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1.
Int J Biol Macromol ; : 134143, 2024 Jul 26.
Article in English | MEDLINE | ID: mdl-39069060

ABSTRACT

In this study, hydroxyapatite (HAp) was synthesized from natural biowaste materials, specifically mussel shells, and combined with chitosan (CS) and gentamicin sulfate antibiotic (GA) using an in-situ method. The resulting composite material, designated HAp/CS-GA, has its physicochemical and structural properties characterized by Fourier transform infrared spectroscopy (FTIR) analysis. The drug-loaded structure was confirmed by UV-visible absorption spectroscopy (UV-Vis) and X-ray diffraction (XRD) analysis. Additionally, field emission scanning electron microscopy (FE-SEM) equipped with the energy dispersive X-ray spectroscopic (EDX) technique was used to determine the surface topography and main components. The composite of HAp/CS-GA was analyzed using a drug release profile and UV-visible spectroscopy (UV-Vis). The fabricated composites antimicrobial behavior was examined against bone infection-causing Gram-positive and Gram-negative bacteria, showing potential activity against Klebsiella pneumoniae, Pseudomonas aeruginosa, and Staphylococcus aureus compared to Escherichia coli, respectively. Simultaneously, the cytotoxicity of the composite was evaluated by MTT assay using an MG-63 osteoblast-like cell line that exhibited no toxicity in the prepared composite. After a 24 h incubation period, the MG-63 cells on the HAp/CS-GA composite showed good proliferation, according to Hoechst 33258 fluorescence staining results. The results suggested that the composite had excellent biocompatibility and antibacterial activity and enhanced the osteoblast cell proliferation. Therefore, the designed HAp/CS-GA composite would be a promising candidate for bone tissue engineering.

2.
Bioorg Med Chem Lett ; 110: 129878, 2024 Sep 15.
Article in English | MEDLINE | ID: mdl-38977107

ABSTRACT

A novel class of pleuromutilin derivatives possessing 1,2,3-triazole as the linker connected to phenyl analogues were designed. The antibacterial properties of the prepared compounds were assessed in vitro against five strains (E. coli, S. aureus, S. epidermidis, and E. faecalis). Most of the tested compounds displayed potent antibacterial activities against gram-positive bacteria and 14-O-[2-(4-((2,4-dinitrophenoxy)-methyl-1H-1,2,3-triazol-1-yl) acetamide)-2-methylpropan-2-yl) thioacetyl]mutilin (7c) exerted antibacterial activities against S. aureus, MRSA and S. epidermidis with MIC values 0.0625 µg/mL, representing 64-fold, 4-fold and 8-fold higher than tiamulin respectively. Compound 6e, 7c and 8c were chosen to carry out killing kinetics, which exhibited concentration-dependent effect. Subsequently, molecular modeling was conducted to further explore the binding of compound 6e, 7a, 7c, 8c and tiamulin with 50S ribosomal subunit from deinococcus radiodurans. The investigation revealed that the main interactions between compound 7c and the ribosomal residues were three hydrogen bonds, π-π, and p-π conjugate effects. Additionally, the free binding energy and docking score of 7c with the ribosome demonstrated the lowest values of -11.90 kcal/mol and -7.97 kcal/mol, respectively, consistent with its superior antibacterial activities.


Subject(s)
Anti-Bacterial Agents , Diterpenes , Microbial Sensitivity Tests , Pleuromutilins , Polycyclic Compounds , Triazoles , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/chemical synthesis , Polycyclic Compounds/chemistry , Polycyclic Compounds/pharmacology , Diterpenes/pharmacology , Diterpenes/chemistry , Diterpenes/chemical synthesis , Triazoles/chemistry , Triazoles/pharmacology , Triazoles/chemical synthesis , Structure-Activity Relationship , Gram-Positive Bacteria/drug effects , Molecular Docking Simulation , Molecular Structure , Escherichia coli/drug effects , Staphylococcus epidermidis/drug effects , Staphylococcus aureus/drug effects , Dose-Response Relationship, Drug , Drug Discovery
3.
World J Microbiol Biotechnol ; 40(9): 281, 2024 Jul 27.
Article in English | MEDLINE | ID: mdl-39060617

