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Targeted delivery of intracellularly active diagnostics and therapeutics in vivo is a major challenge in cancer nanomedicine. A nanocarrier should possess long circulation time yet be small and stable enough to freely navigate through interstitial space to deliver its cargo to targeted cells. Herein, it is shown that by adding targeting ligands to… (More)
Photodynamic therapy is a treatment that combines the use of three non-toxic components, viz. photosensitiser, light and oxygen to cause localised oxidative photodamage. In the present study, the antifungal effect of the photosensitiser, BAM-SiPc, an unsymmetrical bisamino phthalocyanine, was investigated. BAM-SiPc was effective in photo-inactivating… (More)
A novel tetraamino silicon(iv) phthalocyanine has been prepared, of which the fluorescence emission and reactive oxygen species generation efficiency are greatly enhanced at lower pH in the range of ca. 5-7, making it a promising pH-controlled and tumour-selective fluorescence probe and photosensitiser for photodynamic therapy.
A series of silicon(IV) phthalocyanines substituted axially with different polyamine moieties have been prepared. Their fluorescence quantum yields (Φ(F) = 0.03-0.08) in N,N-dimethylformamide are low because of reductive quenching by the amino moieties. The values are significantly increased in aqueous media (Φ(F) = 0.12-0.21) as a result of protonation of… (More)
Two novel glucoconjugated silicon(IV) phthalocyanines (compounds 3 and 4) have been prepared and examined for their photophysical and biological properties. With two axial 1,2:5,6-di-O-isopropylidene-alpha-d-glucofuranose substituents linked to the silicon center through the tetraethylene glycol chain, both compounds are highly soluble and remain… (More)
An unsymmetrical bisferrocenyl silicon(IV) phthalocyanine has been prepared in which the disulfide and hydrazone linkers can be cleaved by dithiothreitol and acid, respectively. The separation of the ferrocenyl quenchers and the phthalocyanine core greatly enhances the fluorescence emission, singlet oxygen production, intracellular fluorescence intensity,… (More)
A zinc(II) phthalocyanine substituted with a triamino moiety and its tri-N-methylated analogue have been prepared and characterized with various spectroscopic methods. Both compounds remain non-aggregated in N,N-dimethylformamide and in water containing 0.05% Cremophor EL (v/v), and can generate singlet oxygen effectively. The photodynamic activities of… (More)
Fibroblast activation protein (FAP) is a cell-surface serine protease highly expressed on cancer-associated fibroblasts of human epithelial carcinomas but not on normal fibroblasts, normal tissues, and cancer cells. We report herein a novel FAP-triggered photodynamic molecular beacon (FAP-PPB) comprising a fluorescent photosensitizer and a black hole… (More)
We report a new class of photodynamic molecular beacon (PMB) with tumor specific mRNA-triggered control of singlet oxygen ((1)O(2)) production. The beacon contains a single-stranded oligonucleotide linker that forms a stem-loop structure (hairpin) in which the sequence is an antisense oligonucleotide (AS-ON) complementary to a target mRNA. The stem is… (More)
A series of unsymmetrical silicon(IV) phthalocyanines with a permethylated β-cyclodextrin unit and a sugar or a diamino moiety as the axial substituents have been prepared. These compounds are highly photocytotoxic with IC(50) values as low as 21 nM, which is ca. sevenfold lower than those of the symmetrical bis(cyclodextrin) analogue.