A comparison on radiochemical behavior and biological property of antisense oligonucleotide labeled with technetium-99m by two methods: NHS-MAG3 versus SHNHP.
- Author:
Yunchun LI
1
;
Tianzhi TAN
;
Jianguo ZHENG
;
Chun ZHANG
Author Information
1. Department of Nuclear Medicine, West China Hospital, Sichuan University, Chengdu 610041, China.
- Publication Type:Journal Article
- MeSH:
Animals;
Colonic Neoplasms;
metabolism;
pathology;
Glycine;
analogs & derivatives;
chemistry;
pharmacokinetics;
Humans;
Isotope Labeling;
methods;
Mice;
Mice, Inbred BALB C;
Niacinamide;
analogs & derivatives;
chemistry;
pharmacokinetics;
Oligonucleotides, Antisense;
chemistry;
pharmacokinetics;
Radiopharmaceuticals;
chemical synthesis;
pharmacokinetics;
Succinimides;
chemistry;
pharmacokinetics;
Technetium Tc 99m Mertiatide;
chemistry;
pharmacokinetics;
Tumor Cells, Cultured
- From:
Journal of Biomedical Engineering
2008;25(4):889-902
- CountryChina
- Language:Chinese
-
Abstract:
This study was undertaken to explore and compare the radiochemical behavior and biological property of antisense oligonucleotide (ASON) labeled with Technetium-99m using two methods: N-hydroxysuccinimidyl S-acetylmercaptoacetyltriglycline (NHS-MAG3) versus hydrazino nicotinamide derivative (SHNH). After SHNH and NHS-MAG3 were synthesized, ASON was labeled with Technetium-99m using SHNH and NHS-MAG3 as a bifunctional chelator, separately. The stability in vivo and in vitro, the combination with plasma albumen of rabbit, the biodistribution in BALB/ C mice and the HT29 cellular uptake were compared between labeled compound 99mTc-SHNH-ASON, using SHNH as a bifunctional complex reagent, and 99mTc-MAG3-ASON, using NHS-MAG3 as a bifunctional chelator. The results revealed that the labeling rate and the stability of 99mTc-MAG3-ASON were evidently higher than that of 99mTc-SHNH-ASON (P < 0.05), the combination rate of 99mTc-MAG3-ASON with plasma albumen was markedly lower than that of 99mTc-SHNH-ASON (P < 0.05); the biodistribution of 99mTc-MAG3-ASON was markedly lower than that of 99mTc-SHNH-ASON in blood, heart, stomach and intestines (P < 0.05), slightly lower than that of 99mTc-SHNH-ASON in liver and spleen (P > 0.05), and markedly higher than that of 99mTc-SHNH-ASON in kidney (P < 0.05); the HT29 cellular uptake rates of 99mTc-MAG3-ASON was markedly higher than that of 99mTc-SHNH-ASON (P < 0.05). Therefore, the radiochemical behavior and biological property of 99mTc-MAG3-ASON labeled using NHS-MAG3 is better than that of 99mTc-SHNH-ASON labeled using SHNH.
