Search for Anti-intlammatory Agents from Marine Invertebrates

从日本太平洋沿岸沿着的不同地方采集了108份海绵、腔肠动物、苔藓虫和被囊动物标本，并对猪胰腺磷脂酶A_2进行了抑制试验。共采集到46个标本，其中海绵动物36个，柳珊瑚6个，苔藓动物3个，被囊动物1个。从活性标本的出现率和活性大小来看，海绵是分离磷脂酶A_2抑制剂的最佳材料，从筛选活性较高的3个海绵中，分离出5个活性物质和磷脂混合物，作为磷脂酶A_2抑制剂。盘皮素A-D是从盘皮属海绵中获得的，IC为<50>0.6-1.7 μ g/ml。偶然地，discodermin A在小鼠中显示出体内抗肿瘤活性。Palinurin是从纪伊半岛的Ircinia sp.中分离得到的。对磷脂酶A_2的抑制IC_（<50>5.0）× 10 ~ 4 μ <-5>M。值得注意的是，从未鉴定的海绵中分离的磷脂显示出显著的活性。

A total of 108 specimens of marine sponges, coelenterates, bryozoans, and tunicates were collected from various places along Pacific coasts of Japan and tested for inhibition of phospholipase A_2 derived from porcine pancreas. A total of 46 specimens, including 36 specimens of sponges, 6 gorgonians, 3 bryozoans and 1 tunicate showed activity. Judging from incidence of active specimens and magnitude of activity, sponges were most suitable tangent for isolation of antiinflammatory agents.From three sponges which were highly active in the screening tests, five active substances together with phospholipid mixture were obtained as phospholipase A_2 inhibitors. Discodermins A-D have been obtained from a sponge of the genus iscodermia and showed IC_<50> 0.6-1.7 mug/ml. Accidentally, discodermin A showed in vivo antiinflammatory activity in mice. Palinurin was isolated from Ircinia sp. collected off the Kii Peninsula. It inhibited phospholipase A_2 with an IC_<50> 5.0 x 10^<-5> M. It is noted that phospholipids isolated an unidentified sponge showed a remarkable activity.