使用聚亚乙基亚胺的油酸衍生物增强 siRNA 传递。
Enhanced siRNA delivery using oleic acid derivative of polyethylenimine.
机构信息
Institute of Life Sciences, Jilin University, Changchun, Jilin, PR China.
出版信息
Anticancer Res. 2012 Apr;32(4):1267-71.
BACKGROUND
RNA interference has promising therapeutic potential. However, safe and efficacious delivery systems are necessary for its application in the clinic.
MATERIALS AND METHODS
An oleic acid (OA) derivative of branched polyethylenimine (PEI, M.W. 2000 Da), PEI-OA, was synthesized and evaluated for small interfering RNA (siRNA) delivery in SK-HEP-1 liver cancer cells stably transfected with luciferase. The physiochemical properties of PEI-OA/siRNA complexes, their cellular uptake, gene silencing activity based on luciferase reporter gene down-regulation, and cytotoxicity were investigated.
RESULTS
PEI-OA complexes effectively delivered siRNA into SK-HEP-1 cells and efficiently induced down-regulation of luciferase reporter gene expression. Compared with free siRNA and PEI/siRNA, PEI-OA/siRNA was significantly more effective, reducing luciferase activity by ~50%.
CONCLUSION
PEI-OA warrants further evaluation for therapeutic delivery of siRNA.
背景
RNA 干扰具有有前景的治疗潜力。然而，安全有效的输送系统对于其在临床上的应用是必要的。
材料与方法
合成了一种油酸（OA）修饰的支化聚乙烯亚胺（PEI，MW2000Da），PEI-OA，并在稳定转染荧光素酶的 SK-HEP-1 肝癌细胞中评价其用于小干扰 RNA（siRNA）的传递。研究了 PEI-OA/siRNA 复合物的物理化学性质、细胞摄取、基于荧光素酶报告基因下调的基因沉默活性以及细胞毒性。
结果
PEI-OA 复合物能有效将 siRNA 递送至 SK-HEP-1 细胞，并能有效诱导荧光素酶报告基因表达下调。与游离 siRNA 和 PEI/siRNA 相比，PEI-OA/siRNA 更为有效，使荧光素酶活性降低约 50%。
结论
PEI-OA 值得进一步评估用于 siRNA 的治疗性传递。
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