References of "De Tullio, Pascal"
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See detailMetabolomics : a new insight into cells and organisms diseases
De Tullio, Pascal ULg

Conference (2010, October 25)

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See detailMetabolomics : Toward a better understanding of cells and organisms diseases
De Tullio, Pascal ULg

Conference (2010, October 08)

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See detailMetabolomic analysis of Echinacea spp. by (1)H nuclear magnetic resonance spectrometry and multivariate data analysis technique.
Frederich, Michel ULg; Jansen, C.; De Tullio, Pascal ULg et al

in Phytochemical Analysis [=PCA] (2010), 21(1), 61-65

Introduction - The genus Echinacea (Asteraceae) comprises about 10 species originally distributed in North America. Three species are very well known as they are used worldwide as medicinal plants ... [more ▼]

Introduction - The genus Echinacea (Asteraceae) comprises about 10 species originally distributed in North America. Three species are very well known as they are used worldwide as medicinal plants: Echinacea purpurea, E. pallida, E. angustifolia.Objective - To discriminate between these three Echinacea species and E. simulata by (1)H NMR-based metabolomics.Methodology - (1)H NMR and multivariate analysis techniques were applied to diverse Echinacea plants including roots and aerial parts, authentic plants, commercial plants and commercial dry extracts.Results - Using the (1)H NMR metabolomics, it was possible, without previous evaporation or separation steps, to obtain a metabolic fingerprint to distinguish between species.Conclusion - A clear distinction between the three pharmaceutical species was possible and some useful metabolites were identified. Copyright (c) 2009 John Wiley & Sons, Ltd. [less ▲]

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See detailCoupling of Liquid Chromatography/Tandem Mass Spectrometry and Liquid Chromatography/Solid-Phase Extraction/NMR Techniques for the Structural Identification of Metabolites following In Vitro Biotransformation of SUR1-Selective ATP-Sensitive Potassium Channel Openers
Gillotin, F.; Chiap, Patrice ULg; Frederich, Michel ULg et al

in Drug Metabolism and Disposition : The Biological Fate of Chemicals (2010), 38(2), 232-240

SUR1-selective ATP-sensitive potassium channel openers (PCOs) have been shown to be of clinical value for the treatment of several metabolic disorders, including type I and type II diabetes, obesity and ... [more ▼]

SUR1-selective ATP-sensitive potassium channel openers (PCOs) have been shown to be of clinical value for the treatment of several metabolic disorders, including type I and type II diabetes, obesity and hyperinsulinemia. Taking into account these promising therapeutic benefits, different series of 3-alkylamino-4H-1,2,4-benzothiadiazine 1,1-dioxides structurally related to diazoxide were developed. In view of the lead optimisation process of the series, knowledge of ADMET parameters, and more particularly the metabolic fate of these compounds, is a fundamental requirement. For such a purpose, two selected promising compounds (BPDZ 73 and BPDZ 157) were incubated in the presence of phenobarbital-induced rat liver microsomes to produce expected mammal in vivo phase I metabolites. The resulting major metabolites were then analysed by both MS and NMR in order to completely elucidate their chemical structures. The two compounds were also further incubated in the presence of non-treated rats and human microsomes in order to compare the metabolic profiles. In the present study, the combined use of an exact mass LC-MS/MS platform and a LC-SPE-NMR system allowed the clarification of some unresolved structural assessments in the accurate chemical structure elucidation process of the selected PCOs drugs. These results greatly help the optimization of the lead compounds. [less ▲]

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See detailNew Fluorinated 1,2,4-Benzothiadiazine 1,1-Dioxides: Discovery of an Orally Active Cognitive Enhancer Acting through Potentiation of the 2-Amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic Acid Receptors
Francotte, Pierre ULg; Goffin, Eric ULg; Fraikin, Pierre ULg et al

in Journal of Medicinal Chemistry (2010), 53

In the search of a potent cognitive enhancer, a series of 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides have been synthesized and evaluated as positive allosteric modulators of the AMPA receptors. In ... [more ▼]

In the search of a potent cognitive enhancer, a series of 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides have been synthesized and evaluated as positive allosteric modulators of the AMPA receptors. In the present work, we focused our efforts on the insertion of mono- or polyfluoro- substituted alkyl chains at the 4-position of the thiadiazine ring in an attempt to enhance the pharmacokinetic behavior of previously described compounds. Among all the described compounds, 7-chloro-4-(2-fluoroethyl)-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide, 12b, was shown to exert a strong activity on AMPA receptors in vitro and a marked cognitive-enhancing effect in vivo after oral administration to Wistar rats. Considering its in vivo activity, the metabolic degradation of 12b was studied and compared to that of its nonfluorinated analogue 9b. Taken together, results of this study clearly validated the positive impact of the fluorine atom on the alkyl chain at the 4-position of benzothiadiazine dioxides on activity and metabolic stability. [less ▲]

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See detailNew Biological Investigations on 3-Bromophenyl 6-Acetoxymethyl-2-oxo-2H-1-Benzopyran-3-Carboxylate as Anti-angiogenic Agent
Hemmer, M.; Kempen, Isabelle; De Tullio, Pascal ULg et al

in Drug Development Research (2010), 71

The development of blood vessels inside tumors is required to provide the nutrients and oxygen needed for tumor growth and to allow the spread of cancer cells at a distance to form metastasis ... [more ▼]

The development of blood vessels inside tumors is required to provide the nutrients and oxygen needed for tumor growth and to allow the spread of cancer cells at a distance to form metastasis. Angiogenesis is also implicated in ocular diseases like age-related macular degeneration. The present work describes the potential anti-angiogenic properties of a coumarinic derivative, 3-bromophenyl 6-acetoxymethyl-2-oxo-2H-1-benzopyran-3-carboxylate (IK9), previously described as a potent inhibitor of HT 1080 fibrosarcoma cell invasion in vitro and tumor growth in vivo. In vivo, ex vivo, and in vitro models were used to delineate the anti-angiogenic properties of IK9. The anti-angiogenic effect of IK9 was demonstrated in vivo in a choroidal neovascularization mice model and additionally ex vivo in a rat aortic ring assay where it was more active than the known matrix metalloproteinase inhibitor Ro 28-2653. IK9 did not affect apoptosis, proliferation, or endothelial cell invasiveness in vitro. These findings suggest a complex mechanism of action of the compound via direct or indirect effects on endothelial cell properties. This study identifies IK9 as a new potent inhibitor of angiogenesis and suggests its potential use as a therapeutic agent. [less ▲]

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See detailOriginal cromakalim analogues as KATP channel openers
Florence, X.; De Tullio, Pascal ULg; Pirotte, Bernard ULg et al

Conference (2009, June)

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See detailLes canaux potassiques ATP-dépendants : nouvelles cibles potentielles pour le traitement de divers troubles métaboliques
Florence, X.; De Tullio, Pascal ULg; Lebrun, Ph. et al

Conference (2009, February 03)

Detailed reference viewed: 9 (0 ULg)
See detailApplication of Metabolomic Approaches to the Age-related Macular Degeneration (AMD)
De Tullio, Pascal ULg

Conference (2009, January 30)

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See detailNew R/S-3,4-dihydro-2,2-dimethyl-2H-1-benzopyrans as KATP channel openers: modulation of the 4-position
Florence, Xavier ULg; Sebille, Sophie; De Tullio, Pascal ULg et al

in Bioorganic & Medicinal Chemistry (2009), 17

Detailed reference viewed: 25 (5 ULg)