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1.
AAPS PharmSciTech ; 25(5): 94, 2024 May 06.
Artigo em Inglês | MEDLINE | ID: mdl-38710898

RESUMO

This study introduces and assesses the potential of a Luliconazole-loaded nanofiber (LUL-NF) patch, fabricated through electrospinning, for enhancing topical drug delivery. The primary objectives involve evaluating the nanofiber structure, characterizing physical properties, determining drug loading and release kinetics, assessing antifungal efficacy, and establishing the long-term stability of the NF patch. LUL-NF patches were fabricated via electrospinning and observed by SEM at approximately 200 nm dimensions. The comprehensive analysis included physical properties (thickness, folding endurance, swelling ratio, weight, moisture content, and drug loading) and UV analysis for drug quantification. In vitro studies explored sustained drug release kinetics, while microbiological assays evaluated antifungal efficacy against Candida albicans and Aspergillus Niger. Stability studies confirmed long-term viability. Comparative analysis with the pure drug, placebo NF patch, LUL-NF patch, and Lulifod gel was conducted using agar diffusion, revealing enhanced performance of the LUL-NF patch. SEM analysis revealed well-defined LUL-NF patches (0.80 mm thickness) with exceptional folding endurance (> 200 folds) and a favorable swelling ratio (12.66 ± 0.73%). The patches exhibited low moisture uptake (3.4 ± 0.09%) and a moisture content of 11.78 ± 0.54%. Drug loading in 1 cm2 section was 1.904 ± 0.086 mg, showing uniform distribution and sustained release kinetics in vitro. The LUL-NF patch demonstrated potent antifungal activity. Stability studies affirmed long-term stability, and comparative analysis highlighted increased inhibition compared to a pure drug, LUL-NF patch, and a commercial gel. The electrospun LUL-NF patch enhances topical drug delivery, promising extended therapy through single-release, one-time application, and innovative drug delivery strategies, supported by thorough analysis.


Assuntos
Antifúngicos , Aspergillus niger , Candida albicans , Sistemas de Liberação de Medicamentos , Liberação Controlada de Fármacos , Imidazóis , Nanofibras , Antifúngicos/administração & dosagem , Antifúngicos/farmacologia , Antifúngicos/química , Nanofibras/química , Candida albicans/efeitos dos fármacos , Aspergillus niger/efeitos dos fármacos , Sistemas de Liberação de Medicamentos/métodos , Imidazóis/química , Imidazóis/administração & dosagem , Imidazóis/farmacologia , Preparações de Ação Retardada , Testes de Sensibilidade Microbiana/métodos , Portadores de Fármacos/química , Estabilidade de Medicamentos
2.
Int J Food Microbiol ; 417: 110710, 2024 Jun 02.
Artigo em Inglês | MEDLINE | ID: mdl-38643598

RESUMO

Postharvest loss caused by a range of pathogens necessitates exploring novel antifungal compounds that are safe and efficient in managing the pathogens. This study evaluated the antifungal activity of ethyl ferulate (EF) and explored its mechanisms of action against Alternaria alternata, Aspergillus niger, Botrytis cinerea, Penicillium expansum, Penicillium digitatum, Geotrichum candidum and evaluated its potential to inhibit postharvest decay. The results demonstrated that EF exerts potent antifungal activity against a wide board of postharvest pathogens. Results also revealed that its antifungal mechanism is multifaceted: EF may be involved in binding to and disturbing the integrity of the fungal plasma membrane, causing leakage of intracellular content and losing normal morphology and ultrastructure. EF also induced oxidative stress in the pathogen, causing membrane lipid peroxidation and malondialdehyde accumulation. EF inhibited the critical gene expression of the pathogen, affecting its metabolic regulation, antioxidant metabolism, and cell wall degrading enzymes. EF exhibited antifungal inhibitory activity when applied directly into peel wounds or after incorporation with chitosan coating. Due to its wide board and efficient antifungal activity, EF has the potential to provide a promising alternative to manage postharvest decay.


Assuntos
Antifúngicos , Botrytis , Ácidos Cafeicos , Penicillium , Penicillium/efeitos dos fármacos , Penicillium/metabolismo , Antifúngicos/farmacologia , Botrytis/efeitos dos fármacos , Ácidos Cafeicos/farmacologia , Alternaria/efeitos dos fármacos , Aspergillus niger/efeitos dos fármacos , Conservação de Alimentos/métodos , Geotrichum/efeitos dos fármacos , Fungos/efeitos dos fármacos , Microbiologia de Alimentos , Frutas/microbiologia , Estresse Oxidativo/efeitos dos fármacos
3.
World J Microbiol Biotechnol ; 40(6): 175, 2024 Apr 22.
Artigo em Inglês | MEDLINE | ID: mdl-38647735

