比色法测定丁胺卡那霉素、卡那霉素、新霉素和妥布拉霉素

本法是基于五氰亚硝酰铁酸二钠(diso—dium pentacyanonitrosylferrate与脂肪族伯胺和仲胺的Rimini反应,可用以测定丁胺卡那霉素、卡那霉素、新霉素和妥布拉霉素;但对该四个抗生素没有分辨能力。该四种抗生素的浓度与反应后在540nm时的吸收峰值符合Beer定律:其适当浓度分别为2.8×10~(-4)～1.7×10~(-3)mol/L、2.6×10~(-4)～2.0×10~(-3)mol/L、1.7×10~(-4)～1.9×10~(-3)mol/L和2.5×10~(-4)～1.6×10~(-3)mol/L。     

安宁和泛酸钙的氨气敏电极测定法

安宁及其制剂和泛酸钙,经降解成相应的铵盐,两者于浓碱存在下均逸出 NH_3,可用氨气敏电极测定。在1×10~(-4)～1×10~(-2)mol/L 浓度范围内,校正曲线呈线性,所测得结果与凯氏定氮法基本一致。     

辐射聚合制备毛果芸香碱—水凝胶释放体系的研究

本文研究的药膜是在室温条件下将含药的单体放在模具中进行辐射交联聚合。该法工艺简便,药膜纯度高不带任何引发剂残余物。我们研究了基质含水率,药物含量、辐射剂量率及总剂量对药物释放速率的影响。结果表明:药物的释放量随着基质含水率及药含量的增加而增加;随着交联剂用量及辐照剂量率和总剂量的增加而降低。药物在剂量率为6.46×10~3Rad/sec及总剂量为1.28×10~6ad条件下辐照与未经辐照处理的药物进行了红外及紫外对比试验,结果表明;辐照对药物结构没有明显的影响。     

口服霍乱活菌苗CVD103-HgR株的志愿者保护性免疫力的开始与持续时间

作者对18～39岁的健康成人志愿者进行两项研究。第1项研究,22人口服1剂3～5×10~8菌落形成单位(cfu)CVD 103-HgR株霍乱活菌苗。2个月后,另7人口服1剂3～5×10~9cfu CVD 103-HgR菌苗,以15名未免疫者作为对照组。分别在口服菌苗后6和4个月以4×10~6 cfu稻叶型霍乱弧菌569B株攻击。第2项研究,11人口服1剂3～5×10~8     

伤寒的血象和骨髓象改变与临床的关系(附33例报告)

为探讨伤寒病的临床表现与血象和骨髓象的相关性,我们搜集1988年2月至1992年2月四年中收治的经细菌和/或血清学明确诊断伤寒的住院患者33例,现报告如下。材料和方法33例中男14例、女19例。年龄5～13岁3例,17～35岁27例,40～51岁3例。血象:WBC 以4～10×10~9/L 为正常。33例中4.2～9.9×10~9/L 8例,14.1×10~9/L 1例(以上为WBC 正常及增高组);0.55～385×10~9/L24例(WBC 低下组);外周全血细胞减少者9例;WBC 小于1×10~9/L3例,最低者0.55×10~9/L。骨髓均采自发热期,经两人共同阅片,其中3例因严重稀释未作分类。结果WBC 减少组24例中有10例腹泻。肝脾肿     

肝癌并发类白血病反应一例

患者男,76岁。主因发热、贫血3个月伴间断上腹痛20余天于1986年2月26日入院。入院前3个月无何诱因出现乏力、厌油及头晕,后出现发热,多在38℃左右,持续约4小时自然下降。无咽痛、咳嗽、咯血及盗汗。曾在外院检查血红蛋白60g/L,白细胞14×10~9/L。胸片示双肺纹理增重,诊断肺部感染,采用青链霉素治疗症状无改善。后查血红蛋白60g/L,白细胞20×10~9～30×10~9/L.血沉80mm/1小时,血、     

急性淋巴细胞型白血病并发睾丸白血病1例报告

患者男性,16岁.以颈部淋巴结肿大、头晕、乏力、低热一个多月于1985年12月5日入院。体检:颈部两侧胸锁乳突肌前缘、颌下可触及3～4个蚕豆大淋巴结,两侧腋窝腹股沟均可触及3～4个成串的淋巴结,无触痛。胸骨压痛明显.心肺(-)。肝大肋下1.5cm,脾大肋下2.5cm、质硬.两侧睾丸呈鸽蛋大、质软,阴茎正常,有少许阴毛.实验室检查:Hb6.5g/LWBC28.5×10~9/L,分类:中性粒细胞10％,原幼淋巴细胞86％,成熟淋巴细胞占4％,pt50×10~9/L,     

~(60)Co-γ射线辐照贮藏对川贝母质量的影响

目的:研究~(60)Co-γ射线辐照贮藏对川贝母质量的影响。方法:对不同剂量~(60)Co-γ射线辐照处理过的川贝母的霉变、虫蛀情况进行观察,并对辐照和未辐照川贝母的总生物碱和水溶性核苷类成分进行含量比较。结果:经辐照后的川贝母的化学成分、感观形态无明显变化,能有效地防止霉变和虫蛀,明显延长药材的贮藏期;川贝母辐照前后总生物碱和水溶性核苷类成分无含量显著变化。结论:应用~(60)Co-γ射线辐照灭菌杀虫工艺可为富含淀粉及贵重中药材的贮藏提供有效方法。     

变价态唐松草新碱—PVC膜离子选择电极的研制及解离常数的测定

本文研制了以四苯硼—唐松草新碱缔合物为电活性物质的变价态唐松草新碱—PVC膜电极。电极膜按电活性物质:PVC:DBP为1:8:8组成。该电极在pH 5.0～6.0,Ⅰ=0.05的NaCl—HCl溶液中Nernst响应范围为1×10~(-3)～1×10~(-5)mol/L。电极斜率为58.2 mV/logc。检测限为2.5×10~(-6)mol/L。用直接电位法考察了TDH~+,TDH_2~(++)共存时溶液pH和电极斜率S的关系。用S—pH关系,测定了25℃,Ⅰ=0.05时的Ka_1值为(2.5±0.2)×10~(-4),用E—pH关系,测定了25℃,Ⅰ=0.05时的Ka_2值为(8.1±0.9)×10~(-8)。     

麦迪霉素在水溶液中稳定性的研究

本实验用分光光度法对麦迪霉素的稳定性进行研究。结果表明在55℃、70℃,于pH2～9范围内稳定,在50℃、55℃,65℃,pH=1.0,pH=12.0不稳定。其水解反应服从一级反应动力学公式,测得:pH=12.0:50℃,K=4.00×10~(-3)min~(-1),55℃,K=7.68×10~(-3)min~(-1),65℃,K=4.12×10~(-2)min~(-1);pH=1.0:50℃,K=1.76×10~(-3)min~(-1),55℃,K=6.41×10~(-3)min~(-1),65℃,K=2.14×10~(-2)min(-1)。并证明温度对反应速度的影响遵守阿累尼乌斯公式。求出pH=12.0,E_a=3.27×10~4cal/mol,A=3.98×10~(19);pH=1.0,E_a=3.43×10~4cal/mol,A=3.98×10~(20),并建立具体的阿累尼乌斯公式: pH=12.0:1gK=-7.1×10~3·_T~1+19.6 pH=1.0:1gK=-7.5×10~3·(1/T)+20.6     

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.