Highly fluorescent red copper nanoclusters (Cu NCs) were synthesized in aqueous medium in the presence of dihydrolipoic acid and poly(vinylpyrrolidone) (PVP). The Cu NCs, in solid form, were stable, retained their optical properties for a month, and could be redispersed for use when required. The NCs in aqueous medium exhibited pH-tunable reversible optical properties. The PVP stabilized NCs, when converted into hydrogel by cross-linking with poly(vinyl alcohol), delivered anticancer drug to cervical cancer (HeLa) cells, thereby inducing apoptotic cell death. The red emission properties of the Cu NCs in the hydrogel were used for optical imaging as well as for flow cytometric probe of cellular uptake. Cell viability assay, Caspase3 assay, and cell cycle analyses demonstrated that the Cu NCs present in the hydrogel composite exhibited synergy of action, along with the drug, cisplatin, against HeLa cells.
Transferrin (Tf)-templated luminescent blue copper nanoclusters (Tf-Cu NCs) are synthesized. They are further formulated into spherical Tf-Cu NC-doxorubicin nanoparticles (Tf-Cu NC-Dox NPs) based on electrostatic interaction with doxorubicin (Dox). The as-synthesized Tf-Cu NC-Dox NPs are explored for bioimaging and targeted drug delivery to delineate high therapeutic efficacy. Förster resonance energy transfer (FRET) within the Tf-Cu NC-Dox NPs exhibited striking red luminescence, wherein the blue luminescence of Tf-Cu NCs (donor) is quenched due to absorption by Dox (acceptor). Interestingly, blue luminescence of Tf-Cu NCs is restored in the cytoplasm of cancer cells upon internalization of the NPs through overexpressed transferrin receptor (TfR) present on the cell surface. Finally, gradual release of Dox from the NPs leads to the generation of its red luminescence inside the nucleus. The biocompatible Tf-Cu NC-Dox NPs displayed superior targeting efficiency on TfR overexpressed cells (HeLa and MCF-7) as compared to the cells expressing less TfR (HEK-293 and 3T3-L1). Combination index (CI) revealed synergistic activity of Tf-Cu NCs and Dox in Tf-Cu NC-Dox NPs. In vivo assessment of the NPs on TfR positive Daltons lymphoma ascites (DLA) bearing mice revealed significant inhibition of tumor growth rendering prolonged survival of the mice.
Herein, different surface charged carbon dots (Cdots) were synthesized by using diethylene glycol as a carbon source with various amine containing surface passivating agents. The synthesis method is very simple and fast microwave oven-based, that results in almost similar sized positive, negative and uncharged fluorescent Cdots which has been confirmed by zeta potential analysis in our case. The formation of Cdots was confirmed by characterization using fluorescence spectroscopy, transmission electron microscopy, XRD, FT-IR, and XPS spectroscopy. To find out relative bactericidal activity of these Cdots, green fluorescence protein expressing recombinant E. coli bacteria were taken as a model system. Time-dependent bacterial growth and FACS study demonstrated that both uncharged Cdots and positively charged Cdots were showing better bactericidal activity as compared to negative charged Cdots. The Cdots caused elevation of reactive oxygen species level, which is possibly leading to bacterial cell death.
Disclosed here are a piperazine, a pyridine, and two carboxylate groups containing pentadentate ligand Hpmpa and its corresponding water-soluble Mn(II) complex (1). DFT-based structural optimization implied that the complex had pentagonal bipyramidal geometry where the axial positions were occupied by two water molecules, and the equatorial plane was constituted by the ligand ONO donor set. Thus, a bis(aquated) disc-like Mn(II) complex has been synthesized. The complex showed higher stability compared with Mn(II)-EDTA complex [log K = 14.29(3)] and showed a very high r relaxivity value of 5.88 mM s at 1.41 T, 25 °C, and pH = 7.4. The relaxivity value remained almost unaffected by the pH of the medium in the range of 6-10. Although the presence of 200 equiv of fluoride and bicarbonate anions did not affect the relaxivity value appreciably, an increase in the value was noticed in the presence of phosphate anion due to slow tumbling of the complex. Cell viability measurements, as well as phantom MR images using clinical MRI imager, consolidated the possible candidature of complex 1 as a positive contrast agent.
pH-responsive luminescent copper nanoclusters (Cu NCs) with aggregation-induced emission (AIE) characteristics have been synthesized. Upon internalization into living cells, the NCs displayed a cellular pH environment-dependent luminescence change with orange-red emission at pH 4.5, whereas bright green emission was observed over time at pH 7.4, through their AIE attributes. Furthermore, the intracellular AIE kinetics of the NC probe was measured in MCF-7 cells and compared to that of HEK-293 cells. Intriguingly, the intracellular rate constant value derived for AIE kinetics in MCF-7 cells was found to be 3-fold higher than that in HEK-293 cell lines, whereas the value was 2-fold higher than that observed in aqueous medium. This provided a new platform to study different cell lines based on intracellular AIE in living cells, with additional potential for future applications in cellular imaging, diagnostics, and disease detection.
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