antimicrobial drug

  • 文章类型: Journal Article
    阴道炎是女性常见的感染,大约75%的女性一生中至少经历过一次发作。虽然抗菌剂被广泛用于治疗阴道炎,复发性阴道炎发生在一些患者中。对这些药物的抗性是复发性阴道炎的主要原因。因此,迫切需要开发新药物。
    我们研究了一种新型生物抑菌剂(BBA)的功效,由溶菌酶组成,植物抗毒素,壳寡糖,sinensetin,18β/20α-甘草酸,和甜菜碱,使用体外和体内研究对抗阴道炎。首先,我们评估了BBA对需氧性阴道炎中常见的13种微生物菌株的抗菌作用,细菌性阴道病,外阴阴道念珠菌病,和健康的阴道。第二,我们评估了雌性小鼠口服不同剂量BBA4周的安全性。第三,我们检查了BBA在白色念珠菌中的体内抗增殖和抗炎作用-,光亮念珠菌-,和加德纳菌诱导的阴道炎模型。最后,我们评估了用0.5%(w/v)丙烯酰二甲基牛磺酸铵/Vp共聚物制备的BBA凝胶的抗阴道炎作用。
    BBA在体外有效抑制了阴道炎的主要病原体的生长。BBA,未稀释或稀释两倍,抑制所有培养8小时的微生物。对小鼠施用BBA时未检测到明显的器官损伤。单独的BBA和凝胶制剂中的70%BBA均有效抑制白色念珠菌的增殖,C.光滑,阴道灌洗样品中的加德纳菌和减轻阴道炎小鼠的组织炎症。70%BBA凝胶在治疗感染阴道加德纳菌的小鼠阴道炎方面比单独的BBA表现更好。
    单独的BBA和70%的BBA凝胶抑制病原体的生长,并有效减轻白色念珠菌引起的炎症,C.光滑,和阴道G.
    UNASSIGNED: Vaginitis is a common infection in women, with approximately 75% of women experiencing at least one episode during their lifetime. Although antimicrobial agents are widely used to treat vaginitis, recurrent vaginitis occurs in some patients. Resistance to these agents is the major cause of recurrent vaginitis. Therefore, there is an urgent need to develop novel drugs.
    UNASSIGNED: We investigated the efficacy of a new biological bacteriostatic agent (BBA), composed of lysozyme, phytoalexin, chitosan oligosaccharide, sinensetin, 18β/20α-glycyrrhizin, and betaine, against vaginitis using in vitro and in vivo studies. First, we evaluated the antibacterial effects of BBA against 13 microbial strains commonly present in aerobic vaginitis, bacterial vaginosis, vulvovaginal candidiasis, and healthy vaginas. Second, we assessed the safety of various doses of BBA administered orally for 4 weeks in female mice. Third, we examined the in vivo anti-proliferative and anti-inflammatory effects of BBA in Candida albicans-, Candida glabrata-, and Gardnerella-induced vaginitis models. Finally, we evaluated the anti-vaginitis effect of a BBA gel prepared with 0.5% (w/v) ammonium acryloyldimethyltaurate/Vp copolymer.
    UNASSIGNED: BBA effectively suppressed the growth of the main causative pathogens of vaginitis in vitro. BBA, either undiluted or diluted two-fold, inhibited all microorganisms cultured for 8 h. No obvious organ damage was detected when BBA was administered to mice. Both BBA alone and 70% BBA in a gel formulation effectively inhibited the proliferation of C. albicans, C. glabrata, and Gardnerella in vaginal lavage samples and alleviated tissue inflammation in mice with vaginitis. The 70% BBA gel performed better than BBA alone at treating vaginitis in mice infected with Gardnerella vaginalis.
    UNASSIGNED: BBA alone and a 70% BBA gel inhibited the growth of pathogens and effectively alleviated inflammation caused by C. albicans, C. glabrata, and G. vaginalis.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Pubmed)

