BACKGROUND: To investigate the in vitro inhibitory effects of PEI-RGD/125I-(αv)ASODN (PEI, polyethylenimine; RGD, Arg-Gly-Asp; ASODN, antisense oligodeoxynucleotide) on the growth and invasion of HepG2 cells.

MATERIAL AND METHODS: ASODN of the integrin αv-subunit was marked with 125I and underwent complexation with PEI-RGD, a PEI derivative. Next, PEI-RGD/125I-(αv) ASODN was introduced into HepG2 cells via receptor-mediated transfection, and its inhibition rate on HepG2 cell growth was tested using the methyl thiazolyl tetrazolium (MTT) method. The effects of PEI-RGD/125I-(αv) ASODN on HepG2 cell invasion ability were evaluated using the Boyden chamber assay.

RESULTS: 1) The 125I marking rate of (αv) ASODN was 73.78±4.09%, and the radiochemical purity was 96.68±1.38% (greater than 90% even after a 48-h incubation period at 37°C), indicating high stability. 2) The cytotoxicity assays showed that the cell inhibition rates did not differ significantly between the PEI-RGD/125I-(αv)ASODN group and the PEI-RGD/(αv) ASODN group, but they were both significantly higher than in the other groups and were positively correlated (r=0.879) with the dosage within a certain range. 3) The invasion assays showed that the inhibition rate was significantly greater in the PEI-RGD/125I-(αv) ASODN group compared to the other groups.

CONCLUSIONS: PEI-RGD/125I-(αv) ASODN can efficiently inhibit the growth and proliferation of HepG2 cells and can also weaken their invasive ability.

Keywords: Cell Proliferation - radiation effects, Base Sequence, Integrin alphaV - genetics, Iodine Radioisotopes - administration & dosage, Oligodeoxyribonucleotides, Antisense - genetics, Oligopeptides - administration & dosage, Polyethyleneimine - analogs & derivatives