RESUMEN
OBJECTIVES: The mannose phosphotransferase system (Man-PTS) plays crucial roles in the adaptive metabolic activity of Enterococcus faecalis (E. faecalis) in adverse environments. The aim of this study was to evaluate the role of Man-PTS in the alkaline resistance of E. faecalis against calcium hydroxide (CH) and the effect of metformin (Met) on the alkaline resistance of E. faecalis to CH. MATERIALS AND METHODS: The regulatory role of Man-PTS EII in the alkaline resistance of E. faecalis was firstly investigated using a wild-type highly alkaline-resistant E. faecalis XS 003, standard ATCC 29212 and Man-PTS EIID gene deficient (â³mptD) and overexpressing (+mptD) strains of E. faecalis. RNA sequencing of Met-treated E. faecalis was performed to further validate the effect of Met on Man-PTS. The effect of Met on CH resistance of E. faecalis was verified by evaluating the survival, membrane potential and permeability, intracellular pH and ATP, and the expression of Man-PTS EII and membrane transporter-related genes of E. faecalis. The effect of Met on the ability of CH to remove E. faecalis biofilm on the dentin surface was also tested. The in vivo therapeutic effect of Met plus CH (CHM) was further investigated in a rat apical periodontitis model induced by E. faecalis XS 003. RESULTS: Man-PTS EII significantly promoted the survival ability of E. faecalis in CH and enhanced its resistance to CH. The inhibition of Man-PTS EII by Met resulted in reduced alkaline resistance of E. faecalis in the presence of CH, while also enhancing the antimicrobial properties of CH against E. faecalis biofilm on dentin. Additionally, Met plus CH showed the synergistically promoted intra-canal E. faecalis infection control and healing of periapical lesion in rats. CONCLUSIONS: Met could significantly reduce the alkaline resistance of E. faecalis against CH through the modulation of Man-PTS EII, and improved the antibacterial effect of CH against E. faecalis infection both in vitro and in vivo. CLINICAL RELEVANCE: Met could significantly enhance the ability of CH to control E. faecalis infection through reducing the alkaline resistance of E. faecalis.
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Hidróxido de Calcio , Enterococcus faecalis , Metformina , Enterococcus faecalis/efectos de los fármacos , Animales , Ratas , Metformina/farmacología , Hidróxido de Calcio/farmacología , Biopelículas/efectos de los fármacos , Técnicas In Vitro , Modelos Animales de Enfermedad , Farmacorresistencia Bacteriana , Masculino , Ratas Sprague-Dawley , Antibacterianos/farmacología , Irrigantes del Conducto Radicular/farmacologíaRESUMEN
Background: Polymeric denture materials can be susceptible to colonization by oral microorganisms. Zein-coated magnesium oxide nanoparticles (zMgO NPs) demonstrate antimicrobial activity. The aim of this study was to investigate the antimicrobial effect and adherence of different oral microorganisms on hybrid polymeric denture materials incorporated with zMgO NPs. Methods: Five types of polymeric denture materials were used. A total of 480 disc-shaped specimens were divided by material type (n=96/grp), then subdivided by zMgO NPs concentration: control with no nanoparticles and other groups with zMgO NPs concentrations of 0.3%, 0.5% and 1% by weight. Characterization of the polymeric denture materials incorporating zMgO NPs was done, and the antimicrobial activity of all groups was tested against four types of microorganisms: 1) Streptococcus mutans, 2) Staphylococcus aureus, 3) Enterococcus faecalis and 4) Candida albicans. The samples underwent an adherence test and an agar diffusion test. Experiments were done in triplicates. Results: The characterization of the hybrid samples revealed variation in the molecular composition, as well as a uniform distribution of the zMgO NPs in the polymeric denture materials. All hybrid polymeric denture materials groups induced a statistically significant antimicrobial activity, while the control groups showed the least antimicrobial activity. The agar diffusion test revealed no release of the zMgO NPs from the hybrid samples, indicating the NPs did not seep out of the matrix. Conclusion: The zMgO NPs were effective in reducing the adherence of the tested microorganisms and enhancing the antimicrobial activity of the polymeric denture materials. This antimicrobial effect with the polymeric dentures could aid in resisting microbial issues such as denture stomatitis.
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Antiinfecciosos , Candida albicans , Staphylococcus aureus , Streptococcus mutans , Zeína , Zeína/química , Zeína/farmacología , Candida albicans/efectos de los fármacos , Streptococcus mutans/efectos de los fármacos , Staphylococcus aureus/efectos de los fármacos , Antiinfecciosos/farmacología , Antiinfecciosos/química , Óxido de Magnesio/química , Óxido de Magnesio/farmacología , Nanopartículas/química , Enterococcus faecalis/efectos de los fármacos , Pruebas de Sensibilidad Microbiana , Humanos , Materiales Dentales/farmacología , Materiales Dentales/química , Dentaduras/microbiología , Polímeros/química , Polímeros/farmacologíaRESUMEN
We developed a synthesis strategy involving a diazo transfer reaction and subsequent click reaction to conjugate a murine cathelicidin-related antimicrobial peptide (CRAMP18-35) to chitosan and hydroxypropyl chitosan (HPC), confirmed the structure, and investigated the antimicrobial activity. Chitosan azide and HPC-azide were prepared with a low degree of azidation by reacting the parent chitosan and HPC with imidazole sulfonyl azide hydrochloride. CRAMP18-35 carrying an N-terminal pentynoyl group was successfully grafted onto chitosan and HPC via copper-catalyzed azide-alkyne cycloaddition (CuAAC) reaction. The chitosan-peptide conjugates were characterized by IR spectroscopy and proton NMR to confirm the conversion of the azide to 1,2,3-triazole and to determine the degree of substitution (DS). The DS of the chitosan and HPC CRAMP18-35 conjugates was 0.20 and 0.13, respectively. The antibacterial activity of chitosan-peptide conjugates was evaluated for activity against two species of Gram-positive bacteria, Staphylococcus aureus (S. aureus) and Enterococcus faecalis (E. faecalis), and two species of Gram-negative bacteria, Escherichia coli (E. coli) and Pseudomonas aeruginosa (P. aeruginosa). The antimicrobial peptide conjugates were selectively active against the Gram-negative bacteria and lacking activity against Gram-positive bacteria.
