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51.
Stefan Bleher Jonas Buck Christian Muhl Sandro Sieber Sabine Barnert Dominik Witzigmann Jrg Huwyler Matthias Barz Regine Süss 《Small (Weinheim an der Bergstrasse, Germany)》2019,15(50)
Circulation lifetime is a crucial parameter for a successful therapy with nanoparticles. Reduction and alteration of opsonization profiles by surface modification of nanoparticles is the main strategy to achieve this objective. In clinical settings, PEGylation is the most relevant strategy to enhance blood circulation, yet it has drawbacks, including hypersensitivity reactions in some patients treated with PEGylated nanoparticles, which fuel the search for alternative strategies. In this work, lipopolysarcosine derivatives (BA‐pSar, bisalkyl polysarcosine) with precise chain lengths and low polydispersity indices are synthesized, characterized, and incorporated into the bilayer of preformed liposomes via a post insertion technique. Successful incorporation of BA‐pSar can be realized in a clinically relevant liposomal formulation. Furthermore, BA‐pSar provides excellent surface charge shielding potential for charged liposomes and renders their surface neutral. Pharmacokinetic investigations in a zebrafish model show enhanced circulation properties and reduction in macrophage recognition, matching the behavior of PEGylated liposomes. Moreover, complement activation, which is a key factor in hypersensitivity reactions caused by PEGylated liposomes, can be reduced by modifying the surface of liposomes with an acetylated BA‐pSar derivative. Hence, this study presents an alternative surface modification strategy with similar benefits as the established PEGylation of nanoparticles, but with the potential of reducing its drawbacks. 相似文献
52.
Fábio J.B. Brum Sandro C. Amico Ivo Vedana Jaime A. Spim 《Journal of Materials Processing Technology》2009,209(7):3166-3171
Autoclave processing is commonly used nowadays for dewaxing in the investment casting process. However, since the use of microwave is steadily growing in industrial processes and the wax interacts with the electromagnetic energy of the microwaves, the present work studies the possibility of carrying out dewaxing via microwave. The wax (mineral wax, vegetable resin, low molecular-weight polymer and anti-oxidant) used in this work was prepared by melting in an oven equipped with a mineral oil bath. The chemical and structural stability of the wax were monitored throughout 12 simulated dewaxing cycles, via various analyses, namely, volumetric expansion, hardness, Fourier transform infrared spectroscopy, ultraviolet–visible spectrophotometry, differential scanning calorimetry and viscosity. The results showed that microwave dewaxing is viable, significantly decreasing the incorporation of dirt and water, which is inevitable in the autoclave dewaxing process. 相似文献
53.
The paper aims to show how regional policy‐makers can stimulate firms' co‐operation with research organizations by granting an R&D subsidy. Using an original dataset for the Italian region of Emilia‐Romagna, propensity score matching is first applied to identify the impact of the subsidy received. A generalized propensity score technique is then employed to investigate the effect of an increasing amount of support. The firm's co‐operation is policy sensitive. The award of a subsidy to regional firms affects their intra‐regional more than their extra‐regional co‐operation. The propensity toward the latter appears subject to a monetary effect and is influenced by the amount of public funding received providing the subsidy overcomes a minimum threshold. 相似文献
54.
The plasticizers di-2-ethylhexyl phthalate (DEHP) and di-2-ethylhexyl adipate (DEHA) are ubiquitous in the environment and undergo partial biodegradation in the presence of soil micro-organisms. The validity of a proposed pathway for the degradation of these plasticizers by Rhodococcus rhodochrous has been confirmed by the identification of 2-ethylhexanal in gas phase emissions. Complete analyses of the aqueous and gas phases were able to account for more than 98% of the 2-ethylhexanol component of the DEHA added at the beginning of a growth study. Of this, 25% was either 2-ethylhexanol or 2-ethylhexanal that had been stripped into the gas phase and, at most, only 2% of the 2-ethylhexanol component could have been removed by mineralization. It is concluded that plasticizers are of significant environmental concern due to the resistance of the metabolites to biodegradation and their known health impacts. Two of the metabolites are of added concern due to their volatility and their potential impact on indoor air quality. 相似文献
55.