RESUMO

The demand for environment-friendly cleanup techniques has arisen due to an increase in environmental pollutants. Fungi is the most prevalent and effective class of heavy metal-resistant microorganisms with the ability to leach metals. The objective of the present study was to isolate the fungi from the agricultural soil of Kashmir valley, investigate their multi-metal tolerance to heavy metals and evaluate the metal uptake capacities of the resistant fungi. The fungi were isolated and identified on the basis of morphological and molecular approach (ITS1 and ITS4). The tolerance limits of the isolated fungal strains to various doses of lead (Pb), cadmium (Cd), zinc (Zn), chromium (Cr), copper (Cu), nickel (Ni), and cobalt (Co) was evaluated. Five fungal strains, Aspergillus niger, Fusarium oxysporum, Fusarium verticillioides, Aspergillus fischeri, Epicoccum mackenziei were isolated from the soil samples. To the best of our knowledge, this is the first report on the study of metal resistance of Aspergillus fischeri and Epicoccum mackenziei. Among the identified fungal species, Aspergillus niger and Fusarium oxysporum were found to be most tolerant with a minimum inhibitory concentration (MIC) of 600 ppm against Cu and Cr respectively. Results indicated removal of considerable amount of heavy metals by some of the fungi. The highest metal uptake of 8.31 mg/g was found in Fusarium verticillioides for Zn. Surprisingly, these fungal strains demonstrated resistance to metal concentrations above the levels that are universally acceptable for polluted soils, and hence prove to be appealing contenders for use as bioremediation agents for cleaning up heavy metal-polluted environments.


Assuntos
Fungos , Fusarium , Metais Pesados , Testes de Sensibilidade Microbiana , Microbiologia do Solo , Poluentes do Solo , Metais Pesados/metabolismo , Poluentes do Solo/metabolismo , Fungos/efeitos dos fármacos , Fungos/isolamento & purificação , Fungos/classificação , Fungos/metabolismo , Fusarium/isolamento & purificação , Fusarium/efeitos dos fármacos , Fusarium/metabolismo , Biodegradação Ambiental , Aspergillus niger/isolamento & purificação , Aspergillus niger/efeitos dos fármacos , Aspergillus niger/metabolismo , Solo/química , Aspergillus/efeitos dos fármacos , Aspergillus/metabolismo , Aspergillus/isolamento & purificação
4.
Int J Food Microbiol ; 417: 110685, 2024 Jun 02.
Artigo em Inglês | MEDLINE | ID: mdl-38579546

RESUMO

Cinnamaldehyde displays strong antifungal activity against fungi such as Aspergillus niger, but its precise molecular mechanisms of antifungal action remain inadequately understood. In this investigation, we applied chemoproteomics and bioinformatic analysis to unveil the target proteins of cinnamaldehyde in Aspergillus niger cells. Additionally, our study encompassed the examination of cinnamaldehyde's effects on cell membranes, mitochondrial malate dehydrogenase activity, and intracellular ATP levels in Aspergillus niger cells. Our findings suggest that malate dehydrogenase could potentially serve as an inhibitory target of cinnamaldehyde in Aspergillus niger cells. By disrupting the activity of malate dehydrogenase, cinnamaldehyde interferes with the mitochondrial tricarboxylic acid (TCA) cycle, leading to a significant decrease in intracellular ATP levels. Following treatment with cinnamaldehyde at a concentration of 1 MIC, the inhibition rate of MDH activity was 74.90 %, accompanied by an 84.5 % decrease in intracellular ATP content. Furthermore, cinnamaldehyde disrupts cell membrane integrity, resulting in the release of cellular contents and subsequent cell demise. This study endeavors to unveil the molecular-level antifungal mechanism of cinnamaldehyde via a chemoproteomics approach, thereby offering valuable insights for further development and utilization of cinnamaldehyde in preventing and mitigating food spoilage.


Assuntos
Acroleína , Acroleína/análogos & derivados , Antifúngicos , Aspergillus niger , Proteínas Fúngicas , Malato Desidrogenase , Acroleína/farmacologia , Aspergillus niger/efeitos dos fármacos , Malato Desidrogenase/metabolismo , Proteínas Fúngicas/metabolismo , Antifúngicos/farmacologia , Trifosfato de Adenosina/metabolismo , Proteômica , Testes de Sensibilidade Microbiana , Ciclo do Ácido Cítrico/efeitos dos fármacos
6.
Int J Biol Macromol ; 266(Pt 1): 130937, 2024 May.
Artigo em Inglês | MEDLINE | ID: mdl-38521301

