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Elena V Pikuta, Rodolfo Javier Menes, Alisa Michelle Bruce, Zhe Lyu, Nisha Patel, Yuchen Liu, Richard Brice Hoover, Hans Jürgen Busse, Paul A Lawson, William Barney Whitman
Gram-positive bacterium, strain LZ-22T, was isolated from a rhizosphere of moss Leptobryum sp. collected at the shore of Lake Zub in Antarctica. Cells were motile, straight or pleomorphic rods with sizes of 0.6-1.0 x 3.5-10 μm. The new isolate was a facultatively anaerobic, catalase positive, psychrotolerant mesophile. Growth was observed at 3-41 oC (optimum 24-30 oC), 0-7 % NaCl, w/v (optimum, 0.25 %) and pH 4.0-9.0 (optimum 7.8). The quinone system of strain LZ-22T possessed predominately menaquinones MK-9(H4)...
October 12, 2016: International Journal of Systematic and Evolutionary Microbiology
D G Arias, F E Herrera, A S Garay, D Rodrigues, P S Forastieri, L E Luna, M D L M Bürgi, C Prieto, A A Iglesias, R M Cravero, S A Guerrero
The rational design and synthesis of a series of 5-nitro-2-furoic acid analogues are presented. The trypanocidal activity against epimastigote forms of Trypanosoma cruzi and the toxic effects on human HeLa cells were tested. Between all synthetic compounds, three of thirteen had an IC50 value in the range of Nfx, but compound 13 exhibited an improved effect with an IC50 of 1.0 ± 0.1 μM and a selective index of 70 in its toxicity against HeLa cells. We analyzed the activity of compounds 8, 12 and 13 to interfere in the central redox metabolic pathway in trypanosomatids, which is dependent of reduced trypanothione as the major pivotal thiol...
October 24, 2016: European Journal of Medicinal Chemistry
Hongxia Zhao, Wuxia Guo, Wenna Quan, Jingqiu Jiang, Baocheng Qu
The occurrence and levels of nitrofuran metabolites (NFMs) in sea cucumber (SC) from Dalian, China, are reported. Four metabolites including 3-amino-5-morpholinomethyl-2-oxazolidinone (AMOZ), 3-amino-2-oxazolidinone (AOZ), semicarbazide (SEM) and 1-aminohydantoin (AHD) in different SC products (fresh, instant and dry salted SCs) were measured. The frequency of occurrence for NFMs in all SC samples was 42.7%. The total NFM concentrations ranged from non-detectable to 64.6 ng g(-)(1), with a mean of 3.59 ng g(-1)...
October 17, 2016: Food Additives & Contaminants. Part A, Chemistry, Analysis, Control, Exposure & Risk Assessment
Zhiwen Zhang, Yuping Wu, Xiaowei Li, Yingyu Wang, Hui Li, Qin Fu, Yawen Shan, Tianhe Liu, Xi Xia
This study describes the development of a multiresidue method for the efficient identification and quantification of nitroimidazoles, nitrofurans, and chloramphenicol in chicken and egg. After derivatization of nitrofuran metabolites, dispersive-solid phase extraction was used for the extraction of target analytes. An optimization strategy involved the selection of sorbents and extraction solutions for dispersive-solid phase extraction in order to achieve acceptably high recoveries and reduce co-extractives in the final extracts...
February 15, 2017: Food Chemistry
Geng-Ruei Chang, Hui-Shan Chen, Feng-Yi Lin
Seafood safety is a crucial public health concern for consumers. In this study, we applied a validated method to analyze the residue of banned veterinary drugs in shellfish, namely chloramphenicol, malachite green, leucomalachite green, and nitrofuran metabolites; additionally, the QuEChERS method was employed to detect 76 herbicides by LC/MS/MS and GC/MS/MS. In total, 42 shellfish samples, which included hard clams, freshwater clams, and oysters, were collected from aquafarms and production areas in Taiwan during 2012...
September 6, 2016: Marine Pollution Bulletin
Peng Cui, Hongxia Niu, Wanliang Shi, Shuo Zhang, Hao Zhang, Joseph Margolick, Wenhong Zhang, Ying Zhang
Persisters are a small population of quiescent bacterial cells that survive exposure to bactericidal antibiotics and are responsible for many persistent infections and post-treatment relapses. However, little is known about how to effectively kill persister bacteria. Here, we found that colistin, a membrane-active antibiotic, was highly active against E. coli persisters at high concentrations (25 or 50 μg/ml). However, at a clinically relevant lower concentration (10 μg/ml) colistin had no apparent effect on E...
September 6, 2016: Antimicrobial Agents and Chemotherapy
Chongshan Dai, Daowen Li, Lijing Gong, Xilong Xiao, Shusheng Tang
Furazolidone (FZD), a synthetic nitrofuran derivative, has been widely used as an antibacterial and antiprotozoal agent. Recently, the potential toxicity of FZD has raised concerns, but its mechanism is still unclear. This study aimed to investigate the protective effect of curcumin on FZD-induced cytotoxicity and the underlying mechanism in human hepatocyte L02 cells. The results showed that curcumin pre-treatment significantly ameliorated FZD-induced oxidative stress, characterized by decreased reactive oxygen species (ROS) and malondialdehyde formation, and increased superoxide dismutase, catalase activities and glutathione contents...
