La 17ß-hydroxysteroïde déshydrogénase de type 2 comme cible pour le traitement de l’ostéoporose

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Oxidative Stress and Antioxidants

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Design, synthesis and study of myeloperoxidase inhibitors in the series of 3-alkylindole

The deleterious effects of MPO make it a new target for medicinal research. The aim of our study is to find promising inhibitors of MPO for using them as starting point of new anti-inflammatory drugs. Depending on previous researches on MPO inhibitors, we selected 5-fluorotryptamine as starting compounds. Using docking experiments, we designed a series of compounds derived from 5-fluorotryptamine. Two modifications were proposed: &Doctorat en Sciences biomédicales et pharmaceutiquesinfo:eu-repo/semantics/nonPublishe

Synthèse D’une Polyhydrazone et Sa Capacité De Chélation De Métaux Pour La Dépollution D’eaux Usées -- Sciences bio-médical et pharmaceutiques

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Halogen bonding in polymer science: From crystal engineering to functional supramolecular polymers and materials

Halogen bonding (XB) is commonly defined as a non-covalent bond where halogen atoms (XSCOPUS: re.jinfo:eu-repo/semantics/publishe

A patent review of myeloperoxidase inhibitors for treating chronic inflammatory syndromes (focus on cardiovascular diseases, 2013-2019)

Introduction: Myeloperoxidase (MPO) is an immune enzyme found in neutrophils and macrophages. It produces the highly oxidative compound HOCl from H2O2 and Cl− ions inside the phagosome of the neutrophil. Leakage of the enzyme outside the cell causes oxidative damages for the biomolecules promoting many inflammatory diseases such as atherosclerosis. Thus, there is a real interest to develop potent inhibitors of MPO as non-steroidal anti-inflammatory agents. This review highlights the several published MPO inhibitors, their activity, and the challenges met during the development of these compounds. Areas covered: This article covers the patent literature published on MPO inhibitors from 2013 to 2019, as well as the potential use of these compounds as therapeutics for inflammatory syndromes, especially that plays an important role in the initiation and progression of atherosclerosis. Expert opinion: To date, many MPO inhibitors with different structures have been studied, many of which have prominent inhibitory activities. Furthermore, the specificity of these drugs offers hope for the targeted therapy of inflammatory syndromes. Although many data have proved that MPO can contribute to several chronic inflammatory syndromes, the usefulness of MPO inhibitors in preventing and treating inflammatory disorders is still under investigation.SCOPUS: re.jinfo:eu-repo/semantics/publishe

Preparation of 3-alkyl-5-fluoroindole derivatives as myeloperoxidase inhibitors

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Anti-inflammatory, antioxidant effects, and bioaccessibility of Tigzirt propolis

This work aims to assess the anti-inflammatory effects of Tigzirt propolis native to Algeria. We divided 48 male Wistar rats into 8 groups. We orally administered ethyl acetate extract of propolis (EAP), pure polyphenols compounds, or diclofenac 5 days before induction of inflammation by of carrageenan (100 μg/ml, i.p.). We determined the development of paw edema, biological parameters, myeloperoxidase activity, TNF-α, and prostaglandin E2 and measured the oxidative status parameters, as well. Finally, we analyzed the absorption and bioaccessibility of propolis in rats’ plasma using GC–MS after orally dosing rats (250 mg/kg). The pretreatment by 200 and 250 mg/kg of propolis significantly reduced the edema rates after the third hour. Propolis can restore the disruption of homeostasis as well as markers of inflammation induced by carrageenan in Wistar rats, and an increase of the enzymatic activities. Furthermore, the inflammation was better resolved in rats that received propolis than in those treated with pure polyphenols. Practical applications: Propolis is a natural mixture that bees produce by mixing gathered resin and gums to bee saliva and wax. Our research investigated the effect of Tigzirt propolis on the inhibition of biomarkers of inflammation and the development of paw edema. Propolis extract helped to reduce PGE2, TNF-α, myeloperoxidase, and malondialdehyde levels and increase the total antioxidant levels in plasma. Our findings emphasized the use of phenolic extract of propolis in industries such as nutraceuticals for the prevention of inflammatory diseases. It can also protect the body against damage under oxidative stress.SCOPUS: ar.jinfo:eu-repo/semantics/publishe

Targeting Cytosolic Phospholipase A2α for Novel Anti-Inflammatory Agents.

Group IV cytosolic phospholipase A2 (cPLA2α) plays a critical role in inflammatory processes. It produces arachidonic acid which is the main source of the pro-inflammatory eicosanoids mediators that are important in innate immune system. In some cases, these pro-inflammatory mediators cause damages to the host tissues and therefore promote autoimmune diseases. Consequently, development of potent inhibitors against cPLA2α could improve the therapy of inflammatory diseases. In the last two decades, intense efforts have been done to find potent cPLA2α inhibitors. Several scaffolds have been developed with the use of structure-activity relationship (SAR) studies, and potent inhibitors have been obtained. The poor absorption of these compounds from intestine was the main challenge for clinical application. This review illustrates the search for cPLA2α inhibitors, their SAR studies and biological effects.SCOPUS: re.jinfo:eu-repo/semantics/publishe

Reactive oxygen species: Inhibition of Myeloperoxidase

Myeloperoxidase participates in innate immune defense mechanism through formation of microbicidal reactive oxidants and diffusible radical species. A unique activity is its ability to use chloride as a cosubstrate with hydrogen peroxide to generate chlorinating oxidants such as hypochlorous acid, a potent antimicrobial agent. However, chronic MPO activation can lead to indiscriminate protein modification causing tissue damage, and has been associated with chronic inflammatory diseases, atherosclerosis, and acute cardiovascular events. This has attracted considerable interest in the development of therapeutically useful MPO inhibitors. Today, based on the profound knowledge of structure and function of MPO and its biochemical and biophysical differences with the other homologous human peroxidases, various rational and high-throughput screening attempts were performed in developing specific irreversible and reversible inhibitors. The most prominent candidates as well as MPO inhibitors already studied in clinical trials are introduced and discussed.info:eu-repo/semantics/publishe