Inhibitory effect of compounds from Goniothalamus tapis Miq. and Goniothalamus uvaroides King on platelet-activating factor receptor binding

Phytother Res. 2012 May;26(5):687-91. doi: 10.1002/ptr.3620. Epub 2011 Oct 17.

Abstract

Phytochemical investigation on the bark of Goniothalamus tapis Miq. and G. uvaroides King has resulted in the isolation of eight styryl-lactones, (-)-cryptomeridiol, liriodenine, 3-methyl-1H-benz[f]indole-4,9-dione, (-)-stigmasterol and dimethyl terephthalate. The structures of the compounds were elucidated by spectroscopic techniques. The compounds were evaluated for their effect on platelet-activating factor (PAF) receptor binding on rabbit platelets using (3) H-PAF as a ligand. Among the compounds tested, (-)-cryptomeridiol, (+)-goniothalamin and (+)-isoaltholactone exhibited a significant and concentration-dependent inhibitory effect on PAF receptor binding, with inhibitory concentration (IC)(50) values of 17.5, 19.7 and 46.5 µm, respectively. The inhibitory effects of the first two compounds were comparable to that obtained from the positive control, cedrol. The results indicated that these compounds were strong PAF receptor binding inhibitors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Blood Platelets / drug effects
  • Blood Platelets / metabolism
  • Dose-Response Relationship, Drug
  • Furans / chemistry
  • Furans / isolation & purification
  • Furans / pharmacology
  • Goniothalamus / chemistry*
  • Inhibitory Concentration 50
  • Lactones / chemistry
  • Lactones / isolation & purification
  • Lactones / pharmacology*
  • Naphthalenes / chemistry
  • Naphthalenes / isolation & purification
  • Naphthalenes / pharmacology
  • Plant Bark / chemistry
  • Plant Extracts / chemistry
  • Plant Extracts / isolation & purification
  • Plant Extracts / pharmacology*
  • Platelet Aggregation / drug effects
  • Platelet Aggregation Inhibitors / chemistry
  • Platelet Aggregation Inhibitors / isolation & purification
  • Platelet Aggregation Inhibitors / pharmacology*
  • Platelet Membrane Glycoproteins / antagonists & inhibitors*
  • Platelet Membrane Glycoproteins / chemistry
  • Platelet Membrane Glycoproteins / drug effects
  • Platelet Membrane Glycoproteins / isolation & purification
  • Protein Binding / drug effects
  • Pyrones / chemistry
  • Pyrones / isolation & purification
  • Pyrones / pharmacology
  • Rabbits
  • Receptors, G-Protein-Coupled / antagonists & inhibitors*
  • Receptors, G-Protein-Coupled / chemistry
  • Receptors, G-Protein-Coupled / drug effects
  • Receptors, G-Protein-Coupled / isolation & purification

Substances

  • Furans
  • Lactones
  • Naphthalenes
  • Plant Extracts
  • Platelet Aggregation Inhibitors
  • Platelet Membrane Glycoproteins
  • Pyrones
  • Receptors, G-Protein-Coupled
  • altholactone
  • cryptomeridiol
  • platelet activating factor receptor
  • goniothalamin