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.

从日本太平洋沿岸各地采集海绵、腔肠动物、苔藓虫和被囊动物共 108 个标本，并检测其对猪胰腺磷脂酶 A_2 的抑制作用。共有46个标本表现出活性，其中海绵36个、柳珊瑚6个、苔藓虫3个和被囊动物1个。从活性标本的发生率和活性大小来看，海绵最适合分离抗炎剂。从筛选试验中活性较高的三块海绵中，获得了五种活性物质与磷脂混合物作为磷脂酶A_2抑制剂。 Discodermins A-D已从iscodermia属的海绵中获得并显示出IC 50 0.6-1.7μg/ml。意外的是，discodermin A 在小鼠体内表现出抗炎活性。 Palinurin 是从 Ircinia sp. 中分离出来的。纪伊半岛附近采集的。它以IC_ 50 5.0×10 ^ -5 M抑制磷脂酶A_2。值得注意的是，从未鉴定的海绵中分离的磷脂显示出显着的活性。

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)。