RESUMO
Increasing antimicrobial resistance among Gram-positive pathogens and pathogenic fungi remains one of the major public healthcare threats. Therefore, novel antimicrobial candidates and scaffolds are critically needed to overcome resistance in Gram-positive pathogens and drug-resistant fungal pathogens. In this study, we explored 1-(2-hydroxyphenyl)-5-oxopyrrolidine-3-carboxylic acid and its 3,5-dichloro-2-hydroxyphenyl analogue for their in vitro antimicrobial activity against multidrug-resistant pathogens. The compounds showed structure-dependent antimicrobial activity against Gram-positive pathogens (S. aureus, E. faecalis, C. difficile). Compounds 14 and 24b showed promising activity against vancomycin-intermediate S. aureus strains, and favorable cytotoxic profiles in HSAEC-1 cells, making them attractive scaffolds for further development. 5-Fluorobenzimidazole, having a 3,5-dichloro-2-hydroxyphenyl substituent, was found to be four-fold, and hydrazone, with a thien-2-yl fragment, was two-fold stronger than clindamycin against methicillin resistant S. aureus TCH 1516. Moreover, hydrazone, bearing a 5-nitrothien-2-yl moiety, showed promising activity against three tested multidrug-resistant C. auris isolates representing major genetic lineages (MIC 16 µg/mL) and azole-resistant A. fumigatus strains harboring TR34/L98H mutations in the CYP51A gene. The anticancer activity characterization demonstrated that the 5-fluorobenzimidazole derivative with a 3,5-dichloro-2-hydroxyphenyl substituent showed the highest anticancer activity in an A549 human pulmonary cancer cell culture model. Collectively these results demonstrate that 1-(2-hydroxyphenyl)-5-oxopyrrolidine-3-carboxylic acid derivatives could be further explored for the development of novel candidates targeting Gram-positive pathogens and drug-resistant fungi.
Assuntos
Anti-Infecciosos , Antineoplásicos , Clostridioides difficile , Staphylococcus aureus Resistente à Meticilina , Humanos , Staphylococcus aureus , Anti-Infecciosos/farmacologia , Fungos , Antibacterianos/farmacologia , Ácidos Carboxílicos , Antineoplásicos/farmacologia , Testes de Sensibilidade MicrobianaRESUMO
The p-aminobenzoic acid was applied for the synthesis of substituted 1-phenyl-5-oxopyrrolidine derivatives containing benzimidazole, azole, oxadiazole, triazole, dihydrazone, and dithiosemicarbazide moieties in the structure. All the obtained compounds were evaluated for their in vitro antimicrobial activity against Staphylococcus aureus, Bacillus cereus, Listeria monocytogenes, Salmonella enteritidis, Escherichia coli, and Pseudomonas aeruginosa by using MIC and MBC assays. This study showed a good bactericidal activity of γ-amino acid and benzimidazoles derivatives. The antimicrobial activity of the most promising compounds was higher than ampicillin. Furthermore, two benzimidazoles demonstrated good antimicrobial activity against L. monocytogenes (MIC 15.62 µg/mL) that was four times more potent than ampicillin (MIC 65 µg/mL). Further studies are needed to better understand the mechanism of the antimicrobial activity as well as to generate antimicrobial compounds based on the 1-phenyl-5-oxopyrrolidine scaffold.
Assuntos
Ácido 4-Aminobenzoico/química , Anti-Infecciosos/síntese química , Anti-Infecciosos/farmacologia , Azóis/síntese química , Azóis/farmacologia , Anti-Infecciosos/química , Azóis/química , Bactérias/efeitos dos fármacos , Técnicas de Química Sintética , Testes de Sensibilidade Microbiana , Triazóis/síntese química , Triazóis/química , Triazóis/farmacologiaRESUMO
Thiazole derivatives attract the attention of scientists both in the field of organic synthesis and bioactivity research due to their high biological activity. In the present study, thiazole ring was obtained by the interaction of 1-(4-(bromoacetyl)phenyl)-5-oxopyrrolidine-3-carboxylic acid with thiocarbamide or benzenecarbothioamide, as well as tioureido acid. A series of substituted 1-(3-(1,3-thiazol-2-yl)phenyl)-5-oxopyrrolidines with pyrrolidinone, thiazole, pyrrole, 1,2,4-triazole, oxadiazole and benzimidazole heterocyclic fragments were synthesized and their antibacterial properties were evaluated against Gram-positive strains of Staphylococcus aureus, Bacillus cereus, Listeria monocytogenes and Gram-negative Pseudomonas aeruginosa, Escherichia coli and Salmonella enterica enteritidis. The vast majority of compounds exhibited between twofold and 16-fold increased antibacterial effect against the test-cultures when compared with Oxytetracycline.