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Alquinos , Antibacterianos , Azidas , Quitosano , Cobre , Reacción de Cicloadición , Pruebas de Sensibilidad Microbiana , Quitosano/química , Quitosano/análogos & derivados , Quitosano/farmacología , Antibacterianos/farmacología , Antibacterianos/química , Antibacterianos/síntesis química , Cobre/química , Azidas/química , Catálisis , Alquinos/química , Péptidos Catiónicos Antimicrobianos/química , Péptidos Catiónicos Antimicrobianos/farmacología , Catelicidinas , Animales , Staphylococcus aureus/efectos de los fármacos , Ratones , Enterococcus faecalis/efectos de los fármacos , Enterococcus faecalis/crecimiento & desarrolloRESUMEN
A series of new unique acetylene derivatives of 8-hydroxy- and 8-methoxyquinoline- 5-sulfonamide 3a-f and 6a-f were prepared by reactions of 8-hydroxy- and 8-methoxyquinoline- 5-sulfonyl chlorides with acetylene derivatives of amine. A series of new hybrid systems containing quinoline and 1,2,3-triazole systems 7a-h were obtained by reactions of acetylene derivatives of quinoline-5-sulfonamide 6a-d with organic azides. The structures of the obtained compounds were confirmed by 1H and 13C NMR spectroscopy and HR-MS spectrometry. The obtained quinoline derivatives 3a-f and 6a-f and 1,2,3-triazole derivatives 7a-h were tested for their anticancer and antimicrobial activity. Human amelanotic melanoma cells (C-32), human breast adenocarcinoma cells (MDA-MB-231), and human lung adenocarcinoma cells (A549) were selected as tested cancer lines, while cytotoxicity was investigated on normal human dermal fibroblasts (HFF-1). All the compounds were also tested against reference strains Staphylococcus aureus ATCC 29213 and Enterococcus faecalis ATCC 29212 and representatives of multidrug-resistant clinical isolates of methicillin-resistant S. aureus (MRSA) and vancomycin-resistant E. faecalis. Only the acetylene derivatives of 8-hydroxyquinoline-5-sulfonamide 3a-f were shown to be biologically active, and 8-hydroxy-N-methyl-N-(prop-2-yn-1-yl)quinoline-5-sulfonamide (3c) showed the highest activity against all three cancer lines and MRSA isolates. Its efficacies were comparable to those of cisplatin/doxorubicin and oxacillin/ciprofloxacin. In the non-cancer HFF-1 line, the compound showed no toxicity up to an IC50 of 100 µM. In additional tests, compound 3c decreased the expression of H3, increased the transcriptional activity of cell cycle regulators (P53 and P21 proteins), and altered the expression of BCL-2 and BAX genes in all cancer lines. The unsubstituted phenolic group at position 8 of the quinoline is the key structural fragment necessary for biological activity.
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Antibacterianos , Antineoplásicos , Pruebas de Sensibilidad Microbiana , Quinolinas , Sulfonamidas , Humanos , Antineoplásicos/farmacología , Antineoplásicos/química , Antineoplásicos/síntesis química , Antibacterianos/farmacología , Antibacterianos/química , Antibacterianos/síntesis química , Sulfonamidas/farmacología , Sulfonamidas/química , Sulfonamidas/síntesis química , Línea Celular Tumoral , Quinolinas/química , Quinolinas/farmacología , Quinolinas/síntesis química , Diseño de Fármacos , Relación Estructura-Actividad , Staphylococcus aureus/efectos de los fármacos , Enterococcus faecalis/efectos de los fármacos , Estructura MolecularRESUMEN
In this work, we describe an improved series of N-phenylpyrrolamide inhibitors that exhibit potent activity against DNA gyrase and are highly effective against high-priority gram-positive bacteria. The most potent compounds show low nanomolar IC50 values against Escherichia coli DNA gyrase, and in addition, compound 7c also inhibits E. coli topoisomerase IV in the nanomolar concentration range, making it a promising candidate for the development of potent dual inhibitors for these enzymes. All tested compounds show high selectivity towards the human isoform DNA topoisomerase IIα. Compounds 6a, 6d, 6e and 6f show MIC values between 0.031 and 0.0625 µg/mL against vancomycin-intermediate S. aureus (VISA) and Enterococcus faecalis strains. Compound 6g shows an inhibitory effect against the methicillin-resistant S. aureus strain (MRSA) with a MIC of 0.0625 µg/mL and against the E. faecalis strain with a MIC of 0.125 µg/mL. In a time-kill assay, compound 6d showed a dose-dependent bactericidal effect on the MRSA strain and achieved bactericidal activity at 8 × MIC after 8 h. The duration of the post-antibiotic effect (PAE) on the MRSA strain for compound 6d was 2 h, which corresponds to the PAE duration for ciprofloxacin. The compounds were not cytotoxic at effective concentrations, as determined in an MTS assay on the MCF-7 breast cancer cell line.
