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T Didbaridze, L Saginashvili, L Akhmeteli, B Iremashvili, N Gogokhia
This study provides a contemporary epidemiology of aspirates taken during surgery from the abdominal cavity among patients with bacterial peritonitis to identify the isolates and study their sensitivity to antibiotics. Our bacteriology investigations included isolation of poor cultures, and detection of microbes was conducted using a rapid identification system (API20E, API Staph, API Strep, API Ana, BioMerieux). Rapid tests for detection of oxidase and catalase activity were also used. Susceptibility of microorganisms to antibiotics was defined by the disc-diffusion method using standard discs (EUCAST guidelines 2015) according to Clinical Laboratory Standard Institute (CLSI) protocols (ATB strips: ATB G, ATB Staph, ATBANA, ATBPse, ATBStrep...
September 2016: Georgian Medical News
Chao-Ming Hung, Ying-Chao Lin, Liang-Chih Liu, Sheng-Chu Kuo, Chi-Tang Ho, Tzong-Der Way
CWF-145, a synthetic 2-phenyl-4-quinolone derivative exerted potent cytotoxicity against prostate cancer. CWF-145 inhibited prostate cancer cell lines PC-3, DU-145 and LNCap. It had a very low IC50 about 200 nM against castrate-resistant prostate cancer (CRPC) PC-3. We found that CWF-145 had a similar effect to clinical trial antimitotic agents in cancer cells and normal cells. CWF-145 arrested cell cycle at G2/M phase by binding to the β-tubulin at the colchicine-binding site then disrupted microtubule polymerization...
October 18, 2016: Chemico-biological Interactions
Yu Cheng, Srinivasa Rao Avula, Wei-Wei Gao, Dinesh Addla, Vijai Kumar Reddy Tangadanchu, Ling Zhang, Jian-Mei Lin, Cheng-He Zhou
A series of new potentially multi-targeting antimicrobial 2-aminothiazolyl quinolones were designed, synthesized and characterized by (1)H NMR, (13)C NMR, IR, MS and HRMS spectra. Bioactive assay manifested that some of the prepared compounds showed moderate to good antibacterial and antifungal activities. Noticeably, compound 10f could effectively inhibit the growth of B. typhi and MRSA with MIC values of 1 and 8 μg/mL, respectively. Experimental results revealed that compound 10f was membrane-active and had the ability to rapidly kill the tested strains and effectively prevent the development of bacterial resistance...
October 7, 2016: European Journal of Medicinal Chemistry
Kenji Sugawara, Kohei Honda, Yoshie Reien, Norihide Yokoi, Chihiro Seki, Harumi Takahashi, Kohtaro Minami, Ichiro Mori, Akio Matsumoto, Haruaki Nakaya, Susumu Seino
Insulin secretagogues are used for treatment of type 2 diabetes. We attempted to discover novel small molecules to stimulate insulin secretion by using in silico similarity search using sulfonylureas as query, followed by measurement of insulin secretion. Among 38 compounds selected by in silico similarity search, we found three diphenylsemicarbazides and one quinolone that stimulate insulin secretion. We focused on compound 8 (C8), which had the strongest insulin-secreting effect. Based on the structure-activity relationship of C8-derivatives, we identified diphenylthiosemicarbazide (DSC) 108 as the most potent secretagogue...
2016: PloS One
Balasundaram Preethi, Veerappapillai Shanthi, Karuppasamy Ramanathan
BACKGROUND: Salmonella typhimurium is the main cause of gastrointestinal illness in humans, and treatment options are decreasing because drug-resistant strains have emerged. OBJECTIVE: The objective of this study was to use computational drug repurposing to identify a novel candidate with an effective mechanism of action to circumvent the drug resistance. METHODS: We used the Mantra 2.0 database to initially screen drug candidates that share similar gene expression profiles to those of quinolones...
October 19, 2016: BioDrugs: Clinical Immunotherapeutics, Biopharmaceuticals and Gene Therapy
Lyudmila Boyanova, Rumyana Markovska, Ivan Mitov
This review focuses on the virulence arsenal of the most pathogenic species among Gram positive anaerobic cocci, Finegoldia magna according to recently published data from 2012-2016. Virulence factors like sortase dependent pili and F. magna adhesion factor (FAF) facilitate the start of the infection. Albumin binding protein (PAB) enhances F. magna survival. FAF, subtilisin-like extracellular serine protease (SufA) and superantigen protein L protect the bacteria from factors of innate defense system. SufA, capsule and tissue-destroying enzymes provide a deep penetration or spread of the infections and the protein L is associated with infection severity...
October 15, 2016: Anaerobe
Kusum Mehla, Jayashree Ramana
Travelers' diarrhea (TD) is one of the most important global health issues among international travelers, especially those traveling to developing countries. Enterotoxigenic Escherichia coli (ETEC) is the most frequently isolated pathogen causing TD. Although TD is self-limiting, it is also severely incapacitating. Ciprofloxacin is one of the standard quinolone antibiotics used in patients with TD. However, the alarming levels of antibiotic resistance have necessitated the urgent need to identify new drugs...
