海南萝芙木季胺碱——大斯配加春的结构

从海南萝芙木生产“降压灵”的母液中,分得一新的二聚体生物碱,命名为大斯配加春(macrospegatrine)。根据红外、紫外、质谱、氢谱及单晶X—射线衍射确定结构为Ⅰ式(图1)。     

甘肃棘豆生物碱部位体内抗肿瘤作用及对免疫功能的影响

目的 研究甘肃棘豆生物碱部位对KM小鼠肝癌H22细胞抑制作用及其对KM小鼠免疫功能的影响。 方法 采用鼠源性肝癌细胞H22移植瘤法,将60只KM小鼠随机分为5组，其中高、中、低剂量组分别给予甘肃棘豆生物碱部位32、16、8 mg/kg体重灌胃，阴性对照组给予生理盐水（NS）20 mL/kg灌胃，5- 氟脲嘧啶（5-FU）组给予5-FU 15 mg/kg体重腹腔注射，每天1次，连续给药10天。检测平均瘤重和抑瘤率,计算脾指数、胸腺指数，MTT法测脾细胞增殖率。 结果 甘肃棘豆生物碱部位高、中、低剂量组对肝癌细胞H22实体移植瘤的抑制率分别为43%、29%、23%；各剂量组小鼠的脾指数和胸腺指数均明显高于阴性对照组，中、高剂量组明显高于5-FU 组（P＜0.05）；各剂量组在24、48、72 h的脾细胞增殖率也明显高于阴性对照组及5-FU 组（P＜0.01）。 结论 甘肃棘豆生物碱部位对KM小鼠肝癌H22移植瘤有抑制作用，并能增强KM小鼠免疫功能。     

中药黄精中的新生物碱

中药黄精中的新生物碱孙隆儒１）王素贤李铣（沈阳药科大学天然药物研究室，沈阳１１００１５）黄精为百合科黄精属植物黄精（ＰｏｌｙｇｏｎａｔｕｍｓｉｂｉｒｉｃｕｍＲｅｄｏｕｔｅ）的根茎，具有补气养阴、ＦｉｇＳｔｒｕｃｔｕｒｅｏｆｔｈｅｃｏｍｐｏｕｎｄ健脾、...     

Fagaronine,a novel antileukaemic alkaloid

A review is presented about fagaronine, a benzophenanthridine alkaloid responsible for antitumoural activity. Plant source, extraction, biosynthesis, medicinal properties, especially antileukaemic activity, are described.     

分光光度法测定抗风痛胶囊中总生物碱的含量

目的：采用分光光度法对抗风痛胶囊中总生物碱进行含量测定。方法：采用将生物碱变成盐酸生物碱，再和溴麝香草酚蓝络合反应后，用氯仿萃取出总生物碱比色测定。结果：与HPLC法测定结果相比，分光光度法对抗风痛胶囊中总生物碱进行含量测定结果可靠。结论：本方法能够作为抗风痛胶囊质量控制方法之一。     

Analysis of Vascular Endothelial Growth Factor (VEGF) and a receptor subtype (KDR/flk-1) in the liver of rats exposed to riddelliine: a potential role in the development of hemangiosarcoma

Riddelliine alters hepatocellular and endothelial cell kinetics and function including stimulating an increase in hepatocytic vascular endothelial growth factor (VEGF) in the absence of increased serological levels of VEGF (Nyska etal. 2002). The objective of this study was to further assess hepatic VEGF and KDR/flk-1 synthesis and expression by hepatic cells under riddelliine treatment conditions. Forty-two male F344/N rats were dosed by gavage with riddelliine (0, 1.0, and 2.5 mg/kg/day) for 6 weeks. Seven animals/group were sacrificed after 8 consecutive daily doses; remaining rats were terminated after 30 daily doses, excluding weekends. Hepatic tissues were evaluated by immunohistochemistry and in situ hybridization. The results showed that VEGF mRNA expression was observed in control and treated animals; however, qualitative differences were noted. Treated animals exhibited VEGF mRNA in clustered, focal hepatocytes and bile duct epithelium, whereas VEGF mRNA in hepatocytes from vehicle control rats was distributed evenly across all hepatocytes. Results evaluating the distribution of the VEGF cognate receptor, KDR/flk-1 showed that randomly distributed, rare sinusoidal endothelium, including those demonstrating karyomegaly and cytomegaly expressed KDR/flk-1. Phosphorylation of KDR/flk-1 at pTyr996 and pTyr1054/1059, but not pTyr951, was also detected, evidence that endothelial cell KDR/flk-1 was activated. These results suggest that both hepatocytes and endothelial cells are targets of riddelliine-induced injury. We speculate that damage to both populations of cells may lead to dysregulated VEGF synthesis by hepatocytes and activation of KDR/flk-1 by endothelium leading to the induction of sustained endothelial cell proliferation, culminating in the development of hepatic hemangiosarcoma.     

