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1.
Braz J Microbiol ; 55(1): 343-355, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-38066229

RESUMO

Sulfonamide derivatives have numerous pharmaceutical applications having antiviral, antibacterial, antifungal, antimalarial, anticancer, and antidepressant activities. The structural flexibility of sulfonamide derivatives makes them an excellent candidate for the development of new multi-target agents, although long-time exposure to sulfonamide drugs results in many toxic impacts on human health. However, sulfonamides may be functionalized for developing less toxic and more competent drugs. In this work, sulfonamides including Sulfapyridine (a), Sulfathiazole (b), Sulfamethoxazole (c), and Sulfamerazine (d) are used to synthesize Schiff bases of 7-hydroxy-4-methyl-2-oxo-2H-chromene-8-carbalde-hyde (1a-1d). The synthesized compounds were spectroscopically characterized and tested against hospital isolates of three Gram-positive (Methicillin-resistant Staphylococcus aureus PH217, Ampicillin-resistant Coagulase-negative Staphylococcus aureus, multidrug-resistant (MDR) Enterococcus faecalis PH007R) and two Gram-negative bacteria (multidrug-resistant Escherichia coli, and Salmonella enterica serovar Typhi), compared to the quality control strains from ATCC (S. aureus 29213, E. faecalis 25922, E. coli 29212) and MTCC (S. Typhi 734). Two of the four Schiff bases 1a and 1b are found to be more active than their counterpart 1c and 1d; while 1a have showed significant activity by inhibiting MRSA PH217 and MDR isolates of E. coli at the minimum inhibitory concentration (MIC) of 150 µg/mL and 128 µg/mL with MBC of 1024 µg/mL, respectively. On the other hand, the MIC of 1b was 150 µg/mL against both S. aureus ATCC 29213 and Salmonella Typhi MTCC 734, compared to the control antibiotics Ampicillin and Gentamycin. Scanning electron microscopy demonstrated the altered surface structure of bacterial cells as a possible mechanism of action, supported by the in-silico molecular docking analysis.


Assuntos
Staphylococcus aureus Resistente à Meticilina , Staphylococcus aureus , Humanos , Simulação de Acoplamento Molecular , Cromonas/farmacologia , Escherichia coli , Bases de Schiff/farmacologia , Antibacterianos/farmacologia , Antibacterianos/química , Sulfanilamida , Ampicilina/farmacologia , Sulfonamidas/farmacologia , Testes de Sensibilidade Microbiana
2.
Metabolites ; 13(7)2023 Jul 18.
Artigo em Inglês | MEDLINE | ID: mdl-37512561

RESUMO

Plant biomass colonized by macrofungi can contain molecules with bioactive properties with applications to human/animal health. This work aimed to verify antibacterial activities from aqueous extracts from oil seed cakes of Jatropha curcas (JSC) and cottonseed (CSC), fermented by macrofungi for probiotic bacteria cultivation. Coriolopsis sp., Tyromyces sp., Panus lecomtei, and Pleurotus pulmonarius were cultivated in solid and submerged media. The aqueous extract of unfermented JSC was more efficient than glucose for the growth of all probiotic bacteria. Extracts from four macrofungi fermented in CSC favored Lactobacillus acidophilus growth. In solid fermentation, macrofungi extracts cultivated in JSC favored Bifidobacterium lactis growth. All fungi extracts showed more significant growth than carbohydrates among the four probiotic bacteria evaluated. Regarding antimicrobial activities, no fungal extract or bacterial supernatant showed a more significant inhibition halo for enteropathogenic bacteria than ampicillin (control). Extracts from P. lecomtei and Coriolopsis sp. in CSC showed inhibition halos for Salmonella enterica. Supernatants from L. acidophilus, B. lactis, and Lactobacillus rhamnosus resulted in more significant inhibition of Staphylococcus aureus than the control, which indicates possible antimicrobial activity. Unfermented JSC supernatant showed better results for bacterial growth, while supernatants and aqueous extracts from CSC fermentation can be used for probiotic bacteria culture.

3.
Rev. argent. microbiol ; Rev. argent. microbiol;54(4): 91-100, dic. 2022. graf
Artigo em Inglês | LILACS-Express | LILACS | ID: biblio-1422970

