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1.
Int J Nanomedicine ; 19: 2995-3007, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38559446

RESUMO

Background: In the past decades, antimicrobial resistance (AMR) has been a major threat to global public health. Long-term, chronic otitis media is becoming more challenging to treat, thus the novel antibiotic alternative agents are much needed. Methods: ZnO@TiO2@AMP (ATZ NPs) were synthesized through a solvothermal method and subjected to comprehensive characterization. The in vitro and in vivo antibacterial effect and biocompatibility of ATZ NPs were evaluated. For the antibacterial mechanism exploration, we utilized the Electron Paramagnetic Resonance (EPR) Spectrometer to detect and analyze the hydroxyl radicals produced by ATZ NPs. Results: ATZ NPs exhibited a spherical structure of 99.85 nm, the drug-loading rate for ZnO was 20.73%, and AMP within ATZ NPs was 41.86%. Notably, the Minimum Inhibitory Concentration (MIC) value of ATZ NPs against Staphylococcus aureus (S. aureus), methicillin-resistant Staphylococcus aureus (MRSA), and Streptococcus pneumoniae (S. pneumoniae) were 10 µg/mL, and Minimum Bactericidal Concentration (MBC) value of ATZ NPs against S. aureus, and S. pneumoniae were 50 µg/mL. In comparison to the model group, the treatment of otitis media with ATZ NPs significantly reduces inflammatory exudation in the middle ear cavity, with no observable damage to the tympanic membrane. Both in vivo and in vitro toxicity tests indicating the good biocompatibility of ATZ NPs. Moreover, EPR spectroscopy results highlighted the superior ability of ATZ NPs to generate hydroxyl radicals (·OH) compared to ZnO NPs. Conclusion: ATZ NPs exhibited remarkable antibacterial properties both in vivo and in vitro. This innovative application of advanced ATZ NPs, bringing great promise for the treatment of otitis media.


Assuntos
Nanopartículas Metálicas , Staphylococcus aureus Resistente à Meticilina , Otite Média , Infecções Estafilocócicas , Óxido de Zinco , Humanos , Staphylococcus aureus , Radical Hidroxila , Óxido de Zinco/farmacologia , Óxido de Zinco/química , Antibacterianos/farmacologia , Antibacterianos/química , Otite Média/tratamento farmacológico , Testes de Sensibilidade Microbiana , Nanopartículas Metálicas/química
2.
Int J Nanomedicine ; 19: 3045-3070, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38559447

RESUMO

Background: Diabetes Mellitus is a multisystem chronic pandemic, wound inflammation, and healing are still major issues for diabetic patients who may suffer from ulcers, gangrene, and other wounds from uncontrolled chronic hyperglycemia. Marshmallows or Althaea officinalis (A.O.) contain bioactive compounds such as flavonoids and phenolics that support wound healing via antioxidant, anti-inflammatory, and antibacterial properties. Our study aimed to develop a combination of eco-friendly formulations of green synthesis of ZnO-NPs by Althaea officinalis extract and further incorporate them into 2% chitosan (CS) gel. Method and Results: First, develop eco-friendly green Zinc Oxide Nanoparticles (ZnO-NPs) and incorporate them into a 2% chitosan (CS) gel. In-vitro study performed by UV-visible spectrum analysis showed a sharp peak at 390 nm, and Energy-dispersive X-ray (EDX) spectrometry showed a peak of zinc and oxygen. Besides, Fourier transforms infrared (FTIR) was used to qualitatively validate biosynthesized ZnO-NPs, and transmission electron microscope (TEM) showed spherical nanoparticles with mean sizes of 76 nm and Zeta potential +30mV. The antibacterial potential of A.O.-ZnO-NPs-Cs was examined by the diffusion agar method against Gram-positive (Staphylococcus aureus and Bacillus subtilis) and Gram-negative bacteria (Escherichia coli and Pseudomonas aeruginosa). Based on the zone of inhibition and minimal inhibitory indices (MIC). In addition, an in-silico study investigated the binding affinity of A.O. major components to the expected biological targets that may aid wound healing. Althaea Officinalis, A.O-ZnO-NPs group showed reduced downregulation of IL-6, IL-1ß, and TNF-α and increased IL-10 levels compared to the control group signaling pathway expression levels confirming the improved anti-inflammatory effect of the self-assembly method. In-vivo study and histopathological analysis revealed the superiority of the nanoparticles in reducing signs of inflammation and wound incision in rat models. Conclusion: These biocompatible green zinc oxide nanoparticles, by using Althaea Officinalis chitosan gel ensure an excellent new therapeutic approach for quickening diabetic wound healing.


