Hairpin conformation of amphidinols possibly accounting for potent membrane permeabilizing activities |
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Authors: | Toshihiro Houdai Nagy Morsy Masayuki Satake |
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Institution: | a Department of Chemistry, Graduate School of Science, Osaka University, 1-16 Machikaneyama, Toyonaka, Osaka 560-0043, Japan b Graduate School of Agricultural Science, Tohoku University, Tsutsumidori-Amemiya, Aoba-ku, Sendai 981-8555, Japan |
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Abstract: | Amphidinols are a unique dinoflagellate metabolite with potent antifungal activity. We examined membrane permeabilizing action by amphidinol analogues with structural variations in polyhydroxy and polyene moieties. Consequently, the polyene and polyhydroxy moieties turned out to play important roles in binding to lipid bilayer membrane and in forming ion-permeable pore/lesion across membrane, respectively. NMR-constrained modeling experiments have revealed for the fist time that amphidinols in membrane generally take a hairpin configuration, which plausibly accounts for their potent antifungal and other membrane permeabilizing activities. |
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Keywords: | Amphidinol membrane-permeabilization |
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