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1.
Int J Biol Macromol ; 272(Pt 1): 132813, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38825276

RESUMO

Bionanocomposite films of three biopolymers including chitosan, gelatin, and pectin incorporated with rosemary essential oil (REO) were developed and characterized in terms of their physical, structural, mechanical, morphological, antioxidant, and antimicrobial properties. Incorporation of REO showed an increased hydrophobic nature thus, improved water vapor transmission rate (WVTR), tensile strength (TS), elongation-at-break (EAB), and thermal stability significantly (P ≤ 0.05) as compared to the control films. The addition of REO leads to more opaque films with relatively increased microstructural heterogeneity, resulting in an increase in film opacity. Fourier transform infrared spectroscopy (FTIR) and particle size revealed that REO incorporation exhibits high physicochemical stability in chitosan, gelatin, and pectin bionanocomposite films. Incorporation of REO exhibited the highest inhibitory activity against the tested pathogenic strains (Bacillus subtilis and Escherichia coli). Furthermore, the addition of REO increased the inhibitory activity of films against ABTS and DPPH free radicals. Therefore, chitosan, gelatin, and pectin-based bionanocomposite films containing REO as food packaging could act as a potential barrier to extending food shelf life.


Assuntos
Antioxidantes , Quitosana , Embalagem de Alimentos , Gelatina , Nanocompostos , Óleos Voláteis , Pectinas , Quitosana/química , Pectinas/química , Gelatina/química , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Nanocompostos/química , Antioxidantes/química , Antioxidantes/farmacologia , Embalagem de Alimentos/métodos , Resistência à Tração , Vapor , Bacillus subtilis/efeitos dos fármacos , Antibacterianos/química , Antibacterianos/farmacologia , Escherichia coli/efeitos dos fármacos , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Espectroscopia de Infravermelho com Transformada de Fourier
2.
Biomater Adv ; 161: 213882, 2024 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-38710121

RESUMO

Metallic lattice scaffolds are designed to mimic the architecture and mechanical properties of bone tissue and their surface compatibility is of primary importance. This study presents a novel surface modification protocol for metallic lattice scaffolds printed from a superelastic Ti-Zr-Nb alloy. This protocol consists of dynamic chemical etching (DCE) followed by silver nanoparticles (AgNP) decoration. DCE, using an 1HF + 3HNO3 + 12H2O23% based solution, was used to remove partially-fused particles from the surfaces of different as-built lattice structures (rhombic dodecahedron, sheet gyroid, and Voronoi polyhedra). Subsequently, an antibacterial coating was synthesized on the surface of the scaffolds by a controlled (20 min at a fixed volume flowrate of 500 mL/min) pumping of the functionalization solutions (NaBH4 (2 mg/mL) and AgNO3 (1 mg/mL)) through the porous structures. Following these treatments, the scaffolds' surfaces were found to be densely populated with Ag nanoparticles and their agglomerates, and manifested an excellent antibacterial effect (Ag ion release rate of 4-8 ppm) suppressing the growth of both E. coli and B. subtilis bacteria up to 99 %. The scaffold extracts showed no cytotoxicity and did not affect cell proliferation, indicating their safety for subsequent use as implants. A cytocompatibility assessment using MG-63 spheroids demonstrated good attachment, spreading, and active migration of cells on the scaffold surface (over 96 % of living cells), confirming their biotolerance. These findings suggest the promise of this surface modification approach for developing superelastic Ti-Zr-Nb scaffolds with superior antibacterial properties and biocompatibility, making them highly suitable for bone implant applications.


Assuntos
Antibacterianos , Nanopartículas Metálicas , Prata , Propriedades de Superfície , Alicerces Teciduais , Titânio , Zircônio , Prata/química , Prata/farmacologia , Nanopartículas Metálicas/química , Titânio/química , Titânio/farmacologia , Antibacterianos/farmacologia , Antibacterianos/química , Alicerces Teciduais/química , Zircônio/química , Zircônio/farmacologia , Humanos , Nióbio/química , Nióbio/farmacologia , Lasers , Escherichia coli/efeitos dos fármacos , Ligas/química , Ligas/farmacologia , Bacillus subtilis/efeitos dos fármacos , Pós , Teste de Materiais , Proliferação de Células/efeitos dos fármacos
3.
J Oleo Sci ; 73(5): 787-799, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38692900

