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https://www.readbyqxmd.com/read/28748397/activity-of-the-novel-siderophore-cephalosporin-cefiderocol-against-multidrug-resistant-gram-negative-pathogens
#1
J Dobias, V Dénervaud-Tendon, L Poirel, P Nordmann
The novel siderophore cephalosporin cefiderocol (S-649266) with potent activity against Gram-negative pathogens was recently developed (Shionogi & Co., Ltd.). Here, we evaluated the activity of this new molecule and comparators against a collection of previously characterized Gram-negative isolates using broth microdilution panels. A total of 753 clinical multidrug-resistant Gram-negative isolates collected from hospitals worldwide were tested against cefiderocol and antibiotic comparators (ceftolozane-tazobactam [CT], meropenem [MEM], ceftazidime [CAZ], ceftazidime-avibactam [CZA], colistin [CST], aztreonam [ATM], amikacin [AMK], ciprofloxacin [CIP], cefepime [FEP], and tigecycline [TGC]) for their susceptibility...
July 26, 2017: European Journal of Clinical Microbiology & Infectious Diseases
https://www.readbyqxmd.com/read/28746830/biophysical-characterization-of-e-coli-tolc-interaction-with-the-known-blocker-hexaamminecobalt
#2
A Gilardi, S P Bhamidimarri, M Brönstrup, U Bilitewski, R K R Marreddy, K M Pos, L Benier, P Gribbon, M Winterhalter, B Windshügel
BACKGROUND: The tripartite efflux pump AcrAB-TolC in E. coli is involved in drug resistance by transporting antibiotics out of the cell. The outer membrane protein TolC can be blocked by various cations, including hexaamminecobalt, thereby TolC represents a potential target for reducing antimicrobial resistance as its blockage may improve efficacy of antibiotics. METHODS: We utilized single channel electrophysiology measurements for studying TolC conductance in absence and presence of the known TolC blocker hexaamminecobalt...
July 23, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28745975/identification-of-chemical-compounds-that-inhibit-the-function-of-histidyl-trna-synthetase-from-pseudomonas-aeruginosa
#3
Yanmei Hu, Stephanie O Palmer, Sara T Robles, Tahyra Resto, Frank B Dean, James M Bullard
Pseudomonas aeruginosa histidyl-tRNA synthetase (HisRS) was selected as a target for antibiotic drug development. The HisRS protein was overexpressed in Escherichia coli and kinetically evaluated. The KM values for interaction of HisRS with its three substrates, histidine, ATP, and tRNA(His), were 37.6, 298.5, and 1.5 μM, while the turnover numbers were 8.32, 16.8, and 0.57 s(-1), respectively. A robust screening assay was developed, and 800 natural products and 890 synthetic compounds were screened for inhibition of activity...
July 1, 2017: SLAS Discovery
https://www.readbyqxmd.com/read/28744944/violacein-antimicrobial-activity-on-staphylococcus-epidermidis-and-synergistic-effect-on-commercially-available-antibiotics
#4
Hilania Valéria Dodou, Andressa Hellen de Morais Batista, Gleilton Weyne Passos Sales, Suelen Carneiro de Mendonça, Matheus Lima Rodrigues, Patrícia Coelho do Nascimento Nogueira, Edilberto Rocha Silveira, Nádia Accioly Pinto Nogueira
AIMS: The study aimed to assess whether violacein has antimicrobial activity on S. epidermidis and synergistically modulates the action of commercially-available antimicrobial drugs. METHODS AND RESULTS: Violacein showed excellent antimicrobial activity on biofilm-forming and non-biofilm forming S. epidermidis strains (ATCC 35984) (ATCC 12228), with bacteriostatic (MIC = 20 μg.mL(-1) and 10 μg.mL(-1) , respectively) and bactericidal effects (MBC = 20 μg.mL(-1) for both strains), observed in short periods of exposure...
