牛黄解毒滴丸解热镇痛和抗炎作用实验

目的：观察牛黄解毒滴丸的解热镇痛和抗炎作用。方法：采用2,4-二硝基酚大鼠致热法观察其解热作用;小鼠扭体法、热板刺激法观察其镇痛作用;小鼠耳部肿胀法、大鼠蛋清足肿胀法观察其抗炎作用。结果：牛黄解毒滴丸显著降低2,4-二硝基酚所致大鼠升高的体温;明显减轻和抑制热板所致的小鼠疼痛及醋酸所致的小鼠扭体反应;抑制二甲苯所致的小鼠耳肿胀和蛋清所致的大鼠足肿胀。结论：牛黄解毒滴丸对实验大鼠、小鼠具有良好的解热、镇痛和抗炎作用。     

三叶青提取物抗炎、镇痛及解热作用的实验研究

目的:探讨三叶青提取物(ERT)的抗炎、镇痛及解热作用,并验证其相关功效.方法:以小鼠腹腔毛细血管通透法、小鼠耳肿胀法及大鼠足肿胀法观察其抗炎作用;以小鼠扭体法、热板法观察其镇痛作用;以干酵母致热法及2,4-二硝基苯酚致热法观察其解热作用.结果:三叶青提取物能明显抑制小鼠腹腔毛细血管炎性渗出,抑制二甲苯所致小鼠耳廓肿胀及10%蛋清致大鼠足跖肿胀;减少醋酸致小鼠扭体次数,提高热板法小鼠痛阈值;并降低干酵母和2,4-二硝基苯酚致大鼠发热模型的体温.结论:三叶青提取物具有较好的抗炎、镇痛及解热作用,与其相关的中医临床功效及主治相符.     

沙枣水提物抗炎、镇痛、解热及抗菌作用研究

目的研究沙枣水提物抗炎、镇痛、解热及抗菌作用。方法采用小鼠二甲苯致耳肿、角叉菜胶致足跖肿胀、乙酸致腹腔毛细管炎性渗出,实验观察抗炎作用;用小鼠扭体实验观察镇痛作用;用2,4-二硝基苯酚及干酵母片致大鼠发热实验观察解热作用,用正常小鼠肠道水分吸收实验观察对肠道水分吸收功能的影响;用常见肠道菌的抗菌实验观察抗菌作用。结果沙枣水提物能抑制二甲苯引起的耳肿胀(P<0.05)、角叉菜胶致小鼠足跖肿(P<0.05)和乙酸致腹腔毛细管炎性渗出(P<0.05);能减少乙酸诱发小鼠扭体反应次数(P<0.05);高剂量对干酵母致大鼠发热有退热作用;对痢疾杆菌的MIC为23.75 g.L-1,MBC为47.5 g.L-1。其对小鼠肠道水分吸收功能没有影响。结论沙枣水提物具有抗炎、镇痛、解热及抗福氏痢疾杆菌的作用。     

银胡感冒海绵剂解热、抗炎、镇痛作用的实验研究

目的：研究银胡感冒海绵剂在解热、镇痛、抗炎等方面的作用,为临床用药提供实验依据。方法：采用2,4-二硝基苯酚致大鼠发热法观察银胡感冒海绵剂的解热作用,小鼠耳肿胀法、大鼠足跖肿胀法观察银胡感冒海绵剂的抗炎作用,小鼠扭体法、小鼠热板法、观察银胡感冒海绵剂的镇痛作用。结果：银胡感冒海绵剂对2,4-二硝基苯酚所致大鼠的发热反应有明显的解热作用;对巴豆油所致小鼠耳壳肿胀和对角又菜胶所致大鼠足跖肿胀均有显著的抑制作用;能显著抑制醋酸所致的小鼠扭体反应次数并能显著提高小鼠热板痛阈值。结论：银胡感冒海绵剂具有显著的解热、抗炎和镇痛作用。     

六应丸抗炎和镇痛活性的实验研究

目的：观察六应丸的抗炎和镇痛作用,为其在临床应用提供实验依据。方法：采用醋酸致小鼠扭体模型和热刺激致疼痛模型,考察其镇痛活性;采用二甲苯所致的小鼠耳肿胀和酵母所致大鼠足趾肿胀,考察其抗炎作用,并和六神丸的疗效进行比较。结果：六应丸能有效抑制醋酸引起的小鼠扭体反应、二甲苯所致的小鼠耳肿胀和酵母所致大鼠足趾肿胀,其抗炎镇痛作用与六神丸无显著差异。结论：六应丸具有显著的抗炎镇痛作用。     