  • 文章类型: Journal Article
    球状马拉色菌,一种亲脂性病原体,已知与各种慢性皮肤病有关。不幸的是,可用的治疗方法有不良的副作用,微生物耐药性正在演变。由于蜂胶的抗菌活性突出,这项研究旨在研究来自无刺蜜蜂的蜂胶对酵母的潜力。Anti-M.在琼脂孔扩散和肉汤微量稀释测定中确定球形生长活性,并确定50%的抑制浓度值(IC50)。由于酵母不能合成自己的脂肪酸,细胞外脂肪酶对其存活很重要。这里,反M还通过比色法和基于琼脂的方法研究了球形细胞外脂肪酶活性。与粗己烷和粗二氯甲烷提取物相比,粗甲醇分配提取物(CMPE)表现出最佳的抗M。球形生长活性,IC50为1.22mg/mL。经硅胶柱层析进一步富集后,级分CMPE1(IC50为0.98mM或184.93μg/mL)表现出最高的活性,随后通过核磁共振分析鉴定为没食子酸甲酯(MG)。随后,成功合成了MG,并显示具有类似的活性,和最低杀真菌浓度为43.44mM或8.00mg/mL。然而,脂肪酶测定分析表明,细胞外脂肪酶可能不是MG的主要靶标机制。这是MG作为新的抗马拉色菌化合物的首次报道。它可能是进一步开发替代治疗剂的良好候选者。
    Malassezia globosa, a lipophilic pathogen, is known to be involved in various chronic skin diseases. Unfortunately, the available treatments have unwanted side effects and microbial drug resistance is evolving. As the antimicrobial activity of propolis is outstanding, this study aimed to examine the potential of propolis from the stingless bee Geniotrigona thoracica against the yeast. Anti-M. globosa growth activity was ascertained in agar well diffusion and broth microdilution assays and the inhibitory concentration value at 50 % (IC50) was determined. Since the yeast cannot synthesize its own fatty acids, extracellular lipase is important for its survival. Here, anti-M. globosa extracellular lipase activity was additionally investigated by colorimetric and agar-based methods. Compared to the crude hexane and crude dichloromethane extracts, the crude methanol partitioned extract (CMPE) exhibited the best anti-M. globosa growth activity with an IC50 of 1.22 mg/mL. After CMPE was further enriched by silica gel column chromatography, fraction CMPE1 (IC50 of 0.98 mM or 184.93 μg/mL) presented the highest activity and was later identified as methyl gallate (MG) by nuclear magnetic resonance analysis. Subsequently, MG was successfully synthesized and shown to have a similar activity, and a minimal fungicidal concentration of 43.44 mM or 8.00 mg/mL. However, lipase assay analysis suggested that extracellular lipase might not be the main target mechanism of MG. This is the first report of MG as a new anti-Malassezia compound. It could be a good candidate for further developing alternative therapeutic agents.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Pubmed)

  • 文章类型: Journal Article
    在这项研究中,开发了一种简单的电化学aptasensor来检测磺胺二甲氧嘧啶(SDM)。它包括由氮化硼量子点(BNQD)和适体功能化的纳米多孔碳(APT/CZ)修饰的玻璃碳电极。CZ首先通过煅烧沸石咪唑酯骨架(ZIF-8)来合成。然后,电活性染料亚甲基蓝(MB)被截留在其孔内。通过将适体连接到CZ表面,APT/CZ充当了沼气,这阻止了MB的释放。因此,在没有SDM的情况下,截留的MB的电化学信号是高的。引入SDM导致适体的构象发生变化,大量的MB被释放,通过洗涤去除。因此,检测策略是根据MB电化学信号强度的变化进行的。应用aptasensor在10-17至10-7M的浓度范围内检测SDM,检测极限为3.6×10-18M。
    In this study, a straightforward electrochemical aptasensor was developed to detect sulfadimethoxine (SDM). It included a glassy carbon electrode decorated by boron nitride quantum dots (BNQDs) and aptamer-functionalized nanoporous carbon (APT/CZ). CZ was first synthesized by calcinating a zeolitic imidazolate framework (ZIF-8). Then, the electroactive dye methylene blue (MB) was entrapped inside its pores. By attaching aptamer to the CZ surface, APT/CZ acted as a bioguard, which prevented the MB release. Therefore, the electrochemical signal of the entrapped MB was high in the absence of SDM. Introducing SDM caused the conformation of aptamers to change, and a large number of MB was released, which was removed by washing. Therefore, the detection strategy was done based on the change in the electrochemical signal intensity of MB. The aptasensor was applied to detect SDM at a concentration range of 10-17 to 10-7 M with a detection limit of 3.6 × 10-18 M.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

