循环超声提取羊栖菜多糖的工艺优化

为研究循环超声提取分离羊栖菜多糖的中试工艺,实验以羊栖菜多糖提取率为指标,采用BoxBenhnken试验设计及响应面分析法优化循环超声提取的温度、固液比、功率、时间工艺参数,并对提取的粗多糖产品进行DPPH·清除的抗氧化评价。结果表明循环超声提取羊栖菜多糖的最佳工艺参数为:温度87℃、固液比1∶35(g/m L)、功率900 W、时间13 min。在此工艺参数下,羊栖菜多糖提取率可达10.54%,与预测值接近;所提取粗多糖产品得率为21.32%,DPPH·清除IC50值为6.64 mg。与传统热水浸提法相比,循环超声提取羊栖菜多糖提取率高,且提取时间短、粗多糖产品抗氧化性好,该工艺可为规模化生产羊栖菜多糖提供参考。     

高效毛细管电泳法测定灵芝多糖中单糖的组成

目的：采用高效毛细管电泳法测定灵芝多糖中单糖的组成。方法：灵芝多糖水解后，经PMP衍生化，高效毛细管电泳分析。电泳条件：缓冲液为50mmol·L^-1硼砂溶液（pH9．3）；柱温25℃；电压20kV；检测波长200nm；气压进样3．445kPa，进样时间5s。结果：灵芝多糖中含葡萄糖、半乳糖、木糖、甘露糖的摩尔比为4．5：2．8：1．3：3．6。结论：该方法具有简单、快速、分离效率高等特点，可用于测定灵芝多糖中单糖的组成。     

高效液相色谱法分析松茸多糖的单糖组成

目的:测定松茸多糖中单糖的组成及其摩尔比。方法:松茸多糖采用2 mol·L-1三氟醋酸水解后通过1-苯基-3-甲基-5-吡唑啉酮(PMP)柱前衍生,用高效液相色谱法梯度洗脱测定;检测波长250 nm。结果:松茸多糖由D-葡萄糖、D-半乳糖、D-阿拉伯糖、D-木糖组成,摩尔比为18.92∶2.68∶1.63∶1。各单体线性关系良好,r>0.998。D-葡萄糖、D-半乳糖、D-阿拉伯糖、D-木糖平均回收率分别为94.0%,88.5%,93.9%,95.9%。结论:该方法简便、准确、重复性良好,适用于分析松茸多糖中单糖组成。     

柱前衍生化HPLC法测定黄河滩枣多糖的单糖组成

目的建立PMP(1-苯基-3-甲基-5-吡唑啉酮)柱前衍生化HPLC法测定黄河滩枣多糖的单糖组成。方法采用水提醇沉法提取黄河滩枣多糖,多糖水解后进行PMP衍生化,HPLC法测定黄河滩枣多糖的单糖组成及摩尔比,并对等度和梯度洗脱两种模式的测定结果进行分析比较。结果黄河滩枣多糖由D-甘露糖、L-鼠李糖、D-半乳糖醛酸、D-葡萄糖、D-半乳糖、L-阿拉伯糖等六种单糖组成,它们的摩尔比约为0.54∶0.50∶0.27∶2.03∶5.40∶1.00,等度和梯度洗脱测定结果基本一致。结论本实验改进的等度洗脱方式更加简便易行,快速准确,适用于黄河滩枣多糖的单糖组成分析。     

瓜蒌多糖的提取及组分分析

目的 从瓜蒌中提取多糖，纯化，并分析其单糖组成。方法用水提醇沉法提取瓜蒌多糖，Saveg法去蛋白，再进行透析、Sephadex G-100分离，真空干燥得瓜蒌多糖，薄层色谱法和GC法分析。结果瓜蒌多糖由三种单糖组成。结论多糖组分是鼠李糖、阿拉伯糖和葡萄糖，各单糖的摩尔比为：1．0：2．4：4．7。     

灵芝孢子多糖两纯组分的单糖组成研究

目的：对灵芝孢子多糖的2个纯多糖组分GLPSl和GLPS3的单糖组成进行分析。方法：将灵芝孢子多糖原料精制，SephacrylS一400SF型凝胶分离纯化得2个主要组分GLPSl和GLPS3，经酸水解后TLC法和HPLC法鉴别单糖组成，改良的1一苯基一3一甲基一5一吡唑啉酮（PMP）柱前衍生化HPLC法分析单糖组成比例，同时采用LC—MS联用技术鉴定单糖PMP衍生化产物。结果：GLPSl的单糖组成为D一甘露糖：D一葡萄糖：D一半乳糖=1：9．228：1．474；GLPS3的单糖组成为D一甘露糖：D．葡萄糖：D．半乳糖=1：15．900：3．686。结论：灵芝孢子多糖二纯组分均含D一甘露糖，D．葡萄糖和D一半乳糖，仅各单糖的比例不同。     

