高共轭性的四苯基卟啉⁃Ru(II)联吡啶配合物的合成、光学性质及光动力抗癌活性

利用β位吡嗪环共轭连接的卟啉-菲咯啉配体L制备了两亲性的卟啉基-钌(Ⅱ)配合物PorRu和PorZn-Ru，对其进行了核磁及质谱的表征、线性与非线性光谱分析及光动力抗癌活性研究。实验结果显示所得的2个钌配合物具有高的¹O₂量子产率(0.93、0.82)和较高的双光子吸收截面(619、621 GM)，鼻咽癌HK-1细胞株的摄取量可达每10⁶个细胞约22 nmol。体外光动力抗癌活性测试显示在2 J·cm^-2的光学剂量及4 μmol·L^-1的给药浓度下，抑制效率分别达到(87.44±2.21)%、(45.03±2.85)%。

Two amphiphilic porphyrin - ruthenium (II) complexes PorRu and PorZn ⁃ Ru were synthesized by the coordination of metal Ru(II) and porphyrin-phenanthroline ligand L which is modified with conjugated pyrazine ring at the β position of porphyrin. Two compounds were characterized and evaluated by NMR and mass spectrometry, linear and nonlinear spectral analysis, and photodynamic anti-cancer activity study. Experimental results show that the two compounds had very high ¹O₂ quantum yields (0.93, 0.82), high two-photon absorption cross-sections (619, 621 GM), and up to about 22 nmol per 10⁶ cell uptakes of nasopharyngeal carcinoma HK-1 cell line. Although no obvious sub - cellular target was observed by the co - staining cell images, the high ¹O₂ yields and good cellular uptakes still made the ruthenium compounds have good photodynamic anticancer activity against HK-1 cells. At the light dose of 2 J·cm^-2 and the administration concentration of 4 µmol·L^-1, the inhibition efficiency reached (87.44± 2.21)% and (45.03±2.85)% respectively.