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See detailBisindole alkaloids from Strychnos guianensis are effective antagonists of nicotinic acetylcholine receptors in cultured human TE671 cells
Wins, Pierre; Margineanu, Ilca; Penelle, Jacques et al

in Naunyn-Schmiedeberg's Archives of Pharmacology (2003), 367(3), 253-259

Several mono- and bisindole quaternary alkaloids isolated from the stem bark of Strychnos guianensis have recently been shown to be effective blockers of neuromuscular transmission in mice. In this study ... [more ▼]

Several mono- and bisindole quaternary alkaloids isolated from the stem bark of Strychnos guianensis have recently been shown to be effective blockers of neuromuscular transmission in mice. In this study, we used a human clonal cell line (TE671) expressing muscle-type nicotinic acetylcholine receptors. The agonist carbamylcholine activated a receptor-mediated Rb-86(+) efflux and this activation was antagonized by the indole alkaloids, the most active being bisindole bisquaternary compounds. The most effective antagonist, guiachrysine, had an IC50 around 0.43 muM in the presence of 0.5 mM carbamylcholine, compared to 0.16 muM for d-tubocurarine, the most potent curarizing alkaloid. Guiaflavine and 5',6'-dehydroguiaflavine were slightly less effective. Monoindole compounds were 10 to 100 times less potent than bisindole alkaloids. Kinetic analysis showed that the inhibition of the carbamylcholine-dependent Rb-86(+) efflux by guiaflavine was of mixed competitive and uncompetitive type. The competitive component (K-I = 0.21 muM) is presumably due to binding at the acetylcholine site, while the uncompetitive component (K'(I) = 0.92 muM) may be due to open channel block. [less ▲]

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See detailStrychnogucines A and B, two new antiplasmodial bisindole alkaloids from Strychnos icaja
Frederich, Michel ULg; Tits, Monique ULg; Penelle, Jacques et al

Poster (2000, September)

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See detailAntiinflammatory and chonroprotective activity of prodelphinidins isolated from Ribes nigrum leaves
Tits, Monique ULg; de Leval Xavier; Dierckxsens, Yvan et al

Poster (2000, July)

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See detailNouvelle méthode d'extraction et d'isolement de l'isostrychnopentamine à partir des feuilles de Strychnos usambarensis
Cristino, Assunçao; Tits, Monique ULg; Penelle, Jacques et al

Poster (2000, July)

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See detailPalicoside: précurseur naturel de l'akagérine
Brandt, Viviane; Tits, Monique ULg; Penelle, Jacques et al

Poster (2000, July)

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See detailQuaternary Indole Alkaloids from the Stem Bark of Strychnos Guianensis
Penelle, Jacques; Tits, Monique ULg; Christen, Philippe et al

in Phytochemistry (2000), 53(8), 1057-66

Two new quaternary alkaloids, 9-methoxy-Nb-methylgeissoschizol and guiachrysine together with the known compounds C-alkaloid O, fluorocurine, mavacurine, macusine B and C-profluorocurine, were isolated ... [more ▼]

Two new quaternary alkaloids, 9-methoxy-Nb-methylgeissoschizol and guiachrysine together with the known compounds C-alkaloid O, fluorocurine, mavacurine, macusine B and C-profluorocurine, were isolated from Strychnos guianensis stembark. The structures of the compounds were elucidated on the basis of spectroscopic studies. [less ▲]

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See detailNew Antimalarial and Cytotoxic Sungucine Derivatives from Strychnos Icaja Roots
Frederich, Michel ULg; Gillet, Marie-Claire ULg; Llabres, Gabriel ULg et al

in Planta Medica (2000), 66(3), 262-9

Reinvestigation of Strychnos icaja Baillon resulted in the isolation of vomicine, isostrychnine and of three new sungucine derivatives, named isosungucine (8), 18-hydroxy-sungucine (9) and 18-hydroxy ... [more ▼]

Reinvestigation of Strychnos icaja Baillon resulted in the isolation of vomicine, isostrychnine and of three new sungucine derivatives, named isosungucine (8), 18-hydroxy-sungucine (9) and 18-hydroxy-isosungucine (10). They were identified by detailed spectroscopic methods. The complete 1H- and 13C-NMR study of sungucine was also realized. Some of these compounds were highly active against Plasmodium falciparum in vitro and more particularly against the chloroquine-resistant strain. Compound 10 showed a selective antiplasmodial activity, with > 100-fold greater toxicity towards Plasmodium falciparum, relative to cultured human cancer cells (KB and HeLa lines) or fibroblasts (WI38). [less ▲]

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See detailAnti-inflammatory and chondroprotective activity of prodelphinidins isolated from Ribes nigrum leaves.
Tits, Monique ULg; de Leval, Xavier; Diercksens, Yves et al

Poster (2000)

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See detailGuiaflavine, a new bisindole quaternary alkaloid from the stem bark of Strychnos guianensis
Penelle, Jacques; Tits, Monique ULg; Christen, P. et al

Poster (1999, July)

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See detailGuiaflavine, un nouvel alcaloïde quaternaire bisindolique isolé à partir de l'écorce de tige du Strychnos guianensis
Penelle, Jacques; Tits, Monique ULg; Christen, Philippe et al

Poster (1999, May)

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See detailQuatre alcaloïdes à noyau bèta-carboline isolés des écorces de tronc du Strychnos mellodora
Brandt, Viviane; Tits, Monique ULg; Geerlings, A et al

Poster (1999, May)

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See detailGuiaflavine, a new bisindole quaternary alkaloid from the stem bark of Strychnos guianensis
Penelle, Jacques; Tits, Monique ULg; Christen, Philippe et al

Conference (1999, May)

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See detailBeta-Carboline Glucoalkaloids from Strychnos mellodora
Brandt, Viviane; Tits, Monique ULg; Geerlings, A. et al

Conference (1999, May)

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See detail10'-Hydroxyusambarensine, a New Antimalarial Bisindole Alkaloid from the Roots of Strychnos Usambarensis
Frederich, Michel ULg; Tits, Monique ULg; Hayette, Marie-Pierre ULg et al

in Journal of Natural Products (1999), 62(4), 619-21

Reinvestigation of Strychnos usambarensis Gilg resulted in the isolation of a tertiary phenolic bisindole alkaloid, 10'-hydroxyusambarensine (1), which was identified by detailed spectroscopic methods ... [more ▼]

Reinvestigation of Strychnos usambarensis Gilg resulted in the isolation of a tertiary phenolic bisindole alkaloid, 10'-hydroxyusambarensine (1), which was identified by detailed spectroscopic methods. Compound 1 was moderately active against two strains of Plasmodium falciparum in vitro. [less ▲]

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