在温和条件下进行 Ga 的选择性放射性标记：一种用于卟啉 PET/PDT 治疗诊断试剂的途径。
Selective radiolabelling with Ga under mild conditions: a route towards a porphyrin PET/PDT theranostic agent.
机构信息
Chemistry, School of Mathematics and Physical Sciences, Faculty of Science and Engineering, University of Hull, HU6 7RX, UK.
出版信息
Chem Commun (Camb). 2018 Jul 12;54(57):7952-7954. doi: 10.1039/c8cc03897j.
A theranostic conjugate for use as a positron emission tomography (PET) radiotracer and as a photosensitiser for photodynamic therapy (PDT) has been synthesised. A water-soluble porphyrin was coupled with the bifunctional chelate, H4Dpaa.ga. This conjugate is capable of rapid 68Ga complexation under physiological conditions; with 93% and 80% radiochemical yields achieved, at pH 4.5 and pH 7.4 respectively, in 15 min at 25 °C. Photocytotoxicity was evaluated on HT-29 cells and showed the conjugate was capable of >50% cell death at 50 μM upon irradiation with light, while causing minimal toxicity in the absence of light (>95% cell survival).
已合成一种用于正电子发射断层扫描（PET）放射性示踪剂和光动力疗法（PDT）光敏剂的治疗性缀合物。将水溶性卟啉与双功能螯合剂 H4Dpaa.ga 偶联。该缀合物能够在生理条件下快速与 68Ga 络合；在 25°C 下，pH 值分别为 4.5 和 7.4 时，15 分钟内分别获得 93%和 80%的放射化学产率。在 HT-29 细胞上评估了光细胞毒性，结果表明，在光照下，当浓度为 50μM 时，该缀合物能够引起>50%的细胞死亡，而在没有光照的情况下，其毒性最小（>95%的细胞存活）。
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