Synthesis and biological evaluation of a novel 99mTc(CO)3 complex of ciprofloxacin dithiocarbamate as a potential agent to target infection |
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Authors: | Junbo Zhang Shijian Zhang Haixun Guo Xuebin Wang |
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Institution: | Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, PR China |
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Abstract: | The ciprofloxacin dithiocarbamate (CPFXDTC) was radiolabeled with 99mTc(CO)3(H2O)3]+ intermediate to form the 99mTc(CO)3–CPFXDTC complex in high yield. The 99mTc(CO)3–CPFXDTC complex was characterized by HPLC and its stability in serum was studied. Its partition coefficient indicated that it was a lipophilic complex. The bacterial binding efficiency of 99mTc(CO)3–CPFXDTC was almost the same as that of 99mTcN–CPFXDTC, and was higher than that of 99mTc–ciprofloxacin. Biodistribution results in induced infection mice showed 99mTc(CO)3–CPFXDTC had higher uptake at the sites of infection and better abscess/blood and abscess/muscle ratios than those of 99mTc–ciprofloxacin and 99mTcN–CPFXDTC. Single photon emission computed tomography (SPECT) static imaging study in infected rabbits demonstrated the uptake in the left thigh infection lesion was observable, while no accumulation in the right thigh muscle was found. These results suggested 99mTc(CO)3–CPFXDTC would be a promising candidate for further evaluation as infection imaging agent. |
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