Strong Antimicrobial Activity of Highly Stable Nanocomposite Containing AgNPs Based on Water-Soluble Triazole-Sulfonate Copolymer

A new hydrophilic polymeric nanocomposite containing AgNPs was synthesized by chemical reduction of metal ions in an aqueous medium in the presence of the copolymer. A new water-soluble copolymer of 1-vinyl-1,2,4-triazole and vinylsulfonic acid sodium salt (poly(VT-co-Na-VSA)) was obtained by free-radical copolymerization and was used as a stabilizing precursor agent. The structural, dimensional, and morphological properties of the nanocomposite were studied by UV–Vis, FTIR, X-ray diffraction, atomic absorption, transmission and scanning electron microscopy, dynamic and electrophoretic light scattering, gel permeation chromatography, thermogravimetric analysis, and differential scanning calorimetry. Hydrodynamic diameter of macroclubs for the copolymer was 171 nm, and for the nanocomposite it was 694 nm. Zeta potential for the copolymer was −63.8 mV, and for the nanocomposite it was −70.4 mV. The nanocomposite had strong antimicrobial activity towards Gram-negative and Gram-positive microorganisms: MIC and MBC values were in the range of 0.25–4.0 and 0.5–8.0 μg/mL, respectively.

ISOLATION AND IDENTIFICATION OF LACTIC ACID BACTERIA (LAB) PRODUCING BACTERIOSIN-LIKE FROM SMOKED GIANT CATFISH (Arius thalassinus)

Bacteriocin was bacterial metabolite that have antimicrobial properties, so it had the potential to be used as food bio preservatives. Bacteriocin was produced by lactic acid bacteria (LAB), one of the sources of which was from smoked fish products. Some regions in Indonesia produce various types of smoked fish from various types of fish, which were thought to contain bacteriocin-producing lactic acid; one of them was giant cathfish (Arius thalassinus). This study aims to obtain LAB isolates that have strong antimicrobial activity and have the potential to produce bacteriocin-like from smoked giant catfish (Arius thalassinus). The research method used an experimental method that analyzed descriptively. Based on the results, there were 15 isolates LAB isolated from smoked giant catfish. Three selected isolates showed strong antimicrobial activity inhibiting E. coli and S. aureus bacteria, and the most effective inhibiting Salmonella sp. One selected LAB isolates identified Pediococcus acidilactici suspected to produce pediocin bacteriocin-like, while the other two isolates identified Lactobacillus plantarum sp 1 and Lactobacillus plantarum sp 2 which suspected to produce plantaricin bacteriocin. Bacteriocin from the three isolates of LAB had characteristics stable to temperatures up to 121oC, stable in pH range 2-6, and bacteriocin activity increased with the addition of SDS (Sodium Dodecyl Sulfate) and EDTA (Ethylenediaminetetraacetic acid) surfactants. The conclusion was that the bacteriocin produced was stable at high temperature, low pH, and resistence in the presence of surfactants, so it had the potential to be developed as biopreservatives material in preserving fish-based foods

Targeting bacteria causing otitis media using nanosystems containing nonspherical gold nanoparticles and ceragenins

Aim: To evaluate the antibacterial and antibiofilm activity of ceragenin-conjugated nonspherical gold nanoparticles against the most common agents of otitis media. Methods: Minimal inhibitory and bactericidal concentrations and colony-counting assays, as well as colorimetric and fluorimetric methods, were used to estimate the antibacterial activity of compounds in phosphate-buffered saline and human cerumen. The nanosystems’ biocompatibility and ability to decrease IL-8 release was tested using keratinocyte cells. Results: The tested compounds demonstrated strong antimicrobial activity against planktonic and biofilm cultures at nontoxic doses due to the induction of oxidative stress followed by the damage of bacterial membranes. Conclusions: This study indicates that ceragenin-conjugated nonspherical gold nanoparticles have potential as new treatment methods for eradicating biofilm-forming pathogens associated with otitis media.

