化香树果序多糖脱蛋白工艺研究

目的 应用木瓜蛋白酶法脱除化香树果序多糖中蛋白,探究最佳工艺条件。方法 通过对酶用量、酶作用时间、酶作用温度及pH值四个单因素考察,采用响应面优化法试验分析。结果 最佳工艺条件,木瓜蛋白酶用量1.508%,温度65 ℃,酶解时间92.3 min,pH＝7.0,多糖蛋白脱除率为90.90%,多糖保留率为84.06%。结论 木瓜蛋白酶法是一种较优的多糖脱除蛋白方法。     

苦豆子多糖脱蛋白工艺比较

目的:优选苦豆子多糖的除蛋白工艺,确定最佳的除蛋白质方法。方法:以多糖损失率和蛋白脱除率为评价指标,比较Sevage法、三氯乙酸法和酶法对苦豆子多糖的脱蛋白效果。结果:Sevage法、三氯乙酸法和酶法的蛋白脱除率分别为85.80%,72.47%,91.99%,多糖损失率分别为23.76%,9.86%,1.99%。酶法脱蛋白效果最佳,最佳脱蛋白工艺为:木瓜蛋白酶用量2.0%(v/v),pH值7.0,温度60℃,时间4 h。结论:酶法是苦豆子多糖脱除蛋白质的最佳方法,此法可以较好地脱除游离蛋白,并使多糖损失较少。     

淫羊藿多糖的提取及其蛋白的脱除

目的 研究淫羊藿多糖提取及脱蛋白工艺.方法 采用不同提取温度、提取时间和料液比进行单因素试验,并采用正交试验优化提取条件.以蛋白质脱除率和多糖损失率为考察指标,比较Sevage法、氯化钠法、氯化钙法、鞣酸法及盐酸法的脱蛋白效果.结果 淫羊藿多糖提取的最优工艺参数为;提取温度90℃、提取时间4 h、料液比1;40.Sevage法的蛋白脱除率高达68.71%,多糖损失率仅为21.5%.结论 淫羊藿多糖提取工艺稳定可行,Sevage法脱蛋白效果较好且多糖损失率最低.     

败酱草多糖的脱蛋白研究

目的研究败酱草多糖的脱蛋白工艺。方法采用Sevag法、三氯乙酸法、酶法对败酱草多糖进行脱蛋白研究。结果酶法脱蛋白效果明显好于Sevag法,三氯乙酸法的多糖损失较多。在木瓜蛋白酶用量4%（W/V）、pH值6.0、温度55℃、酶解时间2.5 h的条件下,败酱草多糖的蛋白脱除率为51.65%,多糖损失率为7.93%。结论用酶法脱蛋白效果较好。     

亮菌多糖提取中脱蛋白和脱色方法比较

目的:探讨亮菌多糖提取过程中的脱蛋白和脱色方法.方法:以蛋白质脱除率和多糖保留率为考察指标,比较Sevage法、氯化钠法、氯化钙法、三氯乙酸法及盐酸法脱蛋白效果.以色素脱除率作为考察指标,比较过氧化氢和活性炭的脱色效果.结果:Sevage法脱蛋白效果较好且多糖得率最高;过氧化氢的脱色效果优于活性炭.结论:确定Sevage法和过氧化氢法为亮菌多糖提取的脱蛋白和脱色的方法.     

马粪海胆生殖腺中多糖的纯化方法及其抗肿瘤作用研究

目的 优化马粪海胆生殖腺中多糖的纯化方法,并评价其体外对肿瘤细胞的生长抑制作用.方法 马粪海胆生殖腺经水提取、木瓜蛋白酶结合Sevage法除蛋白、透析后醇沉、干燥制得马粪海胆总多糖,总多糖应用Sephacryl S-300凝胶柱色谱分离纯化;采用苯酚-硫酸法测定多糖含量;通过噻唑蓝(MTT)法测试多糖的体外抗肿瘤作用.结果 马粪海胆生殖腺的水提液应用木瓜蛋白酶结合Sevage法除蛋白效果最佳,木瓜蛋白酶最佳用量为100∶6(海胆脱脂粉与酶质量比),制得总多糖的纯度达90%;总多糖及分离得到的2个多糖体外对人肝癌Bel7402细胞表现出生长抑制作用.结论 该纯化方法步骤简单、易操作,所得多糖理化性质好、易溶于水,适用于马粪海胆生殖腺多糖的纯化.     

乌骨藤多糖脱蛋白工艺的研究

目的：优选乌骨藤多糖脱蛋白工艺。方法以蛋白脱除率和多糖保留率为评价指标,考察酶-Sevage法对乌骨藤多糖脱蛋白的效果。结果酶-Sevage法的蛋白脱除率分别为75.09%,多糖保留率分别为89.83%。结论酶-Sevage法脱蛋白的方法可行。     

萝藦果壳多糖脱蛋白方法研究

目的确定萝藦果壳多糖脱蛋白的最优方法。方法以蛋白脱除率和多糖损失率为指标,比较氯仿-正丁醇法(Sevag法)、三氯乙酸法(TCA法)、木瓜蛋白酶-Sevag法和木瓜蛋白酶-TCA法。结果 Sevag法、TCA法、木瓜蛋白酶-Sevag法、木瓜蛋白酶-TCA法的蛋白脱除率分别为73.14%,71.55%,86.03%,75.33%,多糖损失率分别为24.40%,25.68%,8.47%,17.13%。结论木瓜蛋白酶-Sevag法是除去萝藦果壳多糖中蛋白的最佳方法。     

金线莲多糖的提取优化与纯化

目的 以响应面法优化超声提取金线莲多糖的工艺,同时,对多糖纯化中除蛋白方法进行考察。方法 以多糖提取率为检测指标,在单因素考察的基础上采用Box-Behnken实验设计及响应面法对料液比、超声时间、超声提取温度3个因素进行优化;以多糖保留率和蛋白脱除率对Sevage试剂法、TCA法、盐法（NaOH-CaCl₂法和NaOH-NaCl法）、盐酸法5种脱蛋白方法进行考察。结果 金线莲多糖最佳提取工艺为: 料液比1∶10,超声提取温度48 ℃,超声提取时间36 min,超声提取次数2次,超声功率为300 W,该条件下金线莲多糖提取率达到了13.13%;同时以NaOH-CaCl₂法脱蛋白,多糖损失率为18.74%,蛋白脱除率为95.62%。结论 超声提取操作简单,优化后提取方法能够取得较高提取率,NaOH-CaCl₂法脱蛋白能够获得较高蛋白脱除率及多糖保留率,该方法适用于金线莲多糖活性成分的开发研究。     

红芪多糖的脱蛋白及脱色素工艺

目的：研究红芪多糖（HPS）的脱蛋白、脱色工艺。方法：采用L9（34）正交试验和单因素试验分别优选Sevage法脱蛋白工艺与过氧化氢脱色素工艺。结果：Sevage法脱蛋白工艺为：样液与试剂的体积比为1∶1,氯仿与正丁醇的体积比为4∶1,振摇30min,静置20min。过氧化氢脱色素条件是脱色时间为2～4h,用量为5～20ml过氧化氢每50ml样液。结论：优化后的条件适合于红芪多糖的脱蛋白、脱色素。     

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.