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https://www.readbyqxmd.com/read/29329277/synthesis-structural-characterization-antimicrobial-activity-and-in-vitro-biocompatibility-of-new-unsaturated-carboxylate-complexes-with-2-2-bipyridine
#1
Gina Vasile Scăețeanu, Mariana Carmen Chifiriuc, Coralia Bleotu, Crina Kamerzan, Luminiţa Măruţescu, Constantin G Daniliuc, Cătălin Maxim, Larisa Calu, Rodica Olar, Mihaela Badea
The synthesis, structural characterization, cytotoxicity, and antimicrobial properties of four new complexes formed by employing acrylate anion and 2,2'-bipyridine are reported herein. X-ray crystallography revealed the trinuclear nature of [Mn₃(2,2'-bipy)₂(C₃H₃O₂)₆] (1), meanwhile complexes with general formula [M(2,2'-bipy)(C₃H₃O₂)₂(H₂O)x]∙yH₂O ((2) M: Ni, x = 1, y = 0; (3) M: Cu, x = 1, y = 0; (4) M: Zn, x = 0, y = 1; 2,2'-bipy: 2,2'-bipyridine; C₃H₃O₂: acrylate anion) were shown to be mononuclear...
January 12, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29325735/whole-transcriptome-analysis-reveals-potential-novel-mechanisms-of-low-level-linezolid-resistance-in-enterococcus-faecalis
#2
Ruoyi Hua, Yun Xia, Wenyao Wu, Jia Yan, Mi Yang
Linezolid is an oxazolidinone antibiotic commonly used to treat serious infections caused by vancomycin-resistant enterococcus. Recently, low-level linezolid resistant Enterococcus faecalis strains have emerged worldwide, but the resistant mechanisms remain undefined. Whole-transcriptome profiling was performed on an E. faecalis strain P10748 with low-level linezolid resistance in comparison with a linezolid-susceptible strain 3138 and the standard control strain ATCC29212. The functions of differentially expressed genes (DEGs) were predicted, with some DEGs potentially involved in drug resistance were validated by PCR and quantitative PCR (qPCR)...
January 8, 2018: Gene
https://www.readbyqxmd.com/read/29324691/physiological-and-comparative-genomic-analysis-of-arthrobacter-sp-srs-w-1-2016-provides-insights-on-niche-adaptation-for-survival-in-uraniferous-soils
#3
Ashvini Chauhan, Ashish Pathak, Rajneesh Jaswal, Bobby Edwards Iii, Demario Chappell, Christopher Ball, Reyna Garcia-Sillas, Paul Stothard, John Seaman
Arthrobacter sp. strain SRS-W-1-2016 was isolated on high concentrations of uranium (U) from the Savannah River Site (SRS) that remains co-contaminated by radionuclides, heavy metals, and organics. SRS is located on the northeast bank of the Savannah River (South Carolina, USA), which is a U.S. Department of Energy (DOE) managed ecosystem left historically contaminated from decades of nuclear weapons production activities. Predominant contaminants within the impacted SRS environment include U and Nickel (Ni), both of which can be transformed microbially into less toxic forms via metal complexation mechanisms...
January 11, 2018: Genes
https://www.readbyqxmd.com/read/29321384/discovery-of-a-novel-fluoroquinolone-antibiotic-candidate-wfq-228-with-potent-antimicrobial-activity-and-the-potential-to-overcome-major-drug-resistance
#4
Tatsuya Hirano, Tomohiko Kinoshita, Daichi Kazamori, Satoshi Inoue, Kouji Nishimura, Asuka Sakurai, Kensuke Ohishi, Yasuhiro Kuramoto, Hirotaka Amano, Akira Yazaki
WFQ-101 with a unique N-1 substituent, 5-amino-4-fluoro-2-(hydroxymethyl)phenyl group, was selected as a lead compound through combination screening based on antimicrobial activity and the efflux index against quinolone-resistant (QR) Pseudomonas aeruginosa (P. aeruginosa). Through structural optimization, we identified WFQ-228 as a novel fluoroquinolone antibiotic candidate. WFQ-228 had potent and superior activity in comparison to levofloxacin (LVX) and ciprofloxacin (CIP) against clinical isolates of P. aeruginosa, Escherichia coli and Acinetobacter baumannii, including QR strains...
January 11, 2018: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/29318976/algerian-propolis-potentiates-doxorubicin-mediated-anticancer-effect-against-human-pancreatic-panc-1-cancer-cell-line-through-cell-cycle-arrest-apoptosis-induction-and-p-glycoprotein-inhibition
#5
Hassiba Rouibah, Lahouel Mesbah, Wided Kebsa, Malek Zihlif, Mamoun Ahram, Bachaer Aburmeleih, Ibtihal Mostafa, Hemzeh El Amir
BACKGROUND: Pancreatic cancer is one of the most aggressive and lethal cancer, with poor prognosis and high resistant to current chemotherapeutic agents. Therefore, new therapeutic strategies and targets are underscored. Propolis has been reported to exhibit a broad spectrum of biological activities including anticancer activity. OBJECTIVE: This study was carried out to assess the possible efficacy of Algerian propolis on the antitumor effect of doxorubicin on human pancreatic cancer cell line (PANC-1)...
