Shah Syed Qaiser, Khan Mohammad Rafiullah
Center for Nuclear and Molecular Studies, Institute of Chemical Sciences, University of Peshawar, KPK, Pakistan.
Phyotopharmaceutical and Neutraceuticals Research Laboratory, University of Peshawar, Peshawar, KPK, Pakistan.
World J Nucl Med. 2014 Sep;13(3):154-8. doi: 10.4103/1450-1147.144813.
Clinafloxacin dithiocarbamate (CNND) preparation and radiolabeling through (99m)Tc ≡ N core with the gamma (γ) emitter ((99m)Tc) was assessed. The potentiality of the (99m)Tc(V) ≡ N-CNND complex was investigated as perspective a Staphylococcus aureus (S.a.) in vivo infection radiotracer in terms of radiochemical stability in normal saline (n.s.), human serum (h.s.), binding efficacy with live and heat killed S.a. and biodistribution in female nude mice model (FNMD). More than 90% stability was observed in n.s. for 4 h with the highest yield of 98.70 ± 0.26% at 30 min after reconstitution. In h.s., the (99m)Tc(V) ≡ N-CNND complex was found stable up to 16 h with 15.35% side products. Maximum in vitro binding (68.75 ± 0.80%, 90 min) with S.a. was observed after 90 min of incubation. In FNMD, (infected with live strain) approximately six-fold higher uptakes was noted in the infected to inflamed and normal muscles. The higher stability in n.s., h.s., higher S.a. (live) up take with specific and targeted in vivo distribution confirmed potentiality of the (99m)Tc(V) ≡ N-CNND complex as perspective S.a. in vivo infection radiotracer.
评估了克林沙星二硫代氨基甲酸盐（CNND）的制备以及通过(99m)Tc≡N核心与γ发射体（(99m)Tc）进行放射性标记的情况。研究了(99m)Tc(V)≡N-CNND配合物作为金黄色葡萄球菌（S.a.）体内感染放射性示踪剂的潜力，涉及在生理盐水（n.s.）、人血清（h.s.）中的放射化学稳定性、与活的和热灭活的S.a.的结合效力以及在雌性裸鼠模型（FNMD）中的生物分布。在生理盐水中4小时内观察到稳定性超过90%，复溶后30分钟时产率最高，为98.70±0.26%。在人血清中，(99m)Tc(V)≡N-CNND配合物在长达16小时内稳定，副产物为15.35%。孵育90分钟后观察到与S.a.的最大体外结合（68.75±0.80%，90分钟）。在FNMD中（感染活菌株），感染部位与发炎和正常肌肉相比，摄取量高出约六倍。在生理盐水、人血清中的较高稳定性、与活的S.a.的较高摄取以及体内特异性和靶向性分布证实了(99m)Tc(V)≡N-CNND配合物作为潜在的S.a.体内感染放射性示踪剂的潜力。