Assuntos
Althaea , Quitosana , Diabetes Mellitus , Nanopartículas Metálicas , Óxido de Zinco , Humanos , Animais , Ratos , Óxido de Zinco/química , Quitosana/química , Althaea/metabolismo , Interleucina-6 , Fator de Necrose Tumoral alfa , Nanopartículas Metálicas/química , Antibacterianos/farmacologia , Antibacterianos/química , Cicatrização , Anti-Inflamatórios/farmacologia , Inflamação , Flores , Testes de Sensibilidade Microbiana , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Espectroscopia de Infravermelho com Transformada de Fourier , Difração de Raios X
3.
J Biochem Mol Toxicol ; 38(4): e23706, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38591869

RESUMO

In this study, our goal was to synthesize novel aryl tacrine derivatives and assess their potential as anticancer, antibacterial agents, and enzyme inhibitors. We adopted a two-step approach, initiating with the synthesis of dibromotacrine derivatives 3 and 4 through the Friedlander reaction. These intermediates underwent further transformation into diarylated tacrine derivatives 3a-e and 4a-e using a Suzuki-Miyaura cross-coupling reaction. Thorough characterization of these novel diarylated tacrines was achieved using various spectroscopic techniques. Our findings highlighted the potent anticancer effects of these innovative compounds across a range of cancer cell lines, including lung, gynecologic, bone, colon, and breast cancers, while demonstrating low cytotoxicity against normal cells. Notably, these compounds surpassed the control drug, 5-Fluorouracil, in terms of antiproliferative activity in numerous cancer cell lines. Moreover, our investigation included an analysis of the inhibitory properties of these novel compounds against various microorganisms and cytosolic carbonic anhydrase enzymes. The results suggest their potential for further exploration as cancer-specific, enzyme inhibitory, and antibacterial therapeutic agents. Notably, four compounds, namely, 5,7-bis(4-(methylthio)phenyl)tacrine (3d), 5,7-bis(4-(trifluoromethoxy)phenyl)tacrine (3e), 2,4-bis(4-(trifluoromethoxy)phenyl)-7,8,9,10-tetrahydro-6H-cyclohepta[b]quinolin-11-amine (4e), and 6,8-dibromotacrine (3), emerged as the most promising candidates for preclinical studies.


Assuntos
Antineoplásicos , Neoplasias , Feminino , Humanos , Tacrina/farmacologia , Tacrina/química , Antifúngicos/farmacologia , Anticonvulsivantes/farmacologia , Antibacterianos/farmacologia , Antibacterianos/química , Inibidores Enzimáticos/farmacologia , Antineoplásicos/química , Relação Estrutura-Atividade , Estrutura Molecular
4.
Sci Rep ; 14(1): 8045, 2024 04 05.
Artigo em Inglês | MEDLINE | ID: mdl-38580674

RESUMO

Silver and titanium-silver nanoparticles have unique properties that make the textile industry progress through the high quality of textiles. Preparation of AgNPs and TiO2-Ag core-shell nanoparticles in different concentrations (0.01% and 0.1% OWF) and applying it to cotton fabrics (Giza 88 and Giza 94) by using succinic acid 5%/SHP as a cross-linking agent. Ultra-violet visible spectroscopy (UV-Vis), X-ray diffraction (XRD), dynamic light scattering (DLS), zeta potential, transmission electron microscopy (TEM), scanning electron microscopy/energy-dispersive X-ray (SEM-EDX) are tools for AgNPs and TiO2-AgNPs characterization and the treated cotton. The resulting AgNPs and TiO2-AgNPs were added to cotton fabrics at different concentrations. The antimicrobial activities, UV protection, self-cleaning, and the treated fabrics' mechanical characteristics were investigated. Silver nanoparticles and titanium dioxide-silver nanoparticles core-shell were prepared to be used in the treatment of cotton fabrics to improve their UV protection properties, self-cleaning, elongation and strength, as well as the antimicrobial activities to use the produced textiles for medical and laboratory uses and to increase protection for medical workers taking into account the spread of infection. The results demonstrated that a suitable distribution of prepared AgNPs supported the spherical form. Additionally, AgNPs and TiO2-AgNPs have both achieved stability, with values of (- 20.8 mV and - 30 mV, respectively). The synthesized nanoparticles spread and penetrated textiles' surfaces with efficiency. The findings demonstrated the superior UV protection value (UPF 50+) and self-cleaning capabilities of AgNPs and TiO2-AgNPs. In the treatment with 0.01% AgNPs and TiO2-AgNPs, the tensile strength dropped, but the mechanical characteristics were enhanced by raising the concentration to 0.1%. The results of this investigation demonstrated that the cotton fabric treated with TiO2-AgNPs exhibited superior general characteristics when compared to the sample treated only with AgNPs.


Assuntos
Anti-Infecciosos , Nanopartículas Metálicas , Humanos , Prata/química , Fibra de Algodão , Ácido Succínico , Nanopartículas Metálicas/química , Têxteis , Antibacterianos/farmacologia , Antibacterianos/química
5.
Sci Rep ; 14(1): 8025, 2024 04 05.
Artigo em Inglês | MEDLINE | ID: mdl-38580807

RESUMO

The modification of the surgical polypropylene mesh and the polytetrafluoroethylene vascular prosthesis with cecropin A (small peptide) and puromycin (aminonucleoside) yielded very stable preparations of modified biomaterials. The main emphasis was placed on analyses of their antimicrobial activity and potential immunomodulatory and non-cytotoxic properties towards the CCD841 CoTr model cell line. Cecropin A did not significantly affect the viability or proliferation of the CCD 841 CoTr cells, regardless of its soluble or immobilized form. In contrast, puromycin did not induce a significant decrease in the cell viability or proliferation in the immobilized form but significantly decreased cell viability and proliferation when administered in the soluble form. The covalent immobilization of these two molecules on the surface of biomaterials resulted in stable preparations that were able to inhibit the multiplication of Staphylococcus aureus and S. epidermidis strains. It was also found that the preparations induced the production of cytokines involved in antibacterial protection mechanisms and stimulated the immune response. The key regulator of this activity may be related to TLR4, a receptor recognizing bacterial LPS. In the present study, these factors were produced not only in the conditions of LPS stimulation but also in the absence of LPS, which indicates that cecropin A- and puromycin-modified biomaterials may upregulate pathways leading to humoral antibacterial immune response.