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Antibacterianos , Girasa de ADN , Relación Dosis-Respuesta a Droga , Pruebas de Sensibilidad Microbiana , Inhibidores de Topoisomerasa II , Antibacterianos/farmacología , Antibacterianos/química , Antibacterianos/síntesis química , Humanos , Inhibidores de Topoisomerasa II/farmacología , Inhibidores de Topoisomerasa II/química , Inhibidores de Topoisomerasa II/síntesis química , Girasa de ADN/metabolismo , Relación Estructura-Actividad , Estructura Molecular , Enterococcus faecalis/efectos de los fármacos , Pirroles/farmacología , Pirroles/química , Pirroles/síntesis química , Amidas/farmacología , Amidas/química , Amidas/síntesis química , Escherichia coli/efectos de los fármacos , Staphylococcus aureus Resistente a Meticilina/efectos de los fármacos , Staphylococcus aureus/efectos de los fármacosRESUMEN
The treatment of infections caused by biofilm-forming organisms is challenging. The newly discovered antibiotic teixobactin shows activity against a wide range of biofilm-forming bacteria. However, the laborious and low-yield chemical synthesis of teixobactin complicates its further development for clinical application. The use of more easily synthesized teixobactin analogues may offer promise in this regard. In this article, three newly developed analogues were tested for efficacy against Staphylococcus aureus and Enterococcus faecalis. Minimum inhibitory and -bactericidal concentrations were investigated. MIC values for S. aureus and E. faecalis ranged from 0.5-2 and 2-4 µg/mL, respectively. Moreover, the ability of the analogues to prevent biofilm formation and to inactivate bacterial cells in already established S. aureus biofilm on medical grade materials (PVC and PTFE) used in the production of infusion tubing and catheters were also tested. The analogues showed an ability to prevent biofilm formation and inactivate bacterial cells in established biofilms at concentrations as low as 1-2 µg/mL. Confocal laser scanning microscopy showed that the most promising analogue (TB3) inactivated S. aureus cells in a preformed biofilm and gave a reduction in biovolume. The relative ease of synthesis of the analogues and their in vitro efficacy, makes them promising candidates for pharmaceutical development.
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Antibacterianos , Biopelículas , Depsipéptidos , Enterococcus faecalis , Pruebas de Sensibilidad Microbiana , Staphylococcus aureus , Biopelículas/efectos de los fármacos , Enterococcus faecalis/efectos de los fármacos , Enterococcus faecalis/fisiología , Enterococcus faecalis/crecimiento & desarrollo , Staphylococcus aureus/efectos de los fármacos , Staphylococcus aureus/fisiología , Antibacterianos/farmacología , Antibacterianos/química , Depsipéptidos/farmacología , Depsipéptidos/químicaRESUMEN
PURPOSE: To evaluate the antimicrobial effect of a new active oxygen fluid (Blue®m) as a root canal irrigant against Enterococcus faecalis compared to sodium hypochlorite (NaOCl). MATERIAL AND METHODS: Forty-five extracted single-canaled human teeth were selected, received root canal preparation, autoclaved, and contaminated with Enterococcus faecalis. The specimens were randomly allocated into three groups: Group (A) served as the negative control, receiving irrigation with saline (n = 15); Group (B) was irrigated with 5.25% NaOCl (n = 15); and Group (C) was irrigated with 10 mL of Blue®m (n = 15). Microbial sampling from the root canals was performed before and after irrigation. The difference between the pre-irrigation and post-irrigation colony-forming units (CFU/mL) was calculated. The data was analysed using a one-way ANOVA followed by post-hoc Tukey tests. The significance level was set at 5%. RESULTS: Blue®m statistically significantly reduced the bacterial load compared to saline (p = 0.009), but NaOCl was most effective, outperforming both (p 0.0001). CONCLUSION: Irrigation with Blue®m demonstrated antibacterial efficacy against Enterococcus faecalis, but it was not as effective as NaOCl.
