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

Takashi KURITA, Yoshiko KOSEMURA, Konosuke KUMAKURA, Hisataka KASAI†† and Hisashi ITO*

Department of Chemistry, College of Science and Engineering, Aoyama Gakuin University; 6-16-1, Chitosedai, Setagaya-ku, Tokyo 157-8572 Japan
Life Science Institute, Sophia University; 7-1, Kioi-cho, Chiyoda-ku, Tokyo 102-8554 Japan
†† Tokyo Metropolitan University of Health Sciences; 7-2-10, Higashiogu, Arakawa-ku, Tokyo 116-8551 Japan

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 8 MP 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 α-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.

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