14-deoxyandrographolide as a platelet activating factor antagonist in bovine neutrophils

Planta Med. 2005 Jul;71(7):604-8. doi: 10.1055/s-2005-871264.

Abstract

14-Deoxyandrographolide (14-DAP) is a labdane diterpene isolated from Andrographis paniculata with previously reported calcium channel blocking activity. Its potential platelet activating factor (PAF) antagonistic activity in bovine neutrophils was assessed. 14-DAP, in concentrations between 10-100 microM, reduced the extracellular acidification rate and the intracellular alkalinization in a dose-dependent manner. In addition, 14-DAP reduced PAF-induced calcium flux in the presence of extracellular calcium, and tyrosine phosphorylation of a 44 kDa protein corresponding to the MAPK(ERK1). However, 14-DAP reduced the 3H-PAF binding with a Ki of 7.8 x 10 (- 9)M, and a Hill slope of 0.63, suggesting that there is more than one binding site for 14-DAP. We concluded that 14-DAP is an effective antagonist of PAF-mediated processes in bovine neutrophils, probably by virtue of its calcium channel blocking property.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Andrographis*
  • Animals
  • Calcium Channel Blockers / administration & dosage
  • Calcium Channel Blockers / pharmacology
  • Calcium Channel Blockers / therapeutic use
  • Cattle
  • Diterpenes / administration & dosage
  • Diterpenes / pharmacology*
  • Diterpenes / therapeutic use
  • Dose-Response Relationship, Drug
  • Mitogen-Activated Protein Kinases / metabolism
  • Neutrophils / drug effects*
  • Phosphorylation / drug effects
  • Phytotherapy*
  • Platelet Activating Factor / antagonists & inhibitors*

Substances

  • 14-deoxyandrographolide
  • Calcium Channel Blockers
  • Diterpenes
  • Platelet Activating Factor
  • Mitogen-Activated Protein Kinases