蒲公英根多糖的分离、纯化及结构的初步分析

目的提取蒲公英根多糖,并对该多糖进行分离、纯化和结构的初步分析。方法采用超声波协同酶法进行提取多糖,分离纯化后,经Sephadex G-75柱分成A,B,C,D4级,采用优化的PMP柱前衍生HPLC分析单糖组成。采用紫外、红外等方法进行结构的初步分析。结果 4种多糖均含有D-鼠李糖、葡萄糖、D-半乳糖、D-木糖和D-阿拉伯糖;它们的单糖的摩尔比依次为,A：0.098∶2.88∶0.125∶0.01∶0.33;B：0.113∶0.68∶0.13∶0.011∶0.19;C：0.139∶2.46∶0.36∶0.13∶0.086;D：0.028∶0.36∶0.031∶0.012∶0.94。结论 4种多糖在结构上有明显的不同。     

天冬多糖的提取与单糖组成分析

目的 从常用中药天冬中提取多糖,并建立柱前衍生化高效液相色谱法分析天冬多糖的单糖组成. 方法采用水提醇沉法提取天冬多糖. 用2 mol•L^-1 硫酸溶液将多糖水解成单糖,用1-苯基-3-甲基-5-吡唑啉酮(PMP)与水解后的单糖进行衍生化反应;衍生产物采用反相高效液相色谱法分离,并在250 nm波长处检测,研究天冬多糖的单糖组成. 结果 水提醇沉法提取的多糖经过精制后,所得多糖的平均含量可达95.84%. 用高效液相色谱法检测天冬多糖中单糖组成比例为甘露糖:鼠李糖:葡萄糖醛酸:葡萄糖:半乳糖:阿拉伯糖(2.18:0.95:1.00:1.62:2.06). 结论 该多糖提取及精制方法可得到含量较高的天冬多糖. 柱前衍生的高效液相色谱法可用于天冬多糖的单糖组分分析,该法操作简便,结果 准确,适用于多糖中的单糖组成分析.     

柱前衍生化气相色谱法测定当归多糖的单糖组成

采用三氟乙酸水解当归多糖。糖腈乙酰衍生化水解单糖产物，用气相色谱法测定当归粗多糖CAP及其组分APF1、APF2和APF3的单糖组成。结果表明，当归粗多糖CAP及其组分APF1、APF2和APF3的单糖组成摩尔比各不相同。CAP由鼠李糖(Rha)、阿拉伯糖(Ara)、甘露糖(Man)、葡萄糖(Glc)、半乳糖(Gal)组成，其摩尔比为1．00：2．72：0．72：4．00：2．32；APF1由Rha．Ara、Glc、Gal组成。其摩尔比为1．00：227：7．80：269；APF2由Rha、Ara、Man、Glc、Gal组成，其摩尔比为1．00：529：3．66：9．11：5．17；APF3由Rha．Ara、Man、Glc、Gal组成。其摩尔比为1．00：454：298：11.09：7.45。     

柱前衍生化HPLC分析蒲公英多糖的单糖组成

目的合理优化衍生方法测定蒲公英多糖中单糖的组成及摩尔比。方法采用1-苯基-3-甲基-5-吡唑啉酮（PMP）柱前衍生,用反相高效液相色谱法进行测定。色谱条件为：ZORBAX-C18柱;流动相：0.1mol·L^-1的磷酸盐缓冲液（pH6.7）-乙腈（83∶17）;流速：1mL·min^-1;检测波长：245nm;进样量：20μL;柱温：室温。结果蒲公英多糖由D-鼠李糖、葡萄糖、D-半乳糖、D-木糖和D-阿拉伯糖组成,以不同方法提取的各单糖含量的摩尔比为：水提取法,Rha∶Glc∶Gal∶Ara=0.088∶0.500∶0.190∶0.340;超声提取法,Rha∶Glc∶Gal∶Ara=0.050∶0.350∶0.080∶0.320;酶提取法,Rha∶Glc∶Gal∶Ara=0.270∶0.630∶0.330∶0.460;超声协提取同酶法,Rha∶Glc∶Gal∶Ara=0.078∶0.550∶0.130∶0.170。结论改进后的衍生化方法和等度洗脱的色谱方法具有操作简单、快速、重复性好等特点,可用于蒲公英多糖中单糖组成和摩尔比的测定。     

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.     

Nachweis einiger Heilmittel in der Kniegelenksynovialflüssigkeit

Zusammenfassung Mittels Gaschromatographie und Dünschichtchromatographie wiesen die Autoren 11 Substanzen nach, welche durch Injektion oder nach Verabreichung per os in die Kniegelenksynovialflüssigkeit eindrangen. In ihrer Aufstellung konnten sie eine direkte Beziehung zwischen Struktur sowie chemischphysikalischen Eigenschaften der Substanz und ihrer Fähigkeit, aus dem Blut in die Kniegelenksynovialflüssigkeit einzudringen, nicht nachweisen, außer der Tatsache, daß Substanzen mit starker Affinität zu Eiweißstoffen erst in höheren Dosen nachweisbar waren.     

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.