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https://www.readbyqxmd.com/read/29333734/synthesis-cytotoxic-and-antibacterial-evaluation-of-quinazolinone-derivatives-with-substituted-amino-moiety
#1
Xiaoping Zhan, Yun Xu, Qi Qi, Yaolin Wang, Huiying Shi, Zhenmin Mao
A series of novel quinazolinone derivatives containing a substituted amino moiety were synthesized, evaluated for their cytotoxic and antibacterial activities. The results of MTT assay showed that all synthesized target compounds 5A~O showed potent cytotoxicity against SGC-7901 (IC50 , 0.72~1.41μM). Moreover, the compounds 5D, 5I and 5K showed better selectivity as compared with positive controls pemetrexed and MTX due to weak cytotoxicity against normal tissue cell line HUVSMC. Among synthesized compounds, the compounds 5E, 5J, 5L and 5N showed broad-spectrum cytotoxic activities against at least four cancer cell lines at a micromolar level...
January 14, 2018: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29333612/fosfomycin-residues-in-colostrum-impact-on-morpho-physiology-and-microbiology-of-suckling-piglets
#2
M B Fernández Paggi, G Martínez, S N Diéguez, D S Pérez Gaudio, J M Decundo, M B Riccio, F A Amanto, M O Tapia, A L Soraci
Fosfomycin is a broad-spectrum bactericidal antibiotic widely used in pig farms for the treatment of a wide variety of bacterial infections. In this study, the elimination of disodium fosfomycin in colostrum/milk of the sow and the impact of this antibiotic on the microbiota and intestinal morpho-physiology of suckling piglets were analyzed. The average amount of fosfomycin eliminated in colostrum (after administration of 15 mg/kg IM) during the first 10 hr postpartum was 0.85 μg/ml, and the mean residual amount ingested by the piglets was 0...
January 14, 2018: Journal of Veterinary Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29333608/the-synergistic-effect-of-pdt-and-oxacillin-on-clinical-isolates-of-staphylococcus-aureus
#3
Natanel Iluz, Yasmin Maor, Natan Keller, Zvi Malik
BACKGROUND: Staphylococcus aureus is a major pathogen in clinical microbiology. It is known to cause infections at various body sites and can be life-threatening. The development of resistance to many well-established antibiotic treatments and the prevalence of methicillin-resistant S. aureus (MRAS) among hospital patients and the general community pose challenges in treating the pathogen. The antimicrobial effect of photodynamic therapy (PDT) has been a subject of study for a long time and can offer new strategies for dealing with resistant strains...
January 15, 2018: Lasers in Surgery and Medicine
https://www.readbyqxmd.com/read/29332251/clinical-pharmacokinetics-and-pharmacodynamics-of-telavancin-compared-with-the-other-glycopeptides
#4
REVIEW
Valentin Al Jalali, Markus Zeitlinger
Telavancin was discovered by modifying the chemical structure of vancomycin and belongs to the group of lipoglycopeptides. It employs its antimicrobial potential through two distinct mechanisms of action: inhibition of bacterial cell wall synthesis and induction of bacterial membrane depolarization and permeabilization. In this article we review the clinically relevant pharmacokinetic and pharmacodynamic data of telavancin. For comparison, the pharmacokinetic and pharmacodynamic data of the other glycopeptides are presented...
January 13, 2018: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/29332105/the-emergence-of-carbapenem-resistant-klebsiella-pneumoniae-isolates-producing-oxa-48-and-ndm-in-the-southern-asir-province-saudi-arabia
#5
Ibrahim A Al-Zahrani, Bander A Alsiri
To identify the prevalence of carbapenem-resistant Klebsiella pneumoniae (CRKP) and the most common types of cabapenemases among CRKP in the Southern (Asir) province hospitals, Saudi Arabia. Methods: The cross-sectional study was conducted between late April and September in 2015. A total of 54 Klebsiella pneumoniae (K. pneumoniae) isolates with reduced sensitivity to carbapenems were obtained from various clinical specimens of the 2 largest hospitals in the Southern province. Minimum inhibitory concentrations (MICs) of carbapenems were confirmed using E-test...
