Search for Anti-intlammatory Agents from Marine Invertebrates

本文在日本太平洋沿岸收集了108种海绵动物、腔肠动物、苔藓虫和被囊动物，对猪胰腺磷脂酶A_2进行了抑制试验。共有46个标本显示活性，其中海绵类36个，柳珊瑚类6个，苔藓虫类3个，被囊动物1个。从活性标本的发生率和活性程度来看，海绵是最适合分离抗炎药物的切线。从3个筛选试验中高活性的海绵中，得到5种活性物质和磷脂混合物作为磷脂酶A_2抑制剂。从iscodermia属海绵中分离得到盘皮素a - d， IC_<50> 0.6 ~ 1.7 mug/ml。偶然地，discodermin A在小鼠体内显示出抗炎活性。Palinurin是从Kii半岛采集的Ircinia sp.中分离得到的。其抑制磷脂酶A_2的IC_<50> 5.0 × 10^<-5> M.注意到从未确定的海绵中分离的磷脂具有显著的活性。

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.