Two new sesquiterpene cyclopentenones, dysidenones A and B (I, II), and a new sesquiterpene aminoquinone, dysidine (III), all contg. the same rearranged drimane skeleton, have been isolated from a Dysidea sp. sponge, along with bolinaquinone. The structures were established from 2D NMR data. Bolinaquinone, dysidine, and a 1:1 mixt. of dysidenones A and B significantly inhibited human synovial phospholipase A2 (PLA2) at 10 mM. Compd. III, which showed an IC50 value of 2.0 mM, exerted a higher potency and selectivity toward this enzyme than the ref. inhibitor manoalide. In addn., all of these compds. modulated at 10 mM other human leukocyte functions such as the degranulation process measured as elastase release and the superoxide prodn. measured by chemiluminescence.
New Sesquiterpene Derivatives from the Sponge Dysidea Species with a Selective Inhibitor Profile against Human Phospholipase A2 and Other Leukocyte Functions
D'AURIA, MARIA VALERIA
2001
Abstract
Two new sesquiterpene cyclopentenones, dysidenones A and B (I, II), and a new sesquiterpene aminoquinone, dysidine (III), all contg. the same rearranged drimane skeleton, have been isolated from a Dysidea sp. sponge, along with bolinaquinone. The structures were established from 2D NMR data. Bolinaquinone, dysidine, and a 1:1 mixt. of dysidenones A and B significantly inhibited human synovial phospholipase A2 (PLA2) at 10 mM. Compd. III, which showed an IC50 value of 2.0 mM, exerted a higher potency and selectivity toward this enzyme than the ref. inhibitor manoalide. In addn., all of these compds. modulated at 10 mM other human leukocyte functions such as the degranulation process measured as elastase release and the superoxide prodn. measured by chemiluminescence.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