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Cavidad Pulpar , Enterococcus faecalis , Irrigantes del Conducto Radicular , Hipoclorito de Sodio , Enterococcus faecalis/efectos de los fármacos , Humanos , Irrigantes del Conducto Radicular/farmacología , Hipoclorito de Sodio/farmacología , Cavidad Pulpar/microbiología , Carga Bacteriana/efectos de los fármacos , Preparación del Conducto Radicular/métodos , Ensayo de Materiales , Recuento de Colonia MicrobianaRESUMEN
Microalgae are of great interest due to their ability to produce valuable compounds, such as pigments, omega-3 fatty acids, antioxidants, and antimicrobials. The dinoflagellate genus Amphidinium is particularly notable for its amphidinol-like compounds, which exhibit antibacterial and antifungal properties. This study utilized a two-stage cultivation method to grow Amphidinium carterae CCAP 1102/8 under varying conditions, such as blue LED light, increased salinity, and the addition of sodium carbonate or hydrogen peroxide. After cultivation, the biomass was extracted and fractionated using solid-phase extraction, yielding six fractions per treatment. These fractions were analyzed using Liquid Chromatography-High-Resolution Mass Spectrometry (LC-HRMS/MS) to identify their chemical components. Key amphidinol compounds (AM-B, AM-C, AM-22, and AM-A) were identified, with AM-B being the most abundant in Fraction 4, followed by AM-C. Fraction 5 also contained a significant amount of AM-C along with an unknown compound. Fraction 4 returned the highest antimicrobial activity against the pathogens Staphylococcus aureus, Enterococcus faecalis, and Candida albicans, with Minimal Biocidal Concentrations (MBCs) ranging from 1 to 512 µg/mL. Results indicate that the modulation of both amphidinol profile and fraction bioactivity can be induced by adjusting the cultivation parameters used to grow two-stage batch cultures of A. carterae.
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Candida albicans , Dinoflagelados , Pruebas de Sensibilidad Microbiana , Dinoflagelados/química , Dinoflagelados/crecimiento & desarrollo , Dinoflagelados/efectos de los fármacos , Candida albicans/efectos de los fármacos , Candida albicans/crecimiento & desarrollo , Antibacterianos/farmacología , Antibacterianos/química , Enterococcus faecalis/efectos de los fármacos , Enterococcus faecalis/crecimiento & desarrollo , Staphylococcus aureus/efectos de los fármacos , Staphylococcus aureus/crecimiento & desarrollo , Cromatografía Liquida , Antifúngicos/farmacología , Antifúngicos/química , Antiinfecciosos/farmacología , Antiinfecciosos/química , AnfidinolesRESUMEN
BACKGROUND AND OBJECTIVES: Mineral Trioxide Aggregate (MTA) is one of the main retrograde filling materials that is used today as a root end filling material and perforation repair material. This study was conducted with the aim of investigating the antibacterial and antifungal properties of four types of bio-ceramic materials, AGM MTA, Ortho MTA, Pro root MTA and Cem cement for oral and dental health. METHODS: In this study, the antibacterial activity of four types of bio-ceramic materials against two bacterial strains of Enterococcus faecalis (ATTC 29212), Escherichia coli (ATTC 35318) and antifungal activity against Candida albicans (ATTC 10231) were investigated using the well diffusion method. RESULTS: In the context of the relationship between the type of microorganism and the diameter of the growth inhibitory zone for each type of bio-ceramic material, there was no significant difference for Enterococcus faecalis, and a significant difference was observed for Escherichia coli and Candida albicans (p < 0.05). CONCLUSION: The results show that each of the bio-ceramic materials AGM, Pro root, Cem cement and Ortho have antibacterial and antifungal properties. AGM MTA bio-ceramic material on Candida albicans fungus and Ortho MTA bio-ceramic material had the most effect on Escherichia coli bacteria. Therefore, the mentioned bio-ceramic materials can play a significant role in oral and dental health by providing a suitable material for restoration.
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Compuestos de Aluminio , Compuestos de Calcio , Candida albicans , Cerámica , Combinación de Medicamentos , Enterococcus faecalis , Escherichia coli , Óxidos , Materiales de Obturación del Conducto Radicular , Silicatos , Compuestos de Calcio/farmacología , Silicatos/farmacología , Candida albicans/efectos de los fármacos , Enterococcus faecalis/efectos de los fármacos , Óxidos/farmacología , Compuestos de Aluminio/farmacología , Escherichia coli/efectos de los fármacos , Materiales de Obturación del Conducto Radicular/farmacología , Humanos , Cementos Dentales/farmacología , Antibacterianos/farmacología , Ensayo de Materiales , Antifúngicos/farmacologíaRESUMEN
The aim of this work was to provide a theoretical and scientific basis for the treatment, prevention, and control of clinical drug-resistant bacterial infections by studying the molecular epidemiology and horizontal transfer mechanism of optrA-carrying linezolid-resistant Enterococcus faecalis strains (LREfs) that were clinically isolated in a tertiary hospital in Kunming, China. Non-repetitive LREfs retained in a tertiary A hospital in Kunming, China. The strains were identified by Matrix-assisted laser desorption/ionization time-of-flight mass spectrometry (MALDI-TOF MS). The transferability and horizontal transfer mechanism of optrA gene were analyzed using polymerase chain reaction (PCR), whole-genome sequencing (WGS), and conjugation experiments. A total of 39 LREfs strains were collected, and all of them were multi-drug resistant. There were 30 LREfs strains (76.9%) carrying the optrA gene, The cfr, poxtA genes and mutations in the 23S rRNA gene were not detected. The conjugation experiments showed that only three of 10 randomly selected optrA-carrying LREfs were successfully conjugated with JH2-2. Further analysis of one successfully conjugated strain revealed that the optrA gene, located in the donor bacterium, formed the IS1216E-erm(A)-optrA-fexA-IS1216E transferable fragment under the mediation of the mobile genetic element (MGE) IS1216E, which was then transferred to the recipient bacterium via horizontal plasmid transfer. Carrying the optrA gene is the primary resistance mechanism of LREfs strains. The optrA gene could carry the erm(A) and fexA genes to co-transfer among E. faecalis. MGEs such as insertion sequence IS1216E play an important role in the horizontal transfer of the optrA gene.