RESUMO

Herein, carvacrol (CRV) and modified cellulose nanocrystal-zinc oxide (CNC-ZnO) were incorporated into a poly (lactic acid) (PLA) matrix to prepare a PLA-based composite film using a simple solution casting method to achieve antimicrobial effects for application in antimicrobial food packaging. Compared with films obtained from neat PLA, the PLA@CRV20%@CNC-ZnO3% composite film shows better performance in terms of mechanical properties, ultraviolet (UV) blocking, and antimicrobial effects. The PLA composites containing CRV and 3 wt% CNC-ZnO blends exhibit improved tensile strength (21.8 MPa) and elongation at break (403.1 %) as well as excellent UV resistance. In particular, CRV and the CNC-ZnO hybrid endow the obtained PLA composite films with a synergistic antibacterial effect, resulting in good antibacterial properties for microbes, such as Escherichia coli, Staphylococcus aureus and Aspergillus niger. The diameters of the inhibition zone of the PLA@CRV20%@CNC-ZnO3% composite films against E. coli, S. aureus, and A. niger were 4.9, 5.0, and 3.4 cm, respectively. Appling the PLA@CRV20%@CNC-ZnO3% composite film as an antibacterial food packaging material, the storage period for strawberries was considerably extended. This study provides a theoretical basis for developing new organic/inorganic composite antimicrobial film materials from PLA.


Assuntos
Antibacterianos , Celulose , Cimenos , Embalagem de Alimentos , Nanopartículas , Poliésteres , Óxido de Zinco , Óxido de Zinco/química , Óxido de Zinco/farmacologia , Poliésteres/química , Cimenos/química , Cimenos/farmacologia , Celulose/química , Antibacterianos/farmacologia , Antibacterianos/química , Nanopartículas/química , Embalagem de Alimentos/métodos , Staphylococcus aureus/efeitos dos fármacos , Nanocompostos/química , Escherichia coli/efeitos dos fármacos , Resistência à Tração , Testes de Sensibilidade Microbiana , Aspergillus niger/efeitos dos fármacos
7.
Int J Biol Macromol ; 266(Pt 2): 131079, 2024 May.
Artigo em Inglês | MEDLINE | ID: mdl-38537860

RESUMO

This study investigates the effects of SCG embedded into biodegradable polymer blends and aimed to formulate and characterise biomass-reinforced biocomposites using spent coffee ground (SCG) as reinforcement in PHB/PLA polymer blend. The effect of SCG filler loading and varying PHB/PLA ratios on the tensile properties and morphological characteristics of the biocomposites were examined. The results indicated that tensile properties reduction could be due to its incompatibility with the PHB/PLA matrixSCG aggregation at 40 wt% content resulted in higher void formation compared to lower content at 10 wt%. A PHB/PLA ratio of 50/50 with SCG loading 20 wt% was chosen for biocomposites with treated SCG. Biological treatment of SCG using Phanerochaete chrysosporium CK01 and Aspergillus niger DWA8 indicated P. chrysosporium CK01 necessitated a higher moisture content for optimum growth and enzyme production, whereas the optimal conditions for enzyme production (50-55 %, w/w) differed from those promoting A. niger DWA8 growth (40 %, w/w). SEM micrographs highlighted uniform distribution and effective wetting of treated SCG, resulting in improvements of tensile strength and modulus of biocomposites, respectively. The study demonstrated the effectiveness of sustainable fungal treatment in enhancing the interfacial adhesion between treated SCG and the PHB/PLA matrix.


Assuntos
Aspergillus niger , Café , Hidroxibutiratos , Poliésteres , Poliésteres/química , Hidroxibutiratos/química , Café/química , Aspergillus niger/efeitos dos fármacos , Resistência à Tração , Polímeros/química
8.
Molecules ; 27(3)2022 Jan 25.
Artigo em Inglês | MEDLINE | ID: mdl-35164034

RESUMO

Vinegar is a natural product widely used in food and traditional medicine thanks to its physicochemical properties and its richness in bioactive molecules. However, its direct use by consumers can have complications and undesirable effects. Therefore, this study contributes to investigating the physicochemical and biological properties of eleven vinegars marketed in Morocco. Determination of pH, acetic acid, conductivity, total soluble solids and alcohol content in vinegar was carried out. The polyphenols (TP), flavonoids (TF), and condensed tannins (CT) content was determined, and their antioxidant activities were evaluated using 2,2-diphenyl-1-picryl Hydrazyl (DPPH), Ferric Reducing Antioxidant Power (FRAP) and Phosphomolybdenum Reduction Assay (TAC). Then, the antimicrobial activity was studied against four pathogenic bacteria and two fungal strains, using the disk diffusion and the microdilution method. This study showed a wide range of acetic acid values from 0.65 ± 0.29 to 5.15 ± 0.20%. The high value of TP, TF, and CT in our samples V10, V9, and V4 was 655.00 ± 22.2 µgGAE/mL, 244.53 ± 11.32 µgQE/mL and 84.63 ± 1.00 µgTAE/mL, respectively. The tested strains showed variable sensitivities to the different samples with inhibition zones ranging from 6.33 ± 2.08 to 34.33 ± 0.58 mm. The lowest minimum inhibition concentrations were recorded against Staphylococcus aureus ATCC29213 ranging from 1.95 to 7.81 µL/mL. While Aspergillus niger ATCC16404 showed resistance against all of the analyzed samples. In general, vinegar commercialized in Morocco presents a variable range of products with variable properties. Indeed, must take into account this diversity when using it. A future study is needed to identify the phytochemical composition that will further the comprehension of this variability and contribute to its valorization.


