Amphotericin B dimers with bisamide linkage bearing powerful membrane-permeabilizing activity |
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Authors: | Yamaji Nahoko Matsumori Nobuaki Matsuoka Shigeru Oishi Tohru Murata Michio |
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Affiliation: | Department of Chemistry, Graduate School of Science, Osaka University, 1-16 Machikaneyama, Toyonaka, Osaka 560-0043, Japan. |
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Abstract: | [structure: see text] Covalently linked dimers of amphotericin B were prepared by cross-linking its carboxylic acid. Among these, a dimer with a linkage of 1,6-hexanediamine revealed potent hemolytic activity (EC50, 0.25 microM) while its N-acetyl derivative gave rise to large K+ ion flux in phosphatidylcholine liposomes, regardless of the presence or absence of sterols, suggesting that the dimers may serve as a tool for elucidating the structure of the ion channel assemblage formed by amphotericin B. |
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