白族药紫地榆体内镇痛抗炎作用初步研究

目的：初步观察紫地榆的体内镇痛、抗炎作用。方法：采用醋酸扭体法观察紫地榆镇痛作用,采用二甲苯致小鼠耳肿胀法,醋酸致小鼠腹腔毛细血管通透性增加,小鼠棉球肉芽肿法观察紫地榆的抗炎作用。结果：抗炎实验中,与对照组比较,紫地榆高、中、低剂量组均可明显抑制二甲苯所致小鼠耳廓的肿胀度,抑制醋酸引起的小鼠毛细血管通透性增加;与模型组比较,紫地榆能减轻小鼠棉球肉芽肿质量。镇痛实验中,与对照组比较,紫地榆可延缓醋酸所致小鼠扭体反应的潜伏期,减少扭体反应次数。结论：紫地榆提具有明显的体内抗炎镇痛作用。     

苦玄参提取物对小鼠的抗炎及镇痛作用

目的:研究苦玄参提取物对小鼠的抗炎及镇痛作用。方法:采用二甲苯诱导小鼠耳郭肿胀试验模型和腹腔毛细血管通透性试验观察抗炎作用;采用小鼠扭体试验观察镇痛作用。结果:苦玄参提取物能明显抑制二甲苯致小鼠耳肿胀和醋酸致小鼠腹腔毛细血管通透性增加;能减少冰醋酸刺激致痛小鼠的扭体次数。结论:苦玄参提取物对小鼠具有较好的抗炎及镇痛作用。     

雪莲培养物的抗炎镇痛作用研究

目的：研究雪莲培养物的抗炎镇痛作用。方法：采用乙酸致小鼠腹腔毛细血管通透性,角叉菜胶致大鼠足趾肿胀率和乙酸扭体法来考察抗炎镇痛作用。结果：雪莲培养物对乙酸引起的小鼠腹腔毛细血管通透性和角叉菜胶致大鼠足趾肿胀率有明显抑制作用,减少了小鼠扭体反应次数,并能显著使角叉菜胶致大鼠炎性肿胀足痛阈降低。结论：雪莲培养物具有显著的抗炎镇痛作用。     

山芝麻的抗炎镇痛作用研究

目的研究山芝麻的抗炎镇痛作用。方法山芝麻高剂量31.2 g生药/kg、中剂量15.6 g生药/kg、低剂量7.8 g生药/kg,连续灌胃7 d抗炎实验采用二甲苯致小鼠耳廓肿胀模型和醋酸致小鼠腹腔毛细血管通透性增高模型,镇痛实验采用热板法和扭体法。结果山芝麻能显著抑制二甲苯引起的小鼠耳廓肿胀,抑制醋酸引起的小鼠腹腔毛细血管通透性增高,并降低小鼠热板痛阈值,减少醋酸引起的扭体次数。结论山芝麻具有抗炎镇痛作用。     

山桔叶醇提物抗炎镇痛作用的研究

目的 观察山桔叶醇提物(GPE)对小鼠的抗炎镇痛作用.方法 通过二甲苯致小鼠耳廓肿胀、0.6％冰乙酸致小鼠腹腔毛细血管通透性、1％角叉菜胶致小鼠足肿胀及用小鼠棉球肉芽肿法观察GPE的抗炎作用;通过冰乙酸致小鼠扭体反应和热板致小鼠疼痛法观察GPE的镇痛作用.结果 GPE高、中、低剂量均可显著抑制二甲苯致小鼠耳廓肿胀的肿胀度、1％角叉菜胶致小鼠的足肿胀、0.7％冰乙酸致小鼠的扭体反应次数;GPE高、低剂量可显著抑制冰乙酸致小鼠腹腔毛细血管通透性的增高;GPE高、中剂量均可抑制角叉菜胶致小鼠足肿胀中PGE2的渗出及小鼠棉球肉芽肿的重量,可增高热板致小鼠疼痛的痛阈值.结论 GPE对小鼠有抗炎镇痛的作用.     

