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

Maryam Ghalbi Ahangari; Mahdi Moridi Farimani; Mostafa Erfani; Mostafa Goudarzi

doi:10.1515/ract-2023-0239

Article

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

Maryam Ghalbi Ahangari , Mahdi Moridi Farimani , Mostafa Erfani and Mostafa Goudarzi

Published/Copyright: March 18, 2024

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From the journal Radiochimica Acta Volume 112 Issue 5

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.

Keywords: xanthomicrol; chelator; technetium-99m; labeling; tumor; imaging

Corresponding author: Mostafa Erfani, Radiation Application Research School, Nuclear Science and Technology Research Institute (NSTRI), Tehran, Iran, E-mail: mgandomkar@aeoi.org.ir

Acknowledgments

The support by NSTRI, Tehran, Iran, is gratefully acknowledged.

Research Ethics: Animals were treated according to ethical principles for animal experiments.
Author contributions: Maryam Ghalbi Ahangari, Mahdi Moridi Farimani, Mostafa Erfani and Mostafa Goudarzi contributed to the study conception and design.
Competing interests: The authors declare no competing interests.
Research funding: There was no funding.
Data availability: The data are available on reasonable request.

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Received: 2023-10-07

Accepted: 2024-01-08

Published Online: 2024-03-18

Published in Print: 2024-05-27

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Articles in the same Issue

https://doi.org/10.1515/ract-2023-0239

Keywords for this article

xanthomicrol; chelator; technetium-99m; labeling; tumor; imaging