    求助全文

  • 文章类型: Journal Article
    VitexL.是唇形科的最大属,它的大多数物种被用于不同国家的传统药用系统。进行了系统的审查,根据PRISMA方法,为了确定Vitex植物作为抗菌剂来源的潜力,产生了2610种科学出版物,从中选择了141篇文章。数据分析证实,Vitex物种在传统医学中用于治疗可能的传染病的症状。进行的研究表明,这些药用植物对枯草芽孢杆菌表现出体外抗菌活性,大肠杆菌,肺炎克雷伯菌,铜绿假单胞菌,和金黄色葡萄球菌。Vitexagnus-castusL.和VitexnegundoL.一直是研究最多的物种,不仅对细菌菌株,而且对真菌,如黑曲霉和白色念珠菌,病毒如HIV-1和寄生虫如恶性疟原虫。像agnucastoside这样的天然产品,negundol,negundoside,已在Vitex提取物中鉴定出vitegnoside,并已确定其对多种微生物菌株的抗菌活性。Negundside对金黄色葡萄球菌显示出显着的抗菌活性(MIC12.5µg/mL)。我们的结果表明,Vitex物种是新的天然抗菌剂的潜在来源。然而,需要进行进一步的实验研究。
    Vitex L. is the largest genus of the Lamiaceae family, and most of its species are used in the traditional medicinal systems of different countries. A systematic review was conducted, according to the PRISMA methodology, to determine the potential of Vitex plants as sources of antimicrobial agents, resulting in 2610 scientific publications from which 141 articles were selected. Data analysis confirmed that Vitex species are used in traditional medicine for symptoms of possible infectious diseases. Conducted studies showed that these medicinal plants exhibited in vitro antimicrobial activity against Bacillus subtilis, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, and Staphylococcus aureus. Vitex agnus-castus L. and Vitex negundo L. have been the most studied species, not only against bacterial strains but also against fungi such as Aspergillus niger and Candida albicans, viruses such as HIV-1, and parasites such as Plasmodium falciparum. Natural products like agnucastoside, negundol, negundoside, and vitegnoside have been identified in Vitex extracts and their antimicrobial activity against a wide range of microbial strains has been determined. Negundoside showed significant antimicrobial activity against Staphylococcus aureus (MIC 12.5 µg/mL). Our results show that Vitex species are potential sources of new natural antimicrobial agents. However, further experimental studies need to be conducted.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Pubmed)

