scholarly journals Thiazole Analogues of the Marine Alkaloid Nortopsentin as Inhibitors of Bacterial Biofilm Formation

Molecules ◽  
2020 ◽  
Vol 26 (1) ◽  
pp. 81
Author(s):  
Anna Carbone ◽  
Stella Cascioferro ◽  
Barbara Parrino ◽  
Daniela Carbone ◽  
Camilla Pecoraro ◽  
...  

Anti-virulence strategy is currently considered a promising approach to overcome the global threat of the antibiotic resistance. Among different bacterial virulence factors, the biofilm formation is recognized as one of the most relevant. Considering the high and growing percentage of multi-drug resistant infections that are biofilm-mediated, new therapeutic agents capable of counteracting the formation of biofilms are urgently required. In this scenario, a new series of 18 thiazole derivatives was efficiently synthesized and evaluated for its ability to inhibit biofilm formation against the Gram-positive bacterial reference strains Staphylococcus aureus ATCC 25923 and S. aureus ATCC 6538 and the Gram-negative strain Pseudomonas aeruginosa ATCC 15442. Most of the new compounds showed a marked selectivity against the Gram-positive strains. Remarkably, five compounds exhibited BIC50 values against S. aureus ATCC 25923 ranging from 1.0 to 9.1 µM. The new compounds, affecting the biofilm formation without any interference on microbial growth, can be considered promising lead compounds for the development of a new class of anti-virulence agents.

Author(s):  
Gabriel Rezende-Pereira ◽  
Julia P Albuquerque ◽  
Monica C Souza ◽  
Barbara A Nogueira ◽  
Marlei G Silva ◽  
...  

Abstract Background Bacterial biofilm on surfaces of mammary implants is a predisposing factor for several outcomes. Since Gram-positive bacteria are potential agents of biomaterial-associated infections (BAIs), their abilities to form biofilm on breast implants should be elucidated. Objectives To evaluate biofilm formation on different mammary prosthesis surfaces by major Gram-positive bacterial pathogens involved in BAIs. Methods We initially evaluated biofilm formation on polystyrene plates with and without fibrinogen or collagen for one reference strain and one clinical isolate of Enterococcus faecalis, Staphylococcus aureus, Staphylococcus epidermidis and Streptococcus pyogenes. We also tested the ability of clinical isolates to form biofilm on four different implant surfaces: polyurethane foam and smooth, microtextured and standard textured silicone. Biofilm structure and cell viability were observed by scanning electron microscopy (SEM) and confocal laser scanning microscopy (CLSM). Results All strains showed strong biofilm formation on polystyrene. After fibrinogen or collagen treatment, biofilm formation varied. With fibrinogen, reference strains of S. aureus and S. pyogenes increased biofilm formation (p<0.05). Reference strains of all species and the clinical isolate of S. pyogenes increased biofilm formation after collagen treatment (p<0.05). In general, S. aureus showed higher capacity to produce biofilm. SEM showed biofilm attached to all surfaces tested, with the presence of extracellular polymeric substances and voids. Viable cells were more frequent for E. faecalis and S. pyogenes. Conclusions All species produced biofilm on all prosthesis surfaces and under different conditions. Micrographies indicated thicker bacterial biofilm formation on microtextured and/or standard textured silicone by all species, except E. faecalis.


Molecules ◽  
2018 ◽  
Vol 23 (10) ◽  
pp. 2522 ◽  
Author(s):  
Gabriel Marc ◽  
Cătălin Araniciu ◽  
Smaranda Oniga ◽  
Laurian Vlase ◽  
Adrian Pîrnău ◽  
...  

C. albicans is the most frequently occurring fungal pathogen, and is becoming an increasing public health problem, especially in the context of increased microbial resistance. This opportunistic pathogen is characterized by a versatility explained mainly by its ability to form complex biofilm structures that lead to enhanced virulence and antibiotic resistance. In this context, a review of the known C. albicans biofilm formation inhibitors were performed and a new N-(oxazolylmethyl)-thiazolidinedione scaffold was constructed. 16 new compounds were synthesized and characterized in order to confirm their proposed structures. A general antimicrobial screening against Gram-positive and Gram-negative bacteria, as well as fungi, was performed and revealed that the compounds do not have direct antimicrobial activity. The anti-biofilm activity evaluation confirmed the compounds act as selective inhibitors of C. albicans biofilm formation. In an effort to substantiate this biologic profile, we used in silico investigations which suggest that the compounds could act by binding, and thus obstructing the functions of, the C. albicans Als surface proteins, especially Als1, Als3, Als5 and Als6. Considering the well documented role of Als1 and Als3 in biofilm formation, our new class of compounds that target these proteins could represent a new approach in C. albicans infection prevention and management.


