Antisense delivery using protamine-oligonucleotide particles.
Antisense delivery using protamine-oligonucleotide particles.
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DOI：
10.1093/nar/28.10.e45
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发表时间：
2000-05-15
影响因子：
14.9
通讯作者：
Zimmer, A
中科院分区：
文献类型：
--
作者：
Junghans, M;Kreuter, J;Zimmer, A
鱼精蛋白是一种多阳离子肽（分子量4000-4500），被认为是磷酸二酯反义寡核苷酸（ODNs）的潜在渗透增强剂。纳米颗粒形式的独特复合物自然形成，我们称之为“原体”。在胎牛血清和细胞培养液中考察了颗粒和结合到卵泡中的odn的稳定性。与游离odn相比，fitc标记的与鱼精蛋白结合的odn在人组织细胞淋巴瘤U 937细胞中的摄取增加。在使用ODNs对抗c- myc原癌基因的细胞增殖试验中，原粒显著降低细胞生长。
Protamine, a polycationic peptide (mol. wt 4000-4500), was evaluated as a potential penetration enhancer for phosphodiester antisense oligonucleotides (ODNs). Unique complexes in the form of nanoparticles were spontaneously formed, which we call 'proticles'. The stability of the particles and the ODNs bound into the proticles was examined in foetal calf serum and cell culture medium. FITC-labelled ODNs bound to protamine showed an increased cellular uptake into human histiocytic lymphoma U 937 cells compared to free ODNs. Proticles significantly decreased cellular growth in a cell proliferation assay using ODNs against the c- myc proto-oncogene.