RESUMO

Abstract Diverse habitats have been screened for novel antimicrobial actinomycetes, while others remain unexplored. In this study, we analyzed the bioactivities of actinomycetes cul-tured from rhizosphere soils of the desert plant Artemisia tridentata and the nearby bulk soils. Actinomycetes were screened for antifungal and antibacterial activities toward a panel of plant pathogens; all comparisons were between activities of rhizosphere soil isolates toward those of its counterpart bulk soil. A selected group of the strongest antifungal isolates were also tested against two antifungal-drug resistant strains of Candida albicans. 16S rDNA partial sequences and phylogenetic analysis of isolates that showed broad-spectrum antifungal activities were performed. Forty-two out of 200 and two soil isolated actinomycetes were selected for their strong antifungal activities. The highest proportion of isolates (p <0.05) from rhizosphere soil of an old plant showed antagonism against gram-positive bacteria (0.483 and 0.224 propor-tions against Bacillus subtilis and Rathayibacter tritici, respectively), and phytopathogenic fungi (0.259, 0.431, and 0.345 proportions against Fusarium oxysporum, Rhizoctonia solani and Pythium ultimum, respectively), while the highest antagonism against the gram-negative bacteria predominated in isolates from the bulk soils. Isolates from a rhizosphere soil of a young plant were characterized for strong antagonist activities against Fusarium oxysporum (0.333 proportion, p<0.05). Phylogenetic analysis of 16S rDNA sequences showed that isolates that exhibited strong antifungal activity were genetically similar. We conclude that the rhizosphere soil of A. tridentata is an excellent source for discovery of actinomycetes with potentially novel antifungal compounds.


Resumen En la búsqueda de actinomicetos antimicrobianos se han estudiado diversos hábitats, pero muchos permanecen aún sin explorar. En este estudio analizamos las actividades biológicas de cultivos de actinomicetos provenientes de suelos rizosféricos de la planta desértica Artemisia tridentata y de suelos no asociados a sus raíces. Los actinomicetos fueron seleccionados por sus actividades antifúngicas y antibacterianas contra un panel de patógenos de plantas. Todas las comparaciones fueron entre las actividades de los aislados rizosféricos y aquellas de los aislados no asociados a las raíces. Un grupo selecto de los aislados con las mayores actividades antifúngicas fueron también evaluados contra 2 cepas de Candida albicans resistentes a antifúngicos. Se realizó la secuenciación parcial del ARNr 16S y el análisis filogenético de los aislados que mostraron actividades antifúngicas de amplio espectro. Se seleccionaron 42 de 202 actinomicetos aislados por sus fuertes actividades antifúngicas. La mayor proporción de aislados de suelo rizosférico de plantas viejas mostraron antagonismo contra bacterias gram positivas y hongos fitopatógenos (proporciones de 0,259; 0,431 y 0,345 contra Fusarium oxyspo-rum, Rhizoctonia solani y Pythium ultimum, respectivamente), mientras que la mayor actividad antagónica contra las bacterias gram negativas predominaron en aislados de suelo no asociado a raíces. Los aislados de suelo rizosférico de plantas jóvenes se caracterizaron por una fuerte actividad antagónica contra F. oxysporum (proporción de 0,333, p < 0,05). El análisis filogenético de secuencias del ADNr 16S mostró que los aislados que presentaron fuerte actividad antifúng-ica fueron genéticamente similares. Concluimos que el suelo rizosférico de A. tridentata es una fuente excelente para el descubrimiento de actinomicetos productores de compuestos antifúngicos potencialmente novedosos.

4.
Cell Immunol ; 382: 104630, 2022 12.
Artigo em Inglês | MEDLINE | ID: mdl-36270066

RESUMO

Neutrophil extracellular traps (NETs) are fiber structures composed of chromatin and granular proteins that capture and eliminate microorganisms. The NETs formation is induced in response to pathogens and physiological stimuli; however, some pathogens have developed strategies to evade NETs activity. Trichinella spiralis excretory-secretory (ES) antigens are proteins that allow the establishment of the parasite in the host, facilitating penetration, migration, nutrition, and survival. In this paper we described that ES antigens inhibit NETs release, since neutrophils incubated with these antigens maintains a delobulated nucleus, without the release fibers structures indicative of NETs. We also found that other antimicrobial functions of neutrophils, such as phagocytic activity, degranulation, and ROS production, remain unchanged after incubation with ES antigens. This is relevant since it could constitute a novel strategy for the treatment of autoimmune pathologies in which the formation of NETs performs an important role.


Assuntos
Anti-Infecciosos , Armadilhas Extracelulares , Trichinella spiralis , Animais , Neutrófilos , Larva
5.
Rev Argent Microbiol ; 54(4): 326-334, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35725666

RESUMO

Diverse habitats have been screened for novel antimicrobial actinomycetes, while others remain unexplored. In this study, we analyzed the bioactivities of actinomycetes cultured from rhizosphere soils of the desert plant Artemisia tridentata and the nearby bulk soils. Actinomycetes were screened for antifungal and antibacterial activities toward a panel of plant pathogens; all comparisons were between activities of rhizosphere soil isolates toward those of its counterpart bulk soil. A selected group of the strongest antifungal isolates were also tested against two antifungal-drug resistant strains of Candida albicans. 16S rDNA partial sequences and phylogenetic analysis of isolates that showed broad-spectrum antifungal activities were performed. Forty-two out of 200 and two soil isolated actinomycetes were selected for their strong antifungal activities. The highest proportion of isolates (p<0.05) from rhizosphere soil of an old plant showed antagonism against gram-positive bacteria (0.483 and 0.224 proportions against Bacillus subtilis and Rathayibacter tritici, respectively), and phytopathogenic fungi (0.259, 0.431, and 0.345 proportions against Fusarium oxysporum, Rhizoctonia solani and Pythium ultimum, respectively), while the highest antagonism against the gram-negative bacteria predominated in isolates from the bulk soils. Isolates from a rhizosphere soil of a young plant were characterized for strong antagonist activities against Fusarium oxysporum (0.333 proportion, p<0.05). Phylogenetic analysis of 16S rDNA sequences showed that isolates that exhibited strong antifungal activity were genetically similar. We conclude that the rhizosphere soil of A. tridentata is an excellent source for discovery of actinomycetes with potentially novel antifungal compounds.