咽喉汤抗炎抗菌作用的实验考察

目的:通过对咽喉汤的抗炎抗菌作用进行药效学研究,为其应用于临床提供实验依据.方法:采用二甲苯致小鼠耳廓肿胀实验模型、大鼠棉球肉芽肿实验模型、醋酸致小鼠腹腔毛细血管通透性的影响实验模型考察咽喉汤的抗炎作用;观察咽喉汤在体外对乙型溶血性链球菌、金黄色葡萄球菌、大肠埃希菌、肺炎双球菌、铜绿假单胞菌的抑菌和杀菌作用.结果:咽喉汤可明显抑制二甲苯所致小鼠耳廓肿胀、棉球肉芽组织增生、毛细血管通透性增高,且其有广谱抑菌作用和杀菌活性.结论:咽喉汤具有一定的抗炎和抑菌杀菌作用.     

两头尖提取物的抗炎镇痛作用初探

目的研究两头尖提取物的抗炎镇痛作用。方法采用二甲苯致小鼠耳肿胀实验、醋酸致小鼠腹腔毛细血管通透性增高实验、新鲜蛋清致大鼠足跖肿胀实验、大鼠棉球肉芽增生实验考察两头尖提取物的抗炎作用,用小鼠扭体实验考察其镇痛作用。结果实验表明,两头尖提取物对各种炎症模型均有显著的抑制作用,并能显著减少醋酸致小鼠扭体反应次数。结论两头尖提取物有良好的抗炎镇痛作用。     

骨湿宁治疗风湿性关节炎的实验研究

目的：观察骨湿宁的主要药理作用。方法：采用佐剂，角叉菜胶，尿酸钠等引发大鼠关节炎症或疼痛模型，小鼠热板，醋酸扭体法以及腹腔毛细血管通透性来评价骨湿宁的抗炎，镇痛作用。结果：骨湿宁能抑制大鼠佐剂性关系炎的原发性和继发性病变；抑制角叉菜胶所致的大鼠炎症肿胀；对由大鼠尿酸钠关节炎致痛，小鼠热板，醋酸扭体致痛均有明显的镇痛作用；并具有降低小鼠腹腔毛细血管通透性，抑制大鼠棉球致组织增生的作用。结论：骨湿宁具有一定的抗炎，镇痛作用。     

口溃宁颗粒对小鼠的抗炎和镇痛作用

目的:探讨口溃宁颗粒的抗炎、镇痛作用。方法:采用小鼠腹腔毛细血管通透性及二甲苯致小鼠耳肿胀试验探讨抗炎作用,采用冰醋酸扭体法和福尔马林致痛试验研究镇痛作用。结果:口溃宁颗粒可明显抑制毛细血管通透性增加、减轻小鼠耳廓肿胀度,减少小鼠扭体反应次数及福尔马林致痛试验的第二时相的疼痛强度。结论:口溃宁颗粒具有较好的镇痛、抗炎作用。     

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。     

Efficacy of gut lavage,hemodialysis, and hemoperfusion in the therapy of paraquat or diquat intoxication

Clinical and in vitro investigations were carried out to test the efficacy of gut lavage, hemodialysis, and hemoperfusion in the treatment of poisoning with paraquat or diquat. In a patient suffering from diquat intoxication 130 times more diquat was removed by gut lavage 30 h after ingestion than was removed by complete aspiration of the gastric contents.Determination of in vitro clearances for paraquat and diquat by hemodialysis showed that, at serum concentrations of 1–2 ppm, such as are frequently encountered in poisoning in man, toxicologically relevant quantities of herbicide cannot be removed from the body. At a concentration of 20 ppm, on the other hand, hemodialysis proved to be effective, the clearance being 70 ml/min at a blood flow rate of 100 ml/min. The efficacy of hemoperfusion with coated activated charcoal was on the whole better. Especially at concentrations around 1–2 ppm, the clearance values for hemoperfusion were some 5–7 times higher than those for hemodialysis.In a patient suffering from paraquat poisoning, both hemodialysis as well as hemoperfusion were carried out. The in vitro results could be confirmed: At serum concentrations of paraquat less than 1 ppm no clearance could be obtained by hemodialysis while by hemoperfusion with activated charcoal quite high clearance values were measured and the serum level dropped down to zero.

