Download PDF
Planta Med 2002; 68(12): 1133-1134
DOI: 10.1055/s-2002-36343
Letter
© Georg Thieme Verlag Stuttgart · New York

In Vitro Inhibitory Effect of Rubraxanthone Isolated from Garcinia parvifolia on Platelet-Activating Factor Receptor Binding

Ibrahim Jantan1 , Mazura Md. Pisar1 , Muhammad Sum Idris2 , M. Taher2 , Rasadah Mat Ali3
  • 1Department of Pharmacy, Universiti Kebangsaan Malaysia, Kuala Lumpur, Malaysia
  • 2Department of Chemistry, Universiti Teknologi Malaysia, Johor Bahru, Malaysia
  • 3Medicinal Plant Division, Forest Research Institute Malaysia, Kepong, Malaysia
Further Information

Publication History

Received: April 5, 2002

Accepted: July 13, 2002

Publication Date:
20 December 2002 (online)

    Permissions and Reprints

Abstract

Rubraxanthone and isocowanol isolated from Garcinia parvifolia Miq. were investigated for their inhibitory effects on platelet-activating factor (PAF) binding to rabbit platelets using 3 H-PAF as a ligand. Rubraxanthone showed a strong inhibition with IC50 value of 18.2 μM. The IC50 values of macluraxanthone, 6-deoxyjacareubin, 2-(3-methylbut-2-enyl)-1,3,5-trihydroxyxanthone, 2-(3-methylbut-2-enyl)-1,3,5,6-tetrahydroxyxanthone and 1,3,5-trihydroxy-6,6′-dimethylpyrano(2′,3′:6,7)-4-(1,1-dimethylprop-2-enyl)-xanthone were also determined for comparison. In the course of our study on structure-activity relationship of xanthones, the results revealed that a geranyl group substituted at C-8 was beneficial to the binding while a hydroxylated prenyl group at C-4 resulted in a significant loss in binding to the PAF receptor.

References

  • 1 Braquet P, Tougui L, Shen T Y, Vargaftig B B. Perspective in platelet activating factor research.  Pharmacological Review. 1987;  39 97-145
    PubMedGoogle Scholar
  • 2 Mallet A T, Cunningham F M. Structural identification of PAF in psoriatic scale.  Biochemical Biophysical Research Communications. 1985;  126 192-8
    PubMedGoogle Scholar
  • 3 Vargaftig B B, Braquet P G. PAF-acether today: relevance for acute experimental anaphylaxis.  British Medical Bulletin. 1987;  43 312-35
    PubMedGoogle Scholar
  • 4 Kloprogge E, Akkerman N. Binding kinetic of PAF-acether (1-O-alkyl-2-acetyl-sn-glycero-3-phosphocholine) to intact human platelets.  Biochemical Journal. 1984;  233 901
    PubMedGoogle Scholar
  • 5 Goh S H, Jantan I, Gray A I, Waterman P G. Prenylated xanthones of Garcinia opaca .  Phytochemistry. 1992;  31 1383-6
    CrossrefPubMedGoogle Scholar
  • 6 Goh S H, Jantan I. A xanthone from Calophyllum inophyllum .  Phytochemistry. 1991;  30 366-7
    CrossrefPubMedGoogle Scholar
  • 7 Jantan I, Juriyati J, Warif N A. Inhibitory effects of xanthones on platelet activating factor receptor binding in vitro .  Journal of Ethnopharmacology. 2001;  75 287-90
    CrossrefPubMedGoogle Scholar
  • 8 Ampofo S A, Waterman P G. Xanthones from three Garcinia species.  Phytochemistry. 1989;  25 2351-5
    PubMedGoogle Scholar
  • 9 Valone F H, Coles E, Reinhold V R, Goetzl E J. Specific binding of phospholipid platelet-activating factor by human platelets.  Journal of Immunology. 1982;  129 1637-41
    PubMedGoogle Scholar

Ibrahim Jantan, PhD

Department of Pharmacy

Faculty of Allied Health Sciences

Universiti Kebangsaan Malaysia

Jalan Raja Muda Abdul Aziz

50300 Kuala Lumpur

Malaysia

Phone: +603-40405331

Fax: +603-26983271

Email: ibj@medic.ukm.my

      >