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Krüppel‐like factor 2 (KLF2) critically regulates activation and function of monocyte, which plays important pathogenic role in progressive joint destruction in rheumatoid arthritis (RA). It is yet to be established the molecular basis of KLF2‐mediated regulation of monocytes in RA pathogenesis. Herein, we show that a class of compound, HDAC inhibitors (HDACi) induced KLF2 expression in monocytes both in vitro and in vivo. KLF2 level was also elevated in tissues, such as bone marrow, spleen and thymus in mice after infusion of HDACi. Importantly, HDACi significantly reduced osteoclastic differentiation of monocytes with the up‐regulation of KLF2 and concomitant down‐regulation of matrixmetalloproteinases both in the expression level as well as in the protein level. In addition, HDACi reduced K/BxN serum‐induced arthritic inflammation and joint destruction in mice in a dose‐dependent manner. Finally, co‐immunoprecipitation and overexpression studies confirmed that KLF2 directly interacts with HDAC4 molecule in cells. These findings provide mechanistic evidence of KLF2‐mediated regulation of K/BxN serum‐induced arthritic inflammation. [ABSTRACT FROM AUTHOR]

Curcumin has shown therapeutic activity against triple-negative breast cancer (TNBC) cells, but it shows low efficacy and low bioavailability when administered as a free drug. We have developed a general synthesis strategy to encapsulate the natural molecule curcumin in monodispersed isoreticular nanoscale metal organic framework (NMOF-3) nanoparticles for targeted drug delivery in triple-negative breast cancer cells (TNBC). The cytotoxicity of IRMOF-3, curcumin-loaded IRMOF-3 (IRMOF-3@CCM) and folic acid-conjugated curcumin-loaded IRMOF-3 (IRMOF-3@CCM@FA) in human and mice TNBC were tested. IRMOF3@CCM@FA induces apoptosis by upregulating of Bax and downregulating of Bcl-2, and it further upregulates JNK and p53 in human TNBC cells. Simultaneously, we studied their effects in mice bearing TNBC induced by 4T1 cells. In in vivo studies, mice receiving targeted delivery of curcumin had increased survivability and reduced tumor volume compared with those observed for mice receiving non-targeted delivery. Our results highlight that folate-conjugated curcumin-loaded IRMOF-3 may be a useful therapeutic agent to treat TNBC. [ABSTRACT FROM AUTHOR]

Abstract: A facile and novel strategy to synthesize nitrogen‐ and phosphorous‐doped carbon dots (NPCDs) by single step pyrolysis method is described here. Citric acid is used as carbon source and di‐ammonium hydrogen phosphate is used as both nitrogen and phosphorous sources, respectively. Through the extensive study on optical properties, morphology and chemical structures of the synthesized NPCDs, it is found that as‐synthesized NPCDs exhibited good excitation‐dependent luminescence property, spherical morphology and high stability. The obtained NPCDs are stable in aqueous medium and possess a quantum yield of 10.58%. In this work, a new assay method is developed to detect iodide ions using the synthesized NPCDs. Here, the inner filter effect is applied to detect the iodide ion and exhibited a wide linear response concentration range (10–60 μM) with a limit of detection (LOD) of 0.32 μM. Furthermore, the synthesized NPCDs are used for the selective detection of iron(III) (Fe3+) ions and cell imaging. Fe3+ ions sensing assay shows a detection range from 0.2 to 30 μM with a LOD of 72 nM. As an efficient photoluminescence sensor, the developed NPCDs have an excellent biocompatibility and low cytotoxicity, allowing Fe3+ ion detection in HeLa cells. [ABSTRACT FROM AUTHOR]

Highly fluorescent nitrogen and phosphorus-doped carbon dots with a quantum yield 59% have been successfully synthesized from citric acid and di-ammonium hydrogen phosphate by single step hydrothermal method. The synthesized carbon dots have high solubility as well as stability in aqueous medium. The as-obtained carbon dots are well monodispersed with particle sizes 1.5–4 nm. Owing to a good tunable fluorescence property and biocompatibility, the carbon dots were applied for intercellular sensing of Fe3+ ions as well as cancer cell imaging. [ABSTRACT FROM AUTHOR]