双黄连口服液解热抗炎作用的实验研究

目的 探讨双黄连口服液的解热抗炎作用.方法 采用2,4-二硝基苯酚致大鼠发热法研究双黄连口服液的解热作用,采用二甲苯致小鼠耳肿胀法和角叉菜胶致大鼠足肿胀法研究双黄连口服液的抗炎作用.结果 与空白对照组比较,双黄连口服液能显著降低2,4-二硝基苯酚致大鼠发热模型的体温(P＜0.05),并能显著抑制二甲苯致小鼠耳肿胀及角叉菜胶致大鼠足肿胀的炎症反应(P＜0.05).结论 双黄连口服液具有显著的解热、抗炎作用.     

NO偶联双氯芬酸衍生物抗炎、镇痛、解热作用实验研究

目的：考察NO偶联双氯芬酸衍生物(澳通，CO-3)的抗炎、镇痛、解热作用。方法：通过小鼠耳二甲苯致炎、角叉菜胶致大鼠足跖肿胀、大鼠棉球肉芽肿及Ⅱ型胶原所致的大鼠关节炎等实验模型，观察CO-3的抗炎作用；通过小鼠醋酸扭体、热板刺激和大鼠甩尾等实验模型，观察CO-3的镇痛作用；通过大鼠啤酒酵母致热实验模型，观察CO-3的解热作用。结果：CO-3可明显抑制二甲苯所致小鼠耳肿胀、角叉菜胶致大鼠足跖肿胀、大鼠棉球肉芽组织增生及Ⅱ型胶原所致的大鼠关节炎；能显著抑制醋酸引起的小鼠扭体反应及提高甩尾及热板刺激的致痛阈值；对啤酒酵母致热大鼠有明显的解热作用。结论：CO-3具有良好的抗炎、镇痛、解热作用。     

双氯芬酸钾喷雾剂抗炎镇痛的药效学研究

目的观察双氯芬酸钾喷雾剂的抗炎镇痛作用.方法采用二甲苯致小鼠耳肿胀、角叉菜胶致大鼠足肿胀和小鼠热板法模型观察双氯芬酸钾喷雾剂的抗炎、镇痛作用.结果双氯芬酸钾喷雾剂对二甲苯致小鼠耳肿胀和角叉菜胶致大鼠足肿胀均有明显的抑制作用,并能增加热刺激小鼠的痛阈.结论双氯芬酸钾喷雾剂具有明显的抗炎、镇痛作用,作用强度与双氯芬酸二乙胺乳胶剂相似.     

双氯芬酸钾喷雾剂抗炎镇痛的药效学研究

目的　观察双氯芬酸钾喷雾剂的抗炎镇痛作用。方法　采用二甲苯致小鼠耳肿胀、角叉菜胶致大鼠足肿胀和小鼠热板法模型观察双氯芬酸钾喷雾剂的抗炎、镇痛作用。结果　双氯芬酸钾喷雾剂对二甲苯致小鼠耳肿胀和角叉菜胶致大鼠足肿胀均有明显的抑制作用,并能增加热刺激小鼠的痛阈。结论　双氯芬酸钾喷雾剂具有明显的抗炎、镇痛作用,作用强度与双氯芬酸二乙胺乳胶剂相似     

金胆片浸膏的主要药效学研究

目的观察金胆片浸膏对小鼠的镇痛、抗炎作用以及对大鼠的利胆作用。方法采用二甲苯致炎剂,观察金胆片浸膏对由此而产生耳廓肿胀作用的影响;观察金胆片浸膏对醋酸刺激所致疼痛的影响;观察金胆片浸膏对大鼠胆汁流量的影响。结果金胆片浸膏对二甲苯所致的小鼠耳肿胀有明显的抑制作用,对醋酸所致小鼠扭体反应也有明显抑制作用,能明显增加大鼠胆汁流量。结论金胆片浸膏具有镇痛、抗炎、利胆作用。     

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.