Hasegawa Seiji, Hirashima Naohide, Nakanishi Mamoru
Graduate School of Pharmaceutical Sciences, Nagoya City University, Tanabe-dori, Mizuho-ku, 467-8603, Nagoya, Japan.
Bioorg Med Chem Lett. 2002 May 6;12(9):1299-302. doi: 10.1016/s0960-894x(02)00119-1.
To develop the efficient non-viral vector for gene delivery, we compared transfection activities of cationic cholesterol derivatives. We found that the stability of the liposome-DNA complex in the presence of endosome deeply related to the transfection efficiency. We also found that the introduction of a hydrophilic group to the amino terminal of the cholesterol derivative decreased stability and facilitated the release of DNA from the endosome, resulting in higher transfection efficiency.
为了开发用于基因递送的高效非病毒载体，我们比较了阳离子胆固醇衍生物的转染活性。我们发现，内体存在时脂质体 - DNA复合物的稳定性与转染效率密切相关。我们还发现，在胆固醇衍生物的氨基末端引入亲水基团会降低稳定性并促进DNA从内体释放，从而导致更高的转染效率。
