Copper-Catalyzed C(sp)-H Bond Hydrazidation.

A catalytic, direct synthetic strategy for preparing ynehydrazides with terminal alkynes and dialkyl azodicarboxylates is described. The protocol utilizes a cheap copper catalyst in combination with a catalytic amount of a weak base. The high sustainability, good practicality, broad substrate scope, and wide functional group tolerance comprised the advantages of this reaction. Synthetic applications and preliminary mechanistic studies have been conducted.

Cell surface expression of nucleolin mediates the antiangiogenic and antitumor activities of kallistatin.

Kallistatin is a unique serine proteinase inhibitor and heparin-binding protein. A previous study conducted by our group indicated that kallistatin has antiangiogenic and antitumoral activities. In the present study, we report that kallistatin specifically binds to membrane surface-expressed nucleolin with high affinity. Antibody-mediated neutralization or siRNA-induced nucleolin knockdown results in loss of kallistatin suppression of endothelial cell proliferation and migration in vitro and tumor angiogenesis and growth in vivo. In addition, we show that kallistatin is internalized and transported into cell nuclei of endothelial cells via nucleolin. Within the nucleus, kallistatin inhibits the phosphorylation of nucleolin, which is a critical step required for cell proliferation. Thus, we demonstrate that nucleolin is a novel functional receptor of kallistatin that mediates its antiangiogenic and antitumor activities. These findings provide mechanistic insights into the inhibitory effects of kallistatin on endothelial cell growth, tumor cell proliferation, and tumor-related angiogenesis.

A novel fluorometric detection of Cu(2+) based on self-assembled bilayers.

Fluorescent reagent sodium 1-naphthylamine diacetate (NADA) was assembled onto gold electrodes via its electrostatic interaction with cysteine (Cys) that was directly assembled on the gold electrode surface. Formation of the self-assembled bilayers was confirmed and primarily characterized by cyclic voltammetry and X-ray photoelectron spectra (XPS). The Cys modification of the gold electrode prevented direct adsorption of NADA onto the gold electrode and hence eliminated fluorescence quenching by gold. Strong fluorescence was observed from the NADA self-assembled bilayers at gold surface and was highly efficiently quenched by Cu(2+) that allowed for an extremely highly sensitive detection of Cu(2+) with a detection limit of 0.2ppt and quantitative detection range of 0.5-9ppt. The fluorescence from NADA/Cys/Au can be easily regenerated and therefore the present report showed a reusable method for immobilizing reagent in fabricating fluorescent chemosensors.