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Albumin enhances the diffusion of lipophilic drugs into the membrane bilayer

机译:白蛋白增强了亲脂性药物向膜双层的扩散

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摘要

In earlier work, we reported on the manner with which lipophilic drug molecules interact with the cell membrane in order to (a) enter the bilayer and laterally diffuse to their respective protein sites of action, or (b) penetrate this biological barrier to reach the cell interior. A remaining uncertainty is how lipophilic molecules reach the hydrophobic membrane core after traversing the aqueous medium and membrane polar surface. Here we present preliminary data using deuterium NMR, demonstrating the role of bovine serum albumin in facilitating this process. Our observation allows us to postulate a mechanism by which the passive transport of lipophilic ligands across the membrane can be greatly enhanced through the assistance of carrier proteins. (c) 2005 Elsevier Inc. All rights reserved.
机译:在较早的工作中,我们报道了亲脂性药物分子与细胞膜相互作用的方式,以便(a)进入双层并横向扩散至其各自的蛋白作用位点,或(b)穿透该生物屏障以达到单元内部。剩下的不确定因素是亲脂性分子在穿过水性介质和膜极性表面后如何到达疏水性膜核心。在这里,我们介绍使用氘核磁共振的初步数据,证明了牛血清白蛋白在促进这一过程中的作用。我们的观察结果允许我们推测一种机制,通过该机制可以通过载体蛋白的帮助大大增强亲脂性配体跨膜的被动转运。 (c)2005 Elsevier Inc.保留所有权利。

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