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β-内酰胺杯芳烃衍生物与模型真核膜的相互作用影响 PLA2 的活性。

Interaction of a β-lactam calixarene derivative with a model eukaryotic membrane affects the activity of PLA2.

机构信息

Department of Physical Chemistry and Electrochemistry, Faculty of Chemistry, Jagiellonian University, ul. R. Ingardena 3, 30-060 Krakow, Poland.

出版信息

Colloids Surf B Biointerfaces. 2013 Mar 1;103:217-22. doi: 10.1016/j.colsurfb.2012.10.045. Epub 2012 Nov 2.

DOI:10.1016/j.colsurfb.2012.10.045
PMID:23201740
Abstract

In this research, the interaction between a membrane phospholipid, 1,2-dilauroyl-sn-glycero-3-phosphocholine (DLPC), and a p-tert-butylcalix[4]arene derivative bearing 6-aminopenicillanic acid (Calix), conceived as a possible drug carrier, was studied. The Langmuir film balance technique was used to measure surface pressure and electrical surface potential of pure and mixed Calix/DLPC monolayers spread on water at different temperatures. Phospholipase A2 (PLA2) activity was used as well to detect the impact of the calixarene derivative on the monolayer properties. Interaction between the molecules in mixed monolayers has been described quantitatively using thermodynamic functions. Interestingly, low amounts of Calix introduce ordering in the lipid film. This effect may be analogous to that of cholesterol interacting with phospholipids. A lower activity of PLA2 observed with the Calix/DLPC films compared to pure DLPC may be related to structural modifications of the mixed systems.

摘要

在这项研究中,研究了一种膜磷脂 1,2-二月桂酰基-sn-甘油-3-磷酸胆碱(DLPC)与一种带有 6-氨基青霉素酸(Calix)的 p-叔丁基杯[4]芳烃衍生物之间的相互作用,该衍生物被设想为一种可能的药物载体。使用 Langmuir 膜天平技术测量了在不同温度下在水上展开的纯和混合 Calix/DLPC 单层的表面压力和电表面电势。还使用磷脂酶 A2(PLA2)活性来检测杯芳烃衍生物对单层性质的影响。使用热力学函数对混合单层中分子之间的相互作用进行了定量描述。有趣的是,少量的 Calix 会使脂质膜有序化。这种效应可能类似于胆固醇与磷脂的相互作用。与纯 DLPC 相比,用 Calix/DLPC 薄膜观察到 PLA2 的活性较低,这可能与混合体系的结构修饰有关。

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