盐酸左氧氟沙星对眼部感染细菌的体外抗菌活性研究

目的 比较盐酸左氧氟沙星，氧氟沙星和环丙沙星对临床分离的150株眼部感染细菌的体外抗菌活性。为眼部感染性疾病的治疗提供新一代喹诺桐药物的药敏信息。方法 用双倍琼腓稀释法测定并比较3种喹诺酮药物的最低抑菌浓度，计算出平均敏感率，并与K-B法平均敏感率对照，结果 盐酸左氧氟沙星对眼部感染的金黄色葡萄球菌，凝固酶阴性葡萄球菌，大肠埃希菌等的MIC50值均低于氧氟沙星，环丙沙星；对铜绿假单胞菌活性稍弱于歪丙沙星。结论 盐酸左氧氟沙星为一个广谱抗生素，对眼部感染的各类病原菌有良好的抗药活性。     

加替沙星与4种喹诺酮类药物体外抗菌活性比较

目的比较加替沙星与环丙沙星、氧氟沙星、左氧氟沙星、罗美沙星的体外抗菌活性,为临床提供用药依据. 方法采用K-B纸片法对2003年以来,我院分离的金黄色葡萄球菌(MSSA)、凝固酶阴性葡萄球菌(MSSCN)、肠球菌、大肠埃希菌、肺炎克雷伯菌、铜绿假单胞菌、鲍氏不动杆菌等共659株进行了体外药敏试验,并将结果用WHONET5.0进行分析. 结果发现加替沙星对除铜绿假单胞菌以外的其他分离菌株的敏感性,普遍高于其他4种药物;对MSSA、MSSCN、MRSA、MRSCN、粪肠球菌、屎肠球菌、大肠埃希菌、肺炎克雷伯菌、铜绿假单胞菌、鲍氏不动杆菌的敏感率分别为100%、96.2%、37.5%(中度敏感率为56.2%)、77%、65.9%、18.2%、32%、84.3%、56.2%、72.1%. 结论加替沙星在这5种药中敏感性最高,是高效、广谱抗菌药物,可以广泛应用于临床各种感染性疾病.     

氟喹诺酮类药物对医院菌株的体外抗菌活性测定分析

应用４种氟喹诺酮类抗菌药物对武汉地区３６０株医院菌株，用双倍琼脂稀释法进行体外抗菌活性测定，并用ＮＣＣＬＳ于１９９０年公布的稀释法药敏试验判读表进行分析，结果表明：４种药物抗菌活性大小依次为：环丙氟哌酸、氟嗪酸、氟啶酸、氟哌酸。它们具有广谱抗菌作用，对革兰氏阴性杆菌抗菌活性明显优于革兰氏阳性球菌，对具有多重耐药性的铜绿假单胞菌、耐甲氧西林金黄色葡萄球菌（ＭＲＳＡ）及不动杆菌均有一定的抑菌作用。同时，也发现氟喹诺酮类药物的广泛应用已促使细菌产生了耐药性，大肠埃希氏菌、铜绿假单胞菌、不动杆菌和ＭＲＳＡ都出现了高度耐药株（ＭＩＣ≥３２ｍｇ／Ｌ），并指出了合理使用抗菌药物的重要性。     

耐头孢他啶大肠埃希菌与肺炎克雷伯菌对氟喹诺酮类药物的耐药性分析

目的 了解临床耐头孢他啶大肠埃希菌与肺炎克雷伯菌分离株对氟喹诺酮类抗菌药物的耐药性,以合理使用氟喹诺酮类抗菌药物,采取有效措施控制耐药株的出现.方法 采用K-B和MIC法测定耐头孢他啶大肠埃希菌与肺炎克雷伯菌对8种常见氟喹诺酮类抗菌药物的敏感性.结果 共分离出耐头孢他啶大肠埃希菌与肺炎克雷伯菌276株,对加替沙星、莫西沙星、吉米沙星、左氧氟沙星、氧氟沙星、环丙沙星、帕珠沙星、司帕沙星的耐药率分别为46.38％、43.48％、42.72％、55.43％、65.22％、61.96％、52.54％、53.62％,且均明显高于头孢他啶敏感株(P＜0.05);呼吸道、非呼吸道标本的耐头孢他啶大肠埃希菌与肺炎克雷伯菌分离株对加替沙星、莫西沙星、氧氟沙星、司帕沙星的耐药率不同,差异均有统计学意义(P＜0.05).结论 耐头孢他啶大肠埃希菌与肺炎克雷伯菌分离株对氟喹诺酮类抗菌药物的耐药率较高,呼吸道、非呼吸道标本分离株对多种常见氟喹诺酮抗菌药物的耐药率不同.     