Chemical Composition of Essential Oils of Aromatic and Medicinal Herbs Cultivated in Greece—Benefits and Drawbacks

The current study investigated and determined the major compounds of six essential oils derived from different plant species cultivated in Greece (Lavandula angustifolia, Origanum vulgare, Pistacia lentiscus var. chia, Citrus reticulata, Citrus limon and Crithmum maritimum). The results proved that all these essential oils have a high potential for use as food preservatives, since among the compounds determined were sabinene, b-myrcene, a-pinene, carvacrol and limonene, all of which were responsible for the strong antimicrobial activity against Staphylococcus aureus. However, the amounts of some compounds, such as linalool and citral, were at high levels, and this can be a danger for some sensitive population groups due to allergic reactions. The essential oil compounds which were identified using GC-MS and quantified through GC-FID represented more than 95% of the total essential oils of the investigated plant species. Finally, all essential oils provided high phenolic content.

Repurposing Candesartan Cilexetil as Antibacterial Agent for MRSA Infection

Staphylococcus aureus is an important pathogen causing hospital-acquired infections. Methicillin-resistant S. aureus (MRSA), biofilms, and persisters are highly tolerant to traditional antibiotics and make it difficult to treat. Therefore, new antimicrobial agents are urgently needed to treat hard-to-eradicate diseases caused by this bacterium. In this study, candesartan cilexetil (CC), an angiotensin hypertension drug, had strong antimicrobial activity against S. aureus with minimal inhibitory concentrations (MICs) and minimal bactericidal concentrations (MBCs) of 8–16 μg/ml and 16–32 μg/ml. CC exhibited limited cytotoxicity and low potential to induce drug resistance. In addition, it showed a synergistic antibacterial effect when combined with gentamicin and tobramycin. The effective concentrations to inhibit MRSA biofilm formation were 16–64 μg/ml, and intractable persisters were killed at 4–8 × MIC. Through the analysis of its mechanism of action, it was evident that the membrane permeability was disrupted as well as the cell structure was damaged. Furthermore, we demonstrated that CC had antibacterial effects in vivo in MRSA-infected murine skin abscess models. In conclusion, these results imply that CC might be a potential antibacterial agent for the treatment of S. aureus-associated infections.

Alkaloid profiling and antimicrobial activities of Papaver glaucum and P. decaisnei

Objective Papaver decaisnei Hochst. & Steud. Ex Elkan and Papaver glaucum Boiss. & Hausskn. growing wild in Northern Iraq have been historically used for medicinal purposes. In this study, both species were evaluated for their alkaloid content and antimicrobial activities. Results Alkaloids were extracted and isolated by preparative thin-layer chromatography (TLC). Identification was carried out by comparing spectral data (UV and 1H-NMR) and TLC Rf values with those of authentic samples. Two alkaloids, proapaorphine-type mecambrine and aporphine-type roemerine were isolated from P. decaisnei. Two benzylisoquinoline type alkaloids papaverine (major alkaloid) and palaudine as well as aporphine-type N-methylasimilobine have been obtained in P. glaucum. Both P. glaucum and P. decaisnei extracts revealed strong antimicrobial activity on Pseudomonas aeruginosa ATCC 27853 and Enterococcus faecalis ATCC 29212. Collectively these results indicate that P. glaucum and P. decaisnei are promising sources of alkaloids that could further be investigated for medicinal purposes.

