RESUMO
The present study aimed to investigate the antibacterial and modulatory activities of (+)-ß-citronellol (ßCT), ß-cyclodextrin (ß-CD), and their complex ßCT/ß-CD and characterize them using infrared spectroscopy. Infrared spectra were recorded in the 750-4000 cm-1 region. The antibacterial effects of these compounds and their modulatory-antibiotic activities were determined using the minimum inhibitory concentration (MIC) test. Signatures of these pure compounds were detected in the infrared spectrum of the ßCT/ß-CD complex. The MIC of the ßCT/ß-CD complex against the tested strains was found to be 1024 µg/mL. The antagonistic and synergistic effects of these compounds were also observed using the modulation tests. ßCT or ß-CD alone did not exhibit any direct antibacterial activity. However, the ßCT/ß-CD complex in combination with gentamicin showed a synergistic effect against E. coli.
Assuntos
Escherichia coli , beta-Ciclodextrinas , Monoterpenos Acíclicos , Antibacterianos/farmacologia , Testes de Sensibilidade Microbiana , Staphylococcus aureus , beta-Ciclodextrinas/farmacologiaRESUMO
INTRODUCTION: Staphylococcus aureus represents the most common etiologic agent of purulent infections, affecting humans and animals. Escherichia coli is one of the principal causes of infectious diseases, mainly diarrheal diseases due to enterotoxin action. There are many reports indicating that these bacteria are multidrug-resistant (MDR) pathogens. OBJECTIVE: In this study, we investigated the antimicrobial and modulatory activities of 5-hydroxy-3,7,4'-trimethoxyflavone (VG.EF.CLII) against E. coli and S. aureus strains. METHODS: 5-Hydroxy-3,7,4'-trimethoxyflavone was isolated from Vitex gardneriana Schauer leaves and structurally characterized using nuclear magnetic resonance. The antibacterial effect of VG.EF.CLII and modulation of antibiotic activity, both determined by minimum inhibitory concentration, were assessed using microtiter plates. RESULTS: VG.EF.CLII showed bacterial growth inhibition at concentrations ≤512 µg/mL, and synergistic effects were observed for the modulation of two distinct antibiotic classes (the fluoroquinolone norfloxacin and the aminoglycoside gentamicin). CONCLUSION: 5-Hydroxy-3,7,4'-trimethoxyflavone isolated from V. gardneriana showed promising antimicrobial activity against MDR bacterial strains S. aureus 358 and E. coli 27 when associated with the antibiotics norfloxacin and gentamicin. Therefore, this natural product can contribute to the control of bacterial resistance.
Assuntos
Antibacterianos/química , Flavonoides/química , Extratos Vegetais/química , Folhas de Planta/química , Vitex/química , Antibacterianos/farmacologia , Farmacorresistência Bacteriana Múltipla/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Flavonoides/farmacologia , Testes de Sensibilidade Microbiana/métodos , Extratos Vegetais/farmacologia , Staphylococcus aureus/efeitos dos fármacosRESUMO
In this study, we report the antibacterial activity and modulation of antibiotic activity by Fe2(MoO4)3 microstructures obtained by the hydrothermal route without use of surfactants or organic additives. This material was characterized by X-ray diffraction (XRD), Raman spectroscopy and scanning electron microscopy (SEM) images. The XRD pattern showed that the Fe2(MoO4)3 crystallize in a monoclinic structure without secondary phases. Raman spectroscopy confirms the formation of Fe2(MoO4)3. SEM images show that the Fe2(MoO4)3 obtained have ball-of-yarn shaped morphology. In the antibacterial assays, strains of Escherichia coli, Pseudomonas aeruginosa and Staphylococcus aureus were assayed by microdilution method to evaluate the antibacterial and modulatory-antibiotic activity with antibiotics as gentamicin, norfloxacin and imipenem. Against all bacteria, the Minimum Inhibitory Concentration (MIC) was Fe2(MoO4)3â¯≥â¯1024⯵g/mL. This high MIC result must be associated with the fact of the iron be an essential microelement to the bacterial growth. However, when the Fe2(MoO4)3 was assayed in association with the antibiotics was observed an antagonistic effect demonstrated by an enhance of the MIC. This fact is associated directly with the pro-oxidative properties of metallic oxides. These compounds enhance the production of free radicals, as H2O2 and superoxide ions that can affect the cell structures as cell membrane and cell wall. Other effect is associated with the possible coordination of the metal, performing bonds with the chemical structure of the antibiotics, reducing their activity. Our results indicated that nanocompounds as Fe2(MoO4)3 can not be used as antimicrobial products for clinical usage, neither directly and neither in association with antibiotics.
