Nasir MAHMOOD, Zulfiqar Ali KHAN, Syed Ali Raza NAQVI, Malik Muhammad ISHFAQ, Saeed Ahmad NAGRA, Iftikhar Hussain BUKHARI, Abdullah Ijaz HUSSAIN, Sohail Anjum SHAHZAD, Asma HAQUE, Tanveer Hussain BOKHARI

7084

$^{99m}Tc$ labeled levofloxacin as an infection imaging agent: a novel method for labeling levofloxacin using cysteine·HCl as co-ligand and in vivo study

$^{99m}Tc$ labeled levofloxacin as an infection imaging agent: a novel method for labeling levofloxacin using cysteine·HCl as co-ligand and in vivo study

Levofloxacin was labeled with $^{99m}Tc$ using cysteine·HCl as co-ligand and $SnCl_2.2H_2O$ as reducing agent. The influence of various parameters such as amount of cysteine·HCl, reducing agent, pH value, and reaction time on labeling process was studied. After optimizing the conditions the labeling was performed at pH 5 using 1 mg of levofloxacin, 500 μg of cysteine· HCl, 50 μg of $SnCl_2.2H_2O$, and 15 min reaction time. The radiochemical purity was determined with the help of instant thin layer chromatography (ITLC) and reverse phase high performance liquid chromatography (RP-HPLC) which was more than 95% and was stable for up to 6 h. Biodistribution of $^{99m}Tc$-levofloxacin ( $^{99m}Tc$-lefx) was studied in infection induced rat models using live Staphylococcus aureus and heat killed S. aureus (sterile inflammation model). In the case of the live S. aureus induced abscess model, the accumulation of $^{99m}Tc$-lefx at target was 3.96, which was higher than that of $^{99m}Tc$-ciprofloxacin ( $^{99m}Tc$-cifx), taken as the control.
PDF

___

  • 1. Naqvi, S. A. R.; Matzow, T.; Finucane, C.; Nagra, S. A.; Ishfaq, M. M.; Mather, S. J.; Sosabowski, J. Cancer Biotherapy & Radiopharmaceuticals 2010, 25, 89-95.
  • 2. von Guggenberg, E.; Dietrich, H.; Skvortsova, I.; Gabriel, M.; Virgolini, I. J.; Decristoforo, C. Eur. J. Nucl. Med. Mol. Imaging 2007, 34, 1209-1218.
  • 3. Signore, A.; Annovazzi, A.; Barone, R.; Bonanno, E.; D’Alessandria, C.; Chianelli, M.; Mather, S. J.; Bottoni, U.; Panetta, C.; Innocenzi, D.; Scopinaro, F.; Calvieri, S. J. Nucl. Med. 2004, 45, 1647-1652.
  • 4. Santin, M.; Podzamczer, D.; Ricart, I.; Mascar´o, J.; Ram´on, J. M.; Dominguez, A.; Ruf´ı, G.; Gudiol, A. F. Clin. Infect. Dis. 1995, 20, 652-656.
  • 5. Froelich, J. W.; Swanson, D. Semin. Nucl. Med. 1984, 14, 128-140.
  • 6. Buscombe, J. R.; Lui, D.; Ensing, G.; de Jong, R.; Ell, P. J. Eur. J. Nucl. Med. 1990, 16, 649-655.
  • 7. Bhatnagar, A.; Singh, A. K.; Singh, T.; Shankar, L. R. Nuclear Medicine Communications 1995, 16, 1052-1062.
  • 8. Flivik, G.; Sloth, M.; Rydholm, U.; Herrlin, K.; Lidgren, L. J. Nucl. Med. 1993, 34, 1646-1650.
  • 9. Seral, C.; Barcia-Macay, M.; Mingeot-Leclercq, M. P.; Tulkens, P. M.; Bambeke, F. V. J. Antimicrob. Chemother. 2005, 55, 511-517.
  • 10. Wagenlehner, F. M. E.; Krieger, J. N. Pelviperineology 2011, 30, 17-26.
  • 11. Carratal`a, J.; Garcia-Vidal, C. Curr Opin Infect Dis 2010, 23, 152-157.
  • 12. Falc´o, V.; Molina, I.; Juste, C.; Crespo, M.; Almirante, B.; Pigrau, C.; Ferrer, A.; Bravo, C.; Palomar, M.; Pahissa, A. Enferm. Infecc. Microbiol. Clin. 2006, 24, 360-364.
  • 13. Griffin, A. T.; Peyrani, P.; Wiemken, T.; Arnold, F. Int J Tuberc Lung Dis 2010, 14, 495-499.
  • 14. Pedro-Botet, M. L.; Garc´ıa-Cruz, A.; Tural, C.; Mateu, L.; Sopena, N.; Roure, S.; Rey-Joly, C.; Sabria, M. J. Chemother. 2006, 18, 559-561.
  • 15. Drago, L.; De Vecchi, E.; Mombelli, B.; Nicola, L.; Valli, M.; Gismondo, M. R. J. Antimicrob. Chemother. 2001, 48, 37-45.
  • 16. Solanki, K. K.; Bomanji, J.; Siraj, Q.; Small, M.; Britton, K. E. J. Nucl. Med. 1993, 34, 119P.
  • 17. Shimpi, H. H.; Nair, N. Indian J. Nucl. Med. 2003, 18, 16.
  • 18. EL-Ghany; Amin, E. A.; Kawy, A. M.; Amin, O. A. Journal of Labelled Compounds and Radiopharmaceuticals 2007, 50, 25-31.
  • 19. Ibrahim, I. T.; Motaleb, M. A.; Attalah, K. M. Journal of Radioanalytical and Nuclear Chemistry 2010, 285, 431-436.
  • 20. Siaens, R. H.; Rennen, H. J.; Boerman, O. C.; Dierckx, R.; Slegers, G. J. Nucl. Med. 2004, 45, 2088-2094.
  • 21. Singh, A. K.; Verma, J.; Bhatnagar, A.; Ali, A. World J. Nucl. Med. 2003, 103-109.
  • 22. Wolfson, J. S.; Hooper, D. C. Antimicrobial Agents and Chemotherapy 1985, 28, 581-586.
  • 23. Evans, M. E.; Titlow, W. B. J. Antimicrob. Chemother. 1998, 41, 285-288.
  • 24. Wimer, S. M.; Schoonover, L.; Garrison, M. W. Clin Ther, 1998, 20, 1049-1070.
Turkish Journal of Chemistry-Cover
  • ISSN: 1300-0527
  • Yayın Aralığı: 6
  • Yayıncı: TÜBİTAK
Arşiv
Sayıdaki Diğer Makaleler

