A new cacospongionolide inhibitor of human secretory phospholipase A2 from the Tyrrhenian sponge Fasciospongia cavernosa and absolute configuration of cacospongionolides

被引:33
作者
De Rosa, S
Crispino, A
De Giulio, A
Iodice, C
Benrezzouk, R
Terencio, MC
Ferrándiz, L
Alcaraz, MJ
Payá, M
机构
[1] CNR, Ist Chim Mol Interesse Biol, I-80072 Napoli, Italy
[2] Univ Valencia, Fac Farm, Dept Pharmacol, Valencia 46100, Spain
来源
JOURNAL OF NATURAL PRODUCTS | 1998年 / 61卷 / 07期
关键词
D O I
10.1021/np980122t
中图分类号
Q94 [植物学];
学科分类号
071001 ;
摘要
A new inhibitor of human secretory phospholipase A(2) (PLA(2)), cacospongionolide E (4a), has been isolated from the Tyrrhenian sponge Fasciospongia cavernosa. The structure was proposed on the basis of spectroscopic data and by chemical transformations. The absolute configuration of cacospongionolides 2a-4a was established using the modified Mosher's method. Cacospongionolide E was the most potent inhibitor toward human synovial PLA(2), showing higher potency than the reference compound manoalide and exerting no signs of toxicity on human neutrophils. It showed high activity in the Artemia salina bioassay and moderate toxicity in the fish (Gambusia affinis) lethality assay.
引用
收藏
页码:931 / 935
页数:5
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