July 26, 2017: Journal of Applied Microbiology
https://www.readbyqxmd.com/read/28743810/polymyxin-combinations-combat-escherichia-coli-harboring-mcr-1-and-blandm-5-preparation-for-a-postantibiotic-era
#5
Zackery P Bulman, Liang Chen, Thomas J Walsh, Michael J Satlin, Yuli Qian, Jürgen B Bulitta, Charles A Peloquin, Patricia N Holden, Roger L Nation, Jian Li, Barry N Kreiswirth, Brian T Tsuji
The rapid increase of carbapenem resistance in Gram-negative bacteria has resurrected the importance of the polymyxin antibiotics. The recent discovery of plasmid-mediated polymyxin resistance (mcr-1) in carbapenem-resistant Enterobacteriaceae serves as an important indicator that the golden era of antibiotics is under serious threat. We assessed the bacterial killing of 15 different FDA-approved antibiotics alone and in combination with polymyxin B in time-killing experiments against Escherichia coli MCR1_NJ, the first reported isolate in the United States to coharbor mcr-1 and a New Delhi metallo-β-lactamase gene (blaNDM-5)...
July 25, 2017: MBio
https://www.readbyqxmd.com/read/28743748/design-and-synthesis-of-theranostic-antibiotic-nanodrugs-that-display-enhanced-antibacterial-activity-and-luminescence
#6
Sheng Xie, Sesha Manuguri, Giampiero Proietti, Joakim Romson, Ying Fu, A Ken Inge, Bin Wu, Yang Zhang, Daniel Häll, Olof Ramström, Mingdi Yan
We report the modular formulation of ciprofloxacin-based pure theranostic nanodrugs that display enhanced antibacterial activities, as well as aggregation-induced emission (AIE) enhancement that was successfully used to image bacteria. The drug derivatives, consisting of ciprofloxacin, a perfluoroaryl ring, and a phenyl ring linked by an amidine bond, were efficiently synthesized by a straightforward protocol from a perfluoroaryl azide, ciprofloxacin, and an aldehyde in acetone at room temperature. These compounds are propeller-shaped, and upon precipitation into water, readily assembled into stable nanoaggregates that transformed ciprofloxacin derivatives into AIE-active luminogens...
July 25, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28741095/phenotype-microarray-analysis-of-the-aders-two-component-system-in-acinetobacter-baumannii
#7
J-R Sun, Y-S Chiang, H-S Shang, C-L Perng, Y-S Yang, T-S Chiueh
Acinetobacter baumannii is a nosocomial pathogen capable of resistance to multiple antimicrobials. The AdeRS two-component system (TCS) is associated with antimicrobial resistance by controlling the AdeABC efflux pump. To elucidate modulation by AdeRS, we made an A. baumannii mutant lacking the AdeRS TCS and characterized it using phenotype microarray (PM) analysis. After disrupting the adeRS operon, lower expression of AdeABC efflux pump was observed in the mutant strain. PM analysis showed that the AdeRS deletion strain and parental strain presented different tolerances to 91 compounds...
July 24, 2017: European Journal of Clinical Microbiology & Infectious Diseases
https://www.readbyqxmd.com/read/28739794/population-pharmacokinetics-of-azd-5847-in-adults-with-pulmonary-tuberculosis
#8
Abdullah Alsultan, Jennifer J Furin, Jeannine Du Bois, Elana van Brakel, Phalkun Chheng, Amour Venter, Bonnie Thiel, Sara A Debanne, W Henry Boom, Andreas H Diacon, John L Johnson, Charles A Peloquin
AZD-5847 is a new oxazolidinone derivative under development for the treatment of tuberculosis. In this study we describe the population pharmacokinetics of AZD-5847 in patients with tuberculosis based on a recently completed phase II study. The study included 60 patients with drug susceptible TB. Patients were randomized to four doses (500 mg once daily, 1200 mg once daily, 500 mg twice daily and 800 mg twice daily). Patients were intensively sampled on day 1 and 14. AZD-5847 pharmacokinetics were best described with a two compartment system with tlag for absorption...
