Objective: To explore the radiolabeling property of oligonucleotide with 99mTc using NHS-MAG3 as a bifunctional chelator.
Methods: Three 15-base single-stranded amine-derivitized oligonucleotides, which were antisense(ASON), sense(SON) and mismatched oligonucleotides(MON) of c-myc oncogene mRNA, were coupled with NHS-MAG3 and labeled with 99mTc. The labeled oligonucleotide was purified by Sephadex G25 column chromatogram, then the stability was evaluated. The labeling efficiency of ON-MAG3 was assessed 15 days, 1 month and 2 months after storage at -20 degrees C. The binding rate of 99mTc-ON with plasma protein was measured by the trichloroacetic acid precipitation method.
Results: The average labeling efficiency of 99mTc-ASON, 99mTc-SON and 99mTc-ON was 68.41%, 66.24% and 69.38% respectively, and the radiochemical purity was 96.98%, 95.34% and 94.62%. 99mTc-ON was stable when placed at room temperature or incubated in human serum at 37 degrees C. The labeling efficiency of ON-MAG3 did not significantly change 2 months after storage at -20 degrees C. The plasma protein binding rate of 99mTc-ON was lower than 13%.
Conclusion: 99mTc-ON labeled with NHS-MAG3 method showed superior radiochemical characteristics. The labeling efficiency and radiochemical purity were desirable. The label was stable in serum and the binding with plasma protein was low. 99mTc-ON could be a sort of potential radiopharmaceutical for in vivo applications.
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