Biological evaluation of [ 99m Tc]Tc-labeled Buthus martensii Karsch Chlorotoxin peptide for glioma imaging
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Biological evaluation of [99mTc]Tc-labeled Buthus martensii Karsch Chlorotoxin peptide for glioma imaging Changcun Liu1,2 · Tiantian Wang1 · Lingzhou Zhao2 · Wenli Qiao2 · Meilin Zhu3 · Jiqin Yang4 · Jinhua Zhao1,2 Received: 4 March 2020 © Akadémiai Kiadó, Budapest, Hungary 2020
Abstract This study was to investigate the synthesis and biological evaluation of [99mTc]Tc-labeled Buthus martensii Karsch Chlorotoxin ([99mTc]Tc-BmK CT) as a radiopharmaceutical for glioma single photon computed emission tomography (SPECT) imaging. The results showed that BmK CT peptide modified with a hexahistidine tag displayed good cytocompatibility in vitro, and could be efficiently radiolabeled with 99mTc via [99mTc]Tc-tricarbonyl chemistry. The [99mTc]Tc-BmK CT showed satisfactory radiochemical purity and stability in vitro, and could be developed as a probe for targeted SPECT imaging of glioma cells in vitro and in a tumor-bearing mouse model. Our data indicated that the synthesized [99mTc]Tc-BmK CT might be developed as a promising imaging agent for glioma diagnostic application. Keywords Buthus martensii Karsch Chlorotoxin · Glioma · 99mTc · SPECT imaging
Introduction Glioma is the most common primary brain cancer in adults, associated with high rates of morbidity and mortality [1, 2]. Even under the current standard of care therapy involving maximum surgical resection combined with radiotherapy and chemotherapy, the prognosis of patients with high-grade gliomas has not substantially improved over the past decades * Meilin Zhu [email protected] * Jiqin Yang qin‑[email protected] * Jinhua Zhao [email protected] 1
Department of Nuclear Medicine, Shanghai General Hospital of Nanjing Medical University, Shanghai 200080, People’s Republic of China
2
Department of Nuclear Medicine, Shanghai General Hospital, Shanghai Jiao Tong University School of Medicine, 100 Haining Road, Shanghai 200080, People’s Republic of China
3
School of Basic Medical Sciences, Ningxia Medical University, Yinchuan 750004, Ningxia, People’s Republic of China
4
Department of Nuclear Medicine, General Hospital of Ningxia Medical University, Yinchuan 750004, Ningxia, People’s Republic of China
[2, 3]. One of the main barriers is its diffusely infiltrative growth pattern and indistinct tumor margins in brain, which frequently results in recurrence following surgery [4]. The ability to adequately distinguish the tumor volume and the extent of infiltration into normal brain parenchyma is critical for glioma treatment. Therefore, a number of efforts have been taken to develop various glioma-specific imaging agents for the solution of this challenge [5–7]. Chlorotoxin (CTX) and CTX-like peptides such as Buthus martensii Karsch Chlorotoxin (BmK CT), have been identified as tumor-targeting agents and radiolabeled with iodine-131 (131I) for the imaging and therapy of gliomas [7, 8]. Several clinical studies suggested that 131I-labeled CTX (131I-CTX) was able to safely enhance the overall survival of recurrent malignant glioma patients in a dos
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