Improved 68Ga-labeling method using ethanol addition: Application to theQ1alpha-helical peptide DOTA-FAMP.
Improved 68Ga-labeling method using ethanol addition: Application to theQ1alpha-helical peptide DOTA-FAMP.
复制标题
使用乙醇添加改进的 68Ga 标记方法：应用于 Q1α-螺旋肽 DOTA-FAMP。
DOI：
10.1002/jlcr.3474
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发表时间：
2017
期刊：
影响因子：
--
通讯作者：
Saku K.
中科院分区：
文献类型：
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作者：
Hasegawa K;Kawachi E;Uehara Y;Yoshida T;Imaizumi S;Ogawa M;Miura S;Saku K.
我们研究了α螺旋肽DOTA-FAMP的68 Ga标记，并评估了放射性标记过程中的构象变化。68 Ga-DOTA-FAMP是动脉粥样硬化斑块的正电子发射断层扫描探针候选者。将Zhernosekov方法（使用丙酮纯化68 Ga）获得的标记产率与原始和2种改进的Mueller方法（使用NaCl溶液）获得的标记产率进行比较。改进的方法I涉及在标记之前对68 Ga进行脱盐，改进的方法II涉及在标记溶液中加入乙醇。使用Zhernosekov方法的标记产率为62% ± 5.4%。相比之下，Mueller的原始方法给出了8.9% ± 1.7%。改良方法I的改善率为32% ± 2.1%。改进的方法II使产率进一步提高到66% ± 3.4%。通过圆二色性光谱法确定了构象变化，表明这些差异可能归因于构象变化。热处理影响肽构象，导致聚集并降低标记产率。Mueller的方法更简单，但苛刻的条件使其无法应用于生物分子。为了抑制聚集，我们在标记溶液中加入了乙醇并进行了标记过程。这些变化显著提高了标记产率。在用于成像之前，应通过圆二色谱法评价放射性标记过程中生物分子的构象变化，以确保标记产物的均匀性。
We examined the68Ga labeling of the α‐helical peptide, DOTA‐FAMP, and evaluated conformational changes during radiolabeling.68Ga‐DOTA‐FAMP is a positron emission tomography probe candidate for atherosclerotic plaques. The labeling yield achieved by Zhernosekov's method (using acetone for68Ga purification) was compared with that achieved by the original and 2 modified Mueller's methods (using NaCl solution). Modified method I involves desalting the68Ga prior to labeling, and modified method II involves the inclusion of ethanol in the labeling solution. The labeling yield using Zhernosekov's method was 62% ± 5.4%. In comparison, Mueller's original method gave 8.9% ± 1.7%. Modified method I gave a slight improvement of 32% ± 2.1%. Modified method II further increased the yield to 66% ± 3.4%. Conformational changes were determined by circular dichroism spectroscopy, revealing that these differences could be attributed to conformational changes. Heat treatment affects peptide conformation, which leads to aggregation and decreases the labeling yield. Mueller's method is simpler, but harsh conditions preclude its application to biomolecules. To suppress aggregation, we included a desalting process and added ethanol in the labeling solution. These changes significantly improved the labeling yield. Before use for imaging, conformational changes of biomolecules during radiolabeling should be evaluated by circular dichroism spectroscopy to ensure the homogeneity of the labeled product.