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Radiosynthesis and biological evaluation of 99mTcN-sitafloxacin dithiocarbamate as a potential radiotracer for Staphylococcus aureus infection

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Abstract

Sitafloxacin dithocarbamate (SFDE) was synthesized, radiolabeled with technetium-99m (99mTc) using [99mTc-N]2+ core and evaluated its biological efficacy as a potential radiotracer for Staphylococcus aureus (S. aureus) infection in artificially infected rats (AIRT) and rabbits (AIRB). The radiochemical stability of the 99mTc labeled SFDE (99mTcN-SFDE) in saline and serum was determined by radio-HPLC and TLC methods, respectively. After, 1 min of reconstitution the value of radiochemical purity (RCP) was 99.00 ± 0.20% and was remained more than 90% unwavering even after 240 min of the radiolabeling. The 99mTcN-SFDE complex showed similar radiochemical permanence behavior in serum at 37 °C. The complex showed almost six fold higher specific in vitro binding with living than heat killed S. aureus. Biodistribution behavior was evaluated in S. aureus AIRT and whole body imaging (WBI) in AIRB, respectively. Seven fold up take was observed in infected muscle of the AIRT as compared to inflamed and normal muscles. The disappearance of activity from blood and appearance in urinary system indicated normal route of excretion of the complex. Scintigraphically, it was confirmed that the labeled SFDE was higher accumulated in the infected muscle higher than in inflamed and normal muscle. The high radiochemical stability in saline and serum, specific in vitro binding with S. aureus, precise in vivo distribution in S. aureus AIRT and targeted WBI in AIRB confirmed the possibility of the 99mTcN-SFDE complex as a potential and promising S. aureus infection radiotracer.

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Authors and Affiliations

  1. Nuclear Medicine Research Laboratory (NMRL), University of Peshawar, Peshawar, NWFP, Pakistan

    Syed Qaiser Shah

  2. Nuclear Medicine, Oncology and Radiotherapy Institute (NORI), Islamabad, Pakistan

    Aakif Ullah Khan

  3. Phytopharmaceutical and Neutraceuticals Research Laboratory (PNRL), University of Peshawar, Peshawar, NWFP, Pakistan

    Muhammad Rafiullah Khan

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  1. Syed Qaiser Shah
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  2. Aakif Ullah Khan
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Correspondence to Syed Qaiser Shah.

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Shah, S.Q., Khan, A.U. & Khan, M.R. Radiosynthesis and biological evaluation of 99mTcN-sitafloxacin dithiocarbamate as a potential radiotracer for Staphylococcus aureus infection. J Radioanal Nucl Chem 287, 827–832 (2011). https://doi.org/10.1007/s10967-010-0833-9

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  • DOI: https://doi.org/10.1007/s10967-010-0833-9

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