Assuntos
Antibacterianos/química , Oxidiazóis/química , Pirrolidinas/química , Antibacterianos/síntese química , Antibacterianos/farmacologia , Bacillus cereus/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Escherichia coli/patogenicidade , Listeria monocytogenes/efeitos dos fármacos , Listeria monocytogenes/patogenicidade , Testes de Sensibilidade Microbiana , Estrutura Molecular , Oxidiazóis/síntese química , Oxidiazóis/farmacologia , Pirrolidinas/síntese química , Pirrolidinas/farmacologia , Staphylococcus aureus/efeitos dos fármacos , Staphylococcus aureus/patogenicidade , Relação Estrutura-Atividade , Tiazóis/químicaRESUMO
The aim of this study was to evaluate the influence of additives of Jerusalem artichoke (JA), fermented with P. acidilactici KTU05-7, P. pentosaceus KTU05-9, L. sakei KTU05-6, on the quality and safety parameters of ready - to cook - minced pork (RCMP). Fermented JA additives reduced pH of the meat products and decreased water holding capacity (WHC) from 2.01 till 2.93 %. Concentrations of biogenic amines in RCMP with additives of the lactic acid bacteria (LAB) - fermented JA were significantly lower comparing with control sample. The number of pathogenic bacteria in artificially contaminated meat samples was significantly reduced in case of LAB-fermented JA additives. The highest antimicrobial activity was obtained using P. acidilactici fermented JA additives. The amounts of microbial pathogens E. coli and Ent. faecalis, S. aureus and Streptococcus spp. were determined 3.41, 3.38, 3,96 and 4.74 log CFU/g correspondingly, whereas without LAB-fermented JA additives were 8.94, 7.75, 8.82 and 8.58 log CFU/g, correspondingly. A possibility to improve sensory properties (flavor) of RCMP using LAB fermented JA additives was investigated. The composition of volatile compounds of RCMP without additive and with LAB-fermented JA additives was analyzed using gas chromatography-mass spectrometry (GC-MS). The results of sensory evaluation of meat products supplemented with fermented JA additives revealed specific odor, which is pleasant and acceptable for consumers might be explainable that LAB-fermented JA additives have shown considerable differences mainly due to the accumulation of volatiles such as toluene, ethylbenzene, decane, undecane, 2 methyl undecane. N-morpholinomethyl-isopropyl-sulfide, 6-undecilamine and N,N-dimethyl-1-pentadecanamine were not determined in RCMP with LAB-fermented JA additives. The results obtained show, that P. acidilactici fermented JA 5 % additive is most suitable for the RCMP processing in order to prevent microbiological spoilage, increase volatile compounds and acceptability of the products.
RESUMO
Benign prostatic hyperplasia (BPH) is an androgen-related non-neoplastic enlargement of the prostate gland that commonly affects both reproductive capabilities and the general health of intact dogs. The subclinical form of BPH can be challenging to diagnose due to a lack of clinical signs, even if rectal palpation is performed. Left untreated, this condition poses risks to the dogs' health and breeding status. This study, involving 65 male dogs, aimed to investigate subclinical BPH through rectal palpation, ultrasonography, and analysis of canine prostatic-specific esterase (CPSE). Of the participants, 35 had subclinical BPH, and 30 served as a healthy control group. Dogs suspected of subclinical BPH, as determined by examination results from ultrasonography and CPSE analysis, underwent fine needle aspiration (FNA) guided by ultrasound to enhance diagnostic precision. Findings revealed distinct differences in rectal palpation and ultrasonography between subclinical BPH and healthy dogs. This study established diagnostic thresholds based on prostatic volume and CPSE values and proposed new thresholds for subclinical BPH. Additionally, results showed that prostate gland volume depended on the weight and the age of the dog. In conclusion, early detection of this condition is possible through various examinations, such as changes in ultrasound features, CPSE levels, and rectal palpation. All together, these methods can aid practitioners in early detection of BPH and assist with scheduling screening programs for dogs, ultimately promoting their overall health and reproductive well-being. In conclusion, we advocate for routine, non-invasive prostate screenings in breeding males, underlining the effectiveness of a combination of various multiple techniques for early subclinical BPH detection.
