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Sara E McNamee, Giulia Rosar, Lidija Persic, Christopher T Elliott, Katrina Campbell
Practical solutions for multiple antibiotic determination in food is required by the food industry and regulators for cost effective screening purposes. This study describes the feasibility in development and preliminary performance of a novel multispot nanoarray for antibiotic screening in honey. Using a multiplex approach the metabolites of the four main nitrofuran antibiotics including morpholinomethyl-2-oxazolidone (AMOZ), 3-amino-2-oxazolidinone (AOZ), semicarbazide (SEM), 1-aminohydantoin (AHD) and chloramphenicol (CAP) were simultaneously detected...
January 12, 2017: Food Additives & Contaminants. Part A, Chemistry, Analysis, Control, Exposure & Risk Assessment
J Gong, P Kelly, C Wang
Salmonella enterica serovar Indiana, first described in 1955, is generally regarded as having a low frequency worldwide with outbreaks of gastroenteritis and abortions described in North America and Europe. In China, S. Indiana was first reported in 1984 and in the subsequent 71 surveys in 35 cities/municipalities from 18 provinces, 70% of which were after 2012, S. Indiana has been shown to have become widely prevalent in people, animals, food and the environment around abattoirs and meat processing facilities...
December 23, 2016: Zoonoses and Public Health
Blake A Winn, Zhe Shi, Graham J Carlson, Yifan Wang, Benson L Nguyen, Evan M Kelly, R David Ross, Ernest Hamel, David J Chaplin, Mary L Trawick, Kevin G Pinney
A variety of solid tumor cancers contain significant regions of hypoxia, which provide unique challenges for targeting by potent anticancer agents. Bioreductively activatable prodrug conjugates (BAPCs) represent a promising strategy for therapeutic intervention. BAPCs are designed to be biologically inert until they come into contact with low oxygen tension, at which point reductase enzyme mediated cleavage releases the parent anticancer agent in a tumor-specific manner. Phenstatin is a potent inhibitor of tubulin polymerization, mimicking the chemical structure and biological activity of the natural product combretastatin A-4...
December 1, 2016: Bioorganic & Medicinal Chemistry Letters
Erina Hanaki, Mikayo Hayashi, Makoto Matsumoto
Nitro-containing compounds such as nitrofuran and nitroimidazole are drugs used for the treatment of infectious diseases. However, many of these nitro-containing drugs are positive in the bacterial reverse mutation assay (Ames test). The recently approved anti-multidrug-resistant tuberculosis (MDR-TB) drug, delamanid (Deltyba™; OPC-67683), a derivative of 4-nitroimidazole, was negative for mutagenicity in the Ames assay. In Salmonella typhimurium, mutagenicity of nitro compounds has been closely associated with the ability of nitroreductase to metabolize (degradation)these compounds...
December 14, 2016: Regulatory Toxicology and Pharmacology: RTP
Zhonghui Li, Zhoumin Li, Danke Xu
A visualized microarray sensing technique has been developed and applied to the screening of honey samples for residues of banned nitrofuran antibiotics. Using a multiplexed approach, metabolites of four main nitrofuran antibiotics can be detected simultaneously. Individual antigens were spotted onto 96-well plates. An indirective competitive assay format, with visualized signal response, was employed. An extraction method, based on derivatization with 2-nitrobenzaldehyde and partition into ethyl acetate, was used for screening...
April 15, 2017: Food Chemistry
Sam Stephenson, P D Brown
INTRODUCTION: Uropathogenic Escherichia coli (UPEC) rely on the correlation of virulence expression with antimicrobial resistance to persist and cause severe urinary tract infections (UTIs). OBJECTIVES: We assessed the virulence pattern and prevalence among UPEC strains susceptible and resistant to multiple antimicrobial classes. METHODS: A total of 174 non-duplicate UPEC strains from patients with clinically significant UTIs were analysed for susceptibility to aminoglycoside, antifolate, cephalosporin, nitrofuran and quinolone antibiotics for the production of extended-spectrum β-lactamases and for the presence of six virulence determinants encoding adhesins (afimbrial, Type 1 fimbriae, P and S-fimbriae) and toxins (cytotoxic necrotising factor and haemolysin)...
October 2016: Indian Journal of Medical Microbiology
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...
January 5, 2017: 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)...
November 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...
December 15, 2016: Marine Pollution Bulletin
Peng Cui, Hongxia Niu, Wanliang Shi, Shuo Zhang, Hao Zhang, Joseph Margolick, Wenhong Zhang, Ying Zhang
Persisters are small populations of quiescent bacterial cells that survive exposure to bactericidal antibiotics and are responsible for many persistent infections and posttreatment relapses. However, little is known about how to effectively kill persister bacteria. In the work presented here, we found that colistin, a membrane-active antibiotic, was highly active against Escherichia coli persisters at high concentrations (25 or 50 μg/ml). At a clinically relevant lower concentration (10 μg/ml), colistin alone had no apparent effect on E...
November 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...
August 22, 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
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