New Trimethoprim-Like Molecules: Bacteriological Evaluation and Insights into Their Action

This work reports a detailed characterization of the antimicrobial profile of two trimethoprim-like molecules (compounds 1a and 1b) identified in previous studies. Both molecules displayed remarkable antimicrobial activity, particularly when combined with sulfamethoxazole. In disk diffusion assays on Petri dishes, compounds 1a and 1b showed synergistic effects with colistin. Specifically, in combinations with low concentrations of colistin, very large increases in the activities of compounds 1a and 1b were determined, as demonstrated by alterations in the kinetics of bacterial growth despite only slight changes in the fractional inhibitory concentration index. The effect of colistin may be to increase the rate of antibiotic entry while reducing efflux pump activity. Compounds 1a and 1b were susceptible to extrusion by efflux pumps, whereas the inhibitor phenylalanine arginyl β-naphthylamide (PAβN) exerted effects similar to those of colistin. The interactions between the target enzyme (dihydrofolate reductase), the coenzyme nicotinamide adenine dinucleotide phosphate (NADPH), and the studied molecules were explored using enzymology tools and computational chemistry. A model based on docking results is reported.

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Pharmacodynamic Interaction ofQuercus infectoriaGalls Extract in Combination with Vancomycin against MRSA Using Microdilution Checkerboard and Time-Kill Assay

Evidence-based Complementary and Alternative Medicine ◽

10.1155/2012/493156 ◽

2012 ◽

Vol 2012 ◽

pp. 1-6 ◽

Cited By ~ 10

Author(s):

Dayang Fredalina Basri ◽

Radhiah Khairon

Keyword(s):

Inhibitory Concentration ◽

Synergistic Effects ◽

Bactericidal Effect ◽

Pharmacodynamic Interaction ◽

Killing Rate ◽

Mrsa Strains ◽

Index Value ◽

Time Kill ◽

Kinetics Of ◽

Quercus Infectoria

The galls ofQuercus infectoriaOlivier possess astringent properties which helps in the tightening of the vaginal epithelium in the post-natal period. The present study aimed to observe the time-kill kinetics of the acetone and methanol extracts of gall ofQ. infectoriain combination with vancomycin against two methicillin-resistantStaphylococcus aureus(MRSA) strains; ATCC 33591 and MU 9495 (laboratory-passaged strain). Minimum inhibitory concentration (MIC) of the extracts were determined using microdilution technique whereas the checkerboard and time-kill kinetics were employed to verify the synergistic effects of treatment with vancomycin. The FIC index value of the combinations against both MRSA strains showed that the interaction was synergistic (FIC index<0.5). Time-kill assays showed the bactericidal effect of the combination treatment at 1/8XMIC of the extract and 1/8XMIC of vancomycin, were respectively at7.2±0.28 hr against ATCC 33591 compared to complete attenuation of the growth of the same strain after 8 hr of treatment with vancomycin alone. In conclusion, the combination extracts ofQ. infectoriawith vancomycin were synergistic according to FIC index values. The time-kill curves showed that the interaction was additive with a more rapid killing rate but, which did not differ significantly with vancomycin.

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Molecular and phenotypic characterization of efflux pump and biofilm in multi-drug resistant non-typhoidal Salmonella Serovars isolated from food animals and handlers in Lagos Nigeria

One Health Outlook ◽

10.1186/s42522-021-00035-w ◽

2021 ◽

Vol 3 (1) ◽

Author(s):

Elizabeth Tolulope Olubisose ◽

Abraham Ajayi ◽

Adeyemi Isaac Adeleye ◽

Stella Ifeanyi Smith

Keyword(s):

