The bound states of amphipathic drugs in lipid bilayers: Study of curcumin
The bound states of amphipathic drugs in lipid bilayers: Study of curcumin
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DOI：
10.1529/biophysj.108.133736
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发表时间：
2008-09-01
影响因子：
3.4
通讯作者：
Huang, Huey W.
中科院分区：
文献类型：
--
作者：
Sun, Yen;Lee, Chang-Chun;Huang, Huey W.
药物-膜相互作用是众所周知的，但知之甚少。在这里，我们描述了双重测量膜厚度的变化和膜面积的变化，由于结合的两亲性药物姜黄素。结合的结果使我们能够分析药物与脂质双层的结合状态，一个在水膜界面上，另一个在双层的烃区域中。这两种状态之间的过渡强烈影响的弹性能量膜变薄（或等效地，面积拉伸）所造成的界面结合。数据很好地描述了一个两状态模型，包括这个弹性能量。姜黄素的结合遵循两亲肽与膜结合的常见模式，表明姜黄素的结合状态是两亲药物的典型结合状态。
Drug-membrane interactions are well known but poorly understood. Here we describe dual measurements of membrane thickness change and membrane area change due to the binding of the amphipathic drug curcumin. The combined results allowed us to analyze the binding states of a drug to lipid bilayers, one on the water-membrane interface and another in the hydrocarbon region of the bilayer. The transition between the two states is strongly affected by the elastic energy of membrane thinning (or, equivalently, area stretching) caused by interfacial binding. The data are well described by a two-state model including this elastic energy. The binding of curcumin follows a common pattern of amphipathic peptides binding to membranes, suggesting that the binding states of curcumin are typical for amphipathic drugs.