Anti-sense oligonucleotide labeled with technetium-99m using hydrazinonictinamide derivative and N-hydroxysuccinimidyl S-acetylmercaptoacetyltriglycline: A comparison of radiochemical behaviors and biological properties

doi:10.3748/wjg.14.2235

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World Journal of Gastroenterology

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1007-9327

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Baishideng Publishing Group Inc, 7041 Koll Center Parkway, Suite 160, Pleasanton, CA 94566, USA

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World J Gastroenterol. Apr 14, 2008; 14(14): 2235-2240
Published online Apr 14, 2008. doi: 10.3748/wjg.14.2235

Anti-sense oligonucleotide labeled with technetium-99m using hydrazinonictinamide derivative and N-hydroxysuccinimidyl S-acetylmercaptoacetyltriglycline: A comparison of radiochemical behaviors and biological properties

Yun-Chun Li, Tian-Zhi Tan, Jian-Guo Zheng, Chun Zhang

Yun-Chun Li, Tian-Zhi Tan, Jian-Guo Zheng, Chun Zhang, Department of Nuclear Medicine, West China Hospital, Sichuan University, 37 Guoxue Alley, Chengdu 610041, Sichuan Province, China

Author contributions: Li YC, Tan TZ, Zheng JG, Zhang C contributed equally to this work.

Correspondence to: Tian-Zhi Tan, Professor, Department of Nuclear Medicine, West China Hospital, Sichuan University, 37 Guoxue Alley, Chengdu 610041, Sichuan Province, China. ttz@mcw-cums.com

Telephone: +86-28-81812589

Fax: +86-28-85422697

Received: November 12, 2007
Revised: January 30, 2008
Published online: April 14, 2008

Abstract

AIM: To explore and compare the radiochemical behavior and biological property of anti-sense oligonucleotide (ASON) labeled with technetium-99m using N-hydroxysuccinimidyl S-acetylmercaptoacetyltriglycline (NHS-MAG₃) and hydrazinonictinamide derivative (HYNIC).

METHODS: After HYNIC and NHS-MAG₃ were synthesized, ASON was labeled with technetium-99m using HYNIC and NHS-MAG₃ as a bifunctional chelator. The in vivo and in vitro stability, binding rates of labeled compounds to serum albumen, biodistribution of ^99mTc-MAG₃-ASON and ^99mTc-HYNIC-ASON in BALB/C mouse and its HT29 tumor cellular uptake were compared.

RESULTS: The labeling efficiency and stability of ^99mTc-MAG₃-ASON were significantly higher than those of ^99mTc-HYNIC-ASON (P = 0.02, and P = 0.03, respectively). ^99mTc-MAG₃-ASON had a significantly lower rate of binding to serum albumen than ^99mTc-HYNIC-ASON (P < 0.05). In contrast to ^99mTc-HYNIC-ASON, the biodistribution of ^99mTc-MAG₃-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 ^99mTc-MAG₃-ASON was significantly higher than that of ^99mTc-HYNIC-ASON (P < 0.05).

CONCLUSION: ^99mTc-MAG₃-ASON shows superior radiochemical behaviors and biological properties than ^99mTc-HYNIC-ASON. ^99mTc-MAG₃-ASON is a potential radiopharmaceutical agent for in vivo application.

Keywords: Anti-sense oligonucleotide, Radiolabeling, Technetium-99m, N-hydroxysuccinimidyl S-acetylmercaptoacetyltriglycline, Hydrazinonictionamide derivative