RESUMO
The aim of this work was to develop and characterize nanoparticles as carriers of lapazine, a phenazine derived from ß-lapachone; its antimycobacterial activity is described for the first time as a potential treatment for tuberculosis. The lapazine was synthesized, and by using gas chromatography coupled to a flame ionization detector, it was possible to evaluate its purity degree of almost 100%. For better elucidation of the molecular structure, mass spectroscopy and 1H NMR were carried out and compared to the literature values. Lapazine was assayed in vitro against H37Rv Mycobacterium tuberculosis and a rifampicin-resistant strain, with minimum inhibitory concentration values of 3.00 and 1.56 µg mL(-1), respectively. The nanoparticles showed a polydispersity index of 0.16,mean diameter of 188.5 ± 1.7 mm, zeta potential of -15.03 mV, and drug loading of 54.71 mg g(-1) for poly-ε-caprolactone (PCL) nanoparticles and a polydispersity index of 0.318,mean diameter of 197.4 ± 2.7 mm, zeta potential of -13.43 mV and drug loading of 137.07 mg g(-1) for poly(DL-lactide-co-glycolide) (PLGA) nanoparticles. These results indicate that both polymeric formulations have good characteristics as potential lapazine carriers in the treatment of tuberculosis.
Assuntos
Antituberculosos/síntese química , Antituberculosos/farmacologia , Ácido Láctico/química , Nanopartículas/química , Fenazinas/síntese química , Fenazinas/farmacologia , Poliésteres/química , Ácido Poliglicólico/química , Antituberculosos/química , Liberação Controlada de Fármacos , Cinética , Testes de Sensibilidade Microbiana , Mycobacterium tuberculosis/efeitos dos fármacos , Nanopartículas/ultraestrutura , Tamanho da Partícula , Fenazinas/química , Copolímero de Ácido Poliláctico e Ácido Poliglicólico , Eletricidade Estática , Difração de Raios XRESUMO
Most magnetotactic bacteria (MB) produce stable, single-domain magnetite nanocrystals with species-specific size, shape and chain arrangement. In addition, most crystals are elongated along the [111] direction, which is the easy axis of magnetization in magnetite, chemically pure and structurally perfect. These special characteristics allow magnetite crystal chains from MB to be recognized in environmental samples including old sedimentary rocks. Ferromagnetic resonance (FMR) has been proposed as a powerful and practical tool for screening large numbers of samples possibly containing magnetofossils. Indeed, several studies were recently published on FMR of cultured MB, mainly Magnetospirillum gryphiswaldense. In this work, we examined both uncultured magnetotactic cocci and the cultured MB M. gryphiswaldense using transmission electron microscopy (TEM) and FMR from 10 K to room temperature (RT). The TEM data supported the FMR spectral characteristics of our samples. The FMR spectra of both bacteria showed the intrinsic characteristics of magnetite produced by MB, such as extended absorption at the low field region of the spectra and a Verwey transition around 100 K. As previously observed, the spectra of M. gryphiswaldense isolated crystals were more symmetrical than the spectra obtained from whole cells, reflecting the loss of chain arrangement due to the small size and symmetrical shape of the crystals. However, the FMR spectra of magnetic crystals isolated from magnetotactic cocci were very similar to the FMR spectra of whole cells, because the chain arrangement was maintained due to the large size and prismatic shape of the crystals. Our data support the use of FMR spectra to detect magnetotactic bacteria and magnetofossils in samples of present and past environments. Furthermore, the spectra suggest the use of the temperature transition of spectral peak-to-peak intensity to obtain the Verwey temperature for these systems.