Assuntos
Ácido Acético/química , Anti-Infecciosos/farmacologia , Antioxidantes/farmacologia , Fenóis/análise , Anti-Infecciosos/química , Antioxidantes/química , Aspergillus niger/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Marrocos , Análise de Componente Principal , Staphylococcus aureus/efeitos dos fármacos
9.
Molecules ; 27(2)2022 01 10.
Artigo em Inglês | MEDLINE | ID: mdl-35056749

RESUMO

Five new dimer compounds, namely Taiwaniacryptodimers A-E (1-5), were isolated from the methanol extract of the roots of Taiwania cryptomerioides. Their structures were established by mean of spectroscopic analysis and comparison of NMR data with those of known analogues. Their antifungal activities were also evaluated. Our results indicated that metabolites 1, 2, 4, and 5 displayed moderate antifungal activities against Aspergillus niger, Penicillium italicum, Candida albicans, and Saccharomyces cerevisiae.


Assuntos
Antifúngicos/química , Antifúngicos/farmacologia , Cupressaceae/química , Raízes de Plantas/química , Antifúngicos/isolamento & purificação , Aspergillus niger/efeitos dos fármacos , Candida albicans/efeitos dos fármacos , Dimerização , Avaliação Pré-Clínica de Medicamentos , Espectroscopia de Ressonância Magnética , Metanol/química , Testes de Sensibilidade Microbiana , Estrutura Molecular , Penicillium/efeitos dos fármacos , Extratos Vegetais/química
10.
Gene ; 809: 146041, 2022 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-34710526

RESUMO

Plant immunity to pathogen infections is a dynamic response that involves multiple organelles and defence signalling systems such as hypersensitive response (HR) and systemic acquired resistance (SAR). The latter requires the function of Pathogenesis-related (PR) proteins, a common plant protein family with diverse roles in plant innate immunity. Our previous proteomics study showed that a PR gene (ITC1587_Bchr9_P26466_MUSBA) was differentially regulated during a compatible banana-M. incognita interaction, substantiating the isolation of this gene in the current study. Here, we successfully isolated and characterised Pathogenesis-related-10 (PR10) gene with ß-1,3-glucanase and ribonuclease (RNase) activities from two Musa acuminata cultivars (denoted as MaPR10) namely Berangan and Grand Naine (ITC1256). We found that MaPR10 cloned sequences possess glycine-rich loop domain and shared conserved motifs specific to PR10 gene group, confirming its identity as a member of this group. Interestingly, we also found a catalytic domain sequence for glycoside hydrolase family 16 (EXDXXE), unique only to MaPR10 cloned sequences. Two peptide variants closely related to the reference sequence ITC1587_Bchr9_P26466_MUSBA namely MaPR10-BeB5 and MaPR10-GNA5 were overexpressed and purified to test for their functionality. Here, we confirmed that both protein variants possess ß-1,3-glucanase and ribonuclease (RNase) activities, and inhibit the growth of Aspergillus fumigatus, a human opportunistic pathogen. To our knowledge, this is the first PR10 plant proteins with such properties to be reported thus far.


Assuntos
Musa/genética , Musa/parasitologia , Proteínas de Plantas/genética , Proteínas de Plantas/metabolismo , Tylenchoidea/patogenicidade , Animais , Antifúngicos/farmacologia , Aspergillus fumigatus/efeitos dos fármacos , Aspergillus niger/efeitos dos fármacos , Regulação da Expressão Gênica de Plantas , Interações Hospedeiro-Parasita/genética , Cebolas/genética , Filogenia , Imunidade Vegetal/genética , Proteínas de Plantas/farmacologia , Raízes de Plantas/genética , Raízes de Plantas/parasitologia , Plantas Geneticamente Modificadas
11.
Bioorg Chem ; 119: 105560, 2022 02.
Artigo em Inglês | MEDLINE | ID: mdl-34942467

