拉呋替丁的合成工艺改进

2-氨基-4-甲基吡啶经溴代、氧化、还原,然后和对甲苯磺酰氯成酯,酯和哌啶反应得到2-溴-4-(哌啶甲基)吡啶,再用4-(2-氧四氢吡喃基)-cis-2-丁烯-1-醇醚化得2-[4-(2-氧四氢吡喃基)-cis-2-丁烯-1-氧]-4-(1-哌啶基)吡啶,经脱THP保护基、氯化、Gabriel反应、肼解、酰胺化制得H2受体拮抗剂拉呋替丁,总收率为13%.     

Calmodulin mediates melatonin cytoskeletal effects

In this article, we review the data concerning melatonin interactions with calmodulin. The kinetics of melatonin-calmodulin binding suggest that the hormone modulates cell activity through intracellular binding to the protein at physiological concentration ranges. Melatonin interaction with calmodulin may allow the hormone to modulate rhythmically many cellular functions. Melatonin's effect on tubulin polymerization, and cytoskeletal changes in MDCK and N1E-115 cells cultured with melatonin, suggest that at low concentrations (10^–9 M) cytoskeletal effects are mediated by its antagonism to Ca²⁺-calmodulin. At higher concentrations (10^–5 M), non-specific binding of melatonin to tubulin occurs thus overcoming the specific melatonin antagonism to Ca²⁺-calmodulin. Since the structures of melatonin and calmodulin are phylogenetically well preserved, calmodulin-melatonin interaction probably represents a major mechanism for regulation and synchronization of cell physiology.     

Sympathectomy enhances the substance P-mediated breakdown of the blood-aqueous barrier in response to infrared irradiation of the rabbit iris

Summary Rabbits were subjected to infrared irradiation of the iris 1 month after unilateral cervical sympathectomy. The resulting breakdown of the blood-aqueous barrier was greatly enhanced on the sympathectomized side. In contrast, the response to intravitreally injected substance P (SP) was the same in both eyes. The enhancement of the response to IR irradiation could be abolished by pretreatment with an SP antagonist, (D-Pro², D-Trp^7,9)-SP.This study was supported by grants from the Swedish MRC (04X-1007, 14X-2321), the Medical Faculty of Lund, Ferring Arzneimitel, Kiel (Federal Republic of Germany) and Ferring Pharmaceuticals, Malmö (Sweden).     

.中度嗜盐菌的分离鉴定及其强化高盐制革废水处理的研究

为探索中度嗜盐菌在高盐有机制革工业废水处理中的应用, 解决高盐有机制革废水处理这一难题,从山东省威海市路道口盐场晒盐池盐水中分离一株嗜盐菌株YS-1,对该菌株进行原子力显微镜观察、生理生化测定,全细胞脂肪酸分析、16S rDNA序列同源性分析.研究表明,YS-1菌株16S rDNA序列与Halomonas sp.(AB167061)的亲缘关系最为接近,结合上述其它各项结果确定该菌株为盐单胞菌属(Halomonas sp. ),属中度嗜盐菌;在SBR反应器中对其进行强化高盐制革废水处理试验,同时结合生物活性碳技术,结果表明,含盐9.3%、CODCr=1738mg/L的高盐制革废水,经168h 的CODCr去除率为86%,216 h 的CODCr去除率为98%,该菌株具有强化高盐制革废水处理的功能,通过分离筛选嗜盐菌强化高盐制革工业废水处理具有可行性,嗜盐微生物的强化作用与生物活性碳技术相结合构建“嗜盐生物活性碳”技术,在高盐制革废水处理中具有重要作用.     

2005～2007年武汉亚洲心脏病医院钙拮抗剂应用分析

目的:分析武汉亚洲心脏病医院钙拮抗剂应用情况及发展趋势.方法:对该院2005年~2007年钙拮抗剂的用药金额、用药频度、消耗金额进行统计.结果:钙拮抗剂的消耗金额呈上升趋势,氨氯地平的消耗金额最高,左氨氯地平和硝苯地平控释片的用药频度占前两位.结论:长效二氢吡啶类钙拮抗剂具有广阔的市场前景.     