Antibiotic Resistance ◽

Biofilm Formation ◽

Efflux Pump ◽

Efflux Pumps ◽

Multidrug Resistant ◽

Diffusion Method ◽

Phenotypic Characterization ◽

Pump Activity ◽

Food Animals

Abstract Background Multidrug resistance efflux pumps and biofilm formation are mechanisms by which bacteria can evade the actions of many antimicrobials. Antibiotic resistant non-typhoidal Salmonella serovars have become wide spread causing infections that result in high morbidity and mortality globally. The aim of this study was to evaluate the efflux pump activity and biofilm forming capability of multidrug resistant non-typhoidal Salmonella (NTS) serovars isolated from food handlers and animals (cattle, chicken and sheep) in Lagos. Methods Forty eight NTS serovars were subjected to antibiotic susceptibility testing by the disc diffusion method and phenotypic characterization of biofilm formation was done by tissue culture plate method. Phenotypic evaluation of efflux pump activity was done by the ethidium bromide cartwheel method and genes encoding biofilm formation and efflux pump activity were determined by PCR. Results All 48 Salmonella isolates displayed resistance to one or more classes of test antibiotics with 100% resistance to amoxicillin-clavulanic acid. Phenotypically, 28 (58.3%) of the isolates exhibited efflux pump activity. However, genotypically, 7 (14.6%) of the isolates harboured acrA, acrB and tolC, 8 (16.7%) harboured acrA, acrD and tolC while 33 (68.8%) possessed acrA, acrB, acrD and tolC. All (100%) the isolates phenotypically had the ability to form biofilm with 23 (47.9%), 24 (50.0%), 1 (2.1%) categorized as strong (SBF), moderate (MBF) and weak (WBF) biofilm formers respectively but csgA gene was detected in only 23 (47.9%) of them. Antibiotic resistance frequency was significant (p < 0.05) in SBF and MBF and efflux pump activity was detected in 6, 21, and 1 SBF, MBF and WBF respectively. Conclusion These data suggest that Salmonella serovars isolated from different food animals and humans possess active efflux pumps and biofilm forming potential which has an interplay in antibiotic resistance. There is need for prudent use of antibiotics in veterinary medicine and scrupulous hygiene practice to prevent the transmission of multidrug resistant Salmonella species within the food chain.

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Characterization of Binding of Magnetic Nanoparticles to Rolling Circle Amplification Products by Turn-On Magnetic Assay

Biosensors ◽

10.3390/bios9030109 ◽

2019 ◽

Vol 9 (3) ◽

pp. 109 ◽

Cited By ~ 2

Author(s):

Sobhan Sepehri ◽

Björn Agnarsson ◽

Teresa Zardán Gómez de la Torre ◽

Justin F. Schneiderman ◽

Jakob Blomgren ◽

...

Keyword(s):

Magnetic Nanoparticles ◽

Specific Binding ◽

Ac Susceptibility ◽

Rolling Circle Amplification ◽

Rolling Circle ◽

Low Concentrations ◽

Assay Performance ◽

Particle Ensemble ◽

Kinetics Of

The specific binding of oligonucleotide-tagged 100 nm magnetic nanoparticles (MNPs) to rolling circle products (RCPs) is investigated using our newly developed differential homogenous magnetic assay (DHMA). The DHMA measures ac magnetic susceptibility from a test and a control samples simultaneously and eliminates magnetic background signal. Therefore, the DHMA can reveal details of binding kinetics of magnetic nanoparticles at very low concentrations of RCPs. From the analysis of the imaginary part of the DHMA signal, we find that smaller MNPs in the particle ensemble bind first to the RCPs. When the RCP concentration increases, we observe the formation of agglomerates, which leads to lower number of MNPs per RCP at higher concentrations of RCPs. The results thus indicate that a full frequency range of ac susceptibility observation is necessary to detect low concentrations of target RCPs and a long amplification time is not required as it does not significantly increase the number of MNPs per RCP. The findings are critical for understanding the underlying microscopic binding process for improving the assay performance. They furthermore suggest DHMA is a powerful technique for dynamically characterizing the binding interactions between MNPs and biomolecules in fluid volumes.

