Preparation of ~(99m) Tc-MAG_3-ASON and distribution in breast carcinoma-bearing nude mouse model / 重庆医科大学学报

ABSTRACT

Objective:To discuss the preparation of ~(99m) Tc-labelled antisense oligonucleotide (ASON) and its distribution in breast carcinoma-bearing nude mouse model.Methods:N-hydroxysuccinimide ester of mercaptoacetylglycylglycylglycine (NHS-MAG_3) was synthesized by one step.A 15-mer single-stranded phosphorothioate ASON complementary to c-erbB2 oncogene mRNA was coupled with NHS-MAG_3 and labelled with ~(99m) Tc subsequently.~(99m)Tc-MAG_3-ASON was purified on a gel filtration column of Sephadex G25,then its stability was evaluated,and finally the distribution was detected in breast carcinoma-bearing nude mice model.Results: The average labeling efficiency of 99mTc-MAG_3-ASON was 70.6%,and the radiochemical purity was 94.3% after being labelled at room temperature for 4h. When incubated with fresh human serum, the radiochemical purity of ~(99m) Tc-MAG_3-ASON was 93.8%. The serum protein binding of ~(99m) Tc-MAG_3-ASON was 11.8%.The highest uptake of breast carcinoma was 6.09%ID/g at 2hs.Conclusion:~(99m)Tc-MAG_3-ASON has desirable stability,higher uptake in breast carcinoma and may provide a new sensitive tool for diagnostic imaging and therapy for breast carcinoma in the future.