Alok Warey Sandro Balestrino Pat Szymkowicz M. R. Malayeri 《Aerosol science and technology》2013,47(2):198-213
Cooled exhaust gas recirculation (EGR) is widely used in diesel engines to control engine out NOx (oxides of nitrogen) emissions. A portion of the exhaust gases is recirculated into the intake manifold of the engine after cooling it through a heat exchanger. EGR cooler heat exchangers, however, tend to lose efficiency and have increased pressure drop as deposit forms on the heat exchanger surface. This adversely affects the combustion process, engine durability, and emissions. In this study, a 1-D model was developed to simulate soot deposition, soot removal, and condensation of several hydrocarbon (HC) species in a circular tube with turbulent gas flow at constant wall temperature. The circular tube, which makes up the computational domain in the model, represents a single channel from any EGR cooler geometry. The model takes into account soot particle deposition due to thermophoresis, diffusion, turbulent impaction, and gravitational drift. However, thermophoresis was found to be the most dominant deposition mechanism for boundary conditions at which EGR coolers typically operate. Soot removal was modeled by considering a force balance between the drag and van der Waals forces. A lognormal distribution of particles was assumed at the tube inlet. The evolution of the particle distribution in the bulk flow along the tube as well as the mass distribution in the deposit layer on the tube walls is predicted by the model. Condensation of six HC species between C15-C24 alkanes was also modeled. Predictions made by the model are in reasonably good agreement with experimental data obtained from a laboratory reactor under the same boundary conditions. There are several assumptions and simplifications built into the model, which can be refined further to improve it. Copyright 2012 American Association for Aerosol Research 相似文献
56.
Dr. Santina Maiorana Prof. Roberta Ettari Dr. Santo Previti Dr. Giorgio Amendola Dr. Annika Wagner Prof. Sandro Cosconati Prof. Ute A. Hellmich Prof. Tanja Schirmeister Prof. Maria Zappalà 《ChemMedChem》2020,15(16):1552-1561
In this paper, we report the design, synthesis and biological investigation of a series of peptidyl vinyl ketones obtained by modifying the P2 fragment of previously reported highly potent inhibitors of rhodesain, the main cysteine protease of Trypanosoma brucei rhodesiense. Investigation of the structure–activity relationship led us to identify new rhodesain inhibitors endowed with an improved selectivity profile (a selectivity index of up to 22 000 towards the target enzyme), and/or an improved antitrypanosomal activity in the sub-micromolar range. 相似文献
57.
Dr. Carolyn Vargas Prof. Dr. Gerald Radziwill Dr. Gerd Krause Dr. Anne Diehl Prof. Dr. Sandro Keller Dr. Nestor Kamdem Prof. Dr. Constantin Czekelius Annika Kreuchwig Dr. Peter Schmieder Dr. Declan Doyle Prof. Dr. Karin Moelling Dr. Volker Hagen Dr. Markus Schade Prof. Dr. Hartmut Oschkinat 《ChemMedChem》2014,9(7):1458-1462
PDZ (PSD‐95, Dlg, ZO‐1) domains are ubiquitous interaction modules that are involved in many cellular signal transduction pathways. Interference with PDZ‐mediated protein–protein interactions has important implications in disease‐related signaling processes. For this reason, PDZ domains have gained attention as potential targets for inhibitor design and, in the long run, drug development. Herein we report the development of small molecules to probe the function of the PDZ domain from human AF6 (ALL1‐fused gene from chromosome 6), which is an essential component of cell–cell junctions. These compounds bind to AF6 PDZ with substantially higher affinity than the peptide (Ile‐Gln‐Ser‐Val‐Glu‐Val) derived from its natural ligand, EphB2. In intact cells, the compounds inhibit the AF6–Bcr interaction and interfere with epidermal growth factor (EGF)‐dependent signaling. 相似文献
58.
