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1.
EMBO Rep ; 21(4): e48938, 2020 04 03.
Artigo em Inglês | MEDLINE | ID: mdl-32052574

RESUMO

Intestinal stem cells (ISCs) fuel the lifelong self-renewal of the intestinal tract and are paramount for epithelial repair. In this context, the Wnt pathway component LGR5 is the most consensual ISC marker to date. Still, the effort to better understand ISC identity and regulation remains a challenge. We have generated a Mex3a knockout mouse model and show that this RNA-binding protein is crucial for the maintenance of the Lgr5+ ISC pool, as its absence disrupts epithelial turnover during postnatal development and stereotypical organoid maturation ex vivo. Transcriptomic profiling of intestinal crypts reveals that Mex3a deletion induces the peroxisome proliferator-activated receptor (PPAR) pathway, along with a decrease in Wnt signalling and loss of the Lgr5+ stem cell signature. Furthermore, we identify PPARγ activity as a molecular intermediate of MEX3A-mediated regulation. We also show that high PPARγ signalling impairs Lgr5+ ISC function, thus uncovering a new layer of post-transcriptional regulation that critically contributes to intestinal homeostasis.


Assuntos
Mucosa Intestinal , Células-Tronco , Animais , Intestinos , Camundongos , Organoides , Receptores Acoplados a Proteínas G/genética , Via de Sinalização Wnt
2.
J Bioenerg Biomembr ; 53(2): 157-167, 2021 04.
Artigo em Inglês | MEDLINE | ID: mdl-33683535

RESUMO

The objective of this work was to evaluate the inhibitory effect of quercetin on S. aureus Efflux Pumps. The MIC of Quercetin was evaluated through the broth microdilution method, as well as the Efflux Pump inhibition assay through the method of reducing the antibiotic minimum inhibitory concentration as well as that of ethidium bromide. The in silico approach through bioinformatics was performed to demonstrate the molecular mechanism of interaction of the substrate and the binding cavity. The Quercetin inhibition concentration was not clinically relevant. With respect to the reversal of bacterial resistance effect by efflux pump inhibition, this effect was observed with the strains carrying the TetK and NorA pumps. Regarding the interaction between the Quercetin complex and the NorA pump, the extra stability was provided by hydrogen bonds produced by the hydroxyl group.


Assuntos
Antibacterianos/uso terapêutico , Quercetina/uso terapêutico , Staphylococcus aureus/efeitos dos fármacos , Antibacterianos/farmacologia , Quercetina/farmacologia
3.
Int J Mol Sci ; 22(6)2021 Mar 13.
Artigo em Inglês | MEDLINE | ID: mdl-33805783

RESUMO

In anaerobic bioreactors, the electrons produced during the oxidation of organic matter can potentially be used for the biological reduction of pharmaceuticals in wastewaters. Common electron transfer limitations benefit from the acceleration of reactions through utilization of redox mediators (RM). This work explores the potential of carbon nanomaterials (CNM) as RM on the anaerobic removal of ciprofloxacin (CIP). Pristine and tailored carbon nanotubes (CNT) were first tested for chemical reduction of CIP, and pristine CNT was found as the best material, so it was further utilized in biological anaerobic assays with anaerobic granular sludge (GS). In addition, magnetic CNT were prepared and also tested in biological assays, as they are easier to be recovered and reused. In biological tests with CNM, approximately 99% CIP removal was achieved, and the reaction rates increased ≈1.5-fold relatively to the control without CNM. In these experiments, CIP adsorption onto GS and CNM was above 90%. Despite, after applying three successive cycles of CIP addition, the catalytic properties of magnetic CNT were maintained while adsorption decreased to 29 ± 3.2%, as the result of CNM overload by CIP. The results suggest the combined occurrence of different mechanisms for CIP removal: adsorption on GS and/or CNM, and biological reduction or oxidation, which can be accelerated by the presence of CNM. After biological treatment with CNM, toxicity towards Vibrio fischeri was evaluated, resulting in ≈ 46% detoxification of CIP solution, showing the advantages of combining biological treatment with CNM for CIP removal.