  • 文章类型: Journal Article
    断奶母牛是一个研究相对不足的生产群体。牛呼吸道疾病(BRD)是抗菌药物(AMD)使用的最常见原因,发病率,和死亡率在这个生产组。抗菌素耐药性(AMR)的研究很复杂,因为许多可能影响AMR的变量是相关的。这项研究产生了关于农场和动物水平变量的假设(例如,疫苗接种,车道清洁,和AMD使用实践),可能与断奶母牛呼吸道分离物中的AMR相关。使用调查数据和呼吸道分离株(多杀巴斯德拉,Mannheimia溶血病,和嗜血杆菌)从加利福尼亚六个农场的341只断奶母牛中收集。使用Logistic回归和贝叶斯网络分析来评估养殖和动物水平变量与呼吸道分离株对11种AMD的最低抑制浓度(MIC)分类之间的关联。与呼吸道分离株的MIC分类相关的农场级变量包括小牛饲养设施的来源农场的数量,农场是否在现场进行挤奶,使用泻湖水清洗冲水道,以及呼吸道和红眼病疫苗接种方法。与MIC分类相关的动物水平变量包括小牛是否为BRD评分阳性以及自上次苯酚治疗以来的时间。
    Weaned dairy heifers are a relatively understudied production group. Bovine respiratory disease (BRD) is the most common cause of antimicrobial drug (AMD) use, morbidity, and mortality in this production group. The study of antimicrobial resistance (AMR) is complicated because many variables that may affect AMR are related. This study generates hypotheses regarding the farm- and animal-level variables (e.g., vaccination, lane cleaning, and AMD use practices) that may be associated with AMR in respiratory isolates from weaned dairy heifers. A cross-sectional study was performed using survey data and respiratory isolates (Pasteurella multocida, Mannheimia haemolytica, and Histophilus somni) collected from 341 weaned dairy heifers on six farms in California. Logistic regression and Bayesian network analyses were used to evaluate the associations between farm- and animal-level variables with minimum inhibitory concentration (MIC) classification of respiratory isolates against 11 AMDs. Farm-level variables associated with MIC classification of respiratory isolates included the number of source farms of a calf-rearing facility, whether the farm practiced onsite milking, the use of lagoon water for flush lane cleaning, and respiratory and pinkeye vaccination practices. Animal-level variables associated with a MIC classification included whether the calf was BRD-score-positive and time since the last phenicol treatment.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Pubmed)

  • 文章类型: Journal Article
    沙门氏菌是细胞内细菌病原体,和许多其他肠杆菌一样,抗生素耐药性正成为一个日益严重的问题。根据世界卫生组织和其他国际机构的建议,正在寻求新的抗生素。这些必须能够穿透巨噬细胞,并感染主要宿主细胞和含沙门氏菌的液泡。这项研究报告筛选了食品和药物管理局(FDA)批准的药物的一个小型图书馆,其在感染了肠炎沙门氏菌快速繁殖突变体的巨噬细胞中的抗菌作用。对巨噬细胞毒性最小的最有效的药物是Nifuratel,已经用于寄生虫感染的硝基呋喃抗生素。在老鼠身上,它在口腔感染后提供了60%的保护,使用致死的肠炎沙门氏菌剂量减少了组织中的细菌数量。它对不同的血清型有效,包括鼠伤寒沙门氏菌的多重耐药菌株,以及来自不同宿主物种的巨噬细胞中,针对单核细胞增生李斯特菌和福氏志贺氏菌。它减少了感染的巨噬细胞中IL-10和STAT3的产生,这应该增加针对沙门氏菌的炎症反应。重要性沙门氏菌可在宿主巨噬细胞中保持长期持续存在,以逃避细胞免疫防御和抗生素攻击,并在某些情况下退出并再次感染引起沙门氏菌病。除了多药耐药性,这个感染圈导致沙门氏菌在宿主中难以清除,因此,人们非常需要新的抗菌剂来减少体内沙门氏菌的存活,以阻断内源性沙门氏菌的再感染。
    Salmonella are intracellular bacterial pathogens for which, as with many of the other Enterobacteriaceae, antibiotic resistance is becoming an increasing problem. New antibiotics are being sought as recommended by the World Health Organization and other international institutions. These must be able to penetrate macrophages, and infect the major host cells and the Salmonella-containing vacuole. This study reports screening a small library of Food and Drug Administration (FDA)-approved drugs for their antibacterial effect in macrophages infected with a rapid-multiplying mutant of Salmonella Enteritidis. The most effective drug that was least toxic for macrophages was Nifuratel, a nitrofuran antibiotic already in use for parasitic infections. In mice, it provided 60% protection after oral infection with a lethal S. Enteritidis dose with reduced bacterial numbers in the tissues. It was effective against different serovars, including multidrug-resistant strains of Salmonella Typhimurium, and in macrophages from different host species and against Listeria monocytogenes and Shigella flexneri. It reduced IL-10 and STAT3 production in infected macrophages which should increase the inflammatory response against Salmonella. IMPORTANCE Salmonella can keep long-term persistence in host\'s macrophages to evade cellular immune defense and antibiotic attack and exit in some condition and reinfect to cause salmonellosis again. In addition to multidrug resistance, this infection circle causes Salmonella clearance difficult in the host, and so there is a great need for new antibacterial agents that reduce intramacrophage Salmonella survival to block endogenous Salmonella reinfection.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Pubmed)