临床常见病原菌对氟喹诺酮药物的耐药趋势分析

目的 分析临床常见病原菌对氟喹诺酮类药物的耐药性趋势，为临床合理应用氟喹诺酮类药物提供依据。方法 用WHONET4（1999版）软件对解放军总医院临床常见病原菌1994年3月－1999年3月6年间对环丙沙星药敏结果和1999年3月－2001年3月两年间对环丙沙星、氧氟沙星和左氧氟沙星的药敏结果进行分析，药敏采用纸片扩散法。结果 7种临床常见菌：表皮葡萄球菌，金黄色葡萄球菌，类肠球菌，大肠埃希菌，肺炎克雷全菌，阴沟肠杆菌，铜绿假单胞菌。6年内对环丙沙星耐药总体呈上升趋势，对氧氟沙星的耐药情况与环丙沙星相比差异无显著性；临床常见革兰阴性病原菌对左氧氟沙星的耐药与环丙沙星相比差异亦无显著性。结论 临床常见病原菌对氟喹诺酮类药物的耐药率高低不但与临床广泛应用氟喹诺酮类药物有关，与经验性应用氟喹诺酮类药物治疗不同部位感染有关。     

2007-2010年左氧氟沙星用药频度与细菌耐药相关性分析

目的 分析医院2007-2010年左氧氟沙星用药频度与临床分离的10种主要细菌耐药相关性,为临床氟喹诺酮类药物合理应用提供依据.方法 提取2007年1月-2010年12月左氧氟沙星使用量(0.5 9)及相应年度大肠埃希菌等10种常见病原菌的分离株及其对左氧氟沙星的耐药资料,采用SPSS13.0统计软件进行分析.结果 2007-2010年大肠埃希菌、铜绿假单胞菌和克雷伯菌属的分离率分别为22.2％、15.9％、9.2％;大肠埃希菌、铜绿假单胞菌和克雷伯菌属对左氧氟沙星的耐药率以2008年为最高,分别为71.6％、49.4％、34.5％;左氧氟沙星用药频度为39.61;左氧氟沙星用药频度与铜绿假单胞菌、克雷伯菌属、金黄色葡萄球菌和肠杆菌属耐药率均呈高度正相关(P＜0.05).结论 左氧氟沙星的用药频度与细菌耐药存在相关性.     

格帕沙星和氧氟沙星的体外抗生素后效应

目的 比较格帕沙星与氧氟沙星对4种病菌的休外抗生素后效应（PAE）。方法 最低抑菌浓度（MIC）的测定采用标准微量平板法,以光密度法测定PAE。结果 MIC测定显示格帕沙星对金黄色葡萄球菌和粪肠球菌的抗菌活性略强于氧氟沙星,格帕沙星和氧氟沙星对大肠埃希菌、铜绿假单胞菌、粪肠球菌、葡萄球菌均有明显PAE,格凰沙星对多黄色葡萄球菌的PAE长于氧氟沙星。结论 格帕沙星具有良好的杀菌活性和明显的PAE,是一具有良好应用前景的新氟喹诺酮类抗菌药物,PAE结果有利于临床给药方案的选择。     

