[18F]-1-脱氧-1-氟代 scyllo-肌醇与 [18F]-FDG 用于荷瘤无胸腺鼠炎症、乳腺癌和脑肿瘤的 PET 显像比较。

Comparisons of [18F]-1-deoxy-1-fluoro-scyllo-inositol with [18F]-FDG for PET imaging of inflammation, breast and brain cancer xenografts in athymic mice.

机构信息

Department of Psychiatry, University of Toronto, Toronto, ON, Canada M5T 1R8.

出版信息

Nucl Med Biol. 2011 Oct;38(7):953-9. doi: 10.1016/j.nucmedbio.2011.02.017. Epub 2011 May 6.

DOI:10.1016/j.nucmedbio.2011.02.017

PMID:21982567

Abstract

INTRODUCTION

The aim of the study was to evaluate the uptake of [(18)F]-1-deoxy-1-fluoro-scyllo-inositol ([(18)F]-scyllo-inositol) in human breast cancer (BC) and glioma xenografts, as well as in inflammatory tissue, in immunocompromised mice. Studies of [(18)F]-2-fluoro-2-deoxy-d-glucose ([(18)F]-FDG) under the same conditions were also performed.

METHODS

Radiosynthesis of [(18)F]-scyllo-inositol was automated using a commercial synthesis module. Tumour, inflammation and normal tissue uptakes were evaluated by biodistribution studies and positron emission tomography (PET) imaging using [(18)F]-scyllo-inositol and [(18)F]-FDG in mice bearing subcutaneous MDA-MB-231, MCF-7 and MDA-MB-361 human BC xenografts, intracranial U-87 MG glioma xenografts and turpentine-induced inflammation.

RESULTS

The radiosynthesis of [(18)F]-scyllo-inositol was automated with good radiochemical yields (24.6%±3.3%, uncorrected for decay, 65±2 min, n=5) and high specific activities (≥195 GBq/μmol at end of synthesis). Uptake of [(18)F]-scyllo-inositol was greatest in MDA-MB-231 BC tumours and was comparable to that of [(18)F]-FDG (4.6±0.5 vs. 5.5±2.1 %ID/g, respectively; P=.40), but was marginally lower in MDA-MB-361 and MCF-7 xenografts. Uptake of [(18)F]-scyllo-inositol in inflammation was lower than [(18)F]-FDG. While uptake of [(18)F]-scyllo-inositol in intracranial U-87 MG xenografts was significantly lower than [(18)F]-FDG, the tumour-to-brain ratio was significantly higher (10.6±2.5 vs. 2.1±0.6; P=.001).

CONCLUSIONS

Consistent with biodistribution studies, uptake of [(18)F]-scyllo-inositol was successfully visualized by PET imaging in human BC and glioma xenografts, with lower accumulation in inflammatory tissue than [(18)F]-FDG. The tumour-to-brain ratio of [(18)F]-scyllo-inositol was also significantly higher than that of [(18)F]-FDG for visualizing intracranial glioma xenografts in NOD SCID mice, giving a better contrast.

摘要

简介

本研究旨在评估 [(18)F]-1-脱氧-1-氟代 scyllo-肌醇 ([(18)F]-scyllo-肌醇) 在荷人乳腺癌 (BC) 和神经胶质瘤异种移植瘤以及免疫缺陷小鼠炎症组织中的摄取情况。还进行了相同条件下 [(18)F]-2-氟-2-脱氧-D-葡萄糖 ([(18)F]-FDG) 的研究。

方法

使用商业合成模块自动合成 [(18)F]-scyllo-肌醇。通过 [(18)F]-scyllo-肌醇和 [(18)F]-FDG 的生物分布研究和正电子发射断层扫描 (PET) 成像，评估肿瘤、炎症和正常组织的摄取情况，在荷有 MDA-MB-231、MCF-7 和 MDA-MB-361 人 BC 异种移植瘤、颅内 U-87 MG 神经胶质瘤异种移植瘤和松节油诱导的炎症的免疫缺陷小鼠中进行。

结果

[(18)F]-scyllo-肌醇的放射合成实现了自动化，放射化学产率良好（未经衰变校正为 24.6%±3.3%，65±2 min，n=5），比活度高（≥195GBq/μmol，在合成结束时）。[(18)F]-scyllo-肌醇在 MDA-MB-231 BC 肿瘤中的摄取最高，与 [(18)F]-FDG 相当（分别为 4.6±0.5%ID/g 和 5.5±2.1%ID/g；P=.40），但在 MDA-MB-361 和 MCF-7 异种移植瘤中略低。[(18)F]-scyllo-肌醇在炎症中的摄取低于 [(18)F]-FDG。虽然颅内 U-87 MG 异种移植瘤中 [(18)F]-scyllo-肌醇的摄取明显低于 [(18)F]-FDG，但肿瘤与脑的比值明显更高（10.6±2.5 比 2.1±0.6；P=.001）。

结论

与生物分布研究一致，[(18)F]-scyllo-肌醇的摄取通过 PET 成像成功可视化，在人 BC 和神经胶质瘤异种移植瘤中的摄取低于 [(18)F]-FDG，在炎症组织中的摄取低于 [(18)F]-FDG。[(18)F]-scyllo-肌醇的肿瘤与脑的比值也明显高于 [(18)F]-FDG，用于可视化 NOD SCID 小鼠颅内神经胶质瘤异种移植瘤，具有更好的对比度。