Search results for "Mace"

Teksty farmaceutyczne i dyskurs farmaceutyczny : definicje, specyfika i krótki przegląd pola badawczego

2020

This chapter aims to familiarize readers with the specificity of pharmaceutical discourse, including its spoken and written text varieties. I paid particular attention to two issues. Firstly, pharmaceutical discourse and pharmaceutical texts are often classified by researchers into broader category of medical or biomedical discourse. Second, pharmaceutical discourse is not autonomous as it is also permeated with medical, legal, academic and other discourses. Next, pharmaceutical discourse was described in greater detail using descriptive models proposed by Bhatia (2004) and Gunnarson (2009). Finally, a selection of research studies, including linguistic and interdisciplinary ones, conducted…

Thiazole Analogues of the Marine Alkaloid Nortopsentin as Inhibitors of Bacterial Biofilm Formation

2020

Anti-virulence strategy is currently considered a promising approach to overcome the global threat of the antibiotic resistance. Among different bacterial virulence factors, the biofilm formation is recognized as one of the most relevant. Considering the high and growing percentage of multi-drug resistant infections that are biofilm-mediated, new therapeutic agents capable of counteracting the formation of biofilms are urgently required. In this scenario, a new series of 18 thiazole derivatives was efficiently synthesized and evaluated for its ability to inhibit biofilm formation against the Gram-positive bacterial reference strains Staphylococcus aureus ATCC 25923 and S. aureus ATCC 6538 a…

Synthesis and anticancer activity of new thiazole nortopsentin analogues

2015

MODIFICATION OF HYDROPHOBIC SURFACE WITH POLYASPARTAMIDE-BASED POLYCATIONS FOR BIOMEDICAL APPLICATION

2013

A convenient way for the achievement of polymer-based solid materials for specific biomedical applications is grafting the appropriate macromolecules onto the surfaces in order to confer them specific properties. To date many approaches have been used to covalently modify polymeric surfaces, and among them chemoselective coupling reactions, usually referred as “click” reactions, gained much attention thanks to simple procedure with high reaction rate under mild reaction conditions (at normal temperature and pressure) [1]. In particular, radical-initiated thiol-yne “photo-click” chemistry has been demonstrated as an effective way to functionalize efficiently surfaces. This method gives also …

Synthesis, antiproliferative activity, and in silico insights of new 3-benzoylamino-benzo[ b ]thiophene derivatives

2014

A new series of 3-benzoylamino-5-imidazol-5-yl-benzo[b]thiophenes and the parent amino derivatives were synthesized and screened as antitumor agents. All tested compounds showed concentration-dependent antiproliferative activity profile against HeLa cell line, exhibiting GI50 values in the low micromolar range. The most active compounds were tested in cell cycle perturbation experiments. A rapid accumulation of cells in the G2/M phase, with a concomitant reduction of cells in both the S and G0/G1 phases, was observed, suggesting that cell exposure to selected derivatives produces mitotic failure. To rationalize the biological results, the 3-benzoylamino-benzo[b]thiophenes were analyzed thro…

Extracellular Vesicle microRNAs Contribute to the Osteogenic Inhibition of Mesenchymal Stem Cells in Multiple Myeloma

2020

Osteolytic bone disease is the major complication associated with the progression of multiple myeloma (MM). Recently, extracellular vesicles (EVs) have emerged as mediators of MM-associated bone disease by inhibiting the osteogenic differentiation of human mesenchymal stem cells (hMSCs). Here, we investigated a correlation between the EV-mediated osteogenic inhibition and MM vesicle content, focusing on miRNAs. By the use of a MicroRNA Card, we identified a pool of miRNAs, highly expressed in EVs, from MM cell line (MM1.S EVs), expression of which was confirmed in EVs from bone marrow (BM) plasma of patients affected by smoldering myeloma (SMM) and MM. Notably,we found that miR-129-5p, whic…

Le médicament homéopathique dans l'histoire du médicament, Co construction, confrontation, coopération. Histoire, Transmission, Représentation

2007

The dynamics of this thesis resides in the search for the breach between the historical positioning (in relation to scientific fact itself) of homeopathic medication in the history of medical sciences, and the representation made of it in the past and present. By distinguishing what may be at stake, we are led to identify the positioning and impact of the mode of transmitting scientific fact as lacking a historical link to the history of medical sciences, notably medication. Our research hypothesis thus postulates that the transmission mode is at the source of discrepancies in representation. The links between context breakthroughs, such as the role of influences, are just parameters that, …

Synthesis and biological evaluation of the antioxidant properties of new analogues of natural products with piperidine based structure and evaluation…

Dipeptidyl Enoates As Potent Rhodesain Inhibitors That Display a Dual Mode of Action

2015

Dipeptidyl enoates were prepared through a high-yielding two-step synthetic route. They have a dipeptidic structure with a 4-oxoenoate moiety as a warhead with multiple reactive sites. Dipeptidyl enoates were screened against rhodesain and human cathepsins B and L, and were found to be potent and selective inhibitors of rhodesain. Among them (S,E)-ethyl 5-((S)-2-{[(benzyloxy)carbonyl]amino}-3-phenylpropanamido)-7-methyl-4-oxooct-2-enoate (6) was the most potent, with an IC50 value of 16.4 nm and kinact/Ki=1.6×106 m−1 s−1 against rhodesain. These dipeptidyl enoates display a reversible mode of inhibition at very low concentrations and an irreversible mode at higher concentrations. Inhibition…

Cortázar y Macedonio:Humorismo y deconstrucción

2014

Tanto los no-personajes y los no-lugares macedonianos, como los multiformes, cambiantes e indefinidos seres que pueblan las Historias de Cortázar se presentan como burlas metafísicas. El recorrido de deconstrucción y simulación que Macedonio empieza en sus textos parece alcanzar en la obra de Cortázar su ápice: de una escritura anti mimética y de un sistema autorreferencial se pasa a la posibilidad de ver la otra realidad que se esconde más allá de nuestra visión del mundo, el misterio que hace vacilar certezas seculares, el origen primero de la interminable búsqueda humana de la verdad.