RESUMO
New N,N-disubstituted ß-amino acids and their derivatives with thiazole, aromatic, and heterocyclic substituents were synthesized from N-phenyl-N-thiocarbamoyl-ß-alanine by the Hantzsch method; derivatives with hydrazone fragments were also obtained. Some of the synthesized compounds exhibited discrete antimicrobial activity, and 3-[(4-oxo-4,5-dihydro-1,3-thiazol-2-yl)(phenyl)amino]propanoic acid was found to promote rapeseed growth and to increase seed yield and oil content.
Assuntos
Propionatos/síntese química , Propionatos/farmacologia , Antibacterianos/química , Antibacterianos/farmacologia , Brassica rapa/química , Brassica rapa/efeitos dos fármacos , Técnicas de Química Combinatória , Ácidos Graxos/química , Testes de Sensibilidade Microbiana , Estrutura Molecular , Ressonância Magnética Nuclear BiomolecularRESUMO
Stable isotope analysis was applied to describe the poultry house environment. The poultry house indoor environment was selected for this study due to the relevant health problems in animals and their caretakers. Air quality parameters including temperature, relative humidity, airflow rate, NH3, CO2 and total suspended particles, as well as mean levels of total airborne bacteria and fungi count, were measured. Carbon isotope ratios (13C/12C) were obtained in size-segregated aerosol particles. The carbon (13C/12C) and nitrogen (15N/14N) isotope ratios were measured in feed, litter, scrapings from the ventilation system, feathers and eggs. Additionally, the distribution of δ13C and δ15N values in different tissues of the chicken was examined. The airborne bacteria and fungi extracted from the air filters collected from poultry farms were grown in the laboratory in media with known isotope values and measured for stable isotope ratios. Analysis of isotope fractionation between microorganisms and their media indicated the applicability of stable isotope analysis in bulk samples for the identification of source material. The analysed examples imply that stable isotope analysis can be used to examine the indoor environment along with its biology and ecology, and serve as an informative bioanalytical tool.
Assuntos
Isótopos de Carbono/análise , Monitoramento Ambiental/métodos , Isótopos de Nitrogênio/análise , Ração Animal/análise , Animais , Galinhas , Plumas/química , Feminino , Pisos e Cobertura de Pisos , Abrigo para Animais , Óvulo/químicaRESUMO
A Mycoplasma hyopneumoniae vaccine (Respisure, Pfizer AH) was tested for its effects on antibody formation, daily weight gain (DWG) in different growing periods, lung lesions and quality of meat (chemical composition, physicochemical properties and fatty acid composition). Two groups of conventional piglets were used for the investigation. One group of 11 females and 11 males was vaccinated intramuscularly at the age of 1 and 3 weeks. The other group of 22 piglets was left nonvaccinated as control. The results showed that antibodies against M. hyopneumoniae in the vaccinated group had been formed 14 days after the second vaccination and remained present till the end of the study at 147 days of age. In the nonvaccinated group, seroconversion started at 49 days of age and by the end of the study 10 out of 22 pigs had become seropositive. Vaccinated pigs achieved significantly higher daily weight gain (+30 g) and finishing body weight (+6.04 kg) than the nonvaccinated animals. In addition, the vaccinated pigs showed lesions involving 3.27% of the lung surface in average, while in the nonvaccinated pigs 9.04% of the lung surface was affected. Investigation of meat quality showed that the longissimus dorsi muscle of vaccinated pigs contained significantly lower percentage of fat (-0.63%) and its tryptophan/hydroxyproline ratio was significantly lower (-23.57) in comparison with the control animals. In addition, some other parameters also showed a favourable tendency, e.g. lean meat percentage was 0.91% higher, the protein content of the longissimus dorsi muscle was 0.35% higher, its water-binding capacity was also higher by 0.78%, its monounsaturated fatty acid concentration was 2.97% lower, while its polyunsaturated fatty acid content was 1.65% higher in the vaccinated pigs than in the nonvaccinated animals.
