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1.
Microb Pathog ; 131: 128-134, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-30959097

RESUMO

Quorum sensing (QS) is the cell density dependent communication network which coordinates the production of pathogenic determinants in majority of pathogenic bacteria. Pseudomonas aeruginosa causes hospital-acquired infections by virtue of its well-defined QS network. As the QS regulatory network in P. aeruginosa regulates the virulence determinants and antibiotic resistance, attenuating the QS system seems to be influential in developing next-generation anti-infective agents. In the current study, the QS attenuation potential of a flavonoid, mosloflavone was investigated against P. aeruginosa virulence and biofilm formation. Mosloflavone inhibited the pyocyanin production, LasB elastase and chitinase by 59.52 ±â€¯2.74, 35.90 ±â€¯4.34 and 61.18 ±â€¯5.52% respectively. The QS regulated biofilm formation and development was also reduced when supplemented with sub-MIC of mosloflavone. The gene expression studies of mosloflavone using RT-PCR depicted its ability to down-regulate the expression levels of QS regulated virulence genes such as lasI (60.64%), lasR (91.70%), rhlI (57.30%), chiC (90.20%), rhlA (47.87%), rhlR (21.55%), lasB (37.80%), phzM (42.40%), toxA (61.00%), aprA (58.4%), exoS (78.01%), algD (46.60%) and pelA (50.45%). The down-regulation of QS virulence phenotypes by mosloflavone could be attributed to its binding affinity with the QS regulatory proteins, LasR and RhlR by competitively inhibiting the binding of natural autoinducers as evidenced from simulation studies. Mosloflavone also exhibited promising potential in controlling bacterial infection in Caenorhabditis elegans model system, in vivo. The anti-biofilm and anti-QS potential of mosloflavone in the current study illustrated the candidature of mosloflavone as a promising biocide.


Assuntos
Antibacterianos/farmacologia , Biofilmes/efeitos dos fármacos , Flavonoides/farmacologia , Fenótipo , Pseudomonas aeruginosa/efeitos dos fármacos , Percepção de Quorum/efeitos dos fármacos , Alginatos , Animais , Proteínas de Bactérias/genética , Biofilmes/crescimento & desenvolvimento , Caenorhabditis elegans , Quitinases/metabolismo , Modelos Animais de Doenças , Regulação Bacteriana da Expressão Gênica/efeitos dos fármacos , Glicolipídeos/metabolismo , Interações Hidrofóbicas e Hidrofílicas , Metaloendopeptidases/genética , Testes de Sensibilidade Microbiana , Pseudomonas aeruginosa/genética , Piocianina/metabolismo , Transativadores/genética , Virulência/efeitos dos fármacos , Virulência/genética , Fatores de Virulência/genética
2.
Int J Med Mushrooms ; 20(6): 569-580, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29953353

RESUMO

Wild edible mushrooms are one of the most fascinating nutraceuticals because of their pleasant texture, peculiar aroma, and tremendous therapeutic potential; they have been used since ancient times. In this study we evaluated the antioxidant potential of 4 wild edible mushrooms-Cantharellus tropicalis, C. cibarius, Lentinus edodes, and Russula delica-collected from Mizoram, India. We performed in vitro and in vivo studies using a Saccharomyces cerevisiae stress response mechanism as the model system. Among the 4 mushrooms, C. cibarius exhibited the most significant antioxidant activity both in vitro and in vivo, followed by L. edodes, R. delica, and C. tropicalis. Gas chromatography-mass spectrometry analysis of methanolic extracts of the mushrooms revealed the presence of substantial amounts of fatty acids, fatty acid esters, and other bioactive constituents. The in vitro antioxidant activity was corroborated by in vivo studies using an S. cerevisiae oxidative stress response mechanism. In spot assays, the C. cibarius methanolic extract showed the highest scavenging potential in wild and mutant (sodlΔ and tsalΔ) strains of S. cerevisiae. These results were confirmed further by determining the level of reactive oxygen species through the use of fluorescent microscopy and intensity studies. The results suggested the efficacy of wild edible mushrooms as prominent therapeutic agents and that they have tremendous nutraceutical properties.


