脂质超声造影剂携半乳糖化多聚赖氨酸靶向结合HepG2细胞的实验研究

Experimental study of lipid ultrasound contrast agent with galactose - carrying poly - L - lysine target to HepG 2 cells

目的探讨连接以半乳糖化多聚赖氨酸作为配体的脂质微泡超声造影剂的细胞靶向能力，为体内靶向显影及治疗肝癌寻求新方法。方法用还原胺化法将多聚赖氨酸进行半乳糖化，人工合成小分子量的靶向配体，在室温下与自制脂质微泡发生化学结合制备成靶向脂质微泡，于荧光显微镜下观察体外靶向效果。结果半乳糖与多聚赖氨酸在摩尔比为1：100，室温下反应24h时，能进行高效连接；靶向脂质微泡粒径平均为2．05μm，大小均一；激光共聚焦荧光显微镜见HepG2肝癌细胞能与靶向造影剂特异性结合。结论连接有以半乳糖化多聚赖氨酸为靶向配体的脂质微泡在HepG2肝癌细胞的内吞作用下能与之有效结合。

Objective To investigate the targeted capacity of ultrasound contrast agent with a galactose- poly L lysine ligand,and lay the foundation for targeted imaging in vivo and the treatment of liver cancer. Methods The small molecular targeted ligand was synthetized by a method of reductive amination, the targeted lipid microbubbles were performed by combining lipid microbubbles with the targeted ligand,the targeted effectiveness was observed by fluorescence microscopy. Results Galactose and poly-L-lysine were combined effectively after 24 b with the molar ratio 1 ： 100,the average particle size of the targeted lipid microbubbles was 2 micron, the targeted combine of the HepG2 liver cancer cells with the targeted ultrasound contrast agent was observed by laser scanning confocal microscope. Conclusions The targeted lipid microbubbles can target effectively to the HepG2 cells.