  • 文章类型: Journal Article
    铜绿假单胞菌(P.铜绿假单胞菌)是医疗机构中常见的病原体,对常见抗菌药物的耐药性不断增加。据报道,其抵抗能力已在世界各地的多个地方得到报道。这项研究评估了当前的抗生素耐药性水平,并试图在铜绿假单胞菌临床分离株的背景下了解抗生素耐药性模式。
    所有临床分离株在37°C的不同培养基中培养24小时:血羊琼脂,麦康基琼脂,和胱氨酸-乳糖-电解质缺乏琼脂(CLED),使用Vitek-2(bioMérieux)自动化系统确定细菌鉴定和抗生素敏感性模式。
    总共,有61029个病人标本,其中5534个被鉴定为非重复铜绿假单胞菌临床分离株,大多数来自60岁以上的男性。研究结果表明,与铜绿假单胞菌分离株相关的最大抗生素耐药性在粘菌素(97%)中发现,其次是哌拉西林/他唑巴坦(75.8%)。铜绿假单胞菌的最大耐药率与头孢吡肟有关(42.7%,)其次是环丙沙星(34.3%)。
    研究期前六年的抗生素耐药率明显高于过去几年,由于在所有沙特医院中应用感染控制协议和严格的政策来控制抗生素处方。
    UNASSIGNED: Pseudomonas aeruginosa (P. aeruginosa) is a common causative pathogen in healthcare settings and displays increasing levels of resistance to common antimicrobial drugs. Its capacity to resist has been reported in multiple locations across the world. This study evaluates current levels of antibiotic resistance and seeks to understand antibiotic resistance patterns in the context of the clinical isolates of P. aeruginosa.
    UNASSIGNED: All clinical isolates were cultured at 37 °C for 24 h in different media: blood sheep agar, McConkey agar, and cystine-lactose-electrolyte-deficient agar (CLED), bacterial identification and antibiotic susceptibility patterns were determined using the Vitek-2 (bioMérieux) automated system.
    UNASSIGNED: In total, there were 61,029 patient specimens, of which 5534 were identified as non-duplicated P. aeruginosa clinical isolates, most being from males aged over 60 years. The research findings revealed that the maximum antibiotic resistance associated with P. aeruginosa isolates was found in colistin (97%), which was followed by piperacillin/tazobactam (75.8%). The maximum resistance rates in P. aeruginosa isolates were found in relation to cefepime (42.7%,) which was followed by ciprofloxacin (34.3%).
    UNASSIGNED: The antibiotic resistance rate during the first six years of the research period was notably higher than in the last years, due to the application of infection control protocols and strict policies to control antibiotic prescriptions in all Saudi hospitals.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Pubmed)

  • 文章类型: Journal Article
    该数据集表达了使用Jamun种子(JS)(Syzygiumcumini)生物炭从合成溶液中分批吸附环丙沙星和拉米夫定的实验数据。独立变量,包括污染物浓度(10-500ppm),接触时间(30-300分钟),吸附剂用量(1-1000mg),使用响应面法(RSM)研究并优化了pH(1-14)和吸附剂煅烧温度(250,300,600和750°C)。建立了预测环丙沙星和拉米夫定最大去除效率的经验模型,并将结果与实验数据进行了比较。污染物的去除受浓度的影响更大,其次是吸附剂的剂量,pH值,接触时间和最大去除量达到90%。
    This dataset expresses the experimental data on the batch adsorption of ciprofloxacin and lamivudine from synthetic solution using jamun seed (JS) (Syzygium cumini) biochar. Independent variables including concentration of pollutants (10-500 ppm), contact time (30-300 min), adsorbent dosage (1-1000 mg), pH (1-14) and adsorbent calcination temperature (250,300, 600 and 750 °C) were studied and optimized using Response Surface Methodology (RSM). Empirical models were developed to predict the maximum removal efficiency of ciprofloxacin and lamivudine, and the results were compared with the experimental data. The removal of polutants was more influenced by concentration, followed by adsorbent dosagage, pH, and contact time and the maximum removal reached 90%.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Pubmed)

