Search results for "In vitro"

Nanoincorporation of curcumin in polymer-glycerosomes and evaluation of their in vitro–in vivo suitability as pulmonary delivery systems

2015

The aim of this work was to deliver curcumin into the lungs by incorporating it into innovative vesicles obtained using phospholipids and high concentrations of glycerol (50%, v/v), so called glycerosomes, which were then combined with two polymers: sodium hyaluronate and trimethyl chitosan to form polymer-glycerosomes. These systems were prepared without the use of organic solvents or acidic solutions and their physico-chemical properties were fully characterized. Cryogenic transmission electron microscopy and small-angle X-ray scattering showed that both glycerosomes and polymer-glycerosomes were spherical, mainly unilamellar and of nanometric size (65–112 nm). The vesicles were readily n…

The combination of PDE4 and PDE5 inhibitors reduces YAP expression in IPF

2017

Background: Pathological fibrosis is associated with repeated episodes of injury to alveolar epithelial cells of largely. Yes-associated protein (YAP) is prominently expressed in fibrotic lung. Roflumilast has demonstrated to exhibit anti-fibrosis effects, while PDE5 inhibitors (sildenafil) combinated with PDE4 inhibitors reduce fibrotic-effects secondary to TGFs1. Apparently, no studies of PDE4 and PDE5 inhibitors on YAP expression there are. Objectives: To study the effects from adding a sildenafil to Roflumilast N- oxide (RNO) on TGF-β/SMAD3/YAP pathway in IPF in vitro models. Methods: A549 cells were pre-incubated with therapeutical concentrations of RNO (2nM) and/or sildenafil (10nM) a…

In vitro and in silico studies of polycondensed diazine systems as anti-infective agents

2011

Infective diseases caused by protozoarian agents are still relevant today more than ever. In fact, they represent the first cause of death all over the world with seventeen millions victims every year. The development of drug resistance and the broad diffusion of these pathologies make actual the research of new molecules able to act as selective and effective anti-infective chemotherapics.[1] Recently several polycondensed diazine derivatives, by means 1,3-dipolar cycloaddition, reactions [2, 3] were synthesized. A broad selection of these compounds chosen with a wide pattern of substitutions were submitted to biological in vitro screening against Plasmodium falciparum, Leishmania Infantum…

Selective downregulation of the MDR1 gene product in Caco-2 cells by stable transfection to prove its relevance in secretory drug transport.

2005

Considerable interest is focused on overcoming multidrug resistance (MDR) in cancer chemotherapy. The in vitro experiments to characterize P-glycoprotein's (P-gp) function and to decrease its effects have led to a variety of strategies such as addition of competitors or supplementation of the medium with oligonucleotides complementary to the 5'-end of the MDR1-mRNA. For the Caco-2 cell line, an in vitro model for absorption screening, expressing multiple transporters including P-gp, which pumps substances back into the apical solution, P-gp activity might mask other relevant transport proteins' activity. The objective of the present study was to construct a Caco-2 subline with reduced P-gp …

Seed mass variation and in vitro embryos culture of Abies nebrodensis (Lojac.) Mattei

2009

Not So Much Societal: The Catholic Church in Poland as a Veto Player

2021

George Tsebelis distinguished two forms of veto players’ actions: institutional and partisan. In a democracy, the Church is not able to play either role because it is not an element of the state’s institutional structure. This was the source for Simon Fink’s proposal to look at the Church as a societal veto player (VP). The case of Poland shows, however, that such an approach becomes inadequate in numerous situations. The Church’s influence on political parties, and particularly the state’s institutions, may be exerted outside society. Performed on the basis of the existing literature and political debates conducted since 1989, the analysis of the social and political reality of Poland all…

Bioaccessibility of calcium, iron and zinc from three legume samples

2004

Legumes can be a source of mineral elements but also of antinutritional factors which can affect their absorption. An in vitro method including gastrointestinal digestion was used to estimate mineral bioavailability. Soluble (bioaccessible) and insoluble calcium, iron and zinc from white beans, chickpeas and lentils were determined after gastrointestinal digestion. The influence of the original sample weight on the soluble mineral fraction was also estimated. The results obtained show that white beans are the legumes with the highest bioaccessible calcium and iron contents. Lentils have a high iron content but its bioaccessibility is much lower than that of iron from white beans and chickpe…

Influence of gamma-aminobutyric acid on baclofen intestinal absorption.

1994

Since previous studies suggested that baclofen absorption in the rat middle intestine was inhibited by beta-alanine and therefore mediated, at least in part, by the beta-aminoacid carrier, we focused our new studies on the analysis of the possible inhibition of the drug by a gamma-aminoacid model compound, gamma-aminobutyric acid (GABA). A rat jejunum in situ study was undertaken in order to evaluate the effect of GABA on baclofen absorption and to establish the inhibition model. Assays using isotonic perfusion solutions of 0.5 mM baclofen with starting GABA concentrations ranging from 0 to 100 mM are reported. The results show that the absorption rate pseudoconstants of the drug decrease a…

Synthesis of polymeric derivatives of isoniazid: characterization and in vitro release from a water-soluble adduct with polysuccinimide.

1989

Coupling of isoniazid with polysuccinimide afforded a water-insoluble polymeric pro-drug; by reaction with ethanolamine it was chemically transformed in a water-soluble adduct. The in vitro release of isoniazid from the drug-polymer adduct was studied by using an artificial stomach wall lipid membrane. The transfer rate constant from simulated gastric juice to simulated plasma was defined and compared with that of an equivalent dose of pure drug.

Dual targeting of higher-order DNA structures by azacryptands induces DNA junction-mediated DNA damage in cancer cells

2021

Abstract DNA is intrinsically dynamic and folds transiently into alternative higher-order structures such as G-quadruplexes (G4s) and three-way DNA junctions (TWJs). G4s and TWJs can be stabilised by small molecules (ligands) that have high chemotherapeutic potential, either as standalone DNA damaging agents or combined in synthetic lethality strategies. While previous approaches have claimed to use ligands that specifically target either G4s or TWJs, we report here on a new approach in which ligands targeting both TWJs and G4s in vitro demonstrate cellular effects distinct from that of G4 ligands, and attributable to TWJ targeting. The DNA binding modes of these new, dual TWJ-/G4-ligands w…