大火草抗慢性前列腺炎作用研究

目的验证大火草抗慢性前列腺炎作用。方法采用二甲苯致小鼠耳肿胀法、小鼠腹腔毛细血管通透性法、小鼠棉球肉芽肿法、角叉菜胶致大鼠慢性非细菌性前列腺炎法。结果大火草对二甲苯所致小鼠炎症、醋酸所致小鼠腹腔毛细血管通透性的增加、小鼠棉球肉芽肿、角叉菜胶所致大鼠非细菌性前列腺炎均有抑制作用,与模型组比较,差异有统计学意义。结论大火草具有明显抑制前列腺炎的作用。     

前列宁栓抗炎镇痛作用实验

目的:研究前列宁栓的抗炎、镇痛作用。方法:采用二甲苯所致小鼠耳廓肿胀实验、角叉菜胶致大鼠足跖肿实验、大鼠棉球肉芽肿的影响实验、小鼠腹腔毛细血管通透性实验,细菌性(大肠杆菌)前列腺炎的抗炎作用。采用醋酸致小鼠扭体反应实验和小鼠热板法实验观察了前列宁栓的镇痛作用。结果:前列宁栓可明显抑制二甲苯所致的小鼠耳廓炎症;在多数时间降低角叉菜胶致大鼠足跖肿胀;明显抑制大鼠棉球肉芽肿的生成;明显降低小鼠腹腔毛细血管通透性;明显抑制大鼠细菌性前列腺炎;明显降低醋酸致小鼠扭体反应数;明显升高小鼠痛阈值。结论:前列宁栓具有明显的抗炎、镇痛作用。     

咽特佳的抗炎镇痛作用

咽持佳灌胃给药对二甲苯所致小鼠耳肿胀、角叉菜胶所致大鼠足肿胀、醋酸所致小鼠腹腔毛细血管通透性增加具有显著抑制作用.同时明显抑制醋酸所致小鼠扭体反应,对热板法和电刺激引起的小鼠疼痛有明显提高痛阈的作用.     

雷公藤多苷抗炎作用的研究

摘要目的研究雷公藤多苷的抗炎作用。方法①对小鼠毛细血管通透性的影响： 小鼠60只,随机分为空白对照组,模型组,雷公藤多苷0.3,0.6,1.2 g•kg－1组,吲哚美辛10 mg•kg－1组,共6组,各10只,灌胃给药5 d后,均静脉注射0.5%伊文思蓝溶液0.01 mL•g－1,小鼠处死后,收集腹腔冲洗液,测定吸光度（A值）;②对大鼠角叉菜胶足肿胀的影响：大鼠50只,随机分为空白对照组,雷公藤多苷0.25,0.50,1.00 g•kg－1组,地塞米松4 mg•kg－1组,共5组,各10只,造模后,连续灌胃给药7 d,测定右后肢容积。结果空白对照组,模型组,雷公藤多苷0.3,0.6,1.2 g•kg－1组,吲哚美辛10 mg•kg－1组小鼠腹腔冲洗液A值分别为0.24±0.16,1.41±0.60,0.99±0.45,0.93±0.45,0.88±0.58,0.52±0.38,显示雷公藤多苷对小鼠毛细血管通透性有一定抑制作用。末次给药5 h后空白对照组,雷公藤多苷0.25,0.50,1.00 g•kg－1组,地塞米松4 mg•kg－1组大鼠足肿胀率分别为（36.3±13.7）%,（26.3±13.9）%,（37.9±14.5）%,（32.5±12.4）%,（17.2±10.9）%。结论雷公藤多苷具有一定的抗炎作用。     

榼藤的镇痛抗炎及急性毒性的实验研究

目的研究榼藤水提液的镇痛抗炎作用,并进行急性毒性试验。方法采用醋酸致扭体反应、热板法测定痛阈,观察榼藤水提液的镇痛作用;抗炎实验采用二甲苯致鼠耳肿胀、角叉菜胶致大鼠足趾肿胀和腹腔毛细血管通透性等方法;采用Bliss法测定了其半数致死量(LD50)。结果榼藤水提液能减少醋酸所致小鼠的扭体次数,延长热板致痛的时间,明显提高小鼠的痛阈;能抑制二甲苯所致小鼠耳廓肿胀和角叉菜胶引起的大鼠足趾肿胀,并增加醋酸所致小鼠腹腔毛细血管的通透性;其LD50为85.4 g(生药)·kg-1,LD50的95%可信限为71.2～103.1 g(生药)·kg-1。结论榼藤水提液对实验动物模型具有显著的镇痛抗炎作用,且具有一定毒性。     