Assuntos
Actinobacteria , Artemisia , Streptomyces , Filogenia , Microbiologia do Solo , Antifúngicos , Artemisia/genética , Artemisia/microbiologia , Actinomyces/genética , Actinobacteria/genética , Rizosfera , Solo , DNA Ribossômico/genética , Doenças das Plantas/microbiologia
6.
Front Microbiol ; 12: 621274, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33597940

RESUMO

In the myrmecophytic mutualistic relationship between Azteca ants and Cecropia plants both species receive protection and exchange nutrients. The presence of microorganisms in this symbiotic system has been reported, and the symbiotic role of some fungi involved in the myrmecophytic interactions has been described. In this work we focus on bacteria within this mutualism, conducting isolations and screening for antimicrobial activities, genome sequencing, and biochemical characterization. We show that Pantoea, Rhizobium, Methylobacterium, Streptomyces and Pseudomonas are the most common cultivable genera of bacteria. Interestingly, Pseudomonas spp. isolates showed potent activity against 83% of the pathogens tested in our antimicrobial activity assays, including a phytopathogenic fungus isolated from Cecropia samples. Given the predicted nitrogen limitations associated with the fungal patches within this myrmecophyte, we performed nitrogen fixation analyses on the bacterial isolates within the Proteobacteria and show the potential for nitrogen fixation in Pseudomonas strains. The genome of one Pseudomonas strain was sequenced and analyzed. The gene cluster involved in the biosynthesis of cyclic lipodepsipeptides (CLPs) was identified, and we found mutations that may be related to the loss of function in the dual epimerization/condensation domains. The compound was isolated, and its structure was determined, corresponding to the antifungal viscosinamide. Our findings of diazotrophy and production of viscosinamide in multiple Pseudomonas isolates suggests that this bacterial genus may play an important role in the Cecropia-Azteca symbiosis.

7.
Braz. arch. biol. technol ; Braz. arch. biol. technol;62: e19180503, 2019. graf
Artigo em Inglês | LILACS | ID: biblio-1011535

RESUMO

Abstract In this review, we explore some aspects of Pseudomonas aeruginosa virulence factors that are related to disease development in healthy organisms and resistance to antibiotics. This pathogen is one of the most clinically and epidemiologically important bacteria in Brazil, being the major cause of opportunistic infections. Among the virulence factors, biofilm formation acting of manner different in the organism. Furthermore, we review several P. aeruginosa genes that act in antimicrobial resistance, such as β-lactamases against β-lactamers. The resistance to pied-lactamases in P. aeruginosa is associated to resistance to the broad-spectrum cephalosporin. On the other hand, there is a group of synthetic broad-spectrum antibiotics acting on DNA synthesis is the quinolones that destroy the microorganism. We also explore the occurence of super bacterium: P. aerufinosa carrying genes blaKPC and blaNDM, which are associated with patient death above the average of other bacterial infections in hospitals. Those genes encode carbapenemases that can potentially hydrolyse all β-lactam antibiotics


Assuntos
Pseudomonas aeruginosa/virologia , Fatores de Virulência , beta-Lactamases/fisiologia , Biofilmes , Anti-Infecciosos
8.
Chem Biodivers ; 15(8): e1800216, 2018 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-29869833

RESUMO

We evaluated the antimicrobial activity of 25 monoketone curcuminoids (MKCs) against a representative panel of cariogenic bacteria in terms of their minimum inhibitory concentration (MIC) values. Curcumin A (10) displayed promising activity against Streptococcus mutans (MIC = 50 µg/ml) and Streptococcus mitis (MIC = 50 µg/ml) as well as moderate activity against S. sanguinis (MIC = 100 µg/ml), Lactobacillus casei (MIC = 100 µg/ml), and Streptococcus salivarius (MIC = 200 µg/ml). Results indicated higher activity of compound 10 than that of its bis-ß-diketone analog. Additionally, compounds 3a (1,5-bis(4-methylphenyl)pentan-3-one) and 7b (1,5-bis(4-bromophenyl)pentan-3-ol) were moderately active against S. mitis (MIC = 100 µg/ml) and S. salivarus (MIC = 200 µg/ml).


