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Antibacterial resistance

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https://www.readbyqxmd.com/read/28109787/synthesis-and-in-vitro-activity-of-dicationic-indolyl-diphenyl-ethers-as-novel-potent-antibiotic-agents-against-drug-resistant-bacteria
#1
Xiaofang Chen, Xinxin Hu, Yanbin Wu, Yonghua Liu, Cong Bian, Tongying Nie, Xuefu You, Laixing Hu
A series of 4,4'-bis-[2-(6-N-substituted-amidino)indolyl] diphenyl ether have been synthesized and tested for their in vitro antibacterial activity including a range of Gram-positive and Gram-negative pathogens and cytotoxicity. Most of these compounds have mainly shown anti-Gram positive bacteria activities especially against drug resistant bacterial strains MRSA, MRSE and VRE. The anti-MRSA and anti-MRSE activities of compound 7a and 7j were more potent than that of the lead compound 2, levofloxacin and vancomycin...
January 10, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28109770/modulation-of-the-antibiotic-activity-against-multidrug-resistant-strains-of-coumarins-isolated-from-rutaceae-species
#2
Sara A L Madeiro, Nathalie H P B Borges, Augusto L Souto, Pedro T R de Figueiredo, José P Siqueira-Junior, Josean F Tavares
The first occurrences and dissemination of resistant microorganisms led to the inefficacy of many antibiotics, available in the market nowadays, therefore, the search for new substances with antimicrobial activity from natural sources has gained a great importance. The purpose of this work is to evaluate the antibacterial activity and modulation of drug resistance in Staphylococcus aureus by coumarins such as bergapten, xantotoxin, isopimpinellin and imperatorin obtained from two Rutaceae species (Metrodorea mollis and Pilocarpus spicatus)...
January 18, 2017: Microbial Pathogenesis
https://www.readbyqxmd.com/read/28108235/the-use-of-bacteriophages-to-biocontrol-oral-biofilms
#3
Szymon P Szafrański, Andreas Winkel, Meike Stiesch
Infections induced by oral biofilms include caries, as well as periodontal, and peri-implant disease, and may influence quality of life, systemic health, and expenditure. As bacterial biofilms are highly resistant and resilient to conventional antibacterial therapy, it has been difficult to combat these infections. An innovative alternative to the biocontrol of oral biofilms could be to use bacteriophages or phages, the viruses of bacteria, which are specific, non-toxic, self-proliferating, and can penetrate into biofilms...
January 17, 2017: Journal of Biotechnology
https://www.readbyqxmd.com/read/28107695/antibacterial-activity-computational-analysis-and-host-toxicity-study-of-thymol-sulfonamide-conjugates
#4
Shasank S Swain, Sudhir K Paidesetty, Rabindra N Padhy
Methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin resistant Enterococcus faecalis (VRE) are notorious pathogenic multidrug resistant (MDR) bacteria in both hospital and community sectors, and today the first antibacterial drug sulfamethoxazole is ineffective. The monoterpene phenol, thymol was conjugated with seven sulfa drug derivatives individually, adopting the dye-azo synthesis protocol, and conjugates were characterized using spectral analysis techniques such as, UV, FTIR, MS, HPLC, (1)H NMR, (13)C NMR and SEM...
January 17, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28107379/experimental-and-in-silico-investigation-of-anti-microbial-activity-of-1-chloro-2-isocyanatoethane-derivatives-of-thiomorpholine-piperazine-and-morpholine
#5
Charles O Nwuche, Oguejiofo T Ujam, Akachukwu Ibezim, Ifeoma B Ujam
The Antibiogram properties of 1-chloro-2-isocyanatoethane derivatives of thiomorpholine (CTC), piperazine (CPC) and morpholine (CMC) were evaluated by the approved agar well diffusion, the minimum inhibitory concentration (MIC) and in silico techniques. A total of fourteen microbial cultures consisting of ten bacteria and four yeast strains were used in the biological study while affinity of the compounds for DNA gyrase, a validated antibacterial drug target, was investigated by docking method. Results indicate that both thiomorpholine and piperazine had zero activity against the Gram negative organisms tested...
