O 羧甲基壳聚糖抑菌作用研究

目的考察自制O 羧甲基壳聚糖（O CMC）的抑菌活性及其影响因素。方法以金黄色葡萄球菌、枯草芽孢杆菌、大肠埃希菌、铜绿假单胞菌为标准菌株,采用菌落计数法计算抑菌率,比较羧甲基不同取代位置、不同浓度、不同pH对O CMC抑菌效果的影响。结果O CMC抑菌作用强于N, O 羧甲基壳聚糖和N 羧甲基壳聚糖;O CMC的抑菌作用与浓度、pH和供试菌种类有关。在一定范围内,其抑菌效果随浓度增大而加强,随pH增加而减弱;O CMC对革兰阳性菌的抑制作用强于革兰阴性菌。结论该O CMC具有广谱抗菌活性。     

羧甲基壳聚糖银的合成及抑菌实验的研究

目的研究羧甲基壳聚糖银的合成方法及其对金黄色葡萄球菌、铜绿假单胞菌、大肠埃希菌、肺炎克雷伯菌和变形杆菌的抑菌作用。方法对壳聚糖经化学修饰后的衍生物进行红外吸收光谱分析。用稀释法和凹环法对烧伤常见的病原菌进行抑菌实验。结果修饰后的衍生物经红外图谱分析表明 ,壳聚糖已被氯乙酸所修饰。羧甲基壳聚糖银对浓度均为 10 4 CFU/ml的金黄色葡萄球菌、大肠埃希菌、铜绿假单胞菌的抑菌率分别为 88%、80 .2 %和 75 .3%。羧甲基壳聚糖银和AgNO3 对金黄色葡萄球菌、铜绿假单胞菌的最低抑菌浓度相同 ,对大肠埃希菌的最低抑菌浓度则前者低于后者。结论羧甲基壳聚糖银对烧伤感染常见致病菌有抑制作用 ,它可作为一种新型的预防、治疗烧伤感染的药物。     

壳聚糖和羧甲基壳聚糖纳米银复合物的抑菌作用

目的研究自制的壳聚糖和羧甲基壳聚糖纳米银复合物对金黄色葡萄球菌、铜绿假单胞菌和大肠埃希菌的抑制作用。方法采用纸片琼脂扩散法及试管液体培养基稀释法进行试验。结果壳聚糖纳米银复合物对大肠埃希菌、金黄色葡萄球菌、铜绿假单胞菌的抑菌效果均明显优于壳聚糖、AgNO3及壳聚糖银。羧甲基壳聚糖纳米银复合物抑菌效果稍低于AgNO3和羧甲基壳聚糖银。结论壳聚糖和羧甲基壳聚糖纳米银复合物对这三种常见致病细菌均有抑制作用。     

月矾中空栓体外抑菌作用研究

目的研究月矾中空栓的体外抑菌作用。方法采用液体培养基2倍稀释法测定月矾中空栓及月矾普通栓对金黄色葡萄球菌、大肠埃希菌、铜绿假单胞菌、白色念珠菌的体外最低抑菌浓度(MIC)。结果月矾中空栓剂和月矾普通栓对白色念珠菌的抑菌作用最强,其余依次为大肠埃希菌、金黄色葡萄球菌、铜绿假单胞菌;中空栓剂与普通栓剂对铜绿假单胞菌的抑制效果无明显差别,对金黄色葡萄球菌和大肠埃希菌的抑菌效力提高1倍左右,对白色念珠菌的抑菌效力提高4倍左右。结论月矾中空栓剂和月矾普通栓对4种实验菌均有抑菌作用,中空栓剂的抑菌作用优于普通栓剂。     

复方紫柄冬青软膏对烧烫伤细菌感染的体外抗菌活性研究1

目的：评价复方紫柄冬青软膏对临床常见菌种的抗菌活性。方法：采用中药抑菌实验方法,测定复方紫柄冬青软膏对3种实验菌（金黄色葡萄球菌、大肠埃希菌、铜绿假单胞菌）的体外抗菌活性。结果：经体外抗菌实验,其结果显示复方紫柄冬青软膏中含生药125（高浓度）,62．50（中浓度）和15．62mg／mL（低浓度）的样品溶液,其高浓度对3种实验菌株均有抑制作用,中浓度对大肠埃希菌和铜绿假单胞菌有抑制作用,而低浓度仅对大肠埃希氏菌有抑制作用。结论：复方紫柄冬青软膏对金黄色葡萄球菌、大肠埃希菌、铜绿假单胞菌均有不同程度的抑菌活性。     

复方明矾混悬液的体外抑菌实验

目的 观察复方明矾混悬液的体外抑菌作用. 方法 以铜绿假单胞菌、大肠埃希菌、金黄色葡萄球菌为受试菌, 磺胺嘧啶银为对照药, 采用二倍肉汤稀释法, 观察比较它们的最小抑菌浓度. 结果 金黄色葡萄球菌、大肠埃希菌、铜绿假单胞菌对复方明矾混悬液均敏感, 对3种致病菌的最小抑菌浓度（MIC）均为2.3×10-3 g•mL^-1. 结论 复方明矾混悬液具有较明显的体外抑菌作用.     

