人工合成两种半乳糖多聚赖氨酸导向配体，与荧光素标记的互补于ＨＢＶｍＲＮＡ多聚腺苷酸信号部分的２１－聚反义硫代脱氧核苷酸（ＡＳＯＤＮ）电性结合，与２．２．１５细胞共同孵育，４０ｍｉｎ后配体组对ＨＢｓＡｇ和ＨＢｅＡｇ的抑制率为４１％～４７％和２８％～３１％，单纯ＡＳＯＤＮ组为１１％和５％；３ｄ后配体组为８８％～８９％和７１％～７４％，单纯组为６４％和５３％。经流式细胞分析，配体组使２．２．１５细胞荧光染色率达７５．３％和８３．８％；单纯组为２４．３％。结果表明，两种人工配体均具有良好的导向ＡＳＯＤＮ入肝细胞的功能，且可以明显提高ＡＳＯＤＮ抗ＨＢＶ的活性。 Two galactose polylysine targeting ligands were artificially synthesized and electrically coupled to fluorescein-labeled 21-poly-antisense thio deoxynucleotides (ASODNs) complementary to the polyadenylation signal region of HBV mRNA, and 2.2.15 cells, the inhibitory rates of HBsAg and HBeAg in the ligand group were 41% -47% and 28% -31% after 40min and 11% and 5% respectively in the ASODN group. After 3d, the ligand group was 88% ~ 89% and 71% ~ 74%, the simple group was 64% and 53%. Flow cytometry analysis showed that the fluorescence intensity of 2.2.15 cells was 75.3% and 83.8% in the ligand group, and 24.3% in the simple group. The results showed that both artificial ligands have a good function of guiding ASODN into hepatocytes, and can significantly enhance the anti-HBV activity of ASODN.