2017: PloS One
https://www.readbyqxmd.com/read/28106774/effects-of-long-term-water-aging-on-novel-anti-biofilm-and-protein-repellent-dental-composite
#6
Ning Zhang, Ke Zhang, Mary A S Melo, Michael D Weir, David J Xu, Yuxing Bai, Hockin H K Xu
The aims of this study were to: (1) synthesize an anti-biofilm and protein-repellent dental composite by combining 2-methacryloyloxyethyl phosphorylcholine (MPC) with quaternary ammonium dimethylaminohexadecyl methacrylate (DMAHDM); and (2) evaluate the effects of water-aging for 180 days on protein resistance, bacteria-killing ability, and mechanical properties of MPC-DMAHDM composite. MPC and DMAHDM were added into a resin composite. Specimens were stored in distilled water at 37 °C for 1, 30, 90, and 180 days...
January 18, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28106379/sustainable-release-of-vancomycin-from-silk-fibroin-nanoparticles-for-treating-severe-bone-infections-in-a-rat-tibia-osteomyelitis-model
#7
Negar Hassani Besheli, Fatemeh Mottaghitalab, Masoud Eslami, Mahdi Gholami, Subhas C Kundu, David L Kaplan, Mehdi Farokhi
The successful treatment of bone infections is a major challenge in the field of orthopedics. There are some common methods for treating bone infections, including systemic antibiotic administration, local non-degradable drug vehicles, and surgical debridement and each of these approaches has advantages and disadvantages. In the present study, the antibiotic vancomycin (VANCO) was loaded in silk fibroin nanoparticles (SFNPs) and the complexes were then entrapped in silk scaffolds to form sustained drug delivery systems...
January 20, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28106348/a-biosurfactant-inspired-heptapeptide-with-improved-specificity-to-kill-mrsa
#8
Yuan Liu, Shuangyang Ding, Richard Dietrich, Erwin Märtlbauer, Kui Zhu
The emergence and rapid spread of methicillin-resistant Staphylococcus aureus (MRSA) poses a serious threat to public health. New antibiotics and strategies are urgently needed to combat S. aureus associated infections. Bacaucin, a novel cyclic lipopeptide from Bacillus subtilis CAU21, is reported. Bacaucin shows broad antibacterial activity against Gram-positive bacteria, but is also hemolytic and cytotoxic. However, bacaucin-1, a bacaucin-inspired ring-opened heptapeptide, shows specific antibacterial activity against MRSA by a membrane-disruptive mechanism without detectable toxicity to mammalian cells or induction of bacterial resistance...
February 1, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28103779/flavone-analogues-as-antimicrobial-agents
#9
Kamlesh Kumar Naik, Sivakumar Thangavel, Afroze Alam
BACKGROUND: Most of the available antimicrobial drugs have developed resistance, some of them suffer from severe toxicity, side effects. So, there is a need to discover novel compound(s) which should not only be potent, but also less toxic and cost effective. OBJECTIVES: The aim of the study is to develop new synthetic antimicrobial agents (Anti-bacterial and anti-fungal) such as 3-substituted flavone/flavanone derivatives, which should be significantly potent with low toxicity...
January 18, 2017: Recent Patents on Inflammation & Allergy Drug Discovery
https://www.readbyqxmd.com/read/28103015/antimicrobial-activity-ame-resistance-and-translation-inhibition-studies-of-anthraquinone-neomycin-conjugates
#10
Natalya N Degtyareva, Changjun Gong, Sandra Story, Nathanael Levinson, Adegboyega K Oyelere, Keith D Green, Sylvie Garneau-Tsodikova, Dev Priya Arya
The antibacterial effects of aminoglycosides are based on their association with the A-site of bacterial ribosomal RNA and interference with the translational process in the bacterial cell, causing cell death. The clinical use of aminoglycosides is complicated by resistance and side effects, some of which arise from their interactions with the human mitochondrial 12S rRNA and its deafness-associated mutations, C1494U and A1555G. We report a rapid assay that allows screening of aminoglycoside compounds to these classes of rRNAs...