  • 文章类型: Journal Article
    RNA解旋酶代表有吸引力的药物靶标,因为它们的活性与几种人类疾病有关并影响微生物感染过程。虽然一些人RNA解旋酶的抑制剂在临床前试验中显示出作为抗癌和抗病毒药物的治疗潜力,微生物RNA解旋酶的化学抑制研究较少。这里,我们通过关注RNA解旋酶的RhlE蛋白质类来解决这个问题。先前表明RhlE2RNA解旋酶对于机会性病原体铜绿假单胞菌的毒力很重要,我们筛选了1280个分子的文库,用于抑制RhlE2RNA依赖性ATP水解活性。最有效的抑制剂是重氮化合物芝加哥天蓝(CSB)。使用氢-氘交换质谱和生化分析,我们绘制了CSB与RhlE2催化核心的结合图,并定义了其抑制机制。靶向微生物RNA解旋酶作为治疗策略是具有挑战性的,因为潜在的副作用与跨生命界的蛋白质保护有关。有趣的是,我们的结构-活性关系分析描述了与CSB密切相关的其他重氮染料对RhlE同系物的影响。因此,我们的工作可以用于未来的药物开发研究,考虑到细菌病原体中抗生素耐药性的日益传播,这是非常及时的。
    RNA helicases represent attractive drug targets as their activity is linked to several human diseases and impacts microbial infectious processes. While some inhibitors of human RNA helicases demonstrated therapeutic potential as anticancer and antiviral drugs in preclinical trials, chemical inhibition of microbial RNA helicases is less investigated. Here, we address this matter by focusing on the RhlE proteobacterial group of RNA helicases. Having previously shown that the RhlE2 RNA helicase is important for the virulence of the opportunistic pathogen Pseudomonas aeruginosa, we screened a library of 1280 molecules for inhibitors of RhlE2 RNA-dependent ATP hydrolytic activity. The most potent inhibitor is the diazo compound Chicago Sky Blue (CSB). Using hydrogen-deuterium exchange mass spectrometry and biochemical assays, we mapped CSB binding to RhlE2 catalytic core and defined its inhibitory mechanism. Targeting microbial RNA helicases as therapeutic strategy is challenging due to potential side-effects linked to protein conservation across life kingdoms. Interestingly, our structure-activity relationship analysis delineates other diazo dyes closely related to CSB differentially affecting RhlE homologs. Our work could thus be exploited for future drug development studies, which are extremely timely considering the increasing spread of antibiotic resistance among bacterial pathogens.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

    求助全文

  • 文章类型: Interview
    Bugarin博士目前是佛罗里达墨西哥湾沿岸大学的化学和物理学副教授。他发表了50多篇同行评审的出版物(h-index=18)。他的研究小组正在开发新的方法来改善或揭示三氮烯的新反应性,N-杂环卡宾,异双金属催化剂,和其他通用分子。此外,他最近加入了在隔离基础上的研究工作,表征,和天然产物的生物学评价。
    Dr Bugarin is currently an Associate Professor of Chemistry and Physics at Florida Gulf Coast University. He has published more than 50 peer-reviewed publications (h-index = 18). His research group is developing new methodology to improve or reveal novel reactivity of triazenes, N-Heterocyclic carbenes, heterobimetallic catalysts, and other versatile molecules. In addition, he recently joined research efforts to build on the isolation, characterization, and biological evaluation of natural products.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

    求助全文

公众号