Synthesis, Radiolabeling, and Bioevaluation of Bis(Trifluoromethanesulfonyl) Imide

Ersoz O. A., Soylu H. M., Er O., Ocakoglu K., Lambrecht F. Y., YILMAZ O.

CANCER BIOTHERAPY AND RADIOPHARMACEUTICALS, vol.30, no.9, pp.395-399, 2015 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 30 Issue: 9
  • Publication Date: 2015
  • Doi Number: 10.1089/cbr.2014.1738
  • Journal Name: CANCER BIOTHERAPY AND RADIOPHARMACEUTICALS
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.395-399
  • Keywords: biodistribution, imidazolium salts, nuclear medicine, I-131, radiolabeling, IMIDAZOLIUM SALTS, BIODISTRIBUTION, I-131
  • Dokuz Eylül University Affiliated: Yes

Abstract

Imidazolium salts have antitumor potential and toxicological effects on various microorganisms. The authors' aim is to synthesize a new imidazolium salt and to assess its pharmacokinetic and antitumor potentials by in vitro and in vivo studies. In this study, bis(trifluoromethanesulfonyl) imide (ITFSI) was synthesized and labeled with I-131 using the iodogen method. The efficiency of radiolabeling was determined with high yield (95.5%+/- 3.7%). Pharmacokinetic properties of the compound were investigated in albino Wistar rats using radiolabeled compound. The radiolabeled compound (I-131-ITFSI) has been stable during a period of 3 hours in human serum. The uptake of I-131-ITFSI reached maximum in the spleen, liver, and blood at 60 minutes, large intestine and heart at 30 minutes, and ovary at 120 minutes. It is observed that intracellular uptake of the radiolabeled compound is higher in the CaCo-2 (colon adenocarcinoma tumor) cell line than HEK-293 (human epithelial kidney) cell line. In further study, antitumor potential of ITFSI on a colon adenocarcinoma tumor-bearing animal model may be investigated.