RESUMO

Launaea sarmentosa, also known as Sa Sam Nam, is a widely used remedy in Vietnamese traditional medicine and cuisine. However, the chemical composition and bioactivity of its essential oil have not been elucidated yet. In this study, we identified 40 compounds (98.6% of total peak area) in the essential oil via GC-MS analysis at the first time. Among them, five main compounds including Thymohydroquinone dimethyl ether (52.4%), (E)-α-Atlantone (9.0%), Neryl isovalerate (6.6%), Davanol D2 (isomer 2) (3.9%), and trans-Sesquisabinene hydrate (3.9%) have accounted for 75.8% of total peak area. The anti-bacterial activity of the essential oil against 4 microorganisms including Staphylococcus aureus, Bacillus subtilis, Escherichia coli, and Pseudomonas aeruginosa has also investigated via agar well diffusion assay. The results showed that the essential oil exhibited a strong antibacterial activity against Bacillus subtilis with the inhibition zones ranging from 8.2 to 18.7 mm. To elucidate the anti-bacterial effect mechanism of the essential oil, docking study of five main compounds of the essential oil (Thymohydroquinone dimethyl ether, (E)-α-Atlantone, Neryl isovalerate, Davanol D2 (isomer 2), and trans-Sesquisabinene hydrate) against some key proteins for bacterial growth such as DNA gyrase B, penicillin binding protein 2A, tyrosyl-tRNA synthetase, and dihydrofolate reductase were performed. The results showed that the main constituents of essential oil were highly bound with penicillin binding protein 2A with the free energies ranging -27.7 to -44.8 kcal/mol, which suggests the relationship between the antibacterial effect of essential oil and the affinity of main compounds with penicillin binding protein. In addition, the free energies of main compounds of the essential oil with human cyclooxygenase 1, cyclooxygenase 2, and phospholipase A2, the crucial proteins related with inflammatory response were less than diclofenac, a non-steroidal antiinflammatory drug. These findings propose the essential oil as a novel and promising anti-bacterial and anti-inflammatory medicine or cosmetic products.


Assuntos
Antibacterianos , Bacillus subtilis , Hemiterpenos , Simulação de Acoplamento Molecular , Óleos Voláteis , Ácidos Pentanoicos , Antibacterianos/farmacologia , Antibacterianos/isolamento & purificação , Antibacterianos/química , Óleos Voláteis/farmacologia , Óleos Voláteis/química , Óleos Voláteis/isolamento & purificação , Bacillus subtilis/efeitos dos fármacos , Staphylococcus aureus/efeitos dos fármacos , Pseudomonas aeruginosa/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Tetra-Hidrofolato Desidrogenase/metabolismo , DNA Girase/metabolismo , Sesquiterpenos/isolamento & purificação , Sesquiterpenos/farmacologia , Testes de Sensibilidade Microbiana , Cromatografia Gasosa-Espectrometria de Massas
4.
Int J Mol Sci ; 25(10)2024 May 13.
Artigo em Inglês | MEDLINE | ID: mdl-38791348

RESUMO

Hybrid nanomaterials have attracted considerable interest in biomedicine because of their fascinating characteristics and wide range of applications in targeted drug delivery, antibacterial activity, and cancer treatment. This study developed a gelatin-coated Titanium oxide/palladium (TiO2/Pd) hybrid nanomaterial to enhance the antibacterial and anticancer capabilities. Morphological and structural analyses were conducted to characterize the synthesized hybrid nanomaterial. The surface texture of the hybrid nanomaterials was examined by high-resolution transmission electron microscopy (HR-TEM) and field-emission scanning electron microscopy (FE-SEM). The FE-SEM image revealed the bulk of the spherically shaped particles and the aggregated tiny granules. Energy dispersive X-ray spectroscopy (EDS) revealed Ti, Pd, C, and O. X-ray diffraction (XRD) revealed the gelatin-coated TiO2/Pd to be in the anatase form. Fourier transform infrared spectroscopy examined the interactions among the gelatin-coated TiO2/Pd nanoparticles. The gelatin-coated TiO2/Pd nanomaterials exhibited high antibacterial activity against Escherichia coli (22 mm) and Bacillus subtilis (17 mm) compared to individual nanoparticles, confirming the synergistic effect. More importantly, the gelatin-coated TiO2/Pd hybrid nanomaterial exhibited remarkable cytotoxic effects on A549 lung cancer cells which shows a linear increase with the concentration of the nanomaterial. The hybrid nanomaterials displayed higher toxicity to cancer cells than the nanoparticles alone. Furthermore, the cytotoxic activity against human cancer cells was verified by the generation of reactive oxygen species and nuclear damage. Therefore, gelatin-coated TiO2/Pd nanomaterials have potential uses in treating cancer and bacterial infections.


Assuntos
Antibacterianos , Antineoplásicos , Escherichia coli , Gelatina , Nanoestruturas , Paládio , Titânio , Titânio/química , Titânio/farmacologia , Antibacterianos/farmacologia , Antibacterianos/química , Humanos , Antineoplásicos/farmacologia , Antineoplásicos/química , Gelatina/química , Paládio/química , Paládio/farmacologia , Escherichia coli/efeitos dos fármacos , Nanoestruturas/química , Células A549 , Bacillus subtilis/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Difração de Raios X , Nanopartículas Metálicas/química
5.
Mar Drugs ; 22(4)2024 Mar 29.
Artigo em Inglês | MEDLINE | ID: mdl-38667774

RESUMO

Five new biflorane-type diterpenoids, biofloranates E-I (1-5), and two new bicyclic diterpene glycosides, lemnaboursides H-I (6-7), along with the known lemnabourside, were isolated from the South China Sea soft coral Lemnalia bournei. Their chemical structures and stereochemistry were determined based on extensive spectroscopic methods, including time-dependent density functional theory (TDDFT) ECD calculations, as well as a comparison of them with the reported values. The antibacterial activities of the isolated compounds were evaluated against five pathogenic bacteria, and all of these diterpenes and diterpene glycosides showed antibacterial activities against Staphylococcus aureus and Bacillus subtilis, with MICs ranging from 4 to 64 µg/mL. In addition, these compounds did not exhibit noticeable cytotoxicities on A549, Hela, and HepG2 cancer cell lines, at 20 µM.