Assuntos
Ciprofloxacina/metabolismo , Elétrons , Nanopartículas de Magnetita/química , Nanotubos de Carbono/química , Esgotos/microbiologia , Poluentes Químicos da Água/metabolismo , Adsorção , Aliivibrio fischeri/efeitos dos fármacos , Aliivibrio fischeri/crescimento & desenvolvimento , Anaerobiose/fisiologia , Biodegradação Ambiental , Reatores Biológicos , Ciprofloxacina/isolamento & purificação , Humanos , Nanopartículas de Magnetita/ultraestrutura , Methanobacterium/metabolismo , Methanobrevibacter/metabolismo , Methanosarcinales/metabolismo , Methanospirillum/metabolismo , Testes de Sensibilidade Microbiana , Nanotubos de Carbono/ultraestrutura , Oxirredução , Poluentes Químicos da Água/isolamento & purificação
4.
Cell Mol Biol (Noisy-le-grand) ; 66(4): 127-132, 2020 Jun 25.
Artigo em Inglês | MEDLINE | ID: mdl-32583777

RESUMO

The aim of this study was to evaluate the antifungal and modulatory potential of the Ziziphus joazeiro bark and leaf extracts, both in isolation and in association with fluconazole, against resistant species from the Candida genus. Antifungal assays were used to determine the half maximal inhibitory concentration (IC50) of the extract in isolation and in combination with fluconazole using the broth microdilution method and spectrophotometric readings, followed by verification of the minimum fungicidal concentration by solid medium subculture. According to the cell viability curve, both extracts inhibited fungal growth in a concentration dependent manner, in addition to showing inhibitory concentrations similar to fluconazole. However, the extracts behaved in a fungistatic manner with minimum inhibitory concentration > 8.19 mg/mL and IC50 values ranging from 0.450 mg/mL to 9 mg/mL. The minimum inhibitory concentration for both extracts decreased when in combination with fluconazole, with the AEL standing out against Candida albicans URM 4387, displaying an IC50 equal to that of fluconazole (0.002 mg/mL). Nevertheless, fluconazole antagonism was observed against the tested strains. Overall, the evaluation of both extracts against Candida spp. presented inhibitory concentration values greater than fluconazole. Moreover, despite these being chemically complex crude extracts, they did demonstrate antifungal effects and properties that concur with their ethno-biological aspect.


Assuntos
Antifúngicos/farmacologia , Metaboloma , Compostos Fitoquímicos/farmacologia , Ziziphus/metabolismo , Antifúngicos/química , Candida/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão , Fluconazol/farmacologia , Concentração Inibidora 50 , Viabilidade Microbiana/efeitos dos fármacos , Compostos Fitoquímicos/química , Extratos Vegetais/farmacologia , Água
5.
Ecotoxicol Environ Saf ; 170: 461-467, 2019 Apr 15.
Artigo em Inglês | MEDLINE | ID: mdl-30553924

RESUMO

The objective of this work was to evaluate the antioxidant, metal chelating and cytoprotective activity of the Eugenia jambolana Lam. extract, as well as of its flavonoid and tannic fractions, against the action of Mercury Chloride (HgCl2). Flavonoids were quantified and an LC-MS chromatographic analysis was performed to identify secondary metabolites. Fe2+ and Fe3+ chelation tests and antioxidant activity were carried out using the FRAP method. Microbiological tests were performed by microdilution to determine the Minimum Inhibitory Concentration (MIC). From these results the Minimum Bactericidal (MBC) and Minimum Fungicide Concentration (MFC) were evaluated. The allelopathy and cytoprotection assays were performed using eukaryotic and prokaryotic models. The results revealed the presence of phenolic acids and flavonoids in the E. jambolana extract and fractions. The sub-allelopathic concentration (64 µg/mL) was used and the results demonstrated the E. jambolana potential cytoprotective effect against mercury chloride.