Assuntos
Anticorpos Antibacterianos/sangue , Vacinas Bacterianas/administração & dosagem , Mycoplasma pneumoniae/imunologia , Pneumonia Suína Micoplasmática/veterinária , Doenças dos Suínos/imunologia , Doenças dos Suínos/prevenção & controle , Animais , Feminino , Masculino , Carne , Pneumonia Suína Micoplasmática/imunologia , Pneumonia Suína Micoplasmática/prevenção & controle , Suínos , Aumento de PesoRESUMO
The possibilities and economic benefits of controlling mycoplasmal pneumonia of pigs caused by Mycoplasma hyopneumoniae by immunisation with Respisure and by Tiamutin treatment were studied. The experiment was carried out in a herd comprising 1000 sows which was free of PRRS, Aujeszky's disease, swine dysentery and leptospirosis, and the prevalence of mycoplasmal pneumonia was low because the farm had recently been restocked. Groups C1 and C2 served as untreated controls, while Groups R1 and R2 received a prestarter diet containing 100 ppm Tiamutin from the time of weaning. Piglets of Group R1 were vaccinated with Respisure vaccine once on day 69, while those of Group R2 twice, on days 65 and 80. Piglets of Groups ST1 and ST2 were fed 100 ppm Tiamutin in the diet for 7 days at the time of weaning and then at 4 months of age, while pigs of Group ST2 received such treatment also in the 6th month of life. The efficacy of treatment was analysed on the basis of the number of animals that died, were emergency slaughtered or were retarded in growth in the different groups, the body weight of animals at weaning, at 94 and 148 days of age and at the time of slaughter, their daily body weight gain, the lung lesions found in animals slaughtered from the different groups, the costs of medication and vaccination, and the cost-benefit calculations of the results. The mortality and emergency slaughter rate was 2.88% and 4.62% in Groups ST2 and ST1, respectively, 4.23% and 4.62% in Groups R2 and R1, respectively, and 8.39% and 9.44% in the control groups (C2 and C1, respectively). The rate of growth retardation was 0.48% and 2.12% in Groups R1 and R2, respectively, 1.59% and 3.46% in Groups ST1 and ST2, respectively, as compared to 8.03% and 6.55% in the control groups (C1 and C2, respectively). The severity score of lung lesions was 1.82 and 1.46 in Groups R1 and R2, 2.18 and 2.93 in Groups ST1 and ST2, and 3.83 and 4.02 in the control groups C1 and C2, respectively. The mean finishing weight of pigs was 102.4-107.8 kg and 95.2-106.6 kg in the treated groups and 94.5-98.6 kg in the control groups. The classification of pigs according to the EUROP categories showed a shift to the E and U categories in the treated groups. The average feed cost per one kg of liveweight was 77.89-82.64 Forints in the treated groups and 85.66 Forints in the control groups.
Assuntos
Antibacterianos/administração & dosagem , Vacinas Bacterianas/administração & dosagem , Diterpenos/administração & dosagem , Mycoplasma pneumoniae/imunologia , Pneumonia Suína Micoplasmática/veterinária , Doenças dos Suínos/economia , Doenças dos Suínos/prevenção & controle , Animais , Dieta , Esquema de Medicação , Feminino , Pneumonia Suína Micoplasmática/economia , Pneumonia Suína Micoplasmática/prevenção & controle , Gravidez , Suínos , Doenças dos Suínos/mortalidade , Resultado do Tratamento , Vacinação/veterináriaRESUMO
Cationic cross-linked starch (CCS)-iodine complexes containing different amounts of quaternary ammonium groups (different degrees of substitution (DS)) and iodine have been obtained by iodine adsorption on CCS from aqueous iodine potassium iodide solution. Equilibrium adsorption studies showed that with an increase of DS the amount of iodine adsorbed on CCS and the affinity of iodine to CCS increased linearly. The influences of the DS of CCS and the amount of adsorbed iodine on the stability of CCS-iodine complexes in a solution of 0.02M sodium acetate and reactivity toward l-tyrosine have been investigated. At the same DS, the stability of CCS-iodine complexes decreased with an increase of the amount of adsorbed iodine. With increasing the DS, the stability of CCS-iodine complexes increased. The iodine consumption in the reaction with l-tyrosine increased significantly with an increase of the amount of adsorbed iodine. The influence of DS on iodine consumption was lower and depended on the amount of adsorbed iodine. The antibacterial activity of CCS-iodine complexes against Bacillus cereus, Staphylococcus aureus, Pseudomonas aeruginosa and Escherichia coli was determined by the broth-dilution and spread-plate methods. The obtained results have demonstrated that an appropriate selection of the CCS-iodine complex composition (the DS of CCS and the amount of adsorbed iodine) could ensure good antimicrobial properties by keeping a low concentration of free iodine in the system. The main advantage of using CCS-iodine complexes as antimicrobial agents is the biodegradability of the polymeric matrix.