Assuntos
Antozoários , Antibacterianos , Bacillus subtilis , Diterpenos , Glicosídeos , Testes de Sensibilidade Microbiana , Staphylococcus aureus , Antozoários/química , Diterpenos/farmacologia , Diterpenos/química , Diterpenos/isolamento & purificação , Antibacterianos/farmacologia , Antibacterianos/química , Antibacterianos/isolamento & purificação , Animais , Glicosídeos/farmacologia , Glicosídeos/química , Glicosídeos/isolamento & purificação , Humanos , Staphylococcus aureus/efeitos dos fármacos , Bacillus subtilis/efeitos dos fármacos , Células HeLa , Linhagem Celular Tumoral , Células Hep G2 , Estrutura Molecular , Células A549 , China
6.
Int J Antimicrob Agents ; 63(5): 107155, 2024 May.
Artigo em Inglês | MEDLINE | ID: mdl-38527561

RESUMO

Due to intramolecular ring structures, the ribosomally produced and post-translationally modified peptide mersacidin shows antimicrobial properties comparable to those of vancomycin without exhibiting cross-resistance. Although the principles of mersacidin biosynthesis are known, there is no information on the molecular control processes for the initial stimulation of mersacidin bioproduction. By using Bacillus subtilis for heterologous biosynthesis, a considerable amount of mersacidin could be produced without the mersacidin-specific immune system and the mersacidin-activating secretory protease. By using the established laboratory strain Bacillus subtilis 168 and strain 3NA, which is used for high cell density fermentation processes, in combination with the construction of reporter strains to determine the promoter strengths within the mersacidin core gene cluster, the molecular regulatory circuit of Spo0A, a master regulator of cell differentiation including sporulation initiation, and the global transcriptional regulator AbrB, which is involved in cell adaptation processes in the transient growth phase, was identified to control the initial stimulation of the mersacidin core gene cluster. In a second downstream regulatory step, the activator MrsR1, encoded in the core gene cluster, acts as a stimulatory element for mersacidin biosynthesis. These findings are important to understand the mechanisms linking environmental conditions and microbial responses with respect to the bioproduction of bioactive metabolites including antimicrobials such as mersacidin. This information will also support the construction of production strains for bioactive metabolites with antimicrobial properties.


Assuntos
Bacillus subtilis , Proteínas de Bactérias , Bacteriocinas , Regulação Bacteriana da Expressão Gênica , Família Multigênica , Fatores de Transcrição , Bacillus subtilis/genética , Bacillus subtilis/metabolismo , Bacillus subtilis/efeitos dos fármacos , Proteínas de Bactérias/genética , Proteínas de Bactérias/metabolismo , Fatores de Transcrição/genética , Fatores de Transcrição/metabolismo , Proteínas de Ligação a DNA/genética , Proteínas de Ligação a DNA/metabolismo , Peptídeos/metabolismo , Peptídeos/genética , Regiões Promotoras Genéticas , Fragmentos de Peptídeos/genética , Fragmentos de Peptídeos/metabolismo
7.
Nature ; 613(7945): 729-734, 2023 01.
Artigo em Inglês | MEDLINE | ID: mdl-36450357

RESUMO

Peptidoglycan and almost all surface glycopolymers in bacteria are built in the cytoplasm on the lipid carrier undecaprenyl phosphate (UndP)1-4. These UndP-linked precursors are transported across the membrane and polymerized or directly transferred to surface polymers, lipids or proteins. UndP is then flipped to regenerate the pool of cytoplasmic-facing UndP. The identity of the flippase that catalyses transport has remained unknown. Here, using the antibiotic amphomycin that targets UndP5-7, we identified two broadly conserved protein families that affect UndP recycling. One (UptA) is a member of the DedA superfamily8; the other (PopT) contains the domain DUF368. Genetic, cytological and syntenic analyses indicate that these proteins are UndP transporters. Notably, homologues from Gram-positive and Gram-negative bacteria promote UndP transport in Bacillus subtilis, indicating that recycling activity is broadly conserved among family members. Inhibitors of these flippases could potentiate the activity of antibiotics targeting the cell envelope.