Assuntos
Anti-Infecciosos , Materiais Biocompatíveis , Materiais Biocompatíveis/farmacologia , Lipopolissacarídeos , Anti-Infecciosos/farmacologia , Antibacterianos/farmacologia , Antibacterianos/química , Polímeros/farmacologia , Staphylococcus epidermidis , Puromicina
6.
J Nanobiotechnology ; 22(1): 161, 2024 Apr 08.
Artigo em Inglês | MEDLINE | ID: mdl-38589895

RESUMO

Antibiotic resistance has garnered significant attention due to the scarcity of new antibiotics in development. Protoporphyrin IX (PpIX)-mediated photodynamic therapy shows promise as a novel antibacterial strategy, serving as an alternative to antibiotics. However, the poor solubility of PpIX and its tendency to aggregate greatly hinder its photodynamic efficacy. In this study, we demonstrate that alkylated EDTA derivatives (aEDTA), particularly C14-EDTA, can enhance the solubility of PpIX by facilitating its dispersion in aqueous solutions. The combination of C14-EDTA and PpIX exhibits potent antibacterial activity against Staphylococcus aureus (S. aureus) when exposed to LED light irradiation. Furthermore, this combination effectively eradicates S. aureus biofilms, which are known to be strongly resistant to antibiotics, and demonstrates high therapeutic efficacy in an animal model of infected ulcers. Mechanistic studies reveal that C14-EDTA can disrupt PpIX crystallization, increase bacterial membrane permeability and sequester divalent cations, thereby improving the accumulation of PpIX in bacteria. This, in turn, enhances reactive oxygen species (ROS) production and the antibacterial photodynamic activity. Overall, this effective strategy holds great promise in combating antibiotic-resistant strains.


Assuntos
Fotoquimioterapia , Staphylococcus aureus , Animais , Protoporfirinas/farmacologia , Ácido Edético/farmacologia , Antibacterianos/farmacologia , Antibacterianos/química , Fármacos Fotossensibilizantes/farmacologia , Fármacos Fotossensibilizantes/química
7.
Proc Natl Acad Sci U S A ; 121(17): e2322363121, 2024 Apr 23.
Artigo em Inglês | MEDLINE | ID: mdl-38640341

RESUMO

Anti-microbial resistance (AMR) is one of the greatest threats to global health. The continual battle between the emergence of AMR and the development of drugs will be extremely difficult to stop as long as traditional anti-biotic approaches are taken. In order to overcome this impasse, we here focused on the type III secretion system (T3SS), which is highly conserved in many Gram-negative pathogenic bacteria. The T3SS is known to be indispensable in establishing disease processes but not essential for pathogen survival. Therefore, T3SS inhibitors may be innovative anti-infective agents that could dramatically reduce the evolutionary selective pressure on strains resistant to treatment. Based on this concept, we previously identified a polyketide natural product, aurodox (AD), as a specific T3SS inhibitor using our original screening system. However, despite its promise as a unique anti-infective drug of AD, the molecular target of AD has remained unclear. In this paper, using an innovative chemistry and genetic biology-based approach, we show that AD binds to adenylosuccinate synthase (PurA), which suppresses the production of the secreted proteins from T3SS, resulting in the expression of bacterial virulence both in vitro and in vivo experiments. Our findings illuminate the potential of PurA as a target of anti-infective drugs and vaccination and could open a avenue for application of PurA in the regulation of T3SS.


Assuntos
Aurodox , Sistemas de Secreção Tipo III , Sistemas de Secreção Tipo III/metabolismo , Aurodox/farmacologia , Antibacterianos/farmacologia , Antibacterianos/química , Bactérias Gram-Negativas/metabolismo , Proteínas de Bactérias/metabolismo
8.
BMC Complement Med Ther ; 24(1): 164, 2024 Apr 19.
Artigo em Inglês | MEDLINE | ID: mdl-38641582