RESUMO

The [2-formyl-4-(trifluoromethyl)phenyl]boronic acid as well as its benzoxaborole and bis(benzoxaborole) derivatives were obtained and their properties studied. The 2-formyl compound displays an unusual structure in the crystalline state, with a significant twist of the boronic group, whereas in DMSO solution it tautomerizes with formation of a cyclic isomer. All the studied compounds exhibit relatively high acidity as well as a reasonable antimicrobial activity. Docking studies showed interactions of all the investigated compounds with the binding pocket of Candida albicans LeuRS. High activity against Bacillus cereus was determined for the 2-formyl compound as well as for the novel bis(benzoxaborole), whereas the studied benzoxaborole shows high antifungal action with MIC values equal to 7.8and 3.9 µg/mL against C. albicans and A. niger respectively. None of the studied compounds exhibits reasonable activity against E. coli.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Antibacterianos/síntese química , Antibacterianos/química , Antifúngicos/síntese química , Antifúngicos/química , Aspergillus niger/efeitos dos fármacos , Bacillus cereus/efeitos dos fármacos , Candida albicans/efeitos dos fármacos , Relação Dose-Resposta a Droga , Escherichia coli/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Relação Estrutura-Atividade
12.
Bioorg Chem ; 119: 105568, 2022 02.
Artigo em Inglês | MEDLINE | ID: mdl-34968884

RESUMO

In this paper, two series of novel multifunctional 1, 4-di (aryl/heteroaryl) substituted piperazine derivatives (6a-d & 7a-d) were synthesized, characterized, and evaluated for their antitubercular, antibacterial, and antifungal activities. A step-wise reduction, bromination and substitution reactions on various aldehydes resulted in alcohols (2a-d), bromides (3a-d), and titled novel compounds (6a-d & 7a-d) in moderate to good yields (48-85%). The novel compounds were evaluated for their antitubercular and antimicrobial activities. Compound 7a exhibited promising antitubercular activity (MIC: 0.65 µg/mL) almost equal to the Rifampicin, while the rest of the compounds were moderately active against MTB H37Rv except 6b. Compounds 7a and 6b showed good activity against tested fungal pathogens. Compounds 7a and 7b were proven as the best bacterial agents. Molecular docking studies were in agreement with the in-vitro results. Docking analyses show that all the synthesized molecules bind to the target protein Mtb RNAP (PDB ID: 5UHC) fairly strongly. All the compounds were evaluated for their in vitro cytotoxicity effect using the MTT assay method against human cancer cell line MCF-7. The compounds demonstrated growth inhibitory effect on the cell line with significant IC50 values ranging between 8.20 and 34.45 µM. Most importantly, compound 7a displayed good binding affinity towards the tested protein with binding energy -7.30 kcal/mol and a stronger hydrogen bond distance of 2.2 Å with ASN-493 residue. Thus, the present research highlighted the potential role of novel piperazine derivatives as potential antitubercular, and antimicrobial candidates and further good research into optimization might result in the development of new antitubercular drug candidates.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Desenho de Fármacos , Simulação de Acoplamento Molecular , Piperazinas/farmacologia , Antibacterianos/síntese química , Antibacterianos/química , Antifúngicos/síntese química , Antifúngicos/química , Aspergillus niger/efeitos dos fármacos , Relação Dose-Resposta a Droga , Avaliação Pré-Clínica de Medicamentos , Escherichia coli/efeitos dos fármacos , Fusarium/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Mycobacterium tuberculosis/efeitos dos fármacos , Piperazinas/síntese química , Piperazinas/química , Staphylococcus aureus/efeitos dos fármacos , Relação Estrutura-Atividade
13.
Acta Chim Slov ; 68(3): 541-547, 2021 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-34897549

RESUMO

A series of five new fluoro-substituted aroylhydrazones were prepared and structurally characterized by elemental analysis, IR, UV-Vis and 1H NMR spectroscopy, as well as single crystal X-ray diffraction. The compounds were evaluated for their antibacterial (Bacillus subtilis, Staphylococcus aureus, Escherichia coli, and Pseudomonas fluorescence) and antifungal (Candida albicans and Aspergillus niger) activities by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide) method. The biological assay indicated that the presence of the electron-withdrawing groups in the aroylhydrazones improved their antimicrobial activities.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Hidrazonas/farmacologia , Antibacterianos/síntese química , Antifúngicos/síntese química , Aspergillus niger/efeitos dos fármacos , Bactérias/efeitos dos fármacos , Candida albicans/efeitos dos fármacos , Hidrazonas/síntese química , Testes de Sensibilidade Microbiana , Estrutura Molecular , Relação Estrutura-Atividade
14.
Molecules ; 26(23)2021 Nov 25.
Artigo em Inglês | MEDLINE | ID: mdl-34885701

