Mislick K A, Baldeschwieler J D, Kayyem J F, Meade T J
Division of Chemistry and Chemical Engineering, California Institute of Technology, Pasadena 91125, USA.
Bioconjug Chem. 1995 Sep-Oct;6(5):512-5. doi: 10.1021/bc00035a002.
We are utilizing the folate receptor for the intracellular delivery of DNA. In this study, a folate-poly-L-lysine (FPLL) conjugate was synthesized and equilibrated with plasmid DNA encoding the firefly luciferase gene. The FPLL-DNA complexes were added to KB cells treated with chloroquine. Luciferase activity of cells incubated with FPLL-DNA was 6-fold higher than of cells exposed to poly-L-lysine (PLL)-DNA. The addition of free folic acid competitively inhibited the enhancement of gene expression. Removal of chloroquine from the media significantly inhibited transfection efficiency of FPLL-DNA complexes. We conclude that FPLL-DNA complexes are delivered into KB cells via folate receptor-mediated endocytosis and likely follow a lysosomal pathway into the cytoplasm.
我们正在利用叶酸受体进行DNA的细胞内递送。在本研究中，合成了叶酸-聚-L-赖氨酸（FPLL）偶联物，并使其与编码萤火虫荧光素酶基因的质粒DNA平衡。将FPLL-DNA复合物添加到用氯喹处理的KB细胞中。与FPLL-DNA一起孵育的细胞的荧光素酶活性比暴露于聚-L-赖氨酸（PLL）-DNA的细胞高6倍。添加游离叶酸竞争性抑制基因表达的增强。从培养基中去除氯喹显著抑制了FPLL-DNA复合物的转染效率。我们得出结论，FPLL-DNA复合物通过叶酸受体介导的内吞作用被递送至KB细胞，并可能沿着溶酶体途径进入细胞质。