Synthesis of some new urea and thiourea derivatives and evaluation of their antimicrobial activities

Yıldız GÜLKOK, Tuba BİÇER, Fatma Kaynak ONURDAĞ, Selda ÖZGEN

Determination of cadmium in high salt content matrices by flow injection cold vapor atomic absorption spectrometry

Orkun ALP, Hakan DEMİRÖZ, Osman Yavuz ATAMAN, Nusret ERTAŞ

Simultaneous determination of Cr(III) and Cr(VI) using differential pulse polarography and application to Gerede River

Olcay ŞENDİL, Nabeel MOHAMMED, Güler SOMER

Influence of reaction parameters on the synthesis of surfactant-assisted tin oxide nanoparticles

Muhammad Akhyar FARRUKH, Prisca Tan And Rohana ADNAN

Preparation and antimicrobial activity evaluation of some quinoline derivatives containing an azole nucleus

Muhammet ÖZYANIK, Serpil DEMİRCİ, Hakan BEKTAŞ, Neslihan DEMİRBAŞ

Theory of adsorption equilibria analysis based on general equilibrium constant expression

Abdul Sattar Ali KHAN

Antimicrobial properties and DNA interactions studies of 3-hetarylazoquinoline-2,4-diol compounds

Fatma ÖZTÜRK, Leyla AÇIK, İzzet ŞENER, Fikret KARCI

99mTc labeled levofloxacin as an infection imaging agent: a novel method for labeling levofloxacin using cysteine\cdot HCl as co-ligand and in vivo study

Syed Ali Raza NAQVI, Malik Muhammad ISHFAQ, Zulfiqar Ali KHAN

Synthesis and evaluation of enzyme inhibitory potential of some derivatives of scopolamine

Durre SHAHWAR, Muhammad Asam RAZA, Tania KHAN

Novel biologically active glycosides from the aerial parts of Cephalaria gazipashensis

Nazlı Böke Sarikahya And Süheyla KIRMIZIGÜL