scholarly journals (E)-(1-(4-Ethoxycarbonylphenyl)-5-(3,4-dimethoxyphenyl)-3-(3,4-dimethoxystyryl)-2-pyrazoline: Synthesis, Characterization, DNA-Interaction, and Evaluation of Activity Against Drug-Resistant Cell Lines

Molbank ◽  
10.3390/m1114 ◽  
2020 ◽  
Vol 2020 (1) ◽  
pp. M1114
Author(s):  
Matiadis ◽  
Mavroidi ◽  
Panagiotopoulou ◽  
Methenitis ◽  
Pelecanou ◽  
...  

(E)-1-(4-Ethoxycarbonylphenyl)-5-(3,4-dimethoxyphenyl)-3-(3,4-dimethoxystyryl)-2-pyrazoline was synthesized via the cyclization reaction between the monocarbonyl curcuminoid (2E,6E)-2,6-bis(3,4-dimethoxybenzylidene)acetone and ethyl hydrazinobenzoate in high yield and purity (>95% by High-performance liquid chromatography (HPLC)). The compound has been fully characterized by 1H, 13C NMR, FTIR, UV-Vis and HRMS and its activity was evaluated in terms of its potential interaction with DNA as well as its cytotoxicity against resistant and non-resistant tumor cells. Both DNA thermal denaturation and DNA viscosity measurements revealed that a significant intercalation binding takes place upon treatment of the DNA with the synthesized pyrazoline, causing an increase in melting temperature by 3.53 ± 0.11 °C and considerable DNA lengthening and viscosity increase. However, neither re-sensitisation of Doxorubicin (DO X)-resistant breast cancer and multidrug resistance (MDR) reversal nor synergistic activity with DOX by potentially increasing the DOX cell killing ability was observed.


2018 ◽  
Author(s):  
Etienne Becht ◽  
Yannick Simoni ◽  
Elaine Coustan-Smith ◽  
Maximilien Evrard ◽  
Yang Cheng ◽  
...  

AbstractMotivationRecent flow and mass cytometers generate 1,000,000 single cell datasets of dimensions 20 to 40. Many tools facilitate the discovery of new cell populations associated with diseases or physiology. These discoveries require the identification of new gating strategies, but gating strategies become exponentially harder to optimize when dimensionality increases. To facilitate this step we developed Hypergate, an algorithm which given a cell population of interest identifies a gating strategy optimized for high yield and purity.ResultsHypergate achieves higher yield and purity than human experts, Support Vector Machines and Random-Forests on public datasets. We use it to revisit some established gating strategies for the identification of Innate lymphoid cells, which identifies concise and efficient strategies that allow gating these cells with fewer parameters but higher yield and purity than the current standards. For phenotypic description, Hypergate’s outputs are consistent with fields’ knowledge and sparser than those from a competing method.Availability and ImplementationHypergate is implemented in R and available at http://github.com/ebecht/hypergate under an Open Source Initiative-compliant licence.



2012 ◽  
Vol 85 (1) ◽  
pp. 120-131 ◽  
Author(s):  
Md. Najib Alam ◽  
Swapan Kumar Mandal ◽  
Subhas Chandra Debnath

Abstract Several zinc dithiocarbamates (ZDCs) as accelerator derived from safe amine has been exclusively studied in the presence of thiazole-based accelerators to introduce safe dithiocarbamate in the vulcanization of natural rubber. Comparison has been made between conventional unsafe zinc dimethyldithiocarbamate (ZDMC) with safe novel ZDC combined with thizole-based accelerators in the light of mechanical properties. The study reveals that thiuram disulfide and 2-mercaptobenzothiazole (MBT) are always formed from the reaction either between ZDC and dibenzothiazyledisulfide (MBTS) or between ZDC and N-cyclohexyl-2-benzothiazole sulfenamide (CBS). It has been conclusively proved that MBT generated from MBTS or CBS reacts with ZDC and produces tetramethylthiuram disulfide. The observed synergistic activity has been discussed based on the cure and physical data and explained through the results based on high-performance liquid chromatography and a reaction mechanism. Synergistic activity is observed in all binary systems studied. The highest tensile strength is observed in the zinc (N-benzyl piperazino) dithiocarbamate-accelerated system at 3:6 mM ratios. In respect of tensile strength and modulus value, unsafe ZDMC can be successfully replaced by safe ZDCs in combination with thiazole group containing accelerator.



