AIM: To explore and compare the radiochemical behavior and biological property of anti-sense oligonuc-leotide (ASON) labeled with technetium-99m using N-hydroxysuccinimidyl S-acetylmercaptoacetyltriglycline (NHS-MAG(3)) and hydrazinonictinamide derivative (HYNIC). METHODS: After HYNIC and NHS-MAG(3) were synthesized, ASON was labeled with technetium-99m using HYNIC and NHS-MAG(3) as a bifunctional chelator. The in vivo and in vitro stability, binding rates of labeled compounds to serum albumen, biodistribution of (99m)Tc-MAG(3)-ASON and (99m)Tc-HYNIC-ASON in BALB/C mouse and its HT29 tumor cellular uptake were compared. RESULTS: The labeling efficiency and stability of (99m)Tc-MAG(3)-ASON were significantly higher than those of (99m)Tc-HYNIC-ASON (P = 0.02, and P = 0.03, respectively). (99m)Tc-MAG(3)-ASON had a significantly lower rate of binding to serum albumen than (99m)Tc-HYNIC-ASON (P < 0.05). In contrast to (99m)Tc-HYNIC-ASON, the biodistribution of (99m)Tc-MAG(3)-ASON was significantly lower in blood, heart, liver and stomach (P < 0.05), slightly lower in intestines and spleen (P > 0.05) and significantly higher in lung and kidney (P < 0.05). The HT29 tumor cellular uptake rate of (99m)Tc-MAG(3)-ASON was significantly higher than that of (99m)Tc-HYNIC-ASON (P < 0.05). CONCLUSION: (99m)Tc-MAG(3)-ASON shows superior radiochemical behaviors and biological properties than (99m)Tc-HYNIC-ASON. (99m)Tc-MAG(3)-ASON is a potential radiopharmaceutical agent for in vivo application.
AIM: To explore and compare the radiochemical behavior and biological property of anti-sense oligonuc-leotide (ASON) labeled with technetium-99m using N-hydroxysuccinimidyl S-acetylmercaptoacetyltriglycline (NHS-MAG(3)) and hydrazinonictinamide derivative (HYNIC). METHODS: After HYNIC and NHS-MAG(3) were synthesized, ASON was labeled with technetium-99m using HYNIC and NHS-MAG(3) as a bifunctional chelator. The in vivo and in vitro stability, binding rates of labeled compounds to serum albumen, biodistribution of (99m)Tc-MAG(3)-ASON and (99m)Tc-HYNIC-ASON in BALB/C mouse and its HT29 tumor cellular uptake were compared. RESULTS: The labeling efficiency and stability of (99m)Tc-MAG(3)-ASON were significantly higher than those of (99m)Tc-HYNIC-ASON (P = 0.02, and P = 0.03, respectively). (99m)Tc-MAG(3)-ASON had a significantly lower rate of binding to serum albumen than (99m)Tc-HYNIC-ASON (P < 0.05). In contrast to (99m)Tc-HYNIC-ASON, the biodistribution of (99m)Tc-MAG(3)-ASON was significantly lower in blood, heart, liver and stomach (P < 0.05), slightly lower in intestines and spleen (P > 0.05) and significantly higher in lung and kidney (P < 0.05). The HT29 tumor cellular uptake rate of (99m)Tc-MAG(3)-ASON was significantly higher than that of (99m)Tc-HYNIC-ASON (P < 0.05). CONCLUSION: (99m)Tc-MAG(3)-ASON shows superior radiochemical behaviors and biological properties than (99m)Tc-HYNIC-ASON. (99m)Tc-MAG(3)-ASON is a potential radiopharmaceutical agent for in vivo application.
Authors: M J Abrams; M Juweid; C I tenKate; D A Schwartz; M M Hauser; F E Gaul; A J Fuccello; R H Rubin; H W Strauss; A J Fischman Journal: J Nucl Med Date: 1990-12 Impact factor: 10.057
Authors: D J Hnatowich; G Mardirossian; M Fogarasi; T Sano; C L Smith; C R Cantor; M Rusckowski; P Winnard Journal: J Pharmacol Exp Ther Date: 1996-01 Impact factor: 4.030
Authors: G Citro; D Perrotti; C Cucco; I D'Agnano; A Sacchi; G Zupi; B Calabretta Journal: Proc Natl Acad Sci U S A Date: 1992-08-01 Impact factor: 11.205