RESUMO

BACKGROUND: Infections caused by Acinetobacter baumannii are becoming a rising public health problem due to its high degree of acquired and intrinsic resistance mechanisms. Bacterial lipases penetrate and damage host tissues, resulting in multiple infections. Because there are very few effective inhibitors of bacterial lipases, new alternatives for treating A. baumannii infections are urgently needed. In recent years, Brassica vegetables have received a lot of attention since their phytochemical compounds have been directly linked to diverse antimicrobial actions by inhibiting the growth of various Gram-positive and Gram-negative bacteria, yeast, and fungi. Despite their longstanding antibacterial history, there is currently a lack of scientific evidence to support their role in the management of infections caused by the nosocomial bacterium, A. baumannii. This study aimed to address this gap in knowledge by examining the antibacterial and lipase inhibitory effects of six commonly consumed Brassica greens, Chinese cabbage (CC), curly and Tuscan kale (CK and TK), red and green Pak choi (RP and GP), and Brussels sprouts (BR), against A. baumannii in relation to their chemical profiles. METHODS: The secondary metabolites of the six extracts were identified using LC-QTOF-MS/MS analysis, and they were subsequently correlated with the lipase inhibitory activity using multivariate data analysis and molecular docking. RESULTS: In total, 99 metabolites from various chemical classes were identified in the extracts. Hierarchical cluster analysis (HCA) and principal component analysis (PCA) revealed the chemical similarities and variabilities among the specimens, with glucosinolates and phenolic compounds being the major metabolites. RP and GP showed the highest antibacterial activity against A. baumannii, followed by CK. Additionally, four species showed a significant effect on the bacterial growth curves and demonstrated relevant inhibition of A. baumannii lipolytic activity. CK showed the greatest inhibition (26%), followed by RP (21%), GP (21%), and TK (15%). Orthogonal partial least squares-discriminant analysis (OPLS-DA) pinpointed 9 metabolites positively correlated with the observed bioactivities. Further, the biomarkers displayed good binding affinities towards lipase active sites ranging from -70.61 to -30.91 kcal/mol, compared to orlistat. CONCLUSION: This study emphasizes the significance of Brassica vegetables as a novel natural source of potential inhibitors of lipase from A. baumannii.


Assuntos
Acinetobacter baumannii , Brassica , Brassica/química , Simulação de Acoplamento Molecular , Antibacterianos/farmacologia , Antibacterianos/química , Espectrometria de Massas em Tandem , Bactérias Gram-Negativas , Bactérias Gram-Positivas , Compostos Fitoquímicos/farmacologia , Lipase
9.
BMC Complement Med Ther ; 24(1): 165, 2024 Apr 19.
Artigo em Inglês | MEDLINE | ID: mdl-38641781

RESUMO

In this study we develop novel type of antibacterial chitosan-propolis NPs to improve theantimicrobial activity against various pathogens. To this aim, we primarily extracted propolis with methylal and ethanol as green solvents and its encapsulation with chitosan NPs. The developed propolis loaded chitosan NPs indicated antimicrobial and anti-biofilm properties against various gram positive and negative. FTIR revealed the successful encapsulation of the propolis extract with Ethanol (PE) and Methylal (PM) into the chitosan nano career matrix. HPLC and GC-MASS also confirmed the presence of flavonoids and phenols compounds of propolis extracted with both solvents. In addition, we confirmed the total phenolic and flavonoid compounds in propolis by calorimetric method of Folin-Ciocalteu and aluminum trichloride complex formation assays, respectively. PE-CH and PM-CH were optimized regarding physicochemical properties such as particle size, zeta potential, and poly dispersity index (PDI) index. DLS and SEM micrographs confirmed a spherical morphology in a range of 360-420 nm with Z potential values of 30-48 mV and PDI of 0.105-0.166 for PE-CH and PM-CH, respectively. The encapsulation efficiency was evaluated using colorimetric analysis, with median values ranging from 90 to 92%. The MIC values within the range of 2 to 230 µg/ml and MBC values between 3 to 346 µg/ml against both gram-positive and negative bacteria. While both PE and PM showed a significant reduction in the number of E. coli, S. aureus, and S. epidermidis, the use of PE-CH and PM-CH led to a statistically significant and greater reduction in number of E. coli, S. aureus, and S. epidermidis strains on the biofilm, pre-formed biofilm and planktonic phases. Besides, the DPPH assay showed significant antioxidant activity for these NPs within the range of 36 to 92%. MTT assay for MHFB-1, HFF, L929, MDF, and MCF-7 cells exhibited statistically significant differences in each other that show the IC50 between 60-160 µg/ml for normal cells and 20 for cancer cells. Finally the present study indicated that both PM and PM-CH greater than PE and PE-CH in which contain high flavonoid and phenolic contents with a high antioxidation potential antioxidant properties, which could be beneficial for cell proliferation and antibiotic and anticancer applications.


Assuntos
Quitosana , Éteres Metílicos , Nanopartículas , Própole , Própole/farmacologia , Quitosana/química , Escherichia coli , Staphylococcus aureus , Antibacterianos/farmacologia , Antibacterianos/química , Solventes , Etanol , Nanopartículas/química , Flavonoides
10.
ACS Appl Bio Mater ; 7(4): 2346-2353, 2024 Apr 15.
Artigo em Inglês | MEDLINE | ID: mdl-38556982

RESUMO

In this study, we designed and synthesized metalloporphyrin derivatives (with Ni and Zn) specifically intended for the fluorescence detection of nicotine in aqueous solutions. Our results showcased a notable selectivity for nicotine over other naturally occurring food toxins, exhibiting an exceptional sensitivity with a limit of detection as low as 7.2 nM. Through mechanistic investigations (1H NMR, FT-IR, etc.), we elucidated the binding mechanism, revealing the specific interaction between the pyridine ring of nicotine and the metal center, while the N atom pyrrolidine unit engaged in the hydrogen bonding with the side chain of the porphyrin ring. Notably, we observed that the nature of the metal center dictated the extent of interaction with nicotine; particularly, Zn-porphyrin demonstrated a superior response compared to Ni-porphyrin. Furthermore, we performed the quantitative estimation of nicotine in commercially available tobacco products. Additionally, we conducted the antibacterial (Staphylococcus aureus and Escherichia coli) and antifungal (Candida albicans) activities of the porphyrin derivatives.


