scholarly journals Aryl Rhodanines Specifically Inhibit Staphylococcal and Enterococcal Biofilm Formation

2009 ◽  
Vol 53 (10) ◽  
pp. 4357-4367 ◽  
Author(s):  
Timothy J. Opperman ◽  
Steven M. Kwasny ◽  
John D. Williams ◽  
Atiyya R. Khan ◽  
Norton P. Peet ◽  
...  

ABSTRACT Staphylococcus epidermidis and Staphylococcus aureus are the leading causative agents of indwelling medical device infections because of their ability to form biofilms on artificial surfaces. Here we describe the antibiofilm activity of a class of small molecules, the aryl rhodanines, which specifically inhibit biofilm formation of S. aureus, S. epidermidis, Enterococcus faecalis, E. faecium, and E. gallinarum but not the gram-negative species Pseudomonas aeruginosa or Escherichia coli. The aryl rhodanines do not exhibit antibacterial activity against any of the bacterial strains tested and are not cytotoxic against HeLa cells. Preliminary mechanism-of-action studies revealed that the aryl rhodanines specifically inhibit the early stages of biofilm development by preventing attachment of the bacteria to surfaces.

2019 ◽  
Vol 66 (3-4) ◽  
pp. 220-226
Author(s):  
J. Efrain Ramirez-Benitez ◽  
Ibis Vargas Paredes ◽  
Luis F. Cuevas Glory ◽  
Enrique Sauri Duch ◽  
Victor M. Moo Huchin ◽  
...  

Plant-essential oils have been considered as an important source of bioactive molecules like antimicrobials, analgesics, anti-inflammatory and anti-carcinogen agents. Biological functions of plant extracts from the genus Capsicum are unknown. In the present work, non-polar fractions of ripe and unripe fruits of Capsicum chinense Jacq. Cultivar (cv.) Jaguar and Criollo were obtained by hexane-batch extraction and tested for antimicrobial activity against Gram-negative bacterial strain Escherichia coli (ATCC 25922), Gram-positive bacterial strains Enterococcus faecalis (ATCC 29212), Staphylococcus aureus (ATCC 25923) and Staphylococcus epidermidis (ATCC 12228), and yeast Candida albicans (ATCC 90028). Non-polar fractions from ripe fruits for both cv. exhibited greater antimicrobial activity compared to unripe fruits. Implication of numbered FFA’s on observed antimicrobial activity are discussed.


2020 ◽  
Author(s):  
Nusrat Abedin ◽  
Abdullah Hamed A Alshehri ◽  
Ali M A Almughrbi ◽  
Olivia Moore ◽  
Sheikh Alyza ◽  
...  

Antimicrobial resistance (AMR) has become one of the more serious threats to the global health. The emergence of bacteria resistant to antimicrobial substances decreases the potencies of current antibiotics. Consequently, there is an urgent and growing need for the developing of new classes of antibiotics. Three prepared novel iron complexes have a broad-spectrum antimicrobial activity with minimum bactericidal concentration (MBC) values ranging from 3.5 to 10 mM and 3.5 to 40 mM against Gram-positive and Gram-negative bacteria with antimicrobial resistance phenotype, respectively. Time-kill studies and quantification of the extracellular DNA confirmed the bacteriolytic mode of action of the iron-halide compounds. Additionally, the novel complexes showed significant antibiofilm activity against the tested pathogenic bacterial strains at concentrations lower than the MBC. The cytotoxic effect of the complexes on different mammalian cell lines show sub-cytotoxic values at concentrations lower than the minimum bactericidal concentrations.


2003 ◽  
Vol 185 (18) ◽  
pp. 5632-5638 ◽  
Author(s):  
Konstantin Agladze ◽  
Debra Jackson ◽  
Tony Romeo

ABSTRACT The complex architecture of bacterial biofilms inevitably raises the question of their design. Microstructure of developing Escherichia coli biofilms was analyzed under static and laminar flow conditions. Cell attachment during early biofilm formation exhibited periodic density patterns that persisted during development. Several models for the origination of biofilm microstructure are considered, including an activator-inhibitor or Turing model.


2009 ◽  
Vol 4 (1) ◽  
pp. 1934578X0900400 ◽  
Author(s):  
Branislava Lakušić ◽  
Violeta Slavkovska ◽  
Milica Pavlović ◽  
Marina Milenković ◽  
Jelena Antić Stanković ◽  
...  

