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51.
Myriam Gonzlez María Ovejero-Snchez Alba Vicente-Blzquez Raquel lvarez Ana B. Herrero Manuel Medarde Rogelio Gonzlez-Sarmiento Rafael Pelez 《International journal of molecular sciences》2021,22(4)
Pan-Gyn cancers entail 1 in 5 cancer cases worldwide, breast cancer being the most commonly diagnosed and responsible for most cancer deaths in women. The high incidence and mortality of these malignancies, together with the handicaps of taxanes—first-line treatments—turn the development of alternative therapeutics into an urgency. Taxanes exhibit low water solubility that require formulations that involve side effects. These drugs are often associated with dose-limiting toxicities and with the appearance of multi-drug resistance (MDR). Here, we propose targeting tubulin with compounds directed to the colchicine site, as their smaller size offer pharmacokinetic advantages and make them less prone to MDR efflux. We have prepared 52 new Microtubule Destabilizing Sulfonamides (MDS) that mostly avoid MDR-mediated resistance and with improved aqueous solubility. The most potent compounds, N-methyl-N-(3,4,5-trimethoxyphenyl-4-methylaminobenzenesulfonamide 38, N-methyl-N-(3,4,5-trimethoxyphenyl-4-methoxy-3-aminobenzenesulfonamide 42, and N-benzyl-N-(3,4,5-trimethoxyphenyl-4-methoxy-3-aminobenzenesulfonamide 45 show nanomolar antiproliferative potencies against ovarian, breast, and cervix carcinoma cells, similar or even better than paclitaxel. Compounds behave as tubulin-binding agents, causing an evident disruption of the microtubule network, in vitro Tubulin Polymerization Inhibition (TPI), and mitotic catastrophe followed by apoptosis. Our results suggest that these novel MDS may be promising alternatives to taxane-based chemotherapy in chemoresistant Pan-Gyn cancers. 相似文献
52.
53.
Daniela Frasca Maria Romero Alain Diaz Denisse Garcia Seth Thaller Bonnie B. Blomberg 《International journal of molecular sciences》2021,22(4)
Senescent cells accumulate in the adipose tissue (AT) of individuals with obesity and secrete multiple factors that constitute the senescence-associated secretory phenotype (SASP). This paper aimed at the identification of B cells with a SASP phenotype in the AT, as compared to the peripheral blood, of individuals with obesity. Our results show increased expression of SASP markers in AT versus blood B cells, a phenotype associated with a hyper-metabolic profile necessary to support the increased immune activation of AT-derived B cells as compared to blood-derived B cells. This hyper-metabolic profile is needed for the secretion of the pro-inflammatory mediators (cytokines, chemokines, micro-RNAs) that fuel local and systemic inflammation. 相似文献
54.
Lorena Rodríguez-López Myriam Rincón-Fontán Xanel Vecino Ana B. Moldes Jose M. Cruz 《Journal of surfactants and detergents》2020,23(1):79-90
Over the last few years, the global biosurfactant market has raised due to the increasing awareness among consumers, for the use of biological or bio-based products. Because of their composition, it can be speculated that these are more biocompatible and more biodegradable than their chemical homologous. However, at the moment, no studies exist in the literature about the biodegradability of biosurfactants. In this work, a biosurfactant contained in a crude extract, obtained from a corn wet-milling industry stream that ferments spontaneously in the presence of lactic acid bacteria, was subjected to a biodegradation study, without addition of external microbial biomass, under different conditions of temperature (5–45 °C), biodegradation time (15–55 days), and pH (5–7). For that, a Box–Behnken factorial design was applied, which allowed to predict the percentage of biodegradation for the biosurfactant contained in the crude extract, between the range of the independent variables selected in the study, obtaining biodegradation values between 3 and 80%. The percentage of biodegradation for the biosurfactant was calculated based on the increase in the surface tension of samples of the crude extract. Furthermore, it was also possible to predict the variation in t1/2 for the biosurfactant (time to achieve the 50% of biodegradation) under different conditions. 相似文献
55.
The separation of iron oxide from banded hematite jasper(BHJ) assaying 47.8% Fe, 25.6% Si O2 and 2.30%Al2O3 using selective magnetic coating was studied. Characterization studies of the low grade ore indicate that besides hematite and goethite,jasper, a microcrystalline form of quartzite, is the major impurity associated with this ore. Beneficiation by conventional magnetic separation technique could yield a magnetic concentrate containing 60.8% Fe with 51% Fe recovery. In order to enhance the recovery of the iron oxide minerals, fine magnetite, colloidal magnetite and oleate colloidal magnetite were used as the coating material. When subjected to magnetic separation, the coated ore produces an iron concentrate containing 60.2% Fe with an enhanced recovery of56%. The AFM studies indicate that the coagulation of hematite particles with the oleate colloidal magnetite facilitates the higher recovery of iron particles from the low grade BHJ iron ore under appropriate conditions. 相似文献
56.
