Phthalocyanine鈭扨olyamine Conjugates as Highly Efficient Photosensitizers for Photodynamic Therapy

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• 作者：Xiong-Jie Jiang ; Sin-Lui Yeung ; Pui-Chi Lo ; Wing-Ping Fong ; Dennis K. P. Ng
• 刊名：Journal of Medicinal Chemistry
• 出版年：2011
• 出版时间：January 13, 2011
• 年：2011
• 卷：54
• 期：1
• 页码：320-330
• 全文大小：1068K
• 年卷期：v.54,no.1(January 13, 2011)
• ISSN：1520-4804

文摘

A series of silicon(IV) phthalocyanines substituted axially with different polyamine moieties have been prepared. Their fluorescence quantum yields (桅_F = 0.03鈭?.08) in N,N-dimethylformamide are low because of reductive quenching by the amino moieties. The values are significantly increased in aqueous media (桅_F = 0.12鈭?.21) as a result of protonation of the amino substituents. All the compounds are highly photocytotoxic against human colon adenocarcinoma HT29 cells and Chinese hamster ovary cells with IC₅₀ values as low as 1.1 nM. Flow cytometric studies of two selected compounds (2 and 5) against HT29 cells have shown that they induce apoptosis extensively. As shown by confocal microscopy, these two compounds also show high affinity toward the lysosomes, but not the mitochondria, of the cells. Their in vivo photodynamic activity has also been investigated using HT29 tumor bearing nude mice. Both of them can effectively inhibit the growth of the tumor without causing apparent injury to the liver of the mice.