Assuntos
Agaricales/química , Antioxidantes/metabolismo , Dieta , Saccharomyces cerevisiae/metabolismo , Agaricales/metabolismo , Antioxidantes/química , Antioxidantes/isolamento & purificação , Ácidos Graxos/análise , Sequestradores de Radicais Livres/metabolismo , Cromatografia Gasosa-Espectrometria de Massas , Índia , Oxirredução/efeitos dos fármacos , Estresse Oxidativo/efeitos dos fármacos , Espécies Reativas de Oxigênio/análise , Verduras/química , Verduras/metabolismo
3.
J Environ Biol ; 37(2): 267-74, 2016 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-27097447

RESUMO

The ability of dried bacterial biomass in azo dye and heavy metal removal from aqueous solution was explored. Biosorption of three textile dyes, Eriochrome black T (EBT), Acid Red 26 (AR) and Trypan blue (TB) and heavy metals (Pb and Cr) by dried biomass of Aeromonas hydrophila RC1, was investigated in a batch system under various parameters such as dye concentration, contact time, concentration of biomass, pH, and temperature. The experimental results showed that the extent of biosorption for dyes increased with increase in initial concentration of dyes, biomass concentration, contact time, temperature and decreased with increase in pH. The experimental isotherms data were analyzed using Langmuir and Freundlich isotherm equations. The Langmuir model yielded good fit to the experimental data (R² approximately 0.794, 0.844 and 0.969 for the dyes, EBT, AR and TB, respectively) with maximum monolayer adsorption capacity of 58.8 mg g⁻¹ for AR. Similarly results were obtained for heavy metals and the data fit in Langmuir model (R² value of 0.849 and 0.787) with q(m) value of 40 mg g⁻¹ for Pb. The results fit in pseudo first order kinetics with removal upto 96.67 % for Pb. Involvement of the surface characteristics of the biomass in biosorption was studied using scanning electron micrographs, FTIR, EDX and XRD analysis. Thus, use ofA. hydrophila RC1 biomass can be extensively employed in water treatment plants in order to get desired water quality in the most economical way.


Assuntos
Aeromonas hydrophila/química , Corantes/química , Metais/química , Adsorção , Biomassa , Fenômenos Químicos , Concentração de Íons de Hidrogênio , Propriedades de Superfície , Temperatura , Indústria Têxtil , Eliminação de Resíduos Líquidos/métodos , Poluentes Químicos da Água/química
4.
Bioorg Med Chem Lett ; 24(17): 4239-42, 2014 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-25096298

RESUMO

A series of novel 10-((1H-indol-3-yl)methylene)-7-aryl-7,10-dihydro-5H-benzo[h]thiazolo[2,3-b]quinazolin-9(6H)-ones (8a-t) have been synthesized in good yields by the reaction of benzo[h]quinazoline-2(1H)-thiones (4a-f) with 2-chloro-N-phenylacetamide (5) followed by Knoevenagel condensation with various indole-3-carbaldehydes (7a-d) under conventional method. All the synthesized compounds were characterized by spectral studies and screened for their in vitro anticancer and antimicrobial activities. Compound 8c has exhibited excellent activity against MCF-7 (breast cancer cell line) than the standard drug Doxorubicin. Compound 8d against both the cancer cell lines, 8q against MCF-7 and 8c, 8h against HepG2 have also shown good activity. Remaining compounds have shown moderate activity against both the cell lines. Antimicrobial activity revealed that, the compound 8q and 8t against Staphylococcus aureus and 8i, 8k, 8l, 8q &8t against Klebsiella pneumoniae have shown equipotent activity on comparing with the standard drug Streptomycin. Remaining compounds have shown significant antibacterial and comparable antifungal activities against all the tested microorganisms.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Antineoplásicos/farmacologia , Compostos Heterocíclicos de 4 ou mais Anéis/farmacologia , Quinazolinas/farmacologia , Tiazóis/farmacologia , Antibacterianos/síntese química , Antibacterianos/química , Antifúngicos/síntese química , Antifúngicos/química , Antineoplásicos/síntese química , Antineoplásicos/química , Aspergillus/efeitos dos fármacos , Candida/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Células Hep G2 , Compostos Heterocíclicos de 4 ou mais Anéis/síntese química , Compostos Heterocíclicos de 4 ou mais Anéis/química , Humanos , Klebsiella pneumoniae/efeitos dos fármacos , Células MCF-7 , Testes de Sensibilidade Microbiana , Conformação Molecular , Pseudomonas aeruginosa/efeitos dos fármacos , Quinazolinas/síntese química , Quinazolinas/química , Staphylococcus/efeitos dos fármacos , Relação Estrutura-Atividade , Tiazóis/síntese química , Tiazóis/química
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