2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Jeyce K F Andrade, Márcia I F Souza, Manoel A Gomes Filho, Diogo M F Silva, André L S Barros, Maria D Rodrigues, Paulo B N Silva, Silene C Nascimento, Jaciana S Aguiar, Dalci J Brondani, Gardênia C G Militão, Teresinha G Silva
BACKGROUND: Nitrofurantoin is a nitroderivative antibiotic that has bactericidal activity against pathogens causing urinary tract infection. A few studies have reported that nitrofurantoin has cytotoxic activity against cancer cells; however, nitrofurans remain a poorly explored class of compounds with respect to their anticancer potential. The aim of this study was to investigate the anticancer effects of a nitrofurantoin derivative, n-pentyl-nitrofurantoin (NFP), on HL-60 leukemia cells...
October 2016: Pharmacological Reports: PR
Ali Ryan
Azoreductases are flavoenzymes that have been characterized in a range of prokaryotes and eukaryotes. Bacterial azoreductases are associated with the activation of two classes of drug, azo drugs for the treatment of inflammatory bowel disease and nitrofuran antibiotics. The mechanism of reduction of azo compounds is presented; it requires tautomerisation of the azo compound to a quinoneimine and provides a unifying mechanism for the reduction of azo and quinone substrates by azoreductases. The importance of further work in the characterization of azoreductases from enteric bacteria is highlighted to aid in the development of novel drugs for the treatment of colon related disorders...
August 3, 2016: British Journal of Pharmacology
Xuewen Lu, Xiaoling Liang, Jianghong Dong, Zhiyuan Fang, Lingwen Zeng
The use of potential mutagenic nitrofuran antibiotic in food animal production has been banned world-wide. Common methods for nitrofuran detection involve complex extraction procedures. In the present study, magnetic beads functionalized with antibody against nitrofuran derivative were used as both the extraction and color developing media in lateral flow biosensor. Derivatization reagent carboxybenzaldehyde is firstly modified with ractopamine. After reaction with nitrofuran metabolites, the resultant molecule has two functional groups: the metabolite moiety and the ractopamine moiety...
September 2016: Analytical and Bioanalytical Chemistry
Kai Ran, Chao Gao, Hongxia Deng, Qian Lei, Xinyu You, Ningyu Wang, Yaojie Shi, Zhihao Liu, Wei Wei, Cuiting Peng, Lu Xiong, Kunjie Xiao, Luoting Yu
The emergence of antibiotic resistant pathogens is an ongoing main problem in the therapy of bacterial infections. In order to develop promising antitubercular and antibacterial lead compounds, we designed and synthesized a new series of derivatives of 2-aminothiazole conjugated nitrofuran with activities against both Mycobacterium tuberculosis and Staphylococcus aureus. Eight compounds 12e, 12k, 12l, 12m, 18a, 18d, 18e, and 18j emerged as promising antitubercular agents. Structure-activity relationships (SARs) were discussed and showed that the derivatives substituted at the position-3 of benzene of 5-nitro-N-(4-phenylthiazol-2-yl)furan-2-carboxamide exhibited superior potency...
August 1, 2016: Bioorganic & Medicinal Chemistry Letters
Seon-Ju Yeo, ChunMei Jin, SungYeon Kim, Hyun Park
Toxoplasma gondii is an important opportunistic pathogen that causes toxoplasmosis, which has very few therapeutic treatment options. The most effective therapy is a combination of pyrimethamine and sulfadiazine; however, their utility is limited because of drug toxicity and serious side effects. For these reasons, new drugs with lower toxicity are urgently needed. In this study, the compound, (Z)-1-[(5-nitrofuran-2-yl)methyleneamino]-imidazolidine-2,4-dione (nitrofurantoin), showed anti-T. gondii effects in vitro and in vivo...
April 2016: Korean Journal of Parasitology
Yue Hao, Taylor B Updegrove, Natasha N Livingston, Gisela Storz
Here, we report the characterization of a set of small, regulatory RNAs (sRNAs) expressed from an Escherichia coli locus we have denoted sdsN located adjacent to the LuxR-homolog gene sdiA Two longer sRNAs, SdsN137 and SdsN178 are transcribed from two σ(S)-dependent promoters but share the same terminator. Low temperature, rich nitrogen sources and the Crl and NarP transcription factors differentially affect the levels of the SdsN transcripts. Whole genome expression analysis after pulse overexpression of SdsN137 and assays of lacZ fusions revealed that the SdsN137 directly represses the synthesis of the nitroreductase NfsA, which catalyzes the reduction of the nitrogroup (NO2) in nitroaromatic compounds and the flavohemoglobin HmpA, which has aerobic nitric oxide (NO) dioxygenase activity...
