目的：探讨以PEIRGD(polyethyleneimineArgGlyAsp)为转染载体的125I(αV)ASODN投递在体外对HepG2肝癌细胞侵袭力的影响。方法:125I标记整合素αV亚基的ASODN，以聚乙烯亚胺衍生物PEIRGD为载体制备PEIRGD/125I(αV)ASODN复合物，通过受体介导方式转染进入HepG2细胞，利用Boyden小室侵袭模型检测复合物对HepG2细胞侵袭力的影响。结果:(1)125I(αV)ASODN的标记率为（73.78±4.09）%，放化纯度为（96.68±1.38）%,37 ℃放置48 h后的放化纯度仍>90%,表明其稳定性良好；(2) HepG2细胞对PEIRGD/ 125I(αV)ASODN的摄取于4 μl/2 μg时达到峰值\[（12.77±085）%\]，之后明显降低，故选择2 μl/1 μg作为PEIRGD/ 125I(αV)ASODN对HepG2细胞的作用剂量；(3)相对于其他实验组和对照组，PEIRGD/ 125I(αV)ASODN组显著降低了HepG2细胞的侵袭能力（P<0.01）。结论:以PEIRGD为载体投递 125I(αV)ASODN能有效抑制HepG2细胞的侵袭力。

Objective:To study the effects of 125I(αV)ASODN on the in vitro invasive ability of heptocellular carcinoma cell line（HepG2）through PEIRGDmediated receptor process. :Methods: :Intergrin αVspecific antisense oligonucleotide was labeled with 125I, and PEIRGD/125I(αV)ASODN complex was prepared by combining 125I(αV)ASODN with polyethyleneimine derivative PEIRGD. PEIRGD/125I(αV)ASODN complex was transferred into HepG2 cells through the receptormediated process. The effect of PEIRGD/125I(αV)ASODN complex on the invasive ability of HepG2 cells was examined by Boyden chamber invasive assay. :Results: :(1) The labeling yield and radiochemical purity of 125I(αV)ASODN were（73.78±4.09）% and（96.68±1.38）%, respectively, and the labeled compound had a good stability in vitro after 48 h at 37 ℃; (2) The ability of HepG2 cells to uptake PEIRGD/125I(αV)ASODN reached its peek（\[1277±0.85\]%) when PEIRGD/125I(αV)ASODN was at 4 μl/2 μg（\[12.77±0.85\]%）, and then gredually decreased thereafter. So the dosage of PEIRGD/125I(αV)ASODN for the following experiment was chosen as 2 μl/1 μg; (3) The invasive capacity of HepG2 cells was significantly reduced in PEIRGD/125I(αV)ASODN group compared with those in other experiment and control groups (P<0.01). :Conclusion:: 125I(αV) ASODN mediated by PEIRGD can effectively inhibit the invasive capacity of HepG2 cells.

国家自然科学基金资助项目（No.30300092)