8 hydroxyquinoline/põletik

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[Spasmolytic and anti-inflammatory activity of 8-hydroxyquinolines].

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It has been shown that quinozole (aqueous solution), enteroseptol and nitroxoline (suspension with Tween-80) in a concentration of 0.2 X 10(-6)-1.10(-5) decrease the tone of the rat and guinea-pig ileum and diminish their peristalsis. When administered in the same concentrations quinozole removes or

Identification of 8-Hydroxyquinoline Derivatives Active Against Somatic V658F Mutant JAK1-Dependent Cells.

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Janus kinases (JAKs) and their gain-of-function mutants have been implicated in a range of oncological, inflammatory, and autoimmune conditions, which has sparked great research interest in the discovery and development of small-molecule JAK inhibitors. Two molecules are currently marketed as JAK

Synthesis of Novel 8-Hydroxyquinoline Derivatives through Mannich Reaction and their Biological Evaluation as Potential Immunomodulatory Agents.

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In continuation of our work on Mannich reaction on 8-hydroxyquinoline, fifteen different combinations of aromatic aldehydes and aniline were subjected to Mannich reaction from which twelve products (eight Mannich bases, two imines and two intramolecularly cyclized products with

Inhibition of the histone demethylase KDM4B leads to activation of KDM1A, attenuates bacterial-induced pro-inflammatory cytokine release, and reduces osteoclastogenesis.

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Periodontal disease (PD) afflicts 46% of Americans with no effective adjunctive therapies available. While most pharmacotherapy for PD targets bacteria, the host immune response is responsible for driving tissue damage and bone loss in severe disease. Herein, we establish that the histone

8-Hydroxyquinolines: a review of their metal chelating properties and medicinal applications.

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Metal ions play an important role in biological processes and in metal homeostasis. Metal imbalance is the leading cause for many neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, and multiple sclerosis. 8-Hydroxyquinoline (8HQ) is a small planar molecule with a lipophilic

8-Hydroxyquinoline inhibits iNOS expression and nitric oxide production by down-regulating LPS-induced activity of NF-kappaB and C/EBPbeta in Raw 264.7 cells.

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In activated macrophage, large amounts of nitric oxide (NO) are generated by inducible nitric oxide synthase (iNOS), resulting in acute or chronic inflammatory disorders. In Raw 264.7 cells stimulated with lipopolysaccharide (LPS) to mimic inflammation, 8-hydroxyquinoline (8HQ) inhibited the

Effect of 8-hydroxyquinoline and derivatives on human neuroblastoma SH-SY5Y cells under high glucose.

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8-Hydroxyquinoline and derivatives exhibit multifunctional properties, including antioxidant, antineurodegenerative, anticancer, anti-inflammatory and antidiabetic activities. In biological systems, elevation of intracellular calcium can cause calpain activation, leading to cell death. Here, the

Quantitative high-throughput screening identifies 8-hydroxyquinolines as cell-active histone demethylase inhibitors.

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BACKGROUND Small molecule modulators of epigenetic processes are currently sought as basic probes for biochemical mechanisms, and as starting points for development of therapeutic agents. N(ε)-Methylation of lysine residues on histone tails is one of a number of post-translational modifications that

Anti-inflammatory thiazine alkaloids isolated from the New Zealand ascidian Aplidium sp.: inhibitors of the neutrophil respiratory burst in a model of gouty arthritis.

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Ascidiathiazones A (3) and B (4), two new tricyclic thiazine-containing quinolinequinone alkaloids, were isolated from the New Zealand ascidian Aplidium species. Both compounds inhibited the in vitro production of superoxide by PMA-stimulated human neutrophils in a dose-dependent manner with IC50

[Studies on D-penicillamine (1): Inhibitory effect of D-penicillamine on the heat-Cu++ induced denaturation of human gamma-globulin (author's transl)].

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The inhibitory effect of D-penicillamine on the denaturation of human gamma-globulin induced by heat and Cu++ was compared with the action of other agents such as antirheumatic drugs, anti-inflammatory drugs, SH reagents, SH inhibitors and chelating reagents. The denaturation of human gamma globulin

Aggregation induced emission enhancement and growth of naphthalimide nanoribbons via J-aggregation: insight into disaggregation induced unfolding and detection of ferritin at the nanomolar level.

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A series of novel V-shaped naphthalimide derivatives are reported herein, designed through a strategy to achieve aggregation induced emission (AIE), giving rise to unexpected self-assembly properties. This includes an aggregation induced emission enhancement (AIEE) active small organic molecule viz.

Synthesis and biological activities of 4-aminoantipyrine derivatives derived from betti-type reaction.

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The present work deals with the synthesis and evaluation of biological activities of 4-aminoantipyrine derivatives derived from a three-component Betti reaction. The synthesis was initiated by the condensation of aromatic aldehyde, 4-aminoantipyrine, and 8-hydroxyquinoline in presence of fluorite as

Iron loading of endothelial cells augments oxidant damage.

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Transition metals, particularly iron, will potentiate oxidant damage to isolated cell organelles, plasma membranes, and DNA when added to in vitro incubation systems. However, similar studies of intact cells have been hampered by the relative impermeability of whole cells to iron. We have iron

Assay and biochemical characterization of angiotensin-I-converting enzyme in cerebrospinal fluid.

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A spectrofluorimetric method was adapted for determination of angiotensin-I-converting enzyme (ACE) in untreated native cerebrospinal fluid (CSF). Benzyloxycarbonyl-phenylalanyl-histidyl-leucine was applied as enzyme substrate. The biochemical behavior of ACE of CSF (CACE) was studied. The pH

Hepatocyte or serum albumin protein carbonylation by oxidized fructose metabolites: Glyceraldehyde or glycolaldehyde as endogenous toxins?

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Excessive sugar intake in animal models may cause tissue damage associated with oxidative and carbonyl stress cytotoxicity as well as inflammation. Fructose became a 100-fold more cytotoxic if hepatocytes were exposed to a non-toxic infusion of H(2)O(2) so as to simulate H(2)O(2) released by Kupffer

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