Controlled intracellular delivery of Multi-functional siRNA and gene silencing

siRNA-NES偶联物合成固相片段偶联可使K562细胞中bcr/abl基因的表达在200nM和50nM处分别抑制至8.3%和11.6%。研究还发现，siRNA和新型多肽（perfect）的复合物被吸收到细胞中，其效率与市售的脂肪感染试剂相当。siRNA-NES缀合物与perfect复合物可将bcr/abl基因的表达抑制至0.5%。siRNA和Pfect复合物无细胞毒性，对核酸酶消化有很强的抗性，半衰期超过48小时。

The expression of bcr/abl gene in K562 cells were suppressed to 8.3% at 200nM and 11.6 % at 50nM by siRNA-NES conjugates synthesized solid phase fragment coupling. It was also found that the complex of siRNA and novel peptides (Pfect) was taken up into cells with comparable efficiency to commercially available lipofection reagent. The expression of bcr/abl gene was suppressed to 0.5% by the complex of siRNA-NES conjugate and Pfect. The complex of siRNA and Pfect showed no cyto-toxicity and an intensive resistance against nucleases digestion to extend the half-life time over 48 hours.