title: 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.affiliation: MerLion Pharmaceuticals, Singapore.
authors.forename: Lay Kien
authors.initials: LK
authors.lastname: Yang
authors.forename: Sok Peng
authors.initials: SP
authors.lastname: Ng
authors.forename: Horst
authors.initials: H
authors.lastname: Flotow
authors.forename: K
authors.initials: K
authors.lastname: Yoganathan
authors.forename: B O
authors.initials: BO
authors.lastname: Daramola
authors.forename: D Doel
authors.initials: DD
authors.lastname: Soejarto
authors.forename: Antony D
authors.initials: AD
authors.lastname: Buss
authors.forename: Mark S
authors.initials: MS
authors.lastname: Butler
mesh_terms: 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
chemical_list: C507336:1-beta-ribofuranosylbrunfelsamidine; D009005:Monosaccharides; D010936:Plant Extracts; D015842:Serine Proteinase Inhibitors; D012697:Serine Endopeptidases; D053802:Tryptases