抗菌新药替考拉宁市场前景看好

替考拉宁在与氨基糖苷类药物合用时，比万古霉素等其它糖肽类抗生素对肾功能的影响要小得多，且很少引起糖肽类抗生素所致的过敏反应。     

糖肽类抗生素雷莫拉宁的研究

雷莫拉宁(Ramoplanin、A 16686、MDL 62,198)是一种新型的糖肽类抗生素,能够特异而迅速地抑制革兰氏阳性菌细胞壁的生物合成,其抑菌机制与万古霉素(Vancomycin)和替考拉宁(Teicoplanin)不同,但是其对葡萄球菌的抑菌率是万古霉素和替考拉宁的4～8倍,对许多具有耐药性的病原菌也有很好的抑菌效果.同时雷莫拉宁的细胞毒性较小且无交叉耐药问题.雷莫拉宁的纯品是由A 1、A 2、A 3 3个组分组成的混合物,其中A 2为主要成分,占80%.     

新型糖肽类抗生素达巴万星

达巴万星是一种新型注射用半合成糖肽抗生素,适用于复杂感染及多重耐药菌造成感染的抗菌治疗。其对革兰阳性病原体有抗菌活性,且对耐甲氧西林金黄色葡萄球菌(MRSA)具有特别强力的活性;对耐G+病原菌包括耐青霉素和头孢曲松肺炎链球菌、替考拉宁不敏感CoNS、非vanA型肠球菌具有活性;对G+厌氧菌也具有活性。介绍了达巴万星的特性、制备工艺以及临床试验,指出了达巴万星具有独特的药动学性质,通过微生物发酵获得,在治疗导管相关的血源性感染以及皮肤和软组织感染已取得了良好的效果,是理想的第二代糖肽抗生素。     

万古霉素发酵工艺研究进展

万古霉素是一种糖肽类抗生素,对革兰氏阳性菌有很强的抑制作用。对万古霉素发酵工艺的国内外研究现状进行了综述,介绍了碳源、氮源、温度、溶解氧、前体物质等因素对万古霉素发酵的影响。不同的碳源和氮源对其发酵单位有显著地影响,温度和pH因素通过影响菌体代谢过程的酶类而影响产物的合成,无机盐直接参与菌体的新陈代谢。通过分析这些因素的作用,为万古霉素发酵培养基的优化和生产中发酵工艺的调控提供了理论参考依据。并对万古霉素的应用前景进行了展望。     

氨基糖苷类抗生素菌渣的残留检测与资源化研究进展

氨基糖苷类抗生素自问世以来就在临床治疗中发挥着重要的作用.随着经济的发展和抗生素的广泛应用,抗生素所引发的细菌耐药性给生态环境以及人类健康带来巨大的风险.本文对国内外氨基糖苷类抗生素菌渣的检测方法以及资源化无害化技术进行总结归纳,为合理利用氨基糖苷类抗生素菌渣、控制抗生素耐药性的传播以及提高菌渣无害化处理与资源化利用安...     

恶唑烷酮类化合物研究进展

近年来，各类抗生素与抗菌剂的耐药菌发展迅速，例如，耐甲氧西林金葡球菌（MRSA）、耐甲氧西林表皮葡萄球菌（MRSE）、耐青霉素肺炎链球菌（PRSP）、多重耐药性结核杆菌，尤其是耐万古霉素肠球菌（VRE）的出现．给临床治疗造成了困难。细菌接触抗菌药物后，通过质粒或染色忭介导发生变异，获得耐药。目前，一致认为细菌耐药性的获得主要有4种作用机制：①产生抗生素酶，灭活抗生素。②作用靶位变异，不应答抗菌药物。③改变膜通透性，阻断药物进入。④增强外排，加速泵出进入体内的药物。由于现有药物尚难有效控制此类药菌感染，因此药物化学家正努力研制新型抗耐药菌的药物，设计并筛选具有新化学结构、新作用机剖或新作用靶位的新抗菌药。     

替考拉宁吸附树脂的筛选

替考拉宁为游动放线菌属发酵产生的糖肽类抗生素,发酵液中含有大量的色素、无机盐、杂蛋白以及同系物等杂质.介绍了替考拉宁富集树脂型号和类型的筛选以及发酵液pH值的筛选.     

