡索中季铵生物碱的高分辨基质辅助激光解吸电离质谱研究

目的：研究中药中季铵生物碱的基质辅助激光解吸电离质谱行为。方法：以延胡索为例，采用2，5-二羟基苯甲酸为基质，以样品和基质混合均匀点样，直接分析中药生物碱提取物；利用高分辨质谱数据确定生物碱化合物的元素组成。结果：从延胡索中检出并鉴定了去氢紫堇碱等5种季铵生物碱。结论：基质辅助激光解吸电离质谱为中药中季铵生物碱提供了一种快速分析方法。