超声波辅助过氧化氢氧化降解制备相对低分子质量异枝麒麟菜硫酸多糖

目的 制备相对低分子质量异枝麒辟菜硫酸多糖。方法 采用超声波辅助过氧化氢氧化降解异枝麒辟菜硫酸多糖，并测定各多糖样品的相对分子质量及硫酸基、3，6-内醚半乳糖含量。结果 制备了相对分子质量为5000～40000的硫酸多糖，其硫酸基含量均在18．5％以上。结论 该方法适合于制备相对低分子质量高水溶性多糖，后处理简单，并能较好地保持多糖中的硫酸基。     

几种O-羧甲基壳聚糖硫酸酯的制备

以甲壳质为原料制备了O-羧甲基壳聚糖，再经不同的硫酸酯化工艺分别制备了O-羧甲基-N-硫酸酯基壳聚糖（Ⅰ），O-羧甲基-O-硫酸酯基壳聚糖（Ⅱ），O-羧甲基-N，O-硫酸酯基壳聚糖(Ⅲ）等3种不同硫酸酯基取代位置的羧甲基壳聚糖衍生物，对各化合物分别采用氧瓶燃烧法测定了硫含量（S%），采用HPGPC法制定了重均相对分子质量和相对分子质量分布宽度。并对各化合物的红外光谱（IR）和^13C-NMR核磁共振图谱进行了分析。     

N-羧烷基-6-O-壳聚糖硫酸酯的制备

以铜离子为模板定向合成了6-O-壳聚糖硫酯酯，然后分别用乙醛酸和丙酮酸在其N-位形成席夫碱，再经NaCNBH3还原制备了N-羧甲基-6-O-壳聚糖硫酸酯和N-（2-甲基-羧甲基）-6-O-壳聚糖硫酸酯，对制得的各化合物分别采用氧瓶燃烧法测定了硫含量（S%），采用HPGPC法测定了重均相对分子质量和相对分子质量分布宽度，并对各化合物的红外光谱（IR）和^13C-NMR核磁共振图谱进行了分析。     

溶菌酶对壳聚糖降解的研究

对溶菌酶降解壳聚糖的过程进行了研究。探讨了降解过程的粘度变化、温度、pH值、反应时间、酶浓度、壳聚糖浓度以及壳聚糖的脱乙酰化度对酶促反应速度的影响。实验结果表明，以壳聚糖为底物的溶菌要不得的催化是属米氏酶的特征，该酶促反应的最适宜温度为50℃，适宜pH值是6.0左右，壳聚糖的脱乙酰度越低降解速度越快。产品经高效液相色谱测定相对分子质量低于1万，相对分子质量组分集中，水溶性良好。     

重量法测定藻酸双酯钠片的含量

目的 建立重重法测定藻酸双酯钠片含量的方法。方法 采用王水氧化、水解，使藻酸双酯钠中的硫转变为硫酸．再以过量的Ba盐在酸性条件下与之产生硫酸钡沉淀，用重量法测定重量．从而间接计算出藻酸双酯钠的含量。结果 藻酸双酯钠与之产生的硫酸镊线性关系良好(r=0．9999)．平均加样回收率99．2％(n=5)．样品测定精密度RSD=l％(n=5)。结论 结果准确可靠，方法简便易行。     

用树脂法纯化脱水山梨醇

脱水山梨醇为一口服脱水药,也是合成抗心绞痛药物硝酸异山梨酯和单硝酸异山梨酯的中间体n’．一般纯化法工序较多,而且残液很难处理．用树脂法纯化后,纯度达到药典标准【’】．由于脱水山梨醇是山梨醇经酸催化发生1,令及36一脱水环合而成,其主要杂质是未反应的原料山梨醇和1,4·或36一单坏合产物,结构中含有卜或～伯羟基,极易被高碘酸盐氧化。而脱水山梨醇结构中的2,5一件羟基。不会与高碘酸盐反应,所以可用高碘酸盐消耗量来控制其杂质含量．1实验材料与仪器材料：脱水山梨醇粗品,由工业山梨醇（50％）浓缩后经硫酸催化脱水,真…     

壳聚糖定位硫酸酯化的制备工艺

对C6－O位壳聚糖硫酸酯（6S），C3－O位壳聚糖硫酸酯（3S），C2－N位壳聚糖硫酸酯（2S），C3，6－O位壳聚糖二硫酸酯（36S），C2－N－C3－O位壳聚糖二硫酸酯（23S），C2－N－C6－O位壳聚糖二硫酸酯（26S）和C2－N－C3，6－O位壳聚糖三硫酸酯（236S）等壳聚糖各种不同位置硫酸酯化的制备工艺条件进行了详细介绍，为进一步对壳聚糖硫酸酯的活性和构效关系进行深入研究提供了参考。     

