A novel series of coumarin–thiadiazole hybrids, derived from substituted coumarin-3-carboxylic acids was isolated and fully characterized with the use of a number of spectroscopic techniques and XRD crystallography. Several of the novel compounds showed intensive fluorescence in the visible region, comparable to that of known coumarin-based fluorescence standards. Moreover, the new compounds were tested as potential antineurodegenerative agents via their ability to act as acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitors. Compared to the commercial standards, only a few compounds demonstrated moderate AChE and BuChE activities. Moreover, the novel derivatives were tested for their antimicrobial activity against a panel of pathogenic bacterial and fungal species. Their lack of activity and toxicity across a broad range of biochemical assays, together with the exceptional emission of some hybrid molecules, highlights the possible use of a number of the novel hybrids as potential fluorescence standards or fluorescence imaging agents.
A series of coumarin-thiadiazole hybrids and their corresponding Cu(II) and Zn(II) complexes were synthesized and characterized with the use of spectroscopic techniques. The results obtained indicate that all the coumarin-thiadiazole hybrids act as bidentate chelators of Cu(II) and Zn(II) ions. The complexes isolated differ in their ligand:metal ratio depending on the central metal. In most cases, the Zn(II) complexes are characteristic of a 1:1 ligand:metal ratio, while in the Cu(II) complexes the ligand:metal ratio is 2:1. All compounds were tested as potential antibacterial agents against Gram-positive (Staphylococcus aureus, Staphylococcus epidermidis) and Gram-negative (Escherichia coli, Pseudomonas aeruginosa) bacterial strains demonstrating activities notably lower than commercially available antibiotics. The more promising results were obtained from the assessment of antineurodegenerative potency as all compounds showed moderate acetylcholinesterase (AChE) inhibition activity
The treatment of proctological conditions, including hemorrhoids, anal fissures, and perianal abscesses, is often complicated by bacterial infections, particularly those involving multidrug-resistant Escherichia coli. This study presents the synthesis, characterization, and biological evaluation of the newly designed synthetic peptide AMPEC4, inspired by cytotoxin 5 from Naja ashei snake venom. AMPEC4 demonstrated potent antimicrobial properties with MIC values of 100 and 200 µg/mL, effectively inhibiting biofilm formation (up to 84%) and eradicating the pre-formed biofilm by up to 35%. The antibacterial activity of AMPEC4 was further supported by a membrane permeabilization assay, demonstrating its capacity to disrupt bacterial membrane integrity in a dose-dependent manner. Furthermore, AMPEC4 significantly promoted fibroblast migration, a critical step in tissue regeneration, while exhibiting notable biocompatibility, as evidenced by the absence of hemolytic, cytotoxic, and genotoxic effects. By addressing both infection control and tissue regeneration, AMPEC4 represents a promising therapeutic strategy for managing chronic wounds, particularly in the challenging environment of the anorectal region. Its ability to target Escherichia coli reference and clinical strains while accelerating the wound-healing process underscores its potential for future clinical applications.
4 February 2025 in Journal of Inorganic Biochemistry
Flavonoids are natural antibacterial agents, and their bioavailability can be improved by metal complexation. This study examines 3-hydroxyflavone complexes with Co(II), Mn(II), and Zn(II) against Staphylococcus aureus and Escherichia coli. Antibacterial activity and membrane permeability were tested in vitro, while Langmuir monolayers modeled physicochemical interactions with bacterial membranes and their major lipid components. The results demonstrated that, particularly at the highest tested molar ratio, the metal complexes of 3HF exhibited greater antibacterial efficacy than the 3HF independently. Escherichia coli demonstrated greater sensitivity to the tested compounds, than S. aureus. The tested 3HF—complexes were identified as bacteriostatic. In E. coli, both physicochemical and microbiological changes were observed following treatment with Co(II)-3HF and Zn(II)-3HF complexes. In contrast, the Mn(II)-3HF complex affected only model membrane properties without notable microbiological effects. For S. aureus, only the zinc(II) complex showed effective microbiological action on the native cell and activity on the inner membrane (in the model studies), with efficacy ranked as follows: Mn(II)-3HF ≥ Co(II-3HF) > Zn(II)-3HF. Increased permeability of E. coli and S. aureus membranes (in vitro assays) has been proposed as a mechanism for the antibacterial action of the Co(II)-3HF and Zn(II)-3HF complexes.
1 June 2022 in Acta Universitatis Cibiniensis. Series E: Food Technology
The leaves and unripe fruits from 5 walnut clones were tested in terms of mineral composition, antioxidant activity, and the inhibitory effect on model urease. It has been shown that the leaves are richer in minerals and also have higher antioxidant potential than unripe fruits. HPTLC polyphenolic profiles of leaves extract were found more abundant in flavonoids regardless of the sample origin. Only green walnut extracts showed an effect as urease inhibitors. Higher antibacterial activity was observed against Staphylococcus aureus in comparison with Staphylococcus epidermidis . Both leaf and fruit extracts showed antibiofilm activity, up to 95% of biofilm inhibition. It was shown that all tested Juglans regia extracts can serve as a valuable antibacterial agent against staphylococci infections.