Hexadecylphosphocholine interaction with lipid monolayers
Hexadecylphosphocholine interaction with lipid monolayers
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DOI：
10.1016/j.bbamem.2004.01.010
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发表时间：
2004-03-09
影响因子：
3.4
通讯作者：
Saint-Pierre-Chazalet, M
中科院分区：
文献类型：
--
作者：
Rakotomanga, M;Loiseau, PM;Saint-Pierre-Chazalet, M
磷脂类似物米替磷脂或十六烷基磷胆碱(HepC)是治疗由杜氏利什曼原虫引起的致死性内脏利什曼病(VL)的重要药物，特别是因为它具有口服途径的活性。在这项研究中，研究了丙型肝炎病毒与单层beta-pahnitoyl-gamma-oleyl-phosphatidylcholine(POPC)作为膜模型或甾醇(麦角甾醇或胆固醇)的相互作用。在25mN/m恒压下，吸附动力学研究表明，在临界胶束浓度(CMC)达到临界胶束浓度(CMC)之前，HepC分子以单体形式插入到脂类单层中。当HEPC的浓度高于CMC时，HEPC的胶束以单体群的形式部署在界面上，进入POPC或甾醇单分子层。对分散在气液界面上的HepC/(POPC或甾醇)混合物的研究表明，HepC与POPC之间只存在简单的混溶，而HepC与甾醇之间出现了高度的缩合，表明HepC与甾醇之间有很高的亲和力。此外，HEPC不作为洗涤剂干扰膜的完整性。(C)2004爱思唯尔B.V.保留所有权利。
The phospholipid analogue miltefosine or hexadecylphosphocholine (HePC) is a drug of high interest in the treatment for fatal visceral leishmaniasis (VL) due to Leishmania donovani particularly because of its activity by oral route. In this study, the interaction of HePC with a monolayer of beta-pahnitoyl-gamma-oleyl-phosphatidylcholine (POPC) as membrane model or sterol (ergosterol or cholesterol) was investigated. At a constant pressure of 25 mN/m, the adsorption kinetics of HePC into the monolayers showed that HePC molecules are inserted into the monolayer of lipids as monomers until the critical micellar concentration (CMC). At HePC concentrations superior to the CMC, the micelles of HePC are deployed at the interface as groups of monomers into the POPC or sterol monolayer. The study of mixture of HePC/(POPC or sterol), spread at the air-water interface, shows that a simple miscibility between HePC and POPC is observed, whereas a high condensation appears between HePC and sterols showing a high affinity between HePC and sterols. hi addition, HePC does not act as detergent disturbing membrane integrity. (C) 2004 Elsevier B.V. All rights reserved.