Assuntos
Produtos Biológicos/química , Cloreto de Mercúrio/toxicidade , Syzygium/química , Alelopatia , Anti-Infecciosos/química , Antioxidantes/química , Citoproteção , Flavonoides/química , Lactuca/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Extratos Vegetais/química
6.
Molecules ; 24(5)2019 Mar 07.
Artigo em Inglês | MEDLINE | ID: mdl-30866456

RESUMO

Multi-spheres adsorptive microextraction using powdered activated carbons (ACs) was studied as a novel enrichment approach, followed by liquid desorption and high-performance liquid chromatography with diode array detection (MSAµE(AC)-LD/HPLC-DAD) to monitor caffeine (CAF) and acetaminophen (ACF) traces in environmental matrices. In this study, commercial activated carbons (N, NOX, and R) were tested, with the latter showing a much better performance for the analysis of both anthropogenic drugs. The main parameters affecting the efficiency of the proposed methodology are fully discussed using commercial AC(R). Textural and surface chemistry properties of the ACs sample were correlated with the analytical results. Assays performed on 30 mL of water samples spiked at 10 µg L-1 under optimized experimental conditions, yielding recoveries of 75.3% for ACF and 82.6% for CAF. The methodology also showed excellent linear dynamic ranges for both drugs with determination coefficients higher than 0.9976, limits of detection and quantification of 0.8⁻1.2 µg L-1 and 2.8⁻4.0 µg L-1, respectively, and suitable precision (RSD < 13.8%). By using the standard addition method, the application of the present method to environmental matrices, including superficial, sea, and wastewater samples, allowed very good performance at the trace level. The proposed methodology proved to be a feasible alternative for polar compound analysis, showing to be easy to implement, reliable, and sensitive, with the possibility to reuse and store the analytical devices loaded with the target compounds for later analysis.


Assuntos
Acetaminofen/isolamento & purificação , Cafeína/isolamento & purificação , Microextração em Fase Sólida/métodos , Água/análise , Adsorção , Carvão Vegetal/química , Cromatografia Líquida de Alta Pressão/métodos , Limite de Detecção , Poluentes Químicos da Água/isolamento & purificação
7.
J Antimicrob Chemother ; 72(2): 511-514, 2017 02.
Artigo em Inglês | MEDLINE | ID: mdl-27834193

RESUMO

OBJECTIVES: To evaluate the relationship between polypharmacy and ART, delivered as conventional multi-tablet three-drug regimens, single-tablet regimens or less-drug regimens (simplified mono or dual regimens). METHODS: We conducted a cross-sectional analysis of electronic data from the prospective Modena HIV Metabolic Clinic Cohort Study. We included the last clinical observation for each patient from January 2006 to December 2015. Polypharmacy was defined as the use of five or more medications (excluding ART). Multi-morbidity was classified as the presence of two or more non-infectious comorbidities. Factors associated with different ART regimens were analysed using multivariable multinomial logistic regression analyses with multi-tablet three-drug regimens as the reference. RESULTS: A total of 2944 patients (33.7% females) were included in the analysis. Multinomial logistic regression analysis identified polypharmacy to be negatively associated with single-tablet regimens [relative risk reduction (RRR) = 0.48, 95% CI = 0.28-0.81] independently from frailty (RRR = 0.68, 95% CI = 0.59-0.78), after correction for age, gender, HIV infection duration, current and nadir CD4 and calendar year. This association was not found comparing multi-tablet three-drug regimens and less-drug regimens. CONCLUSIONS: Single-tablet regimens are less likely to be prescribed in patients with polypharmacy. Single-tablet regimens are perceived to be less flexible in patients with multi-morbidity and at higher risk of drug-drug interaction.


