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[The radiolabeling property of oligonucleotide with 99mTc using NHS-MAG3 as a chelator].
- Source :
-
Sichuan da xue xue bao. Yi xue ban = Journal of Sichuan University. Medical science edition [Sichuan Da Xue Xue Bao Yi Xue Ban] 2004 Mar; Vol. 35 (2), pp. 169-71. - Publication Year :
- 2004
-
Abstract
- Objective: To explore the radiolabeling property of oligonucleotide with 99mTc using NHS-MAG3 as a bifunctional chelator.<br />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.<br />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%.<br />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.
- Subjects :
- Animals
Glycine chemistry
Glycine pharmacokinetics
Oligonucleotides chemical synthesis
Oligonucleotides pharmacokinetics
Oligonucleotides, Antisense chemistry
Oligonucleotides, Antisense pharmacokinetics
Oligopeptides chemical synthesis
Oligopeptides chemistry
Oligopeptides pharmacokinetics
Organotechnetium Compounds chemical synthesis
Organotechnetium Compounds pharmacokinetics
Protein Binding
Rabbits
Radiopharmaceuticals pharmacokinetics
Random Allocation
Succinimides chemical synthesis
Succinimides pharmacokinetics
Technetium Tc 99m Mertiatide pharmacokinetics
Glycine analogs & derivatives
Isotope Labeling methods
Oligonucleotides chemistry
Radiopharmaceuticals chemical synthesis
Succinimides chemistry
Technetium Tc 99m Mertiatide chemistry
Subjects
Details
- Language :
- Chinese
- ISSN :
- 1672-173X
- Volume :
- 35
- Issue :
- 2
- Database :
- MEDLINE
- Journal :
- Sichuan da xue xue bao. Yi xue ban = Journal of Sichuan University. Medical science edition
- Publication Type :
- Academic Journal
- Accession number :
- 15071906