January 10, 2018: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29318780/the-synergistic-role-of-atp-dependent-drug-efflux-pump-and-focal-adhesion-signaling-pathways-in-vinorelbine-resistance-in-lung-cancer
#6
Takao Nakanishi, Toshi Menju, Shigeto Nishikawa, Koji Takahashi, Ryo Miyata, Kei Shikuma, Terumasa Sowa, Naoto Imamura, Masatsugu Hamaji, Hideki Motoyama, Kyoko Hijiya, Akihiro Aoyama, Toshihiko Sato, Toyofumi F Chen-Yoshikawa, Makoto Sonobe, Hiroshi Date
The vinorelbine (VRB) plus cisplatin regimen is widely used to treat non-small cell lung cancer (NSCLC), but its cure rate is poor. Drug resistance is the primary driver of chemotherapeutic failure, and the causes of resistance remain unclear. By focusing on the focal adhesion (FA) pathway, we have highlighted a signaling pathway that promotes VRB resistance in lung cancer cells. First, we established VRB-resistant (VR) lung cancer cells (NCI-H1299 and A549) and examined its transcriptional changes, protein expressions, and activations...
January 10, 2018: Cancer Medicine
https://www.readbyqxmd.com/read/29316665/towards-comprehension-of-the-abcb1-p-glycoprotein-role-in-chronic-myeloid-leukemia
#7
REVIEW
Raquel C Maia, Flavia C Vasconcelos, Paloma S Souza, Vivian M Rumjanek
Abstract: The introduction of imatinib (IM), a BCR-ABL1 tyrosine kinase inhibitor (TKI), has represented a significant advance in the first-line treatment of chronic myeloid leukemia (CML). However, approximately 30% of patients need to discontinue IM due to resistance or intolerance to this drug. Both resistance and intolerance have also been observed in treatment with the second-generation TKIs-dasatinib, nilotinib, and bosutinib-and the third-generation TKI-ponatinib. The mechanisms of resistance to TKIs may be BCR-ABL1-dependent and/or BCR-ABL1-independent...
January 7, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29315884/bacterial-outer-membrane-constriction
#8
REVIEW
Alexander J F Egan
The outer membrane of Gram-negative bacteria is a crucial permeability barrier allowing the cells to survive a myriad of toxic compounds, including many antibiotics. This innate form of antibiotic resistance is compounded by the evolution of more active mechanisms of resistance such as efflux pumps, reducing the already limited number of clinically relevant treatments for Gram-negative pathogens. During cell division Gram-negative bacteria must coordinate constriction of the outer membrane in conjunction with other crucial layers of the cell envelope, the peptidoglycan cell wall and the inner membrane...
January 8, 2018: Molecular Microbiology
https://www.readbyqxmd.com/read/29311083/aspergillus-fumigatus-afssn3-afssn8-pair-reverse-regulates-azole-resistance-by-conferring-extracellular-polysaccharide-sphingolipid-pathway-intermediates-and-efflux-pumps-to-biofilm
#9
Nanbiao Long, Liping Zeng, Shanlei Qiao, Lei Li, Guowei Zhong
Antifungal treatment is often ineffectual, which is partly contributed by biofilm. In this study, combined forward and reverse genetics strategy, we identified the nucleus-localized AfSsn3 and its partner AfSsn8, which constituting a cdk8-cyclin pair, are required for azole resistance in Aspergillus fumigatus Deletion of Afssn3 led to increased absorption and utilization of glucose and amino acids. Interestingly, absorption and utilization of glucose accelerated the extracellular polysaccharide formation, while utilization of the amino acids serine, threonine and glycine increased sphingolipid pathway intermediates accumulation...
January 8, 2018: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/29311061/enhanced-efflux-pump-activity-in-old-candida-glabrata
#10
Somanon Bhattacharya, Bettina C Fries
The effect of replicative aging on antifungal resistance in Candida glabrata was investigated. Our studies demonstrate significantly increased transcription of ABC transporters as well as efflux pump activity in old compared to young C. glabrata cells of a fluconazole sensitive and resistant strain. In addition, higher tolerance to killing by micafungin and amphotericin B was noted and is associated with higher transcription of glucan synthase gene FKS1 and lower ergosterol content in older cells.