Assuntos
Fármacos Anti-HIV/administração & dosagem , Fármacos Anti-HIV/uso terapêutico , Interações Medicamentosas/fisiologia , Infecções por HIV/tratamento farmacológico , Polimedicação , Envelhecimento , Comorbidade , Estudos Transversais , Feminino , Humanos , Masculino , Adesão à Medicação , Estudos Prospectivos
8.
Molecules ; 19(8): 11988-98, 2014 Aug 11.
Artigo em Inglês | MEDLINE | ID: mdl-25116806

RESUMO

A chiral bis(oxazoline) bearing CH2OH groups was synthesized from a commercial bis(oxazoline) and characterized by 1H- and 13C-NMR, high resolution ESI-mass spectrometry and FTIR. The corresponding copper(II) complex was immobilized onto the surface of a mesoporous carbonaceous material (Starbon® 700) in which the double bonds had been activated via conventional bromination. The materials were characterized by elemental analysis, ICP-OES, XPS, thermogravimetry and nitrogen adsorption at 77 K. The new copper(II) bis(oxazoline) was tested both in the homogeneous phase and once immobilized onto a carbonaceous support for the kinetic resolution of hydrobenzoin. Both were active, enantioselective and selective in the mono-benzoylation of hydrobenzoin, but better enantioselectivities were obtained in the homogeneous phase. The heterogeneous catalyst could be separated from the reaction media at the end of the reaction and reused in another catalytic cycle, but with loss of product yield and enantioselectivity.


Assuntos
Catálise , Complexos de Coordenação/síntese química , Cobre/química , Oxazóis/síntese química , Adsorção , Álcoois/química , Benzoína/análogos & derivados , Benzoína/química , Complexos de Coordenação/química , Cinética , Oxazóis/química , Dióxido de Silício/química , Estereoisomerismo
9.
Redox Biol ; 67: 102917, 2023 11.
Artigo em Inglês | MEDLINE | ID: mdl-37804696

RESUMO

Despite intensive research on peroxisome biochemistry, the role of glutathione in peroxisomal redox homeostasis has remained a matter of speculation for many years, and only recently has this issue started to be experimentally addressed. Here, we summarize and compare data from several organisms on the peroxisome-glutathione topic. It is clear from this comparison that the repertoire of glutathione-utilizing enzymes in peroxisomes of different organisms varies widely. In addition, the available data suggest that the kinetic connectivity between the cytosolic and peroxisomal pools of glutathione may also be different in different organisms, with some possessing a peroxisomal membrane that is promptly permeable to glutathione whereas in others this may not be the case. However, regardless of the differences, the picture that emerges from all these data is that glutathione is a crucial component of the antioxidative system that operates inside peroxisomes in all organisms.


Assuntos
Glutationa , Peroxissomos , Peroxissomos/metabolismo , Glutationa/metabolismo , Antioxidantes/metabolismo , Oxirredução , Homeostase
10.
Geroscience ; 45(4): 2267-2287, 2023 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-36749471

RESUMO

Episodic memory decline is a major signature of both normal and pathological aging. Many neural regions have been implicated in the processes subserving both episodic memory and typical aging decline. Here, we demonstrate that the cerebellum is causally involved episodic memory under aging. We show that a 12-day neurostimulation program delivered to the right cerebellum led to improvements in episodic memory performance under healthy aging that long outlast the stimulation period - healthy elderly individuals show episodic memory improvement both immediately after the intervention program and in a 4-month follow-up. These results demonstrate the causal relevance of the cerebellum in processes associated with long-term episodic memory, potentially highlighting its role in regulating and maintaining cognitive processing. Moreover, they point to the importance of non-pharmacological interventions that prevent or diminish cognitive decline in healthy aging.


