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-β-ribofuranosylbrunfelsamidine as the active component with a tryptase IC₅₀ of 3 μM. Brunfelsamidine was also isolated, but was only weakly active.

References

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