Search results for "IPR"
showing 10 items of 1515 documents
TTAS a New Stilbene Derivative that Induces Apoptosis in Leishmania Infantum
2012
Leishmania parasites are able to undergo apoptosis (programmed cell death), similarly to mammalian cells. Recently it was demonstrated in vitro the anti-leishmanial effect of some natural and synthetic stilbenoids including resveratrol and piceatannol. In this study we evaluated the Leishmanicidal activity of a pool of stilbene derivatives which had previously shown high apoptotic efficacy against neoplastic cells. All the compounds tested were capable to decrease the parasite viability in a dose-dependent manner. Trans-stilbenes proved to be markedly more effective than cis-isomers. This was different from that observed in tumor cells in which cis-stilbenes were more potent cytotoxic agent…
Synthesis and antiproliferative activity of thiazolyl-bis-pyrrolo[2,3-b]pyridines and indolyl-thiazolyl-pyrrolo[2,3-c]pyridines, nortopsentin analogu…
2015
Two new series of nortopsentin analogues, in which the imidazole ring of the natural product was replaced by thiazole and indole units were both substituted by 7-azaindole moieties or one indole unit was replaced by a 6-azaindole portion, were efficiently synthesized. Compounds belonging to both series inhibited the growth of HCT-116 colorectal cancer cells at low micromolar concentrations, whereas they did not affect the viability of normal-like intestinal cells. A compound of the former series induced apoptosis, evident as externalization of plasma membrane phosphatidylserine (PS), and changes of mitochondrial trans-membrane potential, while blocking the cell cycle in G2/M phase. In contr…
Role of cyclic nucleotide phosphodiesterase isoenzymes in contractile responses of denuded rat aorta related to various Ca 2+ sources
2001
We have examined the cyclic nucleotide phosphodiesterase isoforms (PDE) involved in the contractile response of rat aorta to different agonists and different experimental procedures for use in functional studies. The inhibitory effect of AAL 05 on the different PDEs isolated from bovine aortic smooth muscle was examined. Compound AAL 05 appeared to be a selective PDE3 inhibitor. We analyzed the ability of the non-selective inhibitor IBMX (3-isobutyl-1-methylxanthine) and the isoenzyme selective inhibitors nimodipine (type 1), AAL 05 (6-(N-methyl-N-cyclohexyl butyl carboxamide) quinolin-2-one) and SKF 94120 (5-(4-acetamidophenyl) pyrazin-2(1H)-one; type3), rolipram (type4) and zaprinast (typ…
Synthesis of novel xanthone and acridone carboxamides with potent antiproliferative activities
2020
Abstract Several new amino-substituted acridone and xanthone derivatives have been designed and synthesized, using an efficient methodology from suitable acridone- or xanthone-carboxylic acid intermediates. The antiproliferative activity of the target compounds has been evaluated against four cancer cell lines, namely breast adenocarcinoma MCF-7, acute lymphocytic leukemia CCRF-CEM, and its doxorubicin-resistant variant CEM/ADR5000 and prostate cancer PC-3 cell lines. Selected derivatives have also been tested against the urinary bladder T24 and metastatic melanoma WM266-4 cancer cell lines. Two nitro substituted acridones, bearing a basic side chain as well, were endowed with a remarkable …
Korpusavusteinen diskurssintutkimus (CADS): analyysiesimerkki homouden ja heterouden digitaalisista diskursseista
2018
The article aims at combining two methodological approaches, namely corpus linguistics and discourse studies. Both of these approaches are present in corpus-assisted discourse studies (CADS) which makes use of both quantitative and qualitative methodologies. First, an attempt is made to discuss the differences and similarities of these two traditions based on Leech’s (2000) listing. However, it turns out that this listing does not include all necessary viewpoints, and those are further discussed. In the empirical section of the paper, the Suomi24 corpus is analysed in order to provide an example of CADS. The analysis was carried out through collocation and discourse prosody analyses. The re…
Reciprocal lower bound on modulus of curve families in metric surfaces
2019
We prove that any metric space $X$ homeomorphic to $\mathbb{R}^2$ with locally finite Hausdorff 2-measure satisfies a reciprocal lower bound on modulus of curve families associated to a quadrilateral. More precisely, let $Q \subset X$ be a topological quadrilateral with boundary edges (in cyclic order) denoted by $\zeta_1, \zeta_2, \zeta_3, \zeta_4$ and let $\Gamma(\zeta_i, \zeta_j; Q)$ denote the family of curves in $Q$ connecting $\zeta_i$ and $\zeta_j$; then $\text{mod} \Gamma(\zeta_1, \zeta_3; Q) \text{mod} \Gamma(\zeta_2, \zeta_4; Q) \geq 1/\kappa$ for $\kappa = 2000^2\cdot (4/\pi)^2$. This answers a question concerning minimal hypotheses under which a metric space admits a quasiconfor…
SURFACE SUBGROUPS OF RIGHT-ANGLED ARTIN GROUPS
2007
We consider the question of which right-angled Artin groups contain closed hyperbolic surface subgroups. It is known that a right-angled Artin group $A(K)$ has such a subgroup if its defining graph $K$ contains an $n$-hole (i.e. an induced cycle of length $n$) with $n\geq 5$. We construct another eight "forbidden" graphs and show that every graph $K$ on $\le 8$ vertices either contains one of our examples, or contains a hole of length $\ge 5$, or has the property that $A(K)$ does not contain hyperbolic closed surface subgroups. We also provide several sufficient conditions for a \RAAG to contain no hyperbolic surface subgroups. We prove that for one of these "forbidden" subgraphs $P_2(6)$, …
Factors associated with first- versus second-generation long-acting antipsychotics prescribed under ordinary clinical practice in Italy
2018
Background For many years, long-acting intramuscular (LAI) antipsychotics have been prescribed predominantly to chronic and severe patients, as a last resort when other treatments failed. Recently, a broader and earlier use of LAIs, particularly second-generation LAIs, has been emphasized. To date, few studies attempted to frame how this change in prescribing took place in real-world practice. Therefore, this study aimed to describe the clinical features of patients prescribed with LAIs, and to explore possible prescribing differences between first- and second-generations LAIs under ordinary clinical practice in Italy. Methods The STAR Network "Depot" Study is an observational, longitudinal…
Usher syndrome: molecular links of pathogenesis, proteins and pathways.
2006
Contains fulltext : 50437.pdf (Publisher’s version ) (Closed access) Usher syndrome is the most common form of deaf-blindness. The syndrome is both clinically and genetically heterogeneous, and to date, eight causative genes have been identified. The proteins encoded by these genes are part of a dynamic protein complex that is present in hair cells of the inner ear and in photoreceptor cells of the retina. The localization of the Usher proteins and the phenotype in animal models indicate that the Usher protein complex is essential in the morphogenesis of the stereocilia bundle in hair cells and in the calycal processes of photoreceptor cells. In addition, the Usher proteins are important in…
Real-time PCR detection of Pseudomonas aeruginosa in clinical and municipal wastewater and genotyping of the ciprofloxacin-resistant isolates
2006
Real-time quantification of Pseudomonas aeruginosa was performed in various wastewater systems including clinical, municipal wastewaters and inflow from a wastewater treatment plant. The highest concentrations of P. aeruginosa-specific targets were detected in clinical wastewaters. Limitations of the detection system resulting from inhibition or cross-reaction were identified. Ciprofloxacin-resistant P. aeruginosa strains were isolated after specific enrichment from clinical and municipal wastewaters. In some cases they were also cultivated from effluent of a wastewater treatment plant, and from its downstream river water. A total of 119 isolates were phenotypically characterized as ciprofl…