Antibacterial, antifungal, and anti-biofilm effects of sulfamethoxazole-complexes against pulmonary infection agents.

Antibiotic resistance associated with pulmonary infection agents has become a public health problem, being considered one of the main priorities for immediate resolution. Thus, to increase the therapeutic options in the fight against resistant microorganisms, the synthesis of molecules from pre-existing drugs has shown to be a promising alternative. In this sense, the present work reports the synthesis, characterization, and biological evaluation (against fungal and bacterial agents that cause lung infections) of potential metallodrugs based on sulfamethoxazole complexed with AuI, AgI, HgII, CdII, NiII, and CuII. The minimal inhibitory concentration (MIC) value was used to evaluate the antifungal and antibacterial properties of the compounds. In addition, it was also evaluated the antibiofilm capacity in Pseudomonas aeruginosa, through the quantification of its biomass and visualization using atomic force microscopy. For each case, molecular docking calculations were carried out to suggest the possible biological target of the assayed inorganic complexes. Our results indicated that the novel inorganic complexes are better antibacterial and antifungal than the commercial antibiotic sulfamethoxazole, highlighting the AgI-complex, which was able to inhibit the growth of microorganisms that cause lung diseases with concentrations in the 2-8 µg mL-1 range, probably at targeting dihydropteroate synthetase - a key enzyme involved in the folate synthesis. Furthermore, sulfamethoxazole complexes were able to inhibit the formation of bacterial biofilms at significantly lower concentrations than free sulfamethoxazole, probably mainly targeting the active site of LysR-type transcriptional regulator (PqsR). Overall, the present study reports preliminary results that demonstrate the derivatization of sulfamethoxazole with transition metal cations to obtain potential metallodrugs with applications as antimicrobial and antifungal against pulmonary infections, being an alternative for drug-resistant strains.

Multifunctional coatings of exfoliated and reassembled graphite on cellulosic substrates.

Exfoliated and reassembled graphite (ERG) forms macroscopic, high aspect ratio (1 : >106) and highly conductive coating layers that are strongly adherent to paper, wood, cloth, ceramic and other substrates. The coating precursor is an aqueous dispersion of graphite that exfoliates spontaneously in alkaline cellulose solutions, forming stable dispersions. These can be applied to the substrates by using different painting, coating and lithography techniques. The coating morphology changes from highly smooth to porous and rough, depending on the finishing procedure used. Coated paper sheets are flexible and they perform as leads in electrical circuitry and as electrodes in electrodeposition, supercapacitors, hygroelectricity cells and other electrochemical devices suitable for flexible and wearable electronics. These unique properties of ERG are explained as a consequence of the amphiphilic character of cellulose, which allows it to play the roles of exfoliant, dispersant, stabilizer, adhesive and plasticizer, while graphite powder is transformed into a cohesive laminated nanocomposite.

Photophysical, photobiological, and mycobacteria photo-inactivation properties of new meso-tetra-cationic platinum(II) metalloderivatives at meta position.

In this manuscript, we report the photo-inactivation evaluation of new tetra-cationic porphyrins with peripheral Pt(II) complexes ate meta N-pyridyl positions in the antimicrobial photodynamic therapy (aPDT) of rapidly growing mycobacterial strains (RGM). Four different metalloderivatives were synthetized and applied. aPDT experiments in the strains of Mycobacteroides abscessus subsp. Abscessus (ATCC 19977), Mycolicibacterium fortuitum (ATCC 6841), Mycobacteroides abscessus subsp. Massiliense (ATCC 48898), and Mycolicibacterium smegmatis (ATCC 700084) conducted with adequate concentration of photosensitizers (PS) under white-light conditions at 90 min (irradiance of 50 mW cm-2 and a total light dosage of 270 J cm-2) showed that the Zn(II) derivative is the most effective PS significantly reduced the concentration of viable mycobacteria. The effectiveness of the molecule as PS for PDI studies is also clear with mycobacteria, which is strongly related with the porphyrin peripheral charge and coordination platinum(II) compounds and consequently about the presence of metal center ion. This class of PS may be promising antimycobacterial aPDT agents with potential applications in medical clinical cases and bioremediation.

