Mechanism of inhibition of IgE-dependent histamine release from rat mast cells by penasterol and penasterone.
Penasterol and penasterone, constituents of the Okinawan marine sponge Penares incrustans, dose-dependently inhibited anti-IgE-induced histamine release from rat mast cells. The concentrations of penasterol and penasterone required for 50% inhibition of anti-IgE-induced histamine release (IC50) were 0.5 and 1.5 microM, respectively. Both compounds dose-dependently inhibited phospholipase A2 (PLA2) activity. Moreover, they inhibited anti-IgE-induced [3H]arachidonic acid from rat mast cells. These results suggest that the mechanism of inhibition by these compounds of the histamine release induced by anti-IgE was through the inhibition of PLA2.
Takei
M
M
Forschungsinstitut Borstel, Germany.
Umeyama
A
A
Shoji
N
N
Arihara
S
S
Endo
K
K
D000818:Animals; D001095:Arachidonic Acids / Q000378:metabolism; D006636:Histamine Release / Q000187:drug effects* / Q000502:physiology; D007073:Immunoglobulin E / Q000502:physiology*; D066298:In Vitro Techniques; D007810:Lanosterol / Q000031:analogs & derivatives* / Q000494:pharmacology; D008297:Male; D008407:Mast Cells / Q000187:drug effects / Q000201:enzymology / Q000378:metabolism*; D010741:Phospholipases A / Q000378:metabolism; D054467:Phospholipases A2; D051381:Rats; D017208:Rats, Wistar
D001095:Arachidonic Acids; C093431:penasterone; C093430:penasterol; D007810:Lanosterol; D007073:Immunoglobulin E; D010741:Phospholipases A; D054467:Phospholipases A2