July 24, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28738715/antimicrobial-modulatory-and-chemical-analysis-of-the-oil-of-croton-limae
#9
Tiago Rodrigues Leite, Maria Arlene Pessoa da Silva, Antônio Carlito Bezerra Dos Santos, Henrique Douglas Melo Coutinho, Antonia Eliene Duarte, José Galberto Martins da Costa
CONTEXT: Croton sp. are plants with a well-reported antimicrobial activity. Croton limae A.P. Gomes, M.F. Sales P.E. Berry (Euphorbiaceae), known as 'marmeleiro-prateado', is commonly used to manage abdominal pain in Brazil. OBJECTIVE: This work evaluates the phytochemical composition, antimicrobial and modulatory activities of the essential oil of C. limae leaves (EOCL). MATERIALS AND METHODS: The minimum inhibitory concentration (MIC) and the modulation of the antibiotic activity were determined using a microdilution method...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/28736816/antinociceptive-activity-of-ent-dihydrotucumanoic-acid-isolated-from-gymnosperma-glutinosum-spreng-less
#10
Angel Josabad Alonso-Castro, Marco Martin González-Chávez, Juan Ramón Zapata-Morales, Alexia Karina Verdinez-Portales, Amanda Sánchez-Recillas, Rolffy Ortiz-Andrade, Mario Isiordia-Espinoza, Fidel Martínez-Gutiérrez, Marco Antonio Ramírez-Morales, Fabiola Domínguez, María Elizabeth Juache-Flores, Roberto Martínez
Preclinical Research The diterpene ent-dihydrotumanoic acid (DTA) was among the compounds isolated from Gymnosperma glutinosum (Spreng) Less (Asteraceae). There are no reports regarding the pharmacological effects of DTA. Cytotoxicity against cancer cells (1-250 µM), and the antibacterial (50-1400 µM) activity of DTA were evaluated using the MTT assay, and the minimum inhibitory concentration test, respectively. The antidiarrheal (1-100 mg/kg p.o.) and anti-inflammatory (2 mg/ear) effects of DTA were evaluated using castor oil and 12-O-tetradecanoylphorbol-13-acetate, respectively...
July 24, 2017: Drug Development Research
https://www.readbyqxmd.com/read/28735083/incidence-of-methicillin-resistant-staphylococcus-aureus-mrsa-in-microbial-community-of-cancer-patients-and-evaluation-of-their-resistant-pattern
#11
Mervat Morsy Abbas Ahmed El-Gendy, Ahmed Mohamed Ahmed El-Bondkly, Abeer Ali Keera, Amal Mohamed Ali
Cancer patients are prone to MRSA infection due to a number of factors include prolongedhospitalization, intravascular catheterization, compromised host immunity, malignancy, chemotherapy, radiotherapy surgery, prior antibiotic therapy and prolonged operative time. Among 468 Staphylococcus isolates, 283 were methicillin resistant Staphylococcus aureus isolates (MRSA), which indicated the occurrence and prevalence of MRSA isolates among cancer patients. The highest number of MRSA strains were isolated from male (124 isolates), female (90 isolates) followed by children (69 isolates) which represent 43...
July 19, 2017: Microbial Pathogenesis
https://www.readbyqxmd.com/read/28735054/linezolid-activity-against-clinical-gram-positive-cocci-with-advanced-antimicrobial-drug-resistance-in-iran
#12
Hamidreza Houri, Hossein Kazemian, Hadi Sedigh Ebrahim-Saraie, Asieh Taji, Zahra Tayebi, Hamid Heidari
OBJECTIVES: The aim of the study was to investigate the linezolid activity against clinical Gram-positive cocci with advanced antimicrobial drug resistance. METHODS: A collection of methicillin resistant Staphylococcus aureus (MRSA), vancomycin resistant enterococci (VRE), penicillin non-susceptible Streptococcus pneumoniae (PNSP), and group B streptococci (GBS) were isolated from various clinical samples. Antimicrobial susceptibility tests were done using standard methods Subsequently, we investigated linezolid antibacterial activities, the first approved oxazolidinone against isolates by the standard broth microdilution method...