Assuntos
Antibacterianos/farmacologia , Curcumina/farmacologia , Lacticaseibacillus casei/efeitos dos fármacos , Streptococcus/efeitos dos fármacos , Antibacterianos/química , Curcumina/análogos & derivados , Curcumina/química , Relação Dose-Resposta a Droga , Testes de Sensibilidade Microbiana , Estrutura Molecular , Relação Estrutura-Atividade
9.
Antonie Van Leeuwenhoek ; 111(8): 1315-1332, 2018 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-29721711

RESUMO

An "in house" taxonomic approach to drug discovery led to the isolation of diverse actinobacteria from hyper-arid, extreme hyper-arid and very high altitude Atacama Desert soils. A high proportion of the isolates were assigned to novel taxa, with many showing activity in standard antimicrobial plug assays. The application of more advanced taxonomic and screening strategies showed that strains classified as novel species of Lentzea and Streptomyces synthesised new specialised metabolites thereby underpinning the premise that the extreme abiotic conditions in the Atacama Desert favour the development of a unique actinobacterial diversity which is the basis of novel chemistry. Complementary metagenomic analyses showed that the soils encompassed an astonishing degree of actinobacterial 'dark matter', while rank-abundance analyses showed them to be highly diverse habitats mainly composed of rare taxa that have not been recovered using culture-dependent methods. The implications of these pioneering studies on future bioprospecting campaigns are discussed.


Assuntos
Actinobacteria/classificação , Biodiversidade , Clima Desértico , Filogenia , Microbiologia do Solo , Actinobacteria/genética , Actinobacteria/isolamento & purificação , Actinobacteria/metabolismo , Altitude , Antibacterianos/isolamento & purificação , Chile , Ecossistema , Metagenômica , Especificidade da Espécie
10.
J Appl Microbiol ; 125(2): 370-382, 2018 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-29624805

RESUMO

AIMS: Since mycosynthesis of metal nanoparticles (NPs) is advertised as a promising and ecofriendly approach. Thus, this study aims to investigate the capability of Aspergillus brasiliensis ATCC 16404 for mycosynthesis of silver NPs (AgNPs). METHODS AND RESULTS: One-factor-at-a-time-technique was used to study the effect of different physicochemical parameters: the reaction time, pH, temperature, different stirring rates, illumination, and finally, the different concentrations of silver nitrate and fungal biomass on the mycosynthesis of AgNPs. The visual observation showed the characteristic brown colour formation due to the bioreduction of Ag+ ions to Ag0 by the mycelial cell-free filtrate (MCFF). The UV/visible spectrophotometric technique displayed a characteristic sharp peak at ʎ440 confirming the mycosynthesis of AgNPs. The zeta potential value -16·7 mV assured the long-term stability of AgNPs and the dynamic light scattering analysis revealed good dispersion and average particle size 77 nm. The energy dispersive X-ray spectroscopy displayed a maximum elemental distribution of silver elements. The X-ray diffraction spectroscopy demonstrated the crystallinity of the mycosynthesized AgNPs. The field emission scanning electron microscope and high-resolution transmission electron microscope revealed monodispersed spherical shaped AgNPs with average particle size of 6-21 nm. The FTIR analysis showed the major peaks of proteins providing the possible role of MCFF in the synthesis and stabilization of the AgNPs. The mycosynthesized AgNPs expressed good biocidal activity against different pathogenic micro-organisms causing some water-related diseases and health problems to local residents. CONCLUSIONS: This study proved that A. brasiliensis ATCC 16404 MCFF has good potential for mycosynthesis of AgNPs, which exhibited good antimicrobial effect on different pathogenic micro-organisms; thus, it can be applied for water disinfection. SIGNIFICANCE AND IMPACT OF THE STUDY: This research provides a helpful insight into the development of a new mycosynthesized antimicrobial agent.


Assuntos
Antibacterianos/farmacologia , Aspergillus/metabolismo , Nanopartículas Metálicas/química , Prata/farmacologia , Antibacterianos/química , Estabilidade de Medicamentos , Nanopartículas Metálicas/ultraestrutura , Testes de Sensibilidade Microbiana , Tamanho da Partícula , Prata/química , Propriedades de Superfície
11.
Spectrochim Acta A Mol Biomol Spectrosc ; 198: 212-221, 2018 Jun 05.
Artigo em Inglês | MEDLINE | ID: mdl-29547823

RESUMO

Coumarins (2H-chromen-2-one) are oxygen-containing heterocyclic compounds that belong to the benzopyranones family. In this work we have synthesized different coordination complexes with coumarin-3-carboxylic acid (HCCA), o-phenanthroline (phen) and zinc(II). In the reported [Zn(CCA)2(H2O)2] complex, coumarin-3-carboxylate (CCA) is acting as a bidentate ligand while in the two prepared complexes, [Zn(phen)3]CCA(NO3) (obtained as a single crystal) and [Zn(CCA)2phen].4H2O, CCA is acting as a counterion of the complex cation [Zn(phen)3]+2 or coordinated to the metal center along with phen, respectively. These compounds were characterized on the basis of elemental analysis and thermogravimetry. NMR, FTIR and Raman spectroscopies of the compounds and the CCA potassium salt (KCCA) allow to determine several similarities and differences among them. Finally, their behavior against alkaline phosphatase enzyme and their antimicrobial activities were also measured.