ABSTRACT

Antibiotics are essential for combating pathogens; however, their misuse has led to increased resistance, necessitating the search for effective, low-toxicity alternatives. Surfactin, a cyclic lipopeptide with a C12-C17 ß-hydroxy fatty acid chain, exhibits significant antibacterial activity and resists resistance, making it a research focus. Nonetheless, the effects of branched-chain amino acids (BCAAs) on surfactin's structure and activity are not well understood. This study examines the influence of BCAAs (L-valine, L-leucine, and L-isoleucine) on the lipopeptide (surfactin) produced by Bacillus velezensis YA215. Process optimization shows that adding 1 g/L of L-Leu and L-Ile, and 0.5 g/L of L-Val, maximized surfactin production to 18.59%, 19.23%, and 20.64%, respectively. Surfactin content peaked at 36 h with L-Val and L-Ile, yielding 19.72% and 11.37%. In contrast, L-Leu addition peaked at 24 h, yielding 11.33%. Notably, L-Val supplementation resulted in the highest relative surfactin content. Antimicrobial testing demonstrated that BCAAs significantly enhance the antibacterial effects of lipopeptides against Escherichia coli and Staphylococcus aureus, with Val showing the most pronounced effect. The addition of BCAAs notably altered the composition of surfactin fatty acid chains. Specifically, Val increased the proportions of iso C14 and iso C16 ß-hydroxy fatty acids from 13.3% and 4.216-23.803% and 8.31%, respectively. Additionally, the amino acid composition at the 7th position of the peptide chain changed significantly, especially with Val addition, which increased the proportion of C14 [Val 7] surfactin by 3.29 times. These structural changes are likely associated with the enhanced antibacterial activity of surfactin. These findings provide valuable insights into the roles of BCAAs in microbial fermentation, underscoring their importance in metabolic engineering to enhance the production of bioactive compounds.


Subject(s)
Amino Acids, Branched-Chain , Anti-Bacterial Agents , Bacillus , Lipopeptides , Microbial Sensitivity Tests , Lipopeptides/pharmacology , Lipopeptides/chemistry , Bacillus/chemistry , Bacillus/drug effects , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/chemistry , Amino Acids, Branched-Chain/pharmacology , Peptides, Cyclic/pharmacology , Peptides, Cyclic/chemistry , Fermentation
4.
Environ Geochem Health ; 46(9): 334, 2024 Jul 26.
Article in English | MEDLINE | ID: mdl-39060662

ABSTRACT

This study successfully synthesized ZnO-CuO nanocomposite using the hydrothermal method with Carica papaya leaf extract. The incorporation of the leaf extract significantly enhanced the nanocomposite properties, a novel approach in scientific research. Characterization techniques, including X-ray diffraction, Fourier Transmission Infrared spectroscopy, and Scanning Electron Microscopy with Energy Dispersive X-Ray Analysis, confirmed a cubic crystal structure with an average size of 22.37 nm. The Fourier Transmission Infrared spectrum revealed distinctive vibrations at 627, 661, and 751 cm-1 corresponding to ZnO-CuO nanocomposite corresponding to stretching and vibration modes. SEM images confirmed a cubic-like and irregular structure. The nanocomposite exhibited outstanding photocatalytic activity, degrading methylene blue dye by 96.73% within 120 min under visible light. Additionally, they showed significant antimicrobial activity, inhibiting Staphylococcus aureus (20 mm) and Klebsiella pneumonia (17 mm). The results highlight the efficiency of Carica papaya leaf-derived ZnO-CuO nanocomposite for environmental and health challenges.


