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https://www.readbyqxmd.com/read/27919287/chemical-profiling-antimicrobial-and-insecticidal-evaluations-of-polygonum-hydropiper-l
#1
Muhammad Ayaz, Muhammad Junaid, Farhat Ullah, Abdul Sadiq, Muhammad Ovais, Waqar Ahmad, Sajjad Ahmad, Anwar Zeb
BACKGROUND: The emergence of multidrug resistant (MDR) pathogens is of great concern to the global health community. Our ability to effectively treat diseases is based on the discovery of potent drugs for the treatment of these challenging diseases. Traditional medicines are one of the major sources for the discovery of safe, effective and economical drug candidates. In order to validate its antibacterial, antifungal and insecticidal potentials with respect to traditional uses, we have screened for the first time Polygonum hydropiper against pathogenic bacterial, fungal strains and a variety of insects...
December 5, 2016: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/27917206/anticancer-and-antibacterial-secondary-metabolites-from-the-endophytic-fungus-penicillium-sp-cam64-against-multi-drug-resistant-gram-negative-bacteria
#2
Jean-Bosco Jouda, Jean-de-Dieu Tamokou, Céline Djama Mbazoa, Prodipta Sarkar, Prasanta Kumar Bag, Jean Wandji
BACKGROUND: The emergence of multiple-drug resistance bacteria has become a major threat and thus calls for an urgent need to search for new effective and safe anti-bacterial agents. OBJECTIVES: This study aims to evaluate the anticancer and antibacterial activities of secondary metabolites from Penicillium sp., an endophytic fungus associated with leaves of Garcinia nobilis. METHODS: The culture filtrate from the fermentation of Penicillium sp...
September 2016: African Health Sciences
https://www.readbyqxmd.com/read/27916605/modulation-of-drug-resistance-and-biofilm-formation-of-staphylococcus-aureus-isolated-from-the-oral-cavity-of-tunisian-children
#3
Tarek Zmantar, Rihab Ben Slama, Kais Fdhila, Bochra Kouidhi, Amina Bakhrouf, Kamel Chaieb
OBJECTIVES: This study aims to investigate the antimicrobial and the anti-biofilm activities of Lactobacillus plantarum extract (LPE) against a panel of oral Staphylococcus aureus (n=9) and S. aureus ATCC 25923. The in vitro ability of LPE to modulate bacterial resistance to tetracycline, benzalchonium chloride (BC), and chlorhexidine (CHX) were tested also. METHODS: The MICs and MBCs of LPE, tetracycline (TET), CHX and BC were determined in absence and in presence of a sub-MIC doses of LPE (1/2 MIC)...
December 1, 2016: Brazilian Journal of Infectious Diseases
https://www.readbyqxmd.com/read/27914798/antimycobacterial-activity-of-novel-hydrazide-hydrazone-derivatives-with-2h-chromene-and-coumarin-scaffold
#4
Violina T Angelova, Violeta Valcheva, Nikolay G Vassilev, Rosen Buyukliev, Georgi Momekov, Ivan Dimitrov, Luciano Saso, Mirjana Djukic, Boris Shivachev
This study reports the synthesis of new 2H-chromene or coumarin based acylhydrazones, which were evaluated for their in vitro antimycobacterial activity against reference strain Mycobacterium tuberculosis H37Rv and compared to the first-line antituberculosis drugs, isoniazid (INH) and ethambutol (EMB). The most active compounds 7m (MIC 0.13μM), 7o (MIC 0.15μM) and 7k (MIC 0.17μM) demonstrated antimycobacterial activity at submicromolar concentration level and remarkably minimal associated cytotoxicity in the human embryonic kidney cell line HEK-293T...
November 25, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27914363/new-insights-into-the-sar-and-drug-combination-synergy-of-2-quinolin-4-yloxy-acetamides-against-mycobacterium-tuberculosis
#5
Bruno Couto Giacobbo, Kenia Pissinate, Valnês Rodrigues-Junior, Anne Drumond Villela, Estêvão Silveira Grams, Bruno Lopes Abbadi, Fernanda Teixeira Subtil, Nathalia Sperotto, Rogério Valim Trindade, Davi Fernando Back, Maria Martha Campos, Luiz Augusto Basso, Pablo Machado, Diógenes Santiago Santos
2-(Quinolin-4-yloxy)acetamides have been described as potent and selective in vitro inhibitors of Mycobacterium tuberculosis (Mtb) growth. Herein, a new series of optimized compounds were found to demonstrate highly potent antitubercular activity, with minimum inhibitory concentration (MIC) values against drug-susceptible and drug-resistant Mycobacterium tuberculosis strains in the submicromolar range. Furthermore, the most active compounds had no apparent toxicity to mammalian cells, and they showed intracellular activities similar to those of isoniazid and rifampin in a macrophage model of Mtb infection...