RESUMO

2-azido-1H-benzo[d]imidazole derivatives 1a,b were reacted with a ß-ketoester such as acetylacetone in the presence of sodium ethoxide to obtain the desired molecules 2a,b. The latter acted as a key molecule for the synthesis of new carbazone derivatives 4a,b that were submitted to react with 2-oxo-N-phenyl-2-(phenylamino)acetohydrazonoyl chloride to obtain the target thiadiazole derivatives 6a,b. The structures of the newly synthesized compounds were inferred from correct spectral and microanalytical data. Moreover, the newly prepared compounds were subjected to molecular docking studies with DNA gyrase B and exhibited binding energy that extended from -9.8 to -6.4 kcal/mol, which confirmed their excellent potency. The compounds 6a,b were found to be with the minimum binding energy (-9.7 and -9.8 kcal/mol) as compared to the standard drug ciprofloxacin (-7.4 kcal/mol) against the target enzyme DNA gyrase B. In addition, the newly synthesized compounds were also examined and screened for their in vitro antimicrobial activity against pathogenic microorganisms Staphylococcus aureus, E. coli, Pseudomonas aeruginosa, Aspergillus niger, and Candida albicans. Among the newly synthesized molecules, significant antimicrobial activity against all the tested microorganisms was obtained for the compounds 6a,b. The in silico and in vitro findings showed that compounds 6a,b were the most active against bacterial strains, and could serve as potential antimicrobial agents.


Assuntos
Anti-Infecciosos/química , Infecções Bacterianas/tratamento farmacológico , DNA Girase/genética , Inibidores da Topoisomerase II/química , Triazóis/química , Anti-Infecciosos/síntese química , Anti-Infecciosos/farmacologia , Aspergillus niger/efeitos dos fármacos , Infecções Bacterianas/microbiologia , Candida albicans/efeitos dos fármacos , Candida albicans/patogenicidade , DNA Girase/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Escherichia coli/patogenicidade , Humanos , Simulação de Acoplamento Molecular , Farmacocinética , Pseudomonas aeruginosa/efeitos dos fármacos , Pseudomonas aeruginosa/patogenicidade , Staphylococcus aureus/efeitos dos fármacos , Staphylococcus aureus/patogenicidade , Relação Estrutura-Atividade , Inibidores da Topoisomerase II/síntese química , Inibidores da Topoisomerase II/farmacologia , Triazóis/síntese química , Triazóis/farmacologia
15.
Cell Mol Biol (Noisy-le-grand) ; 67(1): 165-170, 2021 Jan 31.
Artigo em Inglês | MEDLINE | ID: mdl-34817351

RESUMO

In current study, Maize (Zea mays L.) husk leave extracts were appraised for biological activities such as cytotoxicity, antidiabetic, antioxidant and antimicrobial. Maceration was performed to collect various fractions of husk leave extracts using a pool of solvents i.e., n-hexane, chloroform, ethyl acetate, butanol and methanol. Antioxidant potential was measured by 1,1-diphenyl-2-picrylhydrazyl (DPPH) scavenging, reducing power and linoleic acid oxidation assay, using butylated hydroxy toluene (BHT) as a positive control. Total phenolic and flavonoid contents were found to be 18.47-425.11 mg/100 g GAE and 5.83-16.72 mg/100 g CE, respectively. The DPPH scavenging assay was exhibited in the range of 76.36 to 88.53%. The percentage inhibition in linoleic acid oxidation was found from 10.16 to 79.51%. Significant antimicrobial activity was demonstrated by husk leaf extracts against bacterial strains and fungal strains using disc diffusion and minimum inhibitory concentration (MIC) method. Amylase alpha assay was employed to analyze the antidiabetic activity which ranged between 9.52-24.81%. Cytotoxicity was evaluated by % age lysis (0.35-9.54%), while thrombolytic activity ranged between 7.67 to 31.27%. The results presented in this study revealed that maize (Zea mays L.) husk leaf extracts can be a valuable source of biologically active compounds and may be consumed as a source of potent herbal medicine in pharmaceuticals.


Assuntos
Antioxidantes/farmacologia , Hipoglicemiantes/farmacologia , Folhas de Planta/química , Zea mays/química , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Antioxidantes/química , Aspergillus niger/efeitos dos fármacos , Aspergillus niger/fisiologia , Bacillus subtilis/efeitos dos fármacos , Bacillus subtilis/fisiologia , Sobrevivência Celular/efeitos dos fármacos , Avaliação Pré-Clínica de Medicamentos , Eritrócitos/citologia , Eritrócitos/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Escherichia coli/fisiologia , Hemólise/efeitos dos fármacos , Humanos , Hipoglicemiantes/química , Testes de Sensibilidade Microbiana/métodos , Extratos Vegetais/química , Extratos Vegetais/farmacologia
16.
Drug Deliv ; 28(1): 2348-2360, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-34747275

