Iohexol, a low osmolality nonionic contrast media, is a tri-iodinated benzene derivative with a molecular weight of 821.1Da[1]. Iohexol is used as a marker of glomerular filtration rate (GFR) and as an alternative to radiotracer[2].
In vitro, Iohexol treatment for 72 hours significantly inhibited the viability of CC-531 and AML12 cells, with IC50 values of 46.6mM and 26.8mM, respectively[3]. Treatment of HK-2 cells with 100mgI/ml Iohexol for 24 hours significantly induced apoptosis, mitochondrial damage, and significantly inhibited cell migration[4]. Treatment of NRK 52-E cells with 150mgI/ml Iohexol for 12 hours resulted in massive cell death, resulting in numerous round vacuoles in the cytoplasm[5].
In vivo, Iohexol treatment via single dose injection of 5μl (300mg/mL) into the left paw of mice for 15 minutes increased paw thickness and swelling, inducing a local anaphylactogenic reaction in mice[6]. Intraperitoneal injection of a single dose of Iohexol (3gI/kg) for 24h resulted in renal lesions in C57BL/6 mice, with vacuolization of the renal cortex and induction of proximal tubular inflammation[7].
References:
[1] Seegmiller J C, Eckfeldt J H, Lieske J C. Challenges in measuring glomerular filtration rate: a clinical laboratory perspective[J]. Advances in chronic kidney disease, 2018, 25(1): 84-92.
[2] Brown S C W, O’reilly P H. Iohexol clearance for the determination of glomerular filtration rate in clinical practice: evidence for a new gold standard[J]. The Journal of urology, 1991, 146(3): 675-679.
[3] Melancon M P, Yevich S, Avritscher R, et al. A novel irinotecan-lipiodol nanoemulsion for intravascular administration: pharmacokinetics and biodistribution in the normal and tumor bearing rat liver[J]. Drug delivery, 2021, 28(1): 240-251.
[4] Xiao-Yan G O U, Yong L I, Xiao-Ping F A N. The Role of Mdivi-1 in Reducing Mitochondrial Fission via the NF-κB/JNK/SIRT3 Signaling Pathway in Acute Kidney Injury[J]. Physiological Research, 2025, 74(1): 79.
[5] Jensen H, Doughty R W, Grant D, et al. The effects of the iodinated X-ray contrast media iodixanol, iohexol, iopromide, and ioversol on the rat kidney epithelial cell line NRK 52-E[J]. Renal failure, 2011, 33(4): 426-433.
[6] Yuan F, Zhang C, Sun M, et al. MRGPRX2 mediates immediate-type pseudo-allergic reactions induced by iodine-containing iohexol[J]. Biomedicine & Pharmacotherapy, 2021, 137: 111323.
[7] Lee H T, Jan M, Bae S C, et al. A1 adenosine receptor knockout mice are protected against acute radiocontrast nephropathy in vivo[J]. American Journal of Physiology-Renal Physiology, 2006, 290(6): F1367-F1375.
Iohexol是一种低渗透压非离子型造影剂，为三碘化苯衍生物，分子量为821.1Da[1]。Iohexol被用作肾小球滤过率（GFR）的标志物和放射性示踪剂的替代品[2]。
在体外，Iohexol处理72小时可显著抑制CC-531和AML12细胞活力，IC50值分别为46.6mM和26.8mM[3]。100mgI/ml的Iohexol处理HK-2细胞24小时能显著诱导细胞凋亡和线粒体损伤，并抑制细胞迁移[4]。150mgI/ml的Iohexol处理NRK 52-E细胞12小时会引发大量细胞死亡，导致胞质中出现大量圆形空泡[5]。
在体内，小鼠左爪单次注射5μl的Iohexol（300mg/mL；15分钟）可增加爪部厚度和肿胀，诱发局部过敏反应[6]。C57BL/6小鼠单次腹腔注射3gI/kg的Iohexol（24小时）会引起肾损伤，导致肾皮质空泡化和近端肾小管炎症[7]。