Abstract
Diagnosis of tumour hypoxia is an important aspect in determining the course of tumour therapy. In this study, we developed a novel imaging agent, 99mTcethylenedicysteine- bis-misonidazole (99mTc-EC-MISO), for diagnosing tumour hypoxia. We used 2-nitroimidazole as a reactant to synthesize the amino derivative of misonidazole (MISO) in the first step and then conjugated the di-amino derivative of MISO to the chelating agent ethylenedicysteine (EC) for labelling 99mTc in the second step. 99mTc-pertechnetate (99mTcO4 -) was reduced by tin chloride (SnCl2) for radiolabeling. The radiochemical purity was up to 94%. Tissue biodistribution and SPECT/CT imaging studies were conducted on subcutaneous gliomal tumour-bearing mice. The tumour-to-muscle ratio in the 99mTc-EC-MISO group increased with time, up to 4.6 at 4 h after injection. SPECT/CT imaging confirmed that the tumours could be visualized clearly with 99mTc-EC-MISO at 2 h. By introducing a second 2-nitroimidazole redox centre, an apparent hypoxic accumulation of this novel 99mTc-labeled imaging agent in the tumour was observed.
Keywords: Tumour hypoxia, imaging agent, misonidazole (MISO), technetium-99m-labeled.
Medicinal Chemistry
Title:Preparation and Biodistribution of Technetium-99m-Labeled Bis- Misonidazole (MISO) as an Imaging Agent for Tumour Hypoxia
Volume: 11 Issue: 7
Author(s): Feng Wang, Di Fan, Jun Qian, Zhe Zhang, Jianhua Zhu and Jian Chen
Affiliation:
Keywords: Tumour hypoxia, imaging agent, misonidazole (MISO), technetium-99m-labeled.
Abstract: Diagnosis of tumour hypoxia is an important aspect in determining the course of tumour therapy. In this study, we developed a novel imaging agent, 99mTcethylenedicysteine- bis-misonidazole (99mTc-EC-MISO), for diagnosing tumour hypoxia. We used 2-nitroimidazole as a reactant to synthesize the amino derivative of misonidazole (MISO) in the first step and then conjugated the di-amino derivative of MISO to the chelating agent ethylenedicysteine (EC) for labelling 99mTc in the second step. 99mTc-pertechnetate (99mTcO4 -) was reduced by tin chloride (SnCl2) for radiolabeling. The radiochemical purity was up to 94%. Tissue biodistribution and SPECT/CT imaging studies were conducted on subcutaneous gliomal tumour-bearing mice. The tumour-to-muscle ratio in the 99mTc-EC-MISO group increased with time, up to 4.6 at 4 h after injection. SPECT/CT imaging confirmed that the tumours could be visualized clearly with 99mTc-EC-MISO at 2 h. By introducing a second 2-nitroimidazole redox centre, an apparent hypoxic accumulation of this novel 99mTc-labeled imaging agent in the tumour was observed.
Export Options
About this article
Cite this article as:
Wang Feng, Fan Di, Qian Jun, Zhang Zhe, Zhu Jianhua and Chen Jian, Preparation and Biodistribution of Technetium-99m-Labeled Bis- Misonidazole (MISO) as an Imaging Agent for Tumour Hypoxia, Medicinal Chemistry 2015; 11 (7) . https://dx.doi.org/10.2174/1573406411666150504124103
DOI https://dx.doi.org/10.2174/1573406411666150504124103 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
Call for Papers in Thematic Issues
Carbohydrates in Computational and Medicinal Chemistry
Carbohydrates are the most essential organic molecules and are involved in the maintenance of various physiological and metabolic processes in living organisms. Carbohydrate-based compounds have come to the attention of researchers because of their significant contributions to biological functions, such as cell development and cell proliferation, connections between several cells, ...read more
Recent Advances in the Medicinal Chemistry of Cancer
Scope of the Thematic Issue: Correlation between structure and function is one of the important aspects of the success of anti-cancer compounds associated with their structure-activity interactions, physiology, biochemical, molecular, and genetic processes. Overcoming these obstacles is key to obtaining further insights into developments in rational drug design, bioorganic chemistry, ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Role of AGEs-RAGE System in Cardiovascular Disease
Current Pharmaceutical Design Chronotherapeutic Drug Delivery from Indomethacin Compression Coated Tablets for Early Morning Pain Associated Rheumatoid Arthritis
Current Drug Delivery A Role for Rev-erbα Ligands in the Regulation of Adipogenesis
Current Pharmaceutical Design Prostaglandin EP Receptor Subtypes Involved in Regulating HCO3- Secretion from Gastroduodenal Mucosa
Current Pharmaceutical Design Metabolic Syndrome X is a Low-Grade Systemic Inflammatory Condition with its Origins in the Perinatal Period
Current Nutrition & Food Science Calcium Antagonists: A Ready Prescription for Treating Infectious Diseases?
Current Topics in Medicinal Chemistry Aldehyde Dehydrogenase-2 Roles in Ischemic Cardiovascular Disease
Current Drug Targets Physical Activity: Do Patients Infected with HIV Practice? How Much? A Systematic Review
Current HIV Research Revascularization vs. Optimal Medical Therapy in Women with NSTE-ACS
Current Pharmaceutical Design N6-methyladenine RNA Modification (m<sup>6</sup>A): An Emerging Regulator of Metabolic Diseases
Current Drug Targets Chemokines and Atherosclerotic Plaque Progression: Towards Therapeutic Targeting?
Current Pharmaceutical Design Moderate Wine Consumption in the Prevention of Metabolic Syndrome and its Related Medical Complications
Endocrine, Metabolic & Immune Disorders - Drug Targets Multi-Target Profile of Oleocanthal, An Extra-Virgin Olive Oil Component
Current Bioactive Compounds Mechanisms of Action of Metformin in Type 2 Diabetes and Associated Complications: An Overview
Mini-Reviews in Medicinal Chemistry Psychological Sequelae of Ovarian Cancer Screening and Genetic Testing for Ovarian Cancer Susceptibility
Current Women`s Health Reviews Effect of Electromagnetic Radiations on Neurodegenerative Diseases- Technological Revolution as a Curse in Disguise
CNS & Neurological Disorders - Drug Targets Cell Immunity in Coronary Artery Disease (CAD)
Current Immunology Reviews (Discontinued) Best Practice for Atrial Fibrillation Patient Education
Current Pharmaceutical Design Overview of Green Tea Interaction with Cardiovascular Drugs
Current Pharmaceutical Design Low-Dose Methotrexate (LD-MTX) in Rheumatology Practice - A Most Widely Misunderstood Drug
Current Rheumatology Reviews