Technetium-99m radiolabeling through conjugation with l,l-ethylene dicysteine chelator of a trimethoxylated flavone and its bioevaluation in rat with induced C6 glioma tumor as a new cancer diagnostic agent

IF 1.4 3区 化学 Q4 CHEMISTRY, INORGANIC & NUCLEAR
Maryam Ghalbi Ahangari, Mahdi Moridi Farimani, Mostafa Erfani, Mostafa Goudarzi
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Abstract

Xanthomicrol (4′,5-dihydroxy-6,7,8-trimethoxyflavone) is the main active component of Dracocephalum kotschyi Boiss leaf extract. It has showed selective cytotoxic activity against some cancer cell lines and little effect on human fetal foreskin fibroblast cells used as nonmalignant control. This study aimed to develop 99mTc-labeled xanthomicrol and to evaluate its efficiency as a new tumor imaging agent. l,l-Ethylene dicysteine (EC) chelator was conjugated to xanthomicrol. EC-Xanthomicrol was labeled with technetium-99m by using tin chloride as a reducing agent and incubating at room temperature. Radiochemical purity and in vitro stability were analyzed by thin layer chromatography and high-performance liquid chromatography. In vitro cellular uptake and binding profile of radio-conjugate was determined on C6 glioma cells. In vivo bioevaluation and imaging studies of [99mTc]Tc-EC-Xanthomicrol were performed in C6 glioma tumor induced rat at different time points after injection of radio-conjugate. The high radiochemical yield (>95 %) was achieved for [99mTc]Tc-EC-Xanthomicrol which was stable up to 6 h. The radio-conjugate indicated high cell uptake (35.12 % at 2 h) which demonstrated to be specific. Tumor uptake was seen for [99mTc]Tc-EC-Xanthomicrol (1.23 ± 0.14 %ID/g) at 1 h post injection. Scintigraphy confirmed that tumors could be visualized clearly with [99mTc]Tc-EC-Xanthomicrol. The results indicated that [99mTc]Tc-EC-Xanthomicrol has potential to be considered as a new radiotracer in glioma tumor imaging.
通过与三甲氧基化黄酮的 l,l-亚乙基二半胱氨酸螯合剂共轭进行锝-99m 放射性标记,并在诱发 C6 胶质瘤肿瘤的大鼠身上进行生物评估,作为一种新的癌症诊断剂
黄腐醇(4′,5-二羟基-6,7,8-三甲氧基黄酮)是龙脑叶提取物的主要活性成分。它对一些癌细胞株具有选择性细胞毒性活性,而对作为非恶性对照的人胎儿包皮成纤维细胞则影响甚微。这项研究旨在开发 99mTc 标记的黄独醇,并评估其作为一种新型肿瘤成像剂的效率。以氯化亚锡为还原剂,在室温下培养,用锝-99m标记EC-Xanthomicrol。采用薄层色谱法和高效液相色谱法分析了放射化学纯度和体外稳定性。在 C6 胶质瘤细胞上测定了放射性结合物的体外细胞摄取和结合情况。在大鼠注射[99mTc]Tc-EC-Xanthomicrol后的不同时间点,对[99mTc]Tc-EC-Xanthomicrol进行了体内生物评估和成像研究。[99mTc]Tc-EC-Xanthomicrol的放射化学收率很高(95%),且稳定达6小时。注射后 1 小时,[99mTc]Tc-EC-Xanthomicrol 显示出肿瘤摄取(1.23 ± 0.14 %ID/g)。闪烁照相法证实,[99m锝]锝-EC-黄霉素可清晰显示肿瘤。结果表明,[99m锝]锝-EC-Xanthomicrol有望被视为胶质瘤肿瘤成像的一种新放射性示踪剂。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
Radiochimica Acta
Radiochimica Acta 化学-核科学技术
CiteScore
2.90
自引率
16.70%
发文量
78
审稿时长
6 months
期刊介绍: Radiochimica Acta publishes manuscripts encompassing chemical aspects of nuclear science and technology.
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