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Zusammenfassung Klinische Untersuchungen und Laboratoriumsversuche wurden durchgeführt, um die Wirksamkeit von Darmspülung, Hämodialyse und Hämoperfusion bei Paraquat- und Deiquat-Vergiftungen zu prüfen.Bei einem Patienten wurde 30 Std nach Deiquat-Aufnahme durch Darmspülung 130mal mehr Deiquat entfernt als durch vollständige Aspiration des Mageninhaltes. In vitro-Versuche ergaben, daß bei Blutserumkonzentrationen von 1–2 ppm, die bei Vergiftungen oft gemessen werden, durch Hämodialyse keine toxikologisch relevanten Paraquat- oder Deiquat-Mengen entfernt werden können. Dagegen erwies sich die Hämodialyse bei 20 ppm und einer Blutumlaufgeschwindigkeit von 100 ml/min mit einer Clearance von 70 ml/min als wirksam. Die Hämoperfusion mit beschicheter Aktivkohle war in diesen Versuchen aber eindeutig überlegen, denn insbesondere bei Konzentrationen um 1–2 ppm waren die Clearance-Werte 5–7mal höher als bei der Hämodialyse.Die in vitro-Ergebnisse wurden bei einem Patienten mit einer Paraquat-Vergiftung bestätigt: Bei Konzentrationen unter 1 ppm war die Hämodialyse wirkungslos, während durch Hämoperfusion relativ hohe Clearance-Werte erreicht wurden, so daß der Serumspiegel rasch unter die Nachweisgrenze abfiel.

     

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.     

Aquatic Insects and Trace Metals: Bioavailability,Bioaccumulation, and Toxicity

Abstract

The uptake of metals from food and water sources by insects is thought to be additive. For a given metal, the proportions taken up from water and food will depend both on the bioavailable concentration of the metal associated with each source and the mechanism and rate by which the metal enters the insect. Attempts to correlate insect trace metal concentrations with the trophic level of insects should be made with a knowledge of the feeding relationships of the individual taxa concerned. Pathways for the uptake of essential metals, such as copper and zinc, exist at the cellular level, and other nonessential metals, such as cadmium, also appear to enter via these routes. Within cells, trace metals can be bound to proteins or stored in granules. The internal distribution of metals among body tissues is very heterogeneous, and distribution patterns tend to be both metal and taxon specific. Trace metals associated with insects can be both bound on the surface of their chitinous exoskeleton and incorporated into body tissues. The quantities of trace meals accumulated by an individual reflect the net balance between the rate of metal influx from both dissolved and particulate sources and the rate of metal efflux from the organism. The toxicity of metals has been demonstrated at all levels of biological organization: cell, tissue, individual, population, and community. Much of the literature pertaining to the toxic effects of metals on aquatic insects is based on laboratory observations and, as such, it is difficult to extrapolate the data to insects in nature. The few experimental studies in nature suggest that trace metal contaminants can affect both the distribution and the abundance of aquatic insects. Insects have a largely unexploited potential as biomonitors of metal contamination in nature. A better understanding of the physico-chemical and biological mechanisms mediating trace metal bioavailability and exchange will facilitate the development of general predictive models relating trace metal concentrations in insects to those in their environment. Such models will facilitate the use of insects as contaminant biomonitors.     

Alzheimer’s disease – current trends in basic and clinical research. Highlights from the 16th ECNP

Advances in the molecular biological knowledge of neuronal nicotinic acetylcholine receptors (nAChRs) have led to a growing interest by the pharmaceutical industry in the development of novel compounds that selectively modulate nAChR function. The ability of (-)-nicotine, an activator of nAChRs, to enhance attentional aspects of cognition in animals and humans, to exert neuroprotective and anxiolytic-like effects, and presumably to mediate the negative correlation between smoking and Alzheimer's (and Parkinson's) Disease, has focused interest on the potential therapeutic utility of modulators of nAChR function for treatment of some of the deficits associated with these progressive, neurodegenerative conditions. Numerous compounds are known which activate nAChRs and which might serve as lead compounds toward the development of such agents. The pharmacologic diversity of neuronal nAChR subtypes suggests the possibility of developing selective compounds which would have more favourable side-effect profiles than existing agents. This broader class of agents, collectively called cholinergic channel modulators (ChCMs), is anticipated to encompass compounds which would have more favourable side-effect profiles than existing agents, which generally exhibit low selectivity. This selectivity may be achieved by preferentially activating some subtypes of nAChRs (i.e., Cholinergic Channel Activators, ChCAs) or inhibiting the function of other subtypes (Cholinergic Channel Inhibitors, ChCIs). An overview of the biology of nAChRs and the rationale for the use of ChCMs for the treatment of dementia related to neurodegenerative diseases are presented, followed by a discussion of lead compounds and compounds under consideration for clinical evaluation.     

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.