Fluconazole is a bistriazole derivative with antifungal activity. The major weak points of fluconazole are the development of antifungal resistance and low water solubility, which impairs its administration. Binary systems between fluconazole and beta-cyclodextrin were prepared with the aim of obtaining a new delivery system that will overcome the limitations of fluconazole administration. Using two feasible laboratory methods, inclusion complexes between fluconazole and beta-cyclodextrin were obtained. Thermal and spectroscopic analyses were used to characterize the inclusion complexes.
Recent scientific evidence suggests a link between epigenetic changes (DNA methylation) and tumorigenesis. Moreover, a potential carcinogenic mechanism of cadmium was associated with changes in DNA methylation. In this study we investigated the impact of CdCl 2 and CuSO 4 aqueous solutions on DNA methylation in HT-29 cells by quantifying DNA methyltransferase (DNMT1, DNMT3A and DNMT3B) mRNA expression. Furthermore, we also studied the cytotoxic and anti-migratory potential of these substances. The results showed a dose-dependent decrease of viable cell percentage following 24 h of exposure (at concentrations of 0.05; 0.2; 1; 10 and 100 µg/ml), and an inhibitory effect on HT-29 cell migration capacity. In addition, RT-qPCR results showed that cadmium acts as a hypomethylating agent by suppressing DNMT expression, whereas copper acts as a hypermethylating compound by increasing DNMT expression. These findings suggest a cytotoxic potential of both cadmium and copper on HT-29 cells and their capacity to induce epigenetic changes.
Iron oxide nanoparticles were synthesized starting from two aqueous extracts based on Artemisia absinthium L. leaf and stems, employing a simplest, eco-friendliness and low toxicity method—green synthesis. The nanoparticles were characterized by powder X-ray diffraction (XRD), Fourier transformed infrared spectroscopy (FT-IR), X-ray fluorescence analysis (XRF), thermal analysis (TG/DSC), and scanning electron microscopy (SEM). Lack of magnetic properties and the reddish-brown color of all the samples confirms the presence of hematite as majority phase. The FTIR bands located at 435 cm−1 and 590 cm−1, are assigned to Fe-O stretching vibration from hematite, confirming the formation of α-Fe2O3 nanoparticles (NPs). The in vitro screening of the samples revealed that the healthy cell line (HaCaT) presents a good viability (above 80%) after exposure to iron oxide NPs and lack of apoptotic features, while the tumorigenic cell lines manifested a higher sensitivity, especially the melanoma cells (A375) when exposed to concentration of 500 µg/mL iron oxide NPs for 72 h. Moreover, A375 cells elicited significant apoptotic markers under these parameters (concentration of 500 µg/mL iron oxide NPs for a contact time of 72 h).
The current study was aimed to evaluate the phenolic composition parameters of two hydro-alcoholic extracts of Ocimum basilicum L. (OB) obtained from the aerial part (without leaves) and leaves, in order to determine their contribution to the antioxidant activity (AOA). Both hydro-alcoholic extracts have proven to be rich in polyphenolic compounds, flavonoids, flavonols and tannins. Therefore, the leaves’ extracts reveal an inhibition percentage of 89%, almost comparable with the standard reference (95%). To complete the toxicological profile, the study also assessed the potential cytotoxicity of basil hydro-alcoholic extracts on immortalized human keratinocytes (HaCaT), skin human fibroblasts (1BR3), mice epidermis (JB6Cl41-5a) and primary human melanocytes (HEMa) cells, correlated to A375 antitumor in vitro activity. The extracts did not induce significant cytotoxic effect on any of the selected normal cell lines but showed relevant activity on A375 cells. Considering the low values obtained regarding the irritative effects in the chorionallantoic membrane of the egg on blood vessels, we can emphasize that both extracts can be considered as biocompatible ingredients. Regarding the potential activity of hydro-alcoholic extracts on human skin, the decrease of erythema values after the application of extracts was a relevant observation which indicates the anti-inflammatory potential of Ocimum basilicum L.
The Herpes simplex viruses (HSV-1, HSV-2) are responsible for a wide variety of conditions, from cutaneous-mucosal to central nervous system (CNS) infections and occasional infections of the visceral organs, some of them with a lethal end. Acyclovir is often used intravenously, orally, or locally to treat herpetic infections but it must be administered with caution to patients with kidney disease and to children of early age. The main objectives of this study were to synthesize and evaluate new polyurethane nanoparticles that might be used as proper transmembrane carriers for acyclovir. Polyurethane particles were obtained by a polyaddition process: a mixture of two aliphatic diisocyanates used as organic phase was added to a mixture of butanediol and polyethylene glycol used as aqueous phase. Two different samples (with and without acyclovir, respectively) were synthesized and characterized by UV-Vis spectra in order to assess the encapsulation efficacy and the release profile, FT-IR, DSC, SEM, and SANS for structural characterization, as well as skin irritation tests. Nearly homogeneous samples with particle sizes between 78 and 91 nm have been prepared and characterized revealing a medium tendency to form clusters and a high resistance to heat up to 300 °C. The release profile of these nanoparticles is characteristic to a drug delivery system with a late discharge of the loaded active agents. Very slight increases in the level of transepidermal water loss and erythema were found in a 15-day evaluation on human skin. The results suggest the synthesis of a non-irritative carrier with a high encapsulation efficacy that can be successfully used for the transmembrane transfer of acyclovir.
As prophylactic and therapeutic approaches for melanoma, of great interest and importance are the in vitro studies using cell lines to elucidate several tumoral phenomena. Therefore, the similarities and differences between the different tumor cells must be known and understood in order to obtain a more accurate correlation with processes that occur in vivo. In this study, six cell lines of melanoma, both of mouse and human origin were analyzed from the point of view of cell culture growth, morphology and use in the research of new therapies. In brief, the current paper exhibits a comparison of melanoma cells which can be utilized as a starting point for further in vitro studies and in vivo animal models.
A biomaterial must be biologically compatible, mechanical, functional, corrosion resistant and easily adapt to clinical and laboratory technologies. Dental biomaterials are materials used to replace a part of a living system or to work closely with living tissue. Many scientific articles present different polymeric biocomposites with possible application in dentistry and this is a proof of the opportunity of a research in a field in full ascent and with great availability in the promotion of materials destined to �work under biological constraint� and which must also meet the functional requirements of a dental implant. The objectives of this research were to obtain and to comparatively evaluate different polymeric microparticles that can be used in dentistry. The samples based on poly(lactic-co-glycolic acid) and respectively polyurethane microparticles were characterized by pH and Zetasizer measurements, and in vitro cytotoxicity assays. The results indicate the obtaining of particles with a neutral pH, medium homogeneity, and with different tendencies to form agglomerations. Their low cytotoxicity, tested on the primary human gingival fibroblasts by MTT and LDH techniques, indicates that these microparticles are safe to be tested in further clinical evaluations.
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