Assuntos
Óxido Ferroso-Férrico/análise , Magnetismo/métodos , Magnetossomos/química , Magnetospirillum/citologia , Cristalização , Magnetossomos/ultraestrutura , Magnetospirillum/química , Magnetospirillum/ultraestrutura , Microscopia Eletrônica de TransmissãoRESUMO
The aim of this study was to evaluate the strontium incorporation into specific bones and teeth of rats treated with strontium ranelate. The relative strontium levels [Sr/(Ca + Sr) ratio] were obtained by synchrotron radiation micro X-ray fluorescence. The incisor teeth were further examined by energy dispersive X-ray spectroscopy (EDS) in a scanning electron microscope. The isolated mineral phase was investigated by EDS in a transmission electron microscope and X-ray diffraction. The strontium content was markedly increased in animals treated with strontium ranelate, with different incorporation levels found among specific bones, regions within the same bone and teeth. The highest strontium levels were observed in the iliac crest, mandible and calvaria, while the lowest were observed in the femoral diaphysis, lumbar vertebrae, rib and alveolar bone. The strontium content was higher in the femoral neck than in the diaphysis. The strontium levels also varied within the alveolar bone. High levels of strontium were found in the incisor tooth, with values similar to those in the iliac crest. Strontium was observed in both enamel and dentin. The strontium content of the molar tooth was negligible. Strontium was incorporated into the mineral substance, with up to one strontium replacing one out of 10 calcium ions within the apatite crystal lattice. The mineral from treated animals presented increased lattice parameters, which might be associated to their bone strontium contents. In conclusion, the incorporation of strontium occurred in different levels into distinct bones, regions within the same bone and teeth of rats treated with strontium ranelate.
Assuntos
Conservadores da Densidade Óssea/farmacocinética , Osso e Ossos/metabolismo , Compostos Organometálicos/farmacocinética , Estrôncio/metabolismo , Tiofenos/farmacocinética , Dente/metabolismo , Animais , Densidade Óssea , Ratos , Ratos Wistar , Espectrometria por Raios X , Distribuição Tecidual , Difração de Raios XRESUMO
Magnetotactic bacteria produce magnetosomes, which are magnetic particles enveloped by biological membranes, in a highly controlled mineralization process. Magnetosomes are used to navigate in magnetic fields by a phenomenon called magnetotaxis. Two levels of organization and control are recognized in magnetosomes. First, magnetotactic bacteria create a spatially distinct environment within vesicles defined by their membranes. In the vesicles, the bacteria control the size, composition and purity of the mineral content of the magnetic particles. Unique crystal morphologies are produced in magnetosomes as a consequence of this bacterial control. Second, magnetotactic bacteria organize the magnetosomes in chains within the cell body. It has been shown in a particular case that the chains are positioned within the cell body in specific locations defined by filamentous cytoskeleton elements. Here, we describe an additional level of organization of the magnetosome chains in uncultured magnetotactic cocci found in marine and freshwater sediments. Electron microscopy analysis of the magnetosome chains using a goniometer showed that the magnetic crystals in both types of bacteria are not oriented at random along the crystal chain. Instead, the magnetosomes have specific orientations relative to the other magnetosomes in the chain. Each crystal is rotated either 60°, 180° or 300° relative to their neighbors along the chain axis, causing the overlapping of the (1 1 1) and [Formula in text] capping faces of neighboring crystals. We suggest that genetic determinants that are not present or active in bacteria with magnetosomes randomly rotated within a chain must be present in bacteria that organize magnetosomes so precisely. This particular organization may also be used as an indicative biosignature of magnetosomes in the study of magnetofossils in the cases where this symmetry is observed.
Assuntos
Magnetossomos/ultraestrutura , Bactérias/metabolismo , Bactérias/ultraestrutura , Cristalização , Óxido Ferroso-Férrico/metabolismo , Magnetismo , Magnetossomos/química , Microscopia EletrônicaRESUMO
In this paper, we quantify the magnetic material amount in Solenopsis ants using ferromagnetic resonance (FMR) at room temperature. We sampled S. interrupta workers from several morphologically indistinguishable castes. Twenty-five oriented samples of each body part of S. interrupta (20 units each) showed that FMR line shapes are reproducible. The relative magnetic material amount was 31 +/- 12% (mean +/- SD) in the antennae, 27 +/- 13% in the head, 21 +/- 12% in the thorax and 20 +/- 10% in the abdomen. In order to measure variation in the magnetic material from late summer to early winter, ants were collected each month between March and July. The amount of magnetic material was greatest in all four body parts in March and least in all four body parts in June. In addition, S. richteri majors presented more magnetic material than minor workers. Extending these findings to the genera Solenopsis, the reduction in magnetic material found in winter could be explained by our sampling fewer foraging major ants.