Characterization of the Psychrotrophic Lactic Acid Bacterium Leuconostoc gelidum subsp. aenigmaticum LS4 Isolated from Kimchi Based on Comparative Analyses of Its Genomic and Phenotypic Properties

With the aim of developing a new food starter culture, twenty-three psychrotrophic lactic acid bacteria (LAB) were isolated from 16 kimchi samples. One strain, Leuconostoc gelidum subsp. aenigmaticum LS4, which had typical psychrotrophic characteristics, was selected, and its phenotypic and genomic properties as a starter culture were investigated. The complete genome of L. aenigmaticum LS4 consisted of one circular chromosome (1,988,425 bp) and two plasmids (19,308 bp and 11,283 bp), with a guanine–cytosine content of 36.8%. L. aenigmaticum LS4 could grow at 5 °C but not at 37 °C, and maximum cell growth was obtained at 15~25 °C. L. aenigmaticum LS4 did not show any harmful characteristics such as hemolysis, undesirable enzyme activities, biogenic amine production, or antibiotic resistance. L. aenigmaticum LS4 was investigated for its suitability for technological processes (pH, temperature and NaCl treatment). L. aenigmaticum LS4 exhibited strong antimicrobial activity caused by the production of organic acids and bacteriocin, and it produced an exopolysaccharide composed of glucose with a molecular weight of 3.7 × 106 Da. Furthermore, L. aenigmaticum LS4 improved the organoleptic qualities of kimchi juice. Our results indicate that L. aenigmaticum LS4 could be used as a functional starter culture for food (vegetable or fruit) fermentation at low temperatures.

Design and heterologous expression of a novel dimeric LL37 variant in Pichia pastoris

Background The antimicrobial peptide LL37 is produced by white blood cells (mainly neutrophils) and various epithelial cells, and has the outstanding advantages of participating in immune regulation, causing chemotaxis of immune cells and promoting wound healing. However, the central domain of LL37 needs to be improved in terms of antimicrobial activity. Results In this study, the amino acid substitution method was used to improve the antimicrobial activity of the LL37 active center, and a dimeric design with a better selection index was selected. A flexible linker was selected and combined with the 6 × His-SUMO tag and LG was successfully expressed using Pichia pastoris as a host. Recombinant LG displayed strong antimicrobial activity by destroying the cell membrane of bacteria but had low hemolytic activity. In addition, compared with monomeric peptide FR, rLG had improved ability to tolerate salt ions. Conclusion This research provides new ideas for the production of modified AMPs in microbial systems and their application in industrial production.

Synthesis and Evaluation of Chiral Rhodanine Derivatives Bearing Quinoxalinyl Imidazole Moiety as ALK5 Inhibitors

Background: TGF-β signaling pathway inhibition is considered an effective way to prevent the development of several diseases. In the design and synthesis of TGF-β inhibitors, a rhodanine compound containing a quinoxalinyl imidazole moiety was found to have strong antimicrobial activity. Objective: The purpose of this work was to investigate the antimicrobial activity of other chiral rhodanine TGF-β inhibitors synthesized. Methods: Two series of 3-substituted-5-((5-(6-methylpyridin-2-yl)-4-(quinoxalinyl-6-yl)- 1H-imidazol-2-yl)methylene)-2-thioxothiazolin-4-ones (12a–h and 13a–e) were synthesized and evaluated for their ALK5 inhibitory and antimicrobial activity. The structures were confirmed by their 1H NMR, 13C NMR, and HRMS spectra. All the synthesized compounds were screened against Gram-positive strains, Gram-negative strains, and fungi. Results: Among the synthesized compounds, compound 12h showed the highest activity (IC50 = 0.416 μM) against ALK5 kinase. Compound 12h exhibited a good selectivity index of > 24 against p38α MAP kinase and was 6.0-fold more selective than the clinical candidate, compound 2 (LY-2157299). Nearly all the compounds displayed high selectivity toward both Gram-positive and Gram-negative bacteria. They also showed similar or 2.0-fold greater antifungal activity (minimum inhibitory concentration [MIC] = 0.5 µg/mL) compared with the positive control compounds Gatifloxacin (MIC = 0.5 µg/mL) and fluconazole (MIC = 1 µg/mL). Conclusion: The findings suggest that the synthesized rhodanine compounds have good ALK5 inhibitory activity and can be used for further research and development as potential antifungal drugs.