October 18, 2016: Omics: a Journal of Integrative Biology
Wenyao Chen, Tingzi Fang, Xiujuan Zhou, Daofeng Zhang, Xianming Shi, Chunlei Shi
The wide usage of antibiotics contributes to the increase in the prevalence of antibiotic-resistant Salmonella. Plasmids play a critical role in horizontal transfer of antibiotic resistance markers in Salmonella. This study aimed to screen and characterize plasmid profiles responsible for antibiotic resistance in Salmonella and ultimately to clarify the molecular mechanism of transferable plasmid-mediated antibiotic resistance. A total of 226 Salmonella isolates were examined for antimicrobial susceptibility by a disk diffusion method...
2016: Frontiers in Microbiology
Ikue Okamura, Yukitsugu Nakamura, Yuka Katsurada, Ken Sato, Takashi Ikeda, Fumihiko Kimura
Purpura fulminans (PF) is a life-threatening syndrome comprising progressive hemorrhagic necrosis due to disseminated intravascular coagulation and dermal vascular thrombosis that leads to purpura and tissue necrosis. Various therapies have been used to arrest the progression of this disease, however, there is no established treatment because of the variety of underlying causes. We herein present an adult case of PF associated with leukocytoclastic vasculitis triggered by antibiotic (levofloxacin) intake. As a result of our rapid and accurate identification of the underlying cause, corticosteroid therapy successfully repressed the inflammatory process...
2016: Internal Medicine
Daisuke Nakano, Kenji Ishitsuka, Narumi Matsuda, Ai Kouguchi, Ryota Tsuchihashi, Masafumi Okawa, Hikaru Okabe, Kazuo Tamura, Junei Kinjo
During the course of our studies towards the identification of promising chemotherapeutic candidates from plants against two human T-cell lymphotropic virus type I-infected T-cell lines (MT-1 and MT-2), we screened 17 extracts from 9 rutaceous plants against MT-1 and MT-2 cells. The extracts from the aerial parts and roots of Boenninghausenia japonica, as well as the leaves and roots of Ruta graveolens showed potent antiproliferative effects. After activity-guided fractionation, we isolated 44 compounds from two rutaceous plants, including three new compounds (1-3), which were classified into 26 coumarin analogs (13 coumarins, 8 furanocoumarins, 4 dihydrofuranocoumarins and one dihydropyranocoumarin), 15 alkaloid analogs (7 quinolone alkaloids, 4 acridone alkaloids, 3 furanoquinoline alkaloids and one tetrahydroacridone alkaloid) and 3 flavonoid glycosides...
October 13, 2016: Journal of Natural Medicines
Constantin Hays, Mathilde Louis, Céline Plainvert, Nicolas Dmytruk, Gérald Touak, Patrick Trieu-Cuot, Claire Poyart, Asmaa Tazi
Group B Streptococcus (GBS) is the leading cause of neonatal invasive infections and an emerging pathogen in the elderly. Our objectives were to describe the evolution of GBS resistance to antibiotics in France and to investigate the emergence of fluoroquinolone (FQ) resistant isolates. A total of 8,757 unrelated GBS isolates were collected and tested for antibiotic susceptibility from 2007 and 2014 according to EUCAST recommendations. All isolates were susceptible to penicillin G, amoxicillin, and vancomycin...
October 10, 2016: Antimicrobial Agents and Chemotherapy
Betitera Yanat, Radia Dali Yahia, Leila Yazi, Jesús Machuca, Paula Díaz-De-Alba, Abdelaziz Touati, Álvaro Pascual, José-Manuel Rodríguez-Martínez
QepA is a plasmid-mediated quinolone resistance determinant of low prevalence described worldwide, mainly in Enterobacteriaceae. This study describes, for the first time in Algeria, two clonally related, QepA-producing Escherichia coli clinical isolates positive for CTX-M-15. The clonal spread of these multidrug-resistant isolates is a major public health concern.
October 13, 2016: Microbial Drug Resistance: MDR: Mechanisms, Epidemiology, and Disease
Nandini Chatterjee, Chandan Chatterjee, Sinjan Ghosh, Mainak Mukhopadhyay, Ramkrishna Brahmachari, Kartik Patar
BACKGROUND: Indiscriminate use of antibiotics in urinary tract infections have led to emergence of 'superbugs' worldwide. Periodical review of antibiograms is of utmost importance for optimum patient benefit. OBJECTIVE: To identify the spectrum of organisms responsible for urinary tract infection and evaluate the pattern of antibiotic sensitivity of the organisms. METHODS: Urine samples were collected from all consecutive patients getting admitted in the medicine indoor irrespective of symptomatology...