Assuntos
Proteínas de Bactérias , Proteínas de Transporte , Sequência Conservada , Evolução Molecular , Bactérias Gram-Negativas , Bactérias Gram-Positivas , Fosfatos de Poli-Isoprenil , Antibacterianos/farmacologia , Bacillus subtilis/citologia , Bacillus subtilis/efeitos dos fármacos , Bacillus subtilis/genética , Bacillus subtilis/metabolismo , Proteínas de Bactérias/química , Proteínas de Bactérias/classificação , Proteínas de Bactérias/genética , Proteínas de Bactérias/metabolismo , Proteínas de Transporte/química , Proteínas de Transporte/classificação , Proteínas de Transporte/genética , Proteínas de Transporte/metabolismo , Membrana Celular/efeitos dos fármacos , Membrana Celular/metabolismo , Bactérias Gram-Negativas/citologia , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Negativas/genética , Bactérias Gram-Negativas/metabolismo , Bactérias Gram-Positivas/citologia , Bactérias Gram-Positivas/efeitos dos fármacos , Bactérias Gram-Positivas/genética , Bactérias Gram-Positivas/metabolismo , Fosfatos de Poli-Isoprenil/metabolismo , Sintenia , Peptidoglicano/metabolismo , Parede Celular/química , Parede Celular/metabolismo
8.
J Nat Prod ; 85(11): 2547-2556, 2022 11 25.
Artigo em Inglês | MEDLINE | ID: mdl-36268672

RESUMO

Eight new cyclopiazonic acid (1-8) and five new okaramine (9-13) alkaloids together with 13 known compounds were isolated from the fungus Chrysosporium undulatum YT-1. Compounds 2, 4, 5, 7, 10, 11, and 13 were chlorinated indole alkaloids. The structures of compounds 1-13 were elucidated by HRESIMS and NMR spectroscopic data. Their relative and absolute configurations were established by J-based configuration analysis, NOESY, NOEDIFF experiments, ECD spectroscopic data, and biogenetic considerations. Compound 4 inhibited the growth of Bacillus subtilis with an MIC value of 6.3 µg/mL. Compounds 9-11 exhibited strong insecticidal capacity against the third instar larvae of silkworm and cotton bollworm (LD50: ≤7.56 µg/g). At 40 µM, compound 1 showed obvious neuroprotection to the PC12 cells with 6-OHDA treatment.


Assuntos
Chrysosporium , Alcaloides Indólicos , Chrysosporium/química , Alcaloides Indólicos/química , Alcaloides Indólicos/isolamento & purificação , Alcaloides Indólicos/farmacologia , Estrutura Molecular , Antibacterianos/química , Antibacterianos/isolamento & purificação , Antibacterianos/farmacologia , Bacillus subtilis/efeitos dos fármacos , Células PC12 , Animais , Ratos , Fármacos Neuroprotetores/química , Fármacos Neuroprotetores/isolamento & purificação , Fármacos Neuroprotetores/farmacologia
9.
Mar Drugs ; 20(2)2022 Feb 13.
Artigo em Inglês | MEDLINE | ID: mdl-35200666

RESUMO

Five new sesquiterpenoids, citreobenzofuran D-F (1-3) and phomenone A-B (4-5), along with one known compound, xylarenone A (6), were isolated from the culture of the mangrove-derived fungus Penicillium sp. HDN13-494. Their structures were deduced from extensive spectroscopic data, high-resolution electrospray ionization mass spectrometry (HRESIMS), and electronic circular dichroism (ECD) calculations. Furthermore, the absolute structures of 1 were determined by single-crystal X-ray diffraction analysis. Citreobenzofuran E-F (2-3) are eremophilane-type sesquiterpenoids with rare benzofuran frameworks, while phomenone A (4) contains a rare thiomethyl group, which is the first report of this kind of sesquiterpene with sulfur elements in the skeleton. All the compounds were tested for their antimicrobial and antitumor activity, and phomenone B (5) showed moderate activity against Bacillus subtilis, with an MIC value of 6.25 µM.


Assuntos
Benzofuranos/farmacologia , Naftóis/farmacologia , Penicillium/metabolismo , Sesquiterpenos/farmacologia , Anti-Infecciosos/química , Anti-Infecciosos/isolamento & purificação , Anti-Infecciosos/farmacologia , Antineoplásicos/química , Antineoplásicos/isolamento & purificação , Antineoplásicos/farmacologia , Bacillus subtilis/efeitos dos fármacos , Benzofuranos/química , Benzofuranos/isolamento & purificação , Linhagem Celular Tumoral , Humanos , Testes de Sensibilidade Microbiana , Naftóis/química , Naftóis/isolamento & purificação , Sesquiterpenos/química , Sesquiterpenos/isolamento & purificação
10.
Int J Mol Sci ; 23(3)2022 Jan 25.
Artigo em Inglês | MEDLINE | ID: mdl-35163283