49946株常见病原菌对左旋氧氟沙星耐药性变化分析

目的了解常见病原菌对左旋氧氟沙星的耐药性变化趋势,为临床合理应用喹诺酮类药物提供参考。方法收集郑州大学第一附属医院2011年1月-2016年6月细菌室分离的49 946株不重复菌株,进行回顾性分析,探讨常见病原菌对左旋氧氟沙星的耐药性变迁。结果金黄色葡萄球菌和凝固酶阴性的葡萄球菌是革兰阳性菌感染的主要病原菌(约52.00%),大肠埃希菌、肺炎克雷伯菌是最常见的肠杆菌科细菌(占整个阴性杆菌45.10%),铜绿假单胞菌、鲍曼不动杆菌在非发酵菌感染中占绝对优势(占整个阴性杆菌28.10%)。6年间几种常见病原菌对左旋氧氟沙星总耐药率为53.66%。大肠埃希菌耐药性最严重,为70.11%,其次为鲍曼不动杆菌,耐药率60.86%;金葡菌耐药性呈显著下降趋势,由2011年61.55%降至2016年的41.12%,凝固酶阴性的葡萄球菌始终保持在55%以上;肺炎克雷伯菌与铜绿假单胞菌对左旋氧氟沙星耐药率相对较低,其敏感性均保持在60%左右。结论大肠埃希菌、鲍曼不动杆菌对于喹诺酮类药物具有广泛耐药性,临床应加强此类菌株感染治疗的指导与监测。     

16SrRNA基因快速测序法鉴定3种常见病原微生物

目的改良传统Sanger测序技术,建立16S r RNA快速测序法,并应用于常见病原微生物的鉴定。方法以铜绿假单胞菌、金黄色葡萄球菌和大肠埃希菌标准菌株为实验对象,建立16S r RNA快速测序鉴定方法。再以自医院分离的,已经传统生化方法鉴定的铜绿假单胞菌、金黄色葡萄球菌和大肠埃希菌各30株进行方法验证。结果采用本方法进行细菌鉴定,可以正确、快速鉴定所有3种标准菌株。临床样品中,所有金黄色葡萄球菌和铜绿假单胞菌均可获得与传统生化方法完全一致的带定结果,而在30株大肠埃希菌中,只有8株(占26.7%)被鉴定为大肠埃希氏菌,有10株(占33.3%)被鉴定为宋氏志贺菌,12株(占40%)被鉴定为痢疾志贺菌。结论本方法适用于铜绿假单胞菌和金黄色葡萄球菌的快速准确鉴定,对大肠埃希菌则不完全适用。     

中草药提取物的体外抑菌活性研究

目的探讨10种中草药提取物的体外抗菌活性。方法制备10种中草药提取物,采用试管连续稀释法对金黄色葡萄球菌、大肠埃希菌、铜绿假单胞菌和白色念珠菌进行体外抑菌试验。结果10种中草药的提取物对金黄色葡萄球菌、大肠埃希菌、铜绿假单胞菌和白色念珠菌有不同程度的抑制活性;其中尤以赤芍、石榴皮、五味子和黄连的提取物抗耐药菌活性最高,赤芍提取物对上述4种菌的抑制活性均较高,其最低抑菌浓度(MIC)分别为7.80、1.95、1.957、.80 mg/ml。结论赤芍、石榴皮、五味子和黄连提取物呈现广谱抗菌特性,且具有抗耐药菌作用。     

左氧氟沙星对牙周炎需氧及厌氧菌抗菌活性研究

目的 比较喹诺酮药物左氧氟沙星、氧氟沙星和环丙沙星对牙周炎需氧和厌氧菌抗菌活性。方法 牙周炎患者龈沟液中需氧和厌氧菌的分离培养。最低抑菌浓度(MIC)测定用琼脂稀释多点接触法。最低杀菌浓度(MBC)用肉汤稀释法，并用杀菌曲线方法比较两种喹诺酮药物杀菌性能。结果 喹诺酮药物有广谱的抗菌作用。左氧氟沙星对大肠埃希菌、肺炎链球菌、金黄色葡萄球菌、肠球菌和厌氧菌的MIC50分别为0．25、0．5、0．5、1和0．125μg／ml,，抗菌活性强于氧氟沙星和环丙沙星。对肺炎克雷伯菌、肠杆菌属细菌、变形菌、嗜血菌和不动杆菌的MIC50分别为＜0．03、＜0．03、＜0．03、0．125和0．03μg／ml，，抗菌活性强于氧氟沙星，但与环丙沙星相同。左氧氟沙星对铜绿假单胞菌抗菌活性稍弱于环丙沙星，左氧氟沙星的MIC是氧氟沙星和环丙沙星的2倍。结论 左氧氟沙星是一个广谱抗生素，对口腔需氧和厌氧菌显示了良好的抑菌和杀菌的活性。     