January 19, 2017: ACS Infectious Diseases
https://www.readbyqxmd.com/read/28101308/antibacterial-resistance-in-patients-with-hematopoietic-stem-cell-transplantation
#11
REVIEW
Sehnaz Alp, Murat Akova
Recipients of hematopoietic stem cell transplantation (HSCT) are at substantial risk of bacterial, fungal, viral, and parasitic infections depending on the time elapsed since transplantation, presence of graft-versus-host disease (GVHD), and the degree of immunosuppression. Infectious complications in HSCT recipients are associated with high morbidity and mortality. Bacterial infections constitute the major cause of infectious complications, especially in the early post-transplant period. The emergence of antibacterial resistance complicates the management of bacterial infections in this patient group...
2017: Mediterranean Journal of Hematology and Infectious Diseases
https://www.readbyqxmd.com/read/28101153/upregulated-effects-of-mir-7-in-methicillin-resistant-staphylococcus-aureus
#12
Hong Zhang, Haiqing Li, Yan Liu, Qingyan Li, Yufang Bi, Guiqing Fang
The aim of the study was to investigate the characteristic function of the upregulated effects of miR-7 in methicillin-resistant Staphylococcus aureus (MRSA). After separating the MRSA in clinic, the expression of miR-7 mRNA was tested by reverse transcription polymerase chain reaction. The overexpression, inhibition of miR-7, and control group were established by plasmid in vitro. Following transfection of the bacterial strain, the effect of β-lactam antibiotics in minimum inhibitory concentration (MIC) was observed using the microporous dilution method, and antibacterial effects in vitro were observed using the dynamic growth curve method...
December 2016: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28099001/conformational-dynamics-in-penicillin-binding-protein-2a-of-methicillin-resistant-staphylococcus-aureus-allosteric-communication-network-and-enablement-of-catalysis
#13
Kiran V Mahasenan, Rafael Molina, Renee Bouley, Maria T Batuecas, Jed F Fisher, Juan A Hermoso, Mayland Chang, Shahriar Mobashery
The mechanism of the β-lactam antibacterials is the functionally irreversible acylation of the enzymes that catalyze the cross-linking steps in the biosynthesis of their peptidoglycan cell wall. The Gram-positive pathogen Staphylococcus aureus uses one primary resistance mechanism. An enzyme, called penicillin-binding protein 2a (PBP2a), is brought into this biosynthetic pathway to complete the cross-linking. PBP2a effectively discriminates against the β-lactam antibiotics as potential inhibitors, and in favor of the peptidoglycan substrate...
January 18, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28098806/antibacterial-activities-and-possible-modes-of-action-of-acacia-nilotica-l-del-against-multidrug-resistant-escherichia-coli-and-salmonella
#14
Muhammad Bilal Sadiq, Joel Tarning, Tay Zar Aye Cho, Anil Kumar Anal
Medicinal plants are frequently used for the treatment of various infectious diseases. The objective of this study was to evaluate the antibacterial activity and mode of action of Acacia nilotica and the antibiogram patterns of foodborne and clinical strains of Escherichia coli and Salmonella. The mechanism of action of acacia extracts against E. coli and Salmonella was elucidated by observing morphological damages including cell integrity and cell membrane permeability, as well as changes in cell structures and growth patterns in kill-time experiments...
January 14, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28097636/andrographolide-antibacterial-activity-against-common-bacteria-of-human-health-concern-and-possible-mechanism-of-action
#15
Malabika Banerjee, Debaprasad Parai, Subrata Chattopadhyay, Samir Kumar Mukherjee
Increasing bacterial resistance to common drugs is a major public health concern for the treatment of infectious diseases. Certain naturally occurring compounds of plant sources have long been reported to possess potential antimicrobial activity. This study was aimed to investigate the antibacterial activity and possible mechanism of action of andrographolide (Andro), a diterpenoid lactone from a traditional medicinal herb Andrographis paniculata. Extent of antibacterial action was assessed by minimal bactericidal concentration method...
January 17, 2017: Folia Microbiologica
https://www.readbyqxmd.com/read/28097041/effect-of-catechins-green-tea-extract-and-methylxanthines-in-combination-with-gentamicin-against-staphylococcus-aureus-and-pseudomonas-aeruginosa-combination-therapy-against-resistant-bacteria
#16
Bibi Sedigheh Fazly Bazzaz, Sahar Sarabandi, Bahman Khameneh, Hossein Hosseinzadeh
OBJECTIVES: Bacterial resistant infections have become a global health challenge and threaten the society's health. Thus, an urgent need exists to find ways to combat resistant pathogens. One promising approach to overcoming bacterial resistance is the use of herbal products. Green tea catechins, the major green tea polyphenols, show antimicrobial activity against resistant pathogens. The present study aimed to investigate the effect of catechins, green tea extract, and methylxanthines in combination with gentamicin against standard and clinical isolates of Staphylococcus aureus (S...
