Department of Structural Biology and Biophysics, CNRS, Institut de Pharmacologie et de Biologie Structurale, 205 Route de Narbonne, F-31077 Toulouse, France.
Int J Pharm. 2012 Feb 14;423(1):134-43. doi: 10.1016/j.ijpharm.2011.05.024. Epub 2011 May 12.
The delivery of therapeutic molecules such as plasmid DNA in cells and tissues by means of electric fields holds great promise for anticancer treatment. To allow for their therapeutic action, the molecules have first to traverse the cell membrane. The mechanisms by which the electrotransferred pDNA interacts with and crosses the plasma membrane are not yet fully explained. The aim of this study is to unravel the role of cholesterol during gene electrotransfer in cells. We performed cholesterol depletion experiments and measured its effects on various steps of the electroporation process. The first two steps consisting of electropermeabilization of the plasma membrane and of pDNA interaction with it were not affected by cholesterol depletion. In contrast, gene expression decreased. Colocalization studies with endocytotic markers showed that pDNA is endocytosed with concomitant clathrin- and caveolin/raft-mediated endocytosis. Cholesterol might be involved in the pDNA translocation through the plasma membrane. This is the first direct experimental evidence of the occurrence of endocytosis in gene electrotransfer.
通过电场将治疗分子(如质粒 DNA)递送到细胞和组织中,为癌症治疗带来了很大的希望。为了发挥其治疗作用,这些分子首先必须穿过细胞膜。电转移的 pDNA 与质膜相互作用并穿过质膜的机制尚未完全解释清楚。本研究旨在揭示胆固醇在细胞基因电转移过程中的作用。我们进行了胆固醇耗竭实验,并测量了其对电穿孔过程中各个步骤的影响。前两个步骤包括质膜的电穿孔和 pDNA 与之相互作用不受胆固醇耗竭的影响。相比之下,基因表达减少了。与内吞作用标记物的共定位研究表明,pDNA 与网格蛋白和 caveolin/raft 介导的内吞作用一起被内吞。胆固醇可能参与了 pDNA 通过质膜的转运。这是基因电转移中发生内吞作用的第一个直接实验证据。