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Antimicrobial peptides (AMPs) represent a class of molecules synthesized by different organisms as an ancient innate defense mechanism against different pathogens like bacteria, fungi, viruses. Their characteristics make them good candidates to fight against bacteria together with or as an alternative to antibiotics. To decide on AMPs suitability for use in mammalian systems we redefined a 'therapeutic index' using the concentrations for which AMP is active against pathogens without inducing cytotoxic damage to the mammalian cells. Here we analyzed the toxic effects of eleven, highly active cationic AMPs towards human cells. The AMPs cytotoxicity was determined using common standardized assays measuring their effect on red blood cells (hemolytic index) and on lymphocytes (cell viability). The therapeutic index was calculated for all the AMPs tested. The highest therapeutic index was found for cecropins followed by magainins and the smallest for Melittin. For two peptides, Cecropin A which presents the highest therapeutic index and Melittin with the smallest therapeutic index we characterized in detail the cell death process distinguishing between apoptosis and necrosis. The toxic effects produced by Cecropin A and Melittin are induced mostly by means of apoptosis suggesting that the definition of therapeutic index has to consider the apoptotic effects of AMPs. Thus we provided here a unitary way to characterize the side effects of AMPs. The analysis of in vitro cytotoxic effects of AMPs using the global concept of therapeutic index can be a powerful way to decide which peptide can be taken for further testing in preclinical trials.

Here we describe a new BODIPY-based membrane probe (1) that provides an alternative to dialkylcarbocyanine dyes, such as DiI-C18, that can be excited in the blue spectral region. Compound 1 has unbranched octadecyl chains at the 3,5-positions and a meso-amino function. In organic solvents, the absorption and emission maxima of 1 are determined mainly by solvent acidity and dipolarity. The fluorescence quantum yield is high and reaches 0.93 in 2-propanol. The fluorescence decays are well fitted with a single-exponential in pure solvents and in small and giant unilamellar vesicles (GUV) with a lifetime of ca. 4 ns. Probe 1 partitions in the same lipid phase as DiI-C18(5) for lipid mixtures containing sphingomyelin and for binary mixtures of dipalmitoylphosphatidylcholine (DPPC) and dioleoylphosphatidylcholine (DOPC). The lipid phase has no effect on the fluorescence lifetime but influences the fluorescence anisotropy. The translational diffusion coefficients of 1 in GUVs and OLN-93 cells are of the same order as those reported for DiI-C18. The directions of the absorption and emission transition dipole moments of 1 are calculated to be parallel. This is reflected in the high steady-state fluorescence anisotropy of 1 in high ordered lipid phases. Molecular dynamic simulations of 1 in a model of the DOPC bilayer indicate that the average angle of the transition moments with respect to membrane normal is ca. 70°, which is comparable with the value reported for DiI-C18.

Complexes with mixed ligands [Cu(N-N)2(pmtp)](ClO4)2 ((1) N-N: 2,2′-bipyridine; (2) L: 1,10-phenanthroline and pmpt: 5-phenyl-7-methyl-1,2,4-triazolo[1,5-a]pyrimidine) were synthesized and structurally and biologically characterized. Compound (1) crystallizes into space group Pa and (2) in P-1. Both complexes display an intermediate stereochemistry between the two five-coordinated ones. The biological tests indicated that the two compounds exhibited superoxide scavenging capacity, intercalative DNA properties, and metallonuclease activity. Tests on various cell systems indicated that the two complexes neither interfere with the proliferation of Saccharomyces cerevisiae or BJ healthy skin cells, nor cause hemolysis in the active concentration range. Nevertheless, the compounds showed antibacterial potential, with complex (2) being significantly more active than complex (1) against all tested bacterial strains, both in planktonic and biofilm growth state. Both complexes exhibited a very good activity against B16 melanoma cells, with a higher specificity being displayed by compound (1). Taken together, the results indicate that complexes (1) and (2) have specific biological relevance, with potential for the development of antitumor or antimicrobial drugs.

Due to the fact of their ability to bond with human’s hard tissue, bioglasses have gained interest in the biomedical field with certain purposes regarding their usage in the replacement, healing or repair of bones. In the form of thin films, they trigger an increase in biocompatibility for the inert supports after implantation, based on surface engineering to ensure osteoinduction. For that, this research is focused on obtaining coatings based on cerium-enriched bioglass to generate bioactive and potential additional antimicrobial and antioxidant properties. The addressed oxide system was a novel and complex one, 46.10 SiO2–2.60 P2O5–16.90 CaO–10.00 MgO–19.40 Na2O–5.00 CeO2 (mol%), while two different synthesis methods, laser ablation and spin coating, were tackled comparatively. In the case of the first technique, substrate temperature was selected as variable parameter (room temperature or 300 °C). After conducting a complex characterization, films’ deposition was validated, their bioactive behaviour was proven by the formation of calcium phosphate after immersion in simulated body fluid for four weeks, while the impact exerted on the tested human fibroblast BJ cells (ATCC, CRL-2522) confirmed the applicative potential.

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