Departments of Biomedical Engineering and Chemistry, Boston University , Boston, Massachusetts 02215, United States.
Bioconjug Chem. 2011 Apr 20;22(4):690-9. doi: 10.1021/bc1004526. Epub 2011 Apr 1.
A series of charge-reversal lipids were synthesized that possess varying chain lengths and end functionalities. These lipids were designed to bind and then release DNA based on a change in electrostatic interaction with DNA. Specifically, a cleavable ester linkage is located at the ends of the hydrocarbon chains. The DNA release from the amphiphile was tuned by altering the length and position of the ester linkage in the hydrophobic chains of the lipids through the preparation of five new amphiphiles. The amphiphiles and corresponding lipoplexes were characterized by DSC, TEM, and X-ray, as well as evaluated for DNA binding and DNA transfection. For one specific charge-reversal lipid, stable lipoplexes of approximately 550 nm were formed, and with this amphiphile, effective in vitro DNA transfection activities was observed.
合成了一系列带有不同链长和端基官能团的电荷反转脂质。这些脂质的设计目的是基于与 DNA 的静电相互作用的变化来结合和释放 DNA。具体而言，可裂解的酯键位于烃链的末端。通过制备五种新的两亲分子，通过改变脂质疏水链中酯键的长度和位置来调节 DNA 从两亲分子中的释放。通过 DSC、TEM 和 X 射线对两亲分子和相应的脂质体进行了表征，并评估了它们与 DNA 的结合和 DNA 转染。对于一种特定的电荷反转脂质，形成了约 550nm 的稳定脂质体，并且使用这种两亲分子观察到有效的体外 DNA 转染活性。
