Enhancement of Hemolytic and Catecholamine Releasing Activities of Mastoparan by the Dendrimeric Formation

  • KURITA Takashi
    Department of Chemistry, College of Science and Engineering, Aoyama Gakuin University
  • KOSEMURA Yoshiko
    Department of Chemistry, College of Science and Engineering, Aoyama Gakuin University
  • KUMAKURA Konosuke
    Life Science Institute, Sophia University
  • KASAI Hisataka
    Tokyo Metropolitan University of Health Sciences
  • ITO Hisashi
    Department of Chemistry, College of Science and Engineering, Aoyama Gakuin University

Bibliographic Information

Other Title
  • マストパラン分子の樹状化による赤血球溶血作用とカテコールアミン放出作用の高活性化
  • マストパラン ブンシ ノ ジュジョウカ ニ ヨル セッケッキュウ ヨウ ケツ サヨウ ト カテコールアミン ホウシュツ サヨウ ノ コウカッセイカ

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Abstract

As a trial to enhance activity of bioactive peptide, the dendrimeric formation of mastoparan (MP), a wasp venom toxic peptide, was carried out. We synthesized dendrimeric MPs consisting of 2, 4 and 8MP molecules formed on a branching lysine-core, and examined the hemolytic and catecholamine releasing activities and the circular dichroism. The activities of dendrimeric MPs were higher than that of MP and the a-helical contents increased with the increase of the number of branches in the dendrimers. The most potent dendrimer in hemolytic activity, approximately 8000 times as active as MP, was octameric MP which took 35% α-helical content even in an aqueous buffer. Our results indicated that the dendrimeric formation of an amphipathic peptide should be a useful way to obtain highly active peptide as shown already in immunogenicity.

Journal

  • NIPPON KAGAKU KAISHI

    NIPPON KAGAKU KAISHI 1999 (8), 545-552, 1999-08-10

    The Chemical Society of Japan

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