scholarly journals Microbial Sensor for Determination of Amoxicillin Activity

2020 ◽  
Vol 65 (1-2) ◽  
pp. 3-9
Author(s):  
O. I. Guliy ◽  
B. D. Zaitsev ◽  
A. V. Smirnov ◽  
O. A. Karavaeva ◽  
A. К. М. Alsowaidi ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Lithium Niobate ◽  
High Frequency ◽  
Discharge Plasma ◽  
Film Surface ◽  
Polystyrene Film ◽  
Microbial Cells ◽  
Microbial Sensor ◽  
Argon Discharge

A sensor based on the electrodynamic microwave resonator has been developed to determine the antibacterial activity of antibiotics using amoxicillin as an example. Microbial cells immobilized on the polystyrene film surface were used as a sensitive element of the sensor. The optimal conditions for the immobilization of Escherichia coli Xl-1 microbial cells on the surface of a thin polystyrene film modified in high-frequency argon discharge plasma and deposited on a lithium niobate plate were determined. The effect of amoxicillin on immobilized microbial cells was studied using the developed sensor. It has been established that the increase in con- centration of amoxicillin from 5 to 50 μg/ml leads to a significant change in the reflection coefficient S11 at the resonance frequency from the lithium niobate plate in the range of -12.6 dB — -15.1 dB. It has been shown that the developed sensor allows determining the antibacterial activity of drugs in the studied concentration range with an analysis time of 15 min.

Identification of N-Substituted Triazolo-azetidines as Novel Antibacterials using pDualrep2 HTS Platform

2019 ◽  
Vol 22 (5) ◽  
pp. 346-354
Author(s):  
Yan A. Ivanenkov ◽  
Renat S. Yamidanov ◽  
Ilya A. Osterman ◽  
Petr V. Sergiev ◽  
Vladimir A. Aladinskiy ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Large Scale ◽  
Underlying Mechanism ◽  
Luciferase Assay ◽  
Reporter System ◽  
E Coli ◽  
Starting Point ◽  
High Concentrations ◽  
Mic Value

Aim and Objective: Antibiotic resistance is a serious constraint to the development of new effective antibacterials. Therefore, the discovery of the new antibacterials remains one of the main challenges in modern medicinal chemistry. This study was undertaken to identify novel molecules with antibacterial activity. Materials and Methods: Using our unique double-reporter system, in-house large-scale HTS campaign was conducted for the identification of antibacterial potency of small-molecule compounds. The construction allows us to visually assess the underlying mechanism of action. After the initial HTS and rescreen procedure, luciferase assay, C14-test, determination of MIC value and PrestoBlue test were carried out. Results: HTS rounds and rescreen campaign have revealed the antibacterial activity of a series of Nsubstituted triazolo-azetidines and their isosteric derivatives that has not been reported previously. Primary hit-molecule demonstrated a MIC value of 12.5 µg/mL against E. coli Δ tolC with signs of translation blockage and no SOS-response. Translation inhibition (26%, luciferase assay) was achieved at high concentrations up to 160 µg/mL, while no activity was found using C14-test. The compound did not demonstrate cytotoxicity in the PrestoBlue assay against a panel of eukaryotic cells. Within a series of direct structural analogues bearing the same or bioisosteric scaffold, compound 2 was found to have an improved antibacterial potency (MIC=6.25 µg/mL) close to Erythromycin (MIC=2.5-5 µg/mL) against the same strain. In contrast to the parent hit, this compound was more active and selective, and provided a robust IP position. Conclusion: N-substituted triazolo-azetidine scaffold may be used as a versatile starting point for the development of novel active and selective antibacterial compounds.

Formation of Regular Domain Structures in Quenched Ferroelectrics Under the Influence of an External High-frequency Electric Field

2019 ◽  
Vol 9 (3) ◽  
pp. 344-352 ◽  
Author(s):  
L.I. Stefanovich ◽  
O.Y. Mazur ◽  
V.V. Sobolev
Keyword(s):  
Lithium Niobate ◽  
Electric Field ◽  
Domain Structure ◽  
High Frequency ◽  
Evolution Equations ◽  
Regular Domain ◽  
Field Frequency ◽  
Domain Structures ◽  
Alternating Electric Field ◽  
Lithium Niobate Crystals

Introduction: Within the framework of the phenomenological theory of phase transitions of the second kind of Ginzburg-Landau, the kinetics of ordering of a rapidly quenched highly nonequilibrium domain structure is considered using the lithium tantalate and lithium niobate crystals as an example. Experimental: Using the statistical approach, evolution equations describing the formation of the domain structure under the influence of a high-frequency alternating electric field in the form of a standing wave were obtained. Numerical analysis has shown the possibility of forming thermodynamically stable mono- and polydomain structures. It turned out that the process of relaxation of the system to the state of thermodynamic equilibrium can proceed directly or with the formation of intermediate quasi-stationary polydomain asymmetric phases. Results: It is shown that the formation of Regular Domain Structures (RDS) is of a threshold character and occurs under the influence of an alternating electric field with an amplitude less than the critical value, whose value depends on the field frequency. The conditions for the formation of RDSs with a micrometer spatial scale were determined. Conclusion: As shown by numerical studies, the RDSs obtained retain their stability, i.e. do not disappear even after turning off the external electric field. Qualitative analysis using lithium niobate crystals as an example has shown the possibility of RDSs formation in high-frequency fields with small amplitude under resonance conditions

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