Marcelo A. V. Souza Luiz Claudio de Santa Maria Marcos A. S. Costa Wang S. Hui Luciana C. Costa Hiram C. Araujo Filho Sandro C. Amico 《Polymer Bulletin》2011,67(2):237-249
Phosphinic-derivative poly(styrene-co-divinylbenzene)-based on PS–DVB copolymers with different porosity degrees have been prepared by aromatic electrophilic substitution reaction using PCl3/AlCl3 followed by base-promoted hydrolysis. The phosphorylation reaction was analyzed by infra-red spectroscopy (FTIR), scanning electron microscopy (SEM), and thermogravimetry (TG/DTG). In addition, the phosphorous content of the phosphorylated copolymers was determined by spectrophotometry using the method based on sodium molybdate reactant so that the extension of that modification could be assessed. The performance of the phosphorylated resins in the extraction of Pb2+ from aqueous solutions in a batch system was also evaluated. The Pb2+ content was determined by atomic absorption spectrometry (AAS). These materials presented excellent extraction capacity under the contact time of 30 min and pH 6. 相似文献
59.
Cinzia Ciccacci Sara Rufini Sandro Mancinelli Ersilia Buonomo Emiliano Giardina Paola Scarcella Maria C. Marazzi Giuseppe Novelli Leonardo Palombi Paola Borgiani 《International journal of molecular sciences》2015,16(3):5830-5838
Steven–Johnson Syndrome (SJS) and Toxic Epidermal Necrolysis (TEN) are severe adverse drug reactions, characterized by extensive epidermal detachment and erosions of mucous membrane. SJS/TEN is one of the most serious adverse reactions to Nevirapine (NVP) treatment, commonly used in developing countries as first-line treatment of human immunodeficiency virus infection. In the last years TRAF3IP2 gene variants had been described as associated with susceptibility to several diseases such as psoriasis and psoriatic arthritis. We hypothesized that this gene, involved in immune response and in NF-κB activation, could also be implicated in the SJS/TEN susceptibility. We performed a full resequencing of TRAF3IP2 gene in a population of patients treated with NVP. Twenty-seven patients with NVP-induced SJS/TEN and 78 controls, all from Mozambique, were enrolled. We identified eight exonic and three intronic already described variants. The case/control association analysis highlighted an association between the rs76228616 SNP in exon 2 and the SJS/TEN susceptibility. In particular, the variant allele (C) resulted significantly associated with a higher risk to develop SJS/TEN (p = 0.012 and OR = 3.65 (95% CI 1.33–10.01)). A multivariate analysis by logistic regression confirmed its significant contribution (p = 0.027, OR = 4.39 (95% CI 1.19–16.23)). In conclusion, our study suggests that a variant in TRAF3IP2 gene could be involved in susceptibility to SJS/TEN. 相似文献
60.
Caroline Pigatto Jos Humberto Santos Almeida Heitor Luiz Ornaghi Adriane Lawisch Rodríguez Cludia Mendes Mhlmann Sandro Campos Amico 《Polymer Composites》2012,33(12):2262-2270
Thermoplastics reinforced with natural fibers have attracted much attention from researchers because of their advantages, especially regarding environmental aspects. However, poor impact strength, particularly at low temperatures, limits the application of some thermoplastics, such as polypropylene (PP). To minimize this drawback, impact modifiers have been used, including the terpolymer of ethylene‐propylene‐diene (EPDM). In this work, PP/EPDM/sisal composites of distinct compositions were investigated focusing on the effect of the alkali (NaOH) treatment of the vegetable fiber on the composites properties regarding physical, mechanical, thermal, and morphological behavior. The results indicated that flow rate decreases at higher fiber content due to flow hindering by the presence of the fibers. The addition of the fiber, in general, increased Young's modulus and strength (tensile and flexural), whereas impact strength increased for higher EPDM content. The alkali treatment was considered generally efficient in terms of mechanical properties, even though this was not found in the dynamic mechanical analysis. POLYM. COMPOS., 2012. © 2012 Society of Plastics Engineers 相似文献