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Irradiation behavior of pyrolytic silicon carbide

Proceedings, annual meeting, Electron Microscopy Society of America ◽

10.1017/s0424820100074288 ◽

1983 ◽

Vol 41 ◽

pp. 72-73

Author(s):

R. J. Lauf

Keyword(s):

Silicon Carbide ◽

Fission Products ◽

Thermodynamics And Kinetics ◽

Neutron Fluences ◽

Fuel Particles ◽

Sic Coatings ◽

Irradiation Behavior ◽

Kinetics Of ◽

Htgr Fuel

Fuel particles for the High-Temperature Gas-Cooled Reactor (HTGR) contain a layer of pyrolytic silicon carbide to act as a miniature pressure vessel and primary fission product barrier. Optimization of the SiC with respect to fuel performance involves four areas of study: (a) characterization of as-deposited SiC coatings; (b) thermodynamics and kinetics of chemical reactions between SiC and fission products; (c) irradiation behavior of SiC in the absence of fission products; and (d) combined effects of irradiation and fission products. This paper reports the behavior of SiC deposited on inert microspheres and irradiated to fast neutron fluences typical of HTGR fuel at end-of-life.

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Kinetics of Various 99mTc-Sn-Pyrophosphate Compounds in the Rat

Nuklearmedizin ◽

10.1055/s-0037-1620623 ◽

1977 ◽

Vol 16 (04) ◽

pp. 157-162 ◽

Cited By ~ 1

Author(s):

C. Schümichen ◽

B. Mackenbrock ◽

G. Hoffmann

Keyword(s):

Normal Saline ◽

Half Life ◽

Compound A ◽

Short Half Life ◽

Low Concentrations ◽

The Stability ◽

Kinetics Of ◽

In Vitro Stability

SummaryThe bone-seeking 99mTc-Sn-pyrophosphate compound (compound A) was diluted both in vitro and in vivo and proved to be unstable both in vitro and in vivo. However, stability was much better in vivo than in vitro and thus the in vitro stability of compound A after dilution in various mediums could be followed up by a consecutive evaluation of the in vivo distribution in the rat. After dilution in neutral normal saline compound A is metastable and after a short half-life it is transformed into the other 99mTc-Sn-pyrophosphate compound A is metastable and after a short half-life in bone but in the kidneys. After dilution in normal saline of low pH and in buffering solutions the stability of compound A is increased. In human plasma compound A is relatively stable but not in plasma water. When compound B is formed in a buffering solution, uptake in the kidneys and excretion in urine is lowered and blood concentration increased.It is assumed that the association of protons to compound A will increase its stability at low concentrations while that to compound B will lead to a strong protein bond in plasma. It is concluded that compound A will not be stable in vivo because of a lack of stability in the extravascular space, and that the protein bond in plasma will be a measure of its in vivo stability.

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Intramolecular Proton Transfer in the Isomerization of Hydroxyacetone: A Detailed Characterization Based on Reaction Force Analysis and the Bond Fragility Spectrum

10.26434/chemrxiv.12049062 ◽

2020 ◽

Author(s):

Wallace Derricotte ◽

Huiet Joseph

Keyword(s):

Chemical Potential ◽

Reaction Force ◽

Intramolecular Proton Transfer ◽

Intermediate Energy ◽

Force Analysis ◽

Activation Energy Barrier ◽

Detailed Characterization ◽

Proton Transfers ◽

Reaction Force Constant

The mechanism of isomerization of hydroxyacetone to 2-hydroxypropanal is studied within the framework of reaction force analysis at the M06-2X/6-311++G(d,p) level of theory. Three unique pathways are considered: (i) a step-wise mechanism that proceeds through formation of the Z-isomer of their shared enediol intermediate, (ii) a step-wise mechanism that forms the E-isomer of the enediol, and (iii) a concerted pathway that bypasses the enediol intermediate. Energy calculations show that the concerted pathway has the lowest activation energy barrier at 45.7 kcal mol<sup>-1</sup>. The reaction force, chemical potential, and reaction electronic flux are calculated for each reaction to characterize electronic changes throughout the mechanism. The reaction force constant is calculated in order to investigate the synchronous/asynchronous nature of the concerted intramolecular proton transfers involved. Additional characterization of synchronicity is provided by calculating the bond fragility spectrum for each mechanism.