August 19, 2016: Nucleic Acids Research
Hui Li, Dongju Lin, Ying Peng, Jiang Zheng
1. Nitrofurantoin (NFT), a 5-nitrofuran derivative, has been widely used for the treatment of specific urinary tract infections. It has been reported that exposure to NFT was associated with various adverse effects, particularly hepatotoxicity and pneumotoxicity. The objective of the study was to identify reactive metabolites of NFT and explore the mechanisms of the toxicities. 2. An epoxide intermediate generated in microsomal incubations was trapped by glutathione (GSH) and 4-bromobenzyl mercaptan (BBM), and the resulting GSH and BBM conjugates were characterized by LC-MS/MS...
April 19, 2016: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
Sijun Deng, Shusheng Tang, Chongshan Dai, Yan Zhou, Xiayun Yang, Daowen Li, Xilong Xiao
Furazolidone (FZD), a synthetic nitrofuran with a broad spectrum of antimicrobial activities, has been shown to exhibit marked genotoxity and cytotoxicity in vitro, but the proper mechanism was unclear. P21(Waf1/Cip1) (p21), a cyclin-dependent kinase, is critically involved in cell cycle arrest and apoptosis in response to DNA injury. This study was aimed to explore the role of p21 in FZD-induced apoptosis in HepG2 cells and uncover its possible mechanism. Firstly, we demonstrated that FZD (50 μg/mL) treatment increased the mRNA level of p21 but reduced the protein level of p21 by shortening its half-life...
February 2016: Food and Chemical Toxicology
David F Bruhn, Susan Wyllie, Adaris Rodríguez-Cortés, Angela K Carrillo, Rakesh, R Kiplin Guy, Alan H Fairlamb, Richard E Lee
OBJECTIVES: In response to reports of Trypanosoma brucei resistance to the nitroaromatic drug nifurtimox, we evaluated the potential of antituberculosis nitrofuran isoxazolines as inhibitors of trypanosome growth. METHODS: The susceptibility of T. brucei brucei was assessed in vitro. The lowest effective concentration to inhibit growth (EC90) against drug-susceptible and -resistant parasites, time-kill kinetics, reversibility of inhibition and propensity for P-glycoprotein-mediated exclusion from the blood-brain barrier were determined...
April 2016: Journal of Antimicrobial Chemotherapy
Mark-Jean Gnoth, Peter-Michael Hopfe, Uwe Thuss
BACKGROUND: Nifurtimox is a 5-nitrofuran derived antiprotozoal drug used to treat diseases caused by trypanosomes including Chagas' disease and sleeping sickness (African trypanosomiasis). Available methods for the determination of nifurtimox in plasma are tedious and of low sensitivity. For the first time, an isotope dilution HPLC/MS/MS method for the sensitive quantitation of nifurtimox down to 10.0 μg/l in plasma is described. RESULTS: Protein precipitation was used for sample preparation...
November 2015: Bioanalysis
Yaqian Zhang, Xiang Li, Xiaomao Liu, Jinjie Zhang, Yanzhong Cao, Zhihong Shi, Hanwen Sun
A simple and rapid multi-class multi-residue analytical method was developed for the screening and quantification of veterinary drugs in milk by ultra-performance liquid chromatography coupled to quadrupole time-of-flight mass spectrometry (UPLC-QTOF-MS). A total of 90 veterinary drugs investigated belonged to almost 20 classes including lincomycins, macrolides, sulfonamides, quinolones, tetracyclines, β-agonists, β-lactams, sedatives, β-receptor antagonists, sex hormones, glucocorticoids, nitroimidazoles, benzimidazoles, nitrofurans, and some others...
December 2015: Journal of Dairy Science
Yibei Zhang, Haiou Qiao, Chen Chen, Zhilun Wang, Xiaodong Xia
A method was described for monitoring four nitrofuran metabolites including 5-methylmorpholino-3-amino-2-oxazolidinone (AMOZ), 3-amino-2-oxazolidone (AOZ), 1-amino-hydantoin (AHD) and semicarbazide (SEM) in aquatic products. The analytes were quantified by ultra-performance liquid chromatography-tandem mass spectrometry operating in positive ion multiple monitoring mode (MRM) after 2-nitrobenzaldehyde derivatization. The matrix calibration curve was established with correlation coefficient (R(2)>0.99) in the range of 1-100 ng ml(-1)...
February 1, 2016: Food Chemistry
Ahmed Kamal, S M Ali Hussaini, M Lakshmi Sucharitha, Y Poornachandra, Faria Sultana, C Ganesh Kumar
A series of 5-nitrofuran-triazole congeners were designed and synthesized by carrying out suitable structural modifications of the previously reported counterparts and were evaluated for their antimicrobial potential against both Gram-positive and Gram-negative bacterial strains. The compounds exhibited promising inhibition towards different Gram-positive pathogenic strains, while mild inhibitory effects were observed towards Gram-negative bacterial strains. Some of the compounds 9f, 9g, 9l and 9m were most active among the series, exhibiting a MIC value of 1...
September 28, 2015: Organic & Biomolecular Chemistry
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