Assuntos
Antibacterianos/farmacologia , Compostos Férricos/farmacologia , Molibdênio/farmacologia , Nanopartículas , Antibacterianos/química , Antibacterianos/toxicidade , Química Farmacêutica/métodos , Cristalização , Composição de Medicamentos , Farmacorresistência Bacteriana Múltipla , Escherichia coli/efeitos dos fármacos , Escherichia coli/crescimento & desenvolvimento , Compostos Férricos/química , Compostos Férricos/toxicidade , Testes de Sensibilidade Microbiana , Estrutura Molecular , Molibdênio/química , Molibdênio/toxicidade , Oxirredução , Pseudomonas aeruginosa/efeitos dos fármacos , Pseudomonas aeruginosa/crescimento & desenvolvimento , Staphylococcus aureus/efeitos dos fármacos , Staphylococcus aureus/crescimento & desenvolvimento , Relação Estrutura-AtividadeRESUMO
Cyclodextrins (CDs) have been used as important pharmaceutical excipients for improve the physicochemical properties of the drugs of low solubility as the essential oil of Hyptis martiusii. This oil is important therapeutically, but the low solubility and bioavailability compromises your use. Therein, the aim of this study was to obtain and to characterize physico-chemically the samples obtained by physical mixture (PM), paste complexation (PC) and slurry complexation (SC) of the essential oil Hyptis martiusii (EOHM) in ß-CD, and to compare the antibacterial and modulatory-antibiotic activity of products obtained and oil free. The physicochemical characterization was performed by differential scanning calorimetry (DSC), thermogravimetry/derivative thermogravimetry (TG/DTG), scanning electron microscopy (SEM), X-ray diffraction (XRD) and Karl Fischer titration. Additionally, the antibacterial tests were performed by microdilution technique. Thus, it was observed that the PM method showed low complexing capacity, unlike PC and SC in which it was observed the formation of inclusion complexes. In addition, the second stage of the TG/DTG curves showed that SC was the best method inclusion with mass loss of 6.9% over the PC that was 6.0%. The XRD results corroborate with the results above suggesting the formation of new solid phase and the SEM photomicrographs showed the porous surface of the samples PC and SC. The essential oil alone demonstrated an antibacterial and modulatory effect against the S. aureus and the Gram negative strain, respectively. However, the ß-CD and the inclusion complex did not demonstrate any biological activity in the performed antibacterial assays.
Assuntos
Antibacterianos/química , Hyptis/química , Óleos Voláteis/química , beta-Ciclodextrinas/química , Antibacterianos/farmacologia , Varredura Diferencial de Calorimetria/métodos , Ciclodextrinas/química , Ciclodextrinas/farmacologia , Composição de Medicamentos/métodos , Bactérias Gram-Negativas/efeitos dos fármacos , Óleos Voláteis/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Solubilidade , Espectroscopia de Infravermelho com Transformada de Fourier/métodos , Staphylococcus aureus/efeitos dos fármacos , Difração de Raios X/métodos , beta-Ciclodextrinas/farmacologiaRESUMO
CONTEXT: Ethnozoological studies have shown that Spilotes pullatus Linn. (Colubridae: Ophidia), is associated with medicinal and magic-religious uses in Brazil. OBJECTIVES: This study was designed to determine the chemical composition of the oil extracted from the body fat of S. pullatus and to test its antimicrobial properties, alone and in association with aminoglycosides, against fungi and bacterial strains in concentrations ranging between 1024 and 0.5 µg/mL. MATERIAL AND METHODS: The snakes were collected in the Chapada do Araripe, county of Crato, Ceará State, Brazil. The oil was extracted in a Soxhlet apparatus using hexane. The methyl esters of the fatty acids present in the samples were identified using GC-MS. The antimicrobial and drug modulatory activities of oil were tested by microdilution against fungal and bacterial strains. RESULTS: The chemical composition of the fixed oils of S. pullatus identified 10 constituents representing 94.97% of the total sample. The percentages of saturated and unsaturated fatty acids were 33.59 and 61.38%, respectively, with the most abundant components being elaidic (37.26%). The oil did not demonstrate any antimicrobial or antifungal activity when tested alone, presenting MIC values ≥ 1024 µg/mL. However, when associated with antibiotics, it demonstrated synergistic effects with gentamicin against all the bacterial lineages assayed, and antagonistic effects with amikacin and neomycin against strains of Escherichia coli. CONCLUSIONS: Oil extracted from the body fat of S. pullatus did not demonstrate any inhibitory effects on bacterial or fungal activities, but was effective in modulating the effects of certain antibiotics.