毛细管电泳-电致化学发光法测定维U颠茄铝胶囊中硫酸阿托品的含量

目的：建立一种快速测定硫酸阿托品的电化学发光分析新方法。方法：基于硫酸阿托品对二联吡啶钌在铂电极上的电致发光信号有增敏作用，与毛细管电泳结合，建立一种快速、灵敏、准确的测定制剂中硫酸阿托品含量的方法。结果：在优化的实验条件下，硫酸阿托品在1．0×10^-4～1．0×10^-6mol·L^-1范围内呈良好线性（r=0．9978）；检出限（3σ）为3．0×10^-7mol·L^-1，回收率为87％～91％，RSD小于5％。峰高和迁移时间的RSD分别为4．3％和1．2％（n=6）。结论：本法与高效液相色谱法相比，具有检出限低和线性范围宽的优点，可用于维U颠茄铝胶囊的质量控制及相关药物的含量检测。     

咔唑法同时测定玻璃酸钠和硫酸软骨素的含量

目的：建立咔唑法同时测定玻璃酸钠（SH）和硫酸软骨素（CS）含量的方法。方法：通过醋酸钠调节样品的酸碱度和离子强度,氯化十六烷基吡啶（CPC）可选择性地沉淀CS,而SH不沉淀,从而将SH和CS进行分离。结果：样品预处理条件为：精密量取SH和CS的混合溶液10mL,加入醋酸钠1．6g,12．5mmot／LCPC10mL,充分搅拌后,静置1h,20μm滤膜过滤;滤液用于测定SH的含量;滤饼经1．4mol／L氯化钠溶液超声解离后,用于测定CS的含量;SH和CS的平均回收率分别为101．2％和99．4％,RSD分别为1．05％和0．96％。结论：本法可同时测定SH和CS的含量,相互之间无干扰。     

不同相对分子质量壳聚糖的制备和部分性质研究

目的制备不同相对分子质量 (Mr)壳聚糖并研究其部分性质。方法在中性条件下 ,用过氧化氢氧化法制备不同Mr 的壳聚糖 ,并进行红外表征、热分析和稳定性等研究。结果探索到制备不同Mr 壳聚糖的最适宜条件。结论壳聚糖经过氧化氢降解后 ,结构没有明显变化 ,且随壳聚糖Mr 的降低 ,其稳定性增强     

Synthesis,Cytotoxicity and Antileishmanial Activity of Some N-(2-(indol-3-yl)ethyl)-7-chloroquinolin-4-amines

We report herein the condensation of 4,7-dichloroquinoline (1) with tryptamine (2) and D-tryptophan methyl ester (3) . Hydrolysis of the methyl ester adduct (5) yielded the free acid (6) . The compounds were evaluated in vitro for activity against four different species of Leishmania promastigote forms and for cytotoxic activity against Kb and Vero cells. Compound (5) showed good activity against the Leishmania species tested, while all three compounds displayed moderate activity in both Kb and Vero cells.     

Lung disease and PKCs

The lung offers a rich opportunity for development of therapeutic strategies focused on isozymes of protein kinase C (PKCs). PKCs are important in many cellular responses in the lung, and existing therapies for pulmonary disorders are inadequate. The lung poses unique challenges as it interfaces with air and blood, contains a pulmonary and systemic circulation, and consists of many cell types. Key structures are bronchial and pulmonary vessels, branching airways, and distal air sacs defined by alveolar walls containing capillaries and interstitial space. The cellular composition of each vessel, airway, and alveolar wall is heterogeneous. Injurious environmental stimuli signal through PKCs and cause a variety of disorders. Edema formation and pulmonary hypertension (PHTN) result from derangements in endothelial, smooth muscle (SM), and/or adventitial fibroblast cell phenotype. Asthma, chronic obstructive pulmonary disease (COPD), and lung cancer are characterized by distinctive pathological changes in airway epithelial, SM, and mucous-generating cells. Acute and chronic pneumonitis and fibrosis occur in the alveolar space and interstitium with type 2 pneumocytes and interstitial fibroblasts/myofibroblasts playing a prominent role. At each site, inflammatory, immune, and vascular progenitor cells contribute to the injury and repair process. Many strategies have been used to investigate PKCs in lung injury. Isolated organ preparations and whole animal studies are powerful approaches especially when genetically engineered mice are used. More analysis of PKC isozymes in normal and diseased human lung tissue and cells is needed to complement this work. Since opposing or counter-regulatory effects of selected PKCs in the same cell or tissue have been found, it may be desirable to target more than one PKC isozyme and potentially in different directions. Because multiple signaling pathways contribute to the key cellular responses important in lung biology, therapeutic strategies targeting PKCs may be more effective if combined with inhibitors of other pathways for additive or synergistic effect. Mechanisms that regulate PKC activity, including phosphorylation and interaction with isozyme-specific binding proteins, are also potential therapeutic targets. Key isotypes of PKC involved in lung pathophysiology are summarized and current and evolving therapeutic approaches to target them are identified.     

