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首页> 美国卫生研究院文献>Theranostics >Syntheses and Photodynamic Activity of Pegylated Cationic Zn(II)-Phthalocyanines in HEp2 Cells
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Syntheses and Photodynamic Activity of Pegylated Cationic Zn(II)-Phthalocyanines in HEp2 Cells

机译：聚乙二醇化阳离子Zn（II）-酞菁在HEp2细胞中的合成及光动力活性

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Di-cationic Zn(II)-phthalocyanines (ZnPcs) are promising photosensitizers for the photodynamic therapy (PDT) of cancers and for photoinactivation of viruses and bacteria. Pegylation of photosensitizers in general enhances their water-solubility and tumor cell accumulation. A series of pegylated di-cationic ZnPcs were synthesized from conjugation of a low molecular weight PEG group to a pre-formed Pc macrocycle, or by mixed condensation involving a pegylated phthalonitrile. All pegylated ZnPcs were highly soluble in polar organic solvents but were insoluble in water; they have intense Q absorptions centered at 680 nm and fluorescence quantum yields of ca. 0.2 in DMF. The non-pegylated di-cationic ZnPc >6a formed large aggregates, which were visualized by atomic force microscopy. The cytotoxicity, cellular uptake and subcellular distribution of all cationic ZnPcs were investigated in human carcinoma HEp2 cells. The most phototoxic compounds were found to be the α-substituted Pcs. Among these, Pcs >4a and >16a were the most effective (IC50 ca. 10 μM at 1.5 J/cm2), in part due to the presence of a PEG group and the two positive charges in close proximity (separated by an ethylene group) in these macrocycles. The β-substituted ZcPcs >6b and >4b accumulated the most within HEp2 cells but had low photocytoxicity (IC50 > 100 μM at 1.5 J/cm2), possibly as a result of their lower electron density of the ring and more extended conformations compared with the α-substituted Pcs. The results show that the charge distribution about the Pc macrocycle and the intracellular localization of the cationic ZnPcs mainly determine their photodynamic activity.
机译：双阳离子锌（II）-酞菁（ZnPcs）是有前途的光敏剂，可用于癌症的光动力疗法（PDT）以及病毒和细菌的光灭活。通常，光敏剂的聚乙二醇化增强了它们的水溶性和肿瘤细胞的积累。通过将低分子量PEG基团偶联到预先形成的Pc大环上，或通过涉及聚乙二醇化邻苯二甲腈的混合缩合，合成了一系列聚乙二醇化二阳离子ZnPcs。所有聚乙二醇化的ZnPcs都高度溶于极性有机溶剂，但不溶于水。它们在680 nm处具有强烈的Q吸收，荧光量子产率约为。 DMF中为0.2。非聚乙二醇二阳离子ZnPc > 6a 形成大的聚集体，并通过原子力显微镜观察。在人类癌细胞HEp2中研究了所有阳离子ZnPcs的细胞毒性，细胞摄取和亚细胞分布。发现最具光毒性的化合物是α-取代的Pcs。其中，Pcs > 4a 和> 16a 最有效（IC50在1.5 J / cm 2 时约为10μM），部分原因是这些大环中有一个PEG基团和两个紧邻的正电荷（由亚乙基隔开）。 β取代的ZcPcs > 6b 和> 4b 在HEp2细胞中积累最多，但光毒性低（1.5 J / cm 2 时IC50> 100μM） ），可能是由于其环的电子密度较低，并且与α-取代的Pcs相比具有更大的构象。结果表明，Pc大环的电荷分布和阳离子ZnPcs的胞内定位主要决定了它们的光动力活性。

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