Multifunctional AS1411-functionalized fluorescent gold nanoparticles for targeted cancer cell imaging and efficient photodynamic therapy

•Multifunctional fluorescent gold nanoparticles (named NAANPs) were synthesized.•NAANPs were functionalized with AS1411 and bound with N-methylmesoporphyrin IX (NMM).•NAANPs targeted to the cancer cell via the specific AS1411-nucleolin interaction.•NMM can be fluorescence-enhanced by AS1411 G-quadruplex and used as a photosensitizer.•NAANPs were used for targeted cell imaging and efficient photodynamic therapy.

Herein, one multifunctional AS1411-functionalized fluorescent gold nanoparticles (named NAANPs) is synthesized and successfully applied for both targeted cancer cell imaging and efficient photodynamic therapy (PDT). The NAANPs are obtained by functionalizing the gold nanoparticles with AS1411 aptamer and then bound with one porphyrin derivative N-methylmesoporphyrin IX (NMM). Using HeLa cells over expressing nucleolin as representative cancer cells, the formed NAANPs can target to the cell surface via the specific AS1411-nucleolin interaction, which can discriminate the cancer cells from normal ones (e.g. HEK293) unambiguously. That the fluorescence intensity of NMM increased significantly upon binding to AS1411 G-quadruplex makes the NAANPs appropriate fluorescence reagent for cell imaging. Meanwhile, NMM can also be used as a photosensitizer, thus irradiation of the NAANPs by the white light from a common electric torch can lead to efficient production of cytotoxic reactive oxygen species for establishing a new type of PDT to cancer cells. Gold nanoparticles play the roles of both carrier and enhancer of the functional groups onto the cells. In addition, they not only possess inherently certain cytotoxicity to the cancer cells, but also boost the cellular uptake of the fluorescent groups. As a result, the efficiency of both the targeted cell imaging and PDT could be ensured.

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