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Antibacterianos , Enterococcus faecalis , Transferencia de Gen Horizontal , Infecciones por Bacterias Grampositivas , Linezolid , Enterococcus faecalis/genética , Enterococcus faecalis/efectos de los fármacos , Linezolid/farmacología , Antibacterianos/farmacología , Humanos , Infecciones por Bacterias Grampositivas/microbiología , Infecciones por Bacterias Grampositivas/epidemiología , China/epidemiología , Proteínas Bacterianas/genética , Proteínas Bacterianas/metabolismo , Epidemiología Molecular , Farmacorresistencia Bacteriana/genética , Pruebas de Sensibilidad Microbiana , Farmacorresistencia Bacteriana Múltiple/genética , Secuenciación Completa del Genoma , Conjugación GenéticaRESUMEN
BACKGROUND: Glycopeptides for ampicillin-susceptible Enterococcus faecalis/faecium bacteremia are readily prescribed depending on the severity of the condition. However, there is limited data on the outcomes of glycopeptide use compared to ampicillin-containing regimens for ampicillin-susceptible E. faecalis/faecium bacteremia. From an antibiotic stewardship perspective, it is important to determine whether the use of glycopeptides is associated with improved clinical outcomes in patients with ampicillin-susceptible E. faecalis/faecium bacteremia. METHODS: This retrospective cohort study was conducted at a university-affiliated hospital between January 2010 and September 2019. We collected data from patients with positive blood cultures for Enterococcus species isolates. The clinical data of patients who received ampicillin-containing regimens or glycopeptides as definitive therapy for ampicillin-susceptible E. faecalis/faecium bacteremia were reviewed. Multivariate logistic regression analysis was performed to identify risk factors for 28-day mortality. RESULTS: Ampicillin-susceptible E. faecalis/faecium accounted for 41.2% (557/1,353) of enterococcal bacteremia cases during the study period. A total of 127 patients who received ampicillin-containing regimens (N = 56) or glycopeptides (N = 71) as definitive therapy were included in the analysis. The 28-day mortality rate was higher in patients treated with glycopeptides (19.7%) than in those treated with ampicillin-containing regimens (3.6%) (p = 0.006). However, in the multivariate model, antibiotic choice was not an independent predictor of 28-day mortality (adjusted OR, 3.7; 95% CI, 0.6-23.6). CONCLUSIONS: Glycopeptide use was not associated with improved mortality in patients with ampicillin-susceptible E. faecalis/faecium bacteremia. This study provides insights to reduce the inappropriate use of glycopeptides in ampicillin-susceptible E. faecalis/faecium bacteremia treatment and promote antimicrobial stewardship.
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Ampicilina , Antibacterianos , Bacteriemia , Enterococcus faecalis , Glicopéptidos , Infecciones por Bacterias Grampositivas , Sulbactam , Humanos , Estudios Retrospectivos , Bacteriemia/tratamiento farmacológico , Bacteriemia/microbiología , Bacteriemia/mortalidad , Ampicilina/uso terapéutico , Ampicilina/farmacología , Masculino , Femenino , Antibacterianos/farmacología , Antibacterianos/uso terapéutico , Enterococcus faecalis/efectos de los fármacos , Infecciones por Bacterias Grampositivas/tratamiento farmacológico , Infecciones por Bacterias Grampositivas/microbiología , Infecciones por Bacterias Grampositivas/mortalidad , Anciano , Persona de Mediana Edad , Glicopéptidos/uso terapéutico , Glicopéptidos/farmacología , Sulbactam/uso terapéutico , Sulbactam/farmacología , Resultado del Tratamiento , Pruebas de Sensibilidad Microbiana , Anciano de 80 o más AñosRESUMEN
Two new compounds, macrolactin XY (1) and (5R, 9S, 10S)-5-(hydroxymethyl)-1,3,7-decatriene-9,10-diol (2), together with nine known compounds (3-11) were isolated from the marine Bacillus subtilis sp. 18 by the OSMAC strategy. These compounds were evaluated for antibacterial activity against six tested microorganisms. Compounds 1-5 and 7-10 showed varied antibacterial activity, with the minimum inhibitory concentration (MIC) ranging from 3 to 12 µg/mL. Macrolactin XY (1) was found to possess superior antibacterial activity, especially exhibiting significant effectiveness against Enterococcus faecalis. The antibacterial activity mechanism against E. faecalis was investigated. The mechanism may disrupt bacterial cell membrane integrity and permeability, and also inhibit the expression of genes associated with bacterial energy metabolism, as established by the experiments concerning cell membrane potential, SDS-PAGE electrophoresis, cell membrane integrity, and key gene expressions. This study offers valuable insights and serves as a theoretical foundation for the future development of macrolactins as antibacterial precursors.
