用复性电泳技术研究溶酶体蛋白水解酶的性质和活性

介绍了复性单向电泳（Ｇ－ＰＡＧＥ）和复性双向电泳（ＩＥＦ－Ｇ－ＰＡＧＥ）的概念、原理、方法、应用范围、优缺点和使用该方法应注意的事项。并用该方法定性和定量分析了Ｃ６大白鼠神经胶质瘤细胞酸性溶酶体蛋白水解酶的性质和活性。     

取向电工钢加工过程中第二相粒子的析出行为

利用场发射扫描电镜观察了以MnS为主要抑制剂的普通取向电工钢加工过程中第二相粒子的分布状态,统计了粒子面密度、平均尺寸以及相应的尺寸分布.结果显示,热轧加工造成了大量第二相粒子弥散、细小地析出,同时基体仍保持过饱和状态.冷轧变形会造成第二相粒子的回溶行为,而基体的过饱和状态会减弱回溶现象.中间退火与脱碳退火过程中会同时存在新粒子的形核及已析出粒子的粗化两个过程,而在最终二次再结晶升温阶段则以第二相粒子明显粗化为主.     

一个多用途吡咯烷类氮杂糖中间体的不对称合成

报道了多用途的吡咯烷类氮杂糖中间体6的不对称合成.起始原料(2R,3R,4S)-2-苄氧甲基-3,4-二苄氧基-5-氧代吡咯烷-1-羧酸叔丁酯(8)由手性合成砌块酒石酸酰亚胺7按照先前本实验室报道的方法经4步得到.活化的酰胺8经乙烯基加成、立体选择性还原、环化、氧化断裂双键成醛以及还原醛成醇等步骤得到了氮杂糖中间体(2R,3R,4R,5R)-2-羟甲基-3,4-二苄氧基-5-苄氧甲基吡咯烷-1-羧酸叔丁酯(6).从活化的酰胺8出发,经过5步反应,立体选择性地合成了氮杂糖中间体6,总产率46%.中间体6可用于多个吡咯烷类氮杂糖的合成.     

抗Gleevec(STI-571)耐受的Bcr-Abl蛋白酪氨酸激酶抑制剂研究进展

综述了抗G leevec(ST I-571)耐受的B cr-A b l蛋白酪氨酸激酶抑制剂的研究进展,主要介绍了PD 166326,BM S-354825,AM N 107和ON 012380四种酪氨酸激酶抑制剂.     

Molecular mechanisms in therapy of acid-related diseases

Inhibition of gastric acid secretion is the mainstay of the treatment of gastroesophageal reflux disease and peptic ulceration; therapies to inhibit acid are among the best-selling drugs worldwide. Highly effective agents targeting the histamine H2 receptor were first identified in the 1970s. These were followed by the development of irreversible inhibitors of the parietal cell hydrogen-potassium ATPase (the proton pump inhibitors) that inhibit acid secretion much more effectively. Reviewed here are the chemistry, biological targets and pharmacology of these drugs, with reference to their current and evolving clinical utilities. Future directions in the development of acid inhibitory drugs include modifications of current agents and the emergence of a novel class of agents, the acid pump antagonists. Received 30 May 2007; received after revision 15 August 2007; accepted 13 September 2007     

The neurotrophic receptor TrkB: a drug target in anti-cancer therapy?

Increasing evidence implies altered signaling through the neurotrophic receptor tyrosine kinase TrkB in promoting tumor formation and metastasis. TrkB, sometimes in conjunction with its primary ligand BDNF, is often overexpressed in a variety of human cancers, ranging from neuroblastomas to pancreatic ductal adenocarcinomas, in which it may allow tumor expansion and contribute to resistance to anti-tumor agents. In vitro, TrkB acts as a potent suppressor of anoikis (detachment-induced apoptosis), which is associated with the acquisition of an aggressive tumorigenic and metastatic phenotype in vivo. In view of its predicted contribution to tumorigenicity and metastasis in humans, TrkB corresponds to a potential drug target, and preclinical models have already been established. The encouraging results of pharmacological Trk inhibitors in tumor xenograft models suggest that TrkB inhibition may represent a promising novel anti-tumor therapeutic strategy. This hypothesis is currently being evaluated in clinical trials. Here, we will discuss the latest developments on TrkB in these contexts as well as highlight some critical questions that remain to be addressed for evaluating TrkB as a therapeutic target in cancer. Received 12 October 2005; received after revision 19 December 2005; accepted 11 January 2006     

蕉皮酚酶催化反应的抑制动力学及机理研究

为防止果蔬褐变需抑制多酚氧化酶的活性。本文用新方法从香蕉皮中提取出多酚氧化酶，用氧电极测出酶催化反应的最佳条件是ｐＨ值为７，温度为２５℃；测定反应活化能等于２３．６ｋＪ·ｍｏｌ－１，米氏常数为１．５８×１０－２ｍｏｌＬ－１。研究了九种抑制剂对酶活性的抑制效果，并进一步研究了肉桂酸抑制剂的抑制动力学及机理，得出肉桂酸为竞争性抑制。用原子吸收光谱测出蕉皮酚酶中含有铜离子，并探讨了铜离子的作用。     

人参种子生长抑制物质的特性及其分离鉴定

报道了人参种子生长抑制物质的特性及其主要抑制物质的分离提纯，并测定了其结构。     

次氯酸钠水溶液对碳钢、铜、铝的腐蚀性及缓蚀剂的研究

用挂片失重法测定了次氯酸钠水溶液对碳钢、铜和铝的腐蚀性,葡萄糖酸钠、水杨酸钠和多元醇磷酸酯类缓蚀剂(PC-602)的缓蚀效果及其对次氯酸钠分解率的影响。含有效氯浓度250ppm的次氯酸钠溶液,加入150～250ppm PC-602,对碳钢的缓蚀率可达92～94%。PC-602对次氯酸钠的稳定性无影响,葡萄糖酸钠和水杨酸钠复配具有协同增效作用.但可加速次氯酸钠的分解速率。次氯酸钠溶液对铜和铝两种金属的腐蚀性较小。