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
Highly Conjugated Tetraphenylporphyrin-Ru(Ⅱ) Bipyridine Complex: Synthesis, Optical Properties, and Photodynamic Anticancer Activity
作者单位E-mail
张劲祥 韩山师范学院化学与环境工程学院, 潮州 521041 zhangjx@hstc.edu.cn 
黄伟国 香港浸会大学理学院化学系, 香港 999077  
黄嘉良 香港浸会大学理学院化学系, 香港 999077  
麦乃歧 香港浸会大学理学院生物系, 香港 999077  
摘要: 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PorRuPorZn-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)%。
关键词: 卟啉  钌配合物  两亲性  双光子  光动力治疗
基金项目: 广东省教育厅特色创新类项目(No.2018KTSCX137)、 广东省教育厅创新团队项目(No.2017KCXTD023)、 韩山师范学院博士启动项目(No.QD20180322)和广东省基础与应用基础研究基金项目(No.2021A1515012358)资助。
Abstract: 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 subcellular target was observed by the costaining 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.
Keywords: porphyrin  ruthenium complex  amphiphilicity  two-photon  photodynamic therapy
投稿时间:2022-05-10 修订日期:2022-09-04
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张劲祥,黄伟国,黄嘉良,麦乃歧.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[J].无机化学学报,2022,38(12):2383-2391.
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Support information: 相关附件:   220226_Supporting_information.doc