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Antibacterianos , Bacillus subtilis , Macrólidos , Pruebas de Sensibilidad Microbiana , Bacillus subtilis/efectos de los fármacos , Antibacterianos/farmacología , Antibacterianos/aislamiento & purificación , Antibacterianos/química , Macrólidos/farmacología , Macrólidos/aislamiento & purificación , Macrólidos/química , Enterococcus faecalis/efectos de los fármacos , Organismos Acuáticos , Membrana Celular/efectos de los fármacosRESUMEN
BACKGROUND: Due to the increasing emergence of antibiotic resistance in Enterococcus faecalis (E. faecalis), it indicated as potentially opportunistic pathogen causing various healthcare-associated and life-threatening diseases around the world. OBJECTIVE: The aim of this meta-analysis was to evaluate the weighted pooled resistance rates in clinical E. faecalis isolates based on over time, areas, antimicrobial susceptibility testing (AST), and infection source. METHODS: We searched the studies in PubMed, Scopus, and Web of Science (November 30, 2022). All statistical analyses were carried out using the statistical package R. RESULTS: The analysis encompassed a total of 74 studies conducted in 28 countries. According to the meta-regression, the chloramphenicol, fosfomycin, imipenem, linezolid, minocycline, norfloxacin, quinupristin-dalfopristin, and tetracycline resistance rate increased over time. Analysis revealed statistically significant differences in antibiotic resistance rates for ampicillin, chloramphenicol, erythromycin, gentamicin, penicillin, rifampicin, teicoplanin, tetracycline, and vancomycin across various countries. CONCLUSIONS: Globally, the prevalence of drug resistant E. faecalis strains are on the increase over time. Daptomycin and tigecycline can be an effective agent for the treatment of clinical E. faecalis infections. Considering the low prevalence of antibiotic resistance in continents of Europe and Australia, it is suggested to take advantage of their preventive strategies in order to obtain efficient results in other places with high prevalence of resistance.
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Antibacterianos , Enterococcus faecalis , Infecciones por Bacterias Grampositivas , Pruebas de Sensibilidad Microbiana , Enterococcus faecalis/efectos de los fármacos , Humanos , Antibacterianos/farmacología , Infecciones por Bacterias Grampositivas/microbiología , Infecciones por Bacterias Grampositivas/tratamiento farmacológico , Infecciones por Bacterias Grampositivas/epidemiología , Farmacorresistencia Bacteriana , Salud Global , Farmacorresistencia Bacteriana MúltipleRESUMEN
This study presents the empirical findings of an in-depth genomic analysis of Enterococcus faecalis and Enterococcus lactis isolates from South Africa. It offers valuable insights into their genetic characteristics and their significant implications for public health. The study uncovers nuanced variations in the gene content of these isolates, despite their similar GC contents, providing a comprehensive view of the evolutionary diversity within the species. Genomic islands are identified, particularly in E. faecalis, emphasizing its propensity for horizontal gene transfer and genetic diversity, especially in terms of antibiotic resistance genes. Pangenome analysis reveals the existence of a core genome, accounting for a modest proportion of the total genes, with 2157 core genes, 1164 shell genes, and 4638 cloud genes out of 7959 genes in 52 South African E. faecalis genomes (2 from this study, 49 south Africa genomes downloaded from NCBI, and E. faecalis reference genome). Detecting large-scale genomic rearrangements, including chromosomal inversions, underscores the dynamic nature of bacterial genomes and their role in generating genetic diversity. The study uncovers an array of antibiotic resistance genes, with trimethoprim, tetracycline, glycopeptide, and multidrug resistance genes prevalent, raising concerns about the effectiveness of antibiotic treatment. Virulence gene profiling unveils a diverse repertoire of factors contributing to pathogenicity, encompassing adhesion, biofilm formation, stress resistance, and tissue damage. These empirical findings provide indispensable insights into these bacteria's genomic dynamics, antibiotic resistance mechanisms, and virulence potential, underlining the pressing need to address antibiotic resistance and implement robust control measures.
Asunto(s)
Antibacterianos , Enterococcus faecalis , Variación Genética , Genoma Bacteriano , Factores de Virulencia , Sudáfrica , Enterococcus faecalis/genética , Enterococcus faecalis/efectos de los fármacos , Enterococcus faecalis/patogenicidad , Enterococcus faecalis/aislamiento & purificación , Virulencia/genética , Antibacterianos/farmacología , Factores de Virulencia/genética , Humanos , Farmacorresistencia Bacteriana/genética , Islas Genómicas/genética , Infecciones por Bacterias Grampositivas/microbiología , Enterococcus/genética , Enterococcus/efectos de los fármacos , Enterococcus/patogenicidad , Enterococcus/aislamiento & purificación , Enterococcus/clasificación , Filogenia , Transferencia de Gen Horizontal , Genómica , Pruebas de Sensibilidad MicrobianaRESUMEN
OBJECTIVES: Considering the correlation between survival microenvironment of E. faecalis and acidic pH value, this study aimed to investigate the potential of utilizing pH-responsive DMAEM monomers and their copolymers with resin-based root canal sealers to inhibit E. faecalis. METHODS: Broth microdilution assay, crystal violet staining and qPCR were performed to evaluate antibacterial effects of DMAEM monomers against E. faecalis at different pH. Methacrylate-resin based root canal sealers were prepared and copolymerized with DMAEM. The flow, solubility, water sorption, apical sealing ability and cytotoxicity of sealers were investigated to optimize formulation. The anti-E. faecalis effects of DMAEM copolymers with sealers were evaluated by direct contact test, colony-forming unit counting and live/dead staining. RESULTS: DMAEM monomers inhibited the growth, biofilm formation and virulence factors expression of E. faecalis in a concentration- and pH-dependent manner. Incorporation of 1.25 % and 2.5 % DMAEM into experimental sealers would not affect the flowability, solubility and periapical sealing ability (P > 0.05), but increased the water sorption of sealers (P < 0.01). Cells viability was higher than 90 % in both 1.25 % and 2.5 % DMAEM groups at pH 7.0. DMAEM copolymers with sealers reduced E. faecalis counts, inhibited biofilm formation and decreased live cells within the biofilm in response to pH values. SIGNIFICANCE: DMAEM monomers and their copolymers with resin-based sealers possessed antibacterial and antibiofilm effects on E. faecalis in response to pH values. DMAEM is promising to inhibit intraradicular E. faecalis in response to its acidic survival environment and maintain low cytotoxicity under neutral conditions, ensuring their biosafety in case of inadvertent entry into periapical tissues.
