Vosoughi Sara, Salek Nafise, Maragheh Mohammad Ghannadi, Arani Simindokht Shirvani, Samani Ali Bahrami, Arabieh Masoud
Radiation Application Research School, Nuclear Science and Technology Research Institute (NSTRI), Tehran, Iran.
Nuclear Fuel Research School, Nuclear Science and Technology Research Institute (NSTRI), Tehran, Iran.
Nucl Med Mol Imaging. 2025 Feb;59(1):62-71. doi: 10.1007/s13139-024-00875-0. Epub 2024 Aug 10.
Curcumin as a potent anti-inflammatory and cancer-prevention molecule was labeled with n.c.a Lu. The combination of Lu as a theranostic agent and curcumin as an anti-cancer can be considered for nuclear medicine.
First, n.c.a Lu (specific activity = 48 Ci/mg) was prepared using the extraction chromatography method. Then, semi-empirical quantum chemical calculations were applied to get a deeper insight into the complexation reaction between Lu and curcumin ligand. UV-Vis spectrophotometry was used for the determination of the metal-to-curcumin ratio. Subsequently, a mixture of (111-333 MBq) n.c.a Lu, 50 µL curcumin solution in ethanol, and 450 µL acetate buffer at pH = 5 was incubated for 1 h at 95 ºC. The Lu-curcumin complex chemical structure was characterized using IR spectroscopy. Finally, the prepared complex was analyzed by different quality control tests.
Complexometry using UV-Vis studies showed a 1:2 ratio for Lutetium: curcumin complex which is in agreement with theoretical calculations. The IR-spectra analysis also confirmed the complex formation. The radiochemical purity of n.c.a Lu -curcumin was more than 95% as determined by radio-TLC. The stability of up to 48 h was observed for the prepared complex in serum. The partition coefficient was calculated for the compound (log = -0.31). Evaluating biodistribution in tumoral mice exhibited high tumor uptake (%ID/g = 2.03).
The promising results showed that n.c.a Lu-curcumin can be considered as a possible radiopharmaceutical agent for therapeutic applications.
姜黄素作为一种有效的抗炎和防癌分子，用无载体的镥进行了标记。可考虑将镥作为一种诊疗剂与姜黄素作为抗癌剂的组合应用于核医学。
首先，采用萃取色谱法制备了无载体的镥（比活度 = 48 Ci/mg）。然后，应用半经验量子化学计算，以更深入了解镥与姜黄素配体之间的络合反应。采用紫外可见分光光度法测定金属与姜黄素的比例。随后，将（111 - 333 MBq）无载体的镥、50 μL姜黄素乙醇溶液和450 μL pH = 5的乙酸盐缓冲液混合，在95 ºC下孵育1小时。用红外光谱对镥 - 姜黄素络合物的化学结构进行了表征。最后，通过不同的质量控制测试对制备的络合物进行了分析。
紫外可见光谱的络合滴定法显示镥与姜黄素络合物的比例为1:2，这与理论计算结果一致。红外光谱分析也证实了络合物的形成。放射性薄层色谱法测定无载体的镥 - 姜黄素的放射化学纯度大于95%。观察到制备的络合物在血清中的稳定性高达48小时。计算了该化合物的分配系数（log = -0.31）。对荷瘤小鼠的生物分布评估显示肿瘤摄取率高（%ID/g = 2.03）。
这些有前景的结果表明，无载体的镥 - 姜黄素可被视为一种可能用于治疗应用的放射性药物制剂。
