Inhibition of platelet-activating factor receptor binding by aporphine and phenanthrenoid alkaloids from Aromadendron elegans

作者:

I JantanIAA RafiJ Jalil

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摘要:

Six aporphine and one phenanthrenoid alkaloids isolated from AROMADENDRON ELEGANS Blume were investigated for their inhibitory effect on platelet-activating factor (PAF) binding to rabbit platelets using3H-PAF as a ligand. Of the compounds tested, (-)-N-acetylanonaine, 1-(N-acetyl-N-methylamino)ethyl-3,4,6-trimethoxy-7-hydroxy-phenanthrene, and predicentrine showed strong inhibition of PAF receptor binding, with IC50values of 52.4, 38.6, and 29.8 μM, respectively. The flexibility of the biphenyl system of the aporphine and the presence of methoxy groups at C-9 and C-10 were all preferable in binding to the receptor.

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DOI:

10.1055/s-2001-15819

被引量:

28

年份:

2001

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