December 2016: Journal of Pharmacopuncture
https://www.readbyqxmd.com/read/28096686/peptide-consensus-sequence-determination-for-the-enhancement-of-the-antimicrobial-activity-and-selectivity-of-antimicrobial-peptides
#17
Ammar Almaaytah, Ya'u Ajingi, Ahmad Abualhaijaa, Shadi Tarazi, Nizar Alshar'i, Qosay Al-Balas
The rise of multidrug-resistant bacteria is causing a serious threat to the world's human population. Recent reports have identified bacterial strains displaying pan drug resistance against antibiotics and generating fears among medical health specialists that humanity is on the dawn of entering a post-antibiotics era. Global research is currently focused on expanding the lifetime of current antibiotics and the development of new antimicrobial agents to tackle the problem of antimicrobial resistance. In the present study, we designed a novel consensus peptide named "Pepcon" through peptide consensus sequence determination among members of a highly homologous group of scorpion antimicrobial peptides...
2017: Infection and Drug Resistance
https://www.readbyqxmd.com/read/28096545/thiazomycin-nocathiacin-and-analogs-show-strong-activity-against-clinical-strains-of-drug-resistant-mycobacterium-tuberculosis
#18
Sheo B Singh, Libo Xu, Peter T Meinke, Natalia Kurepina, Barry N Kreiswirth, David B Olsen, Katherine Young
Thiazolyl peptides are a class of natural products with potent Gram-positive antibacterial activities. Lack of aqueous solubility precluded this class of compounds from advancing to clinical evaluations. Nocathiacins and thiazomycins are sub-classes of thiazolyl peptides that are endowed with structural features amenable for chemical modifications. Semi-synthetic modifications of nocathiacin led to a series of analogs with improved water solubility, while retaining potency and antibacterial spectrum. We studied the activities of a selection of two natural products (nocathiacin and thiazomycin) as well as seven polar semi-synthetic analogs against twenty clinical strains of Mycobacterium tuberculosis with MDR phenotypes...
January 18, 2017: Journal of Antibiotics
https://www.readbyqxmd.com/read/28096447/pbp1b-glycosyltransferase-and-transpeptidase-activities-play-different-essential-roles-during-the-de-novo-regeneration-of-rod-shaped-morphology-in-escherichia-coli
#19
Dev K Ranjit, Matthew A Jorgenson, Kevin D Young
: Peptidoglycan is a vital component of nearly all cell wall-bearing bacteria and is a valuable target for antibacterial therapy. However, despite decades of work, there remain important gaps in understanding how this macromolecule is synthesized and molded into a three-dimensional structure that imparts specific morphologies to individual cells. Here, we investigate the particularly enigmatic area of how peptidoglycan is synthesized and shaped during the first stages of creating cell shape de novo, that is, in the absence of a pre-existing template...
January 17, 2017: Journal of Bacteriology
https://www.readbyqxmd.com/read/28096160/determinants-of-antibacterial-spectrum-and-resistance-potential-of-the-elongation-factor-g-inhibitor-argyrin-b-in-key-gram-negative-pathogens
#20
Adriana K Jones, Angela L Woods, Kenneth T Takeoka, Xiaoyu Shen, Jun-Rong Wei, Ruth E Caughlan, Charles R Dean
Argyrins are natural products with antibacterial activity against Gram-negative pathogens such as P. aeruginosa, B. multivorans and S. maltophilia We previously showed that argyrin B targets elongation factor G (FusA). Here we show that Argyrin B activity against P. aeruginosa PAO1 (MIC = 8 μg/mL) was not affected by deletion of the MexAB-OprM, MexXY-OprM, MexCD-OprJ or MexEF-OprN efflux pumps. However, argyrin B induced expression of MexXY causing a slight but reproducible antagonism with the MexXY substrate antibiotic ciprofloxacin...
January 17, 2017: Antimicrobial Agents and Chemotherapy
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