Enhanced Photodynamic Efficacy of Zinc Phthalocyanine by Conjugating to Heptalysine

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• 作者：Linsen Li ; Zhipu Luo ; Zhuo Chen ; Jincan Chen ; Shanyong Zhou ; Peng Xu ; Ping Hu ; Jundong Wang ; Naisheng Chen ; Jinling Huang ; Mingdong Huang
• 刊名：Bioconjugate Chemistry
• 出版年：2012
• 出版时间：November 21, 2012
• 年：2012
• 卷：23
• 期：11
• 页码：2168-2172
• 全文大小：310K
• 年卷期：v.23,no.11(November 21, 2012)
• ISSN：1520-4812

文摘

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.