Herein we report the screening of a small library of aurones and their isosteric counterparts, azaaurones and N-acetylazaaurones, against Mycobacterium tuberculosis. Aurones were found to be inactive at 20 μm , whereas azaaurones and N-acetylazaaurones emerged as the most potent compounds, with nine derivatives displaying MIC99 values ranging from 0.4 to 2.0 μm . In addition, several N-acetylazaaurones were found to be active against multidrug-resistant (MDR) and extensively drug-resistant (XDR) clinical M. tuberculosis isolates. The antimycobacterial mechanism of action of these compounds remains to be determined; however, a preliminary mechanistic study confirmed that they do not inhibit the mycobacterial cytochrome bc1 complex. Additionally, microsomal metabolic stability and metabolite identification studies revealed that N-acetylazaaurones are deacetylated to their azaaurone counterparts. Overall, these results demonstrate that azaaurones and their N-acetyl counterparts represent a new entry in the toolbox of chemotypes capable of inhibiting M. tuberculosis growth. 相似文献
High-performance YBCO 123 (YBa2Cu3O7-x) bulk superconductor samples were produced using the 3D printing paste-extrusion technique. The YBCO powder obtained after sintering a pre-mixture of Y2O3, BaCO3 and CuO powders at 950 °C was used in the formulation of pastes for extrusion in a 3D freeform printer. The 3D samples printed from pastes containing the pre-mixture powders were sintered, while those produced using the YBCO powder were not. X-ray diffraction (XRD), energy dispersive spectroscopy (EDS) and Raman analysis all confirmed the YBCO phase after sintering, both in the powder and in the samples made with the pre-mixture. Scanning electron microscopy (SEM) images revealed powder grains of heterogeneous size and geometry, as well as grain aggregation, in the sintered samples. Superconducting quantum interference device (SQUID) measurements taken within a fixed magnetic range revealed that the printed pieces have a typical magnetization temperature of 92 K, reaching ?1.43 emu/g and ?1.59 emu/g respectively a zero-field-cooled magnetization (ZFC) for sintered and non-sintered printed samples. 相似文献
Insulin is a peptide hormone with many physiological functions, besides its use in diabetes treatment. An important role of insulin is related to the wound healing process—however, insulin itself is too sensitive to the external environment requiring the protective of a nanocarrier. Polymer-based nanoparticles can protect, deliver, and retain the protein in the target area. This study aims to produce and characterize a topical treatment for wound healing consisting of insulin-loaded poly-DL-lactide/glycolide (PLGA) nanoparticles. Insulin-loaded nanoparticles present a mean size of approximately 500 nm and neutral surface charge. Spherical shaped nanoparticles are observed by scanning electron microscopy and confirmed by atomic force microscopy. SDS-PAGE and circular dichroism analysis demonstrated that insulin preserved its integrity and secondary structure after the encapsulation process. In vitro release studies suggested a controlled release profile. Safety of the formulation was confirmed using cell lines, and cell viability was concentration and time-dependent. Preliminary safety in vivo assays also revealed promising results. 相似文献
This research aims to illustrate the potential use of concepts, techniques, and mining process tools to improve the systematic review process. Thus, a review was performed on two online databases (Scopus and ISI Web of Science) from 2012 to 2019. A total of 9649 studies were identified, which were analyzed using probabilistic topic modeling procedures within a machine learning approach. The Latent Dirichlet Allocation method, chosen for modeling, required the following stages: 1) data cleansing, and 2) data modeling into topics for coherence and perplexity analysis. All research was conducted according to the standards of the Preferred Reporting Items for Systematic Reviews and Meta-Analyses in a fully computerized way. The computational literature review is an integral part of a broader literature review process. The results presented met three criteria: (1) literature review for a research area, (2) analysis and classification of journals, and (3) analysis and classification of academic and individual research teams. The contribution of the article is to demonstrate how the publication network is formed in this particular field of research, and how the content of abstracts can be automatically analyzed to provide a set of research topics for quick understanding and application in future projects.
Incorporating spent coffee grounds (SCGs), a by‐product from coffee brewing, in growth substrate of beneficial edible mushrooms is an approach that has to be further studied due to its potential positive outcomes: environmental impact mitigation, production costs reduction and beneficial impact on consumer health. Hence, cultivation of Pleurotus citrinopileatus and Pleurotus salmoneo‐stramineus was tested using SCG which enabled maximum production yield of P. citrinopileatus which was of 25.1% (w/w). Variable antidiabetic potential was observed between aqueous and enzymatic extracts (3.8%–29% inhibition) regardless species and substrates, whereas aqueous extract of P. citrinopileatus grown in substrate without SCG stood out presenting the highest antioxidant activity and inhibition activity of angiotensin I‐converting enzyme (IC50 = 123 μg mL?1). Ethanolic and aqueous extracts of both Pleurotus species grown in the presence or absence of SGC proved to be an interesting prebiotic source for growth of Bifidobacterium animalis Bo in comparison with fructooligosaccharides (FOS). 相似文献
Chitosan microspheres containing bromocresol green, cresol red, and phenolphthalein for corrosion detection, through pH change, are synthesized in order to be used in protective coatings for aluminium alloys. Microspheres containing corrosion detection species are characterized morphologically (SEM) and physico‐chemically (FTIR, TGA). Release studies (UV–vis) are performed in corrosion‐promoting conditions (pH, NaCl), and detection studies by immersion in media associated with corrosion activity while microspheres' sensing activity is evaluated visually. Electrochemical characterization of AA2024 substrates in the presence of chitosan spheres is performed to understand material performance, and a color change is observed as a result of local pH increase in cathodic areas when corrosion takes place. These findings can be correlated with the results from release studies and seem a promising approach for corrosion sensing purposes, not only because pH increase is possible to detect due to corrosion, but also because chitosan is considered an environmentally friendly material. 相似文献
Cellular aggregates are used as relevant regenerative building blocks, tissue models, and cell delivery platforms. Biomaterial-free structures are often assembled either as 2D cell sheets or spherical microaggregates, both incompatible with free-form deposition, and dependent on challenging processes for macroscale 3D upscaling. The continuous and elongated nature of fiber-shaped materials enables their deposition in unrestricted multiple directions. Cellular fiber fabrication has often required exogenously provided support proteins and/or the use of biomaterial-based sacrificial templates. Here, the rapid (<24 h) assembly of fiberoids is reported: living centimeter-long scaffold-free fibers of cells produced in the absence of exogenous materials or supplements. Adipose-derived mesenchymal stem cell fiberoids can be easily modulated into complex multidimensional geometries and show tissue-invasive properties while keeping the secretion of trophic factors. Proangiogenic properties studied on a chick chorioallantoic membrane in an ovo model are observed for heterotypic fiberoids containing endothelial cells. These micro-to-macrotissues may find application as morphogenic therapeutic and tissue-mimetic building blocks, with the ability to integrate 3D and 4D full biological materials. 相似文献
Osteosarcoma (OS) is a rare condition with very poor prognosis in a metastatic setting. Basic research has enabled a better understanding of OS pathogenesis and the discovery of new potential therapeutic targets. Phase I and II clinical trials are already ongoing, with some promising results for these patients. This article reviews OS pathogenesis and new potential therapeutic targets. 相似文献