November 23, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27912884/synergism-of-coumarins-from-the-chinese-drug-zanthoxylum-nitidum-with-antibacterial-agents-against-methicillin-resistant-staphylococcus-aureus-mrsa
#6
Guo-Ying Zuo, Chun-Juan Wang, Jun Han, Yu-Qing Li, Gen-Chun Wang
BACKGROUND: Methicillin-resistant Staphylococcus aureus (MRSA) poses a serious therapeutic challenge in current clinic and new drug development. Natural coumarins have diverse bioactivities and the potential of resistance modifying effects. PURPOSE: This study is to present in-depth evaluations of in vitro antimicrobial activities of four natural coumarins 5-geranyloxy-7-methoxycoumarin (Gm, 1), (5,7-dimethoxy-8-prenyloxycoumarin (artanin, Ar, 2)), isopimpinellin (Is, 3) and phellopterin (Ph, 4) from Zanthoxylum nitidum (Roxb...
December 15, 2016: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/27909995/solithromycin-a-novel-fluoroketolide-for-the-treatment-of-community-acquired-bacterial-pneumonia
#7
REVIEW
George G Zhanel, Erika Hartel, Heather Adam, Sheryl Zelenitsky, Michael A Zhanel, Alyssa Golden, Frank Schweizer, Bala Gorityala, Philippe R S Lagacé-Wiens, Andrew J Walkty, Alfred S Gin, Daryl J Hoban, Joseph P Lynch, James A Karlowsky
Solithromycin is a novel fluoroketolide developed in both oral and intravenous formulations to address increasing macrolide resistance in pathogens causing community-acquired bacterial pneumonia (CABP). When compared with its macrolide and ketolide predecessors, solithromycin has several structural modifications which increase its ribosomal binding and reduce its propensity to known macrolide resistance mechanisms. Solithromycin, like telithromycin, affects 50S ribosomal subunit formation and function, as well as causing frame-shift errors during translation...
December 1, 2016: Drugs
https://www.readbyqxmd.com/read/27908580/antimicrobial-activity-of-novel-4h-4-oxoquinolizine-compounds-against-extensively-drug-resistant-acinetobacter-baumannii-strains
#8
Seok Hyeon Na, Hyejin Jeon, Yoo Jeong Kim, Hyo Il Kwon, Gati Noble Selasi, Asiimwe Nicholas, Chang-Soo Yun, Sang Ho Lee, Je Chul Lee
The aim of this study was to screen lead compounds exhibiting potent in vitro antimicrobial activity against multidrug-resistant (MDR) Acinetobacter baumannii strains from a library of chemical compounds. In a high-throughput screening analysis of 7520 compounds representative of 340,000 small molecules, two 4H-4-oxoquinolizine compounds were the most active against A. baumannii ATCC 17978. Subsequent selection and analysis of 70 4H-4-oxoquinolizine compounds revealed that the top 7 compounds were extremely active against extensively drug-resistant (XDR) A...
November 21, 2016: International Journal of Antimicrobial Agents
https://www.readbyqxmd.com/read/27908268/synthesis-of-new-fluoro-benzimidazole-derivatives-as-an-approach-towards-the-discovery-of-novel-intestinal-antiseptic-drug-candidates
#9
Ulviye Acar, Begüm Nurpelin Sağlık, Yusuf Özkay, Zerrin Cantürk, Juan Bueno, Fatih Demirci
In the present study, nineteen new fluoro-benzimidazole derivatives, including nifuroxazide analogues, were synthesized by microwave-supported reactions and tested against a panel of pathogenic microorganisms consisting of resistant strains. The synthesized compounds were characterised and identified by FT-IR, 1H- and 13C-NMR, mass spectroscopy, and elemental analyses, respectively. In vitro antimicrobial and cytotoxic effects of the synthesized compounds were determined by microdilution and by [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] (MTT) assay...
December 1, 2016: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/27907875/s-substituted-3-5-dinitrophenyl-1-3-4-oxadiazole-2-thiols-and-tetrazole-5-thiols-as-highly-efficient-antitubercular-agents
#10
Galina Karabanovich, Jan Němeček, Lenka Valášková, Alejandro Carazo, Klára Konečná, Jiřina Stolaříková, Alexandr Hrabálek, Oto Pavliš, Petr Pávek, Kateřina Vávrová, Jaroslav Roh, Věra Klimešová
Two new classes of antitubercular agents, namely 5-alkylsulfanyl-1-(3,5-dinitrophenyl)-1H-tetrazoles and 2-alkylsulfanyl-5-(3,5-dinitrophenyl)-1,3,4-oxadiazoles, and their structure-activity relationships are described. These compounds possessed excellent activity against Mycobacterium tuberculosis, including the clinically isolated multidrug (MDR) and extensively drug-resistant (XDR) strains, with no cross resistance with first or second-line anti-TB drugs. The minimum inhibitory concentration (MIC) values of the most promising compounds reached 0...