Assuntos
Metaloporfirinas , Porfirinas , Metaloporfirinas/farmacologia , Nicotina/farmacologia , Espectroscopia de Infravermelho com Transformada de Fourier , Antibacterianos/farmacologia , Antibacterianos/química , Metais , Porfirinas/farmacologia , Porfirinas/química , Escherichia coli
11.
Bioorg Chem ; 146: 107318, 2024 May.
Artigo em Inglês | MEDLINE | ID: mdl-38579613

RESUMO

Twenty-seven rosmarinic acid derivatives were synthesized, among which compound RA-N8 exhibited the most potent antibacterial ability. The minimum inhibition concentration of RA-N8 against both S. aureus (ATCC 29213) and MRSA (ATCC BAA41 and ATCC 43300) was found to be 6 µg/mL, and RA-N8 killed E. coli (ATCC 25922) at 3 µg/mL in the presence of polymyxin B nonapeptide (PMBN) which increased the permeability of E. coli. RA-N8 exhibited a weak hemolytic effect at the minimum inhibitory concentration. SYTOX Green assay, SEM, and LIVE/DEAD fluorescence staining assay proved that the mode of action of RA-N8 is targeting bacterial cell membranes. Furthermore, no resistance in wildtype S. aureus developed after incubation with RA-N8 for 20 passages. Cytotoxicity studies further demonstrated that RA-N8 is non-toxic to the human normal cell line (HFF1). RA-N8 also exerted potent inhibitory ability against biofilm formation of S. aureus and even collapsed the shaped biofilm.


Assuntos
Antibacterianos , Staphylococcus aureus Resistente à Meticilina , Humanos , Antibacterianos/química , Staphylococcus aureus , 60556 , Escherichia coli , Relação Estrutura-Atividade , Testes de Sensibilidade Microbiana , Biofilmes
12.
Eur J Med Chem ; 270: 116392, 2024 Apr 15.
Artigo em Inglês | MEDLINE | ID: mdl-38608408

RESUMO

The emergence of serious bacterial resistance towards clinical oxacins poses a considerable threat to global public health, necessitating the development of novel structural antibacterial agents. Seven types of novel indolylacryloyl-derived oxacins (IDOs) were designed and synthesized for the first time from commercial 3,4-difluoroaniline via an eight-step procedure. The synthesized compounds were characterized by modern spectroscopic techniques. All target molecules were evaluated for antimicrobial activities. Most of the prepared IDOs showed a broad antibacterial spectrum and strong activities against the tested strains, especially ethoxycarbonyl IDO 10d (0.25-0.5 µg/mL) and hydroxyethyl IDO 10e (0.25-1 µg/mL) exhibited much superior antibacterial efficacies to reference drug norfloxacin. These highly active IDOs also displayed low hemolysis, cytotoxicity and resistance, as well as rapid bactericidal capacity. Further investigations indicated that ethoxycarbonyl IDO 10d and hydroxyethyl IDO 10e could effectively reduce the exopolysaccharide content and eradicate the formed biofilm, which might delay the development of drug resistance. Preliminary exploration of the antibacterial mechanism revealed that active IDOs could not only destroy membrane integrity, resulting in changes in membrane permeability, but also promote the accumulation of reactive oxygen species, leading to the production of malondialdehyde and decreased bacterial metabolism. Moreover, they exhibited the capability to bind with DNA and DNA gyrase, forming supramolecular complexes through various noncovalent interactions, thereby inhibiting DNA replication and causing bacterial death. All the above results suggested that the newly developed indolylacryloyl-derived oxacins should hold great promise as potential multitargeting broad-spectrum antibacterial candidates to overcome drug resistance.


Assuntos
Antibacterianos , Norfloxacino , Antibacterianos/farmacologia , Antibacterianos/química , Norfloxacino/farmacologia , Bactérias , Permeabilidade da Membrana Celular , DNA/farmacologia , Testes de Sensibilidade Microbiana
13.
BMC Complement Med Ther ; 24(1): 137, 2024 Apr 02.
Artigo em Inglês | MEDLINE | ID: mdl-38566161

