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目的:探讨以PEI-RGD(polyethyleneimine-Arg-Gly-Asp)为转染载体的125I-(αV)ASODN投递在体外对HepG2肝癌细胞侵袭力的影响。方法:125I标记整合素αV亚基的ASODN,以聚乙烯亚胺衍生物PEI-RGD为载体制备PEI-RGD/125I-(αV)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)125I-(αV)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/125I-(αV)ASODN的摄取于4μl/2μg时达到峰值[(12.77±0.85)%],之后明显降低,故选择2μl/1μg作为PEI-RGD/125I-(αV)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/125I-(αV)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125I-(α)ASODN能有效抑制HepG2细胞的侵袭力。
Objective: To investigate the effect of 125I- (αV) ASODN delivered by PEI-RGD (polyethyleneimine-Arg-Gly-Asp) on invasion of HepG2 hepatoma cells in vitro. METHODS: The ASODN of integrin αV subunit was labeled with 125I, PEI-RGD / 125I- (αV) ASODN complex was prepared by polyethyleneimine derivative PEI-RGD and transfected into HepG2 cells by receptor- The invasiveness of HepG2 cells was evaluated by Boyden chamber invasion assay. The results showed that: (1) The labeling rate of (125.7 ± 4.09)% and the radiochemical purity of 125I- (αV) ASODN were (96.68 ± 1.38)%, (2) HepG2 cells peaked at 4μl / 2μg [(12.77 ± 0.85)%] when PEI-RGD / 125I- (αV) ASODN was taken, and then decreased significantly. Therefore, 2μl / RGD / 125I- (αV) ASODN on HepG2 cells; (3) PEI-RGD / 125I- (αV) ASODN group significantly reduced the invasiveness of HepG2 cells compared with other experimental groups and control groups ). CONCLUSION: Delivery of 125I- (α) ASODN with PEI-RGD as a vector can effectively inhibit the invasiveness of HepG2 cells.