Preparation of PEI-RGD/~(125)I-(α_v)ASODN and its inhibitory effect on invasive ability of HepG2 cells / 中国肿瘤生物治疗杂志

ABSTRACT

Objective:To study the effects of ~(125)I-(α_v)ASODN on the in vitro invasive ability of heptocellular carcino-ma cell line(HepG2) through PEI-RGD-mediated receptor process. Methods: Intergrin α_v-specific antisense oligonucle-otide 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.