P.Y. Raval P.R. Pansara A.R. Makadiya N.H. Vasoya S.N. Dolia K.B. Modi 《Ceramics International》2018,44(15):17667-17674
The consequences of high energy mechanical milling, microwave-assisted heating and rapid thermal cooling on magnetic ordering in polycrystalline CaCu3Ti4O12 cubic perovskite have been investigated by means of X-ray powder diffractometry (300?K), dc magnetization in field – cooled and zero – field cooled modes (H = 100?Oe and 1000?Oe, T?=?5–300?K) (M – T curves) and M – H loop characteristics (T?=?5?K and 300?K, Hmax = 70?kOe). The M – T curves of unmilled and 16?h milled samples show pure antiferromagnetic and weak ferromagnetic ordering, respectively, 1?h and 6?h milled samples demonstrate the coexistence of both the phases while microwave-assisted and quenched samples exhibit classic antiferromagnetic transition and a low temperature paramagnetic–like contribution with different weights, well supported by the M – H loop characteristics. The observed transformations in the magnetic ordering are attributed to the ball-milling induced stress which curtails hybridization of empty Ti-3d orbitals with Cu-3d and O-2p orbitals and secondary phase formation. Oxygen vacancies associated with bound magnetic polarons originate ferromagnetism in the milled samples while unpaired electrons inhabited at the empty sites are the cause of paramagnetic centers. The low-temperature Curie – tail in M – T curve for quenched and microwave assisted samples is attributed to Ti3+ cations. 相似文献
57.
Lecture capture with real‐time rearrangement of visual elements: impact on student performance
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The primary goal of this study is to create and test a lecture‐capture system that can rearrange visual elements while recording is still taking place, in such a way that student performance can be positively influenced. The system we have devised is capable of integrating and rearranging multimedia sources, including learning content, the instructor and students' images, into lecture videos that are embedded in a website for students to review after school. The present study employed a two‐group experimental design, with 153 participants (145 females and 8 males) making up an experimental group in which lecture courses were recorded using the new lecture‐capture system, and 149 participants (140 females and 9 males) forming a control group whose lectures were recorded by traditional means. All participants were in the freshman college and studying Introduction to Computer and Information Science in one of six classes, and were randomly assigned to one of the two groups. The participants' midterm examination and final examination scores were collected as indicators of their academic performance, with their mathematics entrance scores used as a pre‐test. The findings obtained from analysis of covariance (ANCOVA) suggest that appropriate rearrangement of visual elements in lecture videos can significantly impact students' learning performance. 相似文献
58.
Abiodun B. Ogbesejana Zhong Ningning Oluwadayo O. Sonibare 《Petroleum Science and Technology》2019,37(18):1969-1977
The occurrence and distributions of dibenzofurans (DBFs) and benzo[b]naphthofurans were investigated in crude oils from Niger Delta, Nigeria, by gas chromatography-mass spectrometry-mass spectrometry. The distribution of DBFs was characterized by the predominance of C2-dibenzofurans. 4-Methyldibenzofuran was the most abundant among the methyldibenzofurans isomers while dimethyldibenzofuran-2 (DMDBF-2), ethyldibenzofuran-1, DMDBF-3, and DMDBF-6 occurred in higher amounts when compared with other DMDBFs. Among the benzonaphthofurans, the abundance of benzo[b]naphtho[2,1-d]furan was higher than other isomers. The DBFs distributions in the oils were not affected by source facies and depositional environments. However, the DBFs concentrations increased with increasing maturity in oils from ADL and MJO oilfields. 相似文献
59.
60.
László Lőrincz Máté Zsemberi György Bánsághi Tamás Sohajda Edit Székely 《化学工程与技术》2018,41(7):1466-1472
Chiral molecules, especially enantiomers and diastereomers of purity > 99 %, present a significant market share within the chemical, pharmaceutical, and flavor industries. Antisolvent precipitations, both batch and semicontinuous operations to serve the current trends in flow chemistry were demonstrated to be environmentally benign and efficient tools in achieving high optical purities. Although salts are known to be insoluble in supercritical CO2, instabilities of the nascent salts were detected and applied for increasing efficiency. Diastereomeric excess values of the crystalline products exceeded 99 % in maximum of three consecutive steps both by repeated resolution with half molar equivalent of the amine to the acid and by direct recrystallization of the salts. 相似文献