Platelet-activating factor (PAF) receptor binding activity of the roots of Enicosanthellum pulchrum

Noraziah Nordin, Juriyati Jalil, Ibrahim Jantan, Shahnaz Murad

Research output: Contribution to journalArticle

8 Citations (Scopus)

Abstract

Context: Enicosanthellum pulchrum (King) Heusden (Annonaceae) is a coniferous tree that is confined to mountain forests. The chemical constituents of this species have been studied previously; however, its biological activity has never been investigated before and is reported here for the first time. Objective: The extracts, fractions and compounds from the roots of E. pulchrum were investigated for their inhibitory effects on platelet-activating factor (PAF) receptor binding to rabbit platelets using 3H-PAF as a ligand. Materials and methods: The PAF receptor binding inhibitory effect using rabbit platelets was determined in vitro by measuring the difference between total amount of bound 3H-PAF in the presence and the absence of excess unlabelled PAF. The compounds were isolated by bioassay-guided fractionation and their structures were elucidated by spectroscopic techniques. Results and discussion: Among the extracts tested, the ethyl acetate extract was the most active with 85.6% inhibition, while hexane and methanol extracts showed 40.2 and 42.5% inhibition, respectively. Fractionation of the ethyl acetate extract using vacuum liquid chromatography (VLC) yielded six fractions AEA(I-VI). Chromatography fraction AEA(VI) yielded a new compound, 1-(2′,3′, 4′-trimethoxyphenyl)hexan-1-ol, while fraction AEA(III) afforded three compounds, namely liriodenine, cleistopholine and dehydroanonaine. 1-(2′,3′,4′-Trimethoxyphenyl)hexan-1-ol, cleistopholine and dehydroanonaine showed relatively strong inhibition with IC50 values of 26.6, 50.2 and 45.4 M, respectively. Conclusion: The results suggest that these compounds could be responsible for the PAF antagonistic activity of the ethyl acetate extract of this plant.

Original languageEnglish
Pages (from-to)284-290
Number of pages7
JournalPharmaceutical Biology
Volume50
Issue number3
DOIs
Publication statusPublished - Mar 2012

Fingerprint

Platelet Activating Factor
Blood Platelets
Annonaceae
Rabbits
Plant Extracts
Hexanes
Vacuum
Liquid Chromatography
Biological Assay
Inhibitory Concentration 50
Methanol
Chromatography
Ligands
platelet activating factor receptor
ethyl acetate
cleistopholine

Keywords

  • 1-(2′;3′;4′-trimethoxyphenyl)hexan-1-ol
  • Annonaceae
  • Bioassay-guided isolation
  • Cleistopholine
  • Dehydroanonaine
  • Platelet-activating factor antagonists

ASJC Scopus subject areas

  • Drug Discovery
  • Pharmacology
  • Pharmaceutical Science
  • Complementary and alternative medicine
  • Molecular Medicine

Cite this

Platelet-activating factor (PAF) receptor binding activity of the roots of Enicosanthellum pulchrum. / Nordin, Noraziah; Jalil, Juriyati; Jantan, Ibrahim; Murad, Shahnaz.

In: Pharmaceutical Biology, Vol. 50, No. 3, 03.2012, p. 284-290.

Research output: Contribution to journalArticle

Nordin, Noraziah ; Jalil, Juriyati ; Jantan, Ibrahim ; Murad, Shahnaz. / Platelet-activating factor (PAF) receptor binding activity of the roots of Enicosanthellum pulchrum. In: Pharmaceutical Biology. 2012 ; Vol. 50, No. 3. pp. 284-290.
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