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

Advanced Search

BPG is committed to discovery and dissemination of knowledge

Home / Archive / Volume 14, Issue 14

This Article

Citation of this article

Corresponding Author of This Article

Article-Type of This Article

Open-Access Policy of This Article

Times Cited Counts in Google of This Article

Number of Hits and Downloads for This Article

Total Article Views (3597)

All Articles published online

The chart showing PDF series, HTML series, Figures (1-2) series, Tables (1-4) series.

Item

Count

PDF

270

HTML

2966

Figures (1-2)

187

Tables (1-4)

174

Sum=3597

Apr 14, 2008 (publication date) through Nov 4, 2024

Times Cited of This Article

Times Cited (3)

Journal Information of This Article

Publication Name

World Journal of Gastroenterology

ISSN

1007-9327

Publisher of This Article

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

Rapid Communication

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