Radioiodination, and Biological Assessment of Olsalazine, as a Highly Selective Radiotracer for Ulcerative Colitis Imaging in Mice | ||
| Arab Journal of Nuclear Sciences and Applications | ||
| Volume 56, Issue 3, April 2023, Pages 105-120 PDF (853.76 K) | ||
| Document Type: Original Article | ||
| DOI: 10.21608/ajnsa.2022.163538.1639 | ||
| Authors | ||
| Mahmoud H Sanad1; Fawzy Abdel Megeed Marzook2; Safaa Bekheet Challan* 3; Heba Mahmoud Essam4; Ayman B. Farag5 | ||
| 1Labeled Compounds Department, Hot Laboratories Center, Atomic Energy Authority,P.O. Box 13759, Cairo, Egypt | ||
| 2Labelled compound compartment- Hot Lab. Center, Atomic Energy Authority | ||
| 3Cyclotron Project, Nuclear Research Center, Atomic Energy Authority, Inshas , Egypt | ||
| 4Cyclotron Project, Nuclear Research Center, Atomic Energy Authority, Inshas , Egypt. P.O Box 13759 | ||
| 53Pharmaceutical Chemistry Department, Faculty of Pharmacy, Ahram Canadian University, Giza, 12578 Egypt | ||
| Abstract | ||
| Ulcerative colitis (UC) is a chronic, regressive nature disease. The use of conventional diagnostic procedures such as magnetic resonance imaging, ultrasonography, and X-rays during the dormant and early stages of the disease does not aid in diagnosing the disease. As a result, a novel design, such as labelled compounds, was used to image ulcerative colitis disease. In this study, olsalazine was labeled with [125/131I] and the labelling parameters were adjusted to obtain a high radiochemical yield (98.5%). In addition, the olsalazine radiotracer gave 96.0% purity in rate serum for up to twelve hours before it started to degrade at twenty-four hours, it was stable also, in saline for up to twenty-four hours. Molecular docking was used to assess a complex's affinity for its biological target, and the PPAR receptor. We also performed the biological assessment in mice models of both standard and ulcerative colitis. Results demonstrated that [125/131I] iodoolsalazine had a high uptake of 79.5% (ID/g) at 120 minutes post-injection and still high to 77.00% at 24 hours. So, the labelled compound, [131I] iodoolsalazine, could be considered a new potential selective radiotracer for preclinical diagnostic research of ulcerative colitis. | ||
| Keywords | ||
| Keywords: Olsalazine; Iodine-125/131; (PPARγ) Peroxisome Proliferator-Activated Receptors Gamma; Biological Assessment; Imaging Ulcerative Colitis | ||
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