Abstract Objective: To investigate the possibility of using mouse double minute 2(MDM2) mRNA antisense oligonucleotide(ASON) labeled with 99Tcm for the antisense imaging study, the uptake kinetics of the liposome-coated antisense probe and the mistatch probe were studied in the MCF-7. Methods: An ASON and a mismatch oligonucleotide(ASONM) targeted to mRNA MDM2 were synthesized and radiolabeled by 99Tcm with the bifunctional chelator HYNIC, and investigate the labeling efficiency, radiochemical purity and the ability of the labeled ASON to hybridize to the sense oligonucleotide(SON). The uptake kinetics of the liposome-coated antisense probe and the mismatch probe were studied in the MCF-7 at different times, compared with uptake kinetics of the antisense probe and the mismatch probe in the MCF-7. Results: The labeling efficacy of ASON and ASONM were (57.2±2.98)%(n=5) and (56.3±3.01)%(n=5) with the bifunctional chelator HYNIC. The radiochemical purity was above 95% after purification. The labeled ASON still has the ability to hybridize to the SON. At 22℃, the uptake peak value of the liposome-coated antisense probe and the mismatch probe were (34.62±2.91)% and (14.57±1.62)%, respectively. The antisense probe showed significantly higher accumulation and effluxed much slowly than mismatch probe. The MCF-7 uptake of the liposome-coated probe was much higher than that of non-coated probe. Conclusion: MDM2 mRNA antisense oligonucleotide can be radiolabeled successfully with the bifunctional chelator HYNIC. The antisense probe can accumulate in the proliferating MCF-7 cells more specifically which provided a basis for it to be used in antisense imaging study.
FU Peng,ZHAO Chang-jiu,HAN Wei, et al. Labeling of MDM2 antisense oligonucleotide with 99Tcm and the research of the uptake kinetics in human breast cancer cells[J]. , 2007, 18(12): 855-859.
2007, Vol. 18 