Subject(s)
Anti-Bacterial Agents , Carica , Copper , Nanocomposites , Plant Extracts , Plant Leaves , Water Purification , Zinc Oxide , Carica/chemistry , Plant Leaves/chemistry , Nanocomposites/chemistry , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/chemistry , Zinc Oxide/chemistry , Zinc Oxide/pharmacology , Copper/chemistry , Plant Extracts/chemistry , Plant Extracts/pharmacology , Water Purification/methods , Staphylococcus aureus/drug effects , Methylene Blue/chemistry , Methylene Blue/pharmacology , Green Chemistry Technology/methods , Klebsiella pneumoniae/drug effects , Microbial Sensitivity Tests , Microscopy, Electron, Scanning , X-Ray Diffraction
5.
Antibiotics (Basel) ; 13(7)2024 Jul 06.
Article in English | MEDLINE | ID: mdl-39061312

ABSTRACT

Inhaled colistin is used to treat pneumonia and respiratory infections through nebulization or dry powder inhalers. Nevertheless, the development of a metered-dose inhaler (MDI) for colistin, which could enhance patient convenience and treatment efficacy, has not yet been developed. Colistin is known for its ability to induce cellular toxicity. Gold nanoparticles (AuNPs) can potentially mitigate colistin toxicity. Therefore, this study aimed to evaluate the antimicrobial effectiveness of colistin conjugated with chitosan-capped gold nanoparticles (Col-CS-AuNPs) and their potential formulation for use with MDIs to deliver the aerosol directly to the deep lung. Fourier-transform infrared spectroscopy, nuclear magnetic resonance, and elemental analysis were used to characterize the synthesized Col-CS-AuNPs. Drug release profiles fitted with the most suitable release kinetic model were evaluated. An MDI formulation containing 100 µg of colistin per puff was prepared. The aerosol properties used to determine the MDI performance included the fine particle fraction, mass median aerodynamic diameter, and geometric standard deviation, which were evaluated using the Andersen Cascade Impactor. The delivered dose uniformity was also determined. The antimicrobial efficacy of the Col-CS-AuNP formulation in the MDI was assessed. The chitosan-capped gold nanoparticles (CS-AuNPs) and Col-CS-AuNPs had particle sizes of 44.34 ± 1.02 and 174.50 ± 4.46 nm, respectively. CS-AuNPs effectively entrapped 76.4% of colistin. Col-CS-AuNPs exhibited an initial burst release of up to 60% colistin within the first 6 h. The release mechanism was accurately described by the Korsmeyer-Peppas model, with an R2 > 0.95. The aerosol properties of the Col-CS-AuNP formulation in the MDI revealed a high fine particle fraction of 61.08%, mass median aerodynamic diameter of 2.34 µm, and geometric standard deviation of 0.21, with a delivered dose uniformity within 75-125% of the labeled claim. The Col-CS-AuNP MDI formulation completely killed Escherichia coli at 5× and 10× minimum inhibitory concentrations after 6 and 12 h of incubation, respectively. The toxicity of CS-AuNP and Col-CS-AuNP MDI formulations in upper and lower respiratory tract cell lines was lower than that of free colistin. The stability of the Col-CS-AuNP MDI formulation was maintained for at least 3 months. The Col-CS-AuNP MDI formulation effectively eradicated bacteria over a 12-h period, showing promise for advancing lung infection treatments.

6.
Antibiotics (Basel) ; 13(7)2024 Jul 12.
Article in English | MEDLINE | ID: mdl-39061324

ABSTRACT

Pseudomonas aeruginosa lung infections in cystic fibrosis (CF) patients represent a therapeutic challenge due to antibiotic resistance. Repurposing existing drugs is a promising approach for identifying new antimicrobials. A crucial factor in successful drug repurposing is using assay conditions that mirror the site of infection. Here, the impact of growth conditions on the anti-P. aeruginosa activity of a library of 3386 compounds was evaluated. To this, after 24 h exposure, the survival rate of CF P. aeruginosa RP73 planktonic cells was assessed spectrophotometrically under "CF-like" (artificial CF sputum, pH 6.8, 5% CO2) and enriched (Tryptone Soya Broth, pH 7.2, and aerobiosis) conditions. Among non-antibiotic compounds (n = 3127), 13.4% were active regardless of growth conditions, although only 3.2% had comparable activity; 4% and 6.2% were more active under CF-like or enriched conditions, respectively. Interestingly, 22.1% and 26.6% were active exclusively under CF-like and enriched conditions, respectively. Notably, 7 and 12 hits caused 100% killing under CF-like and enriched conditions, respectively. Among antibiotics (n = 234), 42.3% were active under both conditions, although only 18.4% showed comparable activity; 9.4% and 14.5% were more active under CF-like and enriched conditions, respectively. Interestingly, 23% and 16.6% were active exclusively under CF-like and enriched conditions, respectively. Sulphonamides showed higher activity under CF-like conditions, whereas tetracyclines, fluoroquinolones, and macrolides were more effective under enriched settings. Our findings indicated that growth conditions significantly affect the anti-P. aeruginosa activity of antibiotics and non-antibiotic drugs. Consequently, repurposing studies and susceptibility tests should be performed under physicochemical conditions that the pathogen tackles at the site of infection.