头孢吡普的合成进展

头孢吡普为广谱头孢菌素类抗生素,其抗菌谱包括耐甲氧西林金葡菌（MRSA）和耐万古霉素金葡球菌（VR-SA）等,应用前景广阔,属于＂第五代＂头孢菌素类抗生素。介绍了其合成方法。     

我国去甲万古霉素市场行情

2004年全年去甲万古霉素和替考拉宁在16城市典型医院用药数量95万支，同比增长22．6％，用药金额为1．04亿元，较去年增长24．7％，2002～2004年3年平均增长率为25％。目前去甲万古霉素的制剂以华北制药原研的万迅为主，还有浙江浙北（史比欣）和张家口长城制药等，而万古霉素则以进口品牌为主，有礼来公司原研的稳可信、韩国希杰仿制方克林等，浙江新昌药厂已于去年推出国产仿制万古霉素，即来可信。替考拉宁一直是国外品牌，主要有安万特（他格适）和赫斯特公司。     

N-Fmoc-2-(正癸胺基)乙醛的波谱数据和结构确证

N-Fmoc-2-(正癸胺基)乙醛是合成特拉万星的侧链,通过紫外吸收光谱(UV)、红外吸收光谱(IR)、高分辨质谱(HRMS)、核磁共振波谱(1HNMR、13C NMR、DEPT135、1H COSY、HMQC、HMBC)对其进行了结构表征,并对其核磁共振波谱进行了详细的解析和归属.综合运用多种谱学方法确证了其的结构,为其质量研究提供参考.     

新型复合抗菌陶瓷的研制与性能评价

抗菌陶瓷是具有杀菌、抑菌功能的陶瓷材料,金属离子与T iO2光催化抗菌材料都是良好的抗菌剂,但过去抗菌材料中的抗菌剂一般只有一种,本文论述了将两种抗菌剂复合在一起制作抗菌性能更好的抗菌陶瓷的研制过程,并对抗菌效果进行了测试,取得了很好的效果。     

Boronic Acid Modified Polymer Nanoparticles for Enhanced Bacterial Deactivation

A new method has been developed to enhance the antibacterial efficiency of traditional antibiotics. Chloramphenicol-imprinted polymer particles were decorated with boronic acid to improve their binding to both Gram-negative and -positive bacteria. The polymer particles have a high antibiotic loading and provide a slow release of the antibiotic payload to deactivate the target bacteria. The boronic acid modified polymer particles not only contribute to enhanced antibacterial efficiency, but also have the potential to act as scavengers to remove unused antibiotic from the environment.     

Metal and Metal Oxide Nanoparticle as a Novel Antibiotic Carrier for the Direct Delivery of Antibiotics

In addition to the benefits, increasing the constant need for antibiotics has resulted in the development of antibiotic bacterial resistance over time. Antibiotic tolerance mainly evolves in these bacteria through efflux pumps and biofilms. Leading to its modern and profitable uses, emerging nanotechnology is a significant field of research that is considered as the most important scientific breakthrough in recent years. Metal nanoparticles as nanocarriers are currently attracting a lot of interest from scientists, because of their wide range of applications and higher compatibility with bioactive components. As a consequence of their ability to inhibit the growth of bacteria, nanoparticles have been shown to have significant antibacterial, antifungal, antiviral, and antiparasitic efficacy in the battle against antibiotic resistance in microorganisms. As a result, this study covers bacterial tolerance to antibiotics, the antibacterial properties of various metal nanoparticles, their mechanisms, and the use of various metal and metal oxide nanoparticles as novel antibiotic carriers for direct antibiotic delivery.     

Second-Generation Meridianin Analogues Inhibit the Formation of Mycobacterium smegmatis Biofilms and Sensitize Polymyxin-Resistant Gram-Negative Bacteria to Colistin

Drug-resistant bacteria are rapidly becoming a significant problem across the globe. One element that factors into this crisis is the role played by bacterial biofilms in the recalcitrance of some infections to the effects of conventional antibiotics. Bacteria within a biofilm are highly tolerant of both antibiotic treatment and host immune responses. Biofilms are implicated in many chronic infections, including tuberculosis, in which they can act as bacterial reservoirs, requiring an arduous antibiotic regimen to eradicate the infection. A separate, compounding problem is that antibiotics once seen as last-resort drugs, such as the polymyxin colistin, are now seeing more frequent usage as resistance to front-line drugs in Gram-negative bacteria becomes more prevalent. The increased use of such antibiotics inevitably leads to an increased frequency of resistance. Drugs that inhibit biofilms and/or act as adjuvants to overcome resistance to existing antibiotics will potentially be an important component of future approaches to antibacterial treatment. We have previously demonstrated that analogues of the meridianin natural product family possess adjuvant and antibiofilm activities. In this study, we explore structural variation of the lead molecule from previous studies, and identify compounds showing both improved biofilm inhibition potency and synergy with colistin.     

达托霉素及其衍生物生物合成的研究进展

随着高致病耐药菌的不断出现,临床上对新抗生素的需求十分迫切。达托霉素作为环脂肽类抗生素的第一个产品对耐药菌有很好的杀菌效果,且制剂用药方便,毒副作用小,被公认为病原菌最后一道防线--万古霉素的最佳替代品。本文在介绍达托霉素的理化特征和抗菌活性、合成基因簇的研究成果的基础上,重点对达托霉素及其衍生物的研究状况进行了综述,对达托霉素的生产及其衍生物的开发进行了展望：结合系统生物学为已有的达托霉素产生菌进一步进行代谢工程改造提供指导;通过合成生物学使达托霉素衍生物成为新型抗生素。     

