Radiosynthesis and biological evaluation of the (99m)Tc-tricarbonyl moxifloxacin dithiocarbamate complex as a potential Staphylococcus aureus infection radiotracer.
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.
Nuclear Medicine Research Laboratory, University of Peshawar, KPK, Pakistan. ssqaiser2002@yahoo.com
Syed Qaiser
SQ
Shah
Muhammad Rafiullah
MR
Khan
D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use; D001372:Aza Compounds / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use; D002851:Chromatography, High Pressure Liquid; D024841:Fluoroquinolones; D008297:Male; D000077266:Moxifloxacin; D015609:Organotechnetium Compounds / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use; D011804:Quinolines / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use; D051381:Rats; D017208:Rats, Wistar; D013203:Staphylococcal Infections / Q000188:drug therapy / Q000382:microbiology; D013211:Staphylococcus aureus / Q000187:drug effects*
D000900:Anti-Bacterial Agents; D001372:Aza Compounds; D024841:Fluoroquinolones; D015609:Organotechnetium Compounds; D011804:Quinolines; D000077266:Moxifloxacin