Synthesis and study of antibacterial and antifungal activities of novel 8-methyl-7,9-diaryl-1,2,4,8-tetraazaspiro[4.5]decan-3-thiones

Some novel spiropiperidinyl-1,2,4-triazolidin-3-thiones have been synthesized and studied for their antibacterial activity against Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa and antifungal activity against Candida albicans, Candida-6, Candida-51, Aspergillus niger and Aspergillus flavus. Compounds 30-32 exhibited potent in vitro antibacterial activity against E. coli and P. aeruginosa whereas the same set of compounds exerted potent in vitro antifungal activity against Candida-6, A. niger and A. flavus.     

Relationship between rates of antimicrobial consumption and the incidence of antimicrobial resistance in Staphylococcus aureus and Pseudomonas aeruginosa isolates from 47 French hospitals.

OBJECTIVE: To investigate relationships between rates of antimicrobial consumption and the incidence of antimicrobial resistance in Staphylococcus aureus and Pseudomonas aeruginosa isolates from hospitals. METHODS: We conducted an observational study that used retrospective data from 2002 and linear regression to model relationships. Hospitals were asked to collect data on consecutive S. aureus and P. aeruginosa isolates, consumption rates for antibiotics (ie, anti-infectives for systemic use as defined by Anatomical Therapeutic Chemical class J01), and hospital characteristics, including infection control policies. Rates of methicillin resistance in S. aureus and rates of ceftazidime and ciprofloxacin resistance in P. aeruginosa were expressed as the percentage of isolates that were nonsusceptible (ie, either resistant or intermediately susceptible) and as the incidence of nonsuceptible isolates (ie, the number of nonsuceptible isolates recovered per 1,000 patient-days). The rate of antimicrobial consumption was expressed as the number of defined daily doses per 1,000 patient-days. SETTING: Data were obtained from 47 French hospitals, and a total of 12,188 S. aureus isolates and 6,370 P. aeruginosa isolates were tested. RESULTS: In the multivariate analysis, fewer antimicrobials showed a significant association between the consumption rate and the percentage of isolates that were resistant than an association between the consumption rate and the incidence of resistance. The overall rate of antibiotic consumption, not including the antibiotics used to treat methicillin-resistant S. aureus infection, explained 13% of the variance between hospitals in the incidence of methicillin resistance among S. aureus isolates. The incidence of methicillin resistance in S. aureus isolates increased with the use of ciprofloxacin and levofloxacin and with the percentage of the hospital's beds located in intensive care units (adjusted multivariate coefficient of determination [aR(2)], 0.30). For P. aeruginosa, the incidence of ceftazidime resistance was greater in hospitals with higher consumption rates for ceftazidime, levofloxacin, and gentamicin (aR(2), 0.37). The incidence of ciprofloxacin resistance increased with the use of fluoroquinolones and with the percentage of a hospital's beds located in intensive care ( aR(2), 0.28). CONCLUSIONS: A statistically significant relationship existed between the rate of fluoroquinolone use and the rate of antimicrobial resistance among S. aureus and P. aeruginosa isolates. The incidence of resistant isolates showed a stronger association with the rate of antimicrobial use than did the percentage of isolates with resistance.     

铜陵地区细菌耐药性监测与分析

目的　研究铜陵地区临床分离菌对抗菌药物的耐药特征。方法　收集 2 0 0 0年 1月 1日至 2 0 0 1年12月 31日在铜陵地区 3所综合性医院临床分离的致病菌。采用Kirby -Bauer法进行药敏试验 ,按照美国临床实验标准委员会 2 0 0 0年判断标准分析结果。结果　 2年共收集致病菌 2 4 5 9株 ,包括革兰阳性球菌 911株(37.0 % ) ,革兰阴性杆菌 14 75株 (6 0 .0 % ) ;致病菌以表皮葡萄球菌、大肠埃希氏菌、铜绿假单胞菌、金黄色葡萄球菌、克雷伯氏菌属多见。有 79.9%的凝固酶阴性葡萄球菌和 5 0 .3%的金黄色葡萄球菌耐苯唑西林 ,对其它药物耐药率亦高。铜绿假单胞菌、克雷伯氏菌属、肠杆菌属、不动杆菌对第三代头孢菌素和氟喹诺酮类的耐药性均有显著增高。结论　合理用药和控制滥用是当务之急     