烧伤搽剂体外抑菌作用研究

目的探讨烧伤搽剂新剂型的体外抑菌作用。方法采用纸片扩散法测定烧伤搽剂原剂型、新剂型对3种烧伤常见致病菌（金黄色葡萄球菌、铜绿假单胞菌、大肠埃希菌）的抑菌活性,并以0.9%氯化钠溶液和醋酸氯己定溶液为对照。采用琼脂稀释法测定烧伤搽剂新剂型和阳性药物改性甲壳素创面修复凝露对3种菌的最低抑菌浓度,测定烧伤搽剂新剂型对临床烧伤创面分泌物中分离菌株的最低抑菌浓度。结果烧伤搽剂新剂型对金黄色葡萄球菌、铜绿假单胞菌、大肠埃希菌的抑菌圈直径分别为（16.13±0.27）,（15.83±0.20）,（15.55±0.15）mm,均较原剂型大,差异有统计学意义（P＜0.01）,对金黄色葡萄球菌和铜绿假单胞菌的抑菌作用与醋酸氯己定比较,差异有统计学意义（P＜0.05）;对金黄色葡萄球菌、铜绿假单胞菌、大肠埃希菌致病菌的最低抑菌浓度分别为1.56,6.25,1.56 mg•mL－1,对临床烧伤创面分泌物中分离菌株有一定抑菌作用。结论烧伤搽剂新剂型对金黄色葡萄球菌、铜绿假单胞菌、大肠埃希菌均具有较好的抑菌效果。     

金银花水提物及醇提物体外抗菌实验

目的：研究金银花水提物及不同浓度醇提物的体外抑菌和杀菌作用。方法：测定金银花水提物及25%、50%、75%、90%醇提物的最低抑菌浓度（MIC）和最低杀菌浓度（MBC）。结果：金银花水提物及醇提物均对金黄色葡萄球菌有较明显抑菌及杀菌作用,对痢疾杆菌、铜绿假单胞菌、大肠埃希菌的抑菌和杀菌效果一般,高浓度醇提物对铜绿假单胞菌和大肠埃希菌的抗菌作用不明显。结论：金银花不同溶剂提取物对供试菌均有一定的抑菌作用,是有研究、开发价值的天然抗菌中草药。     

天葵菌毒清颗粒的体外抑菌作用研究

目的：探讨天葵菌毒清颗粒的体外抑菌作用,为天葵菌毒清颗粒增加治疗支气管哮喘（Bronchial asthma,BA）适应症提供药效学数据。方法采用平皿二倍稀释法考察天葵菌毒清颗粒对大肠埃希菌、金黄色葡萄球菌、肺炎双球菌、铜绿假单胞菌和流感杆菌的抑菌性。结果天葵菌毒清颗粒对大肠埃希菌、金黄色葡萄球菌、肺炎双球菌、铜绿假单胞菌和流感杆菌具备一定的体外抑菌活性。结论天葵菌毒清颗粒具备一定的体外抑菌活性,为其增加治疗支气管哮喘适应症提供了一定的理论依据。     

皂角刺提取物体外抑菌杀菌作用研究

目的探讨皂角刺提取物对实验室常见菌(大肠埃希菌、枯草芽孢杆菌、金黄色葡萄球菌、白念珠菌、铜绿假单胞菌)的体外抑菌杀菌作用。方法制备不同溶剂不同浓度的皂角刺提取物,采用滤纸片法测其抑菌杀菌作用,二倍稀释法测其最低抑菌浓度。结果皂角刺提取物对大肠埃希菌、枯草芽孢杆菌、白念珠菌和铜绿假单胞菌的抑菌杀菌作用不明显,对金黄色葡萄球菌有一定的抑菌杀菌作用。皂角刺水提取物对金黄色葡萄球菌的最低抑菌浓度为25.0 mg.mL-1;皂角刺乙醇提取物对金黄色葡萄球菌的最低抑菌浓度为12.5 mg.mL-1。结论不同溶剂、不同浓度的皂角刺提取物对金黄色葡萄球菌均有抑菌和杀菌作用。     

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.