RESUMO

To obtain fiber materials with pronounced chemical-biological protection, metal (Zn or Ta) nanoparticles were jointly applied with polyelectrolyte complexes of enzymes and polypeptides being their stabilizers. Computer modeling revealed the preferences between certain polyelectrolyte partners for N-acyl-homoserine lactone acylase and hexahistidine-tagged organophosphorus hydrolase (His6-OPH) possessing the quorum quenching (QQ) behavior with bacterial cells. The combinations of metal nanoparticles and enzymes appeared to function better as compared to the combinations of the same QQ-enzymes with antibiotics (polymyxins), making it possible to decrease the applied quantities by orders of magnitude while giving the same effect. The elimination of Gram-positive and Gram-negative bacterial cells from doubly modified fiber materials notably increased (up to 2.9-fold), whereas His6-OPH retained its hydrolytic activity in reaction with organophosphorus compounds (up to 74% of initially applied activity). Materials with the certain enzyme and Zn nanoparticles were more efficient against Bacillus subtilis cells (up to 2.1-fold), and Ta nanoparticles acted preferentially against Escherichia coli (up to 1.5-fold). Some materials were proved to be more suitable for combined modification by metal nanoparticles and His6-OPH complexes as antimicrobial protectants.


Assuntos
Acil-Butirolactonas/química , Nanopartículas Metálicas/química , Peptídeos/química , Amidoidrolases , Antibacterianos/química , Arildialquilfosfatase/química , Bacillus subtilis/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Hidrólise , Compostos Organofosforados/química , Polieletrólitos/farmacologia , Percepção de Quorum/fisiologia , Tantálio/química , Tantálio/metabolismo , Zinco/química , Zinco/metabolismo
11.
Carbohydr Polym ; 277: 118823, 2022 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-34893240

RESUMO

The conjugation between drug and biopolymers through an easily hydrolysable bond such as ester linkage, disulfide linkage, or imine-bond have been extensively employed to control the drug release pattern and improve its bioavailability. This work described the conjugation of 9-aminoacridine (9-AA) to Gum Arabic (GA) via Schiff's base, as a pH-responsive bond. First, GA was oxidized to Arabic Gum dialdehyde (AGDA), then a different amount of 9-AA (10, 25, and 50 mg 9-AA) was coupled to defined amount of AGDA, the coupling was confirmed by elemental analysis and different spectroscopic tools. In addition, the physical features of Schiff's base conjugates including surface morphology, thermal stability, and crystalline structure were examined. The thermogravimetric analysis revealed that the incorporation of 9-AA slightly improved the thermal stability. The coupling of 9-AA to AGDA dramatically enhanced its in vitro antimicrobial and antitumor activities. All conjugates exhibited broad-spectrum activity against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Bacillus subtilis, and Candida albicans. Moreover, AGA 25 and AGA 50 demonstrated promising capability to suppress the proliferation of human colon cancer cell line (Caco-2), with IC50 190.10 and 180.80 µg/mL respectively.


Assuntos
Aminacrina/farmacologia , Antibacterianos/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Aminacrina/síntese química , Aminacrina/química , Antibacterianos/síntese química , Antibacterianos/química , Antineoplásicos Fitogênicos/síntese química , Antineoplásicos Fitogênicos/química , Bacillus subtilis/efeitos dos fármacos , Células CACO-2 , Candida albicans/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Escherichia coli/efeitos dos fármacos , Humanos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Pseudomonas aeruginosa/efeitos dos fármacos , Bases de Schiff/síntese química , Bases de Schiff/química , Bases de Schiff/farmacologia , Staphylococcus aureus/efeitos dos fármacos , Relação Estrutura-Atividade
12.
Braz. j. biol ; 82: 1-8, 2022. ilus, graf, tab
Artigo em Inglês | LILACS, VETINDEX | ID: biblio-1468571

RESUMO

Green synthesis of silver nanoparticles (AgNPs) is an ecofriendly, cost-effective and promising approach for discovery of novel therapeutics. The aim of the current work was to biogenic synthesize, characterize AgNPs using seed extracts of three economically important varieties of date palm (Iklas, Irziz and Shishi), and assess their anti-pathogenic bacterial activities. AgNPs were synthesised then characterised using electron microscopy and Fourier transform infrared analyses. The bactericidal activities of AgNPs against five different bacterial pathogens, Bacillus subtilis, Escherichia coli, Staphylococcus aureus, methicillin-resistant Staphylococcus aureus and Streptococcus pneumoniae, were determined in vitro. In particular, changes in membrane integrity of virulent bacterial strains in response to AgNPs were investigated. Results of lactate dehydrogenase, alkaline phosphatase activity assays, and measurement of membrane potential revealed that the cytotoxic effects of the AgNPs were mainly centred on the plasma membrane of bacterial cells, leading to loss of its integrity and eventually cell death. In conclusion, green synthesis of AgNPs is an efficient, cost-effective and promising strategy to combat virulent antibiotic-resistant strains.