Assuntos
Disfunção Cognitiva , Memória Episódica , Humanos , Idoso , Envelhecimento/fisiologia , Cognição , Cerebelo
11.
J Hazard Mater Adv ; 10: 100315, 2023 May.
Artigo em Inglês | MEDLINE | ID: mdl-37193121

RESUMO

The COVID-19 pandemic caused by the SARS-CoV-2 virus led to changes in the lifestyle and human behaviour, which resulted in different consumption patterns of some classes of pharmaceuticals including curative, symptom-relieving, and psychotropic drugs. The trends in the consumption of these compounds are related to their concentrations in wastewater systems, since incompletely metabolised drugs (or their metabolites back transformed into the parental form) may be detected and quantified by analytical methods. Pharmaceuticals are highly recalcitrant compounds and conventional activated sludge processes implemented in wastewater treatment plants (WWTP) are ineffective at degrading these substances. As a results, these compounds end up in waterways or accumulate in the sludge, being a serious concern given their potential effects on ecosystems and public health. Therefore, it is crucial to evaluate the presence of pharmaceuticals in water and sludge to assist in the search for more effective processes. In this work, eight pharmaceuticals from five therapeutic classes were analysed in wastewater and sludge samples collected in two WWTP located in the Northern Portugal, during the third COVID-19 epidemic wave in Portugal. The two WWTP demonstrated a similar pattern with respect to the concentration levels in that period. However, the drugs loads reaching each WWTP were dissimilar when normalising the concentrations to the inlet flow rate. Acetaminophen (ACET) was the compound detected at highest concentrations in aqueous samples of both WWTP (98. 516 µg L - 1 in WWTP2 and 123. 506 µg L - 1in WWTP1), indicating that this drug is extensively used without the need of a prescription, known of general public knowledge as an antipyretic and analgesic agent to treat pain and fever. The concentrations determined in the sludge samples were below 1.65 µg g - 1 in both WWTP, the highest value being found for azithromycin (AZT). This result may be justified by the physico-chemical characteristics of the compound that favour its adsorption to the sludge surface through ionic interactions. It was not possible to establish a clear relationship between the incidence of COVID-19 cases in the sewer catchment and the concentration of drugs detected in the same period. However, looking at the data obtained, the high incidence of COVID-19 in January 2021 is in line with the high concentration of drugs detected in the aqueous and sludge samples but prediction of drug load from viral load data was unfeasible.

12.
Microbiology (Reading) ; 158(Pt 9): 2293-2302, 2012 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-22745270

RESUMO

Although arsenic is notoriously poisonous to life, its utilization in therapeutics brings many benefits to human health, so it is therefore essential to discover the molecular mechanisms underlying arsenic stress responses in eukaryotic cells. Aiming to determine the contribution of Ca(2+) signalling pathways to arsenic stress responses, we took advantage of the use of Saccharomyces cerevisiae as a model organism. Here we show that Ca(2+) enhances the tolerance of the wild-type and arsenic-sensitive yap1 strains to arsenic stress in a Crz1-dependent manner, thus providing the first evidence that Ca(2+) signalling cascades are involved in arsenic stress responses. Moreover, our results indicate that arsenic shock elicits a cytosolic Ca(2+) burst in these strains, without the addition of exogenous Ca(2+) sources, strongly supporting the notion that Ca(2+) homeostasis is disrupted by arsenic stress. In response to an arsenite-induced increase of Ca(2+) in the cytosol, Crz1 is dephosphorylated and translocated to the nucleus, and stimulates CDRE-driven expression of the lacZ reporter gene in a Cnb1-dependent manner. The activation of Crz1 by arsenite culminates in the induction of the endogenous genes PMR1, PMC1 and GSC2. Taken together, these data establish that activation of Ca(2+) signalling pathways and the downstream activation of the Crz1 transcription factor contribute to arsenic tolerance in the eukaryotic model organism S. cerevisiae.


