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1992 Fiscal Year Final Research Report Summary

Search for serine protease inhibitors from marine invertebrates.

Research Project

Project/Area Number 03454088
Research Category

Grant-in-Aid for General Scientific Research (B)

Allocation TypeSingle-year Grants
Research Field Fisheries chemistry
Research InstitutionUniversity of Tokyo

Principal Investigator

FUSETANI Nobuhiro  University of Tokyo, Faculty of Agriculture, Professor, 農学部, 教授 (70012010)

Co-Investigator(Kenkyū-buntansha) MATSUNAGA Shigeki  University of Tokyo, Faculty of Agriculture, Assistant, 農学部, 助手 (60183951)
Project Period (FY) 1991 – 1992
KeywordsMarine Invertebrates / Protease Inhibitors / Thrombin / Trypsin / Serine Proteases / Marine Sponges / Nazumamide A / Toxadocial A
Research Abstract

Marine sponges (273 samples), coelenterates (32 samples), bryozoans (7 samples) and tunicates (26 samples) were collected from the Izu Peninsula, Hachijo Island, Kyushu and Shikoku. The hot methanol extracts of samples were partitioned between H_2O and CHCl_3 to give organic and aqueous layers. Each layer was assayed for inhibitory activities against thrombin and trypsin. Forty-five samples of sponges, 5 of coelenterates and 5 of tunicates were active. Genrally, activities were found in the aqueous layers, but some organic layers showed activities.
One of active sponge sample, Theonella swinhoei was extracted, and the extract was fractionated to obtain a thrombin inhibitor named nazumamide A, which inhibited thrombin at an IC_<50> of 2.8 mug/mL. Amino acids analysis and spectral analyses including 2D NMR and FABMS led to a tetrapeptide possessing the N-2,5-dihydroxybenzoate terminus (1).
Another active sponge Toxadocia cylindrica was similarly processed to yield a thrombin inhibitor, toxadocial A, which inhibited thrombin at an IC_<50> of 6.5 mug/mL. The structure elucidation was carried out by means of spectral analyses and chemical transformation to obtain an unusual tetrasulfated aldehyde as shown (2)

  • Research Products

    (4 results)

All Other

All Publications (4 results)

  • [Publications] Nobuhiro Fusetani: "Nazumamide A,a Thrombin-Inhibitory Tetrapeptide,from a Manne Sponge,Theonella sp." Tetrahedron Letters. 32. 7073-7074 (1991)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] Youichi Nakao: "ToxadocialA:A Novel Thrombin Inhibitor from the Marine Sponge Toxadocia cylindrica" Tetrahedron Letters.

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] Nobuhiro Fusetani: "Nazumamide A, a Thrombin-Inhibitory Tetrapeptide, from a Marine Sponge, Theonella sp." Tetrahedron Letters. 32. 7073-7074 (1991)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] Youichi Nakao: "Toxadocial A: A Novel Thrombin Inhibitor from the Marine Sponge Toxadocia cylindrica" Tetrahedron Letters.

    • Description
      「研究成果報告書概要(欧文)」より

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Published: 1994-03-24  

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