Asunto(s)
Biopelículas , Enterococcus faecalis , Metacrilatos , Materiales de Obturación del Conducto Radicular , Enterococcus faecalis/efectos de los fármacos , Concentración de Iones de Hidrógeno , Metacrilatos/farmacología , Metacrilatos/química , Biopelículas/efectos de los fármacos , Materiales de Obturación del Conducto Radicular/farmacología , Materiales de Obturación del Conducto Radicular/química , Antibacterianos/farmacología , Antibacterianos/química , Ensayo de Materiales , SolubilidadRESUMEN
Candida albicans is a common opportunistic fungus in humans, whose morphological switch between yeast and hyphae forms represents a key virulence trait. Developing strategies to inhibit C. albicans hyphal growth may provide insights into designs of novel antivirulent therapeutics. Importantly, the gut commensal bacterium, Enterococcus faecalis, secretes a bacteriocin EntV which has potent antivirulent and antifungal effects against C. albicans in infection models; however, hampered by the challenges to access large quantities of bioactive EntV, the detailed understanding of its mechanisms on C. albicans has remained elusive. In this work, we biochemically reconstituted the proteolytic cleavage reaction to obtain recombinant EntV88-His6 on a large preparative scale, providing facile access to the C-terminal EntV construct. Under in vitro C. albicans hyphal assay with specific inducers, we demonstrated that EntV88-His6 exhibits potent bioactivity against GlcNAc-triggered hyphal growth. Moreover, with fluorescent FITC-EntV88-His6, we revealed that EntV88-His6 enters C. albicans via endocytosis and perturbs the proper localization of the polarisome scaffolding Spa2 protein. Our findings provide important clues on EntV's mechanism of action. Surprisingly, we showed that EntV88-His6 does not affect C. albicans yeast cell growth but potently exerts cytotoxicity against C. albicans under hyphal-inducing conditions in vitro. The combination of EntV88-His6 and GlcNAc displays rapid killing of C. albicans, rendering it a promising antivirulent and antifungal agent.
Asunto(s)
Antifúngicos , Candida albicans , Enterococcus faecalis , Hifa , Candida albicans/efectos de los fármacos , Enterococcus faecalis/efectos de los fármacos , Antifúngicos/farmacología , Antifúngicos/química , Hifa/efectos de los fármacos , Hifa/crecimiento & desarrollo , Proteínas Recombinantes/farmacología , Proteínas Recombinantes/genética , Bacteriocinas/farmacología , Bacteriocinas/química , Pruebas de Sensibilidad Microbiana , Humanos , Proteínas Fúngicas/genética , Proteínas Fúngicas/metabolismo , Proteínas Fúngicas/química , Endocitosis/efectos de los fármacosRESUMEN
Enterococcus faecalis (E. faecalis) is a growing cause of nosocomial and antibiotic-resistant infections. Treating drug-resistant E. faecalis requires novel approaches. The use of bacteriophages (phages) against multidrug-resistant (MDR) bacteria has recently garnered global attention. Biofilms play a vital role in E. faecalis pathogenesis as they enhance antibiotic resistance. Phages eliminate biofilms by producing lytic enzymes, including depolymerases. In this study, Enterococcus phage vB_Efs8_KEN04, isolated from a sewage treatment plant in Nairobi, Kenya, was tested against clinical strains of MDR E. faecalis. This phage had a broad host range against 100% (26/26) of MDR E. faecalis clinical isolates and cross-species activity against Enterococcus faecium. It was able to withstand acidic and alkaline conditions, from pH 3 to 11, as well as temperatures between -80 °C and 37 °C. It could inhibit and disrupt the biofilms of MDR E. faecalis. Its linear double-stranded DNA genome of 142,402 bp contains 238 coding sequences with a G + C content and coding gene density of 36.01% and 91.46%, respectively. Genomic analyses showed that phage vB_Efs8_KEN04 belongs to the genus Kochikohdavirus in the family Herelleviridae. It lacked antimicrobial resistance, virulence, and lysogeny genes, and its stability, broad host range, and cross-species lysis indicate strong potential for the treatment of Enterococcus infections.
