可溶性多氟烷氧基取代金属酞菁 :新型肿瘤光动力治疗光敏剂(英文)

合成了 9个新的多氟烷氧基取代的金属酞菁衍生物 ,它们均可溶于多数有机溶剂 .光氧化能力和对DNA的光切断活性的研究表明 ,中心金属离子为锌和铝的酞菁衍生物 ,具有较好的产生单重态氧的能力 .在乳化剂F68的存在下 ,锌酞菁衍生物

Preparation, Characterization and Pharmacokinetics of Fluorescence Labeled Propylene Glycol Alginate Sodium Sulfate

A rapid and sensitive fluorescence labeling method was developed and validated for the microanalysis of a sulfated polysaccharide drug,namely propylene glycol alginate sodium sulfate(PSS), in rat plasma. Fluorescein isothiocyanate(FITC) was selected to label PSS, and 1, 6-diaminohexane was used to link PSS and FITC in order to prepare FITC-labeled PSS(F-PSS) through a reductive amination reaction. F-PSS was identified by UV-Vis, FT-IR and 1H-NMR spectrum. The cell stability and cytotoxicity of F-PSS were tested in Madin-Darby canine kidney(MDCK) cells. The results indicated that the labeling efficiency of F-PSS was 0.522% ± 0.0248% and the absolute bioavailability was 8.39%. F-PSS was stable in MDCK cells without obvious cytotoxicity. The method was sensitive and reliable; it showed a good linearity, precision, recovery and stability. The FITC labeling method can be applied to investigating the absorption and metabolism of PSS and other polysaccharides in biological samples.

Intracellular protease activation in apoptosis and cell- mediated cytotoxicity characterized by cell-permeable fluorogenic protease substrates

Over the past decade the importance of signaling from reporter molecules inside live cells and tissues has been clearly established. Biochemical events related to inflammation, tumor metastasis and proliferation, and viral infectivity and replication are examples of processes being further defined as more molecular tools for live cell measurements become available. Moreover, in addition to quantitating parameters related to physiologic processes, real-time imaging of molecular interactions that compose basic cellular activities are providing insights into understanding disease mechanisms as well as extending clini- cal efficacy of therapeutic regimens. In this review the use of highly cell-permeable fluorogenic substrates that report protease activities inside live cells is described; applications to defining the molecular events of two cellular processes, i.e., apoptosis and cell-mediated cytotoxicity, are then illustrated.

Polymeric nanocomposites loaded with fluoridated hydroxyapatite Ln^(3+)(Ln = Eu or Tb)/iron oxide for magnetic targeted cellular imaging

Objective： To fabricate polymeric nanocomposites with excellent photoluminescence, magnetic properties, and stability in aqueous solutions, in order to improve specificity and sensitivity of cellular imaging under a magnetic field. Methods： Fluoridated LnS＋-doped HAP （Ln3＋-HAP） NPs and iron oxides （lOs） can be encapsulated with biocompatible polymers via a modified solvent exaction/evaporation technique to prepare polymeric nanocomposites with fluoridated Ln3＋-HAP/iron oxide. The nanocomposites were characterized for surface morphology, fluorescence spectra, magnetic properties and in vitro cytotoxicity. Magnetic targeted cellular imaging of such nanocomposites was also evaluated with confocal laser scanning microscope using A549 cells with or without magnetic field. Results： The fabricated nanocomposites showed good stability and excellent luminescent properties, as well as low in vitro cytotoxicity, indicating that the nanocomposites are suitable for biological applications. Nanocomposites under magnetic field achieved much higher cellular uptake via an energy-dependent pathway than those without magnetic field. Conclusion： 1tie nanocomposites fabricated in this study will be a promising tool for magnetic targeted cellular imaging with improved specificity and enhanced selection.

Enhanced porphyrin-based fluorescence imaging-guided photodynamic/photothermal synergistic cancer therapy by mitochondrial targeting

Mitochondria are the power plants of the cell and play key roles in activating the apoptotic pathway in cancer cells,which are readily susceptible to cytotoxic reactive oxygen species and temperature elevations.Herein,we develop a"nanomissile"that targets mitochondria to enhance tumor treatment effects by facilitating mitochondrial dysfunction and releasing cytochrome C to activate the apoptotic pathway of cancer cells under 650-nm laser irradiation.Porphyringrafted polydopamine nanomaterial(PTPF-MitP)is designed as a nanomissile,with integrated O;-evolving photodynamic therapy and moderate photothermal therapy,which can selectively deliver to the mitochondria through a targeting unit,MitP.The cytotoxicity of PTPF-MitP to human lung tumor cells is twice as high as that of PTPF that does not have mitochondrial targeting units.In addition,it represents a realtime visualization and highly efficient treatment for tumor sites in vivo.This development represents a viable strategy for cancer therapy.

Cytotoxicity of mitochondrial-targeting silica-coated manganese oxide nanoparticles

The mitochondrion is a promising target for diagnosis and therapy. Mitochondrial-targeting silica-coated manganese oxide nanoparticles(Mn O@Si O2-PPh3+ NPs) were successfully synthesized to explore the mitochondrial cytotoxicity of nanoparticles. The mitochondrial targeting property was confirmed by a laser scanning confocal microscopy experiment. Even after incubation for only 4 h, the cytotoxicity of Mn O@Si O2-PPh3+ NPs against cancer cells was obvious; the ATP content was significantly decreased to 40%; and the mitochondrial membrane potential was depleted. All of these results indicated the collapse of mitochondrial function and the start of a cell apoptosis pathway. Our findings suggest that mitochondrial-mediated apoptosis could be strengthened by targeting to the subcellular compartment.