The essential oils of the aerial parts and fruits of Chaerophyllum aureum L., collected from two mountains in Serbia, were analyzed by GC and GC/MS. Sabinene (18.5-31.6%), p-cymene (7.9-25.4%) and limonene (1.9-10.9%) were characterized as the main constituents. The oils were tested against six bacterial strains and one strain of yeast, Candida albicans. The highest antimicrobial activity was observed against the Gram-positive bacteria Staphylococcus aureus, S. epidermidis and Micrococcus luteus, while of the Gram-negative strains, Escherichia coli was the most sensitive.


2002 ◽  
Vol 184 (18) ◽  
pp. 5130-5140 ◽  
Author(s):  
Kazushi Suzuki ◽  
Xin Wang ◽  
Thomas Weilbacher ◽  
Anna-Karin Pernestig ◽  
Öjar Melefors ◽  
...  

ABSTRACT The global regulator CsrA (carbon storage regulator) is an RNA binding protein that coordinates central carbon metabolism, activates flagellum biosynthesis and motility, and represses biofilm formation in Escherichia coli. CsrA activity is antagonized by the untranslated RNA CsrB, to which it binds and forms a globular ribonucleoprotein complex. CsrA indirectly activates csrB transcription, in an apparent autoregulatory mechanism. In the present study, we elucidate the intermediate regulatory circuitry of this system. Mutations affecting the BarA/UvrY two-component signal transduction system decreased csrB transcription but did not affect csrA′-′lacZ expression. The uvrY defect was severalfold more severe than that of barA. Both csrA and uvrY were required for optimal barA expression. The latter observation suggests an autoregulatory loop for UvrY. Ectopic expression of uvrY suppressed the csrB-lacZ expression defects caused by uvrY, csrA, or barA mutations; csrA suppressed csrA or barA defects; and barA complemented only the barA mutation. Purified UvrY protein stimulated csrB-lacZ expression approximately sixfold in S-30 transcription-translation reactions, revealing a direct effect of UvrY on csrB transcription. Disruption of sdiA, which encodes a LuxR homologue, decreased the expression of uvrY′-′lacZ and csrB-lacZ fusions but did not affect csrA′-′lacZ. The BarA/UvrY system activated biofilm formation. Ectopic expression of uvrY stimulated biofilm formation by a csrB-null mutant, indicative of a CsrB-independent role for UvrY in biofilm development. Collectively, these results demonstrate that uvrY resides downstream from csrA in a signaling pathway for csrB and that CsrA stimulates UvrY-dependent activation of csrB expression by BarA-dependent and -independent mechanisms.


2018 ◽  
Vol 13 (4) ◽  
pp. 1934578X1801300
Author(s):  
Daniyar Sadyrbekov ◽  
Timur Saliev ◽  
Yuri Gatilov ◽  
Ivan Kulakov ◽  
Roza Seidakhmetova ◽  
...  

A cyclopropane derivative of limonene, (1 S, 4 S, 6 R)-7,7-dichloro-4-[(1 S)-2,2-dichloro-1-methylcyclopropyl]-1-methylbicyclo [4.1.0] heptane (compound 2), was synthesized and its structure was determined by NMR and X-ray crystallographic methods. In addition, an antimicrobial activity of the compound against Gram-positive ( Staphylococcus aureus, Bacillus subtilis) and Gram-negative ( Escherichia coli, Pseudomonas aeruginosa) bacterial strains was also scrutinized.


2001 ◽  
Vol 2 (1) ◽  
Author(s):  
Ana Marcia De Matos Volpato ◽  
Ester De Moura Rios ◽  
Marilis Dallarmi Miguel ◽  
Paulo Cesar Sander ◽  
Obdúlio Gomes Miguel

