Intramolecular Thermal Condensation of 3-Acetyl-5-Oxopyrazolo[1,5-a]quinoline-4-ethylcarboxylate: a Simple Pathway to the New Tetracyclic System Containing Fluoroquinolone Fragment

Pharmaceutical Chemistry Journal -     

感染日本血吸虫的家兔治疗前后肝纤维化动态观察

感染日本血吸虫的家兔治疗前后肝纤维化Ｂ超声像图模型、血清ＭＡＯ水平及病理学结果表明，血吸虫引起的肝纤维化变化过程与血清ＭＡＯ水平升降趋势趋向一致，均在１８周达到高峰。解剖与病理学检查结果基本相符，血吸虫性肝纤维化形成后，只要及时给予杀虫治疗，肝纤维化部分可发生逆转。     

Loss of Anticoagulant Effect of Heparin During Circulation of Human Blood In Vitro

Device-induced thrombogenesis was studied in an in vitro model using human blood circulated through an artificial ventricle. A new constant pressure filtration technique was used to detect circulating microemboli, the activated partial thromboplastin time (APTT) test was used to monitor the blood for the presence of anticoagulant activity of heparin, and hemolysis was quantified by measuring the plasma free hemoglobin level. Circulation of blood through a 20-ml stroke volume pneumatically driven ventricle for 6-9 h resulted in a significant reduction of APTT, indicating the loss of the anticoagulant effect of heparin. Microemboli concentration was minimal until the APTT decreased below 125 s, at which time the microemboli concentration increased rapidly. This was presumed to be due to the formation of thrombi following a decrease in heparin activity. A significant increase in hemolysis was also noted when blood was pumped. None of these changes was noted in the nonpumped control blood. Spontaneous loss of heparin activity in blood circulated by a pneumatically driven pump may have clinical implications and may help understanding of the problems associated with device-induced thrombogenesis.     

Effects of acute barbiturate administration, tolerance and dependence on brain GABA system: comparison to alcohol and benzodiazepines

Central nervous system depressants, e.g., barbiturates, alcohol and benzodiazepines, have a wide spectrum of activity in humans and animals. Evidence accumulated suggests that some of the pharmacological actions exerted by these agents may be mediated through GABA system by mimicking GABAergic transmission. This review attempts to summarize the evidence available as to how the GABA system plays a part in the barbiturate actions and the development of tolerance to and physical dependence on barbiturates. The comparisons of the effects of alcohol, barbiturates and benzodiazepines at different steps of GABA synapse are also presented. Furthermore, the results which have been reported in the literature are inconsistent. This may be due to differences in: (a) animal models used; (b) brain regions used; (c) protocols (dose, duration, form and route of administration, etc.) used in treating animals and/or (d) techniques (pharmacological, biochemical, physiological, etc.) used.     

Elicitins from Phytophthora and basic resistance in tobacco.

Elicitins are a family of small proteins secreted by species of Phytophthora. They are thought to be major determinants of the resistance response of tobacco against these oomycetes, since purified elicitins, alone and at low concentrations, can induce vigorous defense responses in tobacco (i.e., hypersensitive cell death and resistance against subsequent pathogen attack), and in vitro elicitin production by Phytophthora isolates is strongly negatively correlated with their pathogenicity on tobacco plants. A number of elicitins have been purified and their amino acid sequences have been determined and found to be conserved. A three-dimensional structure for elicitin is emerging from nuclear magnetic resonance studies. Two structural classes, alpha and beta, are distinguished by their biological effects when applied to decapitated stems or petioles; the beta class causes more necrosis on leaves and provides better subsequent protection against pathogen attack. However, both these classes of elicitins will similarly cause necrosis when each is, instead, directly infiltrated into tobacco leaf panels. Effects of elicitins on tobacco cells include rapid electrolyte leakage, changes in protein phosphorylation and amounts of active oxygen species, and later production of ethylene and capsidiol. The sites of initial interaction with tobacco cells are unknown, but the interaction appears to induce general defense-related responses.     

人细胞色素p450IA1基因cDNA的克隆和鉴定

在用３－甲基胆蒽诱导培养人羊膜ＦＬ细胞２４ｈ后，抽提细胞总ＲＮＡ并直接合成ｃＤＮＡ第一链。利用人工合成的一对寡核苷酸引物，采用ＰＣＲ技术特异性地扩增Ｃｙｔ ｐ５０ＩＡ１ ｃＤＮＡ。３０个循环后琼脂糖凝胶电泳显示１．５Ｋｂ大小片段，长度与预计相符。Ｓｏｕｔｈｅｒｎ杂交结果证实此片段确为Ｃｙｔ ｐ４５０ＩＡ１ ｃＤＮＡ。将此片段克隆至质粒ｐＧＥＭ－３Ｚ并进行部份序列分析。结果显示克隆片段包含Ｃｙｔ ｐ     

噻吗洛尔与普萘洛尔治疗高血压病与心绞痛的疗效比较

劳累性心绞痛38例采用噻吗洛尔2.5-5mg, tid,共4wk;另12例采用普萘洛尔10-20mg, tid,共4wk。结果:前者显效率为79％,显著高于后者42％(P<0.05)。高血压病(Ⅰ,Ⅱ期)37例采用噻吗洛尔治疗,方法同上;另13例采用普萘洛尔20-40mg, tid,疗程亦4wk。结果:2组均有显著降压疗效(P<0.01),噻吗洛尔治疗后1h即获显效,普萘洛尔须24h才获显效。噻吗洛尔7％(5/75)、普萘洛尔4％(1/25)治疗后发生窦性心动过缓,前者被迫停药,后者未停药。     

电针改善硬膜外吗啡用于术后镇痛所引起的免疫抑制

为观察硬膜外吗啡和电针对术后患者免疫功能的影响，检测自然杀伤细胞（ＮＫｃｅｌｌ）活性和ＰＨＡ诱导白细胞介素２（ＩＬ－２）水平在单纯胆囊切除术患者术前和术后第１、３、７天的动态变化情况。结果吗啡组ＮＫ活性在术后第１、３、７天抑制，手术组仅在术后第１、３天出现抑制，而抑制率低于同天的吗啡组，电针可拮抗吗啡引起的ＮＫ活性抑制加深状况。在术后第１天，手术组和吗啡组ＩＬ－２水平均下降，吗啡＋电针组无明显变化，术后第７天吗啡＋电针组ＩＬ－２升高接近正常人水平。表明电针能改善硬膜外吗啡引起的免疫抑制，促进术后机体的恢复。硬膜外吗啡结合电针是值得推荐的术后镇痛方法。     

大鼠心脏不同部位α1肾上腺素受体亚型的分布

用放射配体结合实验研究大鼠心脏不同部位α１肾上腺素受体（α１受体）及其亚型的分布。结果表明，大鼠心脏左、右心房及心室中α１受体的密度基本一致；不同部位的α１受体均包含α１Ａ与α１Ｂ两种亚型，左心房及心宝α１Ａ亚型占全部α１受体的３０％左右，α１Ｂ亚型占７０％左右；而在右心房中α１Ａ亚型的比例为１４％左右，显著低于左心房与心室。说明大鼠心脏不同部位的α１受体分布相同，但其亚型分布具有显著的区别。