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(99m)Tc-三羰基莫西沙星二硫代氨基甲酸盐配合物作为潜在的金黄色葡萄球菌感染放射性示踪剂的放射性合成及生物学评价

Radiosynthesis and biological evaluation of the (99m)Tc-tricarbonyl moxifloxacin dithiocarbamate complex as a potential Staphylococcus aureus infection radiotracer.

作者信息

Shah Syed Qaiser, Khan Muhammad Rafiullah

机构信息

Nuclear Medicine Research Laboratory, University of Peshawar, KPK, Pakistan.

出版信息

Appl Radiat Isot. 2011 Apr;69(4):686-90. doi: 10.1016/j.apradiso.2011.01.003. Epub 2011 Jan 11.

DOI:10.1016/j.apradiso.2011.01.003
PMID:21256038
Abstract

In the present investigation, radiosynthesis of the (99m)Tc-tricarbonyl moxifloxacin dithiocarbamate complex ((99m)Tc(CO)(3)-MXND) and its biological evaluation in male Wister rats (MWR) artificially infected with Staphylococcus aureus (S. aureus) was assessed. The (99m)Tc(CO)(3)-MXND complex was radiochemically examined in terms of stability in saline and in serum and biologically its in-vitro binding with S. aureus and percent absorption in MWR models. Radiochemically the (99m)Tc(CO)(3)-MXND complex showed more than 90% stability in saline up to 240 min and in serum 14.95% undesirable species was appeared within 16h. In-vitro the (99m)Tc(CO)(3)-MXND complex showed saturated binding with S. aureus. In MWR artificially infected with live S. aureus the complex showed about six fold higher uptakes in the infected muscle as compared to the normal muscle. However, insignificant change in the uptake of (99m)Tc(CO)(3)-MXND complex in the infected and inflamed or normal muscle was observed in the MWR infected with heat killed S. aureus. The (99m)Tc(CO)(3)-MXND complex disappeared from the circulatory system and appeared in the urinary system within 60-90 min followed by excretion through normal route of urinary system. Based on the elevated and stable radiochemical succumb in saline, serum, saturated in-vitro binding with S. aureus and higher accumulation in the target organ of the MWR, we recommend the (99m)Tc(CO)(3)-MXND complex for radio-localization of the infection induced by S. aureus in human.

摘要

在本研究中,评估了(99m)Tc-三羰基莫西沙星二硫代氨基甲酸盐配合物((99m)Tc(CO)(3)-MXND)的放射性合成及其在人工感染金黄色葡萄球菌的雄性Wistar大鼠(MWR)中的生物学评价。从在生理盐水和血清中的稳定性方面对(99m)Tc(CO)(3)-MXND配合物进行了放射化学检查,并从其与金黄色葡萄球菌的体外结合以及在MWR模型中的吸收百分比方面进行了生物学检查。放射化学方面,(99m)Tc(CO)(3)-MXND配合物在生理盐水中长达240分钟显示出超过90%的稳定性,在血清中16小时内出现了14.95%的不良物种。体外实验中,(99m)Tc(CO)(3)-MXND配合物与金黄色葡萄球菌显示出饱和结合。在人工感染活金黄色葡萄球菌的MWR中,该配合物在感染肌肉中的摄取量比正常肌肉高约六倍。然而,在感染热灭活金黄色葡萄球菌的MWR中,观察到感染和发炎或正常肌肉中(99m)Tc(CO)(3)-MXND配合物的摄取量没有显著变化。(99m)Tc(CO)(3)-MXND配合物在60-90分钟内从循环系统中消失并出现在泌尿系统中,随后通过泌尿系统的正常途径排出。基于在生理盐水、血清中升高且稳定的放射化学稳定性、与金黄色葡萄球菌的体外饱和结合以及在MWR靶器官中的较高积累,我们推荐(99m)Tc(CO)(3)-MXND配合物用于人类金黄色葡萄球菌感染的放射性定位。

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