A atividade antimicrobiana de Calendula officinalis L. (Asteraceae) já foi cientificamente comprovada em outros países. O objetivo deste trabalho foi avaliar a atividade antibacteriana de C. officinalis cultivada no Paraná - Brasil, nas condições de extração etanólica 50%, com filtração e partições sucessivas com hexano, diclorometano, acetato de etila e butanol, frente a cepas Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853, Staphylococcus aureus ATCC 25923, Staphylococcus epidermidis ATCC 12228 e Bacillus cereus, pela técnica da difusão em meio sólido por cavidade e posteriormente pelo método de diluição em placa. Os resultados demonstraram que algumas frações do extrato inibiram as bactérias gram-positivas, com atividade frente a Staphylococcus e Bacilos e inexiste em gram negativas, indicando que o princípio ativo responsável pela atividade antibacteriana observada possa ser isolado a partir das frações Hexânica e DCM nas condições de extração propostas neste trabalho. Abstract The Calendula officinalis L. (Asteraceae) antimicrobial action has already been scientifically proved in other countries. The aim of this study was to assess the antibacterial action of the Callendula officinalis which is grown in Paraná - Brasil, under extraction conditions at ethanol 50%, with filtration and successive partitions with hexane, dichloromethane, ethyl acetate and butane, contrasting with strains Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853, Staphylococcus aureus ATCC 25923, Staphylococcus epidermidis ATCC 12228 and Bacilus cereus, by the difusion technique in solid media by cavity and afterwards by the plaque dilution method. The results showed that some fractions of the extract inhibited the gram-prositive bacteria, with activity in contrast with Staphylococcus and Bacillus and non-existing in gram-negative, also indicating that the active ingredient responsible for the antibacterial action observed can be isolated from the Hexanic and DCM fractions under the extraction conditions proposed in this study.


2004 ◽  
Vol 48 (3) ◽  
pp. 961-969 ◽  
Author(s):  
Astrid Zervosen ◽  
Wei-Ping Lu ◽  
Zhouliang Chen ◽  
Ronald E. White ◽  
Thomas P. Demuth ◽  
...  

ABSTRACT Several non-β-lactam compounds were active against various gram-positive and gram-negative bacterial strains. The MICs of arylalkylidene rhodanines and arylalkylidene iminothiazolidin-4-ones were lower than those of ampicillin and cefotaxime for methicillin-resistant Staphylococcus aureus MI339 and vancomycin-resistant Enterococcus faecium EF12. Several compounds were found to inhibit the cell wall synthesis of S. aureus and the last two steps of peptidoglycan biosynthesis catalyzed by ether-treated cells of Escherichia coli or cell wall membrane preparations of Bacillus megaterium. The effects of the arylalkylidene rhodanines and arylalkylidene iminothiazolidin-4-one derivatives on E. coli PBP 3 and PBP 5, Streptococcus pneumoniae PBP 2xS (PBP 2x from a penicillin-sensitive strain) and PBP 2xR (PBP 2x from a penicillin-resistant strain), low-affinity PBP 2a of S. aureus, and the Actinomadura sp. strain R39 and Streptomyces sp. strain R61 dd-peptidases were studied. Some of the compounds exhibited inhibitory activities in the 10 to 100 μM concentration range. The inhibition of PBP 2xS by several of them appeared to be noncompetitive. The dissociation constant for the best inhibitor (Ki = 10 μM) was not influenced by the presence of the substrate.


Microbiology ◽  
2005 ◽  
Vol 151 (7) ◽  
pp. 2487-2497 ◽  
Author(s):  
Anne Vianney ◽  
Grégory Jubelin ◽  
Sophie Renault ◽  
Corine Dorel ◽  
Philippe Lejeune ◽  
...  

Curli are necessary for the adherence of Escherichia coli to surfaces, and to each other, during biofilm formation, and the csgBA and csgDEFG operons are both required for their synthesis. A recent survey of gene expression in Pseudomonas aeruginosa biofilms has identified tolA as a gene activated in biofilms. The tol genes play a fundamental role in maintaining the outer-membrane integrity of Gram-negative bacteria. RcsC, the sensor of the RcsBCD phosphorelay, is involved, together with RcsA, in colanic acid capsule synthesis, and also modulates the expression of tolQRA and csgDEFG. In addition, the RcsBCD phosphorelay is activated in tol mutants or when Tol proteins are overexpressed. These results led the authors to investigate the role of the tol genes in biofilm formation in laboratory and clinical isolates of E. coli. It was shown that the adherence of cells was lowered in the tol mutants. This could be the result of a drastic decrease in the expression of the csgBA operon, even though the expression of csgDEFG was slightly increased under such conditions. It was also shown that the Rcs system negatively controls the expression of the two csg operons in an RcsA-dependent manner. In the tol mutants, activation of csgDEFG occurred via OmpR and was dominant upon repression by RcsB and RcsA, while these two regulatory proteins repressed csgBA through a dominant effect on the activator protein CsgD, thus affecting curli synthesis. The results demonstrate that the Rcs system, previously known to control the synthesis of the capsule and the flagella, is an additional component involved in the regulation of curli. Furthermore, it is shown that the defect in cell motility observed in the tol mutants depends on RcsB and RcsA.


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