Skip to main content
SpringerLink
Log in

Radiosynthesis and biodistribution of 99mTcN–Garenoxacin dithiocarbamate complex a potential infection imaging agent

  • Published:
Journal of Radioanalytical and Nuclear Chemistry Aims and scope Submit manuscript

Abstract

Garenoxacin (GXN) was modified to its dithiocarbamate followed by radiolabeling with technetium-99m (99mTc) through [99mTc-N]2+ core. The suitability of the 99mTcN–Garenoxacin dithiocarbamate (GXND) complex as a potential multiresistant Staphylococcus aureus (MDRSA) and penicillin-resistant Streptococci (PRSC) infection radiotracer was assessed in artificially infected rats (AFRT). The radiolabeled complex was investigated for its radiochemical purity (RCP), permanence in serum using HPLC and TLC methods. In vitro binding with MDRSA and PRSC was performed at 37 °C. The 99mTcN–GXND showed maximum RCP of 98.00 ± 0.22% and remained more than 90% stable up to 4 h. The 99mTcN–GXND showed saturated in vitro binding with living MDRSA and PRSC, respectively. The complex showed normal biodistribution in healthy rats (HRT), however in AFRT, seven fold uptakes was observed in infected muscle as compared to inflamed and normal muscles. Based on the high RCP, stability in serum, better in vitro binding with bacteria, biodistribution behavior and the target to non-target (infected to inflamed muscle) ratio, we recommend the 99mTcN–GXND complex for in vivo investigation of MDRSA and PRSC infection in human.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Log in via an institution

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

Fig. 1
Fig. 2
Fig. 3
Fig. 4
Fig. 5

Similar content being viewed by others

References

  1. Basu S, Chryssikos T, Moghadam-Kia S, Zhuang H, Torigian DA, Alvai A (2009) Positron emission tomography as a diagnostic tool in infection: present role and future possibilities. Semin Nucl Med 39:36

    Article  Google Scholar 

  2. Gallagher H, Ramsay SC, Barnes J, Maggs J, Cassidy N, Ketheesan N (2006) Neutrophil labeling with [99mTc]-technetium stannous colloid is complement receptor 3-mediated and increases the neutrophil priming response to lipopolysaccharide. Nucl Med Biol 33:433

    Article  CAS  Google Scholar 

  3. Lahiri S, Sarkar S (2007) Studies on 66, 67 Ga- and 199 Tl-poly(N-vinylpyrrolidone) complexes. Appl Radiat Isot 65:309

    Article  CAS  Google Scholar 

  4. Zhang J, Wang X, Tian C (2006) Synthesis of a bis-(N-butyl-dithiocarbamto)-nitrido 99mTc complex: a potential new brain imaging agent. J Radioanal Nucl Chem 273:15

    Article  Google Scholar 

  5. Zhang J, Wang X (2000) Synthesis of 99mTcN(IPDTC)2 and its biodistribution in mice. J Radioanal Nucl Chem 249:573

    Google Scholar 

  6. Hong Z, Ningyi J, Lin Z (2009) Experimental studies on imaging of infected site with 99mTc-labeled ciprofloxacin in mice. Chin Med J 122:1907

    Google Scholar 

  7. Oh SJ, Ryu J, Shin JW, Yoon EJ, Ha H, Cheon JH, Lee HK (2002) Synthesis of 99mTc-ciprofloxacin by different methods and its biodistribution. Appl Radiat Isot 57:193

    Article  CAS  Google Scholar 

  8. Zhang J, Guo H, Zhang S, Lin Y, Wang X (2008) Synthesis and biodistribution of a novel 99mTcN complex of ciprofloxacin dithiocarbamate as a potential agent for infection imaging. Bioorg Med Chem Lett 18:51

    Google Scholar 

  9. Motaleb MA (2007) Preparation of 99mTc-cefoperazone complex, a novel agent for detecting sites of infection. J Radioanal Nucl Chem 272:167

    Article  CAS  Google Scholar 

  10. Motaleb MA (2007) Preparation and biodistribution of 99mTc-lomefloxacin and 99mTc-olfloxacin complex. J Radioanal Nucl Chem 272:95

    Article  CAS  Google Scholar 

  11. EL-Gany EA, EL-Kolaly MT, Amine AM, EL-Sayed AS, Abdel-Gelil F (2005) Synthesis of 99mTc-pefloxacin:a new targeting agent for infectious foci. J Radioanal Nucl Chem 266:131

