Syed Qaiser Shah1, Mohammad Rafiullah Khan2, Syed Mohammad Ali3. 1. Nuclear Medicine Research Laboratory (NMRL), University of Peshawar, Peshawar, KPK Pakistan. 2. Phytopharmaceutical & Neutraceuticals Research Laboratory (PNRL), University of Peshawar, Peshawar, KPK Pakistan. 3. Center of Basic Science, University of Engineering and Technology Peshawar, Peshawar, KPK Pakistan.
Abstract
BACKGROUND: Clinafloxacin dithiocarbamate (CNND) was radiolabeled with technetium-99m ((99m)Tc) using [(99m)Tc(CO)3(H2O)3](+) and assessed for its radiochemical stability in saline and serum, its in vitro binding with methicillin-resistant Staphylococcus aureus (MRSA) and biodistribution in female nude mice (FNM) artificially infected with live and heat-killed MRSA. METHODS: In normal saline (NS) the (99m)Tc(CO)3-clinafloxacin dithiocarbamate ((99m)Tc(CO)3-CNND) showed radiochemical stability with a maximum value of 99.10 ± 0.20% and remained stable up to 4 h (92.65 ± 0.18%). RESULTS: In human serum at 37°C within 16 h of incubation, 14.85% side products as a result of de-tagging developed. Incubation with MRSA gave saturated binding with a maximum value of 72.75 ± 1.20%. Almost six-fold higher uptake was seen in the infected muscle of the FNM as compared to the inflamed and normal muscle. The (99m)Tc(CO)3-CNND complex showed a normal route of excretion from the body of the FNM model. CONCLUSION: The higher stability in NS, HS, saturated in vitro binding with a live strain of MRSA and six-fold higher uptake in the target organ showed the (99m)Tc(CO)3-CNND complex to be a potential MRSA infection radiotracer.
BACKGROUND:Clinafloxacin dithiocarbamate (CNND) was radiolabeled with technetium-99m ((99m)Tc) using [(99m)Tc(CO)3(H2O)3](+) and assessed for its radiochemical stability in saline and serum, its in vitro binding with methicillin-resistant Staphylococcus aureus (MRSA) and biodistribution in female nude mice (FNM) artificially infected with live and heat-killed MRSA. METHODS: In normal saline (NS) the (99m)Tc(CO)3-clinafloxacin dithiocarbamate ((99m)Tc(CO)3-CNND) showed radiochemical stability with a maximum value of 99.10 ± 0.20% and remained stable up to 4 h (92.65 ± 0.18%). RESULTS: In human serum at 37°C within 16 h of incubation, 14.85% side products as a result of de-tagging developed. Incubation with MRSA gave saturated binding with a maximum value of 72.75 ± 1.20%. Almost six-fold higher uptake was seen in the infected muscle of the FNM as compared to the inflamed and normal muscle. The (99m)Tc(CO)3-CNND complex showed a normal route of excretion from the body of the FNM model. CONCLUSION: The higher stability in NS, HS, saturated in vitro binding with a live strain of MRSA and six-fold higher uptake in the target organ showed the (99m)Tc(CO)3-CNND complex to be a potential MRSA infection radiotracer.