January 8, 2018: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/29309877/development-of-a-mechanistic-biokinetic-model-for-hepatic-bile-acid-handling-to-predict-possible-cholestatic-effects-of-drugs
#11
Sylvia Notenboom, Karl M Weigand, Johannes H Proost, Marola M van Lipzig, Evita van de Steeg, Petra H H van den Broek, Rick Greupink, Frans G M Russel, Geny M M Groothuis
Drug-induced liver injury (DILI) is a common reason for drug withdrawal from the market. An important cause of DILI is drug-induced cholestasis. One of the major players involved in drug-induced cholestasis is the bile salt efflux pump (BSEP; ABCB11). Inhibition of BSEP by drugs potentially leads to cholestasis due to increased (toxic) intrahepatic concentrations of bile acids with subsequent cell injury. In order to investigate the possibilities for in silico prediction of cholestatic effects of drugs, we developed a mechanistic biokinetic model for human liver bile acid handling populated with human in vitro data...
January 5, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29308809/synergistic-gold-copper-detoxification-at-the-core-of-gold-biomineralisation-in-cupriavidus-metallidurans
#12
L Bütof, N Wiesemann, M Herzberg, M Altzschner, A Holleitner, F Reith, D H Nies
The bacterium Cupriavidus metallidurans is capable of reducing toxic Au(i/iii)-complexes into metallic gold (Au) nano-particles, thereby mediating the (trans)formation of Au nuggets in Earth surface environments. In this study we describe a novel detoxification pathway, which prevents synergistic copper (Cu)/Au-toxicity. Gold-complexes and Cu-ions exert cooperative toxicity, because cellular uptake of Au(i/iii)-complexes blocks Cu(i) export from the cytoplasm by the Cu-efflux pump CupA. Using a combination of micro-analytical and biochemical methods we show that inducible resistance to these Cu/Au mixtures is mediated by the periplasmic Cu(i)-oxidase CopA, which functions as an oxygen-consuming Au(i)-oxidase...
January 8, 2018: Metallomics: Integrated Biometal Science
https://www.readbyqxmd.com/read/29307862/genetic-characterization-of-tigecycline-resistant-enterobacter-species-in-blood-isolates-causing-bacteremia
#13
Min Kyeong Cha, Cheol-In Kang, Ga Eun Park, So Hyun Kim, Doo Ryeon Chung, Kyong Ran Peck, Jae-Hoon Song
OBJECTIVES: Tigecycline is one of the most important antimicrobial agents used to treat infection with multidrug-resistant bacteria. However, tigecycline-resistant pathogens have increased recently. This study was conducted to identify the antimicrobial susceptibility profile and to investigate the role of efflux pumps in high-level tigecycline-resistant Enterobacter isolates causing bacteremia. METHODS: A total of 323 Enterobacter species causing bacteremia were collected from eight hospitals in various regions of Korea...
January 4, 2018: Journal of Global Antimicrobial Resistance
https://www.readbyqxmd.com/read/29307860/high-frequency-of-the-aac-6-ib-cr-gene-associated-with-double-mutations-in-gyra-and-parc-in-escherichia-coli-isolates-from-patients-with-urinary-tract-infections
#14
Lisiane M Volcão, Juliano P Lacava, Martina F Gewehr, Valéria L Real, Ivy B Ramis, Daniela F Ramos, Carla V Gonçalves, Lia G Possuelo, Luciene A R Minarini, Pedro E A da Silva, Andrea von Groll
OBJECTIVE: The aims of this study were (1) to determine the frequency of plasmid-mediated resistance to fluoroquinolones (FQs) in Escherichia coli isolated from patients with urinary tract infections (UTIs) of nosocomial and community origin and (2) to determine the relationships between the presence of extended spectrum beta lactamases (ESBL), mutations in the gyrA and parC genes, and resistance to FQs. METHODS: A total of 71 E. coli isolates, including 35 ESBL producers and 36 randomly selected non-ESBL-producers, were analysed...
January 4, 2018: Journal of Global Antimicrobial Resistance
https://www.readbyqxmd.com/read/29307119/genetic-characterization-of-phenicol-resistant-escherichia-coli-and-role-of-wild-type-repressor-regulator-gene-acrr-on-phenicol-resistance
#15
Muhammad Yaqoob, Li Ping Wang, Jam Kashif, Javed Memon, Sajid Umar, Muhammad Farooq Iqbal, Muhammad Fiaz, Cheng-Ping Lu
The genetic basis for phenicol resistance was examined in 38 phenicol-resistant clinical Escherichia coli isolates from poultry. Out of 62 isolates, 38 showed resistance for chloramphenicol and nine for florfenicol, respectively. Each strain also demonstrated resistance to a variety of other antibiotics. Molecular detection revealed that the incidence rates of the cat1, cat2, flo, flo-R, cmlA, and cmlB were 32, 29, 18, 13, 0, and 0%, respectively. Nineteen strains were tolerant to organic solvents. PCR amplification of the complete acrR (regulator/repressor) gene of five isolates revealed the amino acid changes in four isolates...
