Takei M, Umeyama A, Shoji N, Arihara S, Endo K
Forschungsinstitut Borstel, Germany.
J Pharm Sci. 1995 Feb;84(2):228-30. doi: 10.1002/jps.2600840222.
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.
冲绳海洋海绵硬壳笔螺（Penares incrustans）的成分海胆甾醇和海胆甾酮能剂量依赖性地抑制抗IgE诱导的大鼠肥大细胞组胺释放。抑制抗IgE诱导的组胺释放50%所需的海胆甾醇和海胆甾酮浓度（IC50）分别为0.5和1.5微摩尔。两种化合物均能剂量依赖性地抑制磷脂酶A2（PLA2）活性。此外，它们还抑制抗IgE诱导的大鼠肥大细胞释放[3H]花生四烯酸。这些结果表明，这些化合物抑制抗IgE诱导的组胺释放的机制是通过抑制PLA2。
