Pyrrole carboxamidine tryptase inhibitors from Leptonychia pubescens.
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.
Yang
Lay Kien
LK
MerLion Pharmaceuticals, Singapore.
Ng
Sok Peng
SP
Flotow
Horst
H
Yoganathan
K
K
Daramola
B O
BO
Soejarto
D Doel
DD
Buss
Antony D
AD
Butler
Mark S
MS
D006801:Humans; D008168:Lung / Q000201:enzymology; D019660:Malvaceae / Q000737:chemistry*; D015394:Molecular Structure; D009005:Monosaccharides / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D024301:Plant Bark / Q000737:chemistry; D010936:Plant Extracts / Q000737:chemistry; D018517:Plant Roots / Q000737:chemistry; D012697:Serine Endopeptidases / Q000378:metabolism*; D015842:Serine Proteinase Inhibitors / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D053802:Tryptases
C507336:1-beta-ribofuranosylbrunfelsamidine; D009005:Monosaccharides; D010936:Plant Extracts; D015842:Serine Proteinase Inhibitors; D012697:Serine Endopeptidases; D053802:Tryptases