小蓟的现代研究与应用分析

小蓟作为食材,含有丰富的氨基酸、维生素,微量元素等,有很好的食疗价值,但缺少如何保鲜、鲜药加工品、鲜药制剂的研究。小蓟以及以小蓟为君药的小蓟饮予临床用于肾炎,能明显减轻肾炎患者的血尿、蛋白尿等症状,可较好缓解肾炎症状;小蓟作为可食用之品,对机体的不良反应很少,可用于肾炎患者的治疗或辅助治疗。     

盐酸替马沙星的新法合成

以２,４－二氯－５－氯苯甲酰乙酸乙酯为原料,经缩合、胺化,环合、螯合,取代,水解及成盐反应合成盐酸替马沙星。经元素分析,红外光谱,质谱和核磁共振谱确证结构,总收率４５％。该工艺路线副反应少,产品纯度高。     

浅谈抗菌药物管理信息系统建设

以卫生部颁布规范为基础进行我院抗菌药物管理信息系统设计和实施,并在此基础上结合医院信息系统和应用环境,实现了相应的信息系统功能及配套具备消息机制平台和抗菌药物控制细化扩展功能。经过近1年使用,建立了整合医院信息资源的平台,并利用其中的扩展功能为抗菌药物进一步深入管控做出了有益的探索。     

清热解毒复方对头孢拉定的抑菌增效作用及机理

目的 研究清热解毒中药复方对头孢拉定的体外抑菌增效作用及其机制.方法 采用棋盘法观察中药复方与头孢拉定联用对金黄色葡萄球菌的抑菌作用;利用生物大分子分析、糖代谢、AKP的含量测定等方法,来验证清热解毒中药复方的药效作用.结果 清热解毒中药复方与头孢拉定两药联用对金黄色葡萄球菌的抑菌浓度指数(FIC)为0.125;中药复方作用金黄色葡萄球菌后,DNA和RNA的含量比正常组仅增加0.47%,糖浓度仅增加5.47%,AKP含量比正常组增加484.7%;菌体可溶性蛋白表达与正常组相比有明显变化.结论 清热解毒中药复方对头孢拉定有协同抑菌作用,其机理与增加细胞壁透性、影响蛋白质表达有关.     

Zeolite-Supported Aggregate as Potential Antimicrobial Agents in Gypsum Composites

Relatively easy treatment of glass aggregates can lead to the formation of a highly porous zeolite aggregate. This study focuses on the possibility of using such an aggregate as an active additive to a gypsum binder. The physical properties of hardened gypsum composites with zeolite fillers doped with various metal ions (Ni²⁺, Cu²⁺, and Zn²⁺) have been compared. In addition to studies of the basic physical properties of the composites, structural and microstructural studies as well as antimicrobial tests were performed. It was found that the parameters of the composites with the addition of various ions do not differ significantly from the reference but modifies the microstructure. Among other things, the ions analyzed reduce the microporosity of gypsum composites. Using all aggregates, a product with adequate strength (above 2 MPa) and thermal conductivity (about 0.35 W/m·K) appropriate for typical lightweight gypsum composites can be obtained. The bacteriostatic effect of formulations with copper and zinc against Escherichia coli and with copper against Staphylococcus aureus was found.     

复方一枝蒿颗粒剂的体外抗菌作用

目的检测复方一枝蒿颗粒剂的体外抗菌作用。方法采用MH(Mueller-Hamilton)肉汤和MH营养琼脂平板倍比稀释培养法。结果复方一枝蒿颗粒剂对金黄色葡萄球菌的最小抑菌浓度(MIC)为1∶16,最小杀菌浓度(MBC)为1∶8;肺炎链球菌的MIC为1∶16,MBC为1∶8;乙型溶血性链球菌的MIC为1∶8,MBC为1∶4;大肠埃希菌的MIC≤1∶2MBC≤1∶2。结论复方一枝蒿颗粒剂对金黄色葡萄球菌、乙型溶血性链球菌和肺炎链球菌有明显抑制作用。     

抗菌肽LL-37对耐甲氧西林金黄色葡萄球菌生物膜的抑制作用

目的 研究人抗菌肽LL-37对耐甲氧西林金黄色葡萄球菌(MRSA)生物膜的相关作用,为MRSA的预防治疗以及新药物开发应用提供新策略.方法 运用微量肉汤稀释法测定LL-37对临床MRSA菌株的最小抑菌浓度;建立96孔板及6孔板生物膜体外模型;通过结晶紫定量法以及激光共聚焦荧光染色法检测LL-37对MRSA生物膜形成的影响.结果 微量肉汤稀释法测得LL-37对临床MRSA菌株的MIC为12.5 μmol/L.不同浓度LL-37作用后,结晶紫定量法结果表明1/20 MIC亚抑菌浓度的LL-37即可抑制生物膜形成(P＜0.01),且抑制率随用药浓度增加也随之提高,在1/4 MIC条件下生物膜形成抑制率可达到63％.与生理盐水对照组相比,激光共聚焦扫描显微镜下可见,用药组生物膜排列稀疏,厚度变薄,组成菌量明显减少.结论 低浓度的LL-37能够抑制MRSA生物膜的形成,并且对成熟生物膜结构也具有一定的破坏作用.     

Carbapenem-Resistant Enterobacteriaceae in Children,United States, 1999–2012

The prevalence of carbapenem-resistant Enterobacteriaceae (CRE) infections is increasing in the United States. However, few studies have addressed their epidemiology in children. To phenotypically identify CRE isolates cultured from patients 1–17 years of age, we used antimicrobial susceptibilities of Enterobacteriaceae reported to 300 laboratories participating in The Surveillance Network–USA database during January 1999–July 2012. Of 316,253 isolates analyzed, 266 (0.08%) were identified as CRE. CRE infection rate increases were highest for Enterobacter species, blood culture isolates, and isolates from intensive care units, increasing from 0.0% in 1999–2000 to 5.2%, 4.5%, and 3.2%, respectively, in 2011–2012. CRE occurrence in children is increasing but remains low and is less common than that for extended-spectrum β-lactamase–producing Enterobacteriaceae. The molecular characterization of CRE isolates from children and clinical epidemiology of infection are essential for development of effective prevention strategies.     

In silico identification,synthesis and biological evaluation of novel tetrazole inhibitors of MurB

In the context of antibacterial drug discovery resurgence, novel therapeutic targets and new compounds with alternative mechanisms of action are of paramount importance. We focused on UDP‐N‐acetylenolpyruvylglucosamine reductase (i.e. MurB), an underexploited target enzyme that is involved in early steps of bacterial peptidoglycan biosynthesis. On the basis of the recently reported crystal structure of MurB in complex with NADP⁺, a pharmacophore model was generated and used in a virtual screening campaign with combined structure‐based and ligand‐based approaches. To explore chemical space around hit compounds, further similarity search and organic synthesis were employed to obtain several compounds with micromolar IC₅₀ values on MurB. The best inhibitors in the reported series of 5‐substituted tetrazol‐2‐yl acetamides were compounds 13 , 26 and 30 with IC₅₀ values of 34, 28 and 25 μm , respectively. None of the reported compounds possessed in vitro antimicrobial activity against Staphylococcus aureus and Escherichia coli.     

Antibacterial Drug Discovery & Development Summit

Over 100 senior researchers and managers from academic and industrial research organisations attended this 2-day annual international discovery summit on antibacterial R&D. A number of firms, particularly biotechnology firms, presented compounds that are advancing through clinical development. In addition, areas for basic research and development included metallo-β-lactamases, ribosomal structural studies and phage-selected targets were described.