April 2016: Journal of the Association of Physicians of India
Wei Chen, Bei Li, Shuai Li, Yi-Wen Ou, Qin Ou
<strong>Objective</strong> To explore the effects of Scutellaria baicalensis on activity and biofilm formation of Klebsiella pneumonia (Kp).<strong>Methods</strong> The broth and agar dilution Methods were carried out to determine minimum inhibitory concentration and minimum bactericidal concentration of Scutellaria baicalensis for TW518. VITEK-32 system was used to assay TW518 susceptibility to antibiotics. Kp biofilms were formed in vitro and stained with BacLight Live/Dead stain. The class integron geneⅠ1 mRNA expression was analyzed with RT-PCR...
September 20, 2016: Chinese Medical Sciences Journal, Chung-kuo i Hsüeh K'o Hsüeh Tsa Chih
Andreas Thomann, Christian Brengel, Carsten Börger, Dagmar Kail, Anke Steinbach, Martin Empting, Rolf W Hartmann
Drug-resistant Pseudomonas aeruginosa (PA) strains are on the rise, making treatment with current antibiotics ineffective. Hence, circumventing resistance or restoring the activity of antibiotics by novel approaches is of high demand. Targeting the Pseudomonas quinolone signal quorum sensing (PQS-QS) system is an intriguing strategy to abolish PA pathogenicity without affecting the viability of the pathogen. Herein we report the structure-activity relationships of 2-sulfonylpyrimidines, which were previously identified as dual-target inhibitors of the PQS receptor PqsR and the PQS synthase PqsD...
October 12, 2016: ChemMedChem
Ezequiel Albornoz, Celeste Lucero, Genara Romero, María Paula Quiroga, Melina Rapoport, Leonor Guerriero, Patricia Andres, Cecilia Rodriguez, Marcelo Galas, Daniela Centrón, Alejandra Corso, Alejandro Petroni
This first nationwide study was conducted to analyze the prevalence of plasmid-mediated quinolone resistance (PMQR) genes in phenotypically unselected (consecutive) clinical enterobacteria. We studied 1,058 isolates that had been consecutively collected in 66 hospitals of the WHONET-Argentina Resistance Surveillance Network. Overall, 26% of isolates were nonsusceptible to at least one of the three quinolones tested (nalidixic acid, ciprofloxacin, and levofloxacin). The overall prevalence of PMQR genes was 8...
October 11, 2016: Microbial Drug Resistance: MDR: Mechanisms, Epidemiology, and Disease
Dávid Szamosvári, Valentin F Reichle, Monica Jureschi, Thomas Böttcher
We explore the chemical space of Pseudomonas quinolone signal analogs as privileged structures and report the discovery of a thioquinolone as a potent inhibitor of the important virulence factor elastase of the human pathogen Pseudomonas aeruginosa. We provide evidence that the derivative binds to the active site zinc of elastase and additionally acts as a fluorescent zinc sensor.
October 6, 2016: Chemical Communications: Chem Comm
Rustam Aminov
The introduction of antibiotics into clinical practice revolutionized the treatment and management of infectious diseases. Before the introduction of antibiotics, these diseases were the leading cause of morbidity and mortality in human populations. This review presents a brief history of discovery of the main antimicrobial classes (arsphenamines, β-lactams, sulphonamides, polypeptides, aminoglycosides, tetracyclines, amphenicols, lipopeptides, macrolides, oxazolidinones, glycopeptides, streptogramins, ansamycins, quinolones, and lincosamides) that have changed the landscape of contemporary medicine...
October 5, 2016: Biochemical Pharmacology
G P Danezis, C J Anagnostopoulos, K Liapis, M A Koupparis
One of the recent trends in Analytical Chemistry is the development of economic, quick and easy hyphenated methods to be used in a field that includes analytes of different classes and physicochemical properties. In this work a multi-residue method was developed for the simultaneous determination of 28 xenobiotics (polar and hydrophilic) using hydrophilic interaction liquid chromatography technique (HILIC) coupled with triple quadrupole mass spectrometry (LC-MS/MS) technology. The scope of the method includes plant growth regulators (chlormequat, daminozide, diquat, maleic hydrazide, mepiquat, paraquat), pesticides (cyromazine, the metabolite of the fungicide propineb PTU (propylenethiourea), amitrole), various multiclass antibiotics (tetracyclines, sulfonamides quinolones, kasugamycin and mycotoxins (aflatoxin B1, B2, fumonisin B1 and ochratoxin A)...
October 26, 2016: Analytica Chimica Acta
Manojkumar Janni, Sahil Arora, S Peruncheralathan
A rapid construction of quinolone fused heterocycles from single S,N-acetal precursors via double heteroannulation is described. The base, radical and metal-mediated reactions can control the C-N, C-S and C-O bond formations of the S,N-acetal with high chemoselectivity.
September 21, 2016: Organic & Biomolecular Chemistry
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