7.
Antibiotics (Basel) ; 13(7)2024 Jul 14.
Article in English | MEDLINE | ID: mdl-39061332

ABSTRACT

Campylobacter jejuni is a major cause of global foodborne illnesses. To develop alternative antimicrobial strategies against C. jejuni, this study designed and optimized the green synthesis of metallic nanoparticles (NPs) with intracellular components of the medicinal fungus Ganoderma sessile to provide the needed reducing and stabilizing agents. NPs were characterized by transmission electron microscopy and dynamic light scattering, and the quasi-spherical NPs had sizes of 2.9 ± 0.9 nm for the copper oxide NPs and 14.7 ± 0.6 nm for the silver NPs. Surface charge assessment revealed zeta potentials of -21.0 ± 6.5 mV and -24.4 ± 7.9 mV for the copper oxide and silver NPs, respectively. The growth inhibition of C. jejuni by the NPs occurred through attachment to the outer cell membrane and subsequent intracellular internalization and resulted in minimum inhibitory concentrations of the silver NPs at 6 µg/mL and copper oxide NPs at 10 µg/mL. On the other hand, a differential ROS production caused by silver and copper NPs was observed. In summary, this research presents the first demonstration of using green synthesis with the medicinal fungus G. sessile to produce metallic NPs that effectively inhibit C. jejuni growth, providing a sustainable and effective approach to the traditional use of antimicrobials.

8.
Antibiotics (Basel) ; 13(7)2024 Jul 18.
Article in English | MEDLINE | ID: mdl-39061347

ABSTRACT

In this research, several analyses were carried out on concentrated fractions of Mexican oregano essential oil (Poliomintha longiflora Gray) in order to determine its ability to inhibit the growth and the motility of Escherichia coli (swimming), Pseudomonas aeruginosa (swimming), and Proteus vulgaris (swarming); these Gram-negative bacteria associated with urinary tract infections are motile due to the presence of flagella, which is considered an important virulence factor that favors their motility when trying to reach the target organ and cause an infection. Also, the resistance pattern to antibiotics of each strain was determined. The results showed resistance pattern (8 out of 12 antibiotics tested) for P. aureginosa, while E. coli and P. vulgaris were resistant to 4 antibiotics out of the 12 tested. On the other hand, fractionated oregano caused an inhibition of growth and a reduction in motility, varying between fractions and among bacteria. Fraction 4 showed major growth reduction, with MBC values ranging from 0.002 to 23.7 mg/mL. Treatment with fractionated oregano (F1, F2, F3, F4) reduced the motility by 92-81% for P. vulgaris, 90-83% for E. coli, and 100-8.9% for P. aeruginosa. These results demonstrated a higher performance with a lower application dose due to its high content of Carvacrol and Thymol; unlike other concentrated fractions, this synergy of oxygenated monoterpenes may cause greater antimicrobial activity.

9.
Mar Biotechnol (NY) ; 2024 Jul 27.
Article in English | MEDLINE | ID: mdl-39066983

ABSTRACT

Naturally occurring 6-pentyl-2H-pyran-2-one and its synthetic analogues greatly inhibit the settlement of Amphibalanus amphitrite cyprids and the growth and biofilm formation of marine bacteria. To optimize the antifouling activities of pyrone derivatives, this study designed pyrone analogues by modifying functional groups, such as the benzyl group, cyclopentane, and halides, substituted on both sides of a pyrone. The antifouling effects of the synthesized pyrone derivatives were subsequently evaluated against five marine biofilm-forming bacteria, Loktanella hongkongensis, Staphylococcus cohnii, S. saprophyticus, Photobacterium angustum, and Alteromonas macleodii, along with barnacle cyprids of Amphibalanus amphitrite. Substituting nonpolar parts-such as the aliphatic, cyclopentyl, or phenyl moieties on C-5 or the furan moieties on C-3-not only increased antibacterial activity and inhibited biofilm formation but also inhibited barnacle cyprid settlement when compared to 6-pentyl-2H-pyran-2-one.