A síntese verde de nanopartículas de prata (AgNPs) é uma abordagem ecologicamente correta, econômica e promissora para a descoberta de novas terapêuticas. O objetivo do presente trabalho foi sintetizar biogênica, caracterizar AgNPs usando extratos de sementes de três variedades economicamente importantes de tamareira (Iklas, Irziz e Shishi) e avaliar suas atividades bacterianas antipatogênicas. AgNPs foram sintetizados e caracterizados usando microscopia eletrônica e análise de infravermelho por transformada de Fourier. As atividades bactericidas de AgNPs contra cinco diferentes patógenos bacterianos, Bacillus subtilis, Escherichia coli, Staphylococcus aureus, Staphylococcus aureus resistente à meticilina e Streptococcus pneumoniae, foram determinadas in vitro. Em particular, foram investigadas alterações na integridade da membrana de cepas bacterianas virulentas em resposta a AgNPs. Os resultados da lactato desidrogenase, dos ensaios da atividade da fosfatase alcalina e da medição do potencial de membrana revelaram que os efeitos citotóxicos dos AgNPs estavam principalmente centrados na membrana plasmática das células bacterianas, levando à perda de sua integridade e, eventualmente, à morte celular. A síntese verde de AgNPs é uma estratégia eficiente, econômica e promissora para combater cepas virulentas resistentes a antibióticos.


Assuntos
Antibiose , Bacillus subtilis/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Nanopartículas/análise , Phoeniceae , Prata/análise , Staphylococcus aureus/efeitos dos fármacos , Streptococcus pneumoniae/efeitos dos fármacos , Microscopia , Técnicas In Vitro
13.
Int J Mol Sci ; 22(24)2021 Dec 17.
Artigo em Inglês | MEDLINE | ID: mdl-34948362

RESUMO

ATP-binding cassette (ABC) transporters are conserved in all kingdoms of life, where they transport substrates against a concentration gradient across membranes. Some ABC transporters are known to cause multidrug resistances in humans and are able to transport chemotherapeutics across cellular membranes. Similarly, BmrA, the ABC transporter of Bacillus subtilis, is involved in excretion of certain antibiotics out of bacterial cells. Screening of extract libraries isolated from fungi revealed that the C14 fatty acid myristic acid has an inhibitory effect on the BmrA ATPase as well as the transport activity. Thus, a natural membrane constituent inhibits the BmrA activity, a finding with physiological consequences as to the activity and regulation of ABC transporter activities in biological membranes.


Assuntos
Transportadores de Cassetes de Ligação de ATP/antagonistas & inibidores , Bacillus subtilis/efeitos dos fármacos , Proteínas de Bactérias/antagonistas & inibidores , Ácido Mirístico/farmacologia , Transportadores de Cassetes de Ligação de ATP/metabolismo , Adenosina Trifosfatases/antagonistas & inibidores , Adenosina Trifosfatases/metabolismo , Bacillus subtilis/metabolismo , Proteínas de Bactérias/metabolismo , Descoberta de Drogas
14.
Molecules ; 26(23)2021 Dec 02.
Artigo em Inglês | MEDLINE | ID: mdl-34885902

RESUMO

(1) Background: Peptides are good candidates for anticancer drugs due to their natural existence in the body and lack of secondary effects. (KLAKLAK)2 is an antimicrobial peptide that also shows good anticancer properties. (2) Methods: The Solid Phase Peptide Synthesis (Fmoc-strategy) was used for the synthesis of target molecules, analogs of (KLAKLAK)2-NH2. The purity of all compounds was monitored by HPLC, and their structures were proven using mass spectrometry. Cytotoxicity and antiproliferative effects were studied using 3T3 NRU and MTT tests, respectively. For determination of antimicrobial activity, the disc-diffusion method was used. Hydrolytic stability at three pH values, which mimic the physiological pH in the body, was investigated by means of the HPLC technique. (3) Results: A good selective index against MCF-7 tumor cell lines, combined with good cytotoxicity and antiproliferative properties, was revealed for conjugates NphtG-(KLAKLAK)2-NH2 and Caf-(KLAKLAK)2-NH2. The same compounds showed very good antifungal properties and complete hydrolytic stability for 72 h. The compound Caf-(KLß-AKLß-AK)2-NH2 containing ß-Ala in its structures exhibited good antimicrobial activity against Escherichia coli K12 407 and Bacillus subtilis 3562, in combination with very good antiproliferative and cytotoxic properties, as well as hydrolytic stability. (4) Conclusions: The obtained results reveal that all synthesized conjugates could be useful for medical practice as anticancer or antimicrobial agents.