水族专用鱼药“水族康泰-I”应用研究

通过一种第三代氟喹诺酮类药物所做的4种水产动物病原菌肠型点状气单细胞、荧光假胞菌、嗜水气单胞菌、鳗弧菌的药效研究和安全性评价,测定了最小抑菌浓度(MIC)分别为0.0125、1.56、0.00625、0.025ug/m L,均对这些病原菌高度敏感。依据该氟喹诺酮类的药效学、药动学和毒力学特性,设计出水族专用新鱼药“水族康泰-I”。本品一般预防剂量为0.2～0.4g/(kg.d),治疗剂量为0.8～1g/(kg.d)。防治鱼病临床显示,其保护率100% ,治愈率在95% 以上,药效快、抗菌广谱,无明显毒副作用。     

动态载片培养法批量制作永久细菌标本片

细菌标本片在《病原生物学》教学过程中占有举足轻重的地位,需要大量的永久标本片。其制作要求背景洁净、分布均匀、染色鲜艳、物象清晰、形态典型、结构完整、大小准确、规律排列、省时省力、耗材量少、成本低廉。制作永久保存的细菌标本片是十分复杂繁琐的过程,而且对技术的精、准要求非常严格。文中用动态载片培养法能批量制作永久标本片且满足以上要求,在标本片的永久保存和提高教学质量方面取得了良好的效果。     

基于THz时域光谱技术的水果杀菌剂农药检测与鉴别

利用太赫兹时域光谱技术对3种水果样品及其与杀菌剂农药混合的样品分别进行THz光谱测试,获得它们在0.2~1.5 THz波段的THz时域数据,计算它们的折射率和吸收系数谱。提取其特征THz吸收光谱,分析水果与噻菌灵样品在不同农药含量条件下吸收系数的变化规律。结果表明:THz吸收谱中吸收峰的位置和幅值随样品种类和含量不同存在差别;为提高光谱的区分度,将3种水果样品的THz吸收光谱的一阶导数作为分类特征数据,用主成分方法(Principal Component Analysis,PCA)进行鉴别,样品类别鉴别正确率可达100%。     

高温高矿化度超稠油油藏细菌多样性分析

运用16S rDNA克隆文库技术分析研究了塔河油田高温高矿化度超稠油油藏中的细菌多样性.研究结果表明:在油藏温度100～130℃、地层水矿化度26×104mg/L、地面原油黏度10×104mPa.s的油藏环境中,存在丰富的细菌群落,其中包括Candidate division OP菌、盐单胞菌(Halomonas sp.)、耐盐芽孢杆菌(Bacillus halodurans)和油杆菌(Petrobacter sp.)等具有耐温、耐盐和降解原油的生理生化特性的菌群,同时还存在大量未培养的微生物.     

Isolation, chemical characteristics and immunity activity of an extracellular polysaccharide EPSⅠ isolated from Antarctic bacterium Pseudoalteromonas sp. S-15-13

A new extracelluar polysaccharide (EPS) was isolated and purified from Antarctic bacterium S-15-13, identified as Pseudoalteromonas sp. After being separated and purified by DEAE-Sephadex A-50 ionexchange and Sephadex G-100 gel chromatography, two mains fractions (EPSⅠand EPSⅡ) were obtained. EPSⅠwas composed of mannose, glucose and galactose with a molecular weight of 23kDa and EPSⅡwas composed of mannose only with a molecular weight of 62kDa.The effect of the polysaccharide EPSⅠ on the cellular immune response of mice was investigated. Results demonstrated that EPSⅠ could markedly facilitate lymphocyte proliferation, and might be a strong immunomodulator.