Assuntos
Arsênio/toxicidade , Cálcio/metabolismo , Proteínas de Ligação a DNA/biossíntese , Regulação Fúngica da Expressão Gênica/efeitos dos fármacos , Proteínas de Saccharomyces cerevisiae/biossíntese , Saccharomyces cerevisiae/efeitos dos fármacos , Saccharomyces cerevisiae/metabolismo , Estresse Fisiológico , Fatores de Transcrição/biossíntese , Cátions Bivalentes/metabolismo , Perfilação da Expressão Gênica , Saccharomyces cerevisiae/genética , Ativação Transcricional
13.
Bioinorg Chem Appl ; 2022: 2302943, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35186052

RESUMO

Titanium nanotubes have attractive morphological and physicochemical properties for several applications, such as high surface area, mesoporous structure, good stability, ion exchange capacity, and antibacterial property. Therefore, the field of nanotube applications is increasingly expanding, such as in solar cells sensitized by dye, photocatalysis, and antibacterial activity, among others. Therefore, a study of the antibacterial properties of sodium titanate nanotubes (Na-TiNTs) was carried out together with physicochemical characterizations, such as Raman spectroscopy which shows a peak characteristic of Na-O-Ti from nanotube-agglomerated regions. The XRD diffractogram confirmed the Raman spectra and evidenced the crystalline structure associated to Na-TiNT, which showed the characteristic peaks of the sodium trititanate crystal. SEM and TEM images showed the morphology of hollow nanotubes and forming semispherical particles. EDS shows the percentage values of each of the compounds in the Na-TiNT. The bacterial activity of the Na-TiNT was analyzed in Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa. Na-TiNT modified the activity of the gentamicin and norfloxacin antibiotics against multiresistant strains. Synergistic effects against Gram-positive S. aureus 10 and Gram-negative P. aeruginosa 15 bacteria were observed when the Na-TiNT was associated with gentamicin, reducing the concentration of this antibiotic that is required to inhibit bacterial growth. Another synergic effect was observed for S. aureus 10 with norfloxacin.

14.
J Appl Stat ; 48(11): 1998-2021, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-35706429

RESUMO

Studies of risk perceived using continuous scales of [0,100] were recently introduced in psychometrics, which can be transformed to the unit interval, but the presence of zeros or ones are commonly observed. Motivated by this, we introduce a full inferential set of tools that allows for augmented and limited data modeling. We considered parameter estimation, residual analysis, influence diagnostic and model selection for zero-and/or-one augmented beta rectangular (ZOABR) regression models and their particular nested models, which is based on a new parameterization of the beta rectangular distribution. Different from other alternatives, we performed maximum-likelihood estimation using a combination of the EM algorithm (for the continuous part) and Fisher scoring algorithm (for the discrete part). Also, we perform an additional step, by considering other link functions, besides the usual logistic link, for modeling the response mean. By considering randomized quantile residuals, (local) influence diagnostics and model selection tools, we identified that the ZOABR regression model is the best one. We also conducted extensive simulations studies, which indicate that all developed tools work properly. Finally, we discuss the use of this type of models to treat psychometric data. It is worthwhile to mention that applications of the developed methods go beyond to Psychometric data. Indeed, they can be useful when the response variable in bounded, including or not the respective limits.

15.
Eur J Med Chem ; 174: 87-115, 2019 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-31029947

RESUMO

Given their therapeutic activity, natural products have been used in traditional medicines throughout the centuries. The growing interest of the scientific community in phytopharmaceuticals, and more recently in marine products, has resulted in a significant number of research efforts towards understanding their effect in the treatment of neurodegenerative diseases, such as Alzheimer's (AD), Parkinson (PD) and Huntington (HD). Several studies have shown that many of the primary and secondary metabolites of plants, marine organisms and others, have high affinities for various brain receptors and may play a crucial role in the treatment of diseases affecting the central nervous system (CNS) in mammalians. Actually, such compounds may act on the brain receptors either by agonism, antagonism, allosteric modulation or other type of activity aimed at enhancing a certain effect. The current manuscript comprehensively reviews the state of the art on the interactions between natural compounds and brain receptors. This information is of foremost importance when it is intended to investigate and develop cutting-edge drugs, more effective and with alternative mechanisms of action to the conventional drugs presently used for the treatment of neurodegenerative diseases. Thus, we reviewed the effect of 173 natural products on neurotransmitter receptors, diabetes related receptors, neurotrophic factor related receptors, immune system related receptors, oxidative stress related receptors, transcription factors regulating gene expression related receptors and blood-brain barrier receptors.