Assuntos
Anti-Infecciosos/química , Peptídeos Antimicrobianos/química , Antineoplásicos/química , Anti-Infecciosos/síntese química , Anti-Infecciosos/farmacologia , Peptídeos Antimicrobianos/síntese química , Peptídeos Antimicrobianos/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Bacillus subtilis/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão , Descoberta de Drogas , Escherichia coli K12/efeitos dos fármacos , Humanos , Células MCF-7 , Técnicas de Síntese em Fase Sólida , beta-Alanina/análogos & derivados , beta-Alanina/síntese química , beta-Alanina/farmacologia
15.
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
16.
Molecules ; 26(21)2021 Oct 31.
Artigo em Inglês | MEDLINE | ID: mdl-34771017

RESUMO

Hazelnut shells represent a waste material (about 42% of the total biomass) deriving from hazelnut harvest. These are mainly used as a heating source; however, they represent an interesting source of polyphenols useful in health field. The impact on phenolic profile and concentrations of hazelnut shell extracts obtained by three extraction methods (maceration, ultrasonic bath, and high-power ultrasonic), as well as temperature, extraction time, and preventive maceration, was studied. The prepared extracts were characterized in terms of chemical composition, antioxidant and antimicrobial activities. Eighteen different phenolic compounds were identified and quantified by chemical analysis and gallic acid was the most abundant in all the extracts analyzed. Other relevant compounds were chlorogenic acid, protocatechuic acid and catechin. Preventive maceration had a positive effect on the extraction of different types of compounds regardless of the method performed. Application of the high-power ultrasonic method had different effects, either positive or negative, depending on the type of compound and extraction time. All the prepared extracts showed antioxidant activity especially those prepared by maceration, and many of them were able to inhibit the growth of both B. subtilis and B. cereus.


Assuntos
Antibacterianos/farmacologia , Antioxidantes/farmacologia , Bacillus cereus/efeitos dos fármacos , Bacillus subtilis/efeitos dos fármacos , Corylus/química , Extratos Vegetais/farmacologia , Antibacterianos/química , Antibacterianos/isolamento & purificação , Antioxidantes/química , Antioxidantes/isolamento & purificação , Benzotiazóis/antagonistas & inibidores , Compostos de Bifenilo/antagonistas & inibidores , Testes de Sensibilidade Microbiana , Picratos/antagonistas & inibidores , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Ácidos Sulfônicos/antagonistas & inibidores
17.
Chem Biodivers ; 18(12): e2100679, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-34651409

RESUMO

Pomelo seeds (PS) are important by-product of pomelo fruits (Citrus grandis Osbeck). The value-added utilization of PS remains highly challenged. This study aimed to investigate the utilization potential of PS as natural antioxidant, antibacterial, herbicidal agents, and their functional components. The ethanolic extract (EE) of PS and its four fractions as PEE (petroleum ether extract), AcOEtE (ethyl acetate extract), BTE (butanol extract), and WE (water extract), were prepared and biologically evaluated. BTE exhibited the best antioxidant activity among all these extracts, in both ABTS (2,2-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt) and FRAP (ferric reducing antioxidant power) assays. AcOEtE was superior to other extracts in herbicidal assay against both Festuca elata Keng (IC50 of 0.48 mg mL-1 ) and Amaranthus retroflexus L. (IC50 of 0.94 mg mL-1 ). Meanwhile, both AcOEtE and BTE demonstrated inhibitory effects against Bacillus subtilis, Escherichia coli, and Xanthomonas citri subsp. citri, with MIC ranging 2.5-5.0 mg mL-1 . Furthermore, the primary chemical components involving naringin, deacetylnomilin, limonin, nomilin, and obacunone, were quantified in all these extracts. PCA (principal component analysis) suggested that naringin might highly contribute to the antioxidant activity of PS, and the herbicidal activity should be ascribed to limonoids. This study successfully identified AcOEtE and BTE as naturally occurring antioxidant, antibacterial, and herbicidal agents, showing application potential in food and cosmetics industries, and organic farming agriculture.


Assuntos
Antibacterianos/farmacologia , Antioxidantes/farmacologia , Citrus/química , Herbicidas/farmacologia , Extratos Vegetais/farmacologia , Sementes/química , Amaranthus/efeitos dos fármacos , Antibacterianos/química , Antibacterianos/isolamento & purificação , Antioxidantes/química , Antioxidantes/isolamento & purificação , Bacillus subtilis/efeitos dos fármacos , Benzotiazóis/antagonistas & inibidores , Escherichia coli/efeitos dos fármacos , Festuca/efeitos dos fármacos , Herbicidas/química , Herbicidas/isolamento & purificação , Testes de Sensibilidade Microbiana , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Ácidos Sulfônicos/antagonistas & inibidores , Xanthomonas/efeitos dos fármacos
18.
Bioorg Med Chem ; 50: 116463, 2021 11 15.
Artigo em Inglês | MEDLINE | ID: mdl-34700238

RESUMO

There is an increasing demand to discover novel antibacterial drugs to counter the ever-evolving genetic machinery of bacteria. The cell division protein FtsZ plays a vital role in bacterial cytokinesis and has been recognized as an effective antibacterial drug target. In this study, we have shown that the madder dye purpurin inhibited bacterial cytokinesis through perturbation of FtsZ assembly. Purpurin inhibited the growth of bacterial cells in a concentration-dependent manner and induced bacterial cell filamentation. Microscopy studies showed that it inhibited the localization of the Z ring at the midcell, and FtsZ was dispersed throughout the cells. Further, purpurin bound firmly to FtsZ with a dissociation constant of 11 µM and inhibited its assembly in vitro. It reduced the GTP hydrolysis by binding closer to the nucleotide-binding site of FtsZ. Purpurin inhibited the proliferation of mammalian cancer cells at higher concentrations without disturbing the polymerization of tubulin. The results collectively suggest that the natural anthraquinone purpurin can potently inhibit the growth of bacteria and serve as a lead molecule for the development of antibacterial agents.