10.
Fitoterapia ; : 106142, 2024 Jul 25.
Article in English | MEDLINE | ID: mdl-39067487

ABSTRACT

The investigation of the leaves of Pittosporum elevaticostatum Chang et Yan led to the isolation of fifteen pentacyclic triterpenoids (1-15), including five previously undescribed ones (1-5), and nine others (16-24). The structures of compounds 1-5 were elucidated based on comprehensive spectroscopic techniques, including one dimension (1D) and 2D nuclear magnetic resonance (NMR), high resolution electrospray ionization mass spectroscopy (HR-ESI-MS), and other methods. Compounds 2 and 13 demonstrated significant inhibitory activity against Listeria monocytogenes (L. monocytogenes) with minimum inhibitory concentration (MIC) values of 32 µM. Scanning electron microscopy (SEM) observations revealed insights into the antibacterial mechanism, indicating that compounds 2 and 13 either prevent biofilm formation of dispersed the preformed cell membranes. Additionally, compounds 1, 5, 7, and 12 exhibited anti-inflammatory activity on lipopolysaccharide (LPS)-stimulated BV-2 microglial cells with IC50 values ranging from 11.27 to 17.80 µM.

11.
Foods ; 13(14)2024 Jul 13.
Article in English | MEDLINE | ID: mdl-39063295

ABSTRACT

Essential oil (EO) extraction is a widespread practice generating huge amounts of solid plant by-products a potential source of bioactive compounds, on the one hand, and a detrimental risk for the environment that needs to be carefully considered on the other hand. The present study aims to valorize Myrtus communis L. leaf by-products obtained following EO extraction using a steam distillation unit through the recovery of phenolic compounds and the evaluation of their biological activities. The total phenols, flavonoids, and proanthocyanidins contents of the ethanolic extract by-product were higher than the control (leaves without extraction of EO). Their amounts increased from 69.30 to 88.06 mg GAE/g for total phenols, from 36.31 to 70.97 mg QE for flavonoids and from 19.74 to 21.49 mg CE/g of extract for proanthocyanidins. The identification of phenolic compounds by high-performance liquid-chromatography equipped with a reversed-phase (RP-HPLC) system revealed that the by-product sample includes more gallic acid, catechin, syringic acid and luteolin 7-O-glucoside but less p-coumaric acid and kaempferol than the control. Moreover, the mid-infrared spectroscopy (MIR) showed the presence of benzene ring characteristic of phenolic compounds at 756 cm-1, esters of aromatic acids and stretching vibrations of polyphenols at 1141-1234 cm-1, C=C stretching present in phenolic acids such as coumaric acid and catechin at 1604 cm-1. The assessment of antioxidant activity revealed that the ABTS+• radical scavenging activity was significantly increased, whereas the DPPH• radical inhibition activity and the ferric reduction antioxidant power were significantly decreased. The results indicated, as well, that Myrtus communis L. leaf by-products maintained a considerable antibacterial activity depending on the tested bacterial strain. Additionally, the anti-α-amylase activity was higher for the Myrtus communis L. leaf by-product extract. Therefore, Myrtus communis L. leaf by-products of EO extraction offer phenolic compounds with significant biological activities, contributing to the sustainable development and the promotion of circular economy by the recovery of valuable inputs from plant by-products.