July 19, 2017: Journal of Global Antimicrobial Resistance
https://www.readbyqxmd.com/read/28735049/in-vitro-activity-of-daptomycin-combinations-with-rifampicin-gentamicin-fosfomycin-and-fusidic-acid-against-mrsa-strains
#13
Gulseren Aktas, Sengul Derbentli
OBJECTIVES: Although new antimicrobial agents designed to treat infections with limited therapeutic options have been introduced in the past few years, resistant Gram positive cocci have continued to emerge and spread. Daptomycin is a cyclic lipopeptide antibiotic that has rapid bactericidal activity against broad spectrum of Gram positive bacteria, including methicillin resistant Staphylococcus aureus (MRSA). Antibiotics are sometimes used in combination in an attempt to prevent or delay the in vivo emergence of drug-resistant subpopulations of pathogenic organisms...
July 19, 2017: Journal of Global Antimicrobial Resistance
https://www.readbyqxmd.com/read/28735046/ceftolozane-tazobactam-activity-against-drug-resistant-enterobacteriaceae-and-pseudomonas-aeruginosa-causing-healthcare-associated-infections-in-australia-and-new-zealand-report-from-an-antimicrobial-surveillance-program-2013-2015
#14
M A Pfaller, D Shortridge, H S Sader, R K Flamm, M Castaneheira
OBJECTIVES: To evaluate the in vitro activity of ceftolozane-tazobactam and comparator agents tested against isolates of Enterobacteriaceae and Pseudomonas aeruginosa from patients in Australia and New Zealand with healthcare-associated infection. METHODS: A total of 1,459 gram-negative organisms (440P. aeruginosa and 1,019 Enterobacteriaceae) were consecutively collected from 11 medical centers located in Australia and New Zealand. The organisms were tested for susceptibility by broth microdilution methods as described by the CLSI M07-A10 document and the results interpreted according to EUCAST and CLSI breakpoint criteria...
July 19, 2017: Journal of Global Antimicrobial Resistance
https://www.readbyqxmd.com/read/28724328/smart-tetrazole-based-antibacterial-nanoparticles-as-multifunctional-drug-carriers-for-cancer-combination-therapy
#15
Elham Zakerzadeh, Roya Salehi, Mehrdad Mahkam
Due to multidrug resistance of cancer tissues and immune-suppression of cancerous patients during chemotherapy in one hand and the use of tetrazole derivatives in medicine because of its anticancer, antifungal and antiviral properties, on the other, we were encouraged to design novel smart antibacterial nanocomposites-based polymer of tetrazole as dual anticancer drug delivery systems. The structures of nanocomposites characterized by FTIR, (1)H NMR, FESEM-EDX and TGA analyses and antibacterial activity of smart carriers were evaluated by determination of minimum inhibitory concentration (MIC) values against some bacteria and fungi...
July 20, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28717309/molecular-characterization-of-antibiotic-resistant-staphylococcus-aureus-from-livestock-bovine-and-swine
#16
Asima Zehra, Randhir Singh, Simranpreet Kaur, J P S Gill
AIM: The aim of this study was to figure the prevalence, phenotypic and genotypic antibiotic resistance (AR) pattern of Staphylococcus aureus isolated from bovine and swine nares. MATERIALS AND METHODS: Colonies with typical morphology on Baird-Parker agar supplemented with egg-yolk tellurite emulsion were selected and biochemically/genotypically identified as S. aureus. These strains were further subjected to epsilometer test for their sensitivity to various clinically important antibiotics and antibiotic susceptibility testing for amoxicillin/clavulanic acid, and double-disk diffusion testing was performed by the standard disc diffusion method following CLSI guidelines...
