synthetic inhibitor
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2021 ◽  
Author(s):  
Ana Popovici ◽  
◽  
Valentina Svetlicenco ◽  
Nicolae Bujoreanu ◽  
◽  
...  

The plum fruits of the President variety were preserved by three methods. I- keeping fruits in the ordinary atmosphere (AO). II - the fruits before being stored for a long time in AO were treated with the synthetic inhibitor of ethylene Fitomag and III - the fruits were kept in a controlled atmosphere (CA). Du-ring the storage of the fruits of the respective variety, the activity of some antioxidant enzymes was de-termined by the mentioned methods. As a result, results were obtained regarding the modification of the activity of the enzymes peroxidase and polyphenol oxidase. Their activity changed depending on the me-tabolic processes that took place when the fruits maturation, as well as the conditions, duration and stora-ge methods. It also depended on the biological peculiarities of the variety and the influence of the sub-stances with which the plum trees were treated during the vegetation period. The highest activity of these enzymes was in the fruits kept in the usual atmosphere, then followed by their activity in the fruits kept with Fitomag and their lowest activity was in the fruits kept in CA. In the fruits preserved by the last two methods, the metabolic processes and those of oxide reduction went slower and the fruits were kept 10, 16 days longer than in AO. There were also significant differences in the activity of these enzymes, being higher in the variant treated with SBA Reglalg and microelements than in the control variant.


Plants ◽  
2021 ◽  
Vol 10 (7) ◽  
pp. 1311
Author(s):  
Magdalena Chmur ◽  
Andrzej Bajguz

Brassinolide (BL) represents brassinosteroids (BRs)—a group of phytohormones that are essential for plant growth and development. Brassinazole (Brz) is as a synthetic inhibitor of BRs’ biosynthesis. In the present study, the responses of Wolffia arrhiza to the treatment with BL, Brz, and the combination of BL with Brz were analyzed. The analysis of BRs and Brz was performed using LC-MS/MS. The photosynthetic pigments (chlorophylls, carotenes, and xanthophylls) levels were determined using HPLC, but protein and monosaccharides level using spectrophotometric methods. The obtained results indicated that BL and Brz influence W. arrhiza cultures in a concentration-dependent manner. The most stimulatory effects on the growth, level of BRs (BL, 24-epibrassinolide, 28-homobrassinolide, 28-norbrassinolide, catasterone, castasterone, 24-epicastasterone, typhasterol, and 6-deoxytyphasterol), and the content of pigments, protein, and monosaccharides, were observed in plants treated with 0.1 µM BL. Whereas the application of 1 µM and 10 µM Brz caused a significant decrease in duckweed weight and level of targeted compounds. Application of BL caused the mitigation of the Brz inhibitory effect and enhanced the BR level in duckweed treated with Brz. The level of BRs was reported for the first time in duckweed treated with BL and/or Brz.


2021 ◽  
Vol 12 ◽  
Author(s):  
Emily Hams ◽  
Joseph Roberts ◽  
Rachel Bermingham ◽  
Padraic G. Fallon

The transcription factor Related Orphan Receptor Alpha (RORα) plays an important role in regulating circadian rhythm, inflammation, metabolism and cellular development. Herein we show that in the absence of functional RORα in mice there is reduced susceptibility to LPS-induced endotoxic shock, with selective decreases in release of pro-inflammatory cytokines. Treatment of mice with a RORα selective synthetic inhibitor also reduced the severity of LPS-induced endotoxemia. The reduction in responses in Rora deficient mice was associated with an alterations in metabolic and pro-inflammatory functions of macrophages, both in vivo peritoneal macrophages and in vitro generated bone marrow derived macrophages. Using LysMCreRorafl/sg mice the reduced susceptibility to LPS was shown to be specific to Rora expression in the macrophages. This study identifies that Rora-mediated regulation of macrophages impacts on the pro-inflammatory responses elicited by LPS.


2021 ◽  
Vol 65 (1) ◽  
Author(s):  
Genaro Bolívar ◽  
Marinela Colina ◽  
Blas Delgado ◽  
Eduardo Mendizabal

Abstract. When oil production by natural flow of reservoirs decreases, it is necessary to increase the production by using improved recovery processes, such as water injection. Injection of incompatible water can cause the formation of saline deposits of calcium and magnesium carbonates. The use of chemical inhibitors to treat incrustations involves the use of chemicals with functional groups such as carboxylic acids (R-COOH) or phosphonates (R-PO32-). A new ecological scale inhibitor, carboxymethyl chitosan (CMC1), has been synthesized and its capacity to modify the CaCO3 crystalline phases obtained in the solid residue was compared with that obtained when using a commercial carboxymethyl chitosan (CMC2) and a commercial poly(acrylic acid). The results show that under the used conditions, the CMC´s produce a slightly larger amount of crystalline phases than the synthetic inhibitor. Using the X-ray powder diffraction technique, calcite, vaterite, and aragonite were identified in the residual solid. The ratio of these phases was modified by increasing the concentration of the inhibitor. Using Scanning Electron Microscopy (SEM), it was observed that increasing the concentration of the CMC's the modifies the crystal´s morphology from plates to spheres.   Resumen. Cuando la producción de petróleo por flujo natural disminuye, es necesario aumentar la producción de petróleo crudo y gas mediante procesos de recuperación mejorados. El agua es el líquido que se inyecta y puede provocar la formación de depósitos salinos de carbonato de calcio y magnesio. El uso de inhibidores químicos para el tratamiento de incrustaciones implica el empleo de productos químicos con grupos funcionales del tipo ácido carboxílico (R-COOH) o grupos fosfonatos (R-PO32-). Se sintetizó un nuevo inhibidor de incrustaciones ambientalmente amigable en base a carboximetilquitosano (CMC1), y se compararon las fases cristalinas de CaCO3 obtenidas en el residuo sólido con las obtenidas al utilizar un carboximetilquitosano comercial (CMC2) y un poli (ácido acrílico) comercial. Los resultados muestran que, en las condiciones utilizadas, las CMC producen una cantidad ligeramente mayor de fases cristalinas en comparación con el inhibidor sintético. Mediante la técnica de difracción de rayos X de polvos, en el sólido residual se identificaron las fases: Calcita, Vaterita y Aragonita. La relación de las fases se modificó aumentando la concentración del inhibidor. Mediante Microscopía Electrónica de Barrido (SEM) de los residuos sólidos, se observó que al aumentar la concentración de las CMC's la morfología de los cristales se modificaba de placas a esferas.


