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  • 2024년 01월호
    [Bioorg Med Chem Lett.] Synthesis and evaluation of 18F-labeled procainamide as a PET imaging agent for malignant melanoma

    경상대 / 표아영, 김동연*

  • 출처
    Bioorg Med Chem Lett.
  • 등재일
    2023 Nov 15:96:129528. doi: 10.1016/j.bmcl.2023.12
  • 저널이슈번호
  • 내용

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    Abstract
    Malignant melanoma has an aggressive nature and a high metastatic propensity resulting in the highest mortality rate of any skin cancer. In this study, we synthesized 18F-labeled procainamide (PCA) for detection of melanoma using positron emission tomography (PET), and evaluated its biological characteristics. The non-decay-corrected radiochemical yield of 18F-PCA was 10-15% and its in vitro stability was over 98% for 2 h. At 1 h, cellular uptake of 18F-PCA was 3.8-fold higher in a group with the presence of l-tyrosine than in a non-l-tyrosine-treated group. Furthermore, 18F-PCA permitted visualization of B16F10 (mouse melanoma) xenografts on microPET after intravenous injection, and was retained in the tumor for 60 min, with a high tumor-to-liver uptake ratio. 18F-PCA showed specific melanoma uptake in primary lesions with a high melanin targeting ability in small animal models. 18F-PCA may have potential as a PET imaging agent for direct melanoma detection.

     

     

    Affiliations

    Ayoung Pyo 1, Misun Yun 2, Boreum Song 1, Seong-Young Kwon 3, Jung-Joon Min 4, Dong-Yeon Kim 5
    1College of Pharmacy and Research Institute of Pharmaceutical Science, Gyeongsang National University, Jinju, Republic of Korea.
    2Hygenic Safety-Material Research Group, Technology Innovation Research Division, World Institute of Kimchi, Gwangju, Republic of Korea.
    3Innovation Center for Molecular Probe Development, Department of Nuclear Medicine, Chonnam National University Medical School and Hwasun Hospital, Hwasun, Republic of Korea.
    4Innovation Center for Molecular Probe Development, Department of Nuclear Medicine, Chonnam National University Medical School and Hwasun Hospital, Hwasun, Republic of Korea; CNCure Biotech, Hwasun, Republic of Korea.
    5College of Pharmacy and Research Institute of Pharmaceutical Science, Gyeongsang National University, Jinju, Republic of Korea; CNCure Biotech, Hwasun, Republic of Korea. Electronic address: dykim@gnu.ac.kr.

  • 키워드
    (18)F-labeling; Malignant melanoma; Molecular imaging; Positron emission tomography; Procainamide.
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