12.
Molecules ; 29(14)2024 Jul 17.
Article in English | MEDLINE | ID: mdl-39064944

ABSTRACT

This work describes the synthesis, characterization, and in vitro and in silico evaluation of the biological activity of new functionalized isoxazole derivatives. The structures of all new compounds were analyzed by IR and NMR spectroscopy. The structures of 4c and 4f were further confirmed by single crystal X-ray and their compositions unambiguously determined by mass spectrometry (MS). The antibacterial effect of the isoxazoles was assessed in vitro against Escherichia coli, Bacillus subtilis, and Staphylococcusaureus bacterial strains. Isoxazole 4a showed significant activity against E. coli and B. subtilis compared to the reference antibiotic drugs while 4d and 4f also exhibited some antibacterial effects. The molecular docking results indicate that the synthesized compounds exhibit strong interactions with the target proteins. Specifically, 4a displayed a better affinity for E. coli, S. aureus, and B. subtilis in comparison to the reference drugs. The molecular dynamics simulations performed on 4a strongly support the stability of the ligand-receptor complex when interacting with the active sites of proteins from E. coli, S. aureus, and B. subtilis. Lastly, the results of the Absorption, Distribution, Metabolism, Excretion and Toxicity Analysis (ADME-Tox) reveal that the molecules have promising pharmacokinetic properties, suggesting favorable druglike properties and potential therapeutic agents.


Subject(s)
Anti-Bacterial Agents , Isoxazoles , Molecular Docking Simulation , Molecular Dynamics Simulation , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/chemical synthesis , Isoxazoles/chemistry , Isoxazoles/pharmacology , Bacillus subtilis/drug effects , Microbial Sensitivity Tests , Escherichia coli/drug effects , Molecular Structure , Staphylococcus aureus/drug effects , Structure-Activity Relationship
13.
Microorganisms ; 12(7)2024 Jul 09.
Article in English | MEDLINE | ID: mdl-39065161

ABSTRACT

Copper-containing materials are attracting attention as self-disinfecting surfaces, suitable for helping healthcare settings in reducing healthcare-associated infections. However, the impact of repeated exposure to disinfectants frequently used in biocleaning protocols on their antibacterial activity remains insufficiently characterized. This study aimed at evaluating the antibacterial efficiency of copper (positive control), a brass alloy (AB+®) and stainless steel (negative control) after repeated exposure to a quaternary ammonium compound and/or a mix of peracetic acid/hydrogen peroxide routinely used in healthcare settings. A panel of six antibiotic-resistant strains (clinical isolates) was selected for this assessment. After a short (5 min) exposure time, the copper and brass materials retained significantly better antibacterial efficiencies than stainless steel, regardless of the bacterial strain or disinfectant treatment considered. Moreover, post treatment with both disinfectant products, copper-containing materials still reached similar levels of antibacterial efficiency to those obtained before treatment. Antibiotic resistance mechanisms such as efflux pump overexpression did not impair the antibacterial efficiency of copper-containing materials, nor did the presence of one or several genes related to copper homeostasis/resistance. In light of these results, surfaces made out of copper and brass remain interesting tools in the fight against the dissemination of antibiotic-resistant strains that might cause healthcare-associated infections.

14.
Polymers (Basel) ; 16(14)2024 Jul 12.
Article in English | MEDLINE | ID: mdl-39065314

ABSTRACT

In this study, we successfully realized the hydrolytic ring-opening co-polymerization of ε-caprolactam (CPL) and lysine derivative. A novel antibacterial modified polyamide 6 with a branched structure was obtained after the quaternization of the co-polymers. The co-polymers exhibited a significant increase in zero shear viscosity, melt index and storage modulus at the low frequency region. The quaternized co-polymers displayed thermal properties different from pure PA6 and good mechanical (tensile) properties. The antibacterial activity of the quaternized co-polymers depends on the quaternary ammonium groups' incorporated content. At 6.2 mol% incorporation of quaternary ammonium groups, the strong antibacterial activity has been introduced to the co-polymers. As the quaternary ammonium groups approached 10.1 mol%, the antibacterial polymers demonstrated nearly complete killing of Staphylococcus aureus (Gram positive) and Escherichia coli (Gram negative). The above research results provided a new approach for the study of high-performance nylon.

