Pyrrole carboxamidine tryptase inhibitors from Leptonychia pubescens.

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.

• Authors: Lay Kien Yang, Sok Peng Ng, Horst Flotow, K Yoganathan, B O Daramola, D Doel Soejarto, Antony D Buss, Mark S Butler
• Journal: Planta medica (Planta Med) Vol. 71 Issue 11 Pg. 1071-2 (Nov 2005) ISSN: 0032-0943 [Print] Germany
• PMID: 16320213 (Publication Type: Journal Article)

Chemical References

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

Topics

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