PARTITIONING OF IONIZING MOLECULES BETWEEN AQUEOUS BUFFERS AND PHOSPHOLIPID-VESICLES
PARTITIONING OF IONIZING MOLECULES BETWEEN AQUEOUS BUFFERS AND PHOSPHOLIPID-VESICLES
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DOI：
10.1002/jps.2600841008
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发表时间：
1995-10-01
影响因子：
3.8
通讯作者：
MANNERS, CN
中科院分区：
文献类型：
--
作者：
AUSTIN, RP;DAVIS, AM;MANNERS, CN
用超滤方法研究了四种电离分子在二肉豆基磷脂酰胆碱（DMPC）单层小囊泡和水缓冲液之间的分布与pH的关系。结果表明，在标准的1-辛醇-水体系中观察到的ph分布行为并不总是适用于模型膜系统，因为一些分子的带电荷形式能够分裂成磷脂双分子层。进一步表明，这些带电物质进入双分子层并不是离子配对的结果。这些结果澄清了有关质子化胺具有惊人的高膜亲和性的报道，并讨论了这些发现对药物设计的影响。
The distribution of four ionizing molecules between small unilamellar vesicles of dimyristoylphosphatidylcholine (DMPC) and aqueous buffers has been studied as a function of pH using an ultrafiltration method. The results show that pH-distribution behavior observed in the standard 1-octanol-water system does not always apply in model membrane systems, since the charged form of some molecules are able to partition into a phospholipid bilayer. It was further shown that the partitioning of these charged species into the bilayer is not as a consequence of ion pairing. The results clarify reports suggesting that protonated amines have a surprisingly high membrane affinity, and the implications of these findings for drug design are discussed.