Abstract: Background: Metal oxide nanoparticles are well known to generate oxidative stress and deregulate normal cellular activities. Among these, transition metals copper oxide nanoparticles (CuO NPs) are more compelling than others and able to modulate different cellular responses. Methods: In this work, we have synthesized and characterized CuO NPs by various biophysical methods. These CuO NPs (~30nm) induce autophagy in human breast cancer cell line, MCF7 in a time- and dose-dependent manner. Cellular autophagy was tested by MDC staining, induction of green fluorescent protein-light chain 3 (GFP-LC3B) foci by confocal microscopy, transfection of pBABE-puro mCherry-EGFP-LC3B plasmid and Western blotting of autophagy marker proteins LC3B, beclin1 and ATG5. Further, inhibition of autophagy by 3-MA decreased LD50 doses of CuO NPs. Such cell death was associated with the induction of apoptosis as revealed by FACS analysis, cleavage of PARP, de-phosphorylation of Bad and increased cleavage product of caspase 3. siRNA mediated inhibition of autophagy related gene beclin1 also demonstrated similar results. Finally induction of apoptosis by 3-MA in CuO NP treated cells was observed by TEM. Results: This study indicates that CuO NPs are a potent inducer of autophagy which may be a cellular defense against the CuO NP mediated toxicity and inhibition of autophagy switches the cellular response into apoptosis. Conclusions: A combination of CuO NPs with the autophagy inhibitor is essential to induce apoptosis in breast cancer cells. General significance: CuO NP induced autophagy is a survival strategy of MCF7 cells and inhibition of autophagy renders cellular fate to apoptosis. [Copyright &y& Elsevier]

Several copper compounds have proven anti-cancer activity. Similarly, curcumin a derivative of 1,3 diketone, which is not plenty in nature, has comparable anti-cancer activity. In this work, we have explored the synergistic anti-cancer activity of copper ion and acetylacetone complex containing 1,3 diketone group. The cytotoxicity of the copper acetylacetonate (CuAA) complex was evaluated on various cancer cells and LD50 doses were determined. To investigate the mechanism, various biochemical assays were performed and reactive oxygen species as well as the glutathione level in the cell were found to be increased after the treatment with the above-mentioned complex. Further this reagent induced apoptosis and reduced mitochondrial membrane potential of the cells. Because of the poor solubility and reasonable cytotoxicity of CuAA, polymer nanoparticles (NPs) of chitosan derivatives were used for delivery in cancer cells. For the targeted delivery, folic acid-tagged hydrophobic-modified chitosan NPs were developed and the CuAA was encapsulated. Finally, these drug-encapsulated NPs were successfully delivered to folate receptor over-expressed cancer cells. Thus using nanotechnology, we developed an anti-cancer agent suitable for targeted delivery. [ABSTRACT FROM AUTHOR]

A facile and novel strategy to synthesize nitrogen- and phosphorous-doped carbon dots (NPCDs) by single step pyrolysis method is described here. Citric acid is used as carbon source and di-ammonium hydrogen phosphate is used as both nitrogen and phosphorous sources, respectively. Through the extensive study on optical properties, morphology and chemical structures of the synthesized NPCDs, it is found that as-synthesized NPCDs exhibited good excitation-dependent luminescence property, spherical morphology and high stability. The obtained NPCDs are stable in aqueous medium and possess a quantum yield of 10.58%. In this work, a new assay method is developed to detect iodide ions using the synthesized NPCDs. Here, the inner filter effect is applied to detect the iodide ion and exhibited a wide linear response concentration range (10-60 μM) with a limit of detection (LOD) of 0.32 μM. Furthermore, the synthesized NPCDs are used for the selective detection of iron(III) (Fe 3+ ) ions and cell imaging. Fe 3+ ions sensing assay shows a detection range from 0.2 to 30 μM with a LOD of 72 nM. As an efficient photoluminescence sensor, the developed NPCDs have an excellent biocompatibility and low cytotoxicity, allowing Fe 3+ ion detection in HeLa cells., (Copyright © 2017 John Wiley & Sons, Ltd.)

In this work, carbon dots conjugated carboxymethyl cellulose-hydroxyapatite nanocomposite has been synthesized by one-pot synthesis method and used for multiple applications like metal ion sensing, osteogenic activity, bio-imaging and drug carrier. The structure and morphology of the nanocomposite were systematically characterized by FTIR, XRD, TGA, FESEM, TEM and DLS. Results clearly demonstrated the formation of fluorescent enabled carbon dots conjugated nanocomposite from carboxymethyl cellulose-hydroxyapatite nanocomposite by a simple thermal treatment. The synthesized nanocomposite is smaller than 100 nm and exhibits fluorescence emission band around 440 nm upon excitation with 340 nm wavelength. In the meantime, the nanocomposite was loaded with a chemotherapeutic drug, doxorubicin to evaluate the drug loading potential of synthesized nanocomposite. Moreover, the as-synthesized nanocomposite showed good osteogenic properties for bone tissue engineering and also exhibited excellent selectivity and sensitivity towards Fe 3+ ions., (Copyright © 2017 Elsevier Ltd. All rights reserved.)

Highly fluorescent nitrogen and phosphorus-doped carbon dots with a quantum yield 59% have been successfully synthesized from citric acid and di-ammonium hydrogen phosphate by single step hydrothermal method. The synthesized carbon dots have high solubility as well as stability in aqueous medium. The as-obtained carbon dots are well monodispersed with particle sizes 1.5-4 nm. Owing to a good tunable fluorescence property and biocompatibility, the carbon dots were applied for intercellular sensing of Fe(3+) ions as well as cancer cell imaging., (Copyright © 2015 John Wiley & Sons, Ltd.)