The First Report of In Vitro Antifungal and Antibiofilm Photodynamic Activity of Tetra-Cationic Porphyrins Containing Pt(II) Complexes against Candida albicans for Onychomycosis Treatment.

Onychomycosis is a prevalent nail fungal infection, and Candida albicans is one of the most common microorganisms associated with it. One alternative therapy to the conventional treatment of onychomycosis is antimicrobial photoinactivation. This study aimed to evaluate for the first time the in vitro activity of cationic porphyrins with platinum(II) complexes 4PtTPyP and 3PtTPyP against C. albicans. The minimum inhibitory concentration of porphyrins and reactive oxygen species was evaluated by broth microdilution. The yeast eradication time was evaluated using a time-kill assay, and a checkerboard assay assessed the synergism in combination with commercial treatments. In vitro biofilm formation and destruction were observed using the crystal violet technique. The morphology of the samples was evaluated by atomic force microscopy, and the MTT technique was used to evaluate the cytotoxicity of the studied porphyrins in keratinocyte and fibroblast cell lines. The porphyrin 3PtTPyP showed excellent in vitro antifungal activity against the tested C. albicans strains. After white-light irradiation, 3PtTPyP eradicated fungal growth in 30 and 60 min. The possible mechanism of action was mixed by ROS generation, and the combined treatment with commercial drugs was indifferent. The 3PtTPyP significantly reduced the preformed biofilm in vitro. Lastly, the atomic force microscopy showed cellular damage in the tested samples, and 3PtTPyP did not show cytotoxicity against the tested cell lines. We conclude that 3PtTPyP is an excellent photosensitizer with promising in vitro results against C. albicans strains.

CAD-CAM milled versus pressed lithium-disilicate monolithic crowns adhesively cemented after distinct surface treatments: Fatigue performance and ceramic surface characteristics.

To evaluate the fatigue failure load (FFL), number of cycles for failure (CFF) and survival probabilities of lithium-disilicate (LD) monolithic crowns manufactured by two processing techniques (pressing vs. CAD/CAM) adhesively cemented to a dentin-analogue material, considering two surface treatments (conventional vs. simplified). Surface characteristics (topography, roughness and fractal dimensions) were also assessed. Forty (40) monolithic crowns were manufactured considering two specific processing techniques for each ceramic system: LDCAD - CAD/CAM lithium-disilicate (IPS e.max CAD, Ivoclar Vivadent); LDPRESS - pressed lithium-disilicate (IPS e.max Press, Ivoclar Vivadent). The crowns were adhesively cemented (Multilink Automix System, Ivoclar Vivadent) onto dentin analogue preparations considering two distinct protocols of surface treatments (conventional - hydrofluoric acid etching + silane application [HF+Sil] or simplified - etching with one-step primer (Monobond Etch&Prime, Ivoclar Vivadent) [EP]). The cemented assembly was stored in distilled water at 37 °C for 3 days and fatigue tests were run (step-stress approach: load ranging from 400 to 2000 N, step-size of 100 N, 15,000 cycles/step, 20 Hz). Fractography, surface topography, roughness, and fractal dimension analyses were performed. LDPRESS[EP] group depicted higher FFL, CFF and survival probabilities in comparison to LDCAD groups, regardless of the conditioning method. A tendency of higher Weibull modulus (mechanical reliability) was observed when using [EP] for both LDPRESS and LDCAD. SEM and AFM analysis showed very distinct initial surface patterns for the distinct processing techniques considered (LDCAD with higher fractal dimension and lower roughness than LDPRESS), and both surface treatments distinctly affected these surface characteristics. All failures were radial cracks originating at the ceramic-cement interface. Pressed lithium-disilicate monolithic crowns showed better fatigue performance in comparison to CAD/CAM milled crowns, especially when they were treated with self-etching ceramic primer. The surface treatment with self-etching primer led to similar fatigue performance when compared to hydrofluoric acid plus silane application for the same processing technique, but it tended to provide higher mechanical reliability.