title: [A comparison on radiochemical behavior and biological property of antisense oligonucleotide labeled with technetium-99m by two methods: NHS-MAG3 versus SHNHP].
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.
authors.affiliation: Department of Nuclear Medicine, West China Hospital, Sichuan University, Chengdu 610041, China.
authors.forename: Yunchun
authors.initials: Y
authors.lastname: Li
authors.forename: Tianzhi
authors.initials: T
authors.lastname: Tan
authors.forename: Jianguo
authors.initials: J
authors.lastname: Zheng
authors.forename: Chun
authors.initials: C
authors.lastname: Zhang
mesh_terms: D000818:Animals; D003110:Colonic Neoplasms / Q000378:metabolism / Q000473:pathology; D005998:Glycine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics; D006801:Humans; D007553:Isotope Labeling / Q000379:methods*; D051379:Mice; D008807:Mice, Inbred BALB C; D009536:Niacinamide / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics; D016376:Oligonucleotides, Antisense / Q000737:chemistry / Q000493:pharmacokinetics*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000493:pharmacokinetics; D013388:Succinimides / Q000737:chemistry / Q000493:pharmacokinetics*; D017263:Technetium Tc 99m Mertiatide / Q000737:chemistry / Q000493:pharmacokinetics*; D014407:Tumor Cells, Cultured
chemical_list: C530515:N-hydroxysuccinimidyl S-acetylmercaptoacetyltriglycline; D016376:Oligonucleotides, Antisense; D019275:Radiopharmaceuticals; D013388:Succinimides; C530514:hydrazinonictinamide; D009536:Niacinamide; D017263:Technetium Tc 99m Mertiatide; D005998:Glycine