Assuntos
Anti-Infecciosos/farmacologia , Complexos de Coordenação/química , Cumarínicos/química , Fenantrolinas/química , Compostos de Zinco/química , Fosfatase Alcalina/química , Fosfatase Alcalina/metabolismo , Anti-Infecciosos/química , Complexos de Coordenação/farmacologia , Cristalografia por Raios X , Avaliação Pré-Clínica de Medicamentos , Espectroscopia de Ressonância Magnética , Testes de Sensibilidade Microbiana , Espectrofotometria Ultravioleta , Espectroscopia de Infravermelho com Transformada de Fourier , Análise Espectral Raman
12.
Braz. J. Pharm. Sci. (Online) ; 54(4): e17724, 2018. tab, graf, ilus
Artigo em Inglês | LILACS | ID: biblio-1001563

RESUMO

As there are a lot of antibacterial and anti-fungal resistant pathogens, researchers attempt to substitute antimicrobial drugs with various medical plants and novel nanoparticles. The present study was conducted to characterize antimicrobial activities of Euphorbia prostrata and Pelargonium graveolens extract alone and in combination with Mn-Ni@Fe3O4-NPs & Mn: Fe (OH)3-NPs on the DNA cleavage of E. coli and also Bacillus subtilis, Pseudomonas aeruginosa, Escherichia coli, Staphylococcus aureus, Aspergillus oryzae, and Candida albicans. The effects of antimicrobial activities on above scenarios were evaluated using disc diffusion, MIC, MBC, and E. coli DNA electrophoresis methods. The results showed that the effects of antibacterial assay values of Euphorbia prostrata & Mn: Fe(OH)3 was 21.00 mm for E. coli and while it was 19.5 mm for Euphorbia prostrata & Mn-Ni@Fe3O4 against Pseudomonas aeruginosa at a concentration of 100mg/mL. The highest level of DNA cleavage was seen in mixed of Euphorbia prostrata & Mn: Fe(OH)3 nanoparticles. In conclusion, the combination of Euphorbia prostrata and Pelargonium graveolens extracts with nanostructures showed synergic effects on eliminating the bacteria via DNA destruction and others mechanisms. Moreover, the synergistic effect of nanoparticles with plant extracts seems to bring about new choices for the treatment of infectious diseases


Assuntos
Extratos Vegetais/análise , Euphorbia prostata/efeitos adversos , Pelargonium/efeitos adversos , Nanopartículas/análise , Candida albicans/metabolismo , Escherichia coli/metabolismo , Anti-Infecciosos/farmacologia
13.
Springerplus ; 5(1): 1788, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27795930

RESUMO

BACKGROUND: In the altiplano of Northern Chile the plant Senecio nutans is habitually used as an infusion to relieve the effects of altitude sickness (locally known as "puna"). It is also used to alleviate the bronchitis, whooping cough, asthma, stomachache, tiredness and fever. The extreme conditions under which these plant grow and scientific data that shows the inhibiting potential of the essential oils of plants of the genus Senecio represents great potential in the study of their application to control pathogens like Vibrio Cholera. METHODS: The essential oil from aerial parts of S. nutans was isolated by hydrodistillation and the chemical composition characterized by GC-MS analyses. The antibacterial potential and determination of MIC value, was estimated in both micro and macro dilution method. RESULTS: The GC-MS analysis of essential oil of S. nutans showed the presence of methyl cinnamate (44.9 %), p-cymenol (27.2 %), and terpinen-4-ol (6.8 %), α-terpineol (4.1 %), t-cadinol (3.5 %), methyl hydrocinnamate (2.1 %), δ-cadinene (2.0 %), p-cymene (1.9 %), γ-terpinene (1.8 %), α-cadinol (1.6 %), cis-sabinene hydrate (1.1 %), caryophyllene (0.9 %), ß-pinene (0.8 %), and α-terpinene (0.6 %) as major components. Moreover, the oil of S. nutans exhibited an important antibacterial activity with a diameter of inhibition zone growth of 22 mm and the MIC value of 0.4 mg/mL against pathogenic bacteria V. cholerae. CONCLUSIONS: The results show for the first time the antibacterial activity of the essential oils of S. nutans against the V. cholerae pathogen, an activity that can be applied as a preventive treatment against the action of pathogen.