RESUMO

BACKGROUND: A study carried out by World Health Organization revealed that around 80% of individuals globally depends on herbal forms of medication with 40% of pharmaceutical products being sourced from medicinal plants. The study objective was to evaluate the phytochemicals composition, in vitro antimicrobial and antioxidant properties of the leaves of Terminalia catappa L. aqueous and methanolic extracts. METHODS: Antimicrobial activity was analyzed by disk diffusion, the minimum inhibitory concentration in-vitro assays with ciprofloxacin as the standard for antibacterial assay while nystatin for antifungal assay. Ferric reducing antioxidant power and 2,2-diphenyl-1-picryl-hydrazyl-hydrate assays were used for the evaluation of antioxidant properties of the crude extracts while the groups responsible for this activity identified using Fourier transform infrared spectrophotometer. RESULTS: The study found that the leaves of Terminalia catappa contained alkaloids, tannins, steroids, cardiac glycosides, flavonoids, phenols, saponins, and coumarins, but terpenoids were absent. Presence of functional groups associated with this class of compounds such as OH vibrational frequencies were observed in IR spectrum of the crude extracts. Methanolic extract from Terminalia catappa exhibited greater antibacterial properties against Pseudomonas aeruginosa, Escherichia coli and Staphylococcus aureus, whereas aqueous extract displayed greater antibacterial activity against Bacillus subtilis for all concentrations tested. The amount of the sample that scavenged 50 percent of DPPH (IC50) was found to be 8.723, 13.42 and 13.04 µg/mL for L-ascorbic acid, Terminalia catappa L. methanolic and aqueous extracts respectively. The antimicrobial and antioxidant activities varied with the extract concentration and solvent used in extractions. CONCLUSION: Terminalia catappa L. leaves are prospective for use as a source of therapeutic agents that could lead to the advancement of new antimicrobial and antioxidant products.


Assuntos
Anti-Infecciosos , Terminalia , Humanos , Antioxidantes/química , Metanol , Terminalia/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Estudos Prospectivos , Anti-Infecciosos/química , Antibacterianos/farmacologia , Antibacterianos/química , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/química , Água
14.
Sci Rep ; 14(1): 7940, 2024 04 04.
Artigo em Inglês | MEDLINE | ID: mdl-38575777

RESUMO

Bacterial infections triggered by patient or healthcare worker contact with surfaces are a major cause of medically acquired infections. By controlling the kinetics of tetrabutyl titanate hydrolysis and condensation during the sol-gel process, it is possible to regulate the content of Ti3+ and oxygen vacancies (OVs) in TiO2, and adjust the associated visible light-induced photocatalytic performance and anti-bacterial adhesion properties. The results have shown that the Ti3+ content in TiO2 was 9.87% at the calcination temperature of the reaction system was 300 °C and pH was 1.0, corresponding to optimal photocatalytic and hydrophilic properties. The formation of a hydrated layer on the superhydrophilic surface provided resistance to bacterial adhesion, preventing cross-contamination on high-touch surfaces. The excellent photocatalytic self-cleaning performance and anti-bacterial adhesion properties can be attributed to synergistic effects associated with the high specific surface area of TiO2 nanoparticles, the mesoporous structure, and the presence of Ti3+ and OVs. The formation of superhydrophilic self-cleaning surfaces under visible light can serve as the basis for the development of a new class of anti-bacterial adhesion materials.


Assuntos
Nanopartículas , Titânio , Humanos , Titânio/farmacologia , Titânio/química , Catálise , Propriedades de Superfície , Luz , Antibacterianos/farmacologia , Antibacterianos/química , Nanopartículas/química
15.
Amino Acids ; 56(1): 28, 2024 Apr 05.
Artigo em Inglês | MEDLINE | ID: mdl-38578302

RESUMO

In the face of increasing antimicrobial resistance in aquaculture, researchers are exploring novel substitutes to customary antibiotics. One potential solution is the use of antimicrobial peptides (AMPs). We aimed to design and evaluate a novel, short, and compositionally simple AMP with potent activity against various bacterial pathogens in aquaculture. The resulting peptide, KK12YW, has an amphipathic nature and net charge of + 7. Molecular docking experiments disclosed that KK12YW has a strong affinity for aerolysin, a virulence protein produced by the bacterial pathogen Aeromonas sobria. KK12YW was synthesized using Fmoc chemistry and tested against a range of bacterial pathogens, including A. sobria, A. salmonicida, A. hydrophila, Edwardsiella tarda, Vibrio parahaemolyticus, Pseudomonas aeruginosa, Escherichia coli, Staphylococcus epidermidis, and methicillin-resistant S. aureus. The AMP showed promising antibacterial activity, with MIC and MBC values ranging from 0.89 to 917.1 µgmL-1 and 3.67 to 1100.52 µgmL-1, respectively. In addition, KK12YW exhibited resistance to high temperatures and remained effective even in the presence of serum and salt, indicating its stability. The peptide also demonstrated minimal hemolysis toward fish RBCs, even at higher concentrations. Taken together, these findings indicate that KK12YW could be a highly promising and viable substitute for conventional antibiotics to combat microbial infections in aquaculture.