January 2018: Saudi Medical Journal
https://www.readbyqxmd.com/read/29331510/effects-of-sub-minimum-inhibitory-concentrations-of-lemon-essential-oil-on-the-acid-tolerance-and-biofilm-formation-of-streptococcus-mutans
#6
Yanwei Sun, Sijia Chen, Chen Zhang, Yali Liu, Li Ma, Xiangyu Zhang
OBJECTIVES: Lemon essential oil (LEO) is a kind of secondary metabolite from lemon peels and has been found to inhibit cariogenic bacteria for decades. However, its effects on main cariogenic virulence factors are rarely reported. The present study aimed to investigate the effects of sub-minimum inhibitory concentrations (sub-MICs) of LEO on the acid tolerance and biofilm formation of Streptococcus mutans (S. mutans) and preliminarily reveal the possible underlying mechanisms. DESIGNS: Effects of LEO on the acid tolerance and biofilm formation of S...
December 29, 2017: Archives of Oral Biology
https://www.readbyqxmd.com/read/29331369/equisetum-telmateia-extracts-chemical-compositions-antioxidant-activity-and-antimicrobial-effect-on-the-growth-of-some-pathogenic-strain-causing-poisoning-and-infection
#7
Marzie Yeganegi, Farideh Tabatabaei Yazdi, Seyed Ali Mortazavi, Javad Asili, Behrooz Alizadeh Behbahani, Adel Beig Babaei
The aerial parts of Equisetum telmateia have been used as a source of biologically active compounds to treat inflammatory, diarrhea, stomach-ache, eczema and mouth infections in traditional medicine. The aim of this work is to evaluate the extraction yield, chemical compositions, antioxidant activity and antimicrobial activity of E. telmateia extracts on Staphylococcus aureus, Bacillus cereus, Escherichia coli, Salmonella typhi and Candida albicans. Chemical compositions E. telmateia was analyzed by high performance liquid chromatography (HPLC) using a C18 column...
January 10, 2018: Microbial Pathogenesis
https://www.readbyqxmd.com/read/29331166/institution-wide-and-within-patient-evolution-of-daptomycin-susceptibility-in-vancomycin-resistant-enterococcus-faecium-bloodstream-infections
#8
Robert J Woods, Twisha S Patel, Jerod L Nagel, Duane W Newton, Andrew F Read
We report daptomycin minimum inhibitory concentrations (MICs) for vancomycin-resistant Enterococcus faecium isolated from bloodstream infections over a 4-year period. The daptomycin MIC increased over time hospital-wide for initial isolates and increased over time within patients, culminating in 40% of patients having daptomycin-nonsusceptible isolates in the final year of the study. Infect Control Hosp Epidemiol 2018;1-3.
January 14, 2018: Infection Control and Hospital Epidemiology
https://www.readbyqxmd.com/read/29330691/bis-guanylhydrazones-as-efficient-anti-candida-compounds-through-dna-interaction
#9
Jelena Lazić, Vladimir Ajdačić, Sandra Vojnovic, Mario Zlatović, Marina Pekmezovic, Selene Mogavero, Igor Opsenica, Jasmina Nikodinovic-Runic
Candida spp. are leading causes of opportunistic mycoses, including life-threatening hospital-borne infections, and novel antifungals, preferably aiming targets that have not been used before, are constantly needed. Hydrazone- and guanidine-containing molecules have shown a wide range of biological activities, including recently described excellent antifungal properties. In this study, four bis-guanylhydrazone derivatives (BG1-4) were generated following a previously developed synthetic route. Anti-Candida (two C...
January 12, 2018: Applied Microbiology and Biotechnology
https://www.readbyqxmd.com/read/29329652/three-new-anthraquinone-derivatives-isolated-from-symplocos-racemosa-and-their-antibiofilm-activity
#10
Umar Farooq, Sara Khan, Sadia Naz, Ajmal Khan, Afsar Khan, Ayaz Ahmed, Abdur Rauf, Syed Majid Bukhari, Shujaat Ali Khan, Arfa Kamil, Nadia Riaz, Abdur Rahman Khan
Three new alkyl substituted anthraquinone derivatives, trivially named as symploquinones A-C (Compounds 1-3) were isolated from Symplocos racemosa. The structures of these compounds were determined on the basis of extensive spectroscopic analyses (UV, IR, Mass, 1H- and 13C-NMR, and two-dimensional (2D) NMR techniques). The resulting data were also compared with the reported literature. These compounds were then subjected to antibacterial or antibiofilm testing. Compounds 1 and 3 exhibited good antibacterial activity in the concentration range of 160-83 μg·mL-1 against Streptococcus mutans, methicillin resistant Staphylococcus aureus and Proteus mirabilis...
