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为探讨阳离子脂质体介导的TGFβ1反义寡核苷酸（antisenseoligonucleotides，ASON）对大鼠肝脏星状细胞激活及其胶原生成的作用，作者合成了特异性的针对TGFβ1mRNA转译起始区的硫代磷酸ASON及其对照（正义、错义寡核苷酸），并和阳离子脂质体形成复合物。通过测定细胞内32P标记的ASON的放射量来观察ASON的细胞摄入率，用细胞免疫化学分析α－SMA的表达来观察星状细胞的激活。结果显示：阳离子脂质体可以明显增加TGFβ1ASON的细胞摄入率（P＜0．05）；阳离子脂质体-TGFβ1ASON复合物和单独使用TGFβ1ASON相比，在相同浓度下（ASON浓度为1μmol／L）可以明显增高ASON对星状细胞激活的抑制作用，而单独使用阳离子脂质体或阳离子脂质体-正义或错义TGFβ1寡核苷酸复合物在相同浓度下未见抑制效应。ASON或阳离子脂质体-ASON复合物均无细胞毒性作用。由此提示，阳离子脂质体-ASON复合物可能发展成一种治疗肝纤维化的药物。
To investigate the effect of cationic liposome-mediated antisense oligonucleotides (ASON) on hepatic stellate cell activation and collagen production in rats, the authors synthesized sulfur specific for the TGFβ1 mRNA translation initiation region Phosphoric acid ASON and its control (sense, missense oligonucleotides) and complexed with cationic liposomes. The rate of cellular uptake of ASON was measured by measuring the radioactivity of 32P-labeled ASON in the cells, and the activation of stellate cells was observed by immunocytochemistry for the expression of α-SMA. The results showed that cationic liposomes could significantly increase the cellular uptake rate of TGFβ1ASON (P <0.05). Compared with TGFβ1ASON alone, the cationic liposome-TGFβ1ASON complex exhibited a higher ASON concentration of 1μmol / L ) Could significantly increase the inhibitory effect of ASON on stellate cell activation, whereas no effect of inhibition was observed at the same concentration with cationic liposomes or cationic liposomes - either positive or negative TGFβ1 oligonucleotide complexes alone. ASON or cationic liposome-ASON complexes have no cytotoxic effects. This suggests that the cationic liposome-ASON complex may develop into a drug for the treatment of hepatic fibrosis.