Assuntos
Staphylococcus aureus Resistente à Meticilina , Animais , Simulação de Acoplamento Molecular , Peptídeos Catiônicos Antimicrobianos/química , Antibacterianos/farmacologia , Antibacterianos/química , Escherichia coli , Peixes , Testes de Sensibilidade Microbiana
16.
Sci Rep ; 14(1): 9144, 2024 04 21.
Artigo em Inglês | MEDLINE | ID: mdl-38644378

RESUMO

In this research, different Co2+ doped ZnO nanoparticles (NPs) were hydrothermally synthesized by an environmentally friendly, sustainable technique using the extract of P. capillacea for the first time. Co-ZnO was characterized and confirmed by FTIR, XPS, XRD, BET, EDX, SEM, TEM, DRS UV-Vis spectroscopy, and TGA analyses. Dislocation density, micro strains, lattice parameters and volume of the unit cell were measured using XRD results. XRD suggests that the average size of these NPs was between 44.49 and 65.69 nm with a hexagonal wurtzite structure. Tauc plot displayed that the optical energy bandgap of ZnO NPs (3.18) slowly declines with Co doping (2.96 eV). Near complete removal of the ciprofloxacin (CIPF) antibiotic was attained using Green 5% of Hy-Co-ZnO in the existence of visible LED light which exhibited maximum degradation efficiency (99%) within 120 min for 30 ppm CIPF initial concentration. The photodegradation mechanism of CIPF using Green Hy-Co-ZnO NPs followed the Pseudo-first-order kinetics. The Green Hy-Co-ZnO NPs improved photocatalytic performance toward CIPF for 3 cycles. The experiments were designed using the RSM (CCD) method for selected parameters such as catalyst dosage, antibiotic dosage, shaking speed, and pH. The maximal CIPF degradation efficiency (96.4%) was achieved under optimum conditions of 39.45 ppm CIPF dosage, 60.56 mg catalyst dosage, 177.33 rpm shaking speed and pH 7.57.


Assuntos
Antibacterianos , Ciprofloxacina , Cobalto , Luz , Fotólise , Óxido de Zinco , Óxido de Zinco/química , Ciprofloxacina/química , Cobalto/química , Antibacterianos/química , Nanopartículas Metálicas/química , Química Verde/métodos , Nanopartículas/química , Cinética , Catálise
17.
J Hazard Mater ; 470: 134279, 2024 May 15.
Artigo em Inglês | MEDLINE | ID: mdl-38613960

RESUMO

The application of antibiotics in freshwater aquaculture leads to increased contamination of aquatic environments. However, limited information is available on the co-metabolic biodegradation of antibiotics by microalgae in aquaculture. Feedstuffs provide multiple organic substrates for microalgae-mediated co-metabolism. Herein, we investigated the co-metabolism of sulfamethoxazole (SMX) by Chlorella pyrenoidosa when adding main components of feedstuff (glucose and lysine). Results showed that lysine had an approximately 1.5-fold stronger enhancement on microalgae-mediated co-metabolism of SMX than glucose, with the highest removal rate (68.77% ± 0.50%) observed in the 9-mM-Lys co-metabolic system. Furthermore, we incorporated reactive sites predicted by density functional theory calculations, 14 co-metabolites identified by mass spectrometry, and the roles of 18 significantly activated enzymes to reveal the catalytic reaction mechanisms underlying the microalgae-mediated co-metabolism of SMX. In lysine- and glucose-treated groups, five similar co-metabolic pathways were proposed, including bond breaking on the nucleophilic sulfur atom, ring cleavage and hydroxylation at multiple free radical reaction sites, together with acylation and glutamyl conjugation on electrophilic nitrogen atoms. Cytochrome P450, serine hydrolase, and peroxidase play crucial roles in catalyzing hydroxylation, bond breaking, and ring cleavage of SMX. These findings provide theoretical support for better utilization of microalgae-driven co-metabolism to reduce sulfonamide antibiotic residues in aquaculture.


Assuntos
Aquicultura , Chlorella , Glucose , Microalgas , Sulfametoxazol , Poluentes Químicos da Água , Sulfametoxazol/metabolismo , Sulfametoxazol/química , Microalgas/metabolismo , Chlorella/metabolismo , Glucose/metabolismo , Poluentes Químicos da Água/metabolismo , Lisina/metabolismo , Lisina/química , Biodegradação Ambiental , Redes e Vias Metabólicas , Antibacterianos/metabolismo , Antibacterianos/química
18.
J Hazard Mater ; 470: 134254, 2024 May 15.
Artigo em Inglês | MEDLINE | ID: mdl-38615644

RESUMO

The existence of antibiotic resistant bacteria (ARB) and antibiotic resistance genes (ARGs) has been a global public environment and health issue. Due to the different cell structures, gram-positive/negative ARB exhibit various inactivation mechanisms in water disinfection. In this study, a gram-negative ARB Escherichia coli DH5α (E. coli DH5α) was used as a horizontal gene transfer (HGT) donor, while a gram-positive ARB Bacillus as a recipient. To develop an efficient and engineering applicable method in water disinfection, ARB and ARGs removal efficiency of Fe(VI) coupled peroxydisulfate (PDS) or peroxymonosulfate (PMS) was compared, wherein hydroxylamine (HA) was added as a reducing agent. The results indicated that Fe(VI)/PMS/HA showed higher disinfection efficiency than Fe(VI)/PDS/HA. When the concentration of each Fe(VI), PMS, HA was 0.48 mM, 5.15 log E. coli DH5α and 3.57 log Bacillus lost cultivability, while the proportion of recovered cells was 0.0017 % and 0.0566 %, respectively, and HGT was blocked. Intracellular tetA was reduced by 2.49 log. Fe(IV) and/or Fe(V) were proved to be the decisive reactive species. Due to the superiority of low cost as well as high efficiency and practicality, Fe(VI)/PMS/HA has significant application potential in ARB, ARGs removal and HGT inhibition, offering a new insight for wastewater treatment.