2014 ◽  
Vol 22 (4) ◽  
pp. 1313-1317 ◽  
Author(s):  
Sijie Yang ◽  
Osama A. Abdel-Razek ◽  
Fei Cheng ◽  
Debjyoti Bandyopadhyay ◽  
Gauri S. Shetye ◽  
...  

Diagnostics ◽  
2021 ◽  
Vol 11 (10) ◽  
pp. 1746
Author(s):  
Cassandra Pouget ◽  
Catherine Dunyach-Remy ◽  
Alix Pantel ◽  
Sophie Schuldiner ◽  
Albert Sotto ◽  
...  

The polymicrobial nature of biofilms and bacterial interactions inside chronic wounds are keys for the understanding of bacterial cooperation. The aim of this present study was to develop a technique to study and visualize biofilm in live imaging under flow conditions (Bioflux™ 200, Fluxion Biosciences). The BiofluxTM system was adapted using an in vitro chronic wound-like medium (CWM) that mimics the environment encountered in ulcers. Two reference strains of Staphylococcus aureus (Newman) and Pseudomonas aeruginosa (PAO1) were injected in the BiofluxTM during 24 h to 72 h in mono and coculture (ratio 1:1, bacteria added simultaneously) in the CWM vs. a control medium (BHI). The quantification of biofilm formation at each time was evaluated by inverted microscopy. After 72 h, different antibiotics (ceftazidime, imipenem, linezolid, oxacillin and vancomycin) at 1x MIC, 10x MIC and 100x MIC were administrated to the system after an automatic increase of the flow that mimicked a debridement of the wound surface. Biofilm studies highlighted that the two species, alone or associated, constituted a faster and thicker biofilm in the CWM compared to the BHI medium. The effect of antibiotics on mature or “debrided” biofilm indicated that some of the most clinically used antibiotic such as vancomycin or imipenem were not able to disrupt and reduce the biofilm biomass. The use of a life cell imaging with an in vitro CWM represents a promising tool to study bacterial biofilm and investigate microbial cooperation in a chronic wound context.


Biofouling ◽  
2019 ◽  
Vol 35 (7) ◽  
pp. 742-757
Author(s):  
Laura Marise de Freitas ◽  
Esteban Nicolás Lorenzón ◽  
Eduardo Maffud Cilli ◽  
Kleber Thiago de Oliveira ◽  
Carla Raquel Fontana ◽  
...  

Marine Drugs ◽  
2018 ◽  
Vol 16 (8) ◽  
pp. 274 ◽  
Author(s):  
Anna Carbone ◽  
Barbara Parrino ◽  
Maria Cusimano ◽  
Virginia Spanò ◽  
Alessandra Montalbano ◽  
...  

New thiazole nortopsentin analogues were conveniently synthesized and evaluated for their activity as inhibitors of biofilm formation of relevant Gram-positive and Gram-negative pathogens. All compounds were able to interfere with the first step of biofilm formation in a dose-dependent manner, showing a selectivity against the staphylococcal strains. The most active derivatives elicited IC50 values against Staphylococcus aureus ATCC 25923, ranging from 0.40–2.03 µM. The new compounds showed a typical anti-virulence profile, being able to inhibit the biofilm formation without affecting the microbial growth in the planktonic form.


Molecules ◽  
2019 ◽  
Vol 24 (1) ◽  
pp. 208 ◽  
Author(s):  
Decha Kumla ◽  
Tida Dethoup ◽  
Luís Gales ◽  
José A. Pereira ◽  
Joana Freitas-Silva ◽  
...  