December 2017: Chinese Journal of Natural Medicines
https://www.readbyqxmd.com/read/29329389/in-vivo-daptomycin-efficacy-against-experimental-vancomycin-resistant-enterococcus-faecium-endocarditis
#11
Sophie Reissier, Azzam Saleh-Mghir, François Guerin, Laurent Massias, Idir Ghout, Clara Sinel, Vincent Cattoir, Anne-Claude Cremieux
Objectives: Daptomycin has become a first-line therapeutic option for vancomycin-resistant Enterococcus faecium infective endocarditis (IE). Although high doses (≥8 mg/kg) are often recommended, optimal doses, particularly for strains with MICs close to the susceptibility breakpoint (4 mg/L), are still debated. Methods: Daptomycin efficacy at doses equivalent to 8 mg/kg daptomycin (DAP8) and 12 mg/kg daptomycin (DAP12) in humans was evaluated in a rabbit model of aortic valve IE induced by 108 cfu of E...
January 9, 2018: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/29329277/synthesis-structural-characterization-antimicrobial-activity-and-in-vitro-biocompatibility-of-new-unsaturated-carboxylate-complexes-with-2-2-bipyridine
#12
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/29329001/improved-antibacterial-activity-of-a-marine-peptide-n2-against-intracellular-salmonella-typhimurium-by-conjugating-with-cell-penetrating-peptides-blfcin6-tat11
#13
Zhanzhan Li, Xiao Wang, Da Teng, Ruoyu Mao, Ya Hao, Na Yang, Huixian Chen, Xiumin Wang, Jianhua Wang
Salmonellae, gram-negative bacteria, are facultative intracellular pathogens that cause a number of diseases in animals and humans. The poor penetration ability of antimicrobial agents limits their use in the treatment of intracellular bacterial infections. In this study, the cell-penetrating peptides (CPPs) bLFcin6 and Tat11 were separately conjugated to the antimicrobial peptide N2, and the antibacterial activity and pharmacodynamics of the CPPs-N2 conjugates were first evaluated against Salmonellae typhimurium in vitro and in macrophage cells...
December 29, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29327960/pharmacokinetics-of-a-single-intramuscular-injection-of-long-acting-ceftiofur-crystalline-free-acid-in-cattle-egrets-bubulcus-ibis
#14
Jennifer A Waldoch, Sherry K Cox, Douglas L Armstrong
We determined the pharmacokinetic properties of ceftiofur crystalline-free acid (CCFA), a long-acting antibiotic, after a single intramuscular injection in cattle egrets ( Bubulcus ibis). A dose of 20 mg/kg was administered intramuscularly to 18 birds and blood samples were collected via jugular venipuncture at 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 144, 168, 192, 216, and 240 hours after CCFA administration. Plasma concentrations of ceftiofur free acid equivalents (CFAEs) were measured via high-performance liquid chromatography...
December 2017: Journal of Avian Medicine and Surgery
https://www.readbyqxmd.com/read/29327293/overexpression-of-spot-gene-in-coccoid-forms-of-clinical-helicobacter-pylori-isolates
#15
Farkhondeh Poursina, Jamshid Fagri, Nasrin Mirzaei, Hajieh Ghasemian Safaei
Helicobacter pylori (H. pylori) can convert to coccoid form in unfavorable conditions or as a result of antibiotic treatment. In order to adapt to harsh environments, H. pylori requires a stringent response which, encoded by the spoT gene, has a bifunctional enzyme possessing both (p)ppGpp synthetic and degrading activity. Our goal in this study was to compare spoT gene expression in spiral and induced coccoid forms of H. pylori with use of amoxicillin. First, clinical isolate coccoid forms were induced with amoxicillin; then, the viability test was analyzed by flow cytometer...