云南萝芙木根中吲哚生物碱及其抗菌活性

目的 研究云南萝芙木Rauvolfia yunnanensis根中的吲哚类生物碱化学成分及抗菌活性,明确该植物抗菌活性成分。方法 采用硅胶柱色谱、RP-C₁₈、Sephadex LH-20、半制备HPLC等方法进行分离纯化,结合波谱数据及文献参数对化合物进行结构鉴定,并采用微量肉汤稀释法对单体化合物进行抗菌活性评价。结果 从云南萝芙木根醋酸乙酯部位共分离得到20个吲哚类生物碱化合物,分别鉴定为维诺任碱（1）、霹雳萝芙木碱（2）、四叶萝芙木新碱（3）、萝加灵（4）、西特斯日钦碱（5）、缝籽木醇（6）、柯楠醇（7）、二氢柯楠醇（8）、毛茶碱（9）、异毛茶碱（10）、佩立任碱（11）、10-羟基-16-表-花菊醇（12）、育亨宾（13）、降马枯星碱B（14）、洛柯碱（15）、阿枯米定碱（16）、去乙酰阿枯米灵（17）、利血平（18）、哈尔满碱（19）、梅林诺宁F（20）。其中化合物20对白色念球菌表现出较好的抗菌活性,最低抑菌浓度（minimum inhibitory concentration,MIC）值为3.12μg/mL,与临床抗真菌药物氟康唑的MIC值相同。化合物1、11对大肠杆菌,化合物11、13、20对枯草芽孢杆菌均表现出一定的抗菌活性,MIC值为6.25～12.50 μg/mL,活性与植物源抗菌药物小檗碱相当。结论 化合物20为首次从萝芙木属中分离得到,化合物6、8～13、16～18均为首次从该植物中分离得到,部分单体化合物表现出潜在抗菌活性。     

海绵中抗肿瘤抗病毒生物活性的生物碱研究进展

海绵中含有很多结构新颖且具有显著生物活性的生物碱。对近5年来具有抗肿瘤、抗病毒生物活性的生物碱加以概括。     

长春花叶片愈伤组织诱导及培养过程中生物碱合成类型的变化和调节及有关酶的分析

在４种不同培养基上诱导长春花叶片愈伤组织发生的过程中,叶片中含量较高的文多灵（ｖｉｎｄｏｌｉｎｅ）和长春质碱（ｃａｔｈａｒａｎｔｈｉｎｅ）迅速降解至极低水平,而在叶片中含量较低的阿玛碱（ａｊ－ｍａｌｉｃｉｎｅ）和蛇根碱（ｓｅｒｐｅｎｔｉｎｅ）的合成却逐渐增加,同时酸性和碱性过氧化物酶（ｐｅｒｏｘｉｄａｓｅ）活性呈上升趋势,尤其碱性过氧化物酶与蛇根碱和阿玛碱的相关性较密切。光照和黑暗中的变化趋势基本一致,但光照可提高过氧化物酶的活性,对培养物的长春质碱、文多灵和蛇根碱的合成有利。不同的培养基对生物碱的合成影响较大,２,４－Ｄ显著抑制生物碱的合成,持续光照使愈伤组织的生长受到抑制,使阿玛碱向其蛇根碱转化。     

Effect of Liposome—Encapsulated Total Alkaloid of Harmaline on Rabbit Lens Epithelial Cells：Experimental Study on the Prevention of Posterior Capsule Opacification

Purpose: To investigate whether liposome encapsulated total alkaloid of Harmaline (TAH) as a therapeutic agent is beneficial to prevention of posterior capsular opacifi-cation (PCO).Methods: Liposome-encapsulated TAH was prepared by modified freeze-thawing method. 0. 1ml of liposome-encapsulated TAH (0. 2mg/ml) was injected into the capsular bag during extracapsular lens extraction (ECLE) of each eye in total 10 rabbit eyes. Blank liposome or balance salt solution (BSS) was used as control. Slit-lamp examination and histopathological examination was used to evaluated capsule opacifica-tion. Intraocular pressure (IOP) , density and morphology of corneal endothelia cells, the amplitude and latency of b wave of ERG were measured.Results: The inflammatory response was mild both in TAH treated and the control group. PCO formation occurred in the control group 2 weeks postoperatively, but the posterior capsule was clear in TAH treated eyes. 4 weeks and 8 weeks after operation, PCO occurred both in TAH treated