Asunto(s)
Bacteriófagos , Biopelículas , Farmacorresistencia Bacteriana Múltiple , Enterococcus faecalis , Genoma Viral , Especificidad del Huésped , Biopelículas/crecimiento & desarrollo , Biopelículas/efectos de los fármacos , Enterococcus faecalis/virología , Enterococcus faecalis/efectos de los fármacos , Kenia , Bacteriófagos/fisiología , Bacteriófagos/genética , Bacteriófagos/aislamiento & purificación , Bacteriófagos/clasificación , Humanos , Antibacterianos/farmacología , Infecciones por Bacterias Grampositivas/microbiología , Aguas del Alcantarillado/virologíaRESUMEN
This study investigated the effect of pumpkin powder (2 %, 4 %, and 6 %) and Enterococcus faecium and Enterococcus faecalis probiotics on the physicochemical, microbiological, and sensory properties of yogurt samples during 28 days of storage at 4 °C. The prebiotic effect of pumpkin powder (Cucurbita pepo) and the probiotic effect of Enterococcus faecium and E. faecalis were determined. Adding pumpkin powder to yogurt did not significantly alter the pH, acidity, fat, protein, and ash content (p > 0.05). Water holding was not changed during the storage time in the samples of probiotic yogurts, but as the pumpkin powder content increased, the water holding capacity also increased (p < 0.05). This situation did lead to a reduction in syneresis (p < 0.05). The lowest gumminess value at the end of storage was found in the D2 sample (p < 0.05), and the highest adhesiveness value was found in the D4 sample (p < 0.05). Furthermore, throughout the 28-day storage period, E. faecium and E. faecalis maintained a live cell count of ≥6 log CFU g-1 in the probiotic product. As a result of the statistical evaluation, there was a decrease in E. faecium in the D4, S2, and S4 samples, and then it increased again (p > 0.05) during the storage time. As a result of the statistical evaluation, it was determined that the smell, consistency in the spoon, consistency in the mouth, flavor, and acidity changes during the storage were not substantial (p > 0.05). In conclusion, it was found that pumpkin, a byproduct of the pumpkin seed industry, has the potential to act as a prebiotic and improve the properties of dairy products. Additionally, the study suggests that E. faecium and E. faecalis strains could be suitable for probiotic yogurts.
Asunto(s)
Cucurbita , Enterococcus faecalis , Enterococcus faecium , Prebióticos , Probióticos , Yogur , Enterococcus faecium/crecimiento & desarrollo , Cucurbita/microbiología , Enterococcus faecalis/crecimiento & desarrollo , Enterococcus faecalis/efectos de los fármacos , Yogur/microbiología , Concentración de Iones de Hidrógeno , Microbiología de Alimentos , Almacenamiento de Alimentos , Recuento de Colonia Microbiana , GustoRESUMEN
Enterococcus faecalis is one of the main microorganisms that infects root canals, ranking among the most prevalent microorganisms associated with endodontic treatment failure. Given its pervasive presence in persistent endodontic infections, the successful elimination of Enterococcus faecalis is crucial for effective endodontic treatment and retreatment. Furthermore, Enterococcus faecalis can form biofilms - defense structures that microbes use to fight environmental threats. These biofilms confer resistance against host immune system attacks and antibiotic interventions. Consequently, the presence of biofilms poses a significant challenge in the complete eradication of Enterococcus faecalis and its associated disease. In response, numerous scholars have discovered promising outcomes in addressing Enterococcus faecalis biofilms within root canals and undertaken endeavors to explore more efficacious approaches in combating these biofilms. This study provides a comprehensive review of strategies and mechanisms for the removal of Enterococcus faecalis biofilms.
Asunto(s)
Biopelículas , Cavidad Pulpar , Enterococcus faecalis , Infecciones por Bacterias Grampositivas , Biopelículas/efectos de los fármacos , Biopelículas/crecimiento & desarrollo , Enterococcus faecalis/efectos de los fármacos , Enterococcus faecalis/fisiología , Humanos , Cavidad Pulpar/microbiología , Infecciones por Bacterias Grampositivas/microbiología , Antibacterianos/farmacologíaRESUMEN
A biofilm is a complex microbial structure that promotes the progression of persistent infections, particularly in nosocomial settings via indwelling medical devices. Conventional antibiotics are often ineffective treatments for biofilms; hence, it is crucial to investigate or design non-antibiotic antibiofilm compounds that can successfully reduce and eradicate biofilm-related infections. This study was an attempt to repurpose chronic disease medications of the antihypertensive and antilipidemic drug classes, including candesartan cilexetil (CC) and ursodeoxycholic acid (UDCA), respectively, to be used as antibiofilm agents against the two infectious pathogens Staphylococcus aureus and Enterococcus faecalis. Crystal violet (CV) staining assay was used to evaluate the antibiofilm activity of the drugs. Real-time polymerase chain reaction (RT-PCR) was performed to determine the transcription levels of the biofilm-related genes (icaA and icaR in S. aureus and fsrC and gelE in E. faecalis) following treatment with different concentrations of CC and UDCA. we found that a concentration of greater than 1.5 µg/ml of CC significantly (p < 0.005) inhibited the biofilm formation of both bacterial isolates, and a concentration of greater than 50 µg/ml of UDCA significantly (p < 0.005) inhibited the biofilm formation of both bacterial isolates. Interestingly, the mRNA expression levels of biofilm-related genes were decreased in the two bacterial isolates at concentrations that were lower than the human pharmaceutical daily doses.