Department of Chemistry, Rhodes University, Grahamstown 6140, South Africa.
Biotechnology Innovation Centre, Rhodes University, Grahamstown 6140, South Africa.
Spectrochim Acta A Mol Biomol Spectrosc. 2017 Feb 15;173:292-300. doi: 10.1016/j.saa.2016.09.032. Epub 2016 Sep 20.
Zinc monocarboxyphenoxy phthalocyanine (ZnMCPPc) was linked to human serum albumin (HSA) and chitosan via amide bond formation. The photophysical behavior and photodynamic therapy (PDT) activity (against human breast adenocarcinoma cell line (MCF-7 cells) of ZnMCPPc alone and its conjugates were investigated. The conjugates showed improved fluorescence, triplet and singlet oxygen quantum yields when compared to ZnMCPPc alone. The in vitro dark cytotoxicity and PDT studies were carried out at a dose of 3.6μg/mL to 57.1μg/mL. The in vitro dark cytotoxicity studies of ZnMCPPc showed cell viability <50% at 28.6μg/mL and 57.1μg/mL, while the conjugates showed > 50% in all their tested concentrations (3.6 to 57.1) μg/mL. Thus, conjugation of ZnMCPPc to HSA and chitosan improves its dark cytotoxicity, an important criteria for molecules meant for photodynamic therapy. Complex 1 showed the most efficacious PDT activity with cell viability <50% at concentration range of (14.3 to 57.1) μg/mL in comparison to the conjugates which only showed <50% cell viability at 28.6μg/mL and 57.1μg/mL for 1-HSA and 57.1μg/mL for 1-Chitosan.
锌卟啉单羧基酞菁（ZnMCPPc）通过酰胺键与人血清白蛋白（HSA）和壳聚糖相连。研究了 ZnMCPPc 及其缀合物的光物理行为和光动力治疗（PDT）活性（针对人乳腺癌腺癌细胞系（MCF-7 细胞））。与单独的 ZnMCPPc 相比，缀合物显示出改善的荧光、三重态和单线态氧量子产率。在 3.6μg/mL 至 57.1μg/mL 的剂量下进行了体外暗毒性和 PDT 研究。ZnMCPPc 的体外暗毒性研究表明，在 28.6μg/mL 和 57.1μg/mL 时细胞活力<50%，而缀合物在所有测试浓度（3.6 至 57.1）μg/mL 时均显示>50%。因此，将 ZnMCPPc 与 HSA 和壳聚糖缀合可提高其暗毒性，这是用于光动力疗法的分子的重要标准。与缀合物相比，复合物 1 在浓度范围为（14.3 至 57.1）μg/mL 时表现出最有效的 PDT 活性，细胞活力<50%，而缀合物仅在 28.6μg/mL 和 57.1μg/mL 时显示<50%细胞活力对于 1-HSA 和 57.1μg/mL 对于 1-壳聚糖。