Expanding the Spectrum of Antibiotics Capable of Killing Multidrug-Resistant Staphylococcus aureus and Pseudomonas aeruginosa

Infections from antibiotic-resistant Staphylococcus aureus and Pseudomonas aeruginosa are a serious threat because reduced antibiotic efficacy complicates treatment decisions and prolongs the disease state in many patients. To expand the arsenal of treatments against antimicrobial-resistant (AMR) pathogens, 600-Da branched polyethylenimine (BPEI) can overcome antibiotic resistance mechanisms and potentiate β-lactam antibiotics against Gram-positive bacteria. BPEI binds cell-wall teichoic acids and disables resistance factors from penicillin binding proteins PBP2a and PBP4. This study describes a new mechanism of action for BPEI potentiation of antibiotics generally regarded as agents effective against Gram-positive pathogens but not Gram-negative bacteria. 600-Da BPEI is able to reduce the barriers to drug influx and facilitate the uptake of a non-β-lactam co-drug, erythromycin, which targets the intracellular machinery. Also, BPEI can suppress production of the cytokine interleukin IL-8 by human epithelial keratinocytes. This enables BPEI to function as a broad-spectrum antibiotic potentiator, and expands the opportunities to improve drug design, antibiotic development, and therapeutic approaches against pathogenic bacteria, especially for wound care.     

农用硫酸链霉素检测方法探究

硫酸链霉素是一种重要的抗生素,在制药工业中占有举足轻重的地位,目前被广泛应用于农业。硫酸链霉素属氨基糖苷类抗生素,较低浓度时能抑制细菌的生长,较高浓度时则杀菌。测定硫酸链霉素的方法有很多,对这些方法进行了比较和探究。     

Simplified Novel Muraymycin Analogues; using a Serine Template Strategy for Linking Key Pharmacophores

The present status of antibiotic research requires the urgent invention of novel agents that act on multidrug-resistant bacteria. The World Health Organization has classified antibiotic-resistant bacteria into critical, high and medium priority according to the urgency of need for new antibiotics. Naturally occurring uridine-derived “nucleoside antibiotics” have shown promising activity against numerous priority resistant organisms by inhibiting the transmembrane protein MraY (translocase I), which is yet to be explored in a clinical context. The catalytic activity of MraY is an essential process for bacterial cell viability and growth including that of priority organisms. Muraymycins are one subclass of naturally occurring MraY inhibitors. Despite having potent antibiotic properties, the structural complexity of muraymycins advocates for simplified analogues as potential lead structures. Herein, we report a systematic structure-activity relationship (SAR) study of serine template-linked, simplified muraymycin-type analogues. This preliminary SAR lead study of serine template analogues successfully revealed that the complex structure of naturally occurring muraymycins could be easily simplified to afford bioactive scaffolds against resistant priority organisms. This study will pave the way for the development of novel antibacterial lead compounds based on a simplified serine template.     

环境中抗生素及抗性基因的污染研究进展

抗生素在医药、畜牧和水产养殖业的大量使用,造成了环境中抗性耐药菌和抗性基因日益增加,抗生素滥用所造成的水环境污染问题(抗生素抗性基因作为一种新型环境污染物)引起人们的广泛关注。对近年来国内外抗生素及抗性基因的研究进展进行了综述,重点介绍了抗生素及抗性基因污染、及相关检测、去除控制技术及治理策略。同时,对抗生素及抗性基因研究过程中存在的问题作了相应阐述,并对未来的相关研究进行了展望。     

Interactions of antibiotics and methanolic crude extracts of afzelia africana (smith.) against drug resistance bacterial isolates

Infection due to multidrug resistance pathogens is difficult to manage due to bacterial virulence factors and because of a relatively limited choice of antimicrobial agents. Thus, it is imperative to discover fresh antimicrobials or new practices that are effective for the treatment of infectious diseases caused by drug-resistant microorganisms. The objective of this experiment is to investigate for synergistic outcomes when crude methanolic extract of the stem bark of Afzelia africana and antibiotics were combined against a panel of antibiotic resistant bacterial strains that have been implicated in infections. Standard microbiological protocols were used to determine the minimum inhibitory concentrations (MICs) of the extract and antibiotics, as well as to investigate the effect of combinations of the methanolic extract of A. africana stem bark and selected antibiotics using the time-kill assay method. The extract of Afzelia africana exhibited antibacterial activities against both Gram-negative and Gram-positive bacteria made up of environmental and standard strains at a screening concentration of 5 mg/mL. The MICs of the crude extracts and the antibiotics varied between 1 μg/mL and 5.0 mg/mL. Overall, synergistic response constituted about 63.79% of all manner of combinations of extract and antibiotics against all test organisms; antagonism was not detected among the 176 tests carried out. The extract from A. africana stem bark showed potentials of synergy in combination with antibiotics against strains of pathogenic bacteria. The detection of synergy between the extract and antibiotics demonstrates the potential of this plant as a source of antibiotic resistance modulating compounds.