5 research outputs found
Jeux vidéos (Les)
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
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>
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>
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