Gorshkov Nikolay Ivanovich, Murko Andrei Yur'evich, Zolotova Yulia Igorevna, Nazarova Olga Vladimirovna, Krasikov Valerii Dmitrievich, Shatik Sergei Vasilievich, Panarin Evgenii Fedorovich
Federal State Budgetary Institution of Science Institute of Macromolecular Compounds, Russian Academy of Sciences (IMC RAS), Russian Federation, V.O. Bolshoy pr. 31, 199004 Saint Petersburg, Russia.
Federal State Budgetary Institution "Russian Research Center for Radiology and Surgical Technologies" of the Ministry of Health of the Russian Federation, Russian Federation, p. Pesochny, ul. Leningradskaya, 70, 197758 Saint Petersburg, Russia.
Polymers (Basel). 2021 Jun 1;13(11):1832. doi: 10.3390/polym13111832.
N-vinylpyrrolidone-co-allylamine copolymers (VP-co-AA) containing iminodiacetic (IDA) chelation units were prepared in the range of molecular masses of the copolymers from 9000 to 30,000 Da depending on polymerization conditions. Non-radioactive organometallic species Re(CO) were introduced into polymeric carriers under mild conditions; the prepared metal-polymeric complexes were characterized by IR, NMR, ESI-MS and HPLC. IR spectra data confirmed the coordination of M(CO) moiety to the polymeric backbone via IDA chelation unit (appearance of characteristic fac-M(CO) vibrations (2005, 1890 cm), as well as the appearance of group of signals in H NMR spectra, corresponding to those inequivalent to methylene protons CHCOO (dd, 4.2 ppm), coordinated to metal ions. The optimal conditions for labeling the PVP-co-AA-IDA copolymers with radioactive Tc(CO) species were determined. The radiochemical yields reached 97%. The obtained radiolabeled polymers were stable in blood serum for 3 h. In vivo distribution experiments in intact animals showed the high primary accumulation of technetium-99m MPC (MM = 15,000 Da) in blood with subsequent excretion via the urinary tract.
根据聚合条件,制备了分子量在9000至30,000 Da范围内、含有亚氨基二乙酸(IDA)螯合单元的N-乙烯基吡咯烷酮-共-烯丙胺共聚物(VP-co-AA)。在温和条件下将非放射性有机金属物种Re(CO)引入聚合物载体中;通过红外光谱(IR)、核磁共振(NMR)、电喷雾电离质谱(ESI-MS)和高效液相色谱(HPLC)对制备的金属-聚合物配合物进行了表征。红外光谱数据证实了M(CO)部分通过IDA螯合单元与聚合物主链配位(出现特征性的面式-M(CO)振动(2005、1890 cm),以及核磁共振氢谱中对应于与金属离子配位的亚甲基质子CHCOO(dd,4.2 ppm)不等价的信号组)。确定了用放射性Tc(CO)物种标记PVP-co-AA-IDA共聚物的最佳条件。放射化学产率达到97%。所获得的放射性标记聚合物在血清中3小时内稳定。在完整动物体内进行的分布实验表明,99m锝标记的MPC(MM = 15,000 Da)在血液中具有较高的初始蓄积,随后通过泌尿系统排出。