5 research outputs found

    Jeux vidéos (Les)

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    Rapport d\u27information fait au nom de la commission des affaires économiques et de la commission de la culture, de l\u27éducation et de la communication par le groupe de travail sur les jeux vidéo

    1-Butyl­quinine tetra­fluoro­borate

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    In the title salt (2S,4S,8R)-1-butyl-2-[(R)-(hydr­oxy)(6-methoxy­quinolin-4-yl)meth­yl]-8-vinyl­quinuclidin-1-ium tetra­fluoro­borate, C24H33N2O2 +·BF4 −, the butyl substituent at the 1-position is in an equatorial conformation with respect to the unsubstituted six-membered ring and the four butyl C atoms are almost coplanar with the ring N and vinyl C atoms (r.m.s. deviation = 0.046 Å). In the crystal, the cations are linked by O—H⋯N hydrogen bonds. The F atoms of the tetra­fluoro­borate group are disordered over two sets of site with an occupancy raitio of 0.552 (8):0.448 (8)

    Natural Inhibitors of the RhoA–p115 Complex from the Bark of <i>Meiogyne baillonii</i>

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    In an effort to find potent natural inhibitors of RhoA and p115 signaling G-proteins, a systematic in vitro evaluation using enzymatic and plasmonic resonance assays was undertaken on 11 317 plant extracts. The screening procedure led to the selection of the New Caledonian endemic species <i>Meiogyne baillonii</i> for a chemical investigation. Using a bioguided isolation procedure, three enediyne-γ-butyrolactones (<b>1</b>–<b>3</b>) and two enediyne-γ-butenolides (<b>4</b> and <b>5</b>), named sapranthins H–L, respectively, two enediyne carboxylic acid (<b>6</b> and <b>7</b>), two depsidones, stictic acid (<b>8</b>) and baillonic acid (<b>9</b>), aristolactams AIa and AIIa (<b>10</b> and <b>11</b>), and two aporphines, dehydroroemerine (<b>12</b>) and noraristolodione (<b>13</b>), were isolated from the ethyl acetate extract of the bark. The structures of the new compounds (<b>1</b>–<b>6</b>, <b>9</b>, and <b>11</b>) and their relative configurations were established by NMR spectroscopic analysis and by X-ray diffraction analysis for compound <b>9</b>. Only stictic acid (<b>8</b>) exhibited a significant inhibiting activity of the RhoA–p115 complex, with an EC<sub>50</sub> value of 0.19 ± 0.05 mM. This is the first time that a natural inhibitor of the complex RhoA–p115’s activity was discovered from an HTS performed over a collection of higher plant extracts. Thus, stictic acid (<b>8</b>) could be used as the first reference compound inhibiting the interaction between RhoA and p115

    Natural Inhibitors of the RhoA–p115 Complex from the Bark of <i>Meiogyne baillonii</i>

    No full text
    In an effort to find potent natural inhibitors of RhoA and p115 signaling G-proteins, a systematic in vitro evaluation using enzymatic and plasmonic resonance assays was undertaken on 11 317 plant extracts. The screening procedure led to the selection of the New Caledonian endemic species <i>Meiogyne baillonii</i> for a chemical investigation. Using a bioguided isolation procedure, three enediyne-γ-butyrolactones (<b>1</b>–<b>3</b>) and two enediyne-γ-butenolides (<b>4</b> and <b>5</b>), named sapranthins H–L, respectively, two enediyne carboxylic acid (<b>6</b> and <b>7</b>), two depsidones, stictic acid (<b>8</b>) and baillonic acid (<b>9</b>), aristolactams AIa and AIIa (<b>10</b> and <b>11</b>), and two aporphines, dehydroroemerine (<b>12</b>) and noraristolodione (<b>13</b>), were isolated from the ethyl acetate extract of the bark. The structures of the new compounds (<b>1</b>–<b>6</b>, <b>9</b>, and <b>11</b>) and their relative configurations were established by NMR spectroscopic analysis and by X-ray diffraction analysis for compound <b>9</b>. Only stictic acid (<b>8</b>) exhibited a significant inhibiting activity of the RhoA–p115 complex, with an EC<sub>50</sub> value of 0.19 ± 0.05 mM. This is the first time that a natural inhibitor of the complex RhoA–p115’s activity was discovered from an HTS performed over a collection of higher plant extracts. Thus, stictic acid (<b>8</b>) could be used as the first reference compound inhibiting the interaction between RhoA and p115
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