2021 ◽  
Vol 11 (10) ◽  
pp. 4659
Author(s):  
Eun-Jung Kim ◽  
Gyu-Min Im ◽  
Chang-Soo Lee ◽  
Yun-Gon Kim ◽  
Byoung Joon Ko ◽  
...  

The calcium-binding protein S100A9 regulates inflammatory processes and the immune response. It is overexpressed in a variety of inflammatory and oncologic conditions. In this study, we produced a recombinant human S100A9 (hS100A9) antigen with high yield and purity and used it to generate a hybridoma cell culture-based monoclonal anti-hS100A9 antibody. We selected five anti-hS100A9 antibodies from cell supernatants that showed high antigen binding efficiency and identified the nucleotide sequences of three antibodies: two with high effective concentration values and one with the lowest value. The antigen and antibody development procedures described herein are useful for producing large amounts of monoclonal antibodies against hS100A9 and other antigens of interest. The nucleotide sequences of the anti-hS100A9 monoclonal antibody revealed herein will be helpful in the generation of recombinant antibodies or antibody fragments against hS100A9.



2021 ◽  
Vol 7 (10) ◽  
pp. eabe8130
Author(s):  
Shangshang Chen ◽  
Xun Xiao ◽  
Hangyu Gu ◽  
Jinsong Huang

Perovskite-based electronic materials and devices such as perovskite solar cells (PSCs) have notoriously bad reproducibility, which greatly impedes both fundamental understanding of their intrinsic properties and real-world applications. Here, we report that organic iodide perovskite precursors can be oxidized to I2 even for carefully sealed precursor powders or solutions, which markedly deteriorates the performance and reproducibility of PSCs. Adding benzylhydrazine hydrochloride (BHC) as a reductant into degraded precursor solutions can effectively reduce the detrimental I2 back to I−, accompanied by a substantial reduction of I3−-induced charge traps in the films. BHC residuals in perovskite films further stabilize the PSCs under operation conditions. BHC improves the stabilized efficiency of the blade-coated p-i-n structure PSCs to a record value of 23.2% (22.62 ± 0.40% certified by National Renewable Energy Laboratory), and the high-efficiency devices have a very high yield. A stabilized aperture efficiency of 18.2% is also achieved on a 35.8-cm2 mini-module.



2021 ◽  
Vol 12 ◽  
pp. 204173142110086
Author(s):  
Jun Yong Kim ◽  
Won-Kyu Rhim ◽  
Yong-In Yoo ◽  
Da-Seul Kim ◽  
Kyoung-Won Ko ◽  
...  

Exosomes derived from mesenchymal stem cells (MSCs) have been studied as vital components of regenerative medicine. Typically, various isolation methods of exosomes from cell culture medium have been developed to increase the isolation yield of exosomes. Moreover, the exosome-depletion process of serum has been considered to result in clinically active and highly purified exosomes from the cell culture medium. Our aim was to compare isolation methods, ultracentrifuge (UC)-based conventional method, and tangential flow filtration (TFF) system-based method for separation with high yield, and the bioactivity of the exosome according to the purity of MSC-derived exosome was determined by the ratio of Fetal bovine serum (FBS)-derived exosome to MSC-derived exosome depending on exosome depletion processes of FBS. The TFF-based isolation yield of exosome derived from human umbilical cord MSC (UCMSC) increased two orders (92.5 times) compared to UC-based isolation method. Moreover, by optimizing the process of depleting FBS-derived exosome, the purity of UCMSC-derived exosome, evaluated using the expression level of MSC exosome surface marker (CD73), was about 15.6 times enhanced and the concentration of low-density lipoprotein-cholesterol (LDL-c), known as impurities resulting from FBS, proved to be negligibly detected. The wound healing and angiogenic effects of highly purified UCMSC-derived exosomes were improved about 23.1% and 71.4%, respectively, with human coronary artery endothelial cells (HCAEC). It suggests that the defined MSC exosome with high yield and purity could increase regenerative activity.



