calixarenes and Breast-Neoplasms

Photodynamic therapy (PDT) has emerged as a promising and spatiotemporally controllable cancer treatment modality. However, serious skin photosensitization during the PDT process limits the clinical application of PDT. Thus, the construction of "smart" and multifunctional photosensitizers has attracted substantial interest. Herein, we develop a mitochondria-targeting and pH-switched hybrid supramolecular photosensitizer by the host-guest interaction. The PDT efficacy of supramolecular photosensitizers can be quenched by the Förster resonance energy transfer (FRET) effect during long circulation and activated by the dissociation of supramolecular photosensitizers in an acidic tumor microenvironment, benefitting from the dynamic feature of the host-guest interaction and pH responsiveness of the water-soluble pillar[5]arene on gold nanoparticles. The rational integration of mitochondria-targeting and reductive glutathione (GSH) elimination in the hybrid switchable supramolecular photosensitizer prolongs the lifetime of reactive oxygen species generated in the PDT near mitochondria and further amplifies the PDT efficacy. Thus, the facile and versatile construction of switchable supramolecular photosensitizer offers not only the targeted and precise phototherapy but also high therapeutic efficacy, which would provide a new path for the clinic application of PDT.

Topics: Animals; Antineoplastic Agents; Breast Neoplasms; Calixarenes; Cell Line, Tumor; Cell Proliferation; Cell Survival; Drug Screening Assays, Antitumor; Fluorescence Resonance Energy Transfer; Hydrogen-Ion Concentration; Macromolecular Substances; Mice; Mitochondria; Particle Size; Photochemotherapy; Photosensitizing Agents; Surface Properties

Polyamines are essential for the growth of eukaryotic cells and can be dysregulated in tumors. Here we describe a strategy to deplete polyamines through host-guest encapsulation using a peptide-pillar[5]arene conjugate (P1P5A, P1 = RGDSK(N

Topics: Animals; Antineoplastic Agents; Apoptosis; Biosynthetic Pathways; Breast Neoplasms; Calixarenes; Cations; Female; Humans; Integrin alphaVbeta3; MCF-7 Cells; Mice; Mice, Nude; Peptides, Cyclic; Polyamines; Xenograft Model Antitumor Assays

Chemotherapy as an important tool for cancer treatment faces many obstacles such as multidrug resistance and adverse toxic effects on healthy tissues. Drug delivery systems has opened a new window to overcome these problems. There has been a strong interest development of new platform and system for delivof chemotherapeutic agents.. In the present study, a green synthesis method was chosen and performed for preparation of a novel amphoteric calix[4]arene (Calix) macrocycle with low toxicity to the human body.. The amphoteric Calix was coated on the surface of Fe. In vitro biological studies including hemolysis assay, erythrocytes sedimentation rate, red blood cells aggregation, cyto cellular internalization, and apoptosis evaluations were performed. Based on results, the developed nanocarrier has many advantages and capability for an efficient codelivery of DOX and MTX, which has a highly potent ability to kill cancer cells.. All these results persuade us, this nanocarrier could be effectively used for cancer therapy of MCF7 breast cancer cells and is suitable for use in further animal studies in future investigations.

Topics: Animals; Antineoplastic Agents; Apoptosis; Breast Neoplasms; Calixarenes; Calorimetry, Differential Scanning; Doxorubicin; Drug Carriers; Drug Delivery Systems; Drug Liberation; Drug Resistance, Multiple; Dynamic Light Scattering; Endocytosis; Female; Humans; Magnetite Nanoparticles; MCF-7 Cells; Methotrexate; Particle Size; Phenols; Spectroscopy, Fourier Transform Infrared

A series of novel azacalix[2]arene[2]pyrimidines were synthesized, and evaluated for their antiproliferative activities against A549, MCF7, SH-SY5Y and CNE human cancer cell lines in vitro by using the CCK-8 assay. A number of compounds showed low micromolar antiproliferative activities against MCF7 cell line. Compound 4j, containing a pyrrolidine moiety, exhibited the strongest inhibitory activity with an IC

Topics: Antineoplastic Agents; Apoptosis; Breast Neoplasms; Calixarenes; Caspase 3; Caspase 9; Cell Proliferation; Drug Design; Drug Screening Assays, Antitumor; Female; Humans; MCF-7 Cells; Pyrimidines