14.
Chem Biodivers ; 13(12): 1715-1719, 2016 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-27603914

RESUMO

Chemical analysis, antimicrobial activity and cytotoxic effects of essential oils (EOs) from leaves of Piper aduncum var. ossanum from two localities Bauta (EO-B) and Ceiba (EO-C), Artemisa Province, Cuba, were determined. EOs were obtained by hydrodistillation and analyzed by gas chromatography/mass spectrometry. EO-B demonstrated higher activity against S. aureus and L. amazonensis; while a lower cytotoxicity on mammalian cells was observed. Both EOs displayed the same activity against Plasmodium falciparum, Trypanosoma cruzi, Trypanosoma brucei, and Leishmania infantum. Both EOs were inactive against Escherichia coli and Candida albicans.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Antiparasitários/farmacologia , Citotoxinas/farmacologia , Óleos Voláteis/farmacologia , Óleos Voláteis/toxicidade , Piper/química , Animais , Antibacterianos/química , Antibacterianos/isolamento & purificação , Antifúngicos/química , Antifúngicos/isolamento & purificação , Antiparasitários/química , Antiparasitários/isolamento & purificação , Candida albicans/efeitos dos fármacos , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Citotoxinas/química , Citotoxinas/isolamento & purificação , Relação Dose-Resposta a Droga , Escherichia coli/efeitos dos fármacos , Humanos , Leishmania infantum/efeitos dos fármacos , Macrófagos/efeitos dos fármacos , Camundongos , Testes de Sensibilidade Microbiana , Óleos Voláteis/química , Óleos Voláteis/isolamento & purificação , Testes de Sensibilidade Parasitária , Folhas de Planta/química , Plasmodium falciparum/efeitos dos fármacos , Relação Estrutura-Atividade , Trypanosoma/efeitos dos fármacos
15.
Molecules ; 21(9)2016 Sep 06.
Artigo em Inglês | MEDLINE | ID: mdl-27608004

RESUMO

(-)-Cytoxazone, originally isolated from cultures of a Streptomyces species has an oxazolidin-2-one 4,5-disubstituted ring. It is known that this natural product presents a cytokine modulator effect through the signaling pathway of Th2 cells (type 2 cytokines), which are involved in the process of growth and differentiation of cells. From this, the interest in the development of research aimed at the total synthesis of this molecule and its analogs has remained high, which can be confirmed by the large number of publications on the topic, more than 30 to date. This review focuses on the various creative methods for the synthesis of (-)-cytoxazone and its congeners. The assessment of the preparation of this oxazolidinone and related structures serves as a treatise on the efforts made in the synthesis of this important class of compound from its first total synthesis in 1999.


Assuntos
Citocinas/metabolismo , Oxazóis , Transdução de Sinais/efeitos dos fármacos , Células Th2/metabolismo , Animais , Humanos , Oxazóis/síntese química , Oxazóis/química , Oxazóis/farmacologia
16.
Braz J Anesthesiol ; 64(2): 84-8, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-24794449

RESUMO

BACKGROUND: Drugs administered as intravenous infusion may be contaminated during several stages of production or preparation. However studies focusing on antibacterial effects of vasopressor drugs are very rare. This study investigates the in vitro antimicrobial activity of the clinically used forms of vasopressors. MATERIALS AND METHODS: In vitro antimicrobial activities of vasopressor drugs of different concentrations were investigated by using the micro dilution technique. Microorganisms used in the test were Escherichia coli ATCC 25922, Yersinia pseudotuberculosis ATCC 911, Pseudomonas aeruginosa ATCC 10145, Listeria monocytogenes ATCC 43251, Enterococcus faecalis ATCC 29212, Staphylococcus aureus ATCC 25923, Bacillus cereus 702 Roma, Mycobacterium smegmatis ATCC607, Candida albicans ATCC 60193, and Saccharomyces cerevisiae RSKK 251. Antibacterial assays were performed in Mueller-Hinton broth at pH 7.3 and antifungal assays were performed in buffered Yeast Nitrogen Base at pH 7.0. RESULTS: Two different dopamine preparations showed antimicrobial activity. No other study drug showed any antimicrobial activity. CONCLUSIONS: In our opinion, dopamine's antibacterial effects may be advantageous for inhibiting the spread of bacterial contamination during the preparation of the infusion solutions. However, it is important that strict guidelines regarding the need for sterile equipment and deliverables be adhered to during all procedures performed in the intensive care units.


Assuntos
Anti-Infecciosos/farmacologia , Vasoconstritores/farmacologia , Acetilcisteína/farmacologia , Concentração de Íons de Hidrogênio , Técnicas In Vitro , Testes de Sensibilidade Microbiana
17.
Rev. bras. anestesiol ; Rev. bras. anestesiol;64(2): 84-88, Mar-Apr/2014. tab
Artigo em Português | LILACS | ID: lil-711135