Synthesis and in vitro antimicrobial activity of some novel substituted benzimidazole derivatives having potent activity against MRSA

The novel benzimidazole derivatives (3, 5, 8, 9, 12-14, 18-41) were prepared in this paper and the antimicrobial activities of these compounds against Staphylococcus aureus, methicillin-resistant S. aureus (MRSA, standard and clinical isolates), Bacillus subtilis, Escherichia coli and Candida albicans were evaluated. Compounds 24-26 which have no substitution of N-1 position displayed better antibacterial activities than those of standards (ciprofloxacin, ampicillin and sultamicillin) against both the drug-resistant bacteria (MRSA, standard and clinical isolates). These derivatives (24-26), 2,5,6-trihalogenobenzimidazole analogues (8, 12), 5,6-dichloro-2-amino derivative (13), and 5-chloro-2-(4-benzyloxyphenyl)benzimidazole (35) exhibited the most potent antibacterial activity with MIC 3.12 microg/ml against S. aureus.     

A comparison of the antimicrobial resistance patterns of gram-negative bacilli isolated from community-private and university-affiliated hospitals from Puerto Rico

Few studies have been performed in Puerto Rico concerning the antimicrobial resistance pattern of clinically significant Gram-negative bacilli. The antimicrobial resistance patterns of 5,590 Gram-negative bacteria obtained from three Community-Private Hospitals (CPH) and three University-Affiliated Hospitals (UAH) were evaluated utilizing the institutions' antimicrobial susceptibility reports for the year 2000. The objectives of this study were: to retrospectively evaluate the reported in vitro resistance of clinical isolates of E. coli, K. pneumoniae, E. cloacae, S. marcescens, P. aeruginosa and A. baumannii to selected standard antibiotics and to compare the antimicrobial resistance patterns between Community-Private (CPH) and University Affiliated hospitals (UAH). E. coli was the most common Gram-negative enteric bacilli in both CPH and UAH. In UAH, E. coli demonstrated a statistically significant higher resistance to the selected beta lactams and amikacin antibiotics but not to ciprofloxacin or gentamicin. For K. pneumoniae, the antimicrobial resistant pattern showed that UAH isolates were significantly more resistant to the tested antibiotics with the exception of ceftriaxone. In CPH, E. cloacae isolates were significantly more resistant to piperacillin-tazobactam, ciprofloxacin and gentamicin, while in UAH this organism was more resistant to amikacin. In UAH, S. marcescens isolates demonstrated a statistically significant higher resistance to all tested antibiotics with the exception of imipenem, which was similar in both hospitals group. Pseudomonas aeruginosa demonstrated a statistically significant higher resistance in UAH to all selected antibiotics with the exception of ciprofloxacin and gentamicin, which was similar in both hospitals group. Acinetobacter baumannii was the most resistant organisms in both hospitals group. UAH isolates were significantly more resistant than CPH isolates for all tested antibiotics. When compare with other large-scale antimicrobial resistance studies, the present study results suggest an apparent higher resistance in the Puerto Rican isolates. The high numbers of antimicrobial resistant Gram-negative bacilli in our study strongly suggest multiple mechanisms of antimicrobial resistance including the presence of extended spectrum and chromosomally derepressed beta-lactamases.     

