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그림 1. (A) 벤즈아마이드의 화학적 구조 및 (B) N-(2-(dimethylamino)ethyl)-4-18F-fluorobenzamide ([18F]DMFB)의 화학적 구조

그림 2. 원발성 및 전이성 흑색종 소동물 모델을 이용한 [18F]DMFB의 영상평가. (A) 피하이식 흑색종 소동물 모델에서 [18F]DMFB 정맥주사 후 10, 30, 60분 후의 PET 영상. (B) 폐 전이, (C) 간 전이, (D) 림프절 전이 흑색종 소동물 모델에서 [18F]DMFB 정맥주사 후 60분 후의 PET 영상

Abstract
Malignant melanoma is an aggressive and serious form of skin cancer, with prognosis and treatment outcome depending heavily on the clinical stage of the disease at the time of diagnosis. Here, we synthesized a novel 18F-labeled benzamide derivative to target melanoma and then evaluated its biologic characteristics in small-animal models. Methods: N-(2-(dimethylamino)ethyl)-4-18F-fluorobenzamide (18F-DMFB) was synthesized by reaction of N-succinimidyl 4-18F-fluorobenzoate with N,N-dimethylethylenediamine. The binding affinity of 18F-DMFB was measured in B16F10 (mouse melanoma) cells with or without l-tyrosine. Small-animal PET imaging with 18F-DMFB was performed on B16F10 xenograft and metastasis mouse models. Results: The overall non-decay-corrected radiochemical yield of 18F-DMFB was approximately 10%-15%. Uptake of 18F-DMFB was melanin-specific, as cellular uptake in B16F10 increased more than 18-fold in the presence of l-tyrosine. Biodistribution studies revealed that 18F-DMFB accumulated, and was retained, in B16F10 xenografts for 120 min (10, 30, 60, and 120 min: 9.24, 10.80, 13.0, and 10.59 percentage injected dose/g, respectively) after radiotracer injection. Liver uptake of 18F-DMFB decreased from 10 to 120 min and showed fast clearance (10, 30, 60, and 120 min: 11.19, 5.7, 2.47, and 0.4 percentage injected dose/g). Furthermore, 18F-DMFB allowed visualization of metastatic lesions immediately after injection and was retained in lesions for over 60 min, with a high tumor-to-background ratio. Conclusion: 18F-DMFB demonstrated a high melanin-targeting ability and tumor-specific tumor uptake in both primary and metastatic lesions in animal models bearing malignant melanoma. 18F-DMFB may be a potential PET imaging agent for melanoma.

Author information

Pyo A1, Kim HS1, Kim HS2, Yun M3, Kim DY4, Min JJ4.
1
Department of Nuclear Medicine, Chonnam National University Medical School and Hwasun Hospital, Hwasun, Korea.
2
Department of Forensic Medicine, Chonnam National University Medical School, Hwasun, Korea; and.
3
Microbiology and Functionality Research Group, Research and Development Division, World Institute of Kimchi, Gwangju, Korea.
4
Department of Nuclear Medicine, Chonnam National University Medical School and Hwasun Hospital, Hwasun, Korea jjmin@jnu.ac.kr blueburr@gmail.com.

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