January 11, 2018: Folia Microbiologica
https://www.readbyqxmd.com/read/29327292/alterations-of-growth-rate-and-gene-expression-levels-of-upec-by-antibiotics-at-sub-mic
#16
Defne Gümüş, Fatma Kalaycı-Yüksek, Emre Yörük, Gülşen Uz, Eşref Çelik, Cansu Arslan, Elif Merve Aydın, Cem Canlı, Mine Anğ-Küçüker
The host is the main environment for bacteria, and they also expose to many antibiotics during the treatment of infectious diseases in host body. In this study, it was aimed to investigate possible changes in growth rate and expression levels of three virulence genes (foc/foc, cnf1, and usp) in a uropathogenic E. coli standard strain within the presence of ciprofloxacin, nitrofurantoin, and trimethoprim-sulfamethoxazole. The UPEC C7 strain was grown on tryptic soy broth-TSB (control), TSB + ciprofloxacin, TSB + nitrofurantoin, and TSB + trimethoprim-sulfamethoxazole for determination of both growth rate and gene expression level...
January 11, 2018: Folia Microbiologica
https://www.readbyqxmd.com/read/29327068/the-specific-effect-of-gallic-acid-on-escherichia-coli-biofilm-formation-by-regulating-pgaabcd-genes-expression
#17
Jiamu Kang, Qianqian Li, Liu Liu, Wenyuan Jin, Jingfan Wang, Yuyang Sun
Escherichia coli (E. coli) is associated with an array of health-threatening contaminations, some of which are related to biofilm states. The pgaABCD-encoded poly-beta-1,6-N-acetyl-D-glucosamine (PGA) polymer plays an important role in biofilm formation. This study was conducted to determine the inhibitory effect of gallic acid (GA) against E. coli biofilm formation. Minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) values of GA against planktonic E. coli were 0.5 and 4 mg/mL, and minimal biofilm inhibitory concentration and minimal biofilm eradication concentration values of GA against E...
January 11, 2018: Applied Microbiology and Biotechnology
https://www.readbyqxmd.com/read/29326510/isolation-and-typing-of-streptococcus-mutans-and-streptococcus-sobrinus-from-caries-active-subjects
#18
Hamzah Abdulrahman Salman, R Senthilkumar, Khalid Imran, K Panneer Selvam
Background: Streptococcus mutans and Streptococcus sobrinus are main etiological agents of dental caries. Aim: The aim of the study was to isolate, identify, characterize, and determine the minimum inhibitory concentration (MIC) of S. mutans and S. sobrinus from caries-active subjects. Materials and Methods: Sixty-five plaque samples were collected from caries-active subjects aged between 35 and 44 years, processed and cultured on mitis salivarius bacitracin agar...
October 2017: Contemporary Clinical Dentistry
https://www.readbyqxmd.com/read/29325862/antibacterial-effects-of-cinnamon-cinnamomum-zeylanicum-bark-essential-oil-on-porphyromonas-gingivalis
#19
Yue Wang, Yi Zhang, Yan-Qin Shi, Xian-Hua Pan, Yan-Hua Lu, Ping Cao
The objective of this study was to investigate the antibacterial effects of cinnamon (Cinnamomum zeylanicum) bark essential oil (CBEO) and its principal constituent cinnamaldehyde against Porphyromonas gingivalis and to elucidate the antibacterial mechanism. GC-MS analysis showed that cinnamaldehyde was the major constituent in CBEO (57.97%). The minimum inhibition concentrations (MICs) of CBEO and cinnamaldehyde were 6.25 μg/mL and 2.5 μM for P. gingivalis, respectively. Nucleic acid and protein leakage was observed with increasing concentrations of CBEO and cinnamaldehyde...
January 8, 2018: Microbial Pathogenesis
https://www.readbyqxmd.com/read/29325762/assessment-of-in-vivo-efficacy-of-eravacycline-against-enterobacteriaceae-exhibiting-various-resistance-mechanisms-a-dose-ranging-study-and-pk-pd-analysis
#20
Abrar K Thabit, Marguerite L Monogue, Joseph V Newman, David P Nicolau
After the pharmacokinetic (PK) profile of eravacycline as a novel fluorocycline was defined, understanding its pharmacodynamic (PD) profile became essential. The aim of this study was to assess the correlation of the PK/PD index of the area under free drug concentration-time curve above the minimum inhibitory concentration (fAUC/MIC) and its magnitude with eravacycline's efficacy against Enterobacteriaceae isolates using the immunocompetent murine thigh infection model to resemble the immunocompetent environment in eravacycline's clinical trials...
January 8, 2018: International Journal of Antimicrobial Agents
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