Search results for "Mace"
showing 10 items of 4713 documents
Artichoke, Cynarin and Cyanidin Downregulate the Expression of Inducible Nitric Oxide Synthase in Human Coronary Smooth Muscle Cells
2014
Artichoke (Cynara scolymus L.) is one of the world’s oldest medicinal plants with multiple health benefits. We have previously shown that artichoke leaf extracts and artichoke flavonoids upregulate the gene expression of endothelial-type nitric oxide synthase (eNOS) in human endothelial cells. Whereas NO produced by the eNOS is a vasoprotective molecule, NO derived from the inducible iNOS plays a pro-inflammatory role in the vasculature. The present study was aimed to investigate the effects of artichoke on iNOS expression in human coronary artery smooth muscle cells (HCASMC). Incubation of HCASMC with a cytokine mixture led to an induction of iNOS mRNA expression. This iNOS induction was c…
Enhancement of premature stop codon readthrough in the CFTR gene by Ataluren (PTC124) derivatives.
2015
Abstract Premature stop codons are the result of nonsense mutations occurring within the coding sequence of a gene. These mutations lead to the synthesis of a truncated protein and are responsible for several genetic diseases. A potential pharmacological approach to treat these diseases is to promote the translational readthrough of premature stop codons by small molecules aiming to restore the full-length protein. The compound PTC124 (Ataluren) was reported to promote the readthrough of the premature UGA stop codon, although its activity was questioned. The potential interaction of PTC124 with mutated mRNA was recently suggested by molecular dynamics (MD) studies highlighting the importanc…
Inhalable nano into micro dry powders for ivacaftor delivery: The role of mannitol and cysteamine as mucus-active agents.
2020
In this paper the innovative approach of Nano into micro (NiM9 was developed to produce Nanoparticles loaded Ivacaftor to incorporate into mannitol or mannitol/cysteamine micromatrices for drug pulmonary administration in CF. Nanoparticles composed by a mixture of two polyhydrohydroxyethtylaspartamide copolymers containing a loading of Ivacaftor of 15.5 % w/w were produced. These Nanoparticles were incorporated into microparticles to obtain NiM that were characterized in terms of size and size distribution, interaction with CF-AM by rheological and turbidimetric studies as well as by aerodynamic diameter measurements. Finally the activity of Ivacaftor into these NiM was evaluated by in vitr…
HETEROCYCLIC COMPOUNDS AND MEDICAL USE THEREOF
2019
The present invention relates to heterocyclic nitrogen compounds, use thereof as a medicament and pharmaceutical compositions thereof. Furthermore, the invention provides combinations of compounds of general formula (I) with therapeutic agents, such as correctors, potentiators and amplifiers of dysfunctional proteins.
Isoenzyme-specific phosphorylation of cytochromes P-450 and other drug metabolizing enzymes.
1987
Abstract A series of fourteen cytochrome P-450 isoenzymes was treated with three different protein kinases and found to devide into isoenzymes phosphorylated (i) by both the cyclic AMP-dependent kinase and the calcium-phospholipid-dependent kinase (P-450 PB 3a and PB 2e), (ii) by none of these kinases (P-450 PB 1b, MC 1b, UT 1, and thromboxane synthase), and (iii) by either the cyclic AMP-dependent kinase (P-450 LM 2, PB 2d, and PB 3b) or the calcium-phospholipid-dependent kinase (P-450 PB 1a, PB 2a, MC 1a, LM 3c, and LM 4). Other components of the monooxygenase system, cytochrome P-450 reductase, cytochrome b5, cytochrome b5 reductase as well as microsomal epoxide hydrolase, were poor subs…
Contribution of Molecular Structure to Self-Assembling and Biological Properties of Bifunctional Lipid-Like 4-(N-Alkylpyridinium)-1,4-Dihydropyridines
2019
The design of nanoparticle delivery materials possessing biological activities is an attractive strategy for the development of various therapies. In this study, 11 cationic amphiphilic 4-(N-alkylpyridinium)-1,4-dihydropyridine (1,4-DHP) derivatives differing in alkyl chain length and propargyl moiety/ties number and position were selected for the study of their self-assembling properties, evaluation of their cytotoxicity in vitro and toxicity on microorganisms, and the characterisation of their interaction with phospholipids. These lipid-like 1,4-DHPs have been earlier proposed as promising nanocarriers for DNA delivery. We have revealed that the mean diameter of freshly prepared nanoparti…
Chińska aktywność na Bałkanach w XXI wieku i jej implikacje
2022
Celem artykułu jest szkicowe przedstawienie, na podstawie analiz i materiałów prasowych, wielosektorowej obecności Chin na Bałkanach i jej wpływu na sytuację ekonomiczną regionu. Bałkany są ważne dla mocarstw ze względu na położenie geopolityczne i geostrategiczne na skrzyżowaniu szlaków międzykontynentalnych. Chiny znacząco wpływają na ekonomikę poszczególnych państw region, wykorzystując dyplomację publiczną celem ograniczenia wpływów ze strony innych ważnych graczy: Unii Europejskiej, Rosji i USA. Autorka przedstawia hipotezę, że Chiny, tak jak USA pod koniec XX wieku, zmierzają do stworzenia sfery wpływów na Półwyspie Bałkańskim, w kontekście swoich interesów globalnych. Bałkany są post…
An Open Innovation Decision Support System to Select a Biopharmaceutical R&D Portfolio
2016
Drugs available in the market today, selected several years ago under very uncertain future scenario, have experienced a long and expensive process of research and development carried out following both a closed and an open innovation path. To support this critical selection process, we propose a Decision Support System, able to choose among different candidates the most promising drugs along their best development path. The Decision Support System, based on a real options portfolio optimization model, mapping tools, and what-if rules as well, has been applied to a numerical example available in literature, and the research findings show interesting managerial and academic implications
Coordinated induction of drug transporters and phase I and II metabolism in human liver slices
2008
Although regulation of phase I drug metabolism in human liver is relatively well studied, the regulation of phase II enzymes and of drug transporters is incompletely characterized. Therefore, we used human liver slices to investigate the PXR, CAR and AhR-mediated induction of drug transporters and phase I and II metabolic enzymes. Precision-cut human liver slices were incubated for 5 or 24 h with prototypical inducers: phenobarbital (PB) (50 mu M) for CAR, beta-naphthoflavone (BNF) (25 mu M) for AhR, and rifampicin (RIF) (10 mu M) for PXR, and gene expression of the phase I enzymes CYP1A1, 1A2, 3A4, 3A5, 2136, 2A6, the phase II enzymes UGT1A1 and 1A6, and the transporters MRP2, MDR1, BSEP, …
Paraugu sagatavošanas metodes optimizācija farmaceitisko savienojumu noteikšanai notekūdens paraugos
2021
Paraugu sagatavošanas metodes optimizācija farmaceitisko savienojumu noteikšanai notekūdens paraugos. Šukajeva V., zinātniskā vadītāja Mag. ķīm. Ikkere L.E. Bakalaura darbs, 59 lpp., 11 attēli, 16 tabulas, 37 literatūras avoti, 1 pielikums. Latviešu valodā. Bakalaura darba ietvaros tika veikta literatūras avotu izpēte par uz notekūdeņiem balstītu epidemioloģiju, Latvijā izplātītākiem farmaceitiski aktīviem savienojumiem, populācijas biomarķieriem un farmaceitisko savienojumu noteikšanas tendencēm ūdens matricās. Klasiskā SPE metode tika optimizēta 56 farmaceitiski aktīvo savienojumu noteikšanai notekūdens paraugos. SPE metodes optimizēšanai tika salīdzinātās Oasis® HLB un dažādas Strata™ ko…