November 21, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27905408/limitations-of-mic-as-sole-metric-of-pharmacodynamic-response-across-the-range-of-antimicrobial-susceptibilities-within-a-single-bacterial-species
#11
Xuesong Wen, Ronette Gehring, Andrea Stallbaumer, Jim E Riviere, Victoriya V Volkova
The minimum inhibitory concentration (MIC) of an antimicrobial drug for a bacterial pathogen is used as a measure of the bacterial susceptibility to the drug. However, relationships between the antimicrobial concentration, bacterial susceptibility, and the pharmacodynamic (PD) inhibitory effect on the bacterial population are more complex. The relationships can be captured by multi-parameter models such as the Emax model. In this study, time-kill experiments were conducted with a zoonotic pathogen Pasteurella multocida and the fluoroquinolone enrofloxacin...
December 1, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27904224/estimation-of-drug-absorption-in-antibiotic-soaked-bone-grafts
#12
Manish Ramesh Shah, Rukesh R Patel, Randhirsinh V Solanki, Shailendra H Gupta
INTRODUCTION: There is paucity of literature about antibiotic uptake in bone grafts soaked in antibiotic solutions at room temperature in the operation theatre. We hypothesized that if bone grafts are dipped in different strengths of antibiotic solutions for sufficient period, their utilization at the target site helps in localized release of antibiotics in adequate inhibitory concentration to achieve the bacterial regression. The purpose of the study was to find out: (1) Optimum duration, strength, and volume of antibiotic solution required for dipping bone grafts at room temperature prior to the use...
November 2016: Indian Journal of Orthopaedics
https://www.readbyqxmd.com/read/27903459/true-rifampicin-resistance-missed-by-the-mgit-prevalence-of-this-pheno-genotype-in-the-uk-and-ireland-after-18-month-surveillance
#13
Ximena Gonzalo, Pauline Claxton, Tim Brown, Lorraine Montgomery, Margaret Fitzgibbon, Ian Laurenson, Francis Drobniewski
OBJECTIVES: To characterise rifampicin resistant strains missed by the MGIT 960 system but not by egg-based media in the UK and Ireland and to ascertain their prevalence. METHODS: All strains sent for second line susceptibility testing were prospectively collected. Drug Susceptibility Testing was performed by Resistance Ratio (RR), Proportion Method (PM), MGIT 960 and MIC determination by microdilution. Rifampicin resistance conferring mutations were detected with line probe assays and sequencing...
November 26, 2016: Clinical Microbiology and Infection
https://www.readbyqxmd.com/read/27902737/a-comparison-of-the-sensititre-mycotb-plate-the-bactec-mgit-960-and-a-microarray-based-molecular-assay-for-the-detection-of-drug-resistance-in-clinical-mycobacterium-tuberculosis-isolates-in-moscow-russia
#14
Elena Y Nosova, Danila V Zimenkov, Anastasia A Khakhalina, Alexandra I Isakova, Ludmila Y Krylova, Marina V Makarova, Ksenia Y Galkina, Maria A Krasnova, Svetlana G Safonova, Vitaly I Litvinov, Dmitry A Gryadunov, Elena M Bogorodskaya
BACKGROUND: The goal of this study was to compare the consistency of three assays for the determination of the drug resistance of Mycobacterium tuberculosis (MTB) strains with various resistance profiles isolated from the Moscow region. METHODS: A total of 144 MTB clinical isolates with a strong bias toward drug resistance were examined using Bactec MGIT 960, Sensititre MycoTB, and a microarray-based molecular assay TB-TEST to detect substitutions in the rpoB, katG, inhA, ahpC, gyrA, gyrB, rrs, eis, and embB genes that are associated with resistance to rifampin, isoniazid, fluoroquinolones, second-line injectable drugs and ethambutol...
2016: PloS One
https://www.readbyqxmd.com/read/27902389/antimicrobial-susceptibility-to-azithromycin-among-salmonella-enterica-typhi-and-paratyphi-a-isolates-from-india
#15
Richa Misra, Kashi N Prasad
Decreased ciprofloxacin susceptibility (DCS) and multi-drug resistance (MDR) in typhoidal Salmonella isolates in areas of endemicity is a significant therapeutic problem. Guidelines for azithromycin disk diffusion and minimal inhibitory concentration (MIC) interpretive criteria for Salmonella enterica serovar Typhi were published recently by CLSI in 2015.We investigated the antimicrobial susceptibility pattern of azithromycin in 100 isolates of Salmonella Typhi (n=80), Paratyphi A (n=18) and B (n=2) recovered from blood stream infections from January 2013 to December 2015...