    Article  Google Scholar 

  12. Roohi S, Mushtaq A, Jehangir M, Ashfaq MS (2006) Synthesis, quality control and biodistribution of 99mTc-kanamycin. J Radioanal Nucl Chem 267:561

    Article  CAS  Google Scholar 

  13. Motaleb MA (2009) Preparation, quality control and stability of 99mTc-sparafloxacin complex, a novel agent for detecting sites of infection. J Label Compd Radiopharm 52:415

    Article  CAS  Google Scholar 

  14. Chattopadhyay S, Das SS, Chandra S, De K, Mishra M, Sarkar BR, Sinha S, Ganguly S (2010) Synthesis and evaluation of 99mTc-moxifloxacin, a potential infection specific imaging agent. Appl Radiat Isot 68:314

    Article  CAS  Google Scholar 

  15. Qaiser SS, Khan AU, Khan MR (2010) Synthesis, biodistribution and evaluation of 99mTc-Sitafloxacin kit: a novel infection imaging agent. J Radioanal Nucl Chem 284:189

    Article  CAS  Google Scholar 

  16. Shah SQ, Khan AU, Khan MR (2010) Radiosynthesis of 99mTc-nitrifuratonin a novel radiotracer for in vivo imaging of Escherichia coli infection. J Radioanal Nucl Chem (in press)

  17. Shah SQ, Khan AU, Khan MR (2010) Radiosynthesis and biodistribution of 99mTc-rifampicin: a novel radiotracer for in vivo infection imaging. Appl Radiat Isot 68:2255

    Article  CAS  Google Scholar 

  18. Shah SQ, Khan AU, Khan MR (2010) 99mTc-Novobiocin: a novel radiotracer for infection imaging. Radiochim Acta (in press)

  19. Shah SQ, Khan AU, Khan MR (2010) Radiosynthesis, biodistribution and scintigraphy of the 99mTc-Teicoplanin complex in artificially infected animal models. J Label Compd Radiopharm (in press)

  20. Shah SQ, Khan AU, Khan MR (2010) Radiosynthesis and biological evaluation of 99mTcN-sitafloxacin dithiocarbamate as a potential radiotracer for Staphylococcus aureus infection. J Radioanal Nucl Chem (in press)

  21. Ohsaki Y, Morita K, Takeda H, Kishino S, Okumura S, Fujiuchi S (2010) Pharmacokinetics of garenoxacin in elderly patients with respiratory tract infections. Int J Antimicrob Agents 35:603

    Article  CAS  Google Scholar 

  22. Goto K, Yabe K, Suzuki T, Jindo T, Sanbuissho A (2010) Chondrotoxicity and toxicokinetics of novel quinolone antibacterial agents DC-159a and DX-619 in juvenile rats. Toxicology 276:122

    Article  CAS  Google Scholar 

  23. Welling MM, Paulusma-Annema A, Batler HS, Pauwels EKJ, Nibbering PH (2000) Technetium-99m labelled antimicrobial peptides discriminate between bacterial infections and sterile inflammations. Eur J Nucl Med 27:292

    Article  CAS  Google Scholar 

  24. Baldas J, Bonnyman J, Poer PM, Williams GA, Mackay MF (1981) Synthesis And Structure of bis(diethyldithiocarbamato)nitridotechnetium(V)—a technetium-nitrogen triple bond. J Chem Soc Dalton Trans 9:1798

    Article  Google Scholar 

Download references

Author information

Authors and Affiliations

  1. Nuclear Medicine Research Laboratory (NMRL), University of Peshawar, Peshawar, KPK, Pakistan

    Syed Qaiser Shah

  2. Nuclear Medicine, Oncology and Radiotherapy Institute (NORI), Islamabad, Pakistan

    Aakif Ullah Khan

  3. Phytopharmaceutical & Neutraceuticals Research Laboratory (PNRL), University of Peshawar, Peshawar, KPK, Pakistan

    Muhammad Rafiullah Khan

Authors
  1. Syed Qaiser Shah
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Aakif Ullah Khan
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. Muhammad Rafiullah Khan
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to Syed Qaiser Shah.

Rights and permissions

Reprints and permissions

About this article

Cite this article

Shah, S.Q., Khan, A.U. & Khan, M.R. Radiosynthesis and biodistribution of 99mTcN–Garenoxacin dithiocarbamate complex a potential infection imaging agent. J Radioanal Nucl Chem 288, 59–64 (2011). https://doi.org/10.1007/s10967-010-0871-3

Download citation

  • Received:

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1007/s10967-010-0871-3

Keywords

Search

Navigation