Weissig V, Lasch J, Erdos G, Meyer H W, Rowe T C, Hughes J
Center for Imaging and Pharmaceutical Research, Massachusetts General Hospital, Charlestown, MA, USA.
Pharm Res. 1998 Feb;15(2):334-7. doi: 10.1023/a:1011991307631.
Dequalinium, a drug known for over 30 years, is a dicationic amphiphile compound resembling bolaform electrolytes. The purpose of our work was to determine the state of aggregation of dequalinium in aqueous medium and to investigate both, its ability to bind DNA and its potential to serve as a novel non-viral transfection vector.
The form of aggregation was determined employing electron microscopic techniques. The DNA binding capacity of dequalinium was assayed using SYBR Green I stain. For in vitro cell transfection experiments plasmid DNA encoding for firefly luciferase was used.
Dequalinium forms in aqueous medium liposome-like aggregates, which we term DQAsomes. These dequalinium vesicles bind DNA and they are able to transfect cells in vitro with an efficiency comparable to Lipofectin.
Based on the intrinsic properties of dequalinium such as the in vivo selectivity for carcinoma cells and selective accumulation in mitochondria we propose DQAsomes as a novel and unique drug and gene delivery system.
地喹氯铵是一种已为人所知30多年的药物，是一种类似于bolaform电解质的双阳离子两亲化合物。我们研究的目的是确定地喹氯铵在水性介质中的聚集状态，并研究其与DNA结合的能力以及作为新型非病毒转染载体的潜力。
采用电子显微镜技术确定聚集形式。用地喹氯铵的DNA结合能力使用SYBR Green I染色进行测定。体外细胞转染实验使用编码萤火虫荧光素酶的质粒DNA。
地喹氯铵在水性介质中形成脂质体样聚集体，我们将其称为地喹氯铵脂质体。这些地喹氯铵囊泡结合DNA，并且它们能够在体外转染细胞，效率与Lipofectin相当。
基于地喹氯铵的固有特性，如对癌细胞的体内选择性和在线粒体中的选择性积累，我们提出地喹氯铵脂质体作为一种新型且独特的药物和基因递送系统。
