Construction of a Nano Biosensor for Cyanide Anion Detection and Its Application in Environmental and Biological Systems

We have developed a Ag@Au core–shell nanoparticle (NP)/iridium­(III) complex-based sensing platform for the sensitive luminescence “turn-on” sensing of cyanide ions, an acutely toxic pollutant. The assay is based on the quenching effect of Ag@Au NPs on the emission of complex <b>1</b>, but luminescence is restored after the addition of cyanide anions due to their ability to dissolve the Au shell. Our sensing platform exhibited a high sensitivity toward cyanide anions with a detection limit of 0.036 μM, and also showed high selectivity for cyanide over 10-fold excess amounts of other anions. The sensing platform was also successfully applied to monitor cyanide anions in drinking water and in living cells

Development of a Long-Lived Luminescence Probe for Visualizing β‑Galactosidase in Ovarian Carcinoma Cells

β-Galactosidase (β-gal) is an important biomarker for ovarian cancers. In this work, we designed and synthesized a novel iridium­(III)-based probe <b>1</b> for discriminating ovarian carcinoma cell lines from normal cell lines. The probe could detect β-gal even in the presence of a highly autofluorescent background. The probe also showed a good linear response to β-gal between 0 and 30 U/mL, with a detection limit of 0.51 U/mL. Importantly, complex <b>1</b> could selectively “light up” ovarian carcinoma cells, while exhibiting negligible luminescence in normal cells. Overall, complex <b>1</b> could be potentially used as a useful probe for detecting β-gal expression in the context of ovarian cancer diagnostics

A Rhodium(III)-Based Inhibitor of Lysine-Specific Histone Demethylase 1 as an Epigenetic Modulator in Prostate Cancer Cells

We report herein a novel rhodium­(III) complex <b>1</b> as a new LSD1 targeting agent and epigenetic modulator. Complex <b>1</b> disrupted the interaction of LSD1-H3K4me2 in human prostate carcinoma cells and enhanced the amplification of p21, FOXA2, and BMP2 gene promoters. Complex <b>1</b> was selective for LSD1 over other histone demethylases, such as KDM2b, KDM7, and MAO activities, and also showed antiproliferative activity toward human cancer cells. To date, complex <b>1</b> is the first metal-based inhibitor of LSD1 activity

A Rhodium(III)-Based Inhibitor of Lysine-Specific Histone Demethylase 1 as an Epigenetic Modulator in Prostate Cancer Cells

We report herein a novel rhodium­(III) complex <b>1</b> as a new LSD1 targeting agent and epigenetic modulator. Complex <b>1</b> disrupted the interaction of LSD1-H3K4me2 in human prostate carcinoma cells and enhanced the amplification of p21, FOXA2, and BMP2 gene promoters. Complex <b>1</b> was selective for LSD1 over other histone demethylases, such as KDM2b, KDM7, and MAO activities, and also showed antiproliferative activity toward human cancer cells. To date, complex <b>1</b> is the first metal-based inhibitor of LSD1 activity

Effects of compounds on cell viability as determined by an MTT assay.

<p>A375 cells were treated with 0.01 to 4 μM of compounds or amentoflavone for 48 h. LO2 cells were treated with the same concentration of compound <b>1</b> for 48 h. PC3, DU145, HepG2 and A2058 cells were treated with 0.01 to 10 μM of compound <b>1</b> for 48 h. Error bars represent the standard deviations of results obtained from three independent experiments.</p

Compound 1 induces apoptosis in A375 cells.

<p>A375 cells were treated with the indicated concentrations of compound <b>1</b> (0.03 to 3 μM) or positive control compound NVP-BBT594 (1 μM) for 24 h. <b>(A)</b> A375 cells were stained with PI and Annexin V, and were analyzed by flow cytometry. <b>(B)</b> Protein lysates were analyzed by Western blotting with the indicated antibodies.</p

Compound 1 reduces phosphorylation of JAK2, STAT3 in A375 cells.

<p>A375 cells were treated with the indicated concentrations of compound <b>1</b> (0.03 to 3 μM) or positive control compound NVP-BBT594 (1 μM) for 24 h. Protein lysates were analyzed by Western blotting with the indicated antibodies. Error bars represent the standard deviation of triplicate results.</p

Effect of compound 1 on Bcl-2 level in A375 cells.

<p><b>(A)</b> A375 cells were treated with the indicated concentrations of compound <b>1</b> (0.1 to 3 μM) or positive control compound NVP-BBT594 (1 μM) for 24 h. Protein lysates were analyzed by Western blotting with the indicated antibodies. <b>(B)</b> The data were analyzed using Image Lab. Error bars represent the standard deviation of triplicate results.</p

Effect of 1 on HIF1α and ubiquitin in A375 cells.

<p>A375 cells were treated with the indicated concentrations of compound <b>1</b> (0.03 to 3 μM) or positive control compound NVP-BBT594 (1 μM) for 24 h. Protein lysates were analysed by Western blotting with the indicated antibodies.</p

Compound 1 stabilizes JAK2 in A375 cells.

<p><b>(A)</b> Stabilization of JAK2 by <b>1</b>. <b>(B)</b> The band intensity of JAK2 with different temperatures. The data were normalized to the JAK2 level of control group at 55°C and are expressed as the means ± SD of three individual experiments. The data were analyzed using Image Lab. Error bars represent the standard deviation of triplicate results. Significant differences versus control at the same temperature are indicated by **<i>p</i> < 0.01.</p