2020 ◽  
Vol 2020 ◽  
pp. 1-14
Author(s):  
Andres F. Yepes-Pérez ◽  
Oscar Herrera-Calderon ◽  
José-Emilio Sánchez-Aparicio ◽  
Laura Tiessler-Sala ◽  
Jean-Didier Maréchal ◽  
...  

COVID-19 is a disease caused by severe acute respiratory syndrome coronavirus 2. Presently, there is no effective treatment for COVID-19. As part of the worldwide efforts to find efficient therapies and preventions, it has been reported the crystalline structure of the SARS-CoV-2 main protease Mpro (also called 3CLpro) bound to a synthetic inhibitor, which represents a major druggable target. The druggability of Mpro could be used for discovering drugs to treat COVID-19. A multilevel computational study was carried out to evaluate the potential antiviral properties of the components of the medicinal herb Uncaria tomentosa (Cat’s claw), focusing on the inhibition of Mpro. The in silico approach starts with protein-ligand docking of 26 Cat’s claw key components, followed by ligand pathway calculations, molecular dynamics simulations, and MM-GBSA calculation of the free energy of binding for the best docked candidates. The structural bioinformatics approaches led to identification of three bioactive compounds of Uncaria tomentosa (speciophylline, cadambine, and proanthocyanidin B2) with potential therapeutic effects by strong interaction with 3CLpro. Additionally, in silico drug-likeness indices for these components were calculated and showed good predicted therapeutic profiles of these phytochemicals. Our findings suggest the potential effectiveness of Cat’s claw as complementary and/or alternative medicine for COVID-19 treatment.


2020 ◽  
Author(s):  
Ana Popovici ◽  
◽  
Nicolae Bujoreanu ◽  
Valentina Svetlicenco ◽  
◽  
...  

When storaging the plum fruits of the varieties Stenley under normal atmospheric conditions and by the method of treating them with the synthetic inhibitor of ethylene Fitomag, the modification of peroxidase and polyphenol oxidase activity in fruits depended on the conditions and duration of storage, metabolic processes course in fruit during storage, the particularities of the varieties and their storage methods. The gradual decrease in peroxidase activity and the increase in polyphenol oxidase activity occurred in the case of fruit preservation by both methods. In the fruits storaged by the Fitomag method, the values of these enzymes were lower compared to those in the ordinary atmosphere. The lower intensity of the redox processes has beneficially influenced the preservation of the quality of the fruits preserved by this method compared to the usual atmosphere. There were also essential differences between the control and the variants treated with SBA Reglalg and microelements, as well as between varieties.


2020 ◽  
Vol 11 (3) ◽  
pp. 370-377
Author(s):  
Govindan Subramanian ◽  
Rajendran Vairagoundar ◽  
Scott J. Bowen ◽  
Nicole Roush ◽  
Theresa Zachary ◽  
...  

New hTrkA kinase domain type 2 inhibitors and mixed type 1/type 2 inhibitor leads disclosed here offers a differential starting point to investigate the disease pathophysiology.


2019 ◽  
Vol 9 (1) ◽  
Author(s):  
Soumyo Sen ◽  
Lela Vuković ◽  
Petr Král

AbstractBlocking the formation, growth, and breaking of amyloid fibrils by synthetic nanosystems could provide a treatment of neurodegenerative diseases. With this in mind, here atomistic molecular dynamics simulations are used to screen for nanoparticles (NPs), covered with different mixtures of ligands, including positively and negatively charged ligands, Aβ40-cut-peptide, and synthetic inhibitor ligands, in their selective coupling to Aβ40 peptides and their fibrils. The simulations reveal that only Aβ40-cut-peptide-covered NPs have strong and selective coupling to Aβ40 monomers. On the other hand, positive, positive-neutral, Janus, and peptide NPs couple to the beta sheet surfaces of Aβ40 fibrils and only the negative-neutral NPs couple to the fibril tips.


2019 ◽  
Vol 34 (1) ◽  
pp. 1711-1715 ◽  
Author(s):  
Gabriella Caminati ◽  
Maria Raffaella Martina ◽  
Stefano Menichetti ◽  
Piero Procacci
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