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-β-ribofuranosylbrunfelsamidine as the active component with a tryptase IC50 of 3 μM. Brunfelsamidine was also isolated, but was only weakly active.
References
-
1
Cairns J A.
Inhibitors of mast cell tryptase beta as therapeutics for the treatment of asthma and inflammatory disorders.
Pulm Pharmacol Ther.
2005;
18
55-66
-
2
Murakami Y, Takei M, Shindo K, Kitazume C, Tanaka J, Higa T. et al .
Cyclotheonamide E4 and E5, new potent tryptase inhibitors from an Ircinia species of sponge.
J Nat Prod.
2002;
65
259-61
-
3
Lloyd H A, Fales H M, Goldman M E, Jerina D M, Plowman T, Schultes R E.
Brunfelsamidine: a novel convulsant from the medicinal plant Brunfelsia grandiflora
.
Tetrahedron Lett.
1985;
26
2623-4
-
4
Buschi C A, Pomilio A B.
Pyrrole-3-carbamidine: a lethal principle from Nierembergia hippomanica
.
Phytochemistry.
1987;
26
863-5
-
5
Ramasamy K, Robins R K, Revankar G R.
Synthesis of brunfelsamidine ribonucleoside and certain related compounds by the stereospecific sodium salt glycosylation procedure.
Nucleosides Nucleotides.
1988;
7
385-92
-
6
Bock K, Pedersen C.
13C N.M.R. spectroscopy of monosaccharides.
Adv Carbohydr Chem Biochem.
1983;
41
44-66
-
7
Martin G E, Hadden C E.
Long-range 1H-15N heteronuclear shift correlation at natural abundance.
J Nat Prod.
2000;
63
543-85
Mark S. Butler
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