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Molecules ; 17(9): 10893-901, 2012 Sep 10.
Article in English | MEDLINE | ID: mdl-22964504

ABSTRACT

The methanol extract of the leaves of Garcinia nervosa var. pubescens King, which showed strong inhibitory effects on platelet-activating factor (PAF) receptor binding, was subjected to bioassay-guided isolation to obtain a new biflavonoid, II-3,I-5, II-5,II-7,I-4',II-4'-hexahydroxy-(I-3,II-8)-flavonylflavanonol together with two known flavonoids, 6-methyl-4'-methoxyflavone and acacetin. The structures of the compounds were elucidated by spectroscopic methods. The compounds were evaluated for their ability to inhibit PAF receptor binding to rabbit platelets using ³H-PAF as a ligand. The biflavonoid and acacetin showed strong inhibition with IC50 values of 28.0 and 20.4 µM, respectively. The results suggest that these compounds could be responsible for the strong PAF antagonistic activity of the plant.


Subject(s)
Biflavonoids/pharmacology , Garcinia/chemistry , Platelet Activating Factor/antagonists & inhibitors , Platelet Membrane Glycoproteins/antagonists & inhibitors , Receptors, G-Protein-Coupled/antagonists & inhibitors , Animals , Biflavonoids/chemistry , Biflavonoids/isolation & purification , Blood Platelets/drug effects , Blood Platelets/metabolism , Flavones/chemistry , Flavones/pharmacology , Inhibitory Concentration 50 , Plant Extracts/chemistry , Plant Leaves/chemistry , Platelet Aggregation/drug effects , Platelet Aggregation Inhibitors/metabolism , Platelet Aggregation Inhibitors/pharmacology , Platelet Membrane Glycoproteins/metabolism , Rabbits , Receptors, G-Protein-Coupled/metabolism
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