A new polyketide erubescensoic acid (1), and the previously reported xanthonopyrone, SPF-3059-26 (2), were isolated from the uninvestigated fractions of the ethyl acetate crude extract of the marine sponge-associated fungus Penicillium erubescens KUFA0220. The structures of the new compound, erubescensoic acid (1), and the previously reported SPF-3059-26 (2), were elucidated by extensive analysis of 1D and 2D-NMR spectra as well as HRMS. The absolute configuration of the stereogenic carbon of erubescensoic acid (1) was determined by X-ray analysis. Erubescensoic acid (1) and SPF-3059-26 (2), together with erubescenschromone B (3), penialidin D (4), and 7-hydroxy-6-methoxy-4-oxo-3-[(1E)-3-oxobut-1-en-1-yl]-4H-chromen-5-carboxylic acid (5), recently isolated from this fungus, were assayed for their antibacterial activity against gram-positive and gram-negative reference strains and the multidrug-resistant (MDR) strains from the environment. The capacity of these compounds to interfere with the bacterial biofilm formation and their potential synergism with clinically relevant antibiotics for the MDR strains were also investigated.


Molecules ◽  
2020 ◽  
Vol 25 (2) ◽  
pp. 383 ◽  
Author(s):  
Maria Grazia Cusimano ◽  
Vita Di Stefano ◽  
Maria La Giglia ◽  
Vincenzo Di Marco Lo Presti ◽  
Domenico Schillaci ◽  
...  

The main objective of this study was to evaluate the efficacy of thymol in controlling environmental contamination in food processing facilities. The effect of thymol was tested as an agent to prevent planktonic and bacterial biofilm growth of twenty-five Listeria monocytogenes isolates from a variety of foods and five Escherichia coli isolates from a farm. The E. coli isolates were positive for extended spectrum β-lactamase (ESBL) genes. All isolates and reference strains were susceptible to thymol at Minimum inhibitory concentration (MIC) values ranging from 250 to 800 μg/mL. An interesting activity of interference with biofilm formation of L. monocytogenes and E. coli was found for thymol at sub-MIC concentrations of 200, 100, 75, and 50 μg/mL. Anti-biofilm activity ranging from 59.71% to 66.90% against pre-formed 24-h-old L. monocytogenes biofilms at concentrations of 500 or 800 µg/mL, corresponding to 2× MIC, was determined against free-living forms of six isolates chosen as the best or moderate biofilm producers among the tested strains. The property of thymol to attack L. monocytogenes biofilm formation was also observed at a concentration of 100 µg/mL, corresponding to 1/4 MIC, by using a stainless-steel model to simulate the surfaces in food industries. This study gives information on the use of thymol in food processing setting.


Author(s):  
R. Banda ◽  
J. Nduko ◽  
J. Matofari

Background: Some microorganisms can adhere to food handling surfaces forming biofilms that pose a safety challenge. This study was done to evaluate bacterial biofilm formation in milking equipments in Lilongwe, Malawi. Methods: Pooled milk (n=54) and water (n=60) samples were collected from households and milk bulking groups in Lilongwe, Malawi. Swabbing (n=46) and rinsing (n=16) were done on milk handling containers after cleaning. Biofilm determination on the containers was done by detecting biofilm indicator bacteria, including Bacillus spp., Salmonella spp., and Pseudomonas spp. The strength of biofilm was determined by the tube method. Data were analyzed by SAS software version 9.1.3.   Results: Prevalence rates of Gram-negative rods were significantly (p<0.05) higher than the Gram-positive rods and the Gram-positive cocci. Of the 176 cases, contamination rates were 36 (20.4%), 32 (18.2%), and 18 (10.2%) for Salmonella spp., Bacillus spp., and Pseudomonas spp., respectively. The biofilm indicator organisms were significantly (p<0.05) more prevalent in dairy farmer households compared with the milk bulking centers. Fourteen out of 86 (16.3%) microbial isolates formed strong/high biofilms, whereas 18 out of 86 (20.93%) of isolates did not form any biofilm. The rate of isolates forming strong/high biofilms in households (17.6%) was significantly (p<0.05) higher than that of milk bulking centers (11.1%). Conclusion: Biofilm formation on milk handling container surfaces in Lilongwe, Malawi could serve as a source of microbial pathogens and spoilage organisms.


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