2021 ◽  
Author(s):  
Benjamin Schmuck ◽  
Gabriele Greco ◽  
Andreas Barth ◽  
Nicola M. Pugno ◽  
Jan Johansson ◽  
...  


1985 ◽  
Vol 148 (1) ◽  
pp. 163-173 ◽  
Author(s):  
Mary C. Byrne ◽  
Michele Sbaschnig-Agler ◽  
Dennis A. Aquino ◽  
Joseph R. Sclafani ◽  
Robert W. Ledeen


2019 ◽  
Vol 8 (11) ◽  
pp. 1995 ◽  
Author(s):  
Moon ◽  
Shin ◽  
Kim ◽  
Lee ◽  
Mankhong ◽  
...  

Exosome-like extracellular vesicles (ELVs) contain biomolecules that have potential as diagnostic biomarkers, such as proteins, micro-RNAs (miRNAs), and lipids. However, it is difficult to enrich ELVs consistently with high yield and purity from clinical samples, which hampers the development of ELV biomarkers. This is particularly true for miRNAs in protein-rich plasma. Hence, we modified ELV isolation protocols of three commercially available polymer-precipitation-based kits using proteinase K (PK) treatment to quantify ELV-associated miRNAs in human plasma. We compared the yield, purity, and characteristics of enriched plasma ELVs, and measured the relative quantity of three selected miRNAs (miR-30c, miR-126, and miR-192) in ELVs using six human plasma samples. Compared with the original protocols, we demonstrated that ELVs can be isolated with PK treatment with high purity (i.e., lack of non-exosomal proteins and homogeneous size of vesicles) and yield (i.e., abundancy of exosomal markers), which were dependent on kits. Using the kit with the highest purity and yield with PK treatment, we successfully quantified ELV miRNAs (levels of 45%–65% in total plasma) with acceptable variability. Collectively, ELV enrichment using the modified easy-to-use method appears suitable for the analysis of miRNAs, although its clinical applicability needs to be confirmed in larger clinical studies.



Author(s):  
Yves Yeboue ◽  
Marion Jean ◽  
Gilles Subra ◽  
Jean Martinez ◽  
Frédéric Lamaty ◽  
...  

Ball-milling enabled to perform [2+1], [2+2], and [2+3] peptide couplings with high yields and, if any, very low epimerization. Very good results were obtained with peptide fragments containing highly epimerization-prone and/or highly hindered amino acids at C-term such as phenylglycine, cysteine and valine. Ball-milling was clearly identified as the key element to obtain both high yield and purity along with low epimerization. Indeed, the ball-milling conditions proved to be superior to the classical solution synthesis approach on a various array of widely used coupling agents. These results open avenues for the development of highly efficient, convergent and flexible peptide synthesis strategies based on peptide fragment couplings mediated by ball-milling.



2020 ◽  
Author(s):  
Yves Yeboue ◽  
Marion Jean ◽  
Gilles Subra ◽  
Jean Martinez ◽  
Frédéric Lamaty ◽  
...  

Ball-milling enabled to perform [2+1], [2+2], and [2+3] peptide couplings with high yields and, if any, very low epimerization. Very good results were obtained with peptide fragments containing highly epimerization-prone and/or highly hindered amino acids at C-term such as phenylglycine, cysteine and valine. Ball-milling was clearly identified as the key element to obtain both high yield and purity along with low epimerization. Indeed, the ball-milling conditions proved to be superior to the classical solution synthesis approach on a various array of widely used coupling agents. These results open avenues for the development of highly efficient, convergent and flexible peptide synthesis strategies based on peptide fragment couplings mediated by ball-milling.



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