Selectivity determinants of the aldose and aldehyde reductase inhibitor-binding sites

Aldose reductase and aldehyde reductase belong to the aldo-keto reductase superfamily of enzymes whose members are responsible for a wide variety of biological functions. Aldose reductase has been identified as the first enzyme involved in the polyol pathway of glucose metabolism which converts glucose into sorbitol. Glucose over-utilization through the polyol pathway has been linked to tissue-based pathologies associated with diabetes complications, which make the development of a potent aldose reductase inhibitor an obvious and attractive strategy to prevent or delay the onset and progression of the complications. Structural studies of aldose reductase and the homologous aldehyde reductase in complex with inhibitor were carried out to explain the difference in the potency of enzyme inhibition. The aim of this review is to provide a comprehensive summary of previous studies to aid the development of aldose reductase inhibitors that may have less toxicity problems than the currently available ones. Received 4 December 2006; received after revision 12 February 2007; accepted 20 April 2007     

Aminoglycoside antibiotics: old drugs and new therapeutic approaches

Aminoglycoside antibiotics kill bacteria by binding to the ribosomal decoding site and reducing fidelity of protein synthesis. Since the discovery of these natural products over 50 years ago, aminoglycosides have provided a mainstay of antibacterial therapy of serious Gram-negative infections. In recent years, aminoglycosides have become important tools to study molecular recognition of ribonucleic acid (RNA). In an ingenious exploitation of the aminoglycosides’ mechanism of action, it has been speculated that drug-induced readthrough of premature stop codons in mutated messenger RNAs might be used to treat patients suffering from certain heritable genetic disorders. Received 23 January 2007; received after revision 25 February 2007; accepted 29 March 2007     

鸽巴氏杆菌病的诊断和治疗试验

对疑似感染巴氏杆菌的病死种鸽进行剖检,取心、肝、脾、肺等脏器的14份病料,进行细菌分离培养与鉴定,结合流行病学、临床症状、病理变化和药敏试验,确诊为鸽巴氏杆菌病;使用磺胺二甲嘧啶治疗,效果显著。     

溶剂乙醇对斑马鱼胚胎发育的影响

作为一种提取生物活性成分的常用有机溶剂,乙醇是药物筛选中溶解水溶性较差样品的候选助溶剂。本文研究了不同浓度乙醇对斑马鱼胚胎存活、循环系统发育、血管生成等的影响,为其作为溶剂在斑马鱼模型抗血管生成药物筛选中的应用提供参考。结果显示,0.01%乙醇不会造成胚胎的死亡和仔鱼循环系统畸形,0.1%乙醇引起仔鱼心囊水肿,乙醇浓度达到1%时出现胚胎死亡。低于或等于1%乙醇对仔鱼体节间血管生成无抑制作用。以上结果表明,浓度低于或等于0.01%的乙醇不会影响对被筛样品抗血管生成活性和毒性的评价。     

微针给药系统的研究进展

微针是一种具有微米尺度的经皮给药技术,从内部结构可分为实心与空心微针.制作微针的材料主要有硅、金属、聚合物等.微针增强了皮肤对药物尤其是大分子药物的渗透性,不会到达神经分布丰富的皮肤深层组织,并且使用方便,因此是一种高效、无痛、安全的经皮给药方式.微针在胰岛素给药、卵清蛋白的免疫接种、缓控释给药、微量输液等方面的研究为微针经皮给药提供了应用可能.     

铜绿假单胞菌耐药性与抗菌药物使用强度相关性分析

为了给临床合理使用抗菌药物提供科学依据,回顾性调查了医院2016年1月1日至2019年12月31日铜绿假单胞菌耐药率变化趋势及同一时间段抗菌药物年用量,计算使用频度,分析了抗菌药物使用强度与铜绿假单胞菌(Pseudomonas aeruginosa)耐药率的相关性.分析结果显示:铜绿假单胞菌对哌拉西林/他唑巴坦、庆大霉...     

甲地孕酮改善晚期肿瘤患者生活质量的疗效观察

目的:观察国产甲地孕酮改善晚期肿瘤患者生活质量的疗效.方法:110例晚期肿瘤患者分为两组,治疗组60例,常规化疗同时口服甲地孕酮,对照组50例仅行常规化疗,观察两组治疗前后生活质量的变化.结果:治疗组食欲改善占80%,体重增加占70%,生活质量指数评分提高占65%.平均生存时间延长,超过6月占55%,明显优于对照组(P＜0.01),化疗后胃肠道反应及白细胞降低明显低于对照组(P＜0.05).结论:甲地孕酮能明显改善晚期肿瘤恶液质状况、提高生活质量、减少化疗后的不良反应发生率,未见明显毒副作用.     

复合载体预制桩的分析与应用

由于滨州市许多地区原为池塘,后用建筑垃圾杂填土填平场地,不能直接作为地基持力层应用。通过实例,对浅部存在较好桩基持力层的建筑垃圾场地采用复合载体预制桩进行探讨分析。     

比较硝酸银和抗生素治疗小鼠金黄色葡萄球菌和铜绿假单胞菌创伤感染的效果

目的比较硝酸银与抗生素治疗小鼠金黄色葡萄球菌和铜绿假单胞菌皮肤创面感染的效果。方法实验分为3个大组,首先建立动物创伤模型,使创面分别感染金黄色葡萄球菌、感染铜绿假单胞菌以及混合感染两种菌,然后每组用不同浓度的硝酸银及抗生素进行治疗,记录感染创面结痂时间及愈合时间并进行分析。结果对皮肤创面细菌感染,硝酸银可以起到和抗生素同样的治疗效果,且对耐药性铜绿假单胞菌感染的治疗同样有效。结论本实验证实了硝酸银在体内的杀菌作用及广谱抗菌性,随着银粒子及银离子在医疗上的作用被重新认识,在临床中可以将硝酸银与抗生素复合使用,以达到更好的杀菌和抑菌效果。     

Tussah Silk Fibroin Porous Scaffolds Prepared with a Mild Self-assembly Process for Controlled Drug Release

Besides excellent biodegradability and biocompatibility,a useful tissue engineering scaffold should provide favorable surface properties,outstanding mechanical strength and controlled drug release property. In this paper,a mild process to prepare porous tussah silk fibroin（ TSF） scaffolds from aqueous solution was described. The n-butanol was used to control the self-assembly of tussah silk. The scaffolds with different TSF concentrations and the same volume showed differences in pore size and distribution. The maximum porosity of the poprepared porous scaffolds was 80% in this paper. And the pore size of the prepared porous scaffolds with different concentrations was between 10μm and 230 μm. X-ray diffraction（ XRD） analysis revealed that amorphous TSF was crystallized to β-sheet secondary structure upon gelatin. The TSF scaffolds for controlled drug release was studied and the result showed that the time of drug release was significantly longer. The produced TSF scaffolds with sustained drug release have potential application in tissue engineering.