Assuntos
Transferência Genética Horizontal , Ferro , Peróxidos , Peróxidos/química , Ferro/química , Purificação da Água/métodos , Escherichia coli/efeitos dos fármacos , Escherichia coli/genética , Farmacorresistência Bacteriana/genética , Desinfecção/métodos , Sulfatos/química , Antibacterianos/farmacologia , Antibacterianos/química , Bacillus/genética , Bacillus/efeitos dos fármacos , Bacillus/metabolismo
19.
Microb Pathog ; 190: 106639, 2024 May.
Artigo em Inglês | MEDLINE | ID: mdl-38616002

RESUMO

BACKGROUND INFORMATION: The advancement of biological-mediated nanoscience towards higher levels and novel benchmarks is readily apparent, owing to the use of non-toxic synthesis processes and the incorporation of various additional benefits. This study aimed to synthesize stable tin oxide nanoparticles (SnO2-NPs) using S. rhizophila as a mediator. METHODS: The nanoparticles that were created by biosynthesis was examined using several analytical techniques, including Scanning Electron Microscopy (SEM) and Transmission Electron Microscopy (TEM), X-ray diffraction (XRD), UV-visible (UV-vis) spectroscopy, and energy dispersive X-ray spectroscopy (EDS). RESULTS: The results obtained from the characterization techniques suggest that S. rhizophila effectively catalyzed the reduction of SnCl2 to SnO2-NPs duration of 90 min at ambient temperature with the ƛmax of 328 nm. The size of the nano crystallite formations was measured to be 23 nm. The present study investigates nanoscale applications' antibacterial efficacy against four bacterial strains, including Klebsiella Sp, Staphylococcus aureus, Pseudomonas aeruginosa, and Escherichia coli. The observed zone of inhibition for the nanoparticles (NPs) varied from 10 to 25 mm. The research findings demonstrate that the nanoparticles (NPs) are effective as antibacterial, phytotoxic, and cytotoxic agents.


Assuntos
Antibacterianos , Biofilmes , Testes de Sensibilidade Microbiana , Compostos de Estanho , Difração de Raios X , Compostos de Estanho/química , Compostos de Estanho/farmacologia , Biofilmes/efeitos dos fármacos , Antibacterianos/farmacologia , Antibacterianos/química , Animais , Staphylococcus aureus/efeitos dos fármacos , Nanopartículas/química , Bactérias/efeitos dos fármacos , Nanopartículas Metálicas/química , Nanopartículas Metálicas/toxicidade , Escherichia coli/efeitos dos fármacos , Pseudomonas aeruginosa/efeitos dos fármacos , Microscopia Eletrônica de Transmissão , Microscopia Eletrônica de Varredura , Tamanho da Partícula
20.
ACS Infect Dis ; 10(4): 1137-1151, 2024 Apr 12.
Artigo em Inglês | MEDLINE | ID: mdl-38606465

RESUMO

Antimicrobial resistance is a global threat to human health. Therefore, efforts have been made to develop new antibacterial agents that address this critical medical issue. Gepotidacin is a novel, bactericidal, first-in-class triazaacenaphthylene antibacterial in clinical development. Recently, phase III clinical trials for gepotidacin treatment of uncomplicated urinary tract infections caused by uropathogens, including Escherichia coli, were stopped for demonstrated efficacy. Because of the clinical promise of gepotidacin, it is important to understand how the compound interacts with its cellular targets, gyrase and topoisomerase IV, from E. coli. Consequently, we determined how gyrase and topoisomerase IV mutations in amino acid residues that are involved in gepotidacin interactions affect the susceptibility of E. coli cells to the compound and characterized the effects of gepotidacin on the activities of purified wild-type and mutant gyrase and topoisomerase IV. Gepotidacin displayed well-balanced dual-targeting of gyrase and topoisomerase IV in E. coli cells, which was reflected in a similar inhibition of the catalytic activities of these enzymes by the compound. Gepotidacin induced gyrase/topoisomerase IV-mediated single-stranded, but not double-stranded, DNA breaks. Mutations in GyrA and ParC amino acid residues that interact with gepotidacin altered the activity of the compound against the enzymes and, when present in both gyrase and topoisomerase IV, reduced the antibacterial activity of gepotidacin against this mutant strain. Our studies provide insights regarding the well-balanced dual-targeting of gyrase and topoisomerase IV by gepotidacin in E. coli.


Assuntos
Acenaftenos , DNA Topoisomerase IV , Escherichia coli , Compostos Heterocíclicos com 3 Anéis , Humanos , DNA Topoisomerase IV/genética , DNA Girase/metabolismo , Antibacterianos/farmacologia , Antibacterianos/química , Aminoácidos/farmacologia
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