RESUMO

The present research work is designed to prepare and optimize butenafine (BT) loaded poly lactic co glycolic acid (PLGA) nanoparticles (BT-NPs). BT-NPs were prepared by emulsification probe sonication method using PLGA (A), PVA (B) as polymer and stabilizer, respectively. The optimum composition of BT-NPs was selected based on the point prediction method given by the Box Behnken design software. The optimized composition of BT-NPop showed a particle size of 267.21 ± 3.54 nm with an entrapment efficiency of 72.43 ± 3.11%. The optimum composition of BT-NPop was further converted into gel formulation using chitosan as a natural polymer. The prepared topical gel formulation (BT-NPopG) was further evaluated for gel characterization, drug release, permeation study, irritation, and antifungal studies. The prepared BT-NPopG formulation showed optimum pH, viscosity, spreadability, and drug content. The release and permeation study results revealed slow BT release (42.76 ± 2.87%) with significantly enhanced permeation across the egg membrane. The irritation study data showed negligible irritation with a cumulative score of 0.33. The antifungal study results conclude higher activity than marketed as well as pure BT. The overall conclusion of the results revealed BT-NPopG as an ideal delivery system to treat topical fungal infection.


Assuntos
Antifúngicos/administração & dosagem , Antifúngicos/farmacologia , Benzilaminas/administração & dosagem , Benzilaminas/farmacologia , Naftalenos/administração & dosagem , Naftalenos/farmacologia , Administração Tópica , Animais , Antifúngicos/efeitos adversos , Antifúngicos/farmacocinética , Aspergillus niger/efeitos dos fármacos , Benzilaminas/efeitos adversos , Benzilaminas/farmacocinética , Candida albicans/efeitos dos fármacos , Química Farmacêutica , Galinhas , Quitosana/química , Portadores de Fármacos/química , Liberação Controlada de Fármacos , Estabilidade de Medicamentos , Ovos , Géis/química , Concentração de Íons de Hidrogênio , Nanopartículas/química , Naftalenos/efeitos adversos , Naftalenos/farmacocinética , Tamanho da Partícula , Copolímero de Ácido Poliláctico e Ácido Poliglicólico/química , Álcool de Polivinil/química , Propriedades de Superfície , Viscosidade
17.
ScientificWorldJournal ; 2021: 7011493, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34754277

RESUMO

In this study, the polyphenol content and the antioxidant and antimicrobial activities of hydroethanolic (MVE) and hydroacetonic (MVA) leaf extracts of Marrubium vulgare L. were examined. The results indicated that the total phenolic content was higher in MVA (112.09 ± 4.77 mg GAE/DW) compared to MVE extract (98.77 ± 1.68 mg GAE/DW). The total flavonoid content was also higher in MVA extract (21.08 ± 0.38 mg QE/g DW) compared to MVE (17.65 ± 0.73 mg QE/g DW). Analysis of the chemical composition revealed the presence of 13 compounds with a total of 96.14%, with the major compound being malic acid (22.57%). Both extracts possess a good total antioxidant activity. DPPH and FRAP assays indicated that the MVE extract possesses a better antioxidant activity, with IC50 = 52.04 µg/mL ± 0.2 and EC50 of 4.51 ± 0.5 mg/mL, compared to MVA extract (IC50 = 60.57 ± 0.6 µg/mL and EC50 of 6.43 ± 0.0411 mg/mL). Moreover, both extracts exhibited strong antimicrobial activity against certain nosocomial strains as indicted by the MIC values, which ranged between 0.93 mg/mL and 10 mg/mL. Taken together, these results reveal the importance of M. vulgare as a natural antioxidant with important antimicrobial activity.


Assuntos
Anti-Infecciosos/análise , Antioxidantes/análise , Marrubium/química , Extratos Vegetais/química , Anti-Infecciosos/isolamento & purificação , Anti-Infecciosos/farmacologia , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Aspergillus niger/efeitos dos fármacos , Bacillus subtilis/efeitos dos fármacos , Candida albicans/efeitos dos fármacos , Testes de Sensibilidade a Antimicrobianos por Disco-Difusão , Escherichia coli/efeitos dos fármacos , Flavonoides/análise , Fenóis/análise , Extratos Vegetais/farmacologia , Folhas de Planta/química , Salmonella enterica/efeitos dos fármacos , Staphylococcus aureus/efeitos dos fármacos
18.
Nucleosides Nucleotides Nucleic Acids ; 40(12): 1159-1197, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34612797

