The purposeful development of synthetic antibacterial compounds requires an understanding of the relationship between effects of compounds and their chemical structure. This knowledge can be obtained by studying changes in bacteria ultrastructure under the action of antibacterial compounds of a certain chemical structure. Our study was aimed at examination of ultrastructural changes in S. aureus cells caused by polycationic amphiphile based on 1,4‒diazabicyclo[2.2.2]octane (DL₄12), ciprofloxacin and their hybrid (DL₅Cip6); the samples were incubated for 15 and 45 min. DL₄12 first directly interacted with bacterial cell wall, damaging it, then penetrated into the cell and disrupted cytoplasm. Ciprofloxacin penetrated into cell without visually damaging the cell wall, but altered the cell membrane and cytoplasm, and inhibited the division of bacteria. The ultrastructural characteristics of S. aureus cells damaged by the hybrid clearly differed from those under ciprofloxacin or DL₄12 action. Signs associated with ciprofloxacin predominated in cell damage patterns from the hybrid. We studied the effect of ciprofloxacin, DL₄12 and their hybrid on S. aureus biofilm morphology using paraffin sections. Clear differences in compound effects on S. aureus biofilm (45 min incubation) were observed. The results obtained allow us to recommend this simple and cheap approach for the initial assessment of antibiofilm properties of synthesized compounds.

Magnetic iron oxide (II,III) nanoparticles (MNPs) are highly interested in biomedicine. However, their application is limited by oxidation, aggregation, rapid clearance from the body, and poor biodistribution. Coating by human serum albumin (HSA), the predominant blood plasma protein, can significantly influence properties, prolong circulation half-life, and enhance tumor capture efficiency. Here, we report the synthesis of oleic acid and Tween20-coated MNPs and their interaction with HSA. The influence of albumin coating on MNP size, zeta potential, aggregation ability, and toxicity was studied. The particles were characterized by dynamic light scattering, transmission electron microscopy, and Fourier transform infrared spectroscopy methods. The nanoparticles’ relaxivities (r₁ and r₂) were assessed under a magnetic field of 1.88 T to evaluate their performance in MRI applications. The anticancer drug doxorubicin (DOX) loading capacity of up to 725 µg/mg for albumin-coated MNPs was determined. DOX-loaded MNPs displayed pH-sensitive drug release during acidic conditions. The series of DOX-loaded nanocomposites indicated inhibition of A549 cell lines, and the IC₅₀ values were evaluated. This research underscores the utility of HSA-coated MNPs in enhancing the efficacy and stability of drug delivery systems in biomedicine.

Ultrastructure changes in S. aureus and E. faecalis bacteria incubated with synthetic cationic amphiphile DL₄12 and its hybrids with the natural monoterpene carvacrol were studied. The hybrid compounds DL₄CAR-6, DL₅CAR-6, DLpCAR-6, and DLoCAR-6 contained two carvacrol molecules and differed in central linker structure. The study was conducted on ultrathin sections of bacteria fixed by the Ryter–Kellenberger method and on a Jem 1400 transmission electron microscope (Jeol, Tokyo, Japan). Ultrastructure changes in S. aureus and E. faecalis incubated with compound DL₄12 were species-specific. Destructive changes in S. aureus cells when exposed to DL₄12 compound and all DL₄12-carvacrol hybrids did not differ. DL₄12 and DL₄12-carvacrol hybrids in E. faecalis cells damaged all structures except the cell wall. Compound DL₄12 and its hybrids disrupted the ultrastructure of nucleoid and DNA strands in both bacterial species. Complete disorganization of ribosomes in cells of both bacteria occurred upon incubation with compound DL₄12 and its carvacrol-bearing analog DL₄CAR-6. Inclusions in bacterial cells exposed to all compounds had the same ultrastructure. The study showed that all compounds used possess multitarget properties; the structure of the central linker of hybrid compounds plays a significant role in the nature of their damaging effect on S. aureus and E. faecalis cells.