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題名 | Synthesis and Evaluation of 67Ga- and 68Ga-DOTA-glutamine=鎵-67-與鎵-68-DOTA-麩醯胺酸之合成及評估 |
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作者 | 郭雅雯; 陳宛柔; 李德偉; 羅建苗; Kou, Ya-wen; Chen, Wan-jou; Lee, Te-wei; Lo, Jem-mau; |
期刊 | 核子醫學雜誌 |
出版日期 | 20090300 |
卷期 | 22:1 2009.03[民98.03] |
頁次 | 頁35-42 |
分類號 | 414.93 |
語文 | eng |
關鍵詞 | 麩醯胺酸; 鎵-67/鎵-68-DOTA-麩醯胺酸; 纖維瘤細胞; 生物分布; Glutamine; □Ga-/□Ga-DOTA-glutamine; Nfsa tumor; Biodistribution; |
中文摘要 | 背景:藉由放射性同位素標幟麩醯胺酸(glutamine)可以動態追蹤其在身體內之作用,尤其可應用於腫瘤造影及腫瘤內蛋白質合成速率之偵測。本研究製備鎵-67及镓-68標幟麩醯胺酸造影劑並評估其作爲腫瘤造影之目的。 方法:以Fmoc固相合成方法將麩醯胺酸與雙官能基螯合濟l, 4, 7, 10-tetraazacyclododecane N, N', N", N"'-tetraacetic acid (DOTA)進行耦合反應,形成l, 4, 7, 10-tetraazacyclododecane N, N', N", N"'-tetraacetic acid-glutamine (DOTA-麩醯胺酸)耦合物。先將DOTA-麩醯胺酸溶解於乙醇中,進而與鎵-67-citrate或鎵-68-(acac)3分別於室溫及65℃下超音波振盪20鐘,經置換反應完成標幟。以薄層層析法及電泳動分析法分析其標幟效率、帶電性及穩定度,並利用植有纖維瘤細胞的C3H/HeN小公鼠進行動物組織器官之生物分佈實驗。 結果:經由放射化學分析證實鎵-67/鎵-68-DOTA-麩醯胺酸爲帶負電性且穩定性高之標幟耦合物。由植有纖維瘤細胞的C3H/HeN小公鼠之生物分佈實驗結果得知,鎵-67-DOTA-麩醯胺酸顯著滯留於血液中;注入標幟耦合物後10分鐘及120分鐘,血中劑量分別爲32.5%和28.7% ID/g。其他器官/組織大致於注入標幟耦合物10分鐘內便迅速達到平衡。相較於肌肉的吸收,腫瘤的吸收相當稀少。 結論:鎵-67-DOTA-麩醯胺酸生物分佈結果與氮-13標幟麩醯胺酸和麩胺酸(glutamic acid)的分佈趨勢具有相當大的差異。鎵-67/鎵-68-DOTA-麩醯胺酸顯然不是合適的麩醯胺酸和麩胺酸的類似物,所以利用鎵-67/鎵-68-DOTA-麩醯胺酸作爲腫瘤造影劑仍有很大的改進空間。 |
英文摘要 | Background: Radiolabeled glutamine can be used for tracing glutamine for its dynamic function in the body, particularly for imaging and for determination of protein synthesis rates in tumors. This study prepared 67Ga-and 68Ga-labeled glutamine and evaluate for their potentials for tumor imaging. Methods: Glutamine was conjugated to a macrocyclic bifunctional chelator, DOTA, by solid phase synthesis using Fmoc approach. The DOTA-glutamine conjugate was labeled with 67Ga or 68Ga conducting by mixing the radioactive Ga(superscript 3+) species with the conjugate in ethanol and reacting at 65℃. Results: The resultant 67Ga-or 68Ga-DOTA-glutamine was characterized to be anionic and assayed to be stable. In biodistribution study using C3H/HeN mice inoculated with Nfsa tumor, 67Ga-DOTA-glutamine was prominently retained in blood, with around 32.5% and 28.7% ID/g at 10 min and 120 min postinjection, respectively. The distribution of 67Ga-DOTA-glutamine in various organs or tissues generally reached equilibrium quickly within 10 min. The tumor uptake was scarce and shielded by comparable muscle uptake. Conclusion: The biodistribution pattern of 67Ga-DOTA-glutamine is much different from the biogenic 13Nlabeled glutamine and glutamic acid. 67Ga-or 68Ga-DOTA-glutamine is apparently not a mimicker of glutamine or glutamic acid and its use as tracer needs to be reevaluated. |
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