Pyrrole carboxamidine tryptase inhibitors from Leptonychia pubescens

Planta Med. 2005 Nov;71(11):1071-2. doi: 10.1055/s-2005-873111.

Abstract

The root and stem bark extracts of a Nigerian sample of Leptonychia pubescens Keay (Sterculiaceae) were found to inhibit the serine protease tryptase, a potential therapeutic target for the treatment of asthma and chronic obstructive pulmonary disease (COPD). Bioassay-guided isolation led to the identification of 1-beta-ribofuranosylbrunfelsamidine as the active component with a tryptase IC (50) of 3 microM. Brunfelsamidine was also isolated, but was only weakly active.

MeSH terms

  • Humans
  • Lung / enzymology
  • Malvaceae / chemistry*
  • Molecular Structure
  • Monosaccharides / chemistry
  • Monosaccharides / isolation & purification
  • Monosaccharides / pharmacology*
  • Plant Bark / chemistry
  • Plant Extracts / chemistry
  • Plant Roots / chemistry
  • Serine Endopeptidases / metabolism*
  • Serine Proteinase Inhibitors / chemistry
  • Serine Proteinase Inhibitors / isolation & purification
  • Serine Proteinase Inhibitors / pharmacology*
  • Tryptases

Substances

  • 1-beta-ribofuranosylbrunfelsamidine
  • Monosaccharides
  • Plant Extracts
  • Serine Proteinase Inhibitors
  • Serine Endopeptidases
  • Tryptases