Radioiodination, and Biological Assessment of Olsalazine, as a Highly Selective Radiotracer for Ulcerative Colitis Imaging in Mice

M. Sanad, F. Marzook, S. Challan, H. Essam, A. Farag
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引用次数: 1

Abstract

Ulcerative colitis (UC) is a chronic, regressive natural 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, were used to image ulcerative colitis disease. In this study, olsalazine was labeled with [ 125/131 I] 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, and 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. The biological assessment was also performed in mice models of both standard and ulcerative colitis. The results demonstrated that [ 125/131 I] iodoolsalazine had a high uptake of 79.5% (ID/g) at 120 minutes post-injection and is still high to 77% at 24 hours. So, the labelled compound, [ 125/131 I] iodoolsalazine, could be considered a new potential selective radiotracer for preclinical diagnostic research of ulcerative colitis.
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Olsalazine作为一种用于小鼠溃疡性结肠炎成像的高选择性放射性示踪剂的放射性碘化和生物学评估
溃疡性结肠炎(UC)是一种慢性、退行性自然疾病。在疾病的休眠和早期阶段使用传统的诊断程序,如磁共振成像、超声检查和x射线,无助于疾病的诊断。因此,一种新的设计,如标记化合物,被用于溃疡性结肠炎疾病的成像。在本研究中,奥萨拉嗪采用[125/131 I]标记,并调整标记参数以获得较高的放化产率(98.5%)。此外,奥萨拉津放射性示踪剂在24小时开始降解之前,在12小时内的纯度为96.0%,在生理盐水中也稳定了24小时。分子对接用于评估复合物对其生物靶点和PPAR受体的亲和力。在标准和溃疡性结肠炎小鼠模型中也进行了生物学评价。结果表明,[125/131 I]碘唑嗪在注射后120分钟的吸收率高达79.5% (ID/g), 24小时的吸收率仍高达77%。因此,所标记的化合物[125/131 I] iodoolsalazine可作为一种新的选择性放射性示踪剂用于溃疡性结肠炎的临床前诊断研究。
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