School of Life Sciences, Faculty of Health Sciences, University of Hull, Cottingham Road, Hull, HU6 7RX, UK.
Positron Emission Tomography Research Center, University of Hull, Cottingham Road, Hull, HU6 7RX, UK.
Chemistry. 2020 Jun 18;26(34):7602-7608. doi: 10.1002/chem.201905776. Epub 2020 May 20.
In this study a bispidine ligand has been applied to the complexation of gallium(III) and radiolabelled with gallium-68 for the first time. Despite its 5-coordinate nature, the resulting complex is stable in serum for over two hours, demonstrating a ligand system well matched to the imaging window of gallium-68 positron emission tomography (PET). To show the versatility of the bispidine ligand and its potential use in PET, the bifunctional chelator was conjugated to a porphyrin, producing a PET/PDT-theranostic, which showed the same level of stability to serum as the non-conjugated gallium-68 complex. The PET/PDT complex killed >90 % of HT-29 cells upon light irradiation at 50 μm. This study shows bispidines have the versatility to be used as a ligand system for gallium-68 in PET.
在这项研究中，首次将双吡啶配体应用于镓（III）的络合，并进行了镓-68 放射性标记。尽管该配合物具有 5 配位性质，但在血清中仍能稳定存在两个多小时，表明该配体系统非常适合镓-68 正电子发射断层扫描（PET）的成像窗。为了展示双吡啶配体的多功能性及其在 PET 中的潜在用途，将双功能螯合剂与卟啉偶联，制得一种 PET/PDT 治疗剂，其对血清的稳定性与未偶联的镓-68 配合物相同。该 PET/PDT 复合物在 50μm 的光照射下能杀死 >90%的 HT-29 细胞。本研究表明双吡啶具有作为镓-68 的 PET 配体系统的多功能性。
