Title of article :
Depsipeptides from a Guamanian marine cyanobacterium, Lyngbya bouillonii, with selective inhibition of serine proteases
Author/Authors :
Rubio، نويسنده , , Brent K. and Parrish، نويسنده , , Stephen M. and Yoshida، نويسنده , , Wesley and Schupp، نويسنده , , Peter J. and Schils، نويسنده , , Tom M. Williams، نويسنده , , Philip G.، نويسنده ,
Abstract :
Bouillomides A (1) and B (2) are two depsipeptide analogues of dolastatin 13. Isolated from a Guamanian sample of Lyngbya bouillonii, the planar structures were elucidated on the basis of HR-ESI-MS and NMR data, while the absolute configurations were determined by employing functional group conversions, modified Marfey’s analysis, and detailed analyses of ROESY correlations. Compounds 1 and 2 selectively inhibited serine proteases elastase (IC50 = 1.9 μM for both) and chymotrypsin (IC50 = 0.17 and 9.3 μM, respectively) while showing no inhibition of trypsin (IC50 >100 μM).