January 6, 2018: Folia Microbiologica
https://www.readbyqxmd.com/read/29307003/nacl-induced-expression-of-atvha-c5-gene-in-the-roots-plays-a-role-in-response-of-arabidopsis-to-salt-stress
#16
Aimin Zhou, Enhui Liu, Hongping Ma, Shuang Feng, Shufang Gong, Jingang Wang
Suppression of AtVHA-c5 expression results in changes in H+ and Na+ fluxes of roots, and increase sensitivity to salt in Arabidopsis. Vacuolar-type H+-ATPase (V-ATPase), a multisubunit endomembrane proton pump, is essential in plant growth and response to environmental stresses. In the present study, the function of Arabidopsis V-ATPase subunit c5 (AtVHA-c5) gene in response to salt stress was investigated. Subcellular localization showed that AtVHA-c5 was mainly localized to endosomes and the vacuolar membrane in Arabidopsis...
January 6, 2018: Plant Cell Reports
https://www.readbyqxmd.com/read/29304406/multixenobiotic-resistance-in-mytilus-edulis-molecular-and-functional-characterization-of-an-abcg2-type-transporter-in-hemocytes-and-gills
#17
Yosra Ben Cheikh, Benoit Xuereb, Céline Boulangé-Lecomte, Frank Le Foll
Among the cellular protection arsenal, ABC transporters play an important role in xenobiotic efflux in marine organisms. Two pumps belonging to B and C subfamily has been identified in Mytilus edulis. In this study, we investigated the presence of the third major subtype ABCG2/BCRP protein in mussel tissues. Transcript was expressed in hemocytes and with higher level in gills. Molecular characterization revealed that mussel ABCG2 transporter shares the sequence and organizational structure with mammalian and molluscan orthologs...
December 28, 2017: Aquatic Toxicology
https://www.readbyqxmd.com/read/29297851/ram-locus-is-a-key-regulator-to-trigger-multidrug-resistance-in-enterobacter-aerogenes
#18
Alexander Molitor, Chloë E James, Séamus Fanning, Jean-Marie Pagès, Anne Davin-Regli
PURPOSE: Several genetic regulators belonging to AraC family are involved in the emergence of MDR isolates of E. aerogenes due to alterations in membrane permeability. Compared with the genetic regulator Mar, RamA may be more relevant towards the emergence of antibiotic resistance. METHODOLOGY: Focusing on the global regulators, Mar and Ram, we compared the amino acid sequences of the Ram repressor in 59 clinical isolates and laboratory strains of E. aerogenes. Sequence types were associated with their corresponding multi-drug resistance phenotypes and membrane protein expression profiles using MIC and immunoblot assays...
January 3, 2018: Journal of Medical Microbiology
https://www.readbyqxmd.com/read/29280358/thermoresponsive-supramolecular-chemotherapy-by-v-shaped-armed-%C3%AE-cyclodextrin-star-polymer-to-overcome-drug-resistance
#19
Xiaoshan Fan, Hongwei Cheng, Xiaoyuan Wang, Enyi Ye, Xian Jun Loh, Yun-Long Wu, Zibiao Li
Pump mediated drug efflux is the key reason to result in the failure of chemotherapy. Herein, a novel star polymer β-CD-v-(PEG-β-PNIPAAm)7 consisting of a β-CD core, grafted with thermo-responsive poly(N-isopropylacrylamide) (PNIPAAm) and biocompatible poly(ethylene glycol) (PEG) in the multiple "V"-shaped arms is designed and further fabricated into supramolecular nanocarriers for drug resistant cancer therapy. The star polymer could encapsulate chemotherapeutics between β-cyclodextrin and anti-cancer drug via inclusion complex (IC)...
December 27, 2017: Advanced Healthcare Materials
https://www.readbyqxmd.com/read/29279590/distribution-of-adeb-and-ndm-1-genes-in-multidrug-resistant-acinetobacter-baumannii-isolated-from-infected-wound-of-patients-admitted-in-a-tertiary-care-hospital-in-bangladesh
#20
M J Hasan, S M Shamsuzzaman
BACKGROUND: The adeB gene in Acinetobacter baumannii regulates the bacterial internal drug efflux pump that plays a significant role in drug resistance. The aim of our study was to determine the occurrence of adeB gene in multidrug resistant and New Delhi metallo-beta-lactamase-1 (NDM- 1) gene in imipenem resistant Acinetobacter baumannii isolated from wound swab samples in a tertiary care hospital of Bangladesh. METHODS: A total of 345 wound swab samples were tested for bacterial pathogens...
December 2017: Malaysian Journal of Pathology
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