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Lipase production by solid‐state fermentation of olive pomace in tray‐type and pressurized bioreactors 下载免费PDF全文
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Maarten Sijm Julianna Siciliano de Araújo Alba Ramos Llorca Dr. Kristina Orrling Lydia Stiny An Matheeussen Prof. Dr. Louis Maes Prof. Dr. Iwan J. P. de Esch Dr. Maria de Nazaré Correia Soeiro Dr. Geert Jan Sterk Prof. Dr. Rob Leurs 《ChemMedChem》2019,14(18):1662-1668
Chagas disease is becoming a worldwide problem; it is currently estimated that over six million people are infected. The two drugs in current use, benznidazole and nifurtimox, require long treatment regimens, show limited efficacy in the chronic phase of infection, and are known to cause adverse effects. Phenotypic screening of an in-house library led to the identification of 2,2′-methylenebis(5-(4-bromophenyl)-4,4-dimethyl-2,4-dihydro-3H-pyrazol-3-one), a phenyldihydropyrazolone dimer, which shows an in vitro pIC50 value of 5.4 against Trypanosoma cruzi. Initial optimization was done by varying substituents of the phenyl ring, after which attempts were made to replace the phenyl ring. Finally, the linker between the dimer units was varied, ultimately leading to 2,2′-methylenebis(5-(3-bromo-4-methoxyphenyl)-4,4-dimethyl-2,4-dihydro-3H-pyrazol-3-one (NPD-0228) as the most potent analogue. NPD-0228 has an in vitro pIC50 value of 6.4 against intracellular amastigotes of T. cruzi and no apparent toxicity against the human MRC-5 cell line and murine cardiac cells. 相似文献
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André Campaniço Dr. Marta P. Carrasco Dr. Mathew Njoroge Ronnett Seldon Prof. Kelly Chibale Dr. João Perdigão Prof. Isabel Portugal Prof. Digby F. Warner Prof. Rui Moreira Prof. Francisca Lopes 《ChemMedChem》2019,14(16):1537-1546
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
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Diogo Mendes David Sousa Ana C. Cerdeira Laura C.J. Pereira Ana Marques João Murta-Pina Anabela Pronto Isabel Ferreira 《Ceramics International》2021,47(1):381-387
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
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Maria Quitrio Sandra Simes Andreia Ascenso Manuela Carvalheiro Ana Paula Leandro Isabel Correia Ana Silveira Viana Pedro Faísca Lia Ascenso Jesús Molpeceres Maria Manuela Gaspar Catarina Pinto Reis 《International journal of molecular sciences》2021,22(8)
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
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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
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Isabel Fernandes Cecília Melo-Alvim Raquel Lopes-Brs Miguel Esperana-Martins Luís Costa 《International journal of molecular sciences》2021,22(2)
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