咽舒宁颗粒抗炎药效试验研究

目的观察咽舒宁颗粒的抗炎作用。方法将实验动物随机分为对照、阳性药和咽舒宁颗粒高、中、低剂量组(8.25,4.12,2.06 g.kg-1),ig 7 d,采用醋酸致小鼠腹腔毛细血管通透性实验、角叉菜胶性足肿胀实验和棉球肉芽肿实验,观察其对不同炎症模型的作用。结果咽舒宁颗粒能明显抑制醋酸致小鼠腹腔毛细血管通透性增高(P<0.05或P<0.01);显著抑制大鼠角叉菜胶性足肿胀程度(P<0.05或P<0.01)和大鼠棉球肉芽肿的形成(P<0.05或P<0.01)。结论咽舒宁颗粒具有明显的抗急慢性炎症作用。     

杠板归抗炎止咳作用的实验研究

目的观察杠板归的抗炎止咳作用。方法采用二甲苯致小鼠耳廓肿胀实验、醋酸致小鼠腹腔毛细血管通透性亢进实验和角叉菜胶致大鼠足趾肿胀实验观察杠板归消炎作用;采用SO2引咳法观察其止咳作用及大鼠毛玻璃管排痰法观察其化痰作用。结果杠板归提取物能明显抑制二甲苯致小鼠耳廓的肿胀度,抑制醋酸所致小鼠腹腔毛细血管通透性的增高,降低角叉菜胶致足趾肿胀大鼠血清和足爪局部炎症组织中前列腺素（PGE2）、丙二醛（MDA）的含量;杠板归能延长SO2引咳的咳嗽潜伏期、减少咳嗽次数、促进大鼠排痰量。结论杠板归有抗炎、止咳化痰作用。     

新癀片药效学及急性毒性实验

目的研究新癀片的镇痛抗炎作用,并观察新癀片的急性毒性试验。方法采用醋酸所致的小鼠扭体反应、热板法测定小鼠的痛阈,观察新癀片的镇痛作用;采用二甲苯致小鼠耳廓肿胀模型、醋酸致小鼠腹腔毛细血管通透性增加模型,观察新癀片的抗炎作用。结果新癀片能减少醋酸所致小鼠扭体次数,明显提高小鼠的痛阈;抑制二甲苯所致小鼠耳廓肿胀和醋酸所致小鼠腹腔毛细血管通透性增加,且无急性毒性反应。结论在本试验条件下,新癀片有显著的镇痛抗炎作用,临床应用具有安全性。     

葛根素注射液拮抗庆大霉素耳蜗毒性的实验研究

目的 探讨葛根素注射液对庆大霉素（GM）所致耳蜗毒性的防护作用. 方法 选择Wistar大鼠50只,随机分成5组（n＝10）. 正常对照组：每日腹腔注射与模型组等量0.9%氯化钠溶液. 模型组：每日腹腔注射硫酸庆大霉素100 mg&#8226;kg^-1. 实验Ⅰ组：每日同时腹腔注射硫酸庆大霉素和葛根素注射液各100 mg&#8226;kg^-1,连续10 d. 实验Ⅱ组：每日腹腔注射硫酸庆大霉素100 mg&#8226;kg^-1,连续10 d后,每日腹腔注射葛根素注射液50 mg&#8226;kg^-1,连续10 d后停药. 实验Ⅲ组：每日腹腔注射硫酸庆大霉素100 mg&#8226;kg-1,连续10 d后,每日腹腔注射葛根素注射液100 mg&#8226;kg^-1,连续10 d后停药. 观察各组耳廓毛细胞的功能. 结果 实验Ⅰ组和实验Ⅲ组大鼠听功能受损明显轻于模型组,DPOAE幅度值降低程度与模型组比较差异有极显著性（P＜ 0.01）. 实验Ⅱ组较模型组DPOAE幅值轻度升高（P＞0.05）. 结论 庆大霉素对耳蜗毛细胞功能有损害作用,葛根素注射液对庆大霉素所致耳蜗毒性有防护作用.     

镇关灵治疗类风湿性关节炎的药效学研究

目的　探索镇关灵治疗类风湿性关节炎 (rheumatoidarthritis ,RA)的作用。方法　以佐剂性关节炎 (AA)、蛋清性关节炎、角叉菜胶性关节炎为实验病理目标 ,建立二硝基氟苯所致小鼠迟发型超敏反应 (DTH)、棉球肉芽肿及醋酸所致小鼠腹腔毛细血管通透性增高和扭体反应等病理模型。结果　镇关灵能显著抑制大鼠佐剂性关节炎、蛋清性关节炎、角叉菜胶所致炎症的足跖肿胀度和棉球肉芽肿 ,抑制由醋酸引起的小鼠扭体反应和腹腔毛细血管通透性增高 ,并可抑制DTH。结论　镇关灵具有良好的抗炎镇痛免疫抑制作用 ,对类风湿性关节炎具有明显的预防和治疗作用。     

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.     

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.