Enhanced Photodynamic Efficacy of Zinc Phthalocyanine by Conjugating to Heptalysine
Enhanced Photodynamic Efficacy of Zinc Phthalocyanine by Conjugating to Heptalysine
复制标题
通过与七赖氨酸缀合增强锌酞菁的光动力功效
DOI：
10.1021/bc3002997
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发表时间：
2012-11-01
影响因子：
4.7
通讯作者：
Huang, Mingdong
中科院分区：
文献类型：
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作者：
Li, Linsen;Luo, Zhipu;Huang, Mingdong
酞菁锌（ZnPc）是一种很有前途的光动力疗法光敏剂，但面临一些挑战：ZnPc不溶于水，因此需要通过以下方式配制ZnPc：脂质体或Cremophor EL，或对Pc环进行化学修饰以增强其生物利用度和光动力功效。在此，我们将单取代的ZnPc-COOH与一系列具有不同数目的赖氨酸残基的寡聚赖氨酸部分（ZnPc-（Lys）（n）（n = 1，3，5，7，9））缀合以改善ZnPc缀合物的水溶性。我们在正常和癌细胞系上测量了这一系列缀合物的光敏功效和细胞摄取。此外，我们还建立了一种灵敏的原位方法来区分缀合物之间的光动力学效应差异。我们的结果表明，与所研究的其他缀合物相比，ZnPc-（Lys）（7）具有最高的光动力学效应。
Zinc phthalocyanine (ZnPc) is a promising photosensitizer for photodynamic therapy, but faces some challenges: ZnPc is insoluble in water and thus requires either special formulation of ZnPc by, e.g., liposome or Cremophor EL, or chemical modification of Pc ring to enhance its bioavailability and photodynamic efficacy. Here, we conjugated monosubstituted ZnPc-COOH with a series of oligolysine moieties with different numbers of lysine residues (ZnPc-(Lys)(n) (n = 1, 3, 5, 7, 9) to improve the water solubility of the ZnPc conjugates. We measured the photosensitizing efficacies and the cellular uptakes of this series of conjugates on a normal and a cancerous cell line. In addition, we developed a sensitive in situ method to distinguish the difference in photodynamic efficacy among conjugates Our results showed that ZnPc-(Lys)(7) has the highest photodynamic efficacy compared to the other conjugates investigated.