Controlled intracellular delivery of Multi-functional siRNA and gene silencing

合成固相片段偶联的siRNA-NES偶联物可抑制K562细胞bcr/abl基因的表达，200 nm时为8.3%，50 nm时为11.6%。还发现，siRNA与新型多肽(Pfect)的复合体被带入细胞的效率与商品化的脂质体相当。SiRNA-NES偶联物与Pfect的复合物可将bcr/abl基因的表达抑制到0.5%。SiRNA与Pfect的复合体没有细胞毒性，对核酸酶的消化有强烈的抵抗力，半衰期延长到48小时以上。

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.