Assuntos
Antraquinonas/farmacologia , Antibacterianos/farmacologia , Antineoplásicos/farmacologia , Bacillus subtilis/efeitos dos fármacos , Proteínas de Bactérias/antagonistas & inibidores , Produtos Biológicos/farmacologia , Proteínas do Citoesqueleto/antagonistas & inibidores , Escherichia coli/efeitos dos fármacos , Antraquinonas/química , Antraquinonas/isolamento & purificação , Antibacterianos/química , Antibacterianos/isolamento & purificação , Antineoplásicos/química , Antineoplásicos/isolamento & purificação , Bacillus subtilis/química , Produtos Biológicos/química , Produtos Biológicos/isolamento & purificação , Proliferação de Células/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Escherichia coli/química , Células HeLa , Humanos , Modelos Moleculares , Estrutura Molecular , Relação Estrutura-Atividade , Células Tumorais Cultivadas
19.
Int J Biol Macromol ; 189: 251-261, 2021 Oct 31.
Artigo em Inglês | MEDLINE | ID: mdl-34425124

RESUMO

This research aims to develop white bread shelf-life extension sachet with controlled release of antimicrobial agent prepared from multicomponent bio-based materials. The structure of antimicrobial sachet consists of two major parts i.e., controlled release part and active part. The first part produced from paper coated with ethylene vinyl alcohol (EVOH). The second one was an active part which produced from biodegradable poly(butylene succinate) (PBS) and geraniol essential oil blend. Inhibition clear zone test results showed that a suitable geraniol concentration, encapsulated in PBS, was 10 wt%. Based on the water vapor transmission test, coating paper with EVOH for three times (around 450 µm) was an optimal condition for the use as a controlled release part. Release test indicated that geraniol migration concentration increased with increasing the relative humidity (RH) in the package which correlated to the moisture liberated from bread slice. Shelf-life extension study informed that the spoilage of bread stored with antimicrobial sachet was delayed by more than three weeks. In summary, this antimicrobial sachet could be used in food shelf-life extension purpose which easily placed in any food container. This is an alternative way of food waste minimization.


Assuntos
Monoterpenos Acíclicos/farmacologia , Anti-Infecciosos/farmacologia , Pão , Butileno Glicóis/química , Preparações de Ação Retardada/farmacologia , Conservação de Alimentos , Papel , Polímeros/química , Polivinil/química , Bacillus subtilis/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Umidade , Testes de Sensibilidade Microbiana , Fenômenos Ópticos , Vapor
20.
Int J Biol Macromol ; 189: 18-33, 2021 Oct 31.
Artigo em Inglês | MEDLINE | ID: mdl-34389391

RESUMO

In the present study, we have used seed extract of P. nigrum as an effective reducing agent for the synthesis of silver nanoparticles (Ag NPs) and silver based chitosan nanocomposite (Ag/CS NC). The silver nanoparticles were characterized by UV-vis spectroscopy, X-ray diffraction (XRD), scanning electron microscope (SEM), transmission electron microscope (TEM) and Fourier transform infrared spectroscopy (FTIR). The appearance of a surface plasmon resonance (SPR) peak located at 430 nm reveals the formation of silver nanoparticles. The TEM analysis indicates that the attained silver nanoparticles were mostly in spherical shapes with sizes ranging between 15 and 38 nm. The high resolution liquid chromatography with mass spectroscopy (HR-LCMS) analysis was performed to screen the phytochemical constituents of P. nigrum seed extract. The silver nanoparticles synthesized by P. nigrum seed extract exhibited effective antibacterial activity against Bacillus subtilis (B. subtilis) and Escherichia coli (E. coli). In addition, the silver nanoparticles showed potent cytotoxicity against hazardous human cancer cell lines MDA-MB-231, PANC-1, SKOV-3, PC-3 and Hela. The observation of bright spots in the TEM dark field images represents the presence of Ag in CS suspension. Besides, the Ag/CS NC coated cotton fabric substantially showed remarkable antibacterial activity against B. subtilis and E. coli.


Assuntos
Antibacterianos/farmacologia , Quitosana/química , Química Verde , Nanopartículas Metálicas/química , Nanocompostos/química , Piper nigrum/química , Extratos Vegetais/farmacologia , Prata/farmacologia , Bacillus subtilis/efeitos dos fármacos , Morte Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Fibra de Algodão , Escherichia coli/efeitos dos fármacos , Humanos , Nanopartículas Metálicas/ultraestrutura , Testes de Sensibilidade Microbiana , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Sementes/química , Espectrometria por Raios X , Espectrofotometria Ultravioleta , Espectroscopia de Infravermelho com Transformada de Fourier , Difração de Raios X
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