RESUMO

Justificativa e objetivo: os medicamentos administrados como perfusão intravenosa podem ser contaminados durante as várias etapas de produção ou preparação. No entanto, estudos sobre os efeitos antibacterianos de vasopressores são muito raros. Este estudo investiga a atividade antimicrobiana in vitro das formas de vasopressores usados clinicamente. Materiais e métodos: atividades antimicrobianas in vitro de substâncias vasopressoras de diferentes concentrações foram investigadas com o uso da técnica de microdiluição. Os microrganismos empregados no teste foram: Escherichia coli ATCC 25922, Yersinia pseudotuberculosis ATCC 911, Pseudomonas aeruginosa ATCC 10145, Listeria monocytogenes ATCC 43251, Enterococcus faecalis ATCC 29212, Staphylococcus aureus ATCC 25923, Bacillus cereus 702 Roma, Mycobacterium smegmatis ATCC607, Candida albicans ATCC 60193 e Saccharomyces cerevisiae RSKK 251. Os ensaios antibacterianos foram feitos em caldo de cultura Mueller-Hinton (pH 7,3) e os ensaios antifúngicos em solução tampão de base nitrogenada para levedura (pH 7,0). Resultados: duas preparações diferentes de dopamina mostraram atividade antimicrobiana. Nenhuma outra substância do estudo mostrou qualquer atividade antimicrobiana. Conclusões: em nossa opinião, os efeitos antibacterianos da dopamina podem ser vantajosos para inibir a propagação de contaminação bacteriana durante a preparação das soluções para perfusão. Contudo, salientamos a importância do seguimento rigoroso das diretrizes de esterilização dos equipamentos e de assepsia durante todos os procedimentos feitos em unidades de terapia intensiva. .


Background: Drugs administered as intravenous infusion may be contaminated during several stages of production or preparation. However studies focusing on antibacterial effects of vasopressor drugs are very rare. This study investigates the in vitro antimicrobial activity of the clinically used forms of vasopressors. Materials and methods: In vitro antimicrobial activities of vasopressor drugs of different concentrations were investigated by using the micro dilution technique. Microorganisms used in the test were Escherichia coli ATCC 25922, Yersinia pseudotuberculosis ATCC 911, Pseudomonas aeruginosa ATCC 10145, Listeria monocytogenes ATCC 43251, Enterococcus faecalis ATCC 29212, Staphylococcus aureus ATCC 25923, Bacillus cereus 702 Roma, Mycobacterium smegmatis ATCC607, Candida albicans ATCC 60193, and Saccharomyces cerevisiae RSKK 251. Antibacterial assays were performed in Mueller-Hinton broth at pH 7.3 and antifungal assays were performed in buffered Yeast Nitrogen Base at pH 7.0. Results: Two different dopamine preparations showed antimicrobial activity. No other study drug showed any antimicrobial activity. Conclusions: In our opinion, dopamine's antibacterial effects may be advantageous for inhibiting the spread of bacterial contamination during the preparation of the infusion solutions. However, it is important that strict guidelines regarding the need for sterile equipment and deliverables be adhered to during all procedures performed in the intensive care units. .


Justificativa y objetivo: Los medicamentos administrados como perfusión intravenosa pueden ser contaminados durante las diversas etapas de producción o preparación. Sin embargo, son muy raros los estudios existentes sobre los efectos antibacterianos de los vasopresores. Este estudio investiga la actividad antimicrobiana in vitro de las formas de vasopresores usados clínicamente. Materiales y métodos: Actividades antimicrobianas in vitro de sustancias vasopresoras de diferentes concentraciones fueron investigadas con el uso de la técnica de microdilución. Los microrganismos usados en el test fueron: Escherichia coli ATCC 25922, Yersinia pseudotuberculosis ATCC 911, Pseudomonas aeruginosa ATCC 10145, Listeria monocytogenes ATCC 43251, Enterococcus faecalis ATCC 29212, Staphylococcus aureus ATCC 25923, Bacillus cereus 702 Roma, Mycobacterium smegmatis ATCC607, Candida albicans ATCC 60193 y Saccharomyces cerevisiae RSKK 251. Los ensayos antibacterianos se hicieron en un caldo de cultivo Mueller-Hinton (pH 7,3) y los ensayos antifúngicos en una solución tapón de base nitrogenada para levadura (pH 7,0). Resultados: Dos preparaciones diferentes de dopamina mostraron actividad antimicrobiana. Ninguna otra sustancia del estudio mostró alguna actividad antimicrobiana. Conclusiones: En nuestra opinión, los efectos antibacterianos de la dopamina pueden ser ventajosos para inhibir la propagación de la contaminación bacteriana durante la preparación de las soluciones para perfusión. Sin embargo, destacamos la importancia del seguimiento riguroso de las directrices de esterilización de los equipos y de asepsia durante todos los procedimientos realizados en las unidades de cuidados intensivos. .


Assuntos
Anti-Infecciosos/farmacologia , Vasoconstritores/farmacologia , Acetilcisteína/farmacologia , Concentração de Íons de Hidrogênio , Técnicas In Vitro , Testes de Sensibilidade Microbiana
18.
R. Inst. Adolfo Lutz ; 72(3): 226-233, 2013.
Artigo em Português | VETINDEX | ID: vti-452562

RESUMO

Many chemicals (alcohol, iodophor, chlorhexidine, etc) are used in laboratories and industries. Unlike disinfectants, no specific norms and criteria have been standardized for evaluating the antiseptics activity. This study analyzed the antimicrobial activity of antiseptics using Time Kill Test (Hobson & Bolsen). This assay assessed the evolution of a population of aerobic microorganisms in a specific period of time when tested against antimicrobial agents. Two different recovery methodologies were evaluated: membrane filtration and pour plate technique The membrane filtration assay was less sensitive. Pour plate technique showed high sensitivity with high colonies counts. Of 25 samples of products analyzed, only the chlorhexidine digluconate-based antiseptics were unsatisfactory, showing no efficacy on all reference micro-organisms strains, and corresponded to 20 % of analyzed samples. However, they were efficacious against clinical strains. Therefore, these products should be used with caution and further studies are needed, as data on its efficacy have still been scarce. These findings might give support to the health surveillance and public health in establishing the future legislation, as these products have been available on the market, but without following any specific legislation.


