Search for Anti-intlammatory Agents from Marine Invertebrates

从日本太平洋沿岸不同地方采集了108个海绵、腔肠动物、苔藓动物和被毛类标本，并对猪胰腺磷脂酶A_2进行了抑制试验。共有46个标本显示活性，包括36个海绵标本、6个柳珊瑚标本、3个苔藓动物标本和1个被囊动物标本。从活性样本的出现率和活性的大小来看，海绵最适合作为分离抗炎药物的切线，从筛选试验中活性较高的3种海绵中，筛选出5种活性物质和磷脂混合物作为磷脂酶A2抑制剂。Discodermins A-D是从软骨病属海绵中获得的，其IC_(50)为0.6-1.7µg/ml。偶然地，Discodermins A在小鼠体内显示出抗炎活性。从Ircinia sp.中分离到棕榈醛。在基伊半岛附近收集的。其抑制磷脂酶A_2的IC_(50)为5.0×10~(-5)~(-5)M。

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.