Gender-related symptoms and correlates of alcohol dependence among men and women with a lifetime diagnosis of alcohol use disorders

This study explored gender-related symptoms and correlates of alcohol dependence in a crosssectional study of 150 men and 150 women with a lifetime diagnosis of alcohol use disorders (AUD). Participants were recruited in equal numbers from treatment settings, correctional centres and the general community. Standardized measures were used to determine participants' use of substances, history of psychiatric disorders and psychosocial stress, their sensation seeking and family history of substance use and mental health disorders. Multivariate analyses were used to detect patterns of variables associated with gender and the lifetime severity of AUD. Men had a longer history of severe AUD than women. Women had similar levels of alcohol dependence and medical and psychological sequelae as men, despite 6 fewer years of AUD. More women than men had a history of severe psychosocial stress, severe dependence on other substances and antecedent mental health problems, especially mood and anxiety disorders. There were differences in family history of alcohol-related problems approximating same-gender aggregation. The severity of a lifetime AUD was predicted by its earlier age at onset and the occurrence of other disorders, especially anxiety, among both men and women. The limitations in the generalizability of these findings due to sample idiosyncrasies are discussed.     

Biochemical and molecular characterisation of cubozoan protein toxins

Class Cubozoa includes several species of box jellyfish that are harmful to humans. The venoms of box jellyfish are stored and discharged by nematocysts and contain a variety of bioactive proteins that are cytolytic, cytotoxic, inflammatory or lethal. Although cubozoan venoms generally share similar biological activities, the diverse range and severity of effects caused by different species indicate that their venoms vary in protein composition, activity and potency. To date, few individual venom proteins have been thoroughly characterised, however, accumulating evidence suggests that cubozoan jellyfish produce at least one group of homologous bioactive proteins that are labile, basic, haemolytic and similar in molecular mass (42-46 kDa). The novel box jellyfish toxins are also potentially lethal and the cause of cutaneous pain, inflammation and necrosis, similar to that observed in envenomed humans. Secondary structure analysis and remote protein homology predictions suggest that the box jellyfish toxins may act as α-pore-forming toxins. However, more research is required to elucidate their structures and investigate their mechanism(s) of action. The biological, biochemical and molecular characteristics of cubozoan venoms and their bioactive protein components are reviewed, with particular focus on cubozoan cytolysins and the newly emerging family of box jellyfish toxins.     

Dose tolerability of chronically inhaled voriconazole solution in rodents

Invasive pulmonary aspergillosis (IPA) is a fungal disease of the lung associated with high mortality rates in immunosuppressed patients despite treatment. Targeted drug delivery of aqueous voriconazole solutions has been shown in previous studies to produce high tissue and plasma drug concentrations as well as improved survival in a murine model of IPA. In the present study, rats were exposed to 20 min nebulizations of normal saline (control group) or aerosolized aqueous solutions of voriconazole at 15.625 mg (low dose group) or 31.25 mg (high dose group). Peak voriconazole concentrations in rat lung tissue and plasma after 3 days of twice daily dosing in the high dose group were 0.85 ± 0.63 μg/g wet lung weight and 0.58 ± 0.30 μg/mL, with low dose group lung and plasma concentrations of 0.38 ± 0.01 μg/g wet lung weight and 0.09 ± 0.06 μg/mL, respectively. Trough plasma concentrations were low but demonstrated some drug accumulation over 21 days of inhaled voriconazole administered twice daily. Following multiple inhaled doses, statistically significant but clinically irrelevant abnormalities in laboratory values were observed. Histopathology also revealed an increase in the number of alveolar macrophages but without inflammation or ulceration of the airway, interstitial changes, or edema. Inhaled voriconazole was well tolerated in a rat model of drug inhalation.