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Submerged upflow biotower operation and computer simulation

Water Science & Technology ◽

10.2166/wst.1994.0554 ◽

1994 ◽

Vol 30 (11) ◽

pp. 143-146

Author(s):

Ronald D. Neufeld ◽

Christopher A. Badali ◽

Dennis Powers ◽

Christopher Carson

Keyword(s):

Computer Simulation ◽

Benzoic Acid ◽

Computer Model ◽

Rate Constants ◽

Batch Mode ◽

Operational Conditions ◽

First Order ◽

Low Concentrations ◽

Biological Transformation ◽

Kinetics Of

A two step operation is proposed for the biodegradation of low concentrations (< 10 mg/L) of BETX substances in an up flow submerged biotower configuration. Step 1 involves growth of a lush biofilm using benzoic acid in a batch mode. Step 2 involves a longer term biological transformation of BETX. Kinetics of biotransformations are modeled using first order assumptions, with rate constants being a function of benzoic acid dosages used in Step 1. A calibrated computer model is developed and presented to predict the degree of transformation and biomass level throughout the tower under a variety of inlet and design operational conditions.

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Detailed Characterization of an Apparently Unspliced Herpes Simplex Virus Type 1 Gene Mapping in the Interior of Another

Journal of Virology ◽

10.1128/jvi.45.2.899-899.1983 ◽

1983 ◽

Vol 45 (2) ◽

pp. 899-899 ◽

Cited By ~ 1

Keyword(s):

Herpes Simplex Virus ◽

Herpes Simplex ◽

Gene Mapping ◽

Virus Type ◽

Herpes Simplex Virus Type ◽

Detailed Characterization ◽

Simplex Virus

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DETAILED CHARACTERIZATION OF EUROPA'S RIDGE MORPHOLOGY

10.1130/abs/2016am-286453 ◽

2016 ◽

Author(s):

Janelle A.F. Heitmeier ◽

◽

Emily S. Martin ◽

Jordan M. Bretzfelder ◽

D. Alex Patthoff ◽

...

Keyword(s):

Detailed Characterization

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Study of nickel-molybdenum catalysts for methanation of carbon monoxide

Collection of Czechoslovak Chemical Communications ◽

10.1135/cccc19800783 ◽

1980 ◽

Vol 45 (3) ◽

pp. 783-790 ◽

Cited By ~ 1

Author(s):

Petr Taras ◽

Milan Pospíšil

Keyword(s):

Carbon Monoxide ◽

Catalytic Activity ◽

Mixed Oxides ◽

Minor Component ◽

Fast Neutrons ◽

Scanning Calorimetry ◽

Low Concentrations ◽

Γ Rays ◽

Molybdenum Catalysts ◽

Kinetics Of

Catalytic activity of nickel-molybdenum catalysts for methanation of carbon monoxide and hydrogen was studied by means of differential scanning calorimetry. The activity of NiMoOx systems exceeds that of carrier-free nickel if x < 2, and is conditioned by the oxidation degree of molybdenum, changing in dependence on the composition in the region Mo-MoO2. The activity of the catalysts is adversely affected by irradiation by fast neutrons, dose 28.1 Gy, or by γ rays using doses in the region 0.8-52 kGy. The system is most susceptible to irradiation in the region of low concentrations of the minor component (about 1 mol.%). The dependence of changes in catalytic activity of γ-irradiated samples on the dose exhibits a maximum in the range of 2-5 kGy. The changes in catalytic activity are stimulated by the change of reactivity of the starting mixed oxides, leading to different kinetics of their reduction and modification of their adsorption properties. The irradiation of the catalysts results in lowered concentration of the active centres for the methanation reaction.

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