Search for Anti-intlammatory Agents from Marine Invertebrates

从海洋无脊椎动物中寻找抗炎剂

• 批准号: 01560218
• 负责人: FUSETANI Nobuhiro
• 金额: $ 1.34万
• 依托单位: University of Tokyo
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for General Scientific Research (C)
• 财政年份: 1989
• 资助国家: 日本
• 起止时间: 1989 至 1990
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-01560218/
• 关键词: marine invertebrates; antiinflammatory; phospholipase A_2; enzyme inhibitor; marine sponges; cyclic peptide; discodermin; furanosesterterpene; 抗炎症剤; ホスホリパ-ゼA_2; リン脂質; 医薬素材; discodermin

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.

从日本太平洋沿岸的各个地方收集了108个海洋海绵，腔植物，bryozoans和束缚的标本，并测试了抑制源自猪胰腺的磷脂酶A_2。共有46个标本，包括36个标本的海绵，6个Gorgonians，3个bryozoans和1张皮曲张，显示了活性。从活性标本的发生率和活性大小的发生率来看，海绵是最适合分离抗炎药的切线。从三个在筛选试验中具有高活性的海绵，将五种与磷脂混合物一起作为磷脂酶A_2抑制剂获得的五种活性物质。 dindererins A-D已从等性属的海绵中获得，并显示IC_ <50> 0.6-1.7杯/ml。偶然的是，椎间硬皮蛋白A在小鼠中表现出体内抗炎活性。从Ircinia sp。从KII半岛收集。它抑制具有IC_ <50> 5.0 x 10^<-5>的磷脂酶A_2。据注意，磷脂分离出一个未鉴定的海绵显示出了显着的活性。

项目成果

Nobuhiro Fusetani: "Research toward“Drugs from the Sea"" New J.Chem.14. 721-728 (1990)

Nobuhiro Fusetani：““来自海洋的药物”的研究”New J.Chem.14（1990）。

Nobuhiro Fusetani: "Research toward "Drugs from the sea"" New J. Chem. 14(10). 721-728 (1990)

Nobuhiro Fusetani：“对“来自海洋的药物”的研究”New J. Chem。

Nobuhiro Fusetani: "Research toward“Drugs from the Sea"" New J.Chem.

Nobuhiro Fusetani：“对“来自海洋的药物”的研究”New J.Chem。

Nobuhiro Fusetani: "Research toward “Drugs from the Sea"" New J.Chem.14. 721-728 (1990)

Nobuhiro Fusetani：“对“来自海洋的药物”的研究”New J.Chem.14 (1990)。