Inúmeros agentes químicos (álcoois, iodóforos, clorexidina, etc.) são utilizados em laboratórios e indústrias. Ao contrário dos desinfetantes, não há padrões e critérios específicos para avaliar a atividade de antissépticos. Neste trabalho foi estudada a atividade antimicrobiana de antissépticos, utilizando-se o ensaio Time Kill (Hobson & Bolsen), que avalia a população de micro-organismos aeróbios em período de tempo específico, diante de agentes antimicrobianos. Foram avaliadas duas metodologias de recuperação dos micro-organismos: filtração por membrana e semeadura em profundidade. A filtração por membranafoi menos sensível. A semeadura em profundidade demonstrou maior sensibilidade com maior contagem de colônias. De 25 amostras de produtos, os antissépticos à base de digluconato de clorexidina foram insatisfatórios e ineficazes para todas as cepas de micro-organismos de referência, correspondendo a 20% das amostras analisadas. Estes produtos apresentaram-se satisfatórios frente às cepas de origem clínica. Portanto, estes produtos devem ser utilizados com cautela e estudos adicionais são necessários, pois são escassas as informações sobre sua eficácia. Os dados deste estudo poderão auxiliar as ações de vigilância sanitária e de saúde pública na elaboração de futuras legislações, pois estes produtos são encontrados no comércio, mas sem seguir nenhuma legislação específica

19.
Rev. Inst. Adolfo Lutz (Online) ; 72(3): 226-233, 2013. tab, graf
Artigo em Português | LILACS, Sec. Est. Saúde SP, SESSP-CTDPROD, Sec. Est. Saúde SP, SESSP-IALPROD, Sec. Est. Saúde SP | ID: lil-742469

RESUMO

Inúmeros agentes químicos (álcoois, iodóforos, clorexidina, etc.) são utilizados em laboratórios e indústrias.Ao contrário dos desinfetantes, não há padrões e critérios específicos para avaliar a atividade de antissépticos.Neste trabalho foi estudada a atividade antimicrobiana de antissépticos, utilizando-se o ensaio Time Kill (Hobson & Bolsen), que avalia a população de micro-organismos aeróbios em período de tempo específico,diante de agentes antimicrobianos. Foram avaliadas duas metodologias de recuperação dos microorganismos: filtração por membrana e semeadura em profundidade. A filtração por membrana foi menos sensível. A semeadura em profundidade demonstrou maior sensibilidade com maior contagem de colônias.De 25 amostras de produtos, os antissépticos à base de digluconato de clorexidina foram insatisfatórios e ineficazes para todas as cepas de micro-organismos de referência, correspondendo a 20 % das amostras analisadas. Estes produtos apresentaram-se satisfatórios frente às cepas de origem clínica. Portanto, estes produtos devem ser utilizados com cautela e estudos adicionais são necessários, pois são escassas as informações sobre sua eficácia. Os dados deste estudo poderão auxiliar as ações de vigilância sanitária e de saúde pública na elaboração de futuras legislações, pois estes produtos são encontrados no comércio, massem seguir nenhuma legislação específica.


Many chemicals (alcohol, iodophor, chlorhexidine, etc) are used in laboratories and industries. Unlikedisinfectants, no specific norms and criteria have been standardized for evaluating the antiseptics activity.This study analyzed the antimicrobial activity of antiseptics using Time Kill Test (Hobson & Bolsen).This assay assessed the evolution of a population of aerobic microorganisms in a specific period oftime when tested against antimicrobial agents. Two different recovery methodologies were evaluated:membrane filtration and pour plate technique The membrane filtration assay was less sensitive. Pour platetechnique showed high sensitivity with high colonies counts. Of 25 samples of products analyzed, onlythe chlorhexidine digluconate-based antiseptics were unsatisfactory, showing no efficacy on all referencemicro-organisms strains, and corresponded to 20 % of analyzed samples. However, they were efficaciousagainst clinical strains. Therefore, these products should be used with caution and further studies areneeded, as data on its efficacy have still been scarce. These findings might give support to the healthsurveillance and public health in establishing the future legislation, as these products have been availableon the market, but without following any specific legislation.


Assuntos
Anti-Infecciosos Locais , Microbiologia , Produtos com Ação Antimicrobiana , Neutralização de Efluentes
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