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1.
Mariana Tasso Thomas Pons Nicolas Lequeux Julie Nguyen Zsolt Lenkei Diana Zala 《Small (Weinheim an der Bergstrasse, Germany)》2019,15(47)
Single‐particle tracking with quantum dots (QDs) constitutes a powerful tool to track the nanoscopic dynamics of individual cell membrane components unveiling their membrane diffusion characteristics. Here, the nano‐resolved population dynamics of QDs is exploited to reconstruct the topography and structural changes of the cell membrane surface with high temporal and spatial resolution. For this proof‐of‐concept study, bright, small, and stable biofunctional QD nanoconstructs are utilized recognizing the endogenous neuronal cannabinoid receptor 1, a highly expressed and fast‐diffusing membrane protein, together with a commercial point‐localization microscope. Rapid QD diffusion on the axonal plasma membrane of cultured hippocampal neurons allows precise reconstruction of the membrane surface in less than 1 min with a spatial resolution of tens of nanometers. Access of the QD nanoconstructs to the synaptic cleft enables rapid 3D topological reconstruction of the entire presynaptic component. Successful reconstruction of membrane nano‐topology and deformation at the second time‐scale is also demonstrated for HEK293 cell filopodia and axons. Named “nanoPaint,” this super‐resolution imaging technique amenable to any endogenous transmembrane target represents a versatile platform to rapidly and accurately reconstruct the cell membrane nano‐topography, thereby enabling the study of the rapid dynamic phenomena involved in neuronal membrane plasticity. 相似文献
2.
Dr. Lilia Clima Bogdan Florin Craciun Dr. Andrea Angeli Andrea Petreni Alessandro Bonardi Dr. Alessio Nocentini Dr. Fabrizio Carta Prof. Paola Gratteri Prof. Mariana Pinteala Prof. Claudiu T. Supuran 《ChemMedChem》2020,15(21):2052-2057
We report novel molecules incorporating the nontoxic squalene scaffold and different carbonic anhydrase inhibitors (CAIs). Potent inhibitory action, in the low-nanomolar range, was detected against isoforms hCA II for sulfonamide derivatives, which proved to be selective against this isoform over the tumor-associate hCA IX and XII isoforms. On the other hand, coumarin derivatives showed weak potency but high selectivity against the tumor-associated isoform CA IX. These compounds are interesting candidates for preclinical evaluation in glaucoma or various tumors in which the two enzymes are involved. In addition, an in silico study of inhibitor-bound hCA II revealed extensive interactions with the hydrophobic pocket of the active site and provided molecular insights into the binding properties of these new inhibitors. 相似文献
3.
María Clara Verdi Constanza Melian Patricia Castellano Graciela Vignolo Mariana Blanco Massani 《International Journal of Food Science & Technology》2020,55(1):267-275
The effectiveness of antimicrobial mixtures against Listeria innocua 7, used as a L. monocytogenes surrogate, was investigated in broth and a food system. Synergistic effects were found for nisin (Nis), potassium sorbate (PS), calcium propionate (CP) and sodium lactate (SL), Nis + PS being the most effective binary mixture that exhibited listericidal activity in broth. To assess the effect of adding lactocin AL705 (AL705) to Nis + organic acid salt combinations, tridimensional isobolograms were generated. Sub-MIC combinations of the antimicrobials exerted bactericidal activity against L. innocua 7 after AL705 addition to the binary mixtures. However, when applied on Sardo cheese contaminated with L. innocua 7 (initial inoculum 4.45 ± 0.06 CFU g−1), only Nis + PS + AL705 produced count reductions respect to the control, reaching 3.04 ± 0.35 CFU g−1 counts after 15 days at 15 °C. Ternary combinations containing AL705 showed potential to reduce antimicrobial usages for L. innocua 7 inhibition. 相似文献
4.
Elisa Garza Montelongo María G. Sánchez Anguiano Leonor M. Blanco Jerez Eduardo D. Pereira Ulloa Bernabé L. Rivas Quiroz Perla Elizondo Martínez 《应用聚合物科学杂志》2020,137(40):49204
Poly(ethylene terephthalate)-based molecularly imprinted polymers (MIPs) were synthesized, and their recognition capability was evaluated. Adsorption isotherm was described by the Langmuir model and the maximum adsorption capacity of MIPTy reached 172.4 mg g−1 in water at pH 6.2. A recognition coefficient of 1.17 was obtained. A solid-phase extraction cartridge was manufactured and its behavior was evaluated for tylosin extraction from aqueous and milk samples. An off-line SPE-UV method was applied. An acceptable linearity was obtained in the range of 1–20 μg ml−1 and the average recovery at three spike levels in milk samples was higher than 92%. The limit of quantification was 2.6 × 10−2 μg ml−1. The manufactured SPE cartridge has a great potential for clean-up processes in complex media. The cartridge offers a fast and sensitive option to the existing sorbents for extracting this drug from milk samples. 相似文献
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6.