Assuntos
Produtos Biológicos/metabolismo , Encéfalo/efeitos dos fármacos , Encéfalo/metabolismo , Fármacos Neuroprotetores/metabolismo , Receptores de Superfície Celular/metabolismo , Animais , Produtos Biológicos/química , Produtos Biológicos/toxicidade , Humanos , Ligantes , Fármacos Neuroprotetores/química , Fármacos Neuroprotetores/toxicidade , Receptores de Superfície Celular/química
16.
J Hazard Mater ; 370: 54-62, 2019 05 15.
Artigo em Inglês | MEDLINE | ID: mdl-29602643

RESUMO

This study aimed to verify the chelating, antioxidant and cytoprotective activities of Psidium brownianum Mart. Ex DC against mercury and aluminum. The ethanolic extract, as well as the tannic and flavonoid fractions, were prepared and subjected to liquid chromatography-mass spectrometry analysis. Ferric ion reduction and antioxidant activity measurement using the FRAP method were performed with P. brownianum. After determining the sub-allelopathic doses, germination tests using Lactuca sativa (lettuce) seeds were performed. The main compounds identified in the extract and fractions were: quercetin and its derivatives; myricetin and its derivatives; gallic acid; ellagic acid; quinic acid and gallocatechin. The Minimum Inhibitory Concentration (MIC) for all samples were ≥ 1024 µg/mL. The flavonoid fraction in association with mercury chloride demonstrated cytoprotection (p < 0.001). The sub-allelopathic concentration used was 64 µg/mL. The extract and fractions were cytoprotective for radicles and caulicles when assayed in association with mercury and against aluminum for radicles. This suggests that the P. brownianum extract and its fractions present cytoprotective activity, possibly related to the antioxidant effect of secondary metabolites, especially flavonoids.


Assuntos
Cloreto de Alumínio/toxicidade , Antioxidantes/farmacologia , Quelantes/farmacologia , Cloreto de Mercúrio/toxicidade , Extratos Vegetais/farmacologia , Psidium , Alelopatia , Antioxidantes/química , Candida albicans/efeitos dos fármacos , Candida albicans/crescimento & desenvolvimento , Quelantes/química , Cromatografia Líquida , Citoproteção , Escherichia coli/efeitos dos fármacos , Escherichia coli/crescimento & desenvolvimento , Flavonoides/análise , Flavonoides/farmacologia , Germinação/efeitos dos fármacos , Ferro/química , Lactuca/efeitos dos fármacos , Lactuca/crescimento & desenvolvimento , Espectrometria de Massas , Extratos Vegetais/química
17.
Chemosphere ; 216: 785-793, 2019 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-30391901

RESUMO

The present study had as its objective to verify the Psidium guajava var. Pomifera L. chelating, antioxidant and cytoprotective effects against mercury and aluminum. The ethanolic extract, tannic and flavonoid fractions were subjected to LC-MS analysis. The Ferric Reducing Antioxidant Power (FRAP) and ferric ion reduction demonstrated a present antioxidant activity. The fungicidal and bactericidal activity of these metals were established. After determining the sub-allelopathic doses, germination tests using Lactuca sativa were performed. Quercetin and its derivatives were the main compounds identified in the extract and the fractions. Mercury chloride significantly reduced the bactericidal effect of the flavonoid fraction (p < 0.001). None of the fractions were cytoprotective against mercury or aluminum in the fungal model assays. Using a sub-allelopathic concentration (64 µg/mL), the ethanolic extract, flavonoid and tannic fractions were found to be cytoprotective against aluminum for radicles, however only the tannic fraction was cytoprotective for caulicles. These data suggest that natural P. guajava products are promising cytoprotective compound sources. This activity may be related to the antioxidant effect of secondary metabolites, mainly flavonoids. Our results point to a potential for environmental intervention product and technique development aimed at mitigating contamination by toxic metals such as mercury and aluminum.