June 2017: Veterinary World
https://www.readbyqxmd.com/read/28716360/comparison-of-synergism-between-colistin-fosfomycin-and-tigecycline-against-extended-spectrum-%C3%AE-lactamase-producing-klebsiella-pneumoniae-isolates-or-with-carbapenem-resistance
#17
Yee-Huang Ku, Chi-Chung Chen, Mei-Feng Lee, Yin-Ching Chuang, Hung-Jen Tang, Wen-Liang Yu
PURPOSE: To investigate the synergistic and bactericidal effects of antimicrobial combinations of any two of colistin, fosfomycin and tigecycline against the nine extended-spectrum β-lactamase (ESBL)-producing Klebsiella pneumoniae (KP) clinical isolates, including 4 carbapenem-susceptible strains and five imipenem and/or meropenem-resistant strains. METHODS: In vitro synergism and bactericidal activity of combination of colistin, fosfomycin and tigecycline were evaluated by time-kill studies in standard inoculum of bacterial densities of a suspension containing 5 × 10(5) CFU/mL by using 1/2× MIC for each alone, and both 1/2× and 1/4× MIC for any two drugs...
July 6, 2017: Journal of Microbiology, Immunology, and Infection, Wei Mian Yu Gan Ran za Zhi
https://www.readbyqxmd.com/read/28709989/evaluating-biapenem-dosage-regimens-in-intensive-care-unit-patients-with-pseudomonas-aeruginosa-infections-a-pharmacokinetic-pharmacodynamic-analysis-using-monte-carlo-simulation
#18
Yongfu Hang, Yafang Chen, Ling Xue, Shusen Sun, Long Liu, Jie Gao, Cheng Xie, Xianfeng Zhang, Jianguo Zhu, Jun Jin, Liyan Miao
This study sought to both identify optimal dosage regimens and estimate pharmacokinetic/pharmacodynamics characteristics of short-infusion (SI) versus extended-infusion (EI) for the use of biapenem against Pseudomonas aeruginosa infections in Chinese Intensive Care patients. A total of 85 strains of P. aeruginosa were collected, and the minimum inhibitory concentration (MIC) of biapenem was measured by the serial two-fold agar dilution method. We designed four frequently used clinical regimens: biapenem 300mg I...
July 11, 2017: International Journal of Antimicrobial Agents
https://www.readbyqxmd.com/read/28706331/bioequivalence-of-generic-and-branded-amoxicillin-capsules-in-healthy-human-volunteers
#19
Priyanka Pathak, Vijaya A Pandit, Priti P Dhande
CONTEXT: The Medical Council of India urges doctors to prescribe generic drugs as far as possible. The Indian Medical Association had responded earlier saying that it requires guarantees on the quality of generic forms of drugs. Although no published scientific reports are available on the issue of therapeutic inequivalence, unconfirmed clinician accounts and newspaper reports of therapeutic inequivalence exist. AIM: This study was planned to ascertain whether bioequivalence of branded and generic amoxicillin capsule is comparable...
March 2017: Indian Journal of Pharmacology
https://www.readbyqxmd.com/read/28705747/synthesis-of-phytochemicals-stabilized-gold-nanoparticles-and-their-biological-activities-against-bacteria-and-leishmania
#20
Aftab Ahmad, Yun Wei, Sadeeq Ullah, Sayyed Ibrahim Shah, Fazli Nasir, Akram Shah, Zafar Iqbal, Kamran Tahir, Usman Ali Khan, Qipeng Yuan
Nanoscale materials have shown promising results in the field of medicine as therapeutic agents and drugs delivery vehicles. In the current study, gold nanoparticles (AuNPs) were prepared by a green and facile method using the aqueous extract of Rhazya stricta decne as a source of reducing and stabilizing agents. The bio-fabricated AuNPs were characterized by UV-visible spectroscopy, X-ray diffraction (XRD), Transmission electron microscopy (TEM) and FTIR spectroscopy. Antimicrobial activities of the biosynthesized AuNPs were tested against Leishmania tropica (HTD7), E...
July 11, 2017: Microbial Pathogenesis
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