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.

Highlights

  • Platelet-activating factor (PAF) is a potent glycerophospholipid mediator, participating in a number of physiological responses such as aggregation [1], chemotaxis [2], granule secretion and oxygen radical generation from leukocytes [3,4]

  • We report on the strong inhibitory effect (62.1%) of the methanol extract of the leaves of G. nervosa var. pubescens on platelet-activating factor (PAF) binding in vitro and the bioassay-guided isolation and structure elucidation of a new biflavonoid from the plant, together with two known flavonoids, and their effect on the binding of 3H-PAF to washed rabbit platelets

  • The methanol extract of the leaves of G. nervosa var pubescens was investigated for platelet-activating factor (PAF) receptor binding inhibitory activity on rabbit platelets at a concentration of 18.2 μg/mL

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Summary

Introduction

Platelet-activating factor (PAF) is a potent glycerophospholipid mediator, participating in a number of physiological responses such as aggregation [1], chemotaxis [2], granule secretion and oxygen radical generation from leukocytes [3,4]. It is involved in several pathophysiological conditions such as inflammation [5], allergy [6], asthma [7] and thrombosis [8]. We report on the strong inhibitory effect (62.1%) of the methanol extract of the leaves of G. nervosa var. pubescens on PAF binding in vitro and the bioassay-guided isolation and structure elucidation of a new biflavonoid from the plant, together with two known flavonoids, and their effect on the binding of 3H-PAF to washed rabbit platelets

Results and Discussion
General Procedures
Plant Material
Bioassay-Guided Isolation
Preparation of Samples for PAF Assay
PAF Receptor Binding Inhibitor Assay

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