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Amphiphilic trismethylpyridylporphyrin-C70 (PC70) dyad with improved photosensitization has been successfully prepared. The PC70 dyad forms a liposomal nanostructure through molecular self-assembling. An increased absorption coefficient in the visible region, good biocompatibility, and high photostability were observed on the self-assembling structure. Surprisingly, in comparison with previously reported photosensitizer porphyrins, PC70 exhibited an enhanced photodynamic therapy (PDT) effect under hypoxia conditions. Further investigations illustrated that PC70 went through an extremely long-life triplet state (211.3 μs) under hypoxia, which enabled the exiguous oxygen to approach and interact with the activated (3P-C70)* more efficiently and produce more singlet oxygen. This would overcome the problem of existing photosensitizers of low PDT efficiency in cancerous tissues under hypoxia. The excellent properties of PC70 dyad make it a promising phototherapeutic agent, especially for the treatment of early- and late-stage cancers under shallow and hypoxia tissues. [ABSTRACT FROM AUTHOR]

A radioactive metallofullerene 177LuxLu(3−x)N@C80 was firstly synthesized by means of neutron irradiation on Lu3N@C80. After modification by methoxypolyethylene glycol amine, in vivo investigation on tumor-bearing mice was performed. The results reveal favorable affinity toward tumors, suggesting that the obtained 177LuxLu(3−x)N@C80–PCBPEG could be promising for tumor diagnosis and therapy. [ABSTRACT FROM AUTHOR]

Abstract: C60-carboxyfullerene, C60[C(COOH)2]2, has been proven to function as peroxidase mimetics that can catalyze the reaction of peroxidase substrate 3,3',5,5'-tetramethylbenzidine (TMB) in the presence of H2O2 to produce a blue color reaction. Kinetic studies further indicate that C60[C(COOH)2]2 has an even higher affinity to TMB than that of the natural enzyme, horseradish peroxidase (HRP). C60[C(COOH)2]2/glucose oxidase (GO x )/TMB system provides a novel colorimetric sensor for glucose and shows good response toward glucose detection over a range of 1.0–40μM with a limit of detection 0.5μM (3σ/slope). Moreover, this sensitive and selective sensor can be successfully applied for the quantitative determination of glucose in human serum. The results indicate that it is a simple, cheap, convenient, highly selective, sensitive, and easy handling colorimetric assay. [Copyright &y& Elsevier]

It is important to maintain a reactive oxygen species (ROS) balance in organisms; thus, a valid ROS scavenger with good biocompatibility is urgently required. To prepare a high-efficiency ROS scavenger, multiple ethylenediamine (EDA) groups are bonded for the first time to a metallofullerene Gd@C 82 to obtain water-soluble Gd@C 82 -(EDA) 8 nanoparticles (NPs) through a facile solid-liquid reaction. Gd@C 82 -(EDA) 8 NPs with a relatively better conjugation possess an excellent capability to scavenge hydroxyl radicals. Moreover, Gd@C 82 -(EDA) 8 NPs exhibited a remarkable cytoprotective effect against H 2 O 2 -induced injuries to human epidermal keratinocytes-adult (HEK-a) cells at a low concentration of 2.5 μM. In contrast, Gd@C 82 -(OH) 26 NPs that modified with hydroxyls show an apparent protective effect at a much higher concentration of 40 μM. This outstanding cytoprotective performance of Gd@C 82 -(EDA) 8 NPs is mainly attributed to their extremely high cellular uptake and comparably strong conjugation. Gd@C 82 -(EDA) 8 NPs with good biocompatibility exhibit excellent ROS scavenging capability even at a significantly low concentration, which promotes its versatile applications in cosmetics and biomedicine.

A radioactive metallofullerene 177 Lu x Lu (3-x) N@C 80 was firstly synthesized by means of neutron irradiation on Lu 3 N@C 80 . After modification by methoxypolyethylene glycol amine, in vivo investigation on tumor-bearing mice was performed. The results reveal favorable affinity toward tumors, suggesting that the obtained 177 Lu x Lu (3-x) N@C 80 -PCBPEG could be promising for tumor diagnosis and therapy.

Amphiphilic trismethylpyridylporphyrin-C 70 (PC 70 ) dyad with improved photosensitization has been successfully prepared. The PC 70 dyad forms a liposomal nanostructure through molecular self-assembling. An increased absorption coefficient in the visible region, good biocompatibility, and high photostability were observed on the self-assembling structure. Surprisingly, in comparison with previously reported photosensitizer porphyrins, PC 70 exhibited an enhanced photodynamic therapy (PDT) effect under hypoxia conditions. Further investigations illustrated that PC 70 went through an extremely long-life triplet state (211.3 μs) under hypoxia, which enabled the exiguous oxygen to approach and interact with the activated ( 3 P-C 70 )* more efficiently and produce more singlet oxygen. This would overcome the problem of existing photosensitizers of low PDT efficiency in cancerous tissues under hypoxia. The excellent properties of PC 70 dyad make it a promising phototherapeutic agent, especially for the treatment of early- and late-stage cancers under shallow and hypoxia tissues.

Fullerene-based photosensitizers exhibit great potential in photodynamic therapy (PDT). Based on the high photodynamic efficacy of trimalonic acid-modified C70 fullerene (TF70), we constructed an aptamer-guided TF70 photosensitizer and investigated its photodynamic effect. Conjugation of the novel aptamer (named R13) could effectively enhance the PDT efficiency of TF70 against A549 lung cancer cells in the presence of serum. The lysosomal location of the TF70-R13 conjugate inside cells facilitates the production of intracellular reactive oxygen species (ROS), which can efficiently kill cells, under light irradiation. The enhanced photodynamic efficiency, along with its good biocompatibility in the dark, makes TF70-R13 a highly promising photosensitizer for tumor-specific PDT., (Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.)