Assuntos
Antioxidantes/química , Flavonoides/química , Metais Pesados/toxicidade , Psidium/química , Antioxidantes/análise , Metais Pesados/análise
18.
Eur J Pharm Sci ; 128: 158-161, 2019 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-30508582

RESUMO

With the increase in bacterial resistance to antibiotics, many studies have been directed towards finding new agents with antibacterial activity, such as studies with natural products. These products can have antibacterial activity such as d-limonene as described in the literature. The aim of this study was to evaluate the antibacterial activity of d-limonene, isolated and complexed with ß-cyclodextrin, and to evaluate its potentiating activity of different antibiotic classes. Antibacterial activity was determined by the broth microdilution method, obtaining in this way the Minimal Inhibitory Concentration (MIC), with the antibiotic modulatory activity being obtained using a sub-inhibitory concentration (MIC/8). d-Limonene showed a MIC equal to 256 µg/mL against standard S. aureus and 512 µg/mL against resistant P. aeruginosa. In the gentamicin modulatory activity, the isolated d-limonene presented synergism against S. aureus and E. coli bacteria. Thus, d-limonene showed relevant clinical antibacterial activity, for both Gram-positive and Gram-negative bacteria as well as a synergistic effect when associated with gentamicin. These results are promising in the combat against bacterial resistance, however further studies are needed to better elucidate the mechanisms of action.


Assuntos
Antibacterianos/farmacologia , Limoneno/química , Limoneno/farmacologia , beta-Ciclodextrinas/química , Bactérias/efeitos dos fármacos
19.
PLoS One ; 12(9): e0184936, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-28957342

RESUMO

This paper describes a simple in-situ process of synthesizing highly dispersed palladium nanoparticles (PdNPs) using aqueous leaf extract of GarciniapedunculataRoxb as bio-reductant and starch (0.3%) as bio-stabilizer. The PdNPs are characterized by techniques like FTIR, TEM, SEM-EDX, XRD and XPS analysis. It is worthnoting thatwhen the synthesis of nanoparticles was carried out in absence of starch, agglomeration of particles has been noticed.The starch-assisted PdNPs showed excellent aqueous-phase catalytic activities for three important reactions: the Suzuki-Miyaura cross-coupling reactions of aryl halides (aryl bromides and iodides) with arylboronic acids; selective oxidations of alcohols to corresponding carbonyl compounds; and reduction of toxic Cr(VI) to nontoxic Cr(III). Our catalyst could be reused up to four cycles without much compromising with its activity. Furthermore, the material also demonstrated excellent antimicrobial and anti-biofilm activities against a novel multidrug resistant clinical bacterial isolate Cronobactersakazakii strain AMD04. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of PdNPswere found to be 0.06 and 0.12 mM respectively.


Assuntos
Anti-Infecciosos/farmacologia , Garcinia/química , Nanopartículas Metálicas/química , Paládio/farmacologia , Álcoois/metabolismo , Bactérias/efeitos dos fármacos , Bactérias/isolamento & purificação , Biofilmes/efeitos dos fármacos , Catálise , Cromo/metabolismo , Farmacorresistência Bacteriana Múltipla/efeitos dos fármacos , Nanopartículas Metálicas/ultraestrutura , Testes de Sensibilidade Microbiana , Oxirredução , Difração de Raios X
20.
Biomed Pharmacother ; 89: 201-207, 2017 May.
Artigo em Inglês | MEDLINE | ID: mdl-28226293

RESUMO

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/farmacologia
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