RESUMO

Novel and synthetically essential flavonoids compounds containing the organosulfur moiety from Schiff bases, as well as their copper complexes, were synthesized from chrysin and 2-(phenylthio)aniline. These complexes were characterized using elemental analysis, mass spectrometry, electronic absorption spectroscopy, IR, 1H, and 13C NMR spectroscopy techniques. All the Cu(II) complexes exhibit square planar geometry. The in vitro antimicrobial activities of the investigated compounds were tested against the bacterial species, Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli, Staphylococcus epidermidis, and Klebsiella pneumoniae and fungal species, Aspergillus niger, Fusarium solani, Culvularia lunata, Rhizoctonia bataicola, and Candida albicans by serial dilution method. The DNA binding and DNA cleavage properties of copper complexes were studied. Free radical scavenging, superoxide dismutase, glutathione peroxidase, and antioxidant activities of the copper complexes have also been studied. In addition, using the egg albumin process, the in vitro anti-inflammatory efficacy of metal chelates was examined. Anti-tuberculosis and α-glucosidase inhibition activity were carried out from the prepared metal complexes. The flavonoid compounds containing the organosulfur moiety of Cu(II) complexes (1-8) exhibited better therapeutic agent.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Antioxidantes/farmacologia , Complexos de Coordenação/farmacologia , DNA/efeitos dos fármacos , Animais , Antibacterianos/síntese química , Antibacterianos/química , Antifúngicos/síntese química , Antifúngicos/química , Antioxidantes/síntese química , Antioxidantes/química , Ascomicetos/efeitos dos fármacos , Aspergillus niger/efeitos dos fármacos , Compostos de Bifenilo/antagonistas & inibidores , Candida albicans/efeitos dos fármacos , Bovinos , Complexos de Coordenação/síntese química , Complexos de Coordenação/química , Cobre/química , Cobre/farmacologia , Clivagem do DNA/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Flavonoides/química , Flavonoides/farmacologia , Fusarium/efeitos dos fármacos , Klebsiella pneumoniae/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Picratos/antagonistas & inibidores , Pseudomonas aeruginosa/efeitos dos fármacos , Rhizoctonia/efeitos dos fármacos , Staphylococcus aureus/efeitos dos fármacos , Staphylococcus epidermidis/efeitos dos fármacos
19.
Toxins (Basel) ; 13(10)2021 10 12.
Artigo em Inglês | MEDLINE | ID: mdl-34679013

RESUMO

Zearalenone (ZEN) is one of the most common mycotoxin contaminants in food. For food safety, an efficient and environmental-friendly approach to ZEN degradation is significant. In this study, an Aspergillus niger strain, FS10, was stimulated with 1.0 µg/mL ZEN for 24 h, repeating 5 times to obtain a stressed strain, Zearalenone-Stressed-FS10 (ZEN-S-FS10), with high degradation efficiency. The results show that the degradation rate of ZEN-S-FS10 to ZEN can be stabilized above 95%. Through metabolomics analysis of the metabolome difference of FS10 before and after ZEN stimulation, it was found that the change of metabolic profile may be the main reason for the increase in the degradation rate of ZEN. The optimization results of degradation conditions of ZEN-S-FS10 show that the degradation efficiency is the highest with a concentration of 104 CFU/mL and a period of 28 h. Finally, we analyzed the degradation products by UPLC-q-TOF, which shows that ZEN was degraded into two low-toxicity products: C18H22O8S (Zearalenone 4-sulfate) and C18H22O5 ((E)-Zearalenone). This provides a wide range of possibilities for the industrial application of this strain.


Assuntos
Aspergillus niger/efeitos dos fármacos , Aspergillus niger/metabolismo , Zearalenona/toxicidade , Aspergillus niger/genética , Inativação Metabólica/efeitos dos fármacos , Metaboloma , Análise de Sequência de DNA , Zearalenona/análogos & derivados , Zearalenona/metabolismo
20.
Molecules ; 26(19)2021 Sep 23.
Artigo em Inglês | MEDLINE | ID: mdl-34641303

RESUMO

Due to their large possibility of the structure modification, alkylammonium gemini surfactants are a rapidly growing class of compounds. They exhibit significant surface, aggregation and antimicrobial properties. Due to the fact that, in order to achieve the desired utility effect, the minimal concentration of compounds are used, they are in line with the principle of greenolution (green evolution) in chemistry. In this study, we present innovative synthesis of the homologous series of gemini surfactants modified at the spacer by the ether group, i.e., 3-oxa-1,5-pentane-bis(N-alkyl-N,N-dimethylammonium bromides). The critical micelle concentrations were determined. The minimal inhibitory concentrations of the synthesized compounds were determined against bacteria Escherichia coli ATCC 10536 and Staphylococcus aureus ATCC 6538; yeast Candida albicans ATCC 10231; and molds Aspergillus niger ATCC 16401 and Penicillium chrysogenum ATCC 60739. We also investigated the relationship between antimicrobial activity and alkyl chain length or the nature of the spacer. The obtained results indicate that the synthesized compounds are effective microbicides with a broad spectrum of biocidal activity.


Assuntos
Anti-Infecciosos/farmacologia , Compostos de Amônio Quaternário/farmacologia , Tensoativos/farmacologia , Anti-Infecciosos/química , Aspergillus niger/efeitos dos fármacos , Candida albicans/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Química Verde , Micelas , Testes de Sensibilidade Microbiana , Estrutura Molecular , Penicillium chrysogenum/efeitos dos fármacos , Compostos de Amônio Quaternário/química , Staphylococcus aureus/efeitos dos fármacos , Tensoativos/química
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