In human, estrogens play important roles in many physiological processes, and is also found to be
connected with numerous cancers. In these diseases, estrogen mediates its effects through the estrogen
receptor (ER), which serves as the basis for many current clinical diagnosis. Two forms of the estrogen
receptor have been identified, ERα and ERβ, and show different and specific functions. The two estrogen
receptors belong to a family of ligand-regulated transcription factors. Estrogen via ERα stimulates
proliferation in the breast, uterus, and developing prostate, while estrogen via ERβ inhibits proliferation and
promotes differentiation in the prostate, mammary gland, colon, lung, and bone marrow stem cells.
MicroRNAs (miRs) are small non-coding RNA molecules that occur naturally and downregulate protein
expression by translational blockade of the target mRNA or by promoting mRNA decay. MiR-21 is one of the
most studied miRNAs in cancers. MiR-21 is overexpressed in the most solid tumors, promoting progression
and metastasis. The miR-21 gene is located on the chromosome 17, in the 10th intron of a protein-coding gene,
TMEM49. While, the function of TMEM49 is currently unknown. Our experiment is designed to identity the
relationship between miR-21 and ERβ in cancer progression. The human cancer cells were transfected with
ERβ. Real-time PCR analysis showed that the expression level of miR-21 was significantly inhibited down by
ERβ treatment. As MTT assay showed the tumor cell survival rate was also inhibited significantly. Go/Gl
phase cell cycle arrest was founded and tumor cell apoptosis was induced in ERβ group.
KEYWORDS: Tumors, Near infrared, Luminescence, In vivo imaging, In vitro testing, Receptors, Confocal microscopy, Optical properties, Rhodamine B, Microscopy
Cell adhesion molecule integrin αvβ3 is an excellent target for tumor interventions because of its unique
expression on the surface of several types of solid tumor cells and on almost all sprouting tumor vasculatures. In this
manuscript, we describe the synthesis of near-infrared (NIR) fluorochrome ICG-Der-02-labeled dimeric cyclic RGD
peptides (ICG-Der-02-c(RGDyK)2) for in vivo tumor integrin targeting. The optical properties and structure of the probe
were intensively characterized. Afterwards, the integrin specificity of the fluorescent probe was tested in vitro for
receptor binding assay and fluorescence microscopy and in vivo for subcutaneous MDA-MB-231 and U87MG tumor
targeting. The results indicated that after labeling RGD peptide, the optical properties of ICG-Der-02 showed no obvious
change. Besides, in vitro and in vivo tumor targeting experiment indicated that the ICG-Der-02-c(RGDyK)2 probe with
high integrin affinity showed excellent tumor activity accumulation. Noninvasive NIR fluorescence imaging is able to
detect tumor integrin expression based upon the highly potent RGD peptide probe.
KEYWORDS: Nanoparticles, Luminescence, Upconversion, Near infrared, System on a chip, Cancer, Optical properties, FT-IR spectroscopy, Tissue optics, Ytterbium
Upconversion nanoparticles (UCNPs) as a new kind of biological luminescence materials have many advantages comparing with organic fluorescence probes and semi-conductive quantum dots, such as sharp fluorescence
emission, long emission lifetimes, high optical and chemical stability and low toxicity, especially low auto-fluorescence
background and deep tissue penetration under near-infrared (NIR) light excitation for bioimaging. Herein, we
demonstrate a facile approach to transfer UCNPs from hydrophobic to hydrophilic and the use of these UCNPs for cell imaging. Oleic acid-capped UCNPs based on NaYF4 were synthesized and modified with amphiphilic chitosan derivative through hydrophobic interaction. The as-prepared chitosan coated UCNPs with an average diameter of 35 nm were mono-dispersed in aqueous solution and possess good optical properties upon NIR light excitation. Cell viability
assays indicated the low cytotoxicity and good biocompatibility of chitosan-coated UCNPs. Cell imaging results
demonstrated that chitosan-coated UCNPs had great potential for bioimaing and biolabeling. Our work suggests a feasible method to modify OA-UCNPs with amphiphilic polymer and the promise of chitosan-based UCNPs for
bioimaging application.
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