November 10, 2016: Journal of Medical Microbiology
https://www.readbyqxmd.com/read/27902365/the-oral-cavities-of-healthy-infants-harbor-high-proportions-of-streptococcus-salivarius-strains-with-phenotypic-and-genotypic-resistance-to-multiple-classes-of-antibiotics
#16
Thaís H Palma, Erika Harth-Chú, Jodie Scott, Rafael N Stipp, Heike Boisvert, Mariana F Salomão, Jéssica D Theobaldo, Rosana F Possobon, Leandro C Nascimento, Jonathan W McCafferty, Lina Faller, Margaret J Duncan, Renata O Mattos-Graner
Emerging antibiotic resistance in the oropharyngeal microbiota, of which Streptococcus salivarius is a prominent species, represents a challenge for treating pediatric populations. In this study, we investigated the role of S. salivarius as a reservoir for antibiotic resistance genes (ARG) in the oral microbiota by analyzing 95 S. salivarius isolates from 22 healthy infants (2 to 16 months of age). Minimum inhibitory concentrations (MIC) of penicillin G, amoxicillin, erythromycin, tetracycline, doxycycline and streptomycin were determined...
October 24, 2016: Journal of Medical Microbiology
https://www.readbyqxmd.com/read/27899033/novel-antibacterial-polymeric-nanocomposite-for-smart-co-delivery-of-anticancer-drugs
#17
Elham Zakerzadeh, Effat Alizadeh, Hossein Samadi Kafil, Azad Mohammad Hassanzadeh, Roya Salehi, Mehrdad Mahkam
Here a novel antibacterial nanocomposite was developed for combination cancer therapy. The synthesized nanocarrier was characterized by FTIR, (1)H NMR, thermogravimetric analysis (TGA), and FESEM-EDX. Its antibacterial activity was assessed by determining minimum inhibitory concentration (MIC) values. Doxorubicin (DOX) and methotrexate (MTX) conjugation with nanocarrier sustained the release of both drugs with apparent pH-triggered manner. Co-administration of DOX with MTX leads to an efficient anticancer performance to MCF7 cell lines verified by qRT-PCR and MTT assay tests...
November 29, 2016: Artificial Cells, Nanomedicine, and Biotechnology
https://www.readbyqxmd.com/read/27895017/molecular-investigation-of-resistance-to-second-line-injectable-drugs-in-multidrug-resistant-clinical-isolates-of-mycobacterium-tuberculosis-in-france
#18
Florence Brossier, Anne Pham, Christine Bernard, Alexandra Aubry, Vincent Jarlier, Nicolas Veziris, Wladimir Sougakoff
The second line injectable drugs (SLID, i.e. amikacin, kanamycin, capreomycin) are key drugs for the treatment of multidrug-resistant tuberculosis. Mutations in rrs region 1400, tlyA and eis promoter are associated with resistance to SLID, to capreomycin and to kanamycin respectively. In this study, the sequencing data of SLID resistance-associated genes were compared to the results of phenotypic drug susceptibility testing by the proportion method for the SLID in 206 multidrug-resistant clinical isolates of Mycobacterium tuberculosis collected in France...
November 28, 2016: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/27895011/evaluation-of-fluoroquinolone-activity-against-emergence-of-resistant-salmonella-enterica-serovar-typhimurium-using-in-vitro-dynamic-models
#19
Seung-Jin Lee, Elias Gebru Awji, Na-Hye Park, Seung-Chun Park
The objectives of this study were to determine pharmacokinetic/pharmacodynamic (PK/PD) indices of fluoroquinolones that minimize the emergence of resistant Salmonella enterica serovar Typhimurium (S. Typhimurium) using in vitro dynamic models, and to establish mechanisms of resistance. Three fluoroquinolones, difloxacin (DIF), enrofloxacin (ENR) and marbofloxacin (MAR), at five dose levels and 3 days of treatment were simulated. Bacterial killing-regrowth kinetics and emergence of resistant bacteria after antibacterial drug- exposure were quantified...
November 28, 2016: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/27894983/a-case-of-clinical-and-microbiological-failure-of-azithromycin-therapy-in-salmonella-enterica-serotype-typhi-despite-low-azithromycin-mic
#20
Abi Manesh, Veeraraghavan Balaji, Devanga Ragupathi Naveen Kumar, Priscilla Rupali
Typhoid fever remains a serious problem in many developing countries. Due to resistance to multiple first line drugs, azithromycin has evolved as an important drug in the treatment of Typhoid. While therapy with azithromycin is highly effective, no clinically validated mean inhibitory concentration (MIC) break points or disc diffusion cutoff guidelines are available so far. We describe an Indian adult with clinical and microbiological failure to azithromycin despite low azithromycin MIC.
November 25, 2016: International Journal of Infectious Diseases: IJID
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