尿液pH对常见泌尿系感染细菌抗生素敏感性的影响

目的 探讨尿液pH对常见泌尿系感染细菌抗生素敏感性的影响。方法 配制不同pH的人工尿液,以大肠杆菌、表皮葡萄球菌、金黄色葡萄球菌、产超广谱β-内酰胺酶(extended-spectrum β-lactamases,ESBL)的肺炎克雷伯菌和产ESBL的铜绿假单胞菌为研究菌种,环丙沙星、左氧氟沙星、磷霉素氨丁三醇和头孢呋辛为研究药物,采用药敏试验中的微量肉汤稀释法比较不同抗生素在不同pH的人工尿液培养基中的抗菌效力。结果 环丙沙星对大肠杆菌、表皮葡萄球菌和产ESBL的肺炎克雷伯菌的抗菌效果随着pH升高而升高;左氧氟沙星对大肠杆菌和表皮葡萄球菌的抗菌效果亦随着pH升高而升高;磷霉素对大肠杆菌、表皮葡萄球菌和金黄色葡萄球菌的抗菌效果随着pH的升高而降低;头孢呋辛对大肠杆菌和金黄色葡萄球菌的抗菌效果亦随着pH的升高而降低。结论 通过调节尿液pH能够改变致病菌对抗生素的敏感性,以期在临床上提高抗生素对泌尿系感染的治疗效果。     

Carbapenem-based prodrugs. Design, synthesis, and biological evaluation of carbapenems

Syntheses of racemic trans-3-hydroxycarbonyl-6-(phenylacetamido)carbapenem (13), trans-3-phosphono-6-(phenylacetamido)carbapenem (17), and beta-lactam based prodrugs 19 and 22 were accomplished. Carbapenem 13 was found to possess antibacterial activity, comparable with imipenem (+)-3, against Staphylococcus aureus FDA 209P, S. aureus 95, Escherichia coli ATCC 39188, Klebsiella pneumoniae NCTC 418, Pseudomonas aeruginosa 1101-75, P. aeruginosa 18S-H, and Xanthomonas maltophilia GN 12873. Like imipenem ((+)-3), carbapenem 13 was not stable to X. maltophilia oxyiminocephalosporinase type II. Its phosphonate analog 17, however, was neither a significant antibacterial agent nor a good beta-lactamase inhibitor. Chemical combinations of trans carbapenem 13 with cis carbapenem 6 (compound 19) as well as clavulanic acid (20) with cis carbapenem 6 (compound 22) via a tetrachloroethane linker exhibited remarkable activity against beta-lactamase producing microorganisms in vitro.     

Investigating the antimicrobial activity of natural honey and its effects on the pathogenic bacterial infections of surgical wounds and conjunctiva

Antimicrobial activities of 10-100% (wt/vol) concentrations of new honey, stored honey, heated honey, ultraviolet-exposed honey, and heated stored honey were tested against common human pathogens, including Escherichia coli, Entrobacter cloacae, Pseudomonas aeruginosa, Shigella dysenteriae, Klebsiella sp., Haemophilus influenzae, Proteus sp., Staphylococcus aureus, Streptococcus hemolyticus group B, and Candida albicans. Antimicrobial activity of honey was tested in acidic, neutral, or alkaline media. These were compared with similar concentrations of glucose in nutrient broth. Surgical wounds were made on the dorsum of mice and infected with S. aureus or Klebsiella sp. The wounds were treated with local application of honey four times a day or appropriate antibiotics and compared with control values. Bacterial conjunctivitis due to E. coli, Proteus sp., S. aureus, Klebsiella sp., and P. aeruginosa was induced in rats. Conjunctival application of honey four times a day or appropriate antibiotics was used for treatment and compared with control values. Growth of all the isolates was completely inhibited by 30-100% honey concentrations. The most sensitive microbes were E. coli, P. aeruginosa, and H. influenzae. Glucose showed less antimicrobial activity than honey, and many microbes showed positive culture even in 100% glucose. Heating to 80 degrees C for 1 hour decreased antimicrobial activity of both new and stored honey. Storage of honey for 5 years decreased its antimicrobial activity, while ultraviolet light exposure increased its activity against some of the microorganisms. Antimicrobial activity of honey was stronger in acidic media than in neutral or alkaline media. Single doses of honey used to prepare the 60% concentration in nutrient broth were bacteriocidal for P. aeruginosa and bacteriostatic for S. aureus and Klebsiella sp. during certain periods. Local application of raw honey on infected wounds reduced redness, swelling, time for complete resolution of lesion, and time for eradication of bacterial infection due to S. aureus or Klebsiella sp. Its potency was comparable to that of local antibiotics. Honey application into infective conjunctivitis reduced redness, swelling, pus discharge, and time for eradication of bacterial infections due to all the isolates tested.