Correlation of structural characterization and viscosity measurements with total unsaturation: An effective method for controlling ozonation in the preparation of ozonated grape seed and sunflower oils 下载免费PDF全文
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8.
Lissy Z. F. Gross Mariana Sacerdoti Prof. Albrecht Piiper Prof. Stefan Zeuzem Dr. Alejandro E. Leroux Dr. Ricardo M. Biondi 《ChemMedChem》2020,15(18):1682-1690
Angiotensin converting enzyme 2 (ACE2) is the human receptor that interacts with the spike protein of coronaviruses, including the one that produced the 2020 coronavirus pandemic (COVID-19). Thus, ACE2 is a potential target for drugs that disrupt the interaction of human cells with SARS-CoV-2 to abolish infection. There is also interest in drugs that inhibit or activate ACE2, that is, for cardiovascular disorders or colitis. Compounds binding at alternative sites could allosterically affect the interaction with the spike protein. Herein, we review biochemical, chemical biology, and structural information on ACE2, including the recent cryoEM structures of full-length ACE2. We conclude that ACE2 is very dynamic and that allosteric drugs could be developed to target ACE2. At the time of the 2020 pandemic, we suggest that available ACE2 inhibitors or activators in advanced development should be tested for their ability to allosterically displace the interaction between ACE2 and the spike protein. 相似文献
9.
José M. León Blanco Pedro L. González-R Carmen Martina Arroyo García María José Cózar-Bernal Marcos Calle Suárez David Canca Ortiz 《Drug development and industrial pharmacy》2018,44(1):135-143
This work was aimed at determining the feasibility of artificial neural networks (ANN) by implementing backpropagation algorithms with default settings to generate better predictive models than multiple linear regression (MLR) analysis. The study was hypothesized on timolol-loaded liposomes. As tutorial data for ANN, causal factors were used, which were fed into the computer program. The number of training cycles has been identified in order to optimize the performance of the ANN. The optimization was performed by minimizing the error between the predicted and real response values in the training step. The results showed that training was stopped at 10?000 training cycles with 80% of the pattern values, because at this point the ANN generalizes better. Minimum validation error was achieved at 12 hidden neurons in a single layer. MLR has great prediction ability, with errors between predicted and real values lower than 1% in some of the parameters evaluated. Thus, the performance of this model was compared to that of the MLR using a factorial design. Optimal formulations were identified by minimizing the distance among measured and theoretical parameters, by estimating the prediction errors. Results indicate that the ANN shows much better predictive ability than the MLR model. These findings demonstrate the increased efficiency of the combination of ANN and design of experiments, compared to the conventional MLR modeling techniques. 相似文献
10.
Carolina Blanco Raúl Bodas Sonia Andrés Jose María Rodríguez-Calleja Javier Mateo Fernando Rozada F. Javier Giráldez 《International Journal of Food Science & Technology》2020,55(3):1119-1125
Thirty-two lambs were finished on a total mixed ration (TMR) pelleted alone (00SS) or including sunflower soap stock (SS): 15SS (15 g SS per kg TMR), 30SS (30 g SS per kg TMR) and 60SS (60 g SS per kg TMR). Lambs (8 per group) were slaughtered at 27 kg live weight. Colour evolution, lipid oxidation, microbial growth and detection of diarrhoeagenic Escherichia coli were studied in meat samples. SS in the diet reduced meat lipid oxidation (P < 0.05), but had no significant effect (P > 0.05) on the cholesterol oxidation products. Meat from 60SS and control animals (00SS) revealed greater discoloration (P < 0.05) than 15SS. SS supplementation did not affect the microbiological populations, whereas high doses of SS seemed to increase the proliferation of diarrhoeagenic E. coli on day 14 (P < 0.10). These results suggest that the rate of SS inclusion in the diet of fattening lambs should not be above 15 g SS per kg TMR. 相似文献