Radiosynthesis and preliminary biological evaluation of 99mTc-labeled 2-methyl-2-pentylmalonic acid as an apoptosis imaging agent

Apoptosis is one of the fundamental phenomena behind successful radiation and chemotherapy treatments. Non-invasive imaging of apoptosis can offer an early diagnosis of disease and the true efficiency of an ongoing treatment procedure. The present study describes an attempt to develop 99m Tc-labeled...

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Bibliographic Details
Published in:Journal of radioanalytical and nuclear chemistry 2017, Vol.313 (1), p.207-215
Main Authors: Mushtaq, Sajid, Jeon, Jongho, Kang, Jung Ae, Nam, You Ree, Jang, Beom Su, Park, Sang Hyun
Format: Article
Language:English
Subjects:
Apoptosis
Bioaccumulation
Chemistry
Chemistry and Materials Science
Chemotherapy
Diagnosis
Diagnostic Radiology
Efficiency
Hadrons
Heavy Ions
Imaging
Inorganic Chemistry
Mice
Nuclear Chemistry
Nuclear Physics
Physical Chemistry
Purity
Radio
Radiochemistry
Technetium isotopes
Testes
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Summary:Apoptosis is one of the fundamental phenomena behind successful radiation and chemotherapy treatments. Non-invasive imaging of apoptosis can offer an early diagnosis of disease and the true efficiency of an ongoing treatment procedure. The present study describes an attempt to develop 99m Tc-labeled 2-methyl-2-pentylmalonic acid ([ 99m Tc] 8 ) as a new SPECT based apoptosis imaging agent. An optimized chemical and radiosynthesis procedure provided desired product [ 99m Tc] 8 with high radiochemical yield (84%, n  = 3) and radiochemical purity (>99%) as determined by radio HPLC. Biodistribution data indicated that the radiotracer has a rapid clearance from blood and other background tissues. High testes accumulation confirmed the ability of the radiotracer to detect testicular apoptosis in mice.
ISSN:0236-5731
1588-2780
DOI:10.1007/s10967-017-5275-1