15.
Pharmaceutics ; 16(7)2024 Jul 05.
Article in English | MEDLINE | ID: mdl-39065598

ABSTRACT

Enrofloxacin (ENR), a member of the fluoroquinolone class of antibiotics, is widely used in veterinary medicine to treat bacterial infections. Like many antibiotics, ENR has limited water solubility and low bioavailability. To address these challenges, drug formulations using solid dispersions, nanosuspensions, surfactants, cocrystal/salt formation, and inclusion complexes with cyclodextrins may be employed. The approach described herein proposes the development of ENR formulations by co-electrospinning ENR with custom-prepared cyclodextrin-oligolactide (CDLA) derivatives. This method benefits from the high solubility of these derivatives, enabling polymer-free electrospinning. The electrospinning parameters were optimized to incorporate significant amounts of ENR into the CDLA nanofibrous webs, reaching up to 15.6% by weight. The obtained formulations were characterized by FTIR and NMR spectroscopy methods and evaluated for their antibacterial activity against Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa. This study indicates that the presence of CDLA derivative does not inhibit the antibacterial activity of ENR, recommending these formulations for further development.

16.
Pharmaceutics ; 16(7)2024 Jul 07.
Article in English | MEDLINE | ID: mdl-39065606

ABSTRACT

In the current study, a smart release system responsive to temperature was developed to improve the efficiency of tetracycline (TC) in antibacterial therapy. The nanovesicles designed consist of a non-ionic surfactant, SPAN60, cholesterol and a phase change material (PCM) as a thermoresponsive gating material. Niosomes were prepared using an increasing amount of PCM and characterized in terms of size, zeta potential, colloidal stability and thermoresponsive properties. The vesicles that developed were homogenous in size, had good biocompatibility and stability for up to 3 months and demonstrated thermoresponsive behavior. A low drug leakage was observed at 37 °C, while a rapid release occurred at 42 °C, due to the faster diffusion rate of the drug trough the melted PCM. This controllable drug release capacity allows us to avoid premature drug release, minimizing unwanted and toxic effects and ensuring a long retention time in the nanodevice so that it reaches the infected sites. In addition, TC-loaded niosomes were screened to investigate their antibacterial activity against various Gram-positive and Gram-negative bacteria by minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) assays. An interesting temperature-dependent antibacterial activity was observed against some bacterial strains: the niosomes activity against S. epidermis, for example, was improved by the temperature increase, as suggested by a reduction in MIC values from 112.81 to 14.10 µM observed at 37 and 42 °C, respectively. Taken together, the thermoresponsive platform developed allows us to use lower antibiotic amounts while ensuring therapeutic efficacy and, so, will advance the development of a novel antibacterial agent in clinical practice.

17.
J Funct Biomater ; 15(7)2024 Jul 05.
Article in English | MEDLINE | ID: mdl-39057308

ABSTRACT

Calcium silicate (CaSi) bone cement with antibacterial and osteogenic properties has attracted significant interest. However, there is a need to develop a variety of new premixed bone cement to meet the clinical requirements of fast setting time, ease of handling, and efficient antibacterial properties. In this study, different volume ratios of polyethylene glycol (PEG) and lactic acid liquids were added to calcium silicate, and the effects of varying liquid-to-powder ratios (L/P) were examined. This study assessed the physicochemical properties, cytotoxicity, and antibacterial activity against S. aureus and E. coli of this premixed cement. The results from the experiments indicated that lactic acid significantly reduced the setting time of the CaSi-based cement and enhanced its mechanical strength. Furthermore, the appropriate concentration of lactic acid and matching L/P ratio improved its washout resistance. The cell viability of all premixed cement was found to be over 80%. The premixed cement containing PEG and lactic acid exhibited superior antibacterial properties compared to the CaSi control. Based on its setting time, washout resistance, and antibacterial activity, a premixed cement with a liquid phase of 80% PEG and 20% lactic acid at an L/P ratio of 0.4 appeared promising for use in dental and orthopedic practice.

18.
J Funct Biomater ; 15(7)2024 Jul 17.
Article in English | MEDLINE | ID: mdl-39057316

ABSTRACT

Nosocomial infections, a prevalent issue in intensive care units due to antibiotic overuse, could potentially be addressed by metal oxide nanoparticles (NPs). However, there is still no comprehensive understanding of the impact of NPs' size on their antibacterial efficacy. Therefore, this study provides a novel investigation into the impact of ZnO NPs' size on bacterial growth kinetics. NPs were synthesized using a sol-gel process with monoethanolamine (MEA) and water. X-ray diffraction (XRD), transmission electron microscopy (TEM), and Raman spectroscopy confirmed their crystallization and size variations. ZnO NPs of 22, 35, and 66 nm were tested against the most common nosocomial bacteria: Escherichia coli, Pseudomonas aeruginosa (Gram-negative), and Staphylococcus aureus (Gram-positive). Evaluation of minimum inhibitory and bactericidal concentrations (MIC and MBC) revealed superior antibacterial activity in small NPs. Bacterial growth kinetics were monitored using optical absorbance, showing a reduced specific growth rate, a prolonged latency period, and an increased inhibition percentage with small NPs, indicating a slowdown in bacterial growth. Pseudomonas aeruginosa showed the lowest sensitivity to ZnO NPs, attributed to its resistance to environmental stress. Moreover, the antibacterial efficacy of paint containing 1 wt% of 22 nm ZnO NPs was evaluated, and showed activity against E. coli and S. aureus.

19.
J Fungi (Basel) ; 10(7)2024 Jul 10.
Article in English | MEDLINE | ID: mdl-39057359

ABSTRACT

Seagrass serves as a quintessential reservoir for obligate marine Lulworthiaceae fungi. Our current knowledge of the mycological diversity associated with seagrass in Hong Kong remains poor. We analyzed the diversity of fungi associated with the most widely distributed seagrass species in Hong Kong Halophila ovalis (Hydrocharitaceae), using a combination of culture-based methods and high-throughput amplicon sequencing. Halophilomyces hongkongensis, a novel fungal species in a newly proposed genus within the Lulworthiaceae family, was isolated from H. ovalis roots and rhizomes. The novel fungus showed distinct morphological characteristics, while both combined 18S-28S and internal transcribed spacer (ITS) phylogenetic trees based on maximum likelihood and Bayesian methods supported its discrimination from other existing Lulworthiaceae members. The ITS2 region in the Illumina sequencing results of multiple H. ovalis compartments, water, and adjacent non-seagrass sediments revealed continuous recruitment of H. hongkongensis by H. ovalis throughout the year despite dramatically fluctuating environmental conditions, with remarkably high proportions of this taxon found in root and rhizome internal tissues, possibly indicating a strong and specialized relationship established between the Lulworthiaceae fungal partner and its seagrass host. The inhibitory abilities exhibited by H. hongkongensis against Staphylococcus aureus SA29213 and ATCC 43300 (methicillin-resistant) may imply its capacity in producing (novel) antibacterial compounds. The discovery of H. hongkongensis as the first novel Lulworthiaceae taxon in Hong Kong, along with its distributional pattern in the seagrass meadow, provides valuable insights into the systematics and ecology of this strictly marine fungal family.

20.
Mar Drugs ; 22(7)2024 Jun 26.
Article in English | MEDLINE | ID: mdl-39057401

ABSTRACT

Four tunicamycin class compounds, tunicamycin VII (1), tunicamycin VIII (2), corynetoxin U17a (3), and tunicamycin IX (4), were isolated from the culture broth of the marine-derived actinomycete Streptomyces sp. MBTG32. The strain was identified using the 16S rDNA sequencing technique, and the isolated strain was closely related to Streptomyces bacillaris. The structures of the isolated compounds were elucidated based on spectroscopic data and comparisons with previously reported NMR data. Compounds 1-4 showed potent antibacterial activities against Gram-positive bacteria, especially Staphylococcus aureus, with MIC values of 0.13-0.25 µg/mL. Through a recombinant enzyme assay and overexpression analysis, we found that the isolated compounds exerted potent inhibitory effects on S. aureus MurNAc-pentapeptide translocase (MraY), with IC50 values of 0.08-0.21 µg/mL. The present results support that the underlying mechanism of action of tunicamycins isolated from marine-derived Streptomyces sp. is also associated with the inhibition of MraY enzyme activity in S. aureus.


Subject(s)
Anti-Bacterial Agents , Bacterial Proteins , Microbial Sensitivity Tests , Staphylococcus aureus , Streptomyces , Tunicamycin , Staphylococcus aureus/drug effects , Tunicamycin/pharmacology , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/isolation & purification , Anti-Bacterial Agents/chemistry , Bacterial Proteins/metabolism , Transferases (Other Substituted Phosphate Groups) , Transferases/antagonists & inhibitors , Transferases/metabolism , Aquatic Organisms
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