Structures of new amphidinols with truncated polyhydroxyl chain and their membrane-permeabilizing activities

Structures of new amphidinols with truncated polyhydroxyl chain and their membrane-permeabilizing activities
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DOI:
10.1016/j.bmc.2006.06.012
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发表时间:
2006-10-01
影响因子:
3.5
通讯作者:
Fujita, Tsuyoshi
Fujita, Tsuyoshi
中科院分区:
医学3区
文献类型:
--
作者:
Morsy, Nagy;Houdai, Toshihiro;Fujita, Tsuyoshi

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从克氏前沟藻(Amphidiniumklebsii)中分离到两个新的前沟醇同系物(AM 14和AM 15)。2D NMR和碰撞诱导解离MS/MS的基础上的结构进行了阐明,原来是AM 7的密切相关的同系物。其弱的膜破坏活性表明疏水多烯链是有效的生物活性所必需的。然后使用具有不同链长的AM同系物检查多羟基部分的结构-活性关系,表明由AM形成的通道/损伤的孔径大小不受多羟基链长度的影响。(c)2006爱思唯尔有限公司保留所有权利。
Two new homologues of amphidinols (AM14 and AM15) were isolated from the cultured dinoflagellate Amphidinium klebsii. The structures were elucidated on the basis of 2D NMR and collision-induced dissociation MS/MS and turned out to be closely related homologues of AM7. Their weak membrane-disrupting activity indicates that the hydrophobic polyene chain is essential for the potent biological activities. Structure-activity relationship for the polyhydroxyl part was then examined with use of AM homologues possessing various chain lengths, indicating that the pore size of the channel/lesion formed by AMs was not greatly affected by the length of the polyhydroxyl chain. (c) 2006 Elsevier Ltd. All rights reserved.