Search results for " DERIVATIVES"
showing 10 items of 391 documents
ChemInform Abstract: Synthesis and anti-Staphylococcal Activity of New Halogenated Pyrroles Related to Pyrrolomycins F.
2008
The chemical synthesis of new halogenated pyrroles related to pyrrolomycins F is described and the anti-staphylococcal activity compared. The replacement of 4′-bromo atom of parent compounds with two chloro atoms at 3′ and 5′ position increase the antibacterial activity against a reference strain of S. aureus.
Temperature effects explain continental scale distribution of cyanobacterial toxins
2018
Insight into how environmental change determines the production and distribution of cyanobacterial toxins is necessary for risk assessment. Management guidelines currently focus on hepatotoxins (microcystins). Increasing attention is given to other classes, such as neurotoxins (e.g., anatoxin-a) and cytotoxins (e.g., cylindrospermopsin) due to their potency. Most studies examine the relationship between individual toxin variants and environmental factors, such as nutrients, temperature and light. In summer 2015, we collected samples across Europe to investigate the effect of nutrient and temperature gradients on the variability of toxin production at a continental scale. Direct and indirect…
Osmolality of various viscoelastic substances: comparative study.
2000
Abstract Purpose To determine the osmolality of various viscoelastic substances. Setting Department of Ophthalmology, Johannes Gutenberg-University, Mainz, and Institute for Medical Device Testing, Memmingen, Germany. Methods The analysis was carried out according to the European Pharmacopoeia by means of a calibrated osmometer using the freezing-point depression method. Each syringe was analyzed as a duplicate analysis. Results Mean osmolalities (mOsmol/kg) of the sodium hyaluronate viscoelastic substances were Allervisc® 299; Allervisc® Plus 307; Amvisc® Plus 335; AMO Vitrax® 284; Biolon® 279; Dispasan® 311; Dispasan® Plus 314; Healon® 295; Healon GV® 312; Healon®5 322; HYA-Ophtal® 376; M…
Acetylcholine mediates the release of IL-8 in human bronchial epithelial cells by a NFkB/ERK-dependent mechanism
2007
Acetylcholine may play a role in cell activation and airway inflammation. We evaluated the levels of both mRNA and protein of muscarinic M(1), M(2), M(3) receptors in human bronchial epithelial cell line (16HBE). 16HBE cells were also stimulated with acetylcholine and extracellular signal-regulated kinase1/2 (ERK1/2) and NFkB pathway activation as well as the IL-8 release was assessed in the presence or absence of the inhibitor of Protein-kinase (PKC) (GF109203X), of the inhibitor of mitogenic activated protein-kinase kinase (MAPKK) (PDO9805), of the inhibitor of kinaseB-alpha phosphorilation (pIkBalpha) (BAY11-7082), and of muscarinic receptor antagonists tiotropium bromide, 4-Diphenylacet…
Nanocapsules generated out of a polymeric dexamethasone shell suppress the inflammatory response of liver macrophages.
2012
Abstract Dexamethasone (DXM) is a synthetic glucocorticoid with anti-inflammatory properties. Targeted delivery of dexamethasone to inflammatory cells, e.g. macrophages and Kupffer cells represents a promising approach to minimize side effects. The aim of the present study was to induce a targeted transport of novel DXM-based biodegradable nanocapsules to phagocytic cells. Nanocapsules (NCs) consisting of a hydroxyethylated glucose polymer (hydroxyethyl starch, HES) shell with encapsulated DXM and NCs synthesized exclusively in inverse miniemulsion out of DXM were investigated. Non-parenchymal murine liver cells served as target cells. HES-DXM NCs were predominantly incorporated by Kupffer …
Pruritus precipitated by hydroxyethyl starch: a review.
2005
Summary Hydroxyethyl starch (HES) is widely used for fluid management in broad populations of patients, particularly in the surgery and intensive care settings. Pruritus, often manifested as pruritic crises, is increasingly being recognized as a common major adverse effect of HES administration. This iatrogenic form of pruritus is frequently severe and protracted with a serious negative impact on patient quality of life, including sleep disturbance, disruption of daily routine and mental distress. Such pruritus is generally refractory to available therapies and can persist for up to 12–24 months. All currently clinically available HES solutions entail the risk of pruritus, including those o…
Cigarette smoke alters non-neuronal cholinergic system components inducing MUC5AC production in the H292 cell line.
2013
Abstract Cigarette smoke extract (CSE) affects the expression of Choline Acetyl-Transferase (ChAT), muscarinic acetylcholine receptors, and mucin production in bronchial epithelial cells. Mucin 5AC (MUC5AC), muscarinic acetylcholine receptor M3, ChAT expression, acetylcholine levels and acetylcholine binding were measured in a human pulmonary mucoepidermoid carcinoma cell line (H292) stimulated with CSE. We performed ChAT/RNA interference experiments in H292 cells stimulated with CSE to study the role of ChAT/acetylcholine in MUC5AC production. The effects of Hemicholinium-3 (HCh-3) (50 μM) (a potent and selective choline uptake blocker) and Tiotropium bromide (Spiriva ® ) (100 nM), alone o…
Steroid and vasoactive treatment for acute deafness after attempted hearing preservation acoustic neuroma surgery.
2004
<i>Objective:</i> To investigate whether intravenous steroid and vasoactive therapy in the acute postoperative period improves hearing outcome in patients who develop acute deafness after attempted hearing preservation surgery for acoustic neuroma (AN) through a retrosigmoid or a middle cranial fossa approach. <i>Study Design and Setting:</i> Retrospective controlled study in a tertiary care center. Thirty-six patients who had developed acute deafness after hearing preservation surgery for treatment of an AN were reviewed. Preoperative AAOHNS hearing class was A in 2, B in 2 and D in 32 patients. Twenty-seven patients were treated with prednisolone, hydroxyethyl star…
Monophosphoryl lipid A coating of hydroxyethyl starch nanocapsules drastically increases uptake and maturation by dendritic cells while minimizing th…
2015
Enhancing delivery of antigens to dendritic cells (DCs) is essential for the induction of vigorous antigen-specific cellular immune responses. Aim of the present study was to evaluate the properties of hydroxyethyl starch nanocapsules (HES-NCs) functionalized with anti-CD40, anti-DEC205, interferon-γ (IFNγ) and/or monophosphoryl lipid A (MPLA) with respect to the overall uptake, the released cytokine profile, and the influence on phenotypic maturation of human monocyte-derived DCs using flow cytometry, confocal microscopy and enzyme-linked immunosorbent assays. NC uptake by DCs was significantly enhanced by functionalizing NCs with anti-CD40 or MPLA. With respect to the cytokine profile and…
Application of Molecular Topology for the Prediction of Reaction Yields and Anti-Inflammatory Activity of Heterocyclic Amidine Derivatives
2011
Topological-mathematical models based on multiple linear regression analyses have been built to predict the reaction yields and the anti-inflammatory activity of a set of heterocylic amidine derivatives, synthesized under environmental friendly conditions, using microwave irradiation. Two models with three variables each were selected. The models were validated by cross-validation and randomization tests. The final outcome demonstrates a good agreement between the